cas 4111-54-0, Lithium diisopropylamide | Articles data

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229. Bestimmung des Aggregationsgrads lithiumorganischer Verbindungen durch Kryoskopie in Tetrahydrofuran
The association behaviour of alkyl-, aryl- and alkinyl-lithium compounds as well as of lithium enolates and chiral lithium azaenolates is determined from-freezing point depression values in dilute tetrahydrofuran solutions at -108 grad C.Compared to X-ray-crystallographic data (lithiated methyldithiane, phenyllithium, lithio derivatives of a ketone, carboxylic amide and -ester, and a diketopiperazine-bislactim-ether), desaggregation is found under these conditions.The structutres determined by 13C-NMR spectroscopy for BuLi, lithiophenylacetylene and (t-butyl)lithioacetylene are confirmed.The dilithio salt of a carboxylic acid is polymeric, a chiral lithio-hydrazone and a chiral lithio-oxazolidine are monomeric and dimeric, respectively.Lithium diisopropylamide is a monomer-dimer equilibrium mixture.The apparatus described permits both synthesis and measurement of the reactive species under inert atmosphere conditions in the same vessel.
Bauer, Walter,Seebach, Dieter
p. 1972 - 1988
(1984)
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Synthesis of novel carborane-containing terminal alkynes
Lithiation of 1-bromomethyl-o-carborane with lithium diisopropylamide (LDA) in THF results in the in situ formation of 1-lithio-2-bromomethyl-o-carborane, the reaction of which with 3-trimethylsilylprop-2-ynal gives 2-(2-trimethylsilylethynyl)-3,4-(о-carborano)-2,5-dihydrofuran. Subsequent base-catalyzed desilylation furnishes new terminal alkynes of closoand nido-carborane series.
Kosenko,Dudarova,Ananyev,Bregadze,Semioshkin
p. 500 - 503
(2018)
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Insight into the solvation and isomerization of 3-halo-1-azaallylic anions from ab initio metadynamics calculations and NMR experiments
A study performed ab initio metadynamics calculations and nuclear magnetic resonance investigations, to demonstrate the solvation and isomerization of 3-halo-1-azaallylic anions. The 3-halo-1-azaallylic anions were solvated and isomerized from the N-isopr
Declerck, Reinout,De Sterck, Bart,Verstraelen, Toon,Verniest, Guido,Mangelinckx, Sven,Jacobs, Jan,De Kimpe, Norbert,Waroquier, Michel,Van Speybroeck, Veronique
p. 580 - 584
(2009)
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Synthesis of C-5a-substituted derivatives of 4-epi-isofagomine: Notable β-galactosidase inhibitors and activity promotors of GM1-gangliosidosis related human lysosomal β-galactosidase mutant R201C
From an easily available partially protected analog of 1-deoxy-L-gulo-nojirimycin, by chain-branching at C-4 and suitable modification, lipophilic analogs of the powerful β-D-galactosidase inhibitor 4-epi-isofagomine have been prepared. New compounds exhibit considerably improved inhibitory activities when compared with the unsubstituted parent compound and may serve as leads toward new pharmacological chaperones for GM1-gangliosidosis and Morquio B disease.
Thonhofer, Martin,Weber, Patrick,Gonzalez Santana, Andres,Tysoe, Christina,Fischer, Roland,Pabst, Bettina M.,Paschke, Eduard,Schalli, Michael,Stütz, Arnold E.,Tschernutter, Marion,Windischhofer, Werner,Withers, Stephen G.
p. 71 - 80
(2016)
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A novel bornane synthesis by an old idea
Aiming at a synthesis of spiro [2.4]hepta-4,6-dienes with a carbon substituent at C-4, we investigated solvolysis reactions of the thiatricycle 2, obtained from spiro[2.4]hepta-4,6-diene (1) and thiophosgene by [4 + 2] cycloaddition. With methanol or ethanol a mixture of the esters 7 and 8 was formed. Desulfurization of the thionoesters 8 gave methyl and ethyl spiro[2.4]hepta-4,6-diene-4-carboxylate (10a,b). The corresponding alcohol (11) was prepared from 10b by LiAlH4 reduction. Ethene-tetracarbonitrile combined with the 4-substituted spiro[2.4]hepta-4,6-dienes to give the [4 + 2] cycloadducts 12a-c. Diels-Alder reaction between 11 and 2-chloroacrylonitrile afforded the spiro(bicyclo[2.2.1]hept-5-ene-7,1′-cyclopropane) derivative 14a that was transformed in three steps to rac-10-hydroxycamphor (17). This synthesis of a bornane derivative opens opportunity for variations and thus may find further applications.
Foehlisch, Baldur,Abu Bakr, Derar,Fischer, Peter
p. 3682 - 3686
(2002)
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Synthesis of a potent antimalarial amphilectene
7-Isocyano-11(20),14-epiamphilectadiene, the most potent of antimalarial amphilectenes, is synthesized in seven steps from readily available materials. The synthesis is enabled by a new dendrimeric triene (Danishefsky [3]-dendralene) and a new method for stereo- and chemoselective isocyanation. This chemistry provides a useful entry into an underexplored yet promising family of antimalarial terpenoids.
Pronin, Sergey V.,Shenvi, Ryan A.
p. 19604 - 19606
(2012)
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The donor-base-free aggregation of lithium diisopropyl amide in hydrocarbons revealed by a DOSY method
Abstract Lithium diisopropyl amide (LDA) is a very prominent reagent that plays a key role in organic synthesis, serving as a base par excellence for a broad range of deprotonation reactions. However, the state of aggregation in solution in the absence of donor bases was unclear. In this paper we solved this problem by employing DOSY NMR experiments based on a newly elaborated external calibration curve (ECC) approach with normalized diffusion coefficients. An important reagent: Lithium diisopropyl amide plays a key role in organic synthesis, serving as a base par excellence for a broad range of deprotonation reactions. However, its state of aggregation in solution in the absence of donor bases was unclear. This problem has been solved by application of a new DOSY NMR experiment.
Neufeld, Roman,John, Michael,Stalke, Dietmar
p. 6994 - 6998
(2015)
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Total synthesis of marine eicosanoid (-)-hybridalactone
(-)-Hybridalactone (1) is a marine eicosanoid isolated from the red alga Laurencia hybrida. This natural product contains cyclopropane, cyclopentane, 13-membered macrolactone and epoxide ring systems incorporating seven stereogenic centers. Moreover, this compound has an acid-labile skipped Z,Z-diene motif. In this paper, we report on the total synthesis of (-)-hybridalactone (1). The unique eicosanoid (-)-hybridalactone (1) was synthesized starting from optically active γ-butyrolactone 2 in a linear sequence comprising 21 steps with an overall yield of 21.9 %. A key step in the synthesis of (-)-hybridalactone (1) is the methyl phenylsulfonylacetate-mediated one-pot synthesis of the cis-cyclopropane-γ-lactone derivative. This reaction provided an efficient and stereoselective access to cis-cyclopropane-γ-lactone 12. Further elaboration of the latter compounds through desulfonylation, epoxidation, oxidation, Wittig olefination and Shiina macrolactonization afforded (-)-hybridalactone.
Ota, Koichiro,Sugata, Naoto,Ohshiro, Yoshihiko,Kawashima, Etsuko,Miyaoka, Hiroaki
p. 13531 - 13537,7
(2012)
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In situ ortho -lithiation/functionalization of pentafluorosulfanyl arenes
A general method for ortho-functionalization of pentafluorosulfanyl arenes has been developed. ortho-Lithiation with lithium tetramethylpiperidide at -60 °C in the presence of silicon, germanium, and tin electrophiles affords trapped products in moderate
Daugulis, Olafs,Le, Thanh V.
supporting information
p. 537 - 540
(2022/01/22)

Synthesis method of 3-oxo-5-hydroxy-6-cyanohexanoic acid tert-butyl ester
The invention relates to a synthesis method of 3-oxo-5-hydroxy-6-cyanohexanoic acid tert-butyl ester. According to the method, by using lithium metal and diisopropylamine as raw materials, reaction isinitiated under the action of styrene to prepare an intermediate product LDA, thereby solving the problem of overlow reaction temperature in the prior art, and the intermediate is directly mixed witha raw material tert-butyl acetate without further treatment to prepare an intermediate tert-butyl lithioacetate in a micro-channel reactor, and then the intermediate tert-butyl lithioacetate and ethyl 4-cyano-3-hydroxybutyrate are used for preparing the target product 3-oxo-5-hydroxy-6-cyanohexanoic acid tert-butyl ester in the micro-channel reactor. The reaction time is greatly shortened, the pollution is small, the pollutant emission is less, the cost is low, and the post-treatment is simple; and the yield reaches 99%, the purity is 99% or above, and the method is especially suitable for industrial large-scale production.
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Paragraph 0017-0018; 0039-0046; 0055-0056; 0065-0066

(2021/03/03)

Oxetane Promise Delivered: Discovery of Long-Acting IDO1 Inhibitors Suitable for Q3W Oral or Parenteral Dosing
3,3-Disubstituted oxetanes have been utilized as bioisosteres for gem-dimethyl and cyclobutane functionalities. We report the discovery of a novel class of oxetane indole-amine 2,3-dioxygenase (IDO1) inhibitors suitable for Q3W (once every 3 weeks) oral and parenteral dosing. A diamide class of IDO inhibitors was discovered through an automated ligand identification system (ALIS). Installation of an oxetane and fluorophenyl dramatically improved the potency. Identification of a biaryl moiety as an unconventional amide isostere addressed the metabolic liability of amide hydrolysis. Metabolism identification (Met-ID)-guided target design and the introduction of polarity resulted in the discovery of potent IDO inhibitors with excellent pharmacokinetic (PK) profiles in multiple species. To enable rapid synthesis of the key oxetane intermediate, a novel oxetane ring cyclization was also developed, as well as optimization of a literature route on kg scale. These IDO inhibitors may enable unambiguous proof-of-concept testing for the IDO1 inhibition mechanism for oncology.
Achab, Abdelghani,Bass, Alan,Bennett, David Jonathan,Bharathan, Indu,Daddio, Suzanne,Ferguson, Heidi,Ferraro, Jude,Fradera, Xavier,Freeland, Elizabeth,Gibeau, Craig,Han, Yongxin,Hilliard, Catherine,Hopkins, Brett,Knemeyer, Ian,Lesburg, Charles A.,Li, Derun,Liu, Kun,Martinot, Theodore A.,McGowan, Meredeth A.,Miller, J. Richard,Otte, Karin M.,Pasternak, Alexander,Pu, Qinglin,Qi, Ji,Sciammetta, Nunzio,Sloman, David L.,Solban, Nicolas,Song, Licheng,Song, Zhiguo J.,Vincent, Stella,Wan, Baoqiang,White, Catherine,Yin, Jingjun,Ykoruk, Bridget,Zamlynny, Beata,Zhai, Jin,Zhang, Hongjun,Zhang, Huangguang,Zhou, Hua
(2022/03/16)

Selective Continuous Flow Iodination Guided by Direct Spectroscopic Observation of Equilibrating Aryl Lithium Regioisomers
The iodination of 4-fluoro-2-(trifluoromethyl)benzonitrile via C-H lithiation and subsequent treatment with iodine under continuous flow conditions is described. Screening identified both LDA and PhLi as effective bases, giving the desired 3-iodo regioisomer as the major product. Use of LDA results in varying amounts of the undesired 5-iodo isomer, while PhLi results in more reliable formation of the 3-iodo product. An initial flow process was developed using PhLi that produced 4-fluoro-3-iodo-2-(trifluoromethyl)benzonitrile in 63% yield on a gram scale. Process modifications to enable pilot-scale operation resulted in a yield decrease to 50%, persistent formation of a byproduct resulting from PhLi addition to the nitrile, and formation of solids during longer runs. As a result, the use of LDA was investigated under continuous flow conditions. In situ NMR and IR spectroscopy allowed observation of the 5-[Li] species and its conversion to the thermodynamically preferred 3-[Li] species. These mechanistic insights drove development of a second-generation continuous flow process using LDA that achieves 30:1 regioselectivity and an 84% solution yield of the desired product (67% isolated yield after recrystallization). Furthermore, this process increases throughput by 10-fold, providing a path to manufacturing-scale operation.
Dunn, Anna L.,Leitch, David C.,Journet, Michel,Martin, Michael,Tabet, Elie A.,Curtis, Neil R.,Williams, Glynn,Goss, Charles,Shaw, Tony,O'Hare, Bernie,Wade, Charles,Toczko, Matthew A.,Liu, Peng
supporting information
p. 129 - 137
(2018/10/09)

Chiroptical and redox properties of a tetrathiafulvalene analogue with an inserted spiro framework
A chiral spiro compound (1a) having 1,3-dithiol units has been synthesized as a stereogenic tetrathiafulvalene analogue. Spiro 1a was resolved into two enantiomers by chiral HPLC, and they exhibited remarkable chiroptical properties featuring dehydroindene-dithiol chromophore in C2 symmetry. In addition, electrochemical properties were also investigated by using cyclic voltammetry and electronic spectra of cationic species.
Hasegawa, Masashi,Kurebayashi, Daisuke,Matsuzawa, Hideyo,Mazaki, Yasuhiro
supporting information
p. 989 - 992
(2018/08/24)

NOVEL CEPHALOSPORIN DERIVATIVE AND PHARMACEUTICAL COMPOSITION THEREOF
The present invention relates to novel cephalosporin derivatives represented by Chemical Formula 1. Wherein, X, Y, L, R1, and R2 are as same as defined in the description of the invention. The present invention also relates to pharmaceutical antibiotic compositions comprising a novel celphalosporin derivative represented by Chemical Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient. According to the present invention, novel cephalosporin derivatives, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an effective ingredient for the broad spectrum of antibiotic resistant, low toxicity, particularly in Gram-negative bacteria, which can be useful with strong antimicrobial activity.
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Paragraph 0201

(2014/03/25)

TARGETED COVALENT PROBES AND INHIBITORS OF PROTEINS CONTAINING REDOX-SENSITIVE CYSTEINES
Covalent, irreversible small-molecule inhibitors that modify the sulfenyl form (i.e., sulfenic acid, RSOH and sulfenamide, RSNR'2) of therapeutically important proteins (particularly kinases and phosphatases) are disclosed, where the compositions include a compound having a substituted aryl or heterocyclic core structure that promotes binding interactions with a specific protein, and a nucleophilic reaction center (carbon, nitrogen, sulfur, or phosphorous) that is capable of forming a covalent bond with a sulfenic acid- or sulfenamide-modified cysteine residue in the protein. Methods for synthesizing these compounds are also disclosed, as well as methods of using them for determining the bioactivity of a chemical composition comprising an active compound toward a specific protein and for determining the potency of an inhibitor against a specific protein.
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Paragraph 0144; 0145; 0146; sheet 6/28

(2014/06/24)

Promising ZnO-based DSSC performance using HMP molecular dyes of high extinction coefficients
Employing newly synthesized di-substituted tri-phenyl amine (HMP-9) and carbazole (HMP-11) dyes (with limited acidic carboxyl anchor groups), a power conversion efficiency as high as 7.03% in ZnO nanocrystallite (NC)-based dye-sensitized solar cells (DSSCs) is achieved. The specific molecular designs of HMP-09 and HMP-11 consisting of with and without hexyloxy spacer groups, and added tri-phenyl amine or 9-phenyl-9H-carbazole donor groups, respectively, attached on the ancillary ligands are advantageous, evidenced from electrochemical impedance spectroscopy measurements, for ZnO NC-based DSSCs. This journal is the Partner Organisations 2014.
Ganesh,Nguyen, Hong-Minh,Mane, Rajaram S.,Kim, Nakjoong,Shinde, Dipak V.,Bhande, Sambhaji S.,Naushad, Mu.,Hui,Han, Sung Hwan
supporting information
p. 11305 - 11308
(2014/07/21)

New antiprotozoal agents: Their synthesis and biological evaluations
Here we report identification of new lead compounds based on quinoline and indenoquinolines with variable side chains as antiprotozoal agents. Quinolines 32, 36 and 37 (Table 1) and indenoquinoline derivatives 14 and 23 (Table 2) inhibit the in vitro growth of the Trypanosoma cruzi, Trypanosoma brucei, Trypanosoma brucei rhodesiense subspecies and Leishmania infantum with IC 50 = 0.25 μM. These five compounds have superior activity to that of the front-line drugs such as benznidazole, nifurtimox and comparable to amphotericin B. Thus these compounds constitute new 'leads' for further structure-activity studies as potential active antiprotozoal agents.
Upadhayaya, Ram Shankar,Dixit, Shailesh S.,F?ldesi, Andras,Chattopadhyaya, Jyoti
supporting information
p. 2750 - 2758
(2013/07/05)

Catalyst-controlled C-O versus C-N allylic functionalization of terminal olefins
The divergent synthesis of syn-1,2-aminoalcohol or syn-1,2-diamine precursors from a common terminal olefin has been accomplished using a combination of palladium(II) catalysis with Lewis acid cocatalysis. Palladium(II)/bis-sulfoxide catalysis with a silver triflate cocatalyst leads for the first time to anti-2-aminooxazolines (C-O) in good to excellent yields. Simple removal of the bis-sulfoxide ligand from this reaction results in a complete switch in reactivity to afford anti-imidazolidinone products (C-N) in good yields and excellent diastereoselectivities. Mechanistic studies suggest the divergent C-O versus C-N reactivity from a common ambident nucleophile arises due to a switch in mechanism from allylic C-H cleavage/functionalization to olefin isomerization/oxidative amination.
Strambeanu, Iulia I.,White, M. Christina
supporting information
p. 12032 - 12037
(2013/09/02)

Biocompatible resists
This invention relates to biomaterials, biocompatible photoresists, and electroactive photoresists, and methods to engineer the interactions between biomaterials and cells. In one aspect, this invention provides for modifying surface topography through micro-patterning techniques that require no organic solvent development to reveal the lithographic patterns. Cells can be cultured on these surfaces directly and exhibit strong cell alignment features.
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(2012/03/10)

Organocatalytic Functionalization of carboxylic acids: Isothiourea- catalyzed asymmetric intra- and intermolecular Michael addition-lactonizations
Tetramisole promotes the catalytic asymmetric intramolecular Michael addition-lactonization of a variety of enone acids, giving carbo- and heterocyclic products with high diastereo- and enantiocontrol (up to 99:1 dr, up to 99% ee) that are readily derivatized to afford functionalized indene and dihydrobenzofuran carboxylates. Chiral isothioureas also promote the catalytic asymmetric intermolecular Michael addition-lactonization of arylacetic acids and α-keto-β,γ-unsaturated esters, giving anti-dihydropyranones with high diastereo- and enantiocontrol (up to 98:2 dr, up to 99% ee).
Belmessieri, Dorine,Morrill, Louis C.,Simal, Carmen,Slawin, Alexandra M. Z.,Smith, Andrew D.
supporting information; experimental part
p. 2714 - 2720
(2011/04/23)

METHOD OF MAKING COUPLED HETEROARYL COMPOUNDS VIA REARRANGEMENT OF HALOGENATED HETEROAROMATICS FOLLOWED BY OXIDATIVE COUPLING
The inventions disclosed and described herein relate to new and efficient generic methods for making a wide variety of compounds having Formulas (I) and (II) as shown below (Formulas (I) and (II)) wherein HAr is an optionally substituted five or six membered heteroaryl ring, and Hal is a halogen, and Y is a bridging radical, such as S, Se, NR5 C(O), C(O)C(O),Si(R5)2, SO, SO2, PR5, BR5, C(R5)2 or P(O)R5. The synthetic methods employ a "Base-Catalyzed Halogen Dance" reaction to prepare a metallated compound comprising a five or six membered heteroaryl ring comprising a halogen atom, and then oxidatively coupling the reactive intermediate compound. The compounds of Formula (II) and/or oligomer or polymers comprising repeat units having Formula (II) can be useful for making semi-conducting materials, and/or electronic devices comprising those materials.
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Page/Page column 49

(2011/09/15)

COMPOUNDS FOR TREATING NEURODEGENERATIVE DISEASES
The invention provides novel spirotetrahydronaphthalene compounds of Formula α that inhibit β-secretase cleavage of APP and are useful as therapeutic agents for treating neurodegenerative diseases.
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Page/Page column 123-124

(2011/10/13)

BENZISOXAZOLE COMPOUND
Disclosed is a compound represented by the general formula (I) or a salt thereof: wherein any one of R1, R2 and R3 represents a group represented by the formula: -(CH2)m-NR11R12 (wherein m is 1 or 2; and R11 and R12 independently represent a hydrogen atom or a C1-6 alkyl group or may, together with a nitrogen atom to which R11 and R12 are bound, form a 4- or 5-membered cyclic group); the remaining two or R1, R2 and R3 independently represent a group represented by the formula: -(O)n-R21 (wherein n is 0 or 1; and R21 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like); and R4 represents a C1-6 alkyl group which may have a substituent or the like.
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Page/Page column 55; 133

(2009/02/10)

Vanilloid receptor ligands and their use in treatments
Bicyclic 3,4-fused piperidine compounds, and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotizing agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
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Page/Page column 22

(2009/04/24)

SPIRO CONDENSED BARBITURIC ACID DERIVATIVES FOR USE AS ANTIBACTERIAL
In one aspect, the present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to method for their preparation.
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Page/Page column 69-70; 73-74; 101

(2009/03/07)

MULTIKINASE INHIBITORS FOR USE IN THE TREATMENT OF CANCER
The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I):...................................................................
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Page/Page column 92

(2009/03/07)

VIRAL POLYMERASE INHIBITORS
Compound of Formula I: wherein, R2, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase
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Page/Page column 91

(2009/04/25)

PROCESS FOR THE PREPARATION OF RENIN INHIBITORS
Disclosed is a process for the preparation of a tetrahydropyran-di-amine represented by Structural Formula (I): wherein R1 is H or alkyl and E is H or an amine protecting group.
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Page/Page column 16; 17; 18

(2009/04/25)

NOVEL CYCLIC BORONATE INHIBITORS OF HCV REPLICATION
Compounds of formula (I) or a salt thereof are provided; wherein R1, R2, R3, R4, R6, R8, R20, R30, Y, Z and n are as defined in the description. Uses of the compounds as medicaments, and in the manufacture of medicaments for treating viral infection, especially HCV infection are also disclosed. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.
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Page/Page column 86-87; 93; 112; 114

(2009/05/29)

Heterocyclic spiro-compounds as aldosterone synthase inhibitors
The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, W, X, Y, Z and n have the definitions elucidated in more detail in the description, to a process for preparing them and to th
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Page/Page column 9

(2009/05/28)

ALKYLSULFONYL-SUBSTITUTED THIAZOLIDE COMPOUNDS
A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.
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Page/Page column 73

(2009/04/24)

FUSED PYRIDINE, PYRIMIDINE AND TRIAZINE COMPOUNDS AS CELL CYCLE INHIBITORS
Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4 mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.
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Page/Page column 112-113

(2009/08/14)

SUBSTITUTED PHENYLCYCLOHEXYLGLYCOLATES
Disclosed herein are substituted phenylcyclohexylglycolate-based muscarinic acetylcholine receptor modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 47-48

(2009/10/06)

INHIBITORS OF JAK2 KINASE
Compounds inhibiting the bioactivity of the protein tyrosine kinase JAK2 are provided, along with methods of using the compounds in the treatment of malconditions wherein inhibition of JAK2 is medically indicated. Methods of preparation are also provided
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Page/Page column 24-25

(2009/03/07)

INDOLYL- PYRIDONE DERIVATIVES HAVING CHECKPOINT KINASE 1 INHIBITORY ACTIVITY
Compounds of formula (I) have checkpoint kinase 1 (CHK1 ) inhibitory activity: wherein R1, R2, R5 and R6 are independently selected from hydrogen, hydroxy, methyl, trifluoromethyl, hydroxymethyl, methoxy, triflu
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Page/Page column 66

(2009/09/05)

Certain Chemical Entities, Compositions and Methods
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
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Page/Page column 14

(2009/10/30)

Synthesis of 2,6-dioxo-1,2,3,4,5,6-hexahydroindoles by acid-catalyzed cyclization of acetal-protected (2,4-dioxocyclohex-l-yl)acetamides and their transformation into 5,8,9,10-tetrahydro-6H-indolo[2,1-a]isoquinolin-9-ones
Acetal-protected (2,4-dioxocyclohex-1-yl)-acetic acids were prepared by allylation of dilithiated 1,3-cyclohexane-1,3-diones, protection of the carbon-yl groups and oxidation of the alkene moiety. Their reaction with amines afforded the corresponding amides which were transformed, by acid-catalyzed cyclization, into various 2,6-dioxo-1,2,3,4,5,6-hexahy-droindoles. The reaction of the latter with triflic acid resulted in the formation of novel 5,8,9,10-tetrahy-dro-6H-indolo[2,1-a]isoquinolin-9-ones.
Juma, Benard,Adeel, Muhammad,Villinger, Alexander,Reinke, Helmut,Spannenberg, Anke,Fischer, Christine,Langer, Peter
supporting information; experimental part
p. 1073 - 1079
(2009/12/05)

SUBSTITUTED SULFONAMIDE COMPOUNDS
Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing these compounds, and the use of such substituted sulfonamide compounds in pharmaceutical compositions for the treatment and/or inhibition of pain and other conditions at least partly mediated by the bradykinin 1 receptor
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Page/Page column 64

(2009/10/30)

SUBSTITUTED PYRIMIDINE DERIVATIVES
The present application describes substituted pyrimidine compounds of formula (I) wherein X, A1, R1, R2, R3, R4, R5, R6, R7, R8, R9, p, q, r, v,
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Page/Page column 26

(2009/10/31)

CYCLIC AMINE COMPOUND
The present invention provides an excellent antihypertensive medicament. The medicament of the present invention comprises a compound having the general formula (I) and the like: [wherein R1: H, substitutable alkyl, substitutable alkenyl, substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; R2: H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R3, R4; H, substitutable alkyl, substitutable alkenyl, substitutable cycloalkyl or the like; R5, R6: H, substitutable alkyl, substitutable cycloalkyl, substitutable alkoxy or the like; R7, R8: H, substitutable alkyl, substitutable cycloalkyl or the like; X: the formula (II) or the like; A: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like; Y: a single bond, substitutable alkylene, substitutable alkenylene, -(CH2)a-X1-(CH2)b- (X1: the formula -NH-, -O- or the like; a, b: 0-5) or the like; B: substitutable cyclic hydrocarbon, substitutable heterocyclyl or the like].
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Page/Page column 72-73

(2009/04/23)

BRYOSTATIN ANALOGUES, SYNTHETIC METHODS AND USES
Biologically active compounds related to the bryostatin family of compounds, having simplified spacer domains and/or improved recognition domains are disclosed, including methods of preparing and utilizing the same.
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Page/Page column 122

(2009/05/28)

Intramolecular carbolithiation reactions for the synthesis of 2,4-disubstituted tetrahydro-quinolines: Evaluation of TMEDA and (-)-sparteine as ligands in the stereoselectivity
The preparation of 4-substituted 2-phenyltetrahydroquinolines from N-alkenylsubstituted 2-iodoanilines via intramolecular carbolithiation reactions has been investigated. The stereochemical outcome of the carbolithiation reactions depends on the nature of organolithium employed to perform the lithium-halogen exchange, the solvent, or the use of additives, for example, TMEDA or chiral bidentated ligands such as (-)-sparteine. Thus, the 2,4-disubstituted tetrahydroquinolines are obtained with moderate diastereoselectivities (up to 77:23) and with ee up to 94% when Weinreb amide derivatives are used (R) CONMe(OMe)).
Martinez-Estibalez, Unai,Sotomayor, Nuria,Lete, Esther
supporting information; experimental part
p. 1237 - 1240
(2009/08/12)

PREPARATION AND ENANTIOMERIC SEPARATION OF 7-(3-PYRIDINYL)-1,7-DIAZASPIRO[4.4] NONANE AND NOVEL SALT FORMS OF THE RACEMATE AND ENANTIOMERS
A novel scalable synthesis for the preparation of 7-(3- pyridinyI)- 1,7- diazaspiro[4.4)nonane has been developed, and7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane salts have been formed with succinic acid and oxalic acid. Additionally, 7-(3-pyridinyl)-1,7- diazaspiro[4.4]nonane has been separated into its stereoisomers via resolution with L and D di-p-toluoyltartaric acids, giving (R)- and (S)-7-(3-pyridinyl)-1,7-diazaspiro[4.4]nonane of high enantiomeric purity. Numerous solid salts of the resulting (R)- and (S)-7-(3-pyridinyl)-1,7- diazaspiro[4.4}nonane have been prepared. Methods for the preparation of the racemic and enantiomeric salts, pharmaceutical compositions comprising such salts, and uses thereof are disclosed. The salts can be administered to patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, to treat and/or prevent such disorders.
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Page/Page column 27

(2009/08/16)

Selective androgen receptor modulators
This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
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Page/Page column 42

(2009/10/18)

Photochromic Compound
[Problem] To provide a photochromic compound that is rapidly colored upon irradiation with ultraviolet light, and is rapidly decolored rapidly upon heat application after termination of irradiation with ultraviolet light, and to provide a process for producing the same. [Means for Solving Problems] A photochromic compound represented by general formula (I). R1, R2 and R3 are each a hydrogen atom; a functional group containing an atom in groups 15-16 of the periodic table; a halogen atom; a hydrocarbon group optionally substituted with said functional group or a halogen atom; or an optionally substituted heterocyclic group. R1 and R2 as well as R2 and R3 may be bonded to each other to form an optionally substituted carbon or heterocyclic ring. Z is a polymantylidene group. W is a divalent organic group that forms an optionally substituted carbon aromatic or heterocyclic aromatic ring together with the carbon-carbon double bond to which it is bonded.
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Page/Page column 11-12

(2009/12/23)

Organic Semiconductors and Their Manufacture
The invention relates to a semiconductor device comprising a compound of the formula I and of the formula XXI, wherein the symbols have the meanings defined in the specification, to the novel compounds of the formula I and XXI and to the use of such a compound as an organic semiconductor for the preparation of an electronic device, and further compounds and devices, as well as other embodiments given in the specification.
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Page/Page column 16

(2009/12/23)

ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
The present invention relates to compounds of the formula (I), wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula (I), their use and pharmaceutical compositions comprising them.
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Page/Page column 152

(2010/01/29)

PROPIOPHENONE DERIVATIVES
This invention relates to novel compounds that are propiophenones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel propiophenones derivatives that are derivatives of bupropion. This invention also provides compositions comprising one or more compounds of this invention and a carrier and use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a norepinephrine dopamine reuptake inhibitor, such as bupropion.
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Page/Page column 30-31

(2009/10/18)

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
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Page/Page column 107-108

(2008/06/13)

AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE
The present invention relates to novel compounds of formula (I)′, pharmaceutically acceptable salts, prodrugs or solvates thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is a group A, K or W wherein A is (II) K is an α or β naphthyl group, optionally substituted by 1 or 2 groups R18, each of them being the same or different; and W is (III) and wherein G is a 5,6-membered monocyclic heteroaryl, or a 8- to 11-membered heteroaryl bicyclic group; such G may be substituted by (R15)p, which can be the same or different; p is an integer from 0 to 5; R3 is selected in the group consisting of: hydrogen, fluorine, and C1-4alkyl; or corresponds to a group X or X1; R4 is selected in the group consisting of: hydrogen, fluorine, and C1-4alkyl; or corresponds to a group X or X1; R5 is hydrogen or C1-4alkyl; R7 is hydrogen or C1-4alkyl; or is a group X, X1, X2 or X3; wherein X is (IV) X1 is (V) X2 is (VI) and X3 is (VII) R6 is hydrogen or C1-4alkyl; or is a group X or X1; R9 is C1-4alkyl; R10 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R8 is a 5-6 membered heterocycle group, which may be substituted by one or two substituents selected from a group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R11 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R12 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R13 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R14 is selected from a group consisting of: hydrogen, halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4aIkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R15 is selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R8; R16 is hydrogen, C1-4alkyl, C3-6cycloalkyl or C3-6cycloalkylC1-3alkyl; R17 is hydrogen or C1-4alkyl; R18 is selected from a group consisting of: halog
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Page/Page column 114-115

(2008/06/13)

BENZENESULFONAMIDE COMPOUNDS AS EDG-1 ANTAGONISTS USEFUL IN THE TREATMENT OF CANCER
This invention relates to novel compounds of formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds possess Edg-1 antagonistic activity and are accordingly useful in the treatment and/or prophylaxis of canc
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Page/Page column 32-33; 46-47; 48

(2008/12/05)

5-SULFANYLMETHYL-PYRAZOLO [1,5-A] PYRIMIDIN-7-OL DERIVATIVES AS CXCR2 ANTAGONISTS
The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.
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Page/Page column 31

(2008/12/05)