Polycyclo Ring System Having The Additional Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/252.06)
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Publication number: 20090286800Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: May 15, 2009Publication date: November 19, 2009Applicant: TAKEDA SAN DIEGO, INC.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Publication number: 20090270408Abstract: The invention relates to novel amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.Type: ApplicationFiled: February 6, 2009Publication date: October 29, 2009Applicant: ABBOTT LABORATORIESInventors: Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf, Chih-Hung Lee, Murali Gopalakrishnan
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Publication number: 20090253705Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: April 2, 2009Publication date: October 8, 2009Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20090239877Abstract: The invention provides 1,2,4-triazole compounds, compositions containing those compounds, methods of treating diseases and/or disorders with those compounds and processes of manufacturing 1,2,4-triazole compounds.Type: ApplicationFiled: March 17, 2009Publication date: September 24, 2009Applicants: AETERNA ZENTARIS GmbH, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUE, University of Montpellier I, University of Montpellier IIInventors: Jean-Alain Fehrentz, Mathieu Bibian, Aline Moulin, Jean Martinez
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Publication number: 20090192146Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Applicant: ACEA BIOSCIENCES, INC.Inventors: Xiao XU, Haoyun An, Xiaobo Wang
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Publication number: 20090191153Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: December 3, 2008Publication date: July 30, 2009Inventors: Ying Sun, Deqiang Niu, Guoyou Xu, Yat Sun Or, Zhe Wang
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Publication number: 20090181964Abstract: It is intended to provide a compound useful as a GnRH receptor antagonist. The inventors further investigated propane-1,3-dione derivatives. As a result, they confirmed that a compound having a benzene ring or a thiophene ring substituted with a group represented by —SO2—R3 in a propane-1,3-dione derivative having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene) has an excellent GnRH receptor antagonistic effect and accomplished the present invention. Because the compound of the present invention has a potent GnRH receptor antagonistic effect, it is useful for the treatment of sex hormone-dependent diseases, particularly GnRH-related diseases. Further, because the compound of the present invention has an excellent metabolic stability in human and few drug interactions, therefore it has preferable characteristics as a pharmaceutical used for the above-mentioned diseases.Type: ApplicationFiled: March 30, 2006Publication date: July 16, 2009Inventors: Masaaki Hirano, Isao Kinoyama, Shunichiro Matsumoto, Eiji Kawaminami, Kei Ohnuki, Hirofumi Yamamoto, Kazuhiko Osoda, Tatsuhisa Takahisa, Takashi Shin, Takanori Koike, Itsuro Shimada, Hiroyuki Hisamichi, Toshiyuki Kusayama
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Publication number: 20090176794Abstract: Compounds of formula (I): wherein: R1 and R2, which may be the same or different, represent a hydrogen atom or a linear or branched (C1-C6)alkyl group, R3 represents a hydrogen or halogen atom, a linear or branched (C1-C6)alkyl group, or a linear or branched (C1-C6)alkoxy group, Het represents a pyridyl, pyrimidinyl or piperidyl group, which are optionally substituted by one or more groups selected from halogen, linear or branched (C1-C6)alkyl and linear or branched (C1-C6)alkoxy, —represents a single bond or a double bond, their enantiomers and diastereoisomers, and also addition salts thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful in the treatment of depression, anxiety, disorders of memory in the course of aging and/or neurodegenerative diseases, and in the palliative treatment of Parkinson's disease, and for adaptation to stress.Type: ApplicationFiled: December 30, 2008Publication date: July 9, 2009Applicants: LES LABORATOIRES SERVIER, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE PARIS SUDInventors: Jean-Daniel Brion, Abdallah Deyine, Alain Le Ridant, Catherine Harpey
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Patent number: 7541354Abstract: Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.Type: GrantFiled: July 25, 2001Date of Patent: June 2, 2009Assignee: Pfizer Italia S.r.l.Inventors: Daniele Fancelli, Valeria Pittala, Mario Varasi
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Publication number: 20090124629Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl and indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; each R2 is independently hydrogen, fluorine or C1-4alkyl; n is 2, 3, 4, or 5; R3 is C1-4alkyl; R4 is hydrogen, or a C1-4alkyl group, a benzyl group, a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5;or R4 is a —SR6 group; R5 is selected from a group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido- 2-isothiType: ApplicationFiled: April 12, 2006Publication date: May 14, 2009Inventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Michel, Luca Tarsi, Silvia Terreni
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Patent number: 7531531Abstract: Bicyclo-pyrazole compounds of formula (I), as herein defined, are useful for treating diseases linked to disregulated protein kinases.Type: GrantFiled: April 10, 2007Date of Patent: May 12, 2009Assignee: Pfizer Italia S.r.l.Inventors: Daniele Fancelli, Valeria Pittalà, Mario Varasi
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Publication number: 20090111825Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: October 24, 2008Publication date: April 30, 2009Inventors: Kenneth GRANBERG, Bjorn Holm, Mats Nagard
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Publication number: 20090105267Abstract: The invention relates to octahydro-pyrrolo[3,4-b]pyrrole N-oxides as prodrugs of CNS-active compounds, compositions comprising such compounds, methods for making the compounds, salts, and polymorphs, and methods of treating conditions and disorders using such compounds and compositions. Octahydro-pyrrolo[3,4-b]pyrrole N-oxides of formula (I) are prodrugs of histamine-3 antagonists, and are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole N-oxide compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.Type: ApplicationFiled: September 11, 2008Publication date: April 23, 2009Applicant: Abbott LaboratoriesInventors: Marlon D. Cowart, Kennan C. Marsh, Huaqing Liu, Jae Y. Lee, Maria G. Beconi, Jill M. Wetter, Lawrence A. Black, Thomas C. Custer
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Publication number: 20090099179Abstract: The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: April 4, 2007Publication date: April 16, 2009Applicant: MYRIAD GENETICS, INCORPORATEDInventors: Christine Klein, Andrew D. Gassman, Leena Bhoite, John Manfredi
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Publication number: 20090093464Abstract: The present invention relates to naphthalene derivatives of formula (I) that are modulators of the glucocorticoid receptor, and to processes for the preparation and use of the same.Type: ApplicationFiled: February 21, 2006Publication date: April 9, 2009Applicant: SMITHKLINE BEECHMA CORPORATIONInventors: Stephen William Rafferty, Philip Stewart Turnbull, Eugene Lee Stewart, Richard Dana Caldwell
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Patent number: 7511038Abstract: New pyridazin-e-(2H)-one derivatives having the chemical structure of general formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of phosphodiesterase 4.Type: GrantFiled: November 8, 2004Date of Patent: March 31, 2009Assignee: Laboratorios Almirall S.A.Inventors: Vittorio Dal Piaz, Nuria Aguilar Izquierdo, Maria Antonia Buil Albero, Yolanda Garrido Rubio, Maria Paola Giovannoni, Jordi Gracia Ferrer, Wenceslao Lumeras Amador, Claudia Vergelli
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Publication number: 20090082282Abstract: The invention relates to the use of a phosphodiesterase type III (PDE III) inhibitor or Ca2+-sensitizing agent or a pharmaceutically acceptable derivative thereof for the preparation of a medication for the reduction of the heart size of a patient suffering from heart failure.Type: ApplicationFiled: March 23, 2005Publication date: March 26, 2009Applicant: Boehringer Ingelheim Vetmedica GmbHInventors: Juergen Daemmgen, Olaf Joens, Rainer Kleemann
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Patent number: 7507734Abstract: Disclosed are compounds according to the general formula (I), where the definitions of the substituents X, R1 and R2 are detailed in the description, as well as their physiologically acceptable salts and solvate, methods for producing these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: November 16, 2006Date of Patent: March 24, 2009Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Gunter Muller, Karl Schoenafinger, David William Will, Hans Matter, Martin Bossart, Cecile Combeau, Christine Delaisi, Ingrid Sassoon, Anke Steinmetz, Didier Benard
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Patent number: 7491722Abstract: Pyridazin-3(2H)-one derivatives of formula (I) are found to inhibit PDE-4. R1, R2 and R4 are organic radicals, R3 is a cyclic group, and R5 is an ester or an aryl or heteroaryl group.Type: GrantFiled: December 22, 2003Date of Patent: February 17, 2009Assignee: Laboratorios Almirall S.A.Inventors: Vittorio Dal Piaz, Nuria Aguilar Izquierdo, Maria Antonia Buil Albero, Marta Carrascal Riera, Jordi Gracia Ferrer, Maria Paola Giovannoni, Claudia Vergelli
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Publication number: 20090042897Abstract: The present invention relates to novel compounds or a pharmaceutically acceptable salt or solvate thereof, selected from a group consisting of: (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(2-fluoro-3-pyridinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(3-pyridazinyl)-1-oxa-3-azaspiro[4.5]decan-2-one; (trans)-8-({[1-(2-fluorophenyl)-1H-pyrazol-3-yl]amino}methyl)-3-(1-methyl-1H-pyrazol-3-yl)-1-oxa-3-azaspiro[4.5]decan-2-one; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.Type: ApplicationFiled: January 30, 2008Publication date: February 12, 2009Applicant: GLAXO GROUP LIMITEDInventors: Jonathan Bentley, Matteo Biagetti, Thorsten Genski, Silvia Rosalia Kopf, Colin Philip Leslie, Sergio Melotto
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Publication number: 20090036461Abstract: The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof: wherein: G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxyl, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3I s C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted byType: ApplicationFiled: August 21, 2006Publication date: February 5, 2009Inventors: Dieter Hamprecht, Christian Heidbreder, Sergio Melotto, Fabrizio Micheli, Tadataka Yamada
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Patent number: 7476673Abstract: Compounds of the formula where the variables are as defined in the specification, are useful for preventing or treating emphysema and related pulmonary conditions of mammals and other diseases and conditions which are responsive to RAR? agonist retinoids, such as skin related diseases, including but not limited to acne and psoriasis.Type: GrantFiled: December 17, 2004Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
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Patent number: 7470689Abstract: Disclosed are compounds of the general formula (I), where the definition of the substituents A, B, D, E, R1 and R2 are detailed in the description, and the physiologically tolerated salts thereof, a process for the preparation of these compounds and their use as pharmaceuticals. These compounds are kinase inhibitors, in particular inhibitors of the kinase CDK2 (cyclin-dependent kinase 2).Type: GrantFiled: August 31, 2006Date of Patent: December 30, 2008Assignee: Aventis Pharma S.A.Inventors: Swen Hoelder, Karl Schoenafinger, David William Will, Hans Matter, Günter Müller, Cécile Combeau, Christine Delaisi, Anke Steinmetz, Ingrid Sassoon
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Publication number: 20080318927Abstract: Compounds of formula I: (wherein variables A1, A2, A2, A4, m, n, J, Q, R4, Ea, Eb, Ec, R6, R7, Re, Rf, RPG and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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: June 19, 2008Publication date: December 25, 2008Inventors: Michael R. Wood, Steven N. Gallicchio, Harold G. Selnick, C. Blair Zartman, Ian M. Bell, Craig A. Stump
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Patent number: 7465811Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.Type: GrantFiled: November 30, 2007Date of Patent: December 16, 2008Assignee: Laboratoires Fournier S.A.Inventors: Luc Lebreton, Christine Dumas, Christine Massardier, Michel Bondoux
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Patent number: 7462613Abstract: The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.Type: GrantFiled: November 19, 2003Date of Patent: December 9, 2008Assignee: SANOFI-AVENTIS Deutschland GmbHInventors: Swen Hölder, Thorsten Naumann, Karl Schönafinger, David William Will, Hans Matter, Günther Müller, Dominique Le Suisse, Bernard Baudoin, Thomas Rooney, Franck Halley, Gilles Tiraboschi, Cécile Combeau, Ingrid Sassoon, Anke Steinmetz
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Publication number: 20080293731Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: December 14, 2006Publication date: November 27, 2008Inventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Publication number: 20080280918Abstract: The invention relates to new therapeutically useful pyridazin-3(2H)-one derivatives of Formula (I) and to pharmaceutical compositions containing them. These compounds are potent and selective inhibitors of phosphodiesterase 4 (PDE4) and are thus useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible of being improved by inhibition of PDE4 such as asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatilis, psoriasis or irritable bowel disease.Type: ApplicationFiled: June 13, 2005Publication date: November 13, 2008Applicant: ALMIRALL PRODESFARMA, SAInventors: Antonia Maria Buil Albero, Vittorio Dal Piaz, Yolanda Garrido Rubio, Jordi Garcia Ferrer, Lluis Miquel Pages Santacana, Joan Taltavull Moll
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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: 7405215Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: GrantFiled: September 21, 2005Date of Patent: July 29, 2008Assignee: WyethInventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
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Patent number: 7399765Abstract: Compounds of formula (I) Z-Ar1—Ar2??(I) wherein Z is a diazabicyclic amine, Ar1 is a 5- or 6-membered aromatic ring, and Ar2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.Type: GrantFiled: September 16, 2004Date of Patent: July 15, 2008Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Jianguo Ji, Tao Li, Jennifer M. Pace, Karin R. Tietje, Kathleen H. Mortell, Diana L. Nersesian, Michael R. Schrimpf
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Publication number: 20080119465Abstract: Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.Type: ApplicationFiled: November 30, 2007Publication date: May 22, 2008Applicant: Laboratories Fournier S.A.Inventors: Luc LEBRETON, Christine Dumas, Christine Massardier, Michel Bondoux
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Patent number: 7361657Abstract: This invention concerns the use of compounds of formula (I) wherein ?a1=a2?a3=a4—is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7309701Abstract: The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl-(C1-C10-alkyl)-, heteroaryl, heteroaryl-(C1-C10-alkyl)-, heterocyclyl, heterocyclyl-(C1-C10-alkyl)-, C3-C10-cycloalkyl, polycycloalkyl, C2-C10-alkenyl or C2-C10-alkinyl and Ar is unsubstituted or at least monosubstituted aryl or heteroaryl.Type: GrantFiled: November 19, 2003Date of Patent: December 18, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Swen Hölder, Thorsten Naumann, Karl Schönafinger, David William Will, Hans Matter, Günther Müller, Dominique Le Suisse, Bernard Baudoin, Thomas Rooney, Franck Halley, Gilles Tiraboschi
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Patent number: 7285551Abstract: The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.Type: GrantFiled: July 8, 2003Date of Patent: October 23, 2007Assignee: Japan Tobacco Inc.Inventors: Hiromasa Hashimoto, Kenji Mizutani, Atsuhito Yoshida
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Patent number: 7282498Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. 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 and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: June 1, 2004Date of Patent: October 16, 2007Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
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Patent number: 7262195Abstract: Compounds are provided which are useful in treating disorders of gastrointestinal motility and which have the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —CO2R4, —SO2N(R4)R4a, —SO2R4, CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle. R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. A method for using such compounds for treating disorders of gastrointestinal motility is also provided.Type: GrantFiled: September 14, 2004Date of Patent: August 28, 2007Assignee: Bristol-Myers Squibb CompanyInventors: James J. Li, Hannguang J. Chao, Joseph A. Tino, William R. Ewing
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Publication number: 20070191313Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.Type: ApplicationFiled: February 15, 2007Publication date: August 16, 2007Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
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Patent number: 7173034Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 3, 2005Date of Patent: February 6, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7148249Abstract: The present invention relates to heterocyclically substituted indolinones of general formula wherein R1 to R5 and X are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and cyclin/CDK complexes and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.Type: GrantFiled: September 5, 2003Date of Patent: December 12, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Joerg Kley, Frank Hilberg, Armin Heckel, Gerald Juergen Roth, Thorsten Lehmann-Lintz, Ralf R. H. Lotz, Ulrike Tontsch-Grunt, Jacobus C. A. Van Meel
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Patent number: 7081458Abstract: 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 in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: April 11, 2005Date of Patent: July 25, 2006Assignee: Neurogen Corp.Inventors: Alan J. Hutchison, John M. Peterson, Dario Doller, Wallace C. Pringle, Helen Yin
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Patent number: 7074793Abstract: The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones.Type: GrantFiled: January 12, 2004Date of Patent: July 11, 2006Assignee: Cephalon, Inc.Inventors: Robert L. Hudkins, Dandu R. Reddy, Jasbir Singh, Rabindranath Tripathy, Ted Underiner
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Patent number: 6974815Abstract: The present invention is directed to compounds having the formula (I): useful in treating inflammatory and immune diseases, in which K is O or S; Q is —C(?O)— or optionally substituted C1-4alkylene; Ar is optionally-substituted aryl or heteroaryl; J1, J2, J3, and Y are selected so that ring A is a five-to-six membered optionally-substituted cycloalkenyl or heterocyclo ring having 0 to 2 nitrogen heteroatoms; Z is N or C(R9); and R1, R2, R3 and R9 are as defined in the specification.Type: GrantFiled: October 9, 2003Date of Patent: December 13, 2005Assignees: Bristol-Myers Squibb Company, Cerep SAInventors: T G. Murali Dhar, Dominique Potin, Magali Jeannine Blandine Maillet, Michele Launay, Eric Antoine Nicolai, Edwin J. Iwanowicz
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Patent number: 6924287Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be replaced; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 20, 2000Date of Patent: August 2, 2005Assignee: Janssen Pharmacatica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 6903112Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: GrantFiled: October 23, 2003Date of Patent: June 7, 2005Assignee: WyethInventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
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Patent number: 6897229Abstract: The PDE4 inhibitor N-(3,5-dichloropyrid-4-yl)-3-cyclopropylmethoxy-4-difluoromethoxy benzamide, a pharmacologically tolerable salt or N-oxide thereof, in combination with a PDE3 inhibitor is disclosed for use in inhibiting bronchospasms and treating acute obstructive bronchitis, asthma or COPD.Type: GrantFiled: November 4, 2002Date of Patent: May 24, 2005Assignee: Altana Pharma AGInventor: Ulrich Kilian
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Patent number: 6867206Abstract: The present invention relates to 6-carboxyphenyldihydropyridazinone derivatives having the formula wherein R1, R2, R3, A, D, G, and E are as defined in the specification and claims, a process for preparing these materials, pharmaceutical compositions containing them, and a method for using them in the treatment of anemias.Type: GrantFiled: June 16, 2000Date of Patent: March 15, 2005Assignee: Bayer AktiengesellschaftInventors: Jürgen Stoltefuss, Gabriele Bräunlich, Michael Lögers, Carsten Schmeck, Ulrich Nielsch, Martin Bechem, Christoph Gerdes, Michael Sperzel, Klemens Lustig, Werner Stürmer
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Patent number: 6861430Abstract: The invention provides compounds of formula (I) wherein R1 to R5 are as defined in the description, and their preparation. The compounds of formula (I) are useful as pharmaceuticals.Type: GrantFiled: April 2, 2002Date of Patent: March 1, 2005Assignee: Novartis AGInventors: Thomas J. Troxler, Konstanze Hurth, Daniel Hoyer
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Patent number: 6849629Abstract: The present invention relates to novel pyridazinone compounds, pharmaceutical compositions comprising those compounds and to methods of using such compounds and compositions to inhibit aldose reductase, lower sorbitol levels and, thus, lower fructose levels, and/or treat or prevent diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. This invention also relates to methods of affording cardioprotection to subjects not suffering from diabetes. This invention also relates to pharmaceutical compositions and kits comprising a combination of an aldose reductase inhibitor (ARI) of this invention and a sorbitol dehydrogenase inhibitor and to methods of using such compositions or kits to treat or prevent the above diabetic complications in mammals.Type: GrantFiled: February 20, 2003Date of Patent: February 1, 2005Assignee: Pfizer, Inc.Inventor: Banavara L. Mylari