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| Number | Title | Issue Date |
| 7973161 | Apoptosis promoters Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an ant... | 07/05/2011 |
| 7579467 | -phenyl-2-pyrimidine-amine derivatives The present invention relates to novel amides and a process for preparing these amides. ... | 08/25/2009 |
| 7407959 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 08/05/2008 |
| 7375134 | Cathepsin cysteine protease inhibitors This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, s... | 05/20/2008 |
| 7371747 | Cyanoalkylamino derivatives as protease inhibitors The present invention is directed to novel cyanoalkylamino derivatives that are inhibitors of cysteine protease such as cathepsins K, S, B and L, in particular cathepsin K Pharmaceutical composition comprising these compounds, method of treating diseases mediated by... | 05/13/2008 |
| 7300936 | α-(N-sulfonamido)acetamide derivatives as β-amyloid inhibitors There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptid... | 11/27/2007 |
| 7291621 | Substituted biaryl amides C5a receptor modulators Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5... | 11/06/2007 |
| 7271289 | Biphenylcarboxylic amide derivatives as p38 kinase inhibitors Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors. ... | 09/18/2007 |
| 7244441 | Stents and intra-luminal prostheses containing map kinase inhibitors A coated stent or intra-luminal prosthesis containing a MAP kinase inhibitor controls, reduces, or prevents restenosis, inflammation, and complications associated with stent or intra-luminal prosthesis implantation and/or cardiovascular disease. ... | 07/17/2007 |
| 7238693 | Aryl carbamate derivatives, preparation and use thereof The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal heal... | 07/03/2007 |
| 7223760 | Substituted triazole compounds Novel substituted triazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors. ... | 05/29/2007 |
| 7214680 | 2-substituted 1-arylpiperazines as tachykinin antagonists and/or serotonin reuptake inhibitors The present invention relates to piperazine of formula (I) wherein R represents halogen, C1-4 alkyl, trifluoromethoxy or trifluoromethyl; R1 is trifluoromethyl, C | 05/08/2007 |
| 7208629 | 5′-Carbamoyl-1,1-biphenyl-4-carboxamide derivatives and their use as p38 kinase inhibitors Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1–6alkyl, C3–7cycloalkyl, C2–6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1–6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, â€... | 04/24/2007 |
| 7189733 | Compositions and methods for inhibiting TGF-β This invention provides compounds that are useful for treating patients having a TGF-β-mediated disease, particularly an ALK5-mediated disease. The compounds are represented by formula I: wherein: a-b is CH... | 03/13/2007 |
| 7153858 | Arylpiperazinyl compounds The invention relates to 5-HT receptor agonists or antagonists. Novel arylpiperazinyl sulfonamide compounds represented by Formulae I: and II, and synthesis and uses of those compounds for treating diseases including those mediated directly or indirectly by 5-HT rec... | 12/26/2006 |
| 7148225 | Substituted biaryl amides as C5A receptor modulators Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in... | 12/12/2006 |
| 7125997 | Differential tumor cytotoxicity compounds and compositions The invention is directed to novel biaryl derivatives, to the uses of these compounds in various medicinal applications, including the treatment, prevention and control of proliferative diseases such as tumors, and to pharmaceutical compositions comprising these com... | 10/24/2006 |
| 7078404 | Acyl-3-carboxyphenylurea derivatives, processes for preparing them and their use The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives. The invention relates to compounds of formula I, in wh... | 07/18/2006 |
| 7056922 | Acylamino cyclopropane derivatives A compound of the formula wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R1, R2, R3, R4, R5, R6 R7 are as defined... | 06/06/2006 |
| 7026323 | Platelet adenosine diphosphate receptor antagonists Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmace... | 04/11/2006 |
| 6969713 | Piperidine and piperazine acetamide derivatives The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy | 11/29/2005 |
| 6906073 | Piperazine CCR-3 receptor antagonists The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions co... | 06/14/2005 |
| 6903120 | Modulators of dopamine neurotransmission New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, O... | 06/07/2005 |
| 6894053 | Serotonergic agents with long-acting in vivo effects Compounds of the formula have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT1A system, such as schizophrenia and other ... | 05/17/2005 |
| 6894052 | Diarylalkylpiperazines active on the lower urinary tract Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compound... | 05/17/2005 |
| 6887876 | Benzamidine derivatives Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psy... | 05/03/2005 |
| 6831080 | Cinnamide derivatives as KCNQ potassium channel modulators There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-ben... | 12/14/2004 |
| 6784183 | Diphenylurea compounds Compounds of formula (I): and medicinal products containing the same which are useful as dual α2/5-HT2c antagonists. ... | 08/31/2004 |
| 6777414 | Nitrogen-containing heterocyclic compounds and benamide compounds and drugs containing the same Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitor... | 08/17/2004 |
| 6770644 | Hydroxamic acid derivatives, process for the production thereof and drug containing the same as the active ingredient Hydroxamic acid derivatives of the formula (I) (wherein all the symbols have the same meaning as defined in the specification.), non-toxic salt thereof or prodrugs thereof. The compounds of the formula (I) ... | 08/03/2004 |
| 6696450 | Serotonergic agents with long-acting in vivo effects Compounds of the formula ##STR1## have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT1A system, such as schizophrenia and other psychotic disorders such as ... | 02/24/2004 |
| 6686360 | N-benzylpiperazine compounds The present invention relates to a compound selected from those of formula (I): ##STR1## wherein: R1 represents alkyl, R2 represents hydroxy, alkoxy, or amino, n represents an integer from 1 to 12 inclusive, R3 represents: hydr... | 02/03/2004 |
| 6680321 | Compounds with analgesic effect Compounds of the formula (I) ##STR1## as well as their pharmaceutically acceptable salts, and pharmaceutical compositions comprising the novel compounds. The novel compounds of the formula (I) are useful in the management of pain.... | 01/20/2004 |
| 6642239 | Dipeptide nitrile cathepsin K inhibitors Dipeptide nitrile Cathepsin K inhibitors of formula I, and pharmaceutically acceptable salts or esters thereof: ##STR1## In which R1 and R2 are independently H or C1 -C7 lower alkyl, or R1 and R | 11/04/2003 |
| 6596866 | Process for the preparation of nefazodone hydrochloride A process for the preparation of Nefazodone hydrochloride comprising direct conversion of semicarbazide dihydrochloride 3 into Nefazodone hydrochloride which process involves a reaction of triethyl orthopropionate in the presence of trimethylsilylchloride... | 07/22/2003 |
| 6593474 | Arylsubstituted piperazines useful in the treatment of benign prostatic hyperplasia This invention relates to a series of arylsubstituted piperazines, of Formula I ##STR1## pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the ³... | 07/15/2003 |
| 6579870 | Bis-arylsulfones The present invention provides pharmaceutically active compounds useful for the treatment of diseases or disorders of the central nervous system.... | 06/17/2003 |
| 6569861 | Melanin concentrating hormone receptor ligands Disclosed are compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12 -R19 are defined herein. These compounds are selective modulators of MCH 1 rec... | 05/27/2003 |
| 6555541 | Substituted phenyl compounds with immunosuppressing activity and pharmaceutical compositions The invention provides substituted phenyl compounds of general formula ##STR1## wherein R1, T, U and Ar are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing t... | 04/29/2003 |
| 6552022 | Benzamide derivatives and their use as ApoB-100 secretion inhibitors The invention relates to therapeutic benzamide compounds of formula (I) ##STR1## wherein A, X, Z, R1, Y, R2, R3, are as defined herein, and physiologically acceptable salts, solvates or derivatives thereof. The present inv... | 04/22/2003 |