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Class 546/187 - Additional hetero ring containing


Subclass of Class 546 - Organic compounds -- part of the class 532-570 series
Definition: Compounds which contain an additional hetero ring.
No. of patents: 712
Last issue date: 05/29/2012


1                      
NumberTitleIssue Date
8188287Piperidyl acrylamide antagonists of CCR2
The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5 and X are as defined in the specification. The invention also comprises a method of ...
05/29/2012
8119809AMPK-activating heterocycloalkyloxy(hetero)aryl carboxamide, sulfonamide and amine compounds and methods for using the same
Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, ...
02/21/2012
8017783Biphenyl compounds useful as muscarinic receptor antagonists
This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as define...
09/13/2011
7897775Crystalline form of a benzimidazole-carboxamide medicinal compound
The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention a...
03/01/2011
7868175Biphenyl compounds useful as muscarinic receptor antagonists
The invention provides compounds of formula I: wherein a, b, c, d, n, R1, R2, R3, R6, R7, W, and A are as defined in the specification. The compounds of formula I are m...
01/11/2011
7723527Benzoimidazole compounds
Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions. ...
05/25/2010
7723526Benzoimidazole compounds
Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions. ...
05/25/2010
7652142Bipiperidinyl derivatives useful as inhibitors of chemokine receptors
In its many embodiments, the present invention provides a novel class of bipiperidinyl compounds as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmac...
01/26/2010
7638631Methylene dipiperidine derivatives
The present invention relates to novel methylene dipiperidine derivatives having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of neurological and psychiatric disorders. ...
12/29/2009
7632949Process for the preparation of stabilizers for polymers
The instant invention relates to a process for the preparation of stabilizers for polymers, especially for polyamides, by condensation of isophthalic acic dichloride (IPC) with sterically hindered amines of the type tetraalkylpiperidine. By using organic solvents or...
12/15/2009
7622587Crystalline form of a benzimidazole-carboxamide medicinal compound
The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention a...
11/24/2009
73880955-substituted indole-2-carboxamide derivatives
The present invention relates to compounds of formula I wherein R1 to R4 and G are as defined in the description and claims and pharmaceutically acceptable salts thereof. The compounds are useful for t...
06/17/2008
7384948Piperidine derivatives useful as CCR5 antagonists
The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined i...
06/10/2008
73717461,2,4-Thiadiazole compounds and pests controlling composition containing the same
The present invention relates to a 1,2,4-thiadiazole compound of the formula (I) represented by the formula (1): wherein R1? represents C3-C7 alkynyl and X represents C4-C7 straight alkylene optionally substituted with one to four of R2?, C4-C7 straight alkenylene o...
05/13/2008
7361682Indole derivatives as H3 inverse agonists
The present invention relates to compounds of formula I: wherein X, R1, R2, R3, R4 and R5 are as defined in the description and claims, and pharmaceutically acceptable ...
04/22/2008
7361755Transition-metal-catalyzed process for the conversion of alkenes to sterically hindered substituted n-alkoxyamines
This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical. ...
04/22/2008
7348324Cyclic amine compounds as CCR5 antagonists
A compound of formula (I) (wherein R1 is a hydrogen atom, a hydrocarbon group which may be substituted, a non-aromatic heterocyclic group which may be substituted, R2 is a hydrocarbon group which may be substituted, a non-aromatic heterocyclic ...
03/25/2008
7342020Arylpiperazines and their use as metalloproteinase inhibiting agents (MMP)
Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13 ...
03/11/2008
7312222Heterocyclic piperidines as modulators of chemokine receptor activity
The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases. ...
12/25/2007
7307090Piperidine derivatives useful as modulators of chemokine receptor activity
The invention provides a compound of formula (I), wherein: T is C(O) or S(O)2; W is C(O) or S(O)2; X is CH2, O or NH; Y is CR5 or N; R1 is optionally substituted aryl or optionally substituted heterocyclyl; R
12/11/2007
7300941Non-imidazole compounds
Disclosed are novel compounds of the formula Also disclosed are pharmaceutical compositions comprising the compounds of Formula I. Also disclosed are methods of treating various diseases or conditions, such ...
11/27/2007
7297693Nitrogen-containing heterocyclic compounds and their use as Raf inhibitors
Compounds and their use as pharmaceuticals particularly as Raf kinase inhibitors for the treatment of neurotraumatic diseases, cancer, chronic neurodegeneration, pain, migraine and cardiac hypertrophy. ...
11/20/2007
7297706Certain glycine derivatives as factor Xa inhibitors for use in the treatment of thrombotic disorders
Compounds of formula (I) in which R, R1, R2, n and X1 have the meanings given in the specification are Factor Xa inhibitors useful in the treatment of thrombotic disorders. ...
11/20/2007
7282507Indole derivatives as selective androgen receptor modulators (SARMS)
The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. ...
10/16/2007
7279471Selected CGRP-antagonists, process for preparing them and their use as pharmaceutical compositions
The present invention relates to the CGRP antagonists of general formula wherein A and R1 to R3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the hydra...
10/09/2007
7279490Ophthalmic compositions for treating ocular hypertension
This invention relates to selective m1 muscarinic agonist, their use or a formulation thereof in the treatment of glaucoma and/or other conditions which are related to elevated intraocular pressure in the eye of a patient. This invention also relates to the use of s...
10/09/2007
7279491Phenylpiperidines and phenylpyrrolidines
Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions. ...
10/09/2007
7276609Process for preparing 4-(hydroxy)-[1,4′]bipiperidinyl-l'carboxylic acid tert-butyl ester
The present invention concerns a process for preparing 4-(hydroxy)-[1,4′]bipiperidinyl-1′-carboxylic acid tert-butyl ester, comprising hydrogenating a mixture of 4-hydroxypiperidine and 1-tert-butoxycarbonyl-4-piperidone in a suitable solvent, in the presence of...
10/02/2007
7262206Cycloalkyl—containing 5-acylindolinones, the preparation thereof and their use as medicaments
The present invention relates to cycloalkyl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined as in claims 1 to 6, the tautomers, the enantiomers, th...
08/28/2007
7256294Crystalline form of a benzimidazole-carboxamide medicinal compound
The invention provides crystalline forms of the novel benzimidazole-carboxamide 5-HT4 receptor agonist compound, 4-(4-{[(2-isopropyl-1H-benzoimidazole-4-carbonyl)amino]methyl}-piperidin-1-ylmethyl)piperidine-1-carboxylic acid methyl ester. The invention a...
08/14/2007
7244847Benzimidazole compounds
The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods...
07/17/2007
7241745Pyridyl alkene and pyridyl alkine acid amides as cytostatics and immunosupressives
The invention relates to a new pyridyl alkene and pyridyl alkine acid amides according to the general formula (I) as well as methods for their production, medicaments containing these compounds as well as their m...
07/10/2007
7235584Non-psychotropic cannabinoids
Novel non-psychotropic cannabinoids are disclosed and pharmaceutical compositions comprising these novel compounds are described for preventing neurotoxicity, neuroinflammation, immune or inflammatory disorders comprising as active ingredient the stereospecific (+) ...
06/26/2007
7223759Antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds
The invention relates to antibacterial 3,5-diaminopiperidine-substituted aromatic and heteroaromatic compounds and pharmaceutical compositions thereof. This invention also relates to a method of using such compounds in the treatment of bacterial infections in mammal...
05/29/2007
7220745Heterocyclic compounds useful to treat HCV
The present invention relates to substituted diphenyl heterocycle compounds and pharmaceutical compositions thereof that inhibit replication of HCV virus. The present invention also relates to the use of the compounds and/or compositions to inhibit HCV replication a...
05/22/2007
RE39608Substituted benzimidazoles and their use as PARP inhibitors
Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, p...
05/01/2007
7205294Selected CGRP-antagonists process for preparing them and their use as pharmaceutical compositions
The present invention relates to substituted piperidines of general formula wherein A, B, D, E, X, R1 and R2 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the...
04/17/2007
7192973Piperidine derivatives and their use as modulators of chemokine receptor activity (especially CCR5)
Compounds of formula (I): wherein L is CH or N; M is CH or N; provided that L and M are not both CH; compositions comprising them, processes for preparing them and their use in medical therapy (for example modulating CCR5 receptor activity in a warm blooded animal)
03/20/2007
7186724Heterocyclic substituted carbonyl derivatives and their use as dopamine Dreceptor ligands
The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine...
03/06/2007
7183274Piperidine-2,6-diones heterocyclically substituted in the 3-position
Piperidine-2,6-diones heterocyclically substituted in the 3-position corresponding to formula I Also the production and use of such compounds in pharmaceutical formulations and related methods of treatment. ...
02/27/2007
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