Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/309)
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Publication number: 20110212959Abstract: The present invention relates to cyanoisoquinoline compounds suitable for use in treating hypoxia inducible factor-mediated and/or erythropoietin-associated conditions.Type: ApplicationFiled: March 7, 2011Publication date: September 1, 2011Inventors: Michael P. Arend, Lee A. Flippin, Min Wu, Eric D. Turtle, Wen-Bin Ho, Shaojiang Deng
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Publication number: 20110212939Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are GPCR (GPR119) agonists and are useful as for the treatment of diabetes and obesity.Type: ApplicationFiled: July 10, 2009Publication date: September 1, 2011Applicant: Prosidion LimitedInventors: Lisa Sarah Bertram, Philip Graham Clarke, Graham John Dawson, Peter Timothy Fry, Matthew Colin Thor Fyfe, William Gattrell, Revathy Perpetua Jeevaratnam, John Keily, Thomas Martin Krulle, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Publication number: 20110201629Abstract: There are described cyclohexyl amide derivatives of Formula I, which are useful as corticotropin releasing factor (CRF) receptor antagonists and as pharmaceuticals.Type: ApplicationFiled: January 31, 2011Publication date: August 18, 2011Inventors: Benjamin Atkinson, David Beattie, Andrew James Culshaw, James Dale, Nicholas James Devereux, Jeffrey McKenna
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Publication number: 20110195018Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.Type: ApplicationFiled: October 20, 2008Publication date: August 11, 2011Inventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wei Zheng, Wenwei Huang, Gerd Krause, Gunnar Kleinau
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Publication number: 20110190339Abstract: The invention relates to 6-substituted isoquinoline and isoquinolinone derivatives of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: December 16, 2010Publication date: August 4, 2011Applicant: SANOFI-AVENTISInventors: Oliver PLETTENBURG, Katrin LORENZ, Matthias LOEHN, John WESTON, Heinz-Werner KLEEMANN
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Publication number: 20110190341Abstract: The invention relates to substituted isoquinoline and isoquinolinones of the formula (I) useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: June 19, 2009Publication date: August 4, 2011Applicant: SANOFI-AVENTISInventors: Oliver Plettenburg, Katrin Lorenz, John Weston, Matthias Loehn, Heinz-Werner Kleemann, Olivier Duclos, Frederic Jeannot
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Publication number: 20110190340Abstract: The invention relates to bi- and polycyclic substituted isoquinoline and isoquinolinones of the formula (I) wherein R1 to R12 are as defined in the application useful for the treatment and/or prevention of diseases associated with Rho-kinase and/or Rho-kinase mediated phosphorylation of myosin light chain phosphatase, and compositions containing such compounds.Type: ApplicationFiled: June 18, 2009Publication date: August 4, 2011Applicant: SANOFI-AVENTISInventors: Oliver Plettenburg, Katrin Lorenz, Matthias Loehn, Olivier Duclos, Sandrine Biscarrat
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Patent number: 7989471Abstract: Inhibitors of HCV of formula (I) and the N-oxides, salts, and stereochemically isomeric forms thereof, wherein the terms R1, L, R2, R3, R4, and n have specific definitions; pharmaceutical compositions containing compounds of formula (I), and processes for preparing compounds of formula (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.Type: GrantFiled: July 28, 2006Date of Patent: August 2, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Sandrine Marie Helene Vendeville, Lili Hu, Wim Van De Vreken, David Craig McGowan, Abdellah Tahri, Dominique Louis Nestor Ghislain Surleraux
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Publication number: 20110166139Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.Type: ApplicationFiled: June 15, 2009Publication date: July 7, 2011Applicant: ASTRAZENECA ABInventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
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Publication number: 20110166178Abstract: The present invention relates to methods for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo. Methods for treating, pretreating or preconditioning, or preventing erythropoietin-associated conditions are also included. Compounds for use in these methods are provided, as are methods of identifying such compounds.Type: ApplicationFiled: February 17, 2011Publication date: July 7, 2011Applicant: FibroGen, Inc.Inventors: Stephen J. Klaus, Al Y. Lin, Thoams B. Neff, Qingjian Wang, Volkmar Guenzler-Pukall, Michael P. Arend, Lee A. Flippin, Alex Melekhov
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Publication number: 20110160208Abstract: The present invention provides the compounds represented by formula (I): or pharmaceutical salts thereof, wherein: X1 represents oxygen atoms and the like, X2 represents nitrogen atoms and the like, X3 represents nitrogen atoms and the like, X4 represents nitrogen atoms and the like, R1 represents formula (II-1): wherein X5 represents sulfur atoms and the like, A1 represents carbon atoms and the like, A2 represents nitrogen atoms and the like and A ring represents phenyl group and the like, having mGluR1 inhibiting effect, and being useful for preventing or treating convulsion, acute pain, inflammatory pain, chronic pain, brain disorder such as cerebral infarction or transient ischemick attack, psychotic disorder such as schizophrenia, anxiety, drug dependence, Parkinson's disease, or gastrointestinal disorder.Type: ApplicationFiled: March 7, 2011Publication date: June 30, 2011Applicant: Banyu Pharmaceutical Co., Ltd.Inventors: Yukari Hirata, Satoru Ito, Hiroshi Kawamoto, Toshifumi Kimura, Yasushi Nagatomi, Hisashi Ohta, Akio Sato, Atsushi Satoh, Gentaroh Suzuki
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Combination therapy with glatiramer acetate and mitoxantrone for the treatment of multiple sclerosis
Patent number: 7968511Abstract: The subject invention provides a method of treating a subject afflicted with a form of multiple sclerosis comprising periodically administering to the subject an amount of glatiramer acetate and an amount of mitoxantrone, wherein the amounts when taken together are effective to alleviate a symptom of the form of multiple sclerosis in the subject so as to thereby treat the subject. The subject invention also provides a package comprising glatiramer acetate, mitoxantrone and instructions for use of the together to alleviate a symptom of a form of multiple sclerosis in a subject. Additionally, the subject invention provides a pharmaceutical composition comprising an amount of glatiramer acetate and an amount of mitoxantrone, wherein the amounts when taken together are effective to alleviate a symptom of a form of multiple sclerosis in a subject.Type: GrantFiled: May 14, 2004Date of Patent: June 28, 2011Assignee: Teva Pharmaceutical Industries, Ltd.Inventor: Timothy Vollmer -
Publication number: 20110152251Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.Type: ApplicationFiled: November 17, 2010Publication date: June 23, 2011Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
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Publication number: 20110152282Abstract: The invention provides a method, compounds and compositions for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or GIi gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula (I).Type: ApplicationFiled: August 24, 2009Publication date: June 23, 2011Applicant: IRM LLCInventors: Dai Cheng, Dong Han, Guobao Zhang, Yongqin Wan, Yun Feng Xie, Jiqing Jiang, Wenqi Gao, Shifeng Pan
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Patent number: 7964613Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydroType: GrantFiled: February 27, 2008Date of Patent: June 21, 2011Assignee: Asahi Kasei Pharma CorporationInventors: Koki Matsubara, Atsushi Iesato, Akifumi Oomura, Koh Kawasaki, Rintaro Yamada, Minoru Seto
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Publication number: 20110144119Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: July 30, 2009Publication date: June 16, 2011Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
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Publication number: 20110136842Abstract: A series of disubstituted dihydroisoquinolinone and isoquinolinedione derivatives represented by Formula I, or pharmaceutically acceptable salts thereof are presented. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: July 27, 2009Publication date: June 9, 2011Inventors: Joseph L. Duffy, Scott B. Hoyt, Clare London, Christian P. Stevenson, Andres M. Ullman
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Publication number: 20110135599Abstract: The present application includes novel inhibitors of HCV, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: December 1, 2010Publication date: June 9, 2011Applicant: Gilead Sciences, Inc.Inventors: Zhenhong R. Cai, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Mingzhe Ji, Choung U. Kim, Hyung-jung Pyun, Xiaoning C. Sheng, Qiaoyin Wu
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Publication number: 20110130420Abstract: Isoquinolone derivatives of the general formula Ik? are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.Type: ApplicationFiled: April 22, 2009Publication date: June 2, 2011Inventors: Nikolay Khanzhin, Karsten Juhl, Soren Moller Nielsen, Klaus Baek Simonsen
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Publication number: 20110130419Abstract: The invention provides a salt of (R)-3-[2-(2-hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one and a crystal thereof. (R)-3-[2-(2-Hydroxymethylpyrrolidin-1-yl)ethyl]-5-methyl-2H-isoquinolin-1-one monophosphate is a compound which is chemically stable, has high solubility, and shows less weight change due to humidity as compared to a free form and monohydrochloride dihydrate, and is superior as a bulk drug for pharmaceutical products.Type: ApplicationFiled: August 8, 2008Publication date: June 2, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Masakazu Fujio, Toshihiko Tanaka, Hisao Takayanagi, Hiroyuki Satoh, Takanori Ito
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Publication number: 20110130407Abstract: Isoquinolone derivatives of the general formula I are provided. The compounds are NK3 antagonists and useful for the treatment of e.g. psychosis and schizophrenia.Type: ApplicationFiled: June 19, 2009Publication date: June 2, 2011Applicant: H. LUNDBECK A/SInventors: Nikolay Khanzhin, Karsten Juhl, Søren Møller Nielsen, Klaus Baek Simonsen
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Publication number: 20110124663Abstract: In one aspect, the invention relates to compounds having a general structure: wherein the variables are defined herein, which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: November 23, 2010Publication date: May 26, 2011Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Darren W. Engers
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Publication number: 20110118287Abstract: Bicycloheteroaryl compounds are disclosed that have formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: March 16, 2007Publication date: May 19, 2011Applicant: RENOVIS, INC.Inventors: Michael G. Kelly, John Kincaid, Yunfeng Fang, Jianhua He, Yeyu Cao, Carl Kaub, Sumithra Gowlugari
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Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20110105509Abstract: Disclosed are compounds of Formula (I): which are useful as antagonists of the CRTH2 receptors. Pharmaceutical compositions containing compounds of Formula (I) and the use of compounds of Formula (I) to treat diseases or disorders that are responsive to inhibition of the binding of endogenous ligands to the CRTH2 receptor are also disclosed. Methods for preparing and using these compounds are further described.Type: ApplicationFiled: November 3, 2010Publication date: May 5, 2011Applicant: Wyeth, LLCInventors: Neelu Kaila, Eddine Saiah, Bruce Christopher Follows, Adrian Huang, Kristin Marie Janz, Michael Dennis Lowe, Alessandro Fabio Moretto, Jennifer Romanic Thomason, Tarek Suhayl Mansour, Cara Margaret May Williams
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Publication number: 20110098247Abstract: Compounds of formula I are provided: wherein Ar1 and Ar2 are substituted aromatic rings and L1 and L2 are independent divalent linking groups. The compounds are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: ApplicationFiled: October 26, 2010Publication date: April 28, 2011Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Shawn M. Bauer, Anjali Pandey, Carrol Anna Crew Scarborough
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Patent number: 7932266Abstract: The invention relates to derivative compounds of partially-reduced isoquinoline with substitution of a sec-butyl group at position 3 with calpain inhibitor activity. The inventive compound comprises an ester or amide derived from (3-sec-butyl-1-oxo-2,3-dihydro-1H-isoquinolin-4-yliden)-acetic acid and (3-sec-butyl-1-thioxo-2, 3-dihydro-1H-isoquinolin-4-yliden)-acetic acid. Compounds having formula I or II can be used in the preventive or therapeutic treatment of a degenerative disease.Type: GrantFiled: December 5, 2005Date of Patent: April 26, 2011Assignee: Consejo Superior de Investigaciones CientificasInventors: Bernardo Herradon García, Roberto Chicharro Martin, Vicente Jesús Aran Redo, Mercedes Alonso Giner
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Publication number: 20110092476Abstract: Bicycloheteroaryl compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.Type: ApplicationFiled: October 18, 2010Publication date: April 21, 2011Inventors: Michael G. Kelly, John Kincaid, Yunfeng Fang, Jianhua He, Yeyu Cao, Carl Kaub, Sumithra Gowlugari, Zhan Wang
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Publication number: 20110081315Abstract: The embodiments provide compounds of the general Formulae I, Ia, II, III, IV, V, VI-1, VI-2, VII, VIII, IX, X, XI, and XII, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: September 24, 2010Publication date: April 7, 2011Applicant: INTERMUNE, INC.Inventors: Brad Buckman, John B. Nicholas, Leonid Beigelman, Vladimir Serebryany, Antitsa Dimitrova Stoycheva, Timothy Thrailkill, Scott Seiwert
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Patent number: 7919508Abstract: The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.Type: GrantFiled: October 24, 2006Date of Patent: April 5, 2011Assignee: Aventis Pharmaceuticals Inc.Inventors: Gregory Shutske, Keith J. Harris, Kenneth J. Bordeau, Michael R. Angelastro, Stanly John, Joseph T. Klein, Jinqi Lu, Catherine Bomont
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Patent number: 7906655Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: August 5, 2009Date of Patent: March 15, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Makonen Belema, Andrew C. Good, Jason Goodrich, Ramesh Kakarla, Guo Li, Omar D. Lopez, Van N. Nguyen, Jayne Kapur, Yuping Qiu, Jeffrey Lee Romine, Denis R. St. Laurent, Michael Serrano-Wu, Lawrence B. Snyder, Fukang Yang
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Patent number: 7906504Abstract: Disclosed herein are 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivative of formula I, or pharmaceutically acceptable salts or solvates thereof wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions comprising 2-(1-oxo-1H-isoquinolin-2-yl)acetamide derivatives according to the present invention and their use in therapy.Type: GrantFiled: September 10, 2007Date of Patent: March 15, 2011Assignee: N.V. OrganonInventors: Jeffrey Letourneau, Jui-Hsiang Chan, Patrick Jokiel, Michael Ohlmeyer, Irina Neagu, Christopher Riviello, John Richard Morphy, Susan Elizabeth Napier, Koc-Kan Ho
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Patent number: 7902223Abstract: Novel compounds of the formula (I), in which D, W, X, Y, T and R1 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.Type: GrantFiled: July 12, 2002Date of Patent: March 8, 2011Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Bertram Cezanne, Christos Tsaklakidis, Werner Mederski, Johannes Gleitz, Christopher Barnes
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Publication number: 20110053975Abstract: The present invention relates to a compound of one of the formulas I to XXI; a pharmaceutical composition comprising at least one such compound; and the use of at least one such compound in preparing a drug to treat, in a subject, a genetic disease resulting from at least one splicing anomaly.Type: ApplicationFiled: January 12, 2009Publication date: March 3, 2011Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS, INSTITUT CURIE, UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUESInventors: Jamal Tazi, David Grierson, Florence Mahuteau-Betzer, Pierre Roux
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Patent number: 7897618Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: where the variables are as define herein, and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: October 29, 2007Date of Patent: March 1, 2011Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Patent number: 7893088Abstract: The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such asType: GrantFiled: August 16, 2007Date of Patent: February 22, 2011Assignee: N.V. OrganonInventors: Peter Christopher Ray, Steven Laats, John Richard Morphy, Brad Sherborne
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Publication number: 20110039886Abstract: The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.Type: ApplicationFiled: July 12, 2010Publication date: February 17, 2011Inventors: Stephen J. Klaus, Christopher J. Molineaux, Thomas B. Neff, Volkmar Guenzler-Pukall, Ingrid Langsetmo Parobok, Todd W. Seeley, Robert C. Stephenson
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Publication number: 20110039878Abstract: The present invention provides methods and medicaments for reducing blood pressure. Methods and medicaments for treating or preventing hypertension are also provided.Type: ApplicationFiled: November 3, 2008Publication date: February 17, 2011Inventors: Volkmar Guenzler-Pukall, Qingjian Wang, Ingrid Langsetmo Parobok, Guangjie Guo
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Publication number: 20110039827Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, m, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: June 21, 2010Publication date: February 17, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Jeffrey P. Ciavarri, Kenneth M. Gigstad, He Xu
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Publication number: 20110034507Abstract: The present invention relates to farnesoid X receptors (FXR, NR1H4). FXR is a member of the nuclear receptor class of ligand-activate transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same. Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease, liver fibrosis, and metabolic syndrome.Type: ApplicationFiled: June 13, 2008Publication date: February 10, 2011Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Adwoa Akwabi-Ameyaw, David Norman Deaton, Robert Blount McFadyen, Frank Navas, III
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Publication number: 20110028420Abstract: A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.Type: ApplicationFiled: April 7, 2009Publication date: February 3, 2011Inventors: Hamid A. Boulares, Chetan P. Hans, Amarjit S. Naura
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Patent number: 7879876Abstract: The present invention is related to sulfonamide derivatives of Formula (Ia) where the groups are as defined in the description, and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: October 24, 2006Date of Patent: February 1, 2011Assignee: Merck Serono SAInventors: Patrick Gerber, Dominique Swinnen, Agnes Bombrun
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Patent number: 7879891Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: GrantFiled: July 20, 2006Date of Patent: February 1, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Publication number: 20110021462Abstract: This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments. These compounds are poly(ADP-ribose) polymerase (PARP) inhibitors.Type: ApplicationFiled: August 4, 2010Publication date: January 27, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Stefan PEUKERT, Stefan GUESSREGEN, Armin HOFMEISTER, Herman SCHREUDER, Uwe SCHWAHN
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Publication number: 20110021505Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.Type: ApplicationFiled: March 30, 2010Publication date: January 27, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Karl RUDOLPHI, Martin MICHAELIS, Hans GUEHRING
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Publication number: 20110020460Abstract: Compounds of Formula I that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: June 4, 2010Publication date: January 27, 2011Inventors: Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20110015223Abstract: The invention relates to methods and compounds for treating anemia of cancer. In particular, methods for treating anemia of cancer in a subject having cancer, and methods for increasing reticulocytes, increasing hemoglobin, increasing hematocrit, and increasing red blood cell count in subjects having anemia of cancer, wherein such subjects are refractory to treatment with recombinant human erythropoietin (EPO) are encompassed herein.Type: ApplicationFiled: August 16, 2010Publication date: January 20, 2011Applicant: FibroGen, Inc.Inventors: Todd W. Seeley, David Y. Liu, Stephen J. Klaus
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Publication number: 20110003843Abstract: The present invention relates to a compound derived from indole corresponding to the following formula II: wherein X represents N, CR8 or N+R8, wherein R8 represents a hydrogen atom, a hydroxyl or alkyl or methoxy group optionally substituted with a phenyl group; R2, R3 and R4 independently represent a hydrogen atom or a halogen atom or an optionally substituted alkyl, amine, alkene, ester, sulfonamide, ether or benzyl group; R5 represents a hydrogen atom or an optionally substituted, saturated or unsaturated alkyl group, amine, benzyl group; R6 represents an optionally substituted C1-C3 alkyl group; R7 represents a hydrogen atom or an optionally substituted C1-C3 alkyl group and R7 is absent when the ring A is in the b position, and A represents a ring; R9 and R10 represent together a carbon bond or independently represent an R11 OR11, SR11 group; wherein R11 represents a hydrogen atom, an optionally substituted, saturated or unsaturated, C1-C3 alkyl group, which may contain one or more sulfur, oxygen orType: ApplicationFiled: February 19, 2008Publication date: January 6, 2011Inventors: Fabrice Lejeune, Jamal Tazi, David Grierson, Christian Rivalle, Florence Mahuteau-Betzer
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Publication number: 20100331298Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: December 10, 2008Publication date: December 30, 2010Applicant: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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Publication number: 20100331362Abstract: The present invention relates to improved methods for treating anemia. Methods and compounds useful for treating anemia, wherein the anemia treatment is associated with a lower risk of thrombosis or hypertension compared to that observed with rhEPO therapy, are provided.Type: ApplicationFiled: August 26, 2010Publication date: December 30, 2010Applicant: FibroGen, Inc.Inventors: Stephen J. Klaus, Thomas B. Neff