Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/309)
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Patent number: 8143274Abstract: The present invention provides: a compound represented by the following formula (I): [wherein Y1 and Y4 represent a hydrogen atom or a halogen atom; either one of Y2 and Y3 represents —NR1R2, and the other represents a hydrogen atom or a halogen atom; X represents an aryl group or a heteroaryl group that may be substituted; R1 represents a hydrogen atom, or a C1-8 alkyl group that may be substituted; and R2 represents a C1-8 alkyl group that is substituted with one or more substituents, —COOR3, —COR4, —COSR5, —CONR6R7, —NR22R23, or —C?NR24R25; or R1 and R2, together with a nitrogen atom to which they are bonded, may form a 4- to 10-membered hetero ring containing at least one nitrogen atom (wherein the hetero ring may be substituted with one or more substituents selected from Group C)], a prodrug thereof, or a pharmaceutically acceptable salt thereof; and a pharmaceutical, a pharmaceutical composition, or the like, which comprises the compound.Type: GrantFiled: February 7, 2005Date of Patent: March 27, 2012Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kazuo Hattori, Satoshi Niizuma, Takehiro Okada, Hiroyuki Eda, Kenji Tatsuno, Miyuki Yoshida
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Publication number: 20120071503Abstract: The disclosure provides compounds and compositions, and methods of using these compounds and compositions, as positive allosteric modulators of the metabotropic glutamate subtype 2 (mGlu2) receptor, and for treating CNS disorders associated with the mGlu2 receptor including schizophrenia, anxiety, addiction, e.g. cocaine addiction, nicotine addiction, and the like.Type: ApplicationFiled: March 18, 2011Publication date: March 22, 2012Applicant: Sanford-Burnham Medical Research InstituteInventors: Nicholas D. P. Cosford, Dhanya Raveendra Panickar, Shyama Sidique
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Publication number: 20120071466Abstract: The compounds of formula (I) are derived from perhydroquinoline and perhydroisoquinoline and are useful as active pharmaceutical ingredients for the prophylaxis or treatment of diseases caused by 11-beta-hydroxysteroid dehydrogenase type I (11-beta-HSD1) enzyme-associated disorders, such as glaucoma, elevated ocular pressure, metabolic disorders, obesity, metabolic syndrome, dyslipidemia, hypertension, diabetes, atherosclerosis, Cushing's syndrome, psoriasis, rheumatoid arthritis, cognitive disorders, Alzheimer's disease or neurodegeneration.Type: ApplicationFiled: June 4, 2010Publication date: March 22, 2012Inventors: Juan Lorenzo Catena Ruiz, Carme Serra Comas, Oscar Rey Puiggros, Albert Antolin Hernandez, Esther Monlleomas
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Publication number: 20120071475Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 26, 2010Publication date: March 22, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata
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Publication number: 20120065185Abstract: Selected heterocyclic compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like.Type: ApplicationFiled: November 15, 2011Publication date: March 15, 2012Applicant: Amgen Inc.Inventors: Guoqing CHEN, Jeffrey Adams, Jean Bemis, Shon Booker, Guolin Cai, Lucian Di Pietro, Celia Dominguez, Daniel Elbaum, Julie Germain, Stephanie Geuns-Meyer, Michael Handley, Qi Huang, Joseph L. Kim, Tae-Seong Kim, Alexander Kiselyov, Xiaohu Ouyang, Vinod F. Patel, Leon M. Smith, Markian Stec, Andrew Tasker, Ning Xi, Shimin Xu, Chester Chenguang Yuan, Michael Croghan
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Publication number: 20120059002Abstract: Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.Type: ApplicationFiled: April 21, 2010Publication date: March 8, 2012Inventors: Henrik C. Hansen, Gregory S. Wagner, Sarah C. Attwell, Kevin G. McLure, Ewelina B. Kulikowski
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Publication number: 20120053192Abstract: This present invention discloses a heterocyclic substituted acardite derivate and application thereof, namely compounds in the general formula (1) or the general formula (2) or pharmaceutically acceptable salts thereof, wherein A is monosubstituted or polysubstituted quinoline, isoquinoline, quinazoline, pyrrole or pyrimidine, and the substituent is halogen, C1-5alkyl, C1-5haloalkyl, C1-5alkoxy, C1-5haloalkoxy, C1-5alkylamino, C1-5haloalkylamino, amino or nitryl; R1 is C1-5alkyl; R2 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy; and R3 is one or more selected from hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy. The compound of the present invention and the pharmaceutically acceptable salt thereof can be used for treating tumor or leukemia.Type: ApplicationFiled: May 4, 2010Publication date: March 1, 2012Applicants: Nanjing Luyesike Pharmaceutical Co., Ltd., Jiangsu Provincial Institute of Materia Medica Co. Ltd.Inventors: Aihua Zhang, Shengtao Yuan, Guang Cheng, Yipeng Shen, Ancheng Ji
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Publication number: 20120053203Abstract: The invention relates to substituted 1-oxo-dihydroisoquinoline-3-carboxamides, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: August 31, 2011Publication date: March 1, 2012Applicant: Grunenthal GmbHInventors: Sven KÜHNERT, Gregor BAHRENBERG, Achim KLESS, Wolfgang SCHRÖDER
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Publication number: 20120046467Abstract: [Problem] The object of the present invention is to provide a novel compound having 132 adrenergic receptor agonist activity and muscarinic receptor antagonist activity. [Means for Solving the Problem] The present invention is a quaternary ammonium salt compounds represented by formula (I), or a pharmaceutically acceptable salt thereof, with superior ?32 adrenergic receptor agonist activity and muscarinic receptor antagonist activity.Type: ApplicationFiled: April 27, 2010Publication date: February 23, 2012Applicant: TEIJIN PHARMA LIMITEDInventors: Etsuko Mitsuyama, Takayuki Hara, Junji Igarashi, Hiroyuki Sugiyama, Satoshi Yamamura, Johji Nomura, Kei Segawa
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Publication number: 20120046242Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: December 21, 2009Publication date: February 23, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. BIechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20120028956Abstract: In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: October 10, 2011Publication date: February 2, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20120028955Abstract: In one aspect, the invention relates to bicyclic mGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: October 10, 2011Publication date: February 2, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20120029011Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.Type: ApplicationFiled: July 19, 2011Publication date: February 2, 2012Inventors: Michael P. Arend, Lee A. Flippin, Volkmar Guenzler-Pukall, Wen-Bin Ho, Eric D. Turtle, Xiaohui Du
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Publication number: 20120015952Abstract: The invention relates to compounds of formulae (1) and (2): and pharmaceutically acceptable salts thereof for the treatment of cancer, inflammation, auto-immune diseases, diabetes and diabetic complications, infection, cardiovascular disease and ischemia-reperfusion injuries.Type: ApplicationFiled: March 25, 2010Publication date: January 19, 2012Applicant: Profectus Biosciences, Inc.Inventors: Jie Zhang, Drago Robert Sliskovic, Charles E. Ducker
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Patent number: 8097627Abstract: The invention relates to multiply-substituted tetrahydronaphthalene derivatives of formula (I) process for their production and their use as anti-inflammatory agents.Type: GrantFiled: December 18, 2009Date of Patent: January 17, 2012Assignee: Bayer Pharma AGInventors: Hartmut Rehwinkel, Stefan Baeurle, Markus Berger, Norbert Schmees, Heike Schaecke, Konrad Krolikiewicz, Anne Mengel, Duy Nguyen, Stefan Jaroch, Werner Skuballa
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Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
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Patent number: 8093273Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.Type: GrantFiled: October 20, 2005Date of Patent: January 10, 2012Assignee: Resverlogix Corp.Inventors: Norman C. W. Wong, Joseph E. L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
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Patent number: 8093288Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.Type: GrantFiled: November 19, 2009Date of Patent: January 10, 2012Assignees: Beth Israel Deaconess Medical Center, Trustees of Boston UniversityInventors: Chen-Yu Zhang, Bradford B. Lowell, John A Porco, Jr., Ruichao Shen, Cheng T. Lin, Stefan Krauss
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Patent number: 8093265Abstract: 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: GrantFiled: March 7, 2008Date of Patent: January 10, 2012Assignee: Renovis, Inc.Inventors: Michael G. Kelly, John Kincaid, Yunfeng Fang, Yeyu Cao, Carl Kaub, Sumithra Gowlugari, Zhan Wang
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Patent number: 8093258Abstract: The present invention relates to methods and compositions for the treatment and/or prevention of neuropathological and/or neurodegenerative diseases. In particular, the invention delivers novel uses of inhibitors of Urokinase-type Plasminogen activator in the treatment of amyotrophic lateral sclerosis.Type: GrantFiled: June 22, 2006Date of Patent: January 10, 2012Assignee: Wilex AGInventors: Stefan Lorenzl, Wolfgang Schmalix
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Publication number: 20120004167Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: July 5, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Elisabeth DEFOSSA, Stefanie KEIL, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Publication number: 20120004166Abstract: The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and A are each defined as specified, and physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.Type: ApplicationFiled: July 5, 2011Publication date: January 5, 2012Applicant: SANOFIInventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
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Patent number: 8084047Abstract: The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.Type: GrantFiled: July 23, 2009Date of Patent: December 27, 2011Assignee: Sarcode Bioscience Inc.Inventors: Wang Shen, Johan D. Oslob, Kenneth Barr, Min Zhong
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Publication number: 20110311519Abstract: Methods of reducing bone loss and treating degenerative bone diseases such as osteoporosis are disclosed. The methods comprise administration of an agent that inhibits signaling through the IL-17 pathway, such as an antibody or a quinazoline analogue such as halofuginone.Type: ApplicationFiled: June 17, 2011Publication date: December 22, 2011Applicant: Washington UniversityInventors: Steven L. Teitelbaum, Carl J. DeSelm
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Publication number: 20110311482Abstract: Hepatitis C virus inhibitors are disclosed having the general formula: wherein R1, R2, R3, R?, B, Y and X are described in the description. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: December 13, 2010Publication date: December 22, 2011Inventors: Xiangdong Alan Wang, Li-Qiang Sun, Sing-Yuen Sit, Ny Sin, Paul Michael Scola, Yan Chen
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Publication number: 20110301172Abstract: The invention relates to a combination, such as a combined preparation or pharmaceutical composition, respectively, which comprises; 1) a dipeptidylpeptidase-IV (DPP-IV) inhibitor, 2) one antidiabetic selected from thiazolidinediones (glitazones), non-glitazone type PPAR? agonists, PPAR? agonists or dual PPAR?/PPAR? agonists, and 3) metformin, for simultaneous, separate or sequential use, especially in the prevention, delay of progression or treatment of conditions mediated by dipeptidylpeptidase-IV (DPP-IV), in particular diabetes, more particular type 2 diabetes mellitus, conditions of impaired glucose tolerance (IGT), conditions of impaired fasting plasma glucose, metabolic acidosis, ketosis, arthritis, obesity and osteoporosis; the use of such combination for the preparation of a pharmaceutical preparation for the prevention, delay of progression or treatment of such conditions; the use of such combination for the cosmetic treatment of a mammal in order to effect a cosmetically beneficial loss of body wType: ApplicationFiled: August 15, 2011Publication date: December 8, 2011Inventors: Bryan Burkey, Thomas Edward Hughes
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Patent number: 8071618Abstract: The present invention provides a compound of formula I: wherein: X is —OR1 or —N(R5)2, Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkenyl, or alkynyl, wherein the alkyl, alkenyl, or alkynyl is optionally substituted with optionally substituted aryl, CF3, CI, F, OMe, OEt, OCF3, CN, or NMe2; C1-6 cycloalkyl, wherein 1-2 carbon atoms in the cycloalkyl is optionally replaced with —O— or —NR5—; R2 is C1-6 straight chained or branched alkyl; Art Unit 1625 R3 is hydrogen, halo, OCF3, CN, or CF3; R4 is hydrogen, halo, OCF3, CN, or CF3; and each R5 is independently H, C1-6 straight chained or branched alkyl, aryl, —O—C1-6 straight chained or branched alkyl, or —O-aryl. The present invention also provides pharmaceutical compositions and methods using such compositions for treating a caspase-mediated disease, particularly in the central nervous system.Type: GrantFiled: September 18, 2009Date of Patent: December 6, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean Damien Charrier, Michael Mortimore, John Studley
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Patent number: 8067457Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein X, n, Y, and R1 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR2 and accordingly are useful for the treatment of a variety of inflammatory, allergic, and autoimmune diseases, disorders, or conditions.Type: GrantFiled: October 26, 2006Date of Patent: November 29, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Shomir Ghosh, Prakash Raman, Kevin Sprott, Amy M. Elder, Sian Griffiths, Francois Soucy, Qing Ye
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Publication number: 20110288120Abstract: Isoquinolone derivatives of the general formula (I) are NK3 antagonists.Type: ApplicationFiled: October 16, 2009Publication date: November 24, 2011Applicant: H. Lundbeck A/SInventors: Nikolay Khanzhin, Karsten Juhl, Soren Moller Nielsen, Klaus Baek Simonsen
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Publication number: 20110281853Abstract: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.Type: ApplicationFiled: May 12, 2011Publication date: November 17, 2011Inventors: Rishi Arora, David E. Zembower
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Publication number: 20110280941Abstract: The present invention relates to compositions, kits and methods of treating diabetes. More specifically, compositions of at least one proton pump inhibitor and at least one insulin secretagogue, kits and methods of their use to treat diabetes.Type: ApplicationFiled: December 11, 2009Publication date: November 17, 2011Applicant: Mefford Scientific, LLCInventor: Ivan Newton Mefford
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Publication number: 20110275612Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.Type: ApplicationFiled: May 14, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
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Publication number: 20110275608Abstract: A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.Type: ApplicationFiled: January 7, 2010Publication date: November 10, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Martha E. Rodriguez, David A. Mareska, Jeremy J. Hans, Darren M. Harvey, Robert D. Groneberg, Michael O'Sullivan
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Patent number: 8048862Abstract: The embodiments provide compounds of the general Formulae I, II, III, IV, V, VI, VII, and X, 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: GrantFiled: April 14, 2009Date of Patent: November 1, 2011Assignee: InterMune, Inc.Inventors: Scott D. Seiwert, Leonid Beigelman, Brad Buckman, Antitsa Dimitrova Stoycheva, Steven B. Porter, Williamson Ziegler Bradford, Vladimir Serebryany
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Publication number: 20110263643Abstract: The present invention is directed to 2,3-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.Type: ApplicationFiled: October 15, 2009Publication date: October 27, 2011Inventors: Christopher D. Cox, Broc Flores, John D. Schreier
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Publication number: 20110263644Abstract: The present invention relates to methods and agents useful for the treatment of stroke, including ischemic stroke and hemorrhagic stroke. In particular, methods and agents for treating stroke in a subject are provided, wherein the agent is administered prior to diagnosis of the stroke as an ischemic stroke or a hemorrhagic stroke.Type: ApplicationFiled: July 11, 2011Publication date: October 27, 2011Applicant: FibroGen, Inc.Inventors: Stephen J. Klaus, Ingrid Langsetmo Parobok, Christopher T. Jacob
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Publication number: 20110263642Abstract: The present invention relates to methods and compounds useful for treating multiple sclerosis.Type: ApplicationFiled: August 26, 2009Publication date: October 27, 2011Applicant: FibroGen, Inc.Inventors: Stephen J. Klaus, Thomas B. Neff, Gail Walkinshaw
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Publication number: 20110263597Abstract: Methods of treating a mammal having a condition characterized by abnormal angiogenesis or hyperpermiability processes using substituted pyridazines having angiogenesis inhibiting activity and the generalized structural formula wherein the ring containing A, B, D, E, and L is phenyl or a nitrogen-containing heterocycle; groups X and Y may be any of a variety of defined linking units; R1 and R2 may be defined independent substituents or together may be a ring-defining bridge; ring J may be an aryl, pyridyl, or cycloalkyl group; and G groups may be any of a variety of defined substituents.Type: ApplicationFiled: July 7, 2011Publication date: October 27, 2011Applicant: Bayer HealthCare LLCInventors: Jacques P. Dumas, Stephen James Boyer, Julie A. Dixon, Teddy Kite Joe, Harold C. E. Kluender, Wendy Lee, Dhanapalan Nagarathnam, Robert N. Sibley, Ning Su
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Patent number: 8044067Abstract: Compounds of the formula (I): were synthesized. In at least one embodiment, they were found to down-regulate or inhibit the expression or function of the IGF-1 receptor.Type: GrantFiled: September 8, 2006Date of Patent: October 25, 2011Assignee: Analytecon S.A.Inventors: Jan Gunzinger, Kurt Leander
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Patent number: 8039484Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.Type: GrantFiled: October 26, 2007Date of Patent: October 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
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Publication number: 20110250176Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit Hepatitis C virus (HCV), compositions comprising such compounds, and methods for treating Hepatitis C using such combinations.Type: ApplicationFiled: October 7, 2010Publication date: October 13, 2011Inventors: Julie A. Lemm, Stacey A. Voss, Min Gao, Susan E. Chaniewski, Amy K. Sheaffer, Fiona McPhee
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Publication number: 20110251226Abstract: The invention relates to 6-cyclohexylamine-substituted isoquinolone derivatives of the formula (I) or isoquinoline 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: June 15, 2011Publication date: October 13, 2011Applicant: SANOFI-AVENTISInventors: Oliver Plettenburg, Armin Hofmeister, Dieter Kadereit, Stefan Peukert, Sven Ruf, Kurt Ritter, Matthias Loehn, Yuri Ivashchenko, Peter Monecke, Matthias Dreyer, Aimo Kannt
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Patent number: 8034806Abstract: In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. 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: GrantFiled: October 31, 2008Date of Patent: October 11, 2011Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Publication number: 20110245247Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: March 28, 2011Publication date: October 6, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker
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Publication number: 20110237621Abstract: Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(?O)—, —O—C(?O)—NR4a— or —O—C(?O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(?O)OR5, —C(?O)R6, —C(?O)NR4aR4b, —C(?O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and wheType: ApplicationFiled: May 17, 2011Publication date: September 29, 2011Inventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Åsa Annica Kristina Rosenquist, Dmitry Antonov
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Publication number: 20110230457Abstract: The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: ApplicationFiled: December 20, 2010Publication date: September 22, 2011Applicant: NOVARTIS AGInventors: Joerg BERGHAUSEN, Nicole BUSCHMANN, Pascal FURET, François GESSIER, Joanna HERGOVICH LISZTWAN, Philipp HOLTZER, Edgar JACOBY, Joerg KALLEN, Keiichi MASUYA, Carole PISSOT SOLDERMANN, Haixia REN, Stefan STUTZ
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Publication number: 20110230472Abstract: It is an object of the present invention to provide a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a ring-fused azole compound shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 25, 2009Publication date: September 22, 2011Applicant: Shionogi & Co., Ltd.Inventors: Yasunori Mitsuoka, Manami Masuda, Daisuke Taniyama
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Publication number: 20110224208Abstract: The present invention relates to a series of Isoquinolone derivatives which are suitable to treat infections with viruses belonging to the family of the Flaviviridae and more preferably infections with Hepatitis C virus (HCV). The present invention also relates to Isoquinolone compounds for use as a medicine for the prevention or treatment of viral infections, preferably infections with viruses belonging to the family of the Flaviviridae.Type: ApplicationFiled: November 16, 2009Publication date: September 15, 2011Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U. LEUVEN R&DInventors: Dorothée Bardiot, Emilie Blanche, Patrick Chaltin, Mohamed Koukni, Pieter Leyssen, Johan Neyts, Arnaud Marchand, Inge Vliegen
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Patent number: 8017625Abstract: The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.Type: GrantFiled: January 16, 2008Date of Patent: September 13, 2011Assignee: Fibrogen, Inc.Inventors: Michael P. Arend, Lee A. Flippin, Volkmar Guenzler-Pukall, Web-Bin Ho, Eric Turtle, Xiaohui Du
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Patent number: 8012979Abstract: The present invention relates to isoquinolinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: April 4, 2008Date of Patent: September 6, 2011Assignee: AstraZeneca ABInventors: Matthew Hallam, Barrie Martin, Piotr Raubo, Bryan Roberts, Stephen St-Gallay, Paul Willis