- A supramolecular oligophenylenevinylene-C60 conjugate
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A new methanofullerene derivative with an ammonium subunit has been prepared and its ability to form a supramolecular complex with an oligophenylenevinylene (OPV)-crown ether conjugate evidenced by NMR, electrospray mass spectrometry and luminescence expe
- Gutiérrez-Nava, Manuel,Nierengarten, Hélène,Masson, Patrick,Van Dorsselaer, Alain,Nierengarten, Jean-Fran?ois
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Read Online
- Development of a selective matrix metalloproteinase 13 (MMP-13) inhibitor for the treatment of Osteoarthritis
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Osteoarthritis (OA) is a chronic disorder that causes damage to the cartilage and surrounding tissues and is characterized by pain, stiffness, and loss of function. Current treatments for OA primarily involve providing only relief of symptoms but does not
- Bendele, Alison M.,Neelagiri, Madhavi,Neelagiri, Venugopal,Sucholeiki, Irving
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- HISTONE DEMETHYLASE INHIBITORS FOR TREATING CANCERS
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The present disclosure provides a new series of 8-hydroxyquinoline derivatives/analogs that are potent KDM4 inhibitors with high activity and selectivity against KDM4 enzymes. Also disclosed are the pharmaceutical compositions comprising such 8-hydroxyqui
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Paragraph 0178-0179
(2021/01/22)
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- PROCESSES FOR MAKING COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE
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The present invention relates to processes and intermediates for preparing compounds useful as inhibitors of ATR kinase, such as aminopyrazine-isoxazole derivatives and related molecules. The present invention also relates to compounds useful as inhibitors of ATR protein kinase. The invention relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and solid forms of the compounds of this invention. The compounds of this invention have formula (I) or (II) wherein the variables are as defined herein.
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Paragraph 00177
(2013/04/13)
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- Pd-catalyzed Suzuki-Miyaura cross-coupling reactions between sulfamates and potassium Boc-protected aminomethyltrifluoroborates
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Sulfamates were studied as the electrophilic partners in the palladium-catalyzed Suzuki-Miyaura cross-coupling reaction with potassium Boc-protected primary and secondary aminomethyltrifluoroborates. A broad range of substrates was successfully coupled to provide the desired products. Complex molecules containing a new carbon-carbon bond and an aminomethyl moiety could be prepared through this developed method.
- Molander, Gary A.,Shin, Inji
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supporting information
p. 2534 - 2537
(2013/06/27)
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- Suzuki-Miyaura cross-coupling reactions of potassium boc-protected aminomethyltrifluoroborate with aryl and hetaryl mesylates
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Palladium-catalyzed Suzuki-Miyaura cross-coupling reactions were studied with potassium Boc-protected aminomethyltrifluoroborate through C-O activation of various mesylate derivatives to afford the corresponding products in moderate to good yields.
- Molander, Gary A.,Shin, Inji
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supporting information; experimental part
p. 3138 - 3141
(2012/08/07)
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- Synthesis of arylglycine and mandelic acid derivatives through carboxylations of α-amido and α-acetoxy stannanes with carbon dioxide
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Incorporation reactions of carbon dioxide (CO2) with N-Boc-α-amido and α-acetoxy stannanes were developed using CsF as a mild tin activator. Monoprotected α-amido stannanes could be used, and the corresponding arylglycine derivatives were obtained in moderate-to-high yields under 1 MPa (10 atm) of CO2 pressure. α-Acetoxy stannanes also underwent carboxylation to afford mandelic acid derivatives in excellent yields under ambient CO2 pressure. Both transformations enabled the synthesis of α-tertiary and α-quaternary carboxylic acid derivatives. In addition, the chirality of (S)-N-tert-butylsulfonyl-α- amido stannanes was transferred with up to 90% inversion of configuration at 100 °C.
- Mita, Tsuyoshi,Sugawara, Masumi,Hasegawa, Hiroyuki,Sato, Yoshihiro
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experimental part
p. 2159 - 2168
(2012/06/01)
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- NEW BRADYKININ B1 ANTAGONISTS
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The invention relates to compounds of formula (I) where in R1, R1a, R1b, R2, R3 and X, X1, X2, X3 have the meaning as cited in the description and the claims. Said compounds are useful as Bradykinin B1 antagonists. The invention also relates to pharmaceutical compositions, the preparation of such compounds as well as the production and use as medicament.
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Page/Page column 206-207
(2010/04/03)
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- NOVEL 2-QUINOLONE DERIVATIVE
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A compound represented by the formula (1) or a pharmaceutically acceptable salt thereof which has a therapeutic or prophylactic effect on an SNS-related disease such as neuropathic pain. (1) wherein R1 and R2 independently represent
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Page/Page column 50
(2008/06/13)
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- NITROGENOUS FUSED BICYCLIC COMPOUND
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A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R 0 represents hydrogen, halogeno, etc.; R 1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D 1 , D 2 and D 3 each represents N or CH; R 2 represents halogeno or optionally halogenated lower alkyl, etc.; R 3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)
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Page/Page column 57
(2010/11/26)
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- HYDRAZONE DERIVATIVE
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A compound represented by the following formula (I): wherein R1 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R2 represents hydrogen, aryl which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc.; R3 represents hydrogen, etc.; Ar represents a divalent group derived from aromatic hydrocarbon, etc.; X represents a single bond, linear or branched alkylene having from 1 to 3 carbon atoms which may have a substituent, etc.; and G represents halogen, a saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group which may have a substituent, a saturated or unsaturated 5- to 7-membered heterocyclic group which may have a substituent, etc., a salt thereof or a solvate thereof; and an agent for inhibiting aggregation and/or deposition of an amyloid protein or an amyloid-like protein, which comprises the compound, a salt thereof or a solvate thereof
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Page/Page column 40-41
(2010/11/08)
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- BASIC AMINE COMPOUND AND USE THEREOF
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Novel amine compounds which are represented by the following formula (1) and efficacious against diseases such as a viral infectious disease with HIV, rheumatism, and cancer metastasis; typically, A 1 and A 2 represent a hydrogen atom or a substitutable monocyclic or polycyclic heteroaromatic ring and W represents a substitutable benzene ring or any group represented by the following formula (10) or (11): where X represents O, CH 2 , C(=O), NR 11 , or CHR 35 and D represents a group represented by the following formula (6): where Q represents a single bond, NR 12 , or a group represented by the formula (13): and Y represents a group represented by the following formula (7) : where z represents a substitutable monocyclic or polycyclic aromatic ring; and B represents -NR 25 R 26 ; and R 1 to R 26 in the above formulae represent a hydrogen atom, an alkyl group, an alkenyl group, or an alkynyl group.
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Page/Page column 48
(2010/11/24)
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- NOVEL ETHYLENEDIAMINE DERIVATIVES
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A compound represented by the following formula (1):Q-Q-T-N(R)-Q-N(R)-T-Q [wherein, R1 and R2 are hydrogen atoms or the like; Q1 is a saturated or unsaturated, 5- or 6- membered cyclic hydrocarbon group which may have a substituent, or the like; Q2 is a single bond or the like; Q3 represents the following group: -C(R3a)(R4a)-{C(R3b)(R4b)}m1-{C(R3c)(R4c)}m2-{C(R3d)(R4d)}m3-{C(R3e)(R4e)}m4-C(R3f)(R4f)- (in which, R3a to R4e represent hydrogen or the like); T0 represents a carbonyl group or the like; and T1 represents -COCONR- or the like]; or salt thereof, solvate thereof, or N-oxide thereof. The compound is useful as a preventive and/or therapeutic agent for cerebral infarction, cerebral embolism, myocardial infarction, angina pectoris, pulmonary infarction, pulmonary embolism, Buerger's disease, deep venous thrombosis, disseminated intravascular coagulation syndrome, thrombus formation after valve or joint replacement, thrombus formation and reocclusion after angioplasty, systemic inflammatory response syndrome (SIRS), multiple organ dysfunction syndrome (MODS), thrombus formation during extracorporeal circulation, or blood clotting upon blood drawing.
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Page/Page column 116
(2010/02/14)
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- ALKYNYL ARYL CARBOXAMIDES
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The present invention is related to alkynyl aryl carboxamides of Formula (I’) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance. insulin resistance, hyperlipidemia, hypertriglyceridemia- hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I’) to modulate, notably to inhibit the activity of PTPs. (I’) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy' is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1and R2 are independently from each other is selected from the group consisting of hydrogen or (CI-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1 -C6 alkyl, carboxy, C1-C6 alkoxy, C1 -C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
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Page/Page column 52
(2008/06/13)
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- Cryptophycin compounds
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The present invention provides cryptophycin compounds of Formula I that are useful in the treatment of neoplasms.
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Page/Page column 151
(2010/02/05)
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- Seleno compounds containing nitrone moiety, their preparation and their therapeutic uses
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The present invention provides novel seleno compounds containing nitrone moiety, a process for preparing the same, the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactiv
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- Sulfonyl derivatives
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Sulfonyl derivatives represented by general formula (I), salts of the same, and solvates of both: and application of them as drugs: [wherein R1is hydrogen, hydroxyl, nitro or the like; R2and R3are each independently hydrogen, halogeno or the like; R4and R5are each dependently hydrogen, halogeno or the like; Q1is an optionally substituted saturated or unsaturated 5- or 6-membered cyclic hydrocarbon group or the like; Q2is a single bond, oxygen or the like; Q3is, e.g., a group represented by formula (a): T1is carbonyl or the like; and X1and X2are each independently methylidyne or nitrogen]. These compounds exhibit potent Fxa inhibiting activities and serve as excellent anticoagulants which speedily exert satisfactory and persistent anti-thrombotic effects through oral administration and little cause adverse effects.
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- NOVEL SULFONYL DERIVATIVES
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Sulfonyl derivatives represented by the following general formula (I): Q1-Q2-T1-Q3-SO2-QA and drugs containing the same (wherein Q1 is an optionally substituted, saturated or unsaturated, five- or six-membered cyclic hydrocarbon group, a five- or six-membered heterocyclic group, or the like; Q2 is a single band, oxygen, sulfur, C1-C6 alkylene or the like; QA is optionally substituted arylalkenyl, heteroarylalkenyl or the like; and T1 is carbonyl or the like). These compounds have potent FXa-inhibitory effects and promptly exert satisfactory and persistent antithrombotic effects through oral administration, thus being useful as anticoagulant agents little accompanied with side effects.
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- Synthesis and biological activity of (S)-2-amino-3-(2,5-dihydro-5-oxo-4-isoxazolyl)propanoic acid (TAN-950 A) derivatives
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(S)-2-Amino-3-(2,5-dihydro-5-oxo-4-isoxazolyl)propanoic acid (TAN-950 A (1)) is a novel amino acid antibiotic which shows a high affinity for glutamate receptors of the central nervous system. To improve the affinity for glutamate receptors, the structure
- Tamura,Matsushita,Iwama,Harada,Kishimoto,Itoh
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p. 1199 - 1212
(2007/10/02)
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- A New Method for the Synthesis of Amides from Amines: Ruthenium Tetroxide Oxidation of N-Protected Alkylamines
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A simple synthetic method for the preparation of amides from the corresponding primary alkylamines was elaborated using ruthenium tetroxide (RuO4) oxidation as a key step.
- Tanaka, Ken-Ichi,Yoshifuji, Shigeyuki,Nitta, Yoshihiro
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p. 3125 - 3129
(2007/10/02)
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