Polycyclo Ring System Which Contains The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/211.09)
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Publication number: 20090075973Abstract: The present invention provides benzo-fused heterocyclic compounds having the structure of formula I, as well as prodrugs, stereoisomers, racemates, salts, hydrates, solvates, acid salt hydrates and isomorphic crystalline forms thereof. The compounds directly or indirectly modulate the activity of one or more cannabinoid receptors and can be incorporated into pharmaceutical preparations that are useful for the prevention and treatment of a variety of diseases and conditions, including pain, inflammation and pruritis.Type: ApplicationFiled: September 10, 2008Publication date: March 19, 2009Applicant: CARA THERAPEUTICS, INC.Inventors: Jason S. Newcom, Carla M. Gauss, Gary R. Gustafson
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Publication number: 20090054400Abstract: The present invention provides new progesterone receptor modulators which are dibenzo[b,f]pyrido[1,2-d]oxazepine-2-amines or dibenzo[b,f]prido[1,2-d]thiazepine-2-amines, and uses thereof.Type: ApplicationFiled: May 6, 2008Publication date: February 26, 2009Inventors: Johannes Bernardus Maria Rewinkel, Brigitte Johanna Bernita Folmer, Maria Lourdes Ollero, Hemen Ibrahim
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Publication number: 20090048177Abstract: The invention features methods of treating mood disorders, such as manic disorders, and stabilizing moods by administering a kappa agonist or partial agonist to a subject in need thereof.Type: ApplicationFiled: August 27, 2008Publication date: February 19, 2009Applicant: The McLean Hospital CorporationInventors: Bruce M. Cohen, Beth L. Murphy
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Patent number: 7491714Abstract: Quinoline and naphthridine derivatives useful in the treatment of bacterial infections in mammals, particularly humans.Type: GrantFiled: December 3, 2003Date of Patent: February 17, 2009Assignee: Glaxo Group LimitedInventors: Jeffrey Michael Axten, Catherine Genevieve Yvette Dartois, Guy Marguerite Marie Gerard Nadler, Neil David Pearson
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Publication number: 20090029965Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: August 24, 2005Publication date: January 29, 2009Applicant: Ferring B.V.Inventors: Andrzej Roman Batt, Martin Lee Stockley, Michael Bryan Roe, Celine Marguerite Simone Heeney, Andrew John Baxter, Peter Hudson, Rachel Handy
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Patent number: 7482337Abstract: Disclosed are substituted xanthines of general formula wherein R1 to R4 are defined hereinbelow, the tautomers, the stereoisomers, the mixtures thereof, the prodrugs thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: October 28, 2003Date of Patent: January 27, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Roland Maier, Michael Mark, Mohammad Tadayyon, Ralf R. H. Lotz
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Publication number: 20080305169Abstract: [Problems] The present invention provides pharmaceutical composition which is effective for the prophylaxis or treatment of pathology showing involvement of uric acid (hyperuricemia, gouty tophus, acute gout arthritis, chronic gout arthritis, gouty kidney, urolithiasis, renal function disorder, coronary arterial disease, ischemic heart disease and the like) and the like, and is superior in the time-course stability and dissolution property (disintegration property). [Solving Means] The pharmaceutical composition of the present invention is a pharmaceutical composition comprising a nitrogen-containing fused ring compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable additives, wherein the nitrogen-containing fused ring compound or a pharmaceutically acceptable salt thereof is not in contact with a basic additive: wherein each symbol is as described in the specification.Type: ApplicationFiled: May 24, 2007Publication date: December 11, 2008Applicant: Japan Tobacco Inc.Inventors: Kazuki Miki, Fuyuki Arimoto, Masaki Sunami
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Publication number: 20080293690Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: April 30, 2008Publication date: November 27, 2008Inventors: John M. Fevig, Dean A. Wacker
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Publication number: 20080269192Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)-group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: December 29, 2005Publication date: October 30, 2008Applicant: Coley Pharmaceutical Group, Inc.Inventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Publication number: 20080261951Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.Type: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
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Publication number: 20080242656Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) wherein R1 is —W-A1-W1-A2, W is —(CH2)m—X—(CH2)n—, wherein W1 is —(CH2)m1—X1—(CH2)n1—, m, m1, n and n1 are the same or different and each is 0 to 6, X and X1 are the same or different and each is a single bond, etc., A1 is an optionally substituted C3-14 hydrocarbon ring group, etc. and A2 is a substituted C3-14 hydrocarbon ring group etc.; R2 is —(CH2)r—CO—R8, etc., wherein r is 0 to 6 and R8 is a C1-6 alkoxy group, etc.; R3 and R4 are the same or different and each is a hydrogen atom, a C1-6 alkyl group, etc.; and R5 is —CO2R21, etc.; R30 and R31 are the same or different and each is a hydrogen atom, etc.; or a prodrug thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 19, 2007Publication date: October 2, 2008Inventors: Andrew M. Fryer, Makoto Shiozaki, Nicole M. Littmann, Takashi Inaba, Steven W. Andrews, Katsutaka Yasue, Ellen R. Laird, Masahiro Yokota, Julia Haas, Hiroto Imai, Katsuya Maeda, Yuichi Shinozaki, Yoshikazu Hori
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Publication number: 20080234250Abstract: The invention concerns compounds according to general formulae 1, wherein G1 is an amine. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents.Type: ApplicationFiled: August 18, 2005Publication date: September 25, 2008Inventor: Gary Robert William Pitt
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Patent number: 7419974Abstract: The present invention relates to the compounds of formula (I): in which A is a group of formula (a) or (b) in which R represents a hydrogen or halogen atom, an —S(O)z(C1-C4)alkyl group, an —NHSO2(C1-C4)alkyl group, an —SO2NH(C1-C4)alkyl group, an —NHSO2phenyl-(C1-C4)alkyl group or an —NHSO2phenyl group, said phenyl possibly being substituted with a halogen atom, with a (C1-C4)alkyl group or with a (C1-C4)alkoxy group; R1 represents a hydrogen atom or a (C1-C4)alkyl group, a —CO(C1-C4)alkyl group, a phenyl-(C1-C4)alkyl group or a —COphenyl group, said phenyl also possibly being substituted with a halogen atom or with a (C1-C4)alkoxy group; R2 is a hydrogen atom or an —SO2(C1-C4)alkyl group, an —SO2phenyl-(C1-C4)alkyl group or an —SO2phenyl group; X completes a ring of 5 to 8 atoms, said ring being saturated or unsaturated, possibly being substituted with one or two (C1-C4)alkyl groups and bearing one or two carbonyl groups; n, m and z are, independently, 0, 1 or 2; R3 represents a hydrogen or halogenType: GrantFiled: August 15, 2006Date of Patent: September 2, 2008Assignee: Sanofi-AventisInventors: Philippe R. Bovy, Roberto Cecchi, Gilles Courtemanche, Tiziano Croci, Ambrogio Oliva, Nunzia Viviani
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Publication number: 20080207592Abstract: The invention relates to the compound of the formula (A) and also to its physiologically acceptable salts. The compound is suitable as, for example, a hypolipidemic.Type: ApplicationFiled: January 7, 2008Publication date: August 28, 2008Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Wendelin FRICK, Heiner GLOMBIK, Hubert HEUER, Hans-Ludwig SCHAEFER, Stefan THEIS
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Publication number: 20080194539Abstract: The invention relates to annelated phenyl piperazine and phenyl diazepane carboxamides of general formula (I) containing oxygen. The compounds are suitable for medical use.Type: ApplicationFiled: December 27, 2005Publication date: August 14, 2008Applicant: Schwarz Pharma AGInventors: Peter Gmeiner, Harald Hubner, Karin Schlotter
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Patent number: 7410961Abstract: The present invention is further directed to compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R16, R17, R18, R19, R20, R21 and R22 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which chemokine receptors are involved.Type: GrantFiled: January 14, 2005Date of Patent: August 12, 2008Assignee: Merck & Co., Inc.Inventors: Lihu Yang, Sander G. Mills, Changyou Zhou, Stephen D. Goble, Alexander Pasternak
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Patent number: 7407950Abstract: The invention concerns compounds of general formula (I), wherein n, X1, X2, X3, X4, Z1, Z2, Z3, Z4, Z5 and W are as defined herein. Said compounds are ligands of the TRPV1 vanilloid receptor, and are therefore, useful for treating diseases associated with TRPV1 receptors, such as pain and inflammation.Type: GrantFiled: June 20, 2007Date of Patent: August 5, 2008Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Andre Malanda
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Patent number: 7390798Abstract: The present invention is directed to compounds of Formula I: I (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache.Type: GrantFiled: February 9, 2005Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
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Publication number: 20080113966Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: October 12, 2005Publication date: May 15, 2008Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
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Patent number: 7358238Abstract: The use of fused 1,2,4-triazoles for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions has been described. Also a novel class of fused 1,2,4-triazoles, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments has been described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: GrantFiled: October 11, 2005Date of Patent: April 15, 2008Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Inge Thoger Christensen, John Patrick Mogensen, Annette Rosendal Larsen
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Patent number: 7323455Abstract: This invention provides progesterone receptor modulators having the structure: wherein R1 to R7, X, and Q are as defined in the specification; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 22, 2005Date of Patent: January 29, 2008Assignee: WyethInventors: Puwen Zhang, Jay Edward Wrobel, Eugene Anthony Terefenko, Jeffrey Curtis Kern
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Patent number: 7320974Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are related to natural Latrunculin A or Latrunculin B. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with actin polymerization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or II, wherein said amount is effective to influence the cytoskeleton, for example by inhibiting actin polymerization.Type: GrantFiled: March 23, 2006Date of Patent: January 22, 2008Assignee: Inspire Pharmaceuticals, Inc.Inventors: John W. Lampe, Robert Plourde, Jr., Jin She, Jason L. Vittitow, Paul S. Watson, Michael T. Crimmins, David J. Slade
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Patent number: 7312208Abstract: Drugs useful for the treatment and prevention of hyperlipidemia, moreover drugs useful for the treatment and prevention of cholestasis-caused hepatopathy, particularly primary biliary cirrhosis and primary sclerosing cholangitis, and drugs for the treatment and prevention of obesity, fatty liver and steatohepatitis, containing as active ingredients benzothiazepine compounds having a thioamide bond and a quaternary ammonium substituent, represented by formula (1) below are provided. Also, drugs containing ileal bile acid transporter inhibiting compounds as active ingredients for the treatment and prevention of cholestasis-caused hepatopathy are provided.Type: GrantFiled: August 26, 2003Date of Patent: December 25, 2007Assignee: Asahi Kasei Pharma CorporationInventors: Takehiko Sasahara, Mitsunobu Mohri
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Patent number: 7238685Abstract: The invention relates to novel benzo-fused heterocycles 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, pharmaceutical compositions containing one or more of those compounds and especially their use as endothelin receptor antagonists.Type: GrantFiled: July 31, 2002Date of Patent: July 3, 2007Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli, Thomas Weller, Judith Marfurt
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Patent number: 7192947Abstract: The present invention relates to compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia.Type: GrantFiled: June 10, 2003Date of Patent: March 20, 2007Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, Suzanne Alenfalk, Tore Skjaret, Malin Lemurell
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Patent number: 7192946Abstract: The present invention relates to compounds of formula (I), wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia.Type: GrantFiled: August 30, 2002Date of Patent: March 20, 2007Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, David Blomberg, Suzanne Alenfalk, Peter Nordberg, Andreas Christer Wallberg, Stig Jonas Bostrom
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Patent number: 7192945Abstract: The present invention relates to compounds of the formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia.Type: GrantFiled: December 17, 2001Date of Patent: March 20, 2007Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Dahlstrom, David Blomberg
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Patent number: 7176195Abstract: Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists.Type: GrantFiled: June 21, 2001Date of Patent: February 13, 2007Assignee: Ferring BVInventors: Doreen Ashworth, Gary R. W. Pitt, Peter Hudson, Christopher Yea, Richard J. Franklin, Graeme Semple, David Paul Jenkins
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Patent number: 7132416Abstract: The present invention relates to compounds of formula (I) wherein Rv, R1, R2, Rx, Ry, M, Rz, v, R3, R4, R5 and R6 are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: GrantFiled: September 5, 2002Date of Patent: November 7, 2006Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, David Blomberg, Suzanne Alenfalk, Tore Skjaret, Malin Lemurell
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Patent number: 7129235Abstract: The present invention relates to compounds of formula (I-VII) or a pharmaceutically acceptable salt or prodrug thereof, in which A, L, R6, R7 and R8 are defined herein. The present invention also relates to methods of trating pain using these compounds and pharmaceutical compositions including these compounds.Type: GrantFiled: July 8, 2004Date of Patent: October 31, 2006Assignee: Abbott LaboratoriesInventors: Guo Zhu Zheng, Brian S. Brown, Sean C. Turner, Tammie K. White, Robert G. Schmidt, John R. Koenig, Chih-Hung Lee
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Patent number: 7125864Abstract: The present invention relates to compounds of formula (I): wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidemia.Type: GrantFiled: September 5, 2002Date of Patent: October 24, 2006Assignee: AstraZeneca ABInventors: Ingemar Starke, Mikael Ulf Johan Dahlstrom, David Blomberg
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Patent number: 7122536Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described.Type: GrantFiled: August 27, 2004Date of Patent: October 17, 2006Assignee: Pfizer Inc.Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 7101869Abstract: Novel compounds according to the formula and pharmaceutically acceptable salts, solvates, or hydrates thereof; wherein each occurrence of A is independently selected from CH or N; X is selected from the group consisting of —CH2—, —O—, —NH—, (C1-C6)alkylamino-, (C1-C6)alkylaminocarbonylamino-, (C1-C6)alkylcarbonylamino-, (C1-C6)alkylsulfonylamino-, phenylsulfonylamino-, carbonyl, —NH—C(O)—, —N(C1-C6)alkyl-C(O)—, —S(O)y— where y is 0, 1 or 2, and; n in —(CH2)n— is 1, 2 or 3; and R1, R2, and R3 are as described herein; pharmaceutical compositions that including these compounds, and methods for the treatment of autoimmune disease, inflammation, allergy, transplant rejection, and other circumstances where administration of an immunosuppressive agent is of therapeutic benefit.Type: GrantFiled: November 22, 2002Date of Patent: September 5, 2006Assignee: Pfizer Inc.Inventors: Todd A. Blumenkopf, Eileen Elliott Mueller, Eric Jan Roskamp
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Patent number: 7091198Abstract: The present invention relates to novel 2,5-disubstituted pyrimidine derivatives which stimulate soluble guanylate cyclase, to processes for the preparation thereof, and to the use thereof for producing medicaments, in particular medicaments for the treatment of central nervous system diseases.Type: GrantFiled: July 7, 2003Date of Patent: August 15, 2006Assignee: Bayer HealthCare AGInventors: Achim Feurer, Joachim Luithle, Stephan-Nicholas Wirtz, Gerhard König, Johannes-Peter Stasch, Elke Stahl, Rudy Schreiber, Frank Wunder
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Patent number: 7056929Abstract: A method for treating a living body afflicted with a cancer selected from lung and ovarian carcinoma, comprising the step of administering to the living animal body an amount of a compound selected from those of formula (I): wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, —ORa, —NRaRb, —NRa—C(O)-T1, —O—C(O)-T1, —O-T2-NRaRb, —O-T2-ORa, —NRa-T2-NRaRb, —NRa-T2-ORa and —NRa-T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the description, or X and Y together form a methylenedioxy or ethylenedioxy, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, —ORa, —NRaRb, —NRa—C(O)-T1, —O—C(O)-T1, —O-T2-NRaRb, —O-T2-ORa, —NRa-T2-NRaRb, —NRa-T2-ORa and —NRa-T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula —CH(R5)—CH(R6)—, —CH?C(R7)—, —C(R7)?CH— or —C(O)—CH(R8)— wherein R5, R6, R7 and R8 are as defined in the descriptType: GrantFiled: July 26, 2003Date of Patent: June 6, 2006Assignee: Les Laboratoires ServierInventors: Michel Koch, Francois Tillequin, Sylvie Michel, Elisabeth Seguin, Abdelhakim El Omri, John Hickman, Alain Pierre, Bruno Pfeiffer, Pierre Renard
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Patent number: 7041661Abstract: The invention relates to the use of compound of Formula I in treating patients for inflammatory or neuropathic pain as well as various symptoms of multiple sclerosisType: GrantFiled: December 16, 2003Date of Patent: May 9, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Bin Zhu, Joseph Wettstein, Margaret A. Petty
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Patent number: 7008938Abstract: A benzene-fused heteroring derivative of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of immune diseases (autoimmune diseases, infectious diseases, etc.), inflammatory diseases (inflammatory bowel diseases, multiple cerebrosclerosis, arthritis, etc.), nerve degeneration diseases (Alzheimer's disease, muscular dystrophy, etc.), bone resorption diseases (osteoporosis, etc.), respiratory system diseases, diabetes, shock, etc.Type: GrantFiled: July 29, 2004Date of Patent: March 7, 2006Assignee: Nokia CorporationInventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 6995154Abstract: The invention provides compounds of formula I: wherein R1 to R5 have any of the values defined in the specification, as well as pharmaceutically acceptable salts of the compounds, pharmaceutical compositions comprising the compounds, and methods of using the compounds, compositions, or salts to treat cancer. In embodiments, R4 and R5 taken together can be a 3, 4, or 5 membered saturated or unsaturated chain comprising members selected from the group consisting of non-peroxide oxygen, sulfur, N(X), and carbon, optionally substituted by oxo; wherein each X is independently absent or is H, O, (C1–C4)alkyl, phenyl or benzyl; and wherein at least one of the chain members is an N—H group.Type: GrantFiled: October 21, 2003Date of Patent: February 7, 2006Assignee: Rutgers, The State University of New JerseyInventors: Edmond J. LaVoie, Jung Sun Kim, Leroy Fong Liu
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Patent number: 6924280Abstract: This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis.Type: GrantFiled: February 21, 2003Date of Patent: August 2, 2005Assignee: Pfizer Inc.Inventors: Philip Albert Carpino, David Andrew Griffith, Bruce Allen Lefker
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Patent number: 6867204Abstract: Compounds of the formula: or pharmaceutically acceptable salts or prodrugs thereof, where each of n and p independently is 2 or 3, Y is —SO2— or —SO2—N(R10)—, Z1 is CH or N, and R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. The compounds have selective 5-HT6 affinity and are useful in the treatment of certain CNS disorders. Also provided are compositions comprising, methods for using, and methods for preparing Compounds of Formula I.Type: GrantFiled: May 9, 2003Date of Patent: March 15, 2005Assignee: Roche Palo Alto LLCInventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
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Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
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Publication number: 20040254160Abstract: The present invention relates to compounds of formula (I), wherein variable groups are as defined within; pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: ApplicationFiled: July 23, 2004Publication date: December 16, 2004Inventors: Ingemar Starke, Mikael ulf Johan Dahlstrom, David Blomberg, Suzanne Alenfalk, Peter Nordberg, Andreas Christer Wallberg, Stig Jonas Bostrom
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Patent number: 6806267Abstract: The present invention relates to pyrrolobenzoxazepines, pyrrolobenzthiazepines and related compounds having the ability to induce apoptosis, to pharmaceutical compositions comprising these compounds and to their use as anti-tumour agents.Type: GrantFiled: February 16, 2000Date of Patent: October 19, 2004Assignees: The Universita'di Siena, The Provost, Fellows and Scholars of the College of the Holy and Undivided Trinity of Queen Elizabeth Near DublinInventors: David Clive Williams, Daniela M. Zisterer, Vito Nacci, Giuseppe Campiani
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Publication number: 20040138199Abstract: The present invention provides compounds of Formula I 1Type: ApplicationFiled: December 22, 2003Publication date: July 15, 2004Inventors: Rocco Dean Gogliotti, Keri Lynn Muccioli, Kimberly Suzanne Para, Melean Visnick
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Publication number: 20040127705Abstract: A pyrrolesulfonamide derivative having the following formula (I): 1Type: ApplicationFiled: July 10, 2003Publication date: July 1, 2004Applicant: DAIICHI PHARMACEUTICAL CO., LTD.Inventors: Akira Mizuno, Makoto Shibata, Tomoe Kamei, Harukazu Fukami, Norio Inomata
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Patent number: 6727258Abstract: The present invention relates to compounds of formula (IA): the preparation thereof, pharmaceutical formulations thereof, and their use in medicine as allosteric adenosine receptor modulators for uses including protection against hypoxia and ischemia induced injury and treatment of adenosine-sensitive cardiac arrhythmias.Type: GrantFiled: March 19, 2001Date of Patent: April 27, 2004Assignee: King Pharmaceutical Research & Development, Inc.Inventor: Pier Giovanni Baraldi
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Publication number: 20040077625Abstract: Compounds, pharmaceutical compositions, and methods for the treatment of a hyperlipidemic condition in a subject.Type: ApplicationFiled: August 11, 2003Publication date: April 22, 2004Inventors: Samuel J. Tremont, Kevin J. Koeller, William L. Neumann
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Publication number: 20040067933Abstract: The present invention relates to compounds of the formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as ileal bile acid transport (IBAT) inhibitors for the treatment of hyperlipidaemia. Processes for their manufacture and pharmaceutical compositions containing them are also described.Type: ApplicationFiled: June 20, 2003Publication date: April 8, 2004Inventors: Ingemar Starke, Mikael Dahlstrom, David Blomberg
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Publication number: 20040063685Abstract: The present invention relates to a pharmaceutical agent containing an anti-sepsis drug (e.g., cycloalkene compound), and at least one kind of drug selected from the group consisting of an antibacterial agent, an antifungal agent, a non-steroidal antiinflammatory drug, a steroid and an anticoagulant in combination.Type: ApplicationFiled: June 6, 2003Publication date: April 1, 2004Inventors: Juji Ilzawa, Masayuki Ii, Shohei Hashiguchi, Tomoyuki Kitazaki
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Publication number: 20040058908Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia and atherosclerosis. Combinations disclosed include an ileal bile acid transport inhibitor combined with a cholesteryl ester transport protein (CETP) inhibitor, a fibric acid derivative, a nicotinic acid derivative, a microsomal triglyceride transfer protein inhibitor, a cholesterol abosrption antagonist, a phytosterol, a stanol, an antihypertensive agent, or others. Further combinations include a CETP inhibitor with a fibric acid derivative, a nicotinic acid derivative, a bile acid sequestrant, a microsomal triglyceride transfer protein inhibitor, a cholesterol abosrption antagonist, or others.Type: ApplicationFiled: October 9, 2002Publication date: March 25, 2004Applicant: G.D. SEARLE, LLCInventors: Bradley T. Keller, David B. Reitz, Joseph R. Schuh, James A. Sikorski, Samuel J. Tremont, Rodney W. Lappe