- TLR2 MODULATOR COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
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The present disclosure relates to compounds which modulate the activity of Toll-like receptor (TLR) proteins, including agonists or activators, partial agonists, and antagonists. Of particular interest of compounds that modulate the activity of TLR2, as well as methods of using such compounds to treat cancer and other disorders associated with a TLR2 pathway.
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Paragraph 001011-001012
(2021/12/08)
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- NOVEL JAK1 SELECTIVE INHIBITORS AND USES THEREOF
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The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic di
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- Synthesis method of moCys section of marine natural product apratoxin E
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The invention relates to a synthesis method of moCys section of a marine natural product apratoxin E, and belongs to the field of chemical synthesis. The moCys section (C27 to C30 section) of the marine natural product apratoxin E is prepared from cheap a
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Paragraph 0012
(2017/01/19)
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- PROCESSES OF PREPARING A JAK1 INHIBITOR AND NEW FORMS THERETO
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This invention relates to processes for preparing a JAKl inhibitor having Formula la: as well as new forms of the inhibitor.
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Page/Page column 64; 74; 75
(2015/11/24)
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- New approach toward the total synthesis of (+)-batzellaside B
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A new synthetic approach to (+)-batzellaside B from naturally abundant L-pyroglutamic acid is presented in this article. The key synthetic step involves Sharpless asymmetric dihydroxylation of an olefinic substrate functionalized with an acetoxy group to
- Wierzejska, Jolanta,Motogoe, Shin-Ichi,Makino, Yuto,Sengoku, Tetsuya,Takahashi, Masaki,Yoda, Hidemi
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p. 1831 - 1838,8
(2020/09/16)
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- RENIN INHIBITORS
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Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the t
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Page/Page column 33-34
(2010/08/07)
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- Copper(I) mediated cross-coupling of amino acid derived organozinc reagents with acid chlorides
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This paper describes the development of a straightforward experimental protocol for copper-mediated cross-coupling of amino acid derived β-amido-alkylzinc iodides 1 and 3 with a range of acid chlorides. The present method uses CuCN·2LiCl as the copper source and for organozinc reagent 1 the methodology appears to be limited to reaction with more stable acid chlorides, providing the desired products in moderate yields. When applied to organozinc reagent 3, however, the protocol is more general and provides the products in good yields in all but one of the cases tested. The Royal Society of Chemistry 2006.
- Hjelmgaard, Thomas,Tanner, David
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p. 1796 - 1805
(2008/02/05)
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- HALOARYL SUBSTITUTED AMINOPURINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Aminopurine Compounds having the following structure: (I) wherein R1 , R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
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Page/Page column 151
(2008/06/13)
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- COMBINATION THERAPY WITH INHIBITORS OF INDUCIBLE NITRIC OXIDE SYNTHASE AND ALKYLATING AGENTS
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A combination therapy comprising administration of a carbamoylating chemotherapeutic agent in conjunction with administration of a selective iNOS inhibitor compound is disclosed. Optionally, resection and radiation therapy are provided with the therapeutic combination. A medicament comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound together with a pharmaceutically acceptable carrier is further disclosed. A kit comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound is further disclosed.
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Page/Page column 61
(2010/02/11)
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- NEW HETEROCYCLIC AMIDE COMPOUNDS USEFUL FOR THE TREATMENT OF INFLAMMATORY AND ALLERGIC DISORDERS: PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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The present invention relates to novel heterocyclic compounds that inhibit phosphodiesterase type 4 (PDE 4). The compounds are useful for treating inflammatory conditions, diseases of the central nervous systems and insulin resistant diabetes.
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- METHODS FOR TREATMENT AND PREVENTION OF GASTROINTESTINAL CONDITIONS
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Therapeutic methods for the prevention ad treatment of conditions and diseases of the gastrointestinal tract involving an overproduction of nitric oxide by inducible nitric oxide synthase are described, the methods including administering to a subject in need thereof a therapeutically effective amount of a selective inhibitor of inducible nitric oxide synthase (iNOS). The methods also include the use of selective inhibitors of iNOs in combination with other therapeutic agents, including antimicrobial agents and antisecretory agents.
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Page/Page column 54
(2010/02/06)
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- Synthesis of enantiomerically pure β- and γ-amino acid derivatives using functionalized organozinc reagents
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β-Amido zinc reagents 4 and 5 readily undergo β-elimination when prepared in THF, but when a polar aprotic solvent such as DMF is employed, β-elimination is suppressed. Using DMF, reaction of 4 with aryl iodides provides β-homophenylalanine derivatives (12 examples, 20-89% yield), and analogous reactions of 5 give γ-bishomophenylalanine derivatives (7 examples, 34-80% yield). The related zinc/copper reagents 17 and 18 are also useful intermediates that undergo subsequent cross-coupling reactions with a wide range of electrophiles (9 examples, 28-87% yield).
- Dexter, Charles S.,Jackson, Richard F. W.,Elliott, Jason
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p. 7579 - 7585
(2007/10/03)
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- Efficient synthesis of β- and γ-amino acid derivatives using new functionalised zinc reagents: Enhanced stability and reactivity of β-amido zinc reagents in dimethylformamide
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The new zinc reagents 3 and 4 are not sufficiently stable to be prepared efficiently in THF, but they can be prepared in DMF under mild and convenient conditions; subsequent palladium- catalysed coupling with aromatic iodides gives protected β- and γ-amin
- Dexter, Charles S.,Jackson, Richard F. W.
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- 2,9-DIAMINO- AND 2-AMINO-8-CARBAMOYL-4-HYDROXY-ALKANOIC ACID AMIDE DERIVATIVES
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Compounds of the formula I STR1 in which R 1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R 2 and R 3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R 4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R 5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R 6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R 7 is hydrogen or lower alkyl, or R 6 and R. sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R 8 denotes an aliphatic, cycloaliphatic-aliphatic or heteroarylaliphatic radical, and their salts can be used as active ingredients for medicaments for treatment of high blood pressure.
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- Synthesis of enantiomerically pure β- and γ-amino acids from aspartic and glutamic acid derivatives
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An efficient synthesis of enantiomerically pure β- and γ-amino acids starting from commercially available aspartic and glutamic acid derivatives is described. The acid function, α to the amino group, is first transformed to a good leaving group and the pr
- El Marini,Roumestant,Viallefont,Razafindramboa,Bonato,Follet
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p. 1104 - 1108
(2007/10/02)
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- Synthesis of Four Diastereomeric L-2-(Carboxycyclopropyl)glycines. Conformationally Constrained L-Glutamate Analogues
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To determine what conformations of L-glutamate (L-Glu) activate that compound's different receptors in the mammalian central nervous system, four diastereochemically L-2-(carboxycyclopropyl)glycines, 1-4, which are conformationally constrained analogues o
- Shimamoto, Keiko,Ishida, Michiko,Shinozaki, Haruhikio,Ohfune, Yasufumi
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p. 4167 - 4176
(2007/10/02)
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- NEW ROUTES TO THE SYNTHESES OF CIS-α-(CARBOXYCYCLOPROPYL)GLYCINES FROM L-GLUTAMIC ACID. CONFORMATIONALLY RESTRICTED ANALOGUES OF THE EXCITATORY NEUROTRANSMITTER L-GLUTAMIC ACID
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Potent neuroactive amino acids, (2S,2S,4R) and (2S,3R,4S) isomers of α-(carboxycyclopropyl)glycines (CCG-III and CCG-IV), were synthesized from L-glutamic acid via a palladium(II) catalyzed cyclopropanation of the α,β-unsaturated pyrrolidone and γ-amino-δ-lactone derivatives, respectively.
- Shimamoto, Keiko,Ohfune, Yasufumi
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p. 3803 - 3804
(2007/10/02)
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