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Class 548/492 - Having -C(=X)-, wherein X is chalcogen, bonded directly to ring carbon of the five-membered hetero ring (e.g., indole-2-carboxylic acids, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein a ring carbon of the five-membered hetero
No. of patents: 351
Last issue date: 06/14/2011


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NumberTitleIssue Date
7960569Indole antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
The present invention provides indole compounds of Formula (I) or (II): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables ring A, X1, X2, X
06/14/2011
7923570Process for the preparation of crystalline perindopril
The present invention relates to a new process for the preparation of crystalline perindopril. The present invention also relates to new alkyl ammonium salts of perindopril and the processes for the preparation thereof. ...
04/12/2011
7732621Process for the preparation of enantiomerically enriched indoline-2-carboxylic acid
The present invention relates to a process for the preparation of an enantiomerically enriched optionally substituted indoline-2-carboxylic acid or a salt thereof, wherein an enantiomerically enriched chiral ortho-X-substituted phenylalanine compound, wherein X is a...
06/08/2010
7728151Process for the purification of perindopril
A dicyclohexyamine salt of compound of formula I, namely perindopril, having an X-ray powder diffraction pattern with characteristic peaks (2θ): 8.462, 10.624, 18.693, 9.424, 17.272, 14.177, 19.499, 20.765, 21.409, and 14.540. ...
06/01/2010
7671215Process for the preparation of compounds having an ace inhibitory action
The present invention relates to the process for the preparation of compounds of formula (I) having an ACE inhibitory action wherein carboxy group of stereospecific amino acid is activated with an uranium salt in the presen...
03/02/2010
7521566Process for preparation of perindopril and salts thereof
A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe, convenient and cost-effective. The process involves reaction of compound of formula (I),
04/21/2009
7456296Method for preparation of crystalline perindopril erbumine
A process for preparation of crystalline perindopril erbumine of formula (II) which exhibits the X-ray (powder) diffraction pattern like that shown in FIG. 2 The process comprises reacting a solution of peri...
11/25/2008
7442790Caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and...
10/28/2008
7442805Substituted sulfonamide-indoles
The present invention relates generally to substituted sulfonamide indoles such as substituted sulfonamide indoles, and methods of using them. ...
10/28/2008
7439036Process for producing optically active octahydro-1H-indole-2-carboxylic acid
To provide an enzymatic resolution process for efficiently producing an optically active N-protected-octahydro-1H-indole-2-carboxylic acid denoted by the formula (2): by using an enzyme capable of asymmetrically hydrolyzing...
10/21/2008
7429611Indole inhibitors of 15-lipoxygenase
The present invention provides indole inhibitors of 15-LO, pharmaceutical compositions containing such inhibitors and methods for treating diseases related to the 15-LO cascade using such compounds and compositions. ...
09/30/2008
7410995N-linked sulfonamide of heterocyclic thioesters for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using N-linked sulfonamides of heterocyclic thioesters. ...
08/12/2008
74053063-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics
The invention discloses and claims therapeutic uses of compounds of general formula (I) Wherein X, R1, R2 and R3 are as described herein. The invention further discloses processes for prepar...
07/29/2008
74026823-heteroaryl-3,5-dihydro-4-oxo-4-pyridazino[4,5-B]indole-1-carboxamide derivatives, their preparation and therapeutic use
A subject-matter of the invention is the compounds of general formula (I) in which X represents a hydrogen or halogen atom; R1 represents a hydrogen atom or a (C1-C4)alkyl group; R2
07/22/2008
7402604Positive modulators of nicotinic receptor agonists
Compounds according to formula I: wherein R1, W, R2, R3, X, R4 and R5 are as described in the specification, enantiomers thereof, pharmaceutically acceptable salts ther...
07/22/2008
7396940Combinatorial library of 3-aryl-1H-indole-2-carboxylic acid
Combinatorial libraries that contains various different 4, 5 fused 3-substituted-2-pyrrolocarboxylic acids for screening pharmacological activity and methods of synthesizing said libraries. ...
07/08/2008
7384945Indole or benzimidazole derivatives as CB1 inverse agonists
Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound...
06/10/2008
7368471Substituted indole acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
This invention provides compounds of the formula: wherein: X is a chemical bond, —CH2— or —C(O)—; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, ...
05/06/2008
73650612-Amino-3-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia...
04/29/2008
7361670Amide derivatives as NMDA receptor antagonists
Compounds having NR2B selective NMDA receptor antagonist activity are disclosed of the formula (I) wherein one of the neighboring R1, R2, R3
04/22/2008
7358373Cathepsin K inhibitors
The present invention provides a compound of the Formula: a pharmaceutically acceptable salt, a solvate, or a prodrug thereof, wherein m, n, Ar1, R1, R2, R3, R4, and R
04/15/2008
7351726Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
04/01/2008
7351730Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8,...
04/01/2008
7348351Substituted 3-alkyl and 3-arylalkyl -indol-1yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
The invention formula substituted 3-alkyl and 3-arylalkyl 1H indol-1yl acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure ...
03/25/2008
7348355Triamide-substituted heterobicyclic compounds
The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for prep...
03/25/2008
7345068Aromatic amino acid derivatives and medicinal compositions
1. An aromatic amino acid derivative represented by the formula (I) or its pharmacologically acceptable salt: wherein, R1 is a hydrogen atom or an amino-protecting group, ...
03/18/2008
7342039Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them. ...
03/11/2008
7338976Heterocyclic esters or amides for vision and memory disorders
This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic esters and amides. ...
03/04/2008
7332521Substituted indoles
The present invention relates generally to substituted indoles such as substituted 1H-indole-2-carboxylic acid derivatives, and methods of using them. ...
02/19/2008
7326794Process for the preparation of high purity perindopril and intermediates useful in the synthesis
The invention relates to 1-{2(S)-[1(S)-(ethoxycarbonyl)butylamino]propionyl}-(3aS,7aS)octahydroindol-2(S)-carboxylic acid of the Formula I and the t-butylamine salt of the Formula I′ thereof free of contaminations derivable from dicyclohexyl carbodiimide, and a pr...
02/05/2008
7323575Process for the synthesis of (2S)-indoline-2-carboxylic acid
Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): Application in the synthesis of perindopril and its pharmaceutically acceptable salts. ...
01/29/2008
7291745Process for the preparation of perindopril
A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula II...
11/06/2007
7288661Process for the synthesis of (2S,3aS,7aS)-1-[(S)-alanyl]-octahydro-1-indole-2-carboxylic acid compounds and application in the synthesis of perindopril
Process for the synthesis of compounds of formula (I): wherein R represents a hydrogen atom or a protecting group for the amino function. Application in the synthesis of perindopril and pharmaceutically a...
10/30/2007
7268159Substituted indoles
The present invention relates generally to substituted indoles and methods of using them. ...
09/11/2007
7265150Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds for vision and memory disorders
This invention relates to novel compositions and uses of N-heterocyclic carboxylic acids and carboxylic acid isosteres for treating a vision disorder, improving vision, treating memory impairment or enhancing memory performance in an animal. ...
09/04/2007
7265148Substituted pyrrole-indoles
The present invention relates generally to substituted pyrrole-indoles such as substituted pyrrole-indoles, and methods of using them. ...
09/04/2007
7259182Aryl, aryloxy, and aklyloxy substituted 1-indol-3-yl glyoxylic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula I are provided: wherein: R1, R2, and R3, are as defined herein, as well as pharmaceutical composition and methods using the compounds as inhibitors of plasminogen activator inhibitor ...
08/21/2007
7259181β crystalline form of perindopril tert-butylamine salt
A β crystalline form of the compound of formula (I): characterized by its powder X-ray diffraction data. Medicinal products containing the same which are useful as inhibitors of angiotensin I converting ...
08/21/2007
7232817α- and β-amino acid hydroxyethlamino sulfonyl urea derivatives useful as retroviral protease inhibitors
α- and β-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. ...
06/19/2007
72269422-amino-4-functionalized tetralin derivatives and related glycogen phosphorylase inhibitors
Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia...
06/05/2007
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