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Class 548/516 - Two double bonds between ring members of the five-membered hetero ring (e.g., 4,5,6,7-tetrahydroindoles, etc.)


Subclass of Class 548 - Organic compounds -- part of the class 532-570 series
Definition: Compounds wherein there are two double bonds between ring
No. of patents: 84
Last issue date: 05/12/2009


1      
NumberTitleIssue Date
7531672Preparation of heterocyclic ketones
The present invention relates to a process for preparing heterocyclic ketones of the formulae (I) and (la), by reacting a heterocyclic compound of the formula (II), with an α, β-unsaturated carboxylic acid of the formula (III), or with its anhydride of the formula...
05/12/2009
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
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
7351726Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
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
7342039Substituted indole oximes
The present invention relates to substituted indole oximes and methods of using them. ...
03/11/2008
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
7268159Substituted indoles
The present invention relates generally to substituted indoles and methods of using them. ...
09/11/2007
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
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
72237862-aminonaphthalene 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...
05/29/2007
72147042-Amino-1-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...
05/08/2007
7199148Broadspectrum substituted oxindole sulfonamide HIV protease inhibitors
The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are ...
04/03/2007
7186749Pyrrolo-naphthyl acids and methods for using them
The present invention relates to pyrrolo-naphthyl compounds of the formula and methods of using them to modulate PAI-1 expression and to treat PAI-1 related disorders. ...
03/06/2007
7163954Substituted naphthyl benzothiophene acids
The present invention relates generally to substituted naphthyl benzothiophene acids and methods of using them. ...
01/16/2007
7141592Substituted oxadiazolidinediones
The present invention relates generally to substituted oxadiazolidinediones and methods of using them. ...
11/28/2006
7109351Fused pyrrolecarboxamides; GABA brain receptor ligands
Substituted pyrrolecarboxamide compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors ...
09/19/2006
7101903Substituted dihydropyrano indole-3,4-dione derivatives as inhibitiors of plasminogen activator inhibitor-1 (PAI-1)
Compounds of formula (I) and II) are provided wherein: X is an alkali metal or a basic amine moiety; R1 is alkyl, cycloalkyl, —CH2-cycloalkyl, pyridinyl, —CH2-pyridinyl, pheny...
09/05/2006
7078429Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1)
Substituted 3-carbonyl-1H-indol-1-yl acetic acid derivatives of formula I are provided: wherein: R1, R2, R3, R4 and R5 are as defined herein which are useful a...
07/18/2006
7078535Method for the production of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1h-pyrrolizin-5-ylacetic acid
The invention relates to a process for the preparation of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-ylacetic acid, in which 5-benzyl-3,3-dimethyl-3,4-dihydro-2H-pyrrole is reacted with ω-bromo-4-chloroacetophenone with formation of 6-(4-c...
07/18/2006
7074817Substituted 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-pyridi...
07/11/2006
6936632Fused pyrrole compounds, pharmaceutical agents containing the same, and the use thereof
The present invention relates to fused pyrrole compounds of the formula 1. in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl. These compounds are in particular pyrrolizines, indol...
08/30/2005
6930190Process for the preparation of heterocyclic pentalene derivatives
A process for preparing heterocyclic pentalene derivative having formula (I): wherein w is a sulfur atom (S), an oxygen atom (O) or a NR or PR group, wherein R is an hydrocarbon group; R1, R2, R3, and R4, equal to or diffe...
08/16/2005
6878738Anti-inflammatory oxo derivatives and hydroxy derivatives of pyrrolizines, and their pharmaceutical use
The present invention relates to compounds of the formula I in which one of the radicals R8 and R9 is a hydrogen atom or an alkyl group and the other is hydroxyl, alkoxy or acyloxy or where R8 and R9, together with the...
04/12/2005
6559319Synthesis of compounds useful in the manufacture of ketorolac
A multi-step method of synthesizing ketorolac, an analgesic compound, is shown. Several of the reactions and intermediate compounds are novel. The reaction sequence begins with the known compound N-2-bromoethylpyrrole....
05/06/2003
6548532Indolecarboxylic compounds for treating seborrhea and complications thereof
Indolecarboxylic acid compounds and derivatives thereof are useful for treating seboarhea and the dermatitides associated therewith, especially acne and/or blackheads and/or comedones....
04/15/2003
6541507Indolecarboxylic compounds for inducing/stimulating hair growth and/or retarding hair loss
Indolecarboxylic acid compounds and derivatives thereof, notably 4,6-dimethoxyindole-2-carboxylic acid and derivatives thereof, are especially useful for inducing/stimulating mammalian hair growth and/or preventing/retarding mammalian hair loss....
04/01/2003
64482431,4-substituted cyclic amine derivatives
A novel 1,4-substituted cyclic amine derivative represented by the following formula or a pharmacologically acceptable salt thereof: ##STR1## (wherein A, B, C, D, T, Y and Z represent each methine or nitrogen; R1, R2, R3, ...
09/10/2002
6433199Quinone derivatives
The invention relates to a quinone derivative of the following formula: ##STR1## which is capable of converting into two alkylating agents upon bioreduction. Substituents A, B, C, and D are as described herein....
08/13/2002
6417371Process for preparing 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1H-pyrrolizin-5-yl-ac etic acid
The present invention relates to a process process for the preparation of the compound of the formula I ##STR1## where the compound of the formula III ##STR2## is reacted with oxalyl chloride and the product obtained is treated with hydrazine and an ...
07/09/2002
6395766Tetrahydroindolone derivatives as gabaaalpha5 ligands for enhancing cognition
Compounds according to Formula (I) or a pharmaceutically acceptable salt thereof are GABA-A Alpha 5 ligands useful for enhancing cognition: ##STR1## where A is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloa...
05/28/2002
6391917Dialkyl ureas as calcitonin mimetics
Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the de...
05/21/2002
6376489Cyclic AMP-specific phosphodiesterase inhibitors
Novel compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory disease and other diseases involving elevated levels of cytokines, as well as cen...
04/23/2002
6353109Certain fused pyrrolecarboxamides; a new class of GABA brain receptor
Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alky...
03/05/2002
6323344Preparation of ketorolac
5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula ##STR1## where R1 is alkyl and R2 is optionally substituted phenyl; and the method for their preparation and their conversion to ketorolac and its pharmaceutically ac...
11/27/2001
6291507Chemical compounds
A pharmaceutical composition which comprises a compound of formula (I) ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1, and wherein A and B form an optionally substituted ...
09/18/2001
6255351Dialkyl ureas as calcitonin mimetics
Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the de...
07/03/2001
6218419Aminoiminoquinone and aminoquinone alkaloid compounds and methods of use
The subject application concerns novel compounds with useful biological properties. For example, these compounds can be used as antinflammatory, anti-proliferative, immunomodulatory, and/or neuroprotective agents. Specific examples of the compounds of the...
04/17/2001
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