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Class 514/254.08 - Polycyclo ring system having the additional five-membered nitrogen hetero ring as one of the cyclos


Subclass of Class 514 - Drug, bio-affecting and body treating compositions
Definition: Subject matter wherein the five-membered hetero ring is
No. of patents: 158
Last issue date: 02/21/2012


1        
NumberTitleIssue Date
81196411H-furo[3,2-C]pyrazole compounds useful as kinase inhibitors
Furo[3,2-c]pyrazole derivatives of formula (I) as defined in the description, and pharmaceutically acceptable salts thereof, wherein A is an aryl or heteroaryl ring, —NHZR5 is at the ortho position to the CONH linker; —R1 and R2 ...
02/21/2012
8053437Furo[3. 2-B] pyrrol derivatives
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optional...
11/08/2011
80394742,3,4,9-tetrahydro-1-carbazole derivatives as CRTH2 receptor antagonists
The invention relates to novel tetrahydro-1H-carbazole derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceut...
10/18/2011
7846935Furo[3,2-B]pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optio...
12/07/2010
7846934Furo[3,2-B] pyrrol-3-one derivatives and their use as cysteinyl proteinase inhibitors
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substitut...
12/07/2010
7803803Tetrahydrofuro[3,2-B] pyrrol-3-ones as cathepsin K inhibitors
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; one of R1 and R2 is H, and the other is select...
09/28/2010
7737150Furo[3, 2-b] pyrrol derivatives
The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is tert-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optional...
06/15/2010
7456183Guanidino compounds
Compounds having the general structure I are provided. X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R...
11/25/2008
7297711Arylalkyl indoles having serotonin receptor affinity useful as therapeutic agents, process for their preparation and pharmaceutical compositions containing them
The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel interm...
11/20/2007
72561883-aminoalkyl-2-aryl-indole derivatives and their use as GnRH antagonists
The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicam...
08/14/2007
7238695Imidazolyl derivatives
The present invention is directed to imidazolyl derivatives or pharmaceutically acceptable salts thereof which are useful as agonists or antagonists of somatostatin receptors, having the following formula (I), wh...
07/03/2007
72237654-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives
The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bo...
05/29/2007
7153848Inhibitors of HCV replication
Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing ...
12/26/2006
7144883Bicyclic sulfonamide compounds
The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obe...
12/05/2006
7141568Pyrrolo[3,4-c]pyrazole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
Pyrrolo[3,4-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be usefu...
11/28/2006
7091229Tricyclic lactam and sultam derivatives and their use as histone deacetylase inhibitors
A compound of formula (I) wherein A and B are optionally substituted cyclohexenyl or phenyl groups, X is carbonyl or sulfonyl, and Y is 5–7 atoms-linker, is useful as histone deacetylase inhibitors, particularl...
08/15/2006
70747964-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives
The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W i...
07/11/2006
7074782Carbamate caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; Y is an electron...
07/11/2006
7005439Compounds
The invention provides compounds of general formula (I) wherein m, n, Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the specification, process...
02/28/2006
6998403Benzoindoline compounds
A compound of formula (I): wherein: R1 and R2 together form a benzo ring optionally substituted by halogen or by alkyl, alkoxy, cyano, nitro, hydroxy, amin...
02/14/2006
6953801Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues
Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors i...
10/11/2005
6951874Compounds
The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions contai...
10/04/2005
6916822Phenoxyalkylamine derivatives useful as opioid δ receptor agonists
A medicament useful for preventive and/or therapeutic treatment of nerve system diseases which comprises, as an active ingredient, a compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof:
07/12/2005
6916812Alpha-aminoamide derivatives as melanocortin agonists
Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present inven...
07/12/2005
69140641,4-Disubstituted piperazine derivatives useful as uro-selective α1-adrenoceptor blockers
The present invention relates to a novel 1,4-disubstituted piperazine derivatives of Formula I, and their pharmaceutically acceptable acid addition salts having excellent uro-selective α1-adrenoceptor antag...
07/05/2005
6903085Substituted piperidine compounds useful as modulators of chemokine receptor activity
The invention provides compounds of formula (I) wherein R1, R2, R3, R6, Z, Q, m, n, X1, X2, X3, X4 and T are as defined in the specification, processes for their preparation, pha...
06/07/2005
6890921Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia
This invention relates to a series of arylsubstituted piperazines, of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibi...
05/10/2005
6861432Piperazine derivatives that destabilize androgen receptors
This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R′, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the inventio...
03/01/2005
6852725Imidazolyl derivatives
The present invention is directed to imidazolyl derivatives of the formula: where the substituents are defined in the specification, or a pharmaceutically acceptable salt thereof. The derivatives bind selectively to th...
02/08/2005
6849631Semicarbazides and their uses
The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I): that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the ca...
02/01/2005
68415523a,4,5,9b-tetrahydro-1H-benz[e]indol-2-yl amine-derived neuropeptide Y receptors ligands useful in the treatment of obesity and other disorders
Compounds of the formula: are disclosed as ligands for neuropeptide Y receptors and as such are useful in the treatment of obesity and disorders of the central nervous system. ...
01/11/2005
6784183Diphenylurea compounds
Compounds of formula (I): and medicinal products containing the same which are useful as dual α2/5-HT2c antagonists. ...
08/31/2004
6740636Non-peptide CCR1 receptor antagonists in combination with cyclosporin A for the treatment of heart transplant rejection
This invention is directed to pharmaceutical compositions useful in treating heart transplant rejection in mammals comprising a pharmaceutically acceptable excipient, a therapeutically effective amount of a non-peptide CCR1 receptor antagonist and a sub-nephrotoxic ...
05/25/2004
6713473Tricyclic compounds
A compound represented by the formula (I) [A represents a 5- to 7-membered hydrocarbon ring group; L represents —NR3—CO—, —CO—NR3— and the like (R3 represents a hydrogen atom, a lower alkyl group, a lower acyl group and t...
03/30/2004
6689784Carbamate caspase inhibitors and uses thereof
This invention provides caspase inhibitors of formula I: ##STR1## wherein Z is oxygen or sulfur; R1 is hydrogen, --CHN2, R, CH2 OR, CH2 SR, or --CH2 Y; Y is an electronegative leaving group; R2
02/10/2004
6676931Buccal, polar and non-polar spray or capsule
Buccal aerosol sprays or capsule using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the in...
01/13/2004
6664258Spirocyclic dopamine receptor subtype ligands
This invention relates to novel, pharmaceutically active compounds of formula (I) wherein a, b and R1 through R6 are as defined in the specification ##STR1## These compounds exhibit central dopaminergic activity and are useful in the...
12/16/2003
6555537Piperazine derivatives and their use as anti-inflammatory agents
This invention is directed to acyl piperazine derivatives, for example, of the following formula (Ia): ##STR1## wherein R1a, R2, R3, R4, R5, and R6 are described herein. These derivatives a...
04/29/2003
6498251Tetrahydrobenzindole derivatives
Compounds containing tetrahydrobenzindole which bind to serotonin receptor and are useful in treatment or prevention of disease induced by abnormality of central peripheral serotonin controlling functions....
12/24/2002
6407112Optically active tetrahydrobenzindole derivative
Optically active tetrahydrobenzindole type compounds having affinity for a 5-HT receptor, useful for prevention and treatment of mental diseases. A species compound is (S)-2a-4-(4-(2-methoxyphenyl)piperazinyl)butyl)-2a,3,4,5,-tetrahydro 1 H-benz[cd]i...
06/18/2002
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