Polycyclo Ring System Having The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/219)
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Publication number: 20110014154Abstract: The disclosure provides compounds of formula (I), including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: ApplicationFiled: March 24, 2009Publication date: January 20, 2011Inventors: John A. Bender, Zhong Yang, John F. Kadow
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Patent number: 7855196Abstract: A composition comprising a benzodiazepine agonist, a benzodiazepine antagonist, and a pharmaceutical acceptable carrier in an effective ratio so as to preserve the therapeutic effects of the benzodiazepine agonist while modulating the side effects of the benzodiazepine agonist.Type: GrantFiled: August 22, 2005Date of Patent: December 21, 2010Inventor: Pierre Mainville
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Publication number: 20100317645Abstract: Certain novel substituted diazepine sulfonamides are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.Type: ApplicationFiled: December 7, 2007Publication date: December 16, 2010Inventors: Robert K. Baker, Linda L. Chang, Marc Chioda, Harry R. Chobanian, Ying-Duo Gao, Yan Guo, Linus S. Lin, Ping Liu, Ravi P. Nargund, Kathleen M. Rupprecht, Shouwu Miao
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Patent number: 7851464Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K 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: GrantFiled: November 14, 2006Date of Patent: December 14, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Harold G. Selnick, Michael R. Wood, Cory R. Theberge, Craig A. Stump, Steven N. Gallicchio, C. Blair Zartman
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Patent number: 7781427Abstract: Methods for synthesizing tetrahydroquinoline-containing compounds are provided, along with synthetic intermediates and products associated with such methods.Type: GrantFiled: November 4, 2005Date of Patent: August 24, 2010Assignee: Wyeth LLCInventors: Christoph Dehnhardt, Sreenivasulu Megati, Jerry Sun
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Publication number: 20100204214Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: February 11, 2010Publication date: August 12, 2010Inventors: Milan Chytil, Sharon R. Engel, Qun Kevin Fang, Kerry L. Spear
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Publication number: 20100203007Abstract: The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: February 4, 2010Publication date: August 12, 2010Applicant: Immunogen Inc.Inventors: Wei Li, Nathan Fishkin, Robert Zhao, Michael Miller, Ravi Chari
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Patent number: 7767660Abstract: Compounds of the formula (I): wherein A, B, D, M, Ar, W, X, Y, Z and R1 are as defined herein, are useful in the prevention and treatment of hepatitis C infections. The compounds, their preparation, pharmaceutical compositions containing them and their use in medicine are disclosed.Type: GrantFiled: December 19, 2007Date of Patent: August 3, 2010Assignee: Istituto di Richerche di Biologia Molecolare P. Angeletti SpAInventors: Ian Stansfield, Uwe Koch, Joerg Habermann, Frank Narjes
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Publication number: 20100173896Abstract: The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, to the manufacture and to the use thereof.Type: ApplicationFiled: March 16, 2010Publication date: July 8, 2010Inventors: JUNICHI SAKAKI, KAZUHIDE KONISHI, MASASHI KISHIDA, MASAAKI KIMURA, HIDEFUMI UCHIYAMA, HIRONOBU MITANI
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Publication number: 20100160291Abstract: This invention is directed to tricyclic spiro-oxindole derivatives of formula (I), wherein j, k, m, n, w, q, Y, Q, X, R1, R2 and R3 are as defined herein, as a stereoisomer, enantiomer, tautomer thereof or mixtures thereof; or a pharmaceutically acceptable salt, solvate or prodrug thereof, which are useful for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. Pharmaceutical compositions comprising the compounds and methods of preparing and using the compounds are also disclosed.Type: ApplicationFiled: October 12, 2007Publication date: June 24, 2010Applicant: XENON PHARMACEUTICALS INC.Inventors: Mikhail Chafeev, Sultan Chowdhury, Jianmin Fu, Ranjender Kamboj
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Patent number: 7709470Abstract: The present invention relates to novel benzodiazepine compounds exhibiting RXR-antagonist efficacy, for delaying progression of, preventing or treating a condition or disease being associated with RXR-antagonism, in particular selected from diabetes, complication of diabetes such as retinopathy, nephropathy, neuropathy, and hyperlipidemia, obesity, dyslipidemia, and osteoporosis.Type: GrantFiled: April 8, 2004Date of Patent: May 4, 2010Assignee: Novartis AGInventors: Junichi Sakaki, Kazuhide Konishi, Masashi Kishida, Masaaki Kimura, Hidefumi Uchiyama, Hironobu Mitani
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Publication number: 20100105666Abstract: Compounds of formula (I): wherein: R1 represents hydrogen, (C1-C6)alkyl, (C1-C6)aminoalkyl or (C1-C6)hydroxyalkyl, R2 represents hydrogen, or R1 and R2, together with the carbon atoms carrying them, form a carbon-carbon bond, R3 represents hydrogen, R4 represents hydrogen, methyl or (C3-C6)alkyl, (C1-C6)aminoalkyl, (C1-C6)hydroxyalkyl, aryl-(C1-C6)alkyl or heterocycloalkyl-(C1-C6)alkyl, or R3 and R4 together with the carbon atoms carrying them, form a carbon-carbon bond, R5, R6, R7 and R8 represent hydrogen, or a pair of geminal substituents (R5 and R6 and/or R7 and R8) form an oxo, thioxo or imino group, R9 represents hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, cyano, nitro, (C1-C6)polyhaloalkyl or optionally substituted amino, R10 and R11 represent hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, cyano, nitro, (C1-C6)polyhaloalkyl or optionally substituted amino, n represents an integer between 0 and 4 inclusive, m represents an integer between 0 and 2 inclusive, p represents anType: ApplicationFiled: January 4, 2008Publication date: April 29, 2010Inventors: Jean-Daniel Brion, Maud Hervet, Anne Moreau, Zafiarisoa Dolor Renko, Alain Le Ridant, Catherine Harpey
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Publication number: 20100081646Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators.Type: ApplicationFiled: August 19, 2009Publication date: April 1, 2010Applicant: KALYPSYS, INC.Inventors: Steven P. Govek, Clay Beauregard, Daniel A. Gamache, Mark R. Hellberg, Stewart A. Noble, Andrew K. Shiau, David J. Thomas, John M. Yanni
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Publication number: 20100075954Abstract: The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.Type: ApplicationFiled: November 16, 2009Publication date: March 25, 2010Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
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Patent number: 7671048Abstract: The present invention is concerned with a method of treating a disease selected from the group consisting of cognitive disorders, anxiety, Alzheimer's disease, and schizophrenia comprising administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein R1 is halogen, lower alkyl, lower alkynyl, cycloalkyl, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is hydrogen, methyl or aryl which is unsubstituted or substituted by one or two substituents selected from the group consisting of halogen and lower alkoxy; R3 is hydrogen, lower alkyl, lower alkenyl, cycloalkyl, lower alkoxy, —O(CH2)n+1—O-lower alkyl, —(CH2)n-aryl which is optionally substituted by lower alkyl or halogen, heteroaryl, —NHR, —N(R)2, wherein each R can be the same or different, —NHCH2C?CH, or pyrrolidin-1-one; R is hydrogen, lower alkyl, lower alkyl substituted by halogen, heteroaryl, —(CH2)nO-lower alkyl, —NH-lower alkyl, cycloalkyl orType: GrantFiled: October 7, 2005Date of Patent: March 2, 2010Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Heinz Stadler, Andrew William Thomas
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Patent number: 7659263Abstract: The present invention relates to a thienopyrrole compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound as an active ingredient. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: GrantFiled: November 10, 2005Date of Patent: February 9, 2010Assignee: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Takahiro Oka, Kenta Aoki, Satoru Noji, Yoko Matsumoto, Toshihiro Sato, Izuru Ando, Yasushi Niwa
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Publication number: 20100004226Abstract: The present invention provides compositions and methods of using stereospecific benzodiazepine derivatives, their salts and prodrugs for the treatment of anxiolytic or convulsant disorders having the side effects of reduced alcohol craving in human alcoholics and a concomitant reduced sedative, hypnotic, muscle relaxant and ataxic side-effects. The invention further provides pharmaceutical compositions for treatment of anxiolytic and convulsant disorders in subjects in need thereof, comprising a compound, prodrug or a salt having a chemical structure represented by any one of Formula I-IV, VI-XI, XV-XVIII and XX-XXI and a pharmaceutically-acceptable carrier.Type: ApplicationFiled: August 7, 2009Publication date: January 7, 2010Inventors: James M. Cook, Hao Zhou, Shengming Huang, P.V.V.S. Sarma, Chunchun Zhang
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Publication number: 20090298813Abstract: Use of neuroprotective compounds in obtaining medicaments intended for the curative treatment of neurodegenerative disease and/or the prevention of the appearance of disorders ensuing from those diseases.Type: ApplicationFiled: January 4, 2008Publication date: December 3, 2009Applicant: LES LABORATOIRES SERVIERInventors: Alain Le Ridant, Catherine Harpey
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Publication number: 20090297502Abstract: Anti-chemokine monoclonal antibody therapy is provided for the prevention, control or reversal of chronic rejection mediated vascular remodeling, including, e.g., but not limited to MCP-1/CCR2 antagonist antibody therapy for the modulation of cardiovascular pathologies associated with cardiac graft rejection including intimal thickening, arteritis, fibrosis, and necrosis.Type: ApplicationFiled: June 14, 2007Publication date: December 3, 2009Inventors: Li Li, Sicco H. Popma
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Patent number: 7611694Abstract: The present invention relates to a propellant-free, aqueous aerosol formulation for anticholinergics of formula 1 wherein X? denotes an anion.Type: GrantFiled: June 15, 2006Date of Patent: November 3, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventor: Friedrich Schmidt
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Publication number: 20090270373Abstract: Pharmaceutical compositions and methods of treating Down Syndrome, mental retardation or both are provided. The pharmaceutical compositions comprise one or more benzodiazepine receptor antagonists, such as flumazenil.Type: ApplicationFiled: April 21, 2009Publication date: October 29, 2009Applicant: Cypress Biosciences, Inc.Inventors: Srinivas Rao, Jay Kranzler, Jeffery Anderson
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Publication number: 20090197856Abstract: Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses.Type: ApplicationFiled: December 19, 2008Publication date: August 6, 2009Inventors: Salvador G. Alvarez, Janos Botyanszki, Joseph de los Angeles, Jiping Fu, Roger Fujimoto, Joshua Michael Gralapp, Ronald Conrad Griffith, Peichao Lu, Son Minh Pham, Christopher Don Roberts, Franz Ulrich Schmitz, Mohindra Seepersaud, Ruben Tommasi, Adam Christopher Villa, Sompong Wattanasin, Aregahagn Yifru, Rui Zheng, Xiaoling Zheng
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Publication number: 20090124604Abstract: The invention concerns a compound of the Formula (I) wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen or halogeno; and R4 is isoxazolyl; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: February 23, 2006Publication date: May 14, 2009Inventors: Ian Alun Nash, Jonathan Erle Finlayson, Caroline Rachel Thompson
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Publication number: 20090124605Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: October 31, 2008Publication date: May 14, 2009Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Gabriella Traquandi, Maria Gabriella Brasca, Roberto D'Alessio, Paolo Polucci, Fulvia Roletto, Anna Vulpetti, Paolo Pevarello, Achille Panzeri, Francesca Quartieri, Ron Ferguson, Paola Vianello, Daniele Fancelli
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Patent number: 7524840Abstract: The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.Type: GrantFiled: October 5, 2005Date of Patent: April 28, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Jin-Jun Liu, Kin-Chun Luk, Giacomo Pizzolato, Yi Ren, Kshitij Chhabilbhai Thakkar, Peter Michael Wovkulich, Zhuming Zhang
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Publication number: 20090105227Abstract: The present invention relates to tetracyclic thienopyrrole compounds of formula (I), wherein Ar, A, D1, D2, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: ApplicationFiled: May 3, 2006Publication date: April 23, 2009Applicant: Istituto Di Ricerche Di Biologia Molecolare P. Angeletti SPAInventors: Stefania Colarusso, Joerg Habermann, Frank Narjes, Simona Ponzi, Maria del Rosario Rico Ferreira
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Patent number: 7514426Abstract: The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF3, —NHR, —NHC(O)R or —NHSO2R; R2 is lower alkyl substituted by halogen; R3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: October 17, 2005Date of Patent: April 7, 2009Assignee: Hoffman-La Roche Inc.Inventors: Henner Knust, Andrew William Thomas
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Patent number: 7507729Abstract: The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the following formula wherein the definition of substituents is described in the claims. This class of compounds shows high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as a cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: October 4, 2006Date of Patent: March 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Henner Knust, Andrew Thomas
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Patent number: 7507728Abstract: The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used as a cognitive enhancer or for the treatment of cognitive disorders, anxiety, Alzheimer's disease and schizophrenia.Type: GrantFiled: October 17, 2005Date of Patent: March 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Andrew William Thomas
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Patent number: 7494991Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4?,5? or 5?,6? positions.Type: GrantFiled: May 17, 2007Date of Patent: February 24, 2009Assignee: ActivBiotics Pharma, LLCInventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
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Publication number: 20090048239Abstract: A class of macrocyclic compounds of formula (I), wherein R7, A, Ar, B, D, F, M, Q1, Q2, W, X, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.Type: ApplicationFiled: July 15, 2008Publication date: February 19, 2009Inventors: Immacolata Conte, Joerg Habermann, Angela Mackay, Frank Narjes, Maria del Rosario Rico Ferreira, Ian Stansfield
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Publication number: 20090042866Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: November 23, 2005Publication date: February 12, 2009Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20080312189Abstract: The invention provides methods for treating and/or preventing cerebral autosomal dominant arteriopathy with subcortical infarcts and leukoencephalopathy (CADASIL) in a patient in need thereof by administering a therapeutically effective amount of at least one cholinesterase inhibitor. The invention also provides methods for treating and/or preventing neurovascular diseases caused by one or more mutations of the human Notch3 gene by administering a therapeutically effective amount of at least one cholinesterase inhibitor. In one embodiment, the cholinesterase inhibitor is donepezil, a stereoisomer thereof and/or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 4, 2005Publication date: December 18, 2008Applicant: EISAI CO., LTD.Inventor: Raymond Pratt
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Publication number: 20080279784Abstract: Particulate formulations of benzodiazepines, such as diazepam, are used for nasal administration of diazepine drugs to patients. Multimodal particulate formulations of benzodiazepines and methods for their use, e.g. by nasal administration for the treatment of seizure, are also provided.Type: ApplicationFiled: May 7, 2008Publication date: November 13, 2008Applicant: QUESTCOR PHARMACEUTICALS, INC.Inventors: Steve Cartt, David Medeiros
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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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Patent number: 7442694Abstract: The present invention relates to a compounds of formula I: wherein A, B, D, E and F are defined herein; that are useful in treating central nervous system (CNS) diseases, disorders and conditions, such as but not limited to nicotine addiction, schizophrenia, depression, Alzheimer's disease, Parkinson's disease and ADHD. The present invention further comprises pharmaceutical compositions containing such compounds and methods of treatment comprising the use of such compounds.Type: GrantFiled: September 8, 2003Date of Patent: October 28, 2008Assignee: Pfizer IncInventors: Jotham W. Coe, Christopher J. O'Donnell, Brian T. O'Neill, Lawrence A. Vincent
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Patent number: 7432256Abstract: The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of the formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, nitro, cycloalkyl, —O(CH2)mO(CH2)mOH or —C?C—R?; R2 is hydrogen or methyl; R3 is lower alkyl, lower alkyl substituted by halogen, lower alkenyl, lower alkenyl substituted by halogen, lower alkynyl, —(CH2)n-cycloalkyl, —(CR?R?)m—CH3, phenyl that is unsubstituted or substituted by halogen, pyridinyl or thienyl each of which is unsubstituted or substituted by lower alkyl, —(CH2)n—NH-cycloalkyl, lower alkenyl-cycloalkyl, lower alkynyl-(CR?R?)mOH, or lower alkynyl-phenyl wherein the phenyl ring is unsubstituited or substituted by halogen, CF3, lower alkyl or lower alkoxy; R? is hydrogen or lower alkyl; R? is hydrogen, hydroxy or lower alkyl; n is 0, 1 or 2; m is 1, 2 or 3; and o is 1 or 2; and pharmaceutically acceptable acid addition salts thType: GrantFiled: December 8, 2005Date of Patent: October 7, 2008Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Henner Knust, Andrew William Thomas
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Patent number: 7384934Abstract: Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionallyType: GrantFiled: July 28, 2003Date of Patent: June 10, 2008Assignee: Eli Lilly and CompanyInventors: Thomas Daniel Aicher, Zhaogen Chen, Yvan LeHuerou, Fionna Mitchell Martin, Marta Maria Pineiro-Nunez, Vincent Patrick Rocco, Kevin Michael Ruley, John Mehnert Schaus, Patrick Gianpietro Spinazze, David Edward Tupper
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Patent number: 7273861Abstract: Compounds represented by formula 1: wherein R1 is H, halogen, (C1-4)alkyl, O(C1-4)alkyl, and haloalkyl; R2 is H or methyl; R3 is H or (C1-4)alkyl; R4 is H or (C1-4)alkyl; R5 is (C1-4)alkyl, (C1-4)alkyl(C3-7)cyclo-alkyl or (C3-7)cycloalkyl; and W is a fused phenyl-5 or 6-membered heterocycle having one or two heteroatoms selected from N or S; or W is phenyl, 1,1?-biphenyl, 2,3-dihydro-1H-indene, 1,2,3,4-tetrahydronaphthyl, or naphthyl; said W being optionally substituted with (C1-4)alkyl, which in turn can be optionally substituted with a carboxy or (C1-4)alkoxycarbonyl, or a salt or ester thereof. The compounds have inhibitory activity against Wild Type, single and double mutant strains of HIV.Type: GrantFiled: September 15, 2003Date of Patent: September 25, 2007Assignee: Boehringer Ingelheim (Canada) Ltd.Inventors: Christiane Yoakim, Jeffrey O'Meara, Bruno Simoneau, William Ogilvie, Robert Déziel
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Patent number: 7271162Abstract: This invention provides compounds of formula I having the structure wherein: R1 and R2 are H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated, acyl, or aroyl; R3, R4 are H, alkyl, cycloalkyl or —CH2-cycloalkyl; R5 is H or alkyl; R6 is H or alkyl; and wherein the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods for using these compounds to treat central nervous system disorders, including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.Type: GrantFiled: June 18, 2004Date of Patent: September 18, 2007Assignee: WyethInventors: Annmarie L. Sabb, Robert L. Vogel
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Patent number: 7271164Abstract: This invention provides compounds of the formula: wherein R1 and R2 are each, independently, H, alkyl, cycloalkyl, —CH2-cycloalkyl, alkoxy, halogen, fluorinated alkyl, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; R3 and R4 are each, independently, H, alkyl or cycloalkyl; R5 is H or alkyl; R6 is H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.Type: GrantFiled: October 15, 2004Date of Patent: September 18, 2007Assignee: WyethInventors: Annmarie L. Sabb, Robert L. Vogel
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Patent number: 7271163Abstract: This invention provides compounds of the formulae: wherein: R1 is hydrogen, —C(O)CH3 or alkyl of 1-6 carbon atoms; R2 and R3 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, cycloalkyl, alkoxy of 1-6 carbon atoms, —CH2OH, fluoroalkyl, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, aryl, or aroyl; R4 and R5 are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, fluoroalkyl, —CN, alkyl sulfonamide of 1-6 carbon atoms, alkyl amide of 1-6 carbon atoms, amino, alkylamino of 1-6 carbon atoms, dialkylamino of 1-6 carbon atoms per alkyl moiety, fluoroalkoxy of 1-6 carbon atoms, acyl of 2-7 carbon atoms, or aroyl; R6 and R7 are each independently hydrogen, C1-C6 alkyl or cycloalkyl; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions containing theseType: GrantFiled: July 23, 2004Date of Patent: September 18, 2007Assignee: WyethInventors: Annmarie L. Sabb, Robert L. Vogel, James A. Nelson, Sharon J. Rosenzweig-Lipson, Gregory S. Welmaker, Joan E. Sabalski
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Patent number: 7220738Abstract: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3?-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4?,5? or 5?,6? positions.Type: GrantFiled: December 9, 2004Date of Patent: May 22, 2007Assignee: ActivBiotics, Inc.Inventors: John H. van Duzer, Arthur F. Michaelis, William B. Geiss, Douglas G. Stafford, Xiang Y. Yu, James M. Siedlecki, Yingfei Yang
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Patent number: 7141563Abstract: This invention provides processes for preparing compounds formula: wherein R is H, alkyl, acyl, aryl, aroyl or —C(O)R?; R? is alkyl or aryl; R1, R2, R4 and R5 are H, —OH, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl or alkoxy, —CN, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, acyl, aryl or aroyl; R3 is H, alkyl, cycloalkyl, alkoxy, fluorinated alkyl, —NH—SO2-alkyl, —SO2—NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, aryl, or aroyl; or a pharmaceutically acceptable salt thereof, as well as novel compounds useful in the synthesis of these compounds.Type: GrantFiled: November 2, 2001Date of Patent: November 28, 2006Assignee: WyethInventors: Gregory S. Welmaker, Joan E. Sabalski, Michael D. Smith
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Patent number: 7132451Abstract: The impact of lipoxin A4 (LXA4) and aspirin-triggered-lipoxins (ATL) was investigated in tumor necrosis factor (TNF?)-initiated neutrophil (PMN) responses in vitro and in vivo using metabolically stable LX analogs. At concentrations as low as 1–10 nM, the LXA4 and ATL analogs each inhibited TNF?-stimulated superoxide anion generation and IL-1? release by human PMN.Type: GrantFiled: March 5, 2004Date of Patent: November 7, 2006Inventor: Charles N. Serhan
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Patent number: 7132418Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.Type: GrantFiled: July 25, 2002Date of Patent: November 7, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael J. Costanzo, Bruce E. Maryanoef, Stephen C. Yabut
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Patent number: 7129237Abstract: Compounds of Formula I or a pharmaceutically acceptable salt thereof are provided: where R1 through R7 are defined herein. The compounds of Formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.Type: GrantFiled: April 24, 2003Date of Patent: October 31, 2006Assignee: WyethInventor: P. Sivaramakrishnan Ramamoorthy
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Patent number: 7119087Abstract: Compound corresponding to the general formula (I) in which R2 represents a chlorine atom, a methyl group or a 3-thienyl group. Therapeutic application.Type: GrantFiled: November 20, 2002Date of Patent: October 10, 2006Assignee: Sanofi-AventisInventors: Frédéric Galli, Odile Leclerc, Alistair Lochead
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Patent number: 7105506Abstract: Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: May 2, 2002Date of Patent: September 12, 2006Assignee: Lilly Icos LLCInventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
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Patent number: RE39680Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 16, 2006Date of Patent: June 5, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Michael Guang Yang, Simon Haydar, Wenting Chen, Christopher D. McClung, Emile J. B. Calvello, David M. Zawrotny, Parthasarathl Rajagopalan