Halogen Or Nitrogen Attached Directly To Diazine Ring Carbon By Nonionic Bonding Patents (Class 544/356)
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Publication number: 20120232084Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: ApplicationFiled: May 23, 2012Publication date: September 13, 2012Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20120225874Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutical composition thereof, with all the variables being defined in the text. The present invention further relates to the use of the compounds herein for treatment of or delay progression to overt to diseases in which CETP is involved.Type: ApplicationFiled: May 17, 2012Publication date: September 6, 2012Applicant: NOVARTIS AGInventors: Masashi KISHIDA, Naoko MATSUURA, Hidetomo IMASE, Yuki IWAKI, Ichiro UMEMURA, Osamu OHMORI, Eiji KAWAHARA
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Publication number: 20120225863Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
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Publication number: 20120211736Abstract: A compound for an organic photoelectric device, the compound being represented by the following Chemical Formula (“CF”) 1:Type: ApplicationFiled: May 3, 2012Publication date: August 23, 2012Applicant: CHEIL INDUSTRIES, INC.Inventors: Hyung-Sun KIM, Eun-Sun YU, Soo-Hyun MIN, Ho-Jae LEE, Eui-Su KANG, Mi-Young CHAE, Young-Hoon KIM, Ja-Hyun KIM
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Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
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Publication number: 20120202783Abstract: Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo[3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 9, 2012Inventors: Bryan James Branstetter, Michael A. Letavic, Kiev S. Ly, Dale A. Rudolph, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman
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Publication number: 20120196845Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Patent number: 8231984Abstract: Target is to provide an organic compound material having a bipolar character. A quinoxaline derivative represented by a general formula (1) is provided. In the formula, R1-R12 each independently represents a hydrogen atom, a halogen atom, a lower alkyl group, an alkoxy group, an acyl group, a nitro group, a cyano group, an amino group, a dialkylamino group, a diarylamino group, a vinyl group, an aryl group, or a heterocyclic residue group. R9 and R10, R10 and R11, and R11 and R12 are each independent or respectively mutually bonded to form an aromatic ring. Ar1-Ar4 each independently represents an aryl group or a heterocyclic residue group. Ar1, Ar2, Ar3 and Ar4 are each independent or Arl and Ar2, and Ar3 and Ar4 are respectively mutually bonded directly, or Ar1 and Ar3, and Ar3 and Ar4 are bonded via oxygen (O), sulfur (S) or a carbonyl group.Type: GrantFiled: September 11, 2009Date of Patent: July 31, 2012Assignee: Semiconductor Energy Laboratory Co., Ltd.Inventors: Satoko Shitagaki, Atsushi Tokuda, Hiroko Abe, Ryoji Nomura, Satoshi Seo
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Publication number: 20120165318Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: February 29, 2012Publication date: June 28, 2012Applicant: BIOENERGENIXInventors: John M. McCall, John McKearn, Donna L. Romero, Michael Clare
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Patent number: 8193199Abstract: Substituted bicyclic heteroaryls having the structures: and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid LeukemiType: GrantFiled: March 24, 2008Date of Patent: June 5, 2012Assignee: Amgen Inc.Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
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Publication number: 20120108596Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: April 29, 2011Publication date: May 3, 2012Inventors: Kimberley A. Lentz, Rex Denton, James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Robert A. Mate, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor, Matthew D. Hill, Haiquan Fang
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Publication number: 20120101103Abstract: Compounds of Formula I: (I) in which A, A1, R1, R7a, R7b, R8 and R10 have the meanings given in the specification, are DP2 receptor inhibitors useful in the treatment of useful in the treatment and prevention of immunologic diseases, allergic diseases such as asthma, allergic rhinitis and atopic dermatitis, and other inflammatory diseases mediated by prostaglandin D2 (PGD2). The compounds of Formula I may also be useful in treating diseases or medical conditions involving the Th2 T cell via production of IL-4, IL-5 and/or IL-13.Type: ApplicationFiled: December 18, 2009Publication date: April 26, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Adam Cook, Kevin W. Hunt, Robert Kirk Delisle, Todd Romoff, Christopher T. Clark, Ganghyeok Kim, Christopher P. Corrette, George A. Doherty, Laurence E. Burgess
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Publication number: 20120094976Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.Type: ApplicationFiled: April 19, 2011Publication date: April 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Christiane Kofink, Darryl McConnell
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Publication number: 20120071478Abstract: The invention provides compounds of the formula (1): or salts or tautomers thereof; wherein X1 is N or N+(O?); X2 is N or CH; Q is a C1-3 alkylene group; R1 is selected from hydrogen, C1-4 hydrocarbyl and hydroxy-C2-4 hydrocarbyl; R2, R3 and R4 are the same or different and each is selected from hydrogen, fluorine, chlorine and methyl; Ar1 is an optionally substituted monocyclic 5 or 6-membered aryl or heteroaryl ring containing 0, 1 or 2 heteroatom ring members selected from O, N and S, or a naphthyl ring and Ar2 is an optionally substituted monocyclic 5 or 6-membered heteroaryl ring containing 1, 2 or 3 heteroatom ring members selected from O, N and S. The compounds of formula (1) are inhibitors of p70S6 kinase and are useful in the treatment of proliferative diseases.Type: ApplicationFiled: May 26, 2010Publication date: March 22, 2012Applicant: Sentinel Oncology LimitedInventors: Robert George Boyle, David Winter Walker
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Publication number: 20120015950Abstract: Compound corresponding to general formula (I): in which R2 is a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or NR8R9 group; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C1-8-alkylene group; R1 is a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; R3 is a hydrogen or fluorine atom, a C1-6-alkyl group or a tritluoromethyl group; R4 is a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or oType: ApplicationFiled: November 13, 2009Publication date: January 19, 2012Applicant: SANOFI-AVENTISInventors: Ahmed Abouabdellah, Nathalie Chereze, Aude Fayol, Mourad Saady, Julien Vache, Corinne Veronique, Philippe Yaiche
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Publication number: 20110312960Abstract: The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: August 31, 2011Publication date: December 22, 2011Applicant: MERCK SERONO SAInventors: Pascale Gaillard, Anna Quattropani, Vincent Pomel, Thomas Rueckle, Jasna Klicic, Dennis Church
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Publication number: 20110306587Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 11, 2011Publication date: December 15, 2011Inventors: Jennifer R. ALLEN, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
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Publication number: 20110306588Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 12, 2011Publication date: December 15, 2011Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Patent number: 8063045Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.Type: GrantFiled: February 1, 2010Date of Patent: November 22, 2011Assignee: Sanofi-AventisInventors: Peter Aranyi, Laszlo Balazs, Imre Bata, Sandor Batori, Eva Boronkay, Philippe Bovy, Karoly Kanai, Zoltan Kapui, Edit Susan, Tibor Szabo, Lajos T. Nagy, Katalin Urban-Szabo, Marton Varga
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Publication number: 20110244486Abstract: Methods, assays and compositions for the diagnosis and treatment of diabetes, in which the glutamate transporters and/or receptors expressed in pancreatic islet cells are used as therapeutic targets or tools for the identification or treatment of individuals suffering from or susceptible to diabetes.Type: ApplicationFiled: November 20, 2009Publication date: October 6, 2011Inventors: Carla Perego, Eliana Sara Di Cairano, Alberto Davalli, Franco Folli
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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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Patent number: 8030495Abstract: The present invention is directed to cyclopropyl proline bis-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: GrantFiled: May 19, 2008Date of Patent: October 4, 2011Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Publication number: 20110218200Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.Type: ApplicationFiled: August 28, 2009Publication date: September 8, 2011Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
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Publication number: 20110207712Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.Type: ApplicationFiled: April 28, 2011Publication date: August 25, 2011Applicant: Exelixis, Inc.Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
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Publication number: 20110190241Abstract: Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.Type: ApplicationFiled: May 14, 2009Publication date: August 4, 2011Inventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
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Patent number: 7989622Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.Type: GrantFiled: October 9, 2006Date of Patent: August 2, 2011Assignee: Exelixis, Inc.Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison B. Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
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Publication number: 20110172236Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. 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: September 21, 2009Publication date: July 14, 2011Inventors: Prasun K. Chakravarty, Joseph L. Duffy, Pengcheng Patric Shao
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Publication number: 20110160214Abstract: The invention provides compositions and methods for whitening of eyes. The provided compositions and methods utilize low concentrations of selective ?-2 adrenergic receptor agonists. The compositions preferably include brimonidine.Type: ApplicationFiled: December 17, 2010Publication date: June 30, 2011Inventor: Gerald Horn
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Publication number: 20110101312Abstract: This invention relates to deuterated indolocarbazole compounds that are useful in electronic applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.Type: ApplicationFiled: December 21, 2009Publication date: May 5, 2011Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: Daniel David LeCloux, Kalindi Dogra, Weishi Wu, Adam Fenninmore, Eric Maurice Smith
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Publication number: 20110105513Abstract: Compounds of the Formula (I), where W represents CH or N; and Q represents —CN, —C(?NOH)NH2, —CONHR1 or various herein described heterocyclic radicals; as well as pharmaceutically acceptable salts, solvates, esters and prodrugs thereof. Care adenosine A2a receptor antagonists and, therefore, are useful in the treatment of central nervous system diseases, in particular Parkinson's disease.Type: ApplicationFiled: March 3, 2009Publication date: May 5, 2011Inventors: Joel M. Harris, Bernard R. Neustadt, Hong Liu, Jinsong Hao, Andrew W. Stamford
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Publication number: 20110071154Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: ApplicationFiled: December 2, 2010Publication date: March 24, 2011Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 7897627Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.Type: GrantFiled: December 15, 2008Date of Patent: March 1, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20110039857Abstract: The invention relates to piperidine and pyrrolidine compounds of formula (I) wherein A, B, n and X are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.Type: ApplicationFiled: April 29, 2009Publication date: February 17, 2011Inventors: Hamed Aissaoui, Christoph Boss, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
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Patent number: 7863291Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: GrantFiled: April 14, 2009Date of Patent: January 4, 2011Assignee: Bristol-Myers Squibb CompanyInventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
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Publication number: 20100314615Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.Type: ApplicationFiled: December 22, 2008Publication date: December 16, 2010Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Yumiko Mizuki, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
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Publication number: 20100266538Abstract: The invention provides quinoxalines of the general formula I which are used as medicaments preferably for treating tumour disorders, in particular in cases of drug resistance to other active compounds and in cases of metastasic carcinoma. The possible applications are not limited to tumour disorders.Type: ApplicationFiled: March 25, 2010Publication date: October 21, 2010Applicant: AETERNA ZENTARIS GmbHInventors: Matthias Gerlach, Irene Seipelt, Eckhard Guenther, Tilmann Schuster, Emmanuel Polymeropoulos, Michael Czech, Eckhard Claus
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Publication number: 20100266539Abstract: The present invention relates to a compound represented by formula (I), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medical use thereof (the symbols in the formula are as described in the specification). The compound represented by formula (I) has chemokine receptor (especially in CCR4 and/or CCR5) antagonistic activity. Therefore it is useful for prevention and/or treatment of a chemokine receptor-mediated disease such as inflammatory and/or allergic diseases [systemic inflammatory response syndrome (SIRS), anaphylaxis, anaphylactoid reaction, allergic angiitis, transplant rejection reaction, hepatitis, nephritis, nephropathy, pancreatitis, rhinitis, arthritis, inflammatory ocular disease, inflammatory bowel disease, disease in cerebro and/or circulatory system, respiratory disease, dermatosis, autoimmune disease, and the like], infection [viral disease (human immunodeficiency virus infection, acquired immunodeficiency syndrome, SARS, etc.Type: ApplicationFiled: March 25, 2010Publication date: October 21, 2010Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu HABASHITA, Hiroshi Ochiai, Natsuko Tokuda, Shiro Shibayama, Noriki Watanabe, Takaki Komiya, Kazuhiko Takeda
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Patent number: 7807671Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with diketo piperazine and piperadine derivatives that possess unique antiviral activity useful for the treatment of HIV and AIDS.Type: GrantFiled: April 10, 2007Date of Patent: October 5, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, John F. Kadow, Zhongxing Zhang, Zhiwei Yin, Nicholas A. Meanwell, Alicia Regueiro-Ren, Jacob Swidorski, Ying Han, David J. Carini
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Patent number: 7790726Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: August 14, 2006Date of Patent: September 7, 2010Assignee: Chemocentryx, Inc.Inventors: Penglie Zhang, Andrew M. K. Pennell, John J. Kim Wright, Lianfa Li, Edward J. Sullivan, Wei Chen, Kevin Lloyd Greenman
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Publication number: 20100210838Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.Type: ApplicationFiled: February 1, 2010Publication date: August 19, 2010Applicant: SANOFI-AVENTISInventors: Peter Arányi, László Balázs, Imre Bata, Sándor Bátori, Éva Boronkay, Philippe Bovy, Károly Kánai, Zoltán Kapui, Edit Susán, Tibor Szabó, Lajos T. Nagy, Katalin Urbán-Szabó, Márton Varga
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Publication number: 20100160331Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: April 30, 2008Publication date: June 24, 2010Inventors: Ki Ho Lee, Han Ju Yi, Hyeon Cho, Dae Joong Im, Eun Hee Chae, Yeon Jung Choi
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Publication number: 20100152191Abstract: The present invention is directed to cyclopropyl proline bis-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: May 19, 2008Publication date: June 17, 2010Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
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Publication number: 20100137308Abstract: The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: February 21, 2008Publication date: June 3, 2010Applicant: MERCK SERONO SAInventors: Pascale Gaillard, Vincent Pomel, Isabelle Jeanclaude-Etter, Jerome Dorbais, Jasna Klicic, Cyril Montagne
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Patent number: 7728131Abstract: The present invention is directed to an amide derivative having excellent BCR-ABL tyrosine kinase inhibitory activity, or a salt thereof. The present invention provides an amide derivative represented by the following general formula (1): [Chemical 23] (wherein R1 represents —CH2—R11, etc.; R2 represents alkyl, halogen, haloalkyl, etc.; R3 represents hydrogen, etc.; Het1 represents a group of the formula [6] as above, etc.; and Het2 represents pyrimidinyl, etc.), or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention is useful as a BCR-ABL tyrosine kinase inhibitor.Type: GrantFiled: December 27, 2004Date of Patent: June 1, 2010Assignee: Nippon Shinyaku Co., Ltd.Inventors: Tetsuo Asaki, Yukiteru Sugiyama, Jun Segawa
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Publication number: 20100099684Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic ?7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.Type: ApplicationFiled: October 28, 2009Publication date: April 22, 2010Inventors: James H. Cook, II, Ivar M. McDonald, Dalton King, Richard E. Olson, Nenghui Wang, Christiana I. Iwuagwu, F. Christopher Zusi, John E. Macor
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Publication number: 20100087440Abstract: The present invention comprises small molecule inhibitors of phosphatidylinositol 3-kinase (PI3K), which is associated with a number of malignancies such as ovarian cancer, cervical cancer, breast cancer, colon cancer, rectal cancer, and glioblastomas, among others. Accordingly, the compounds of the present invention are useful for treating, preventing, and/or inhibiting these diseases.Type: ApplicationFiled: October 9, 2006Publication date: April 8, 2010Inventors: William Bajjalieh, Lynne Canne Bannen, S. David Brown, Patrick Kearney, Morrison B. Mac, Charles K. Marlowe, John M. Nuss, Zerom Tesfai, Yong Wang, Wei Xu
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Publication number: 20100029664Abstract: The present invention is concerned with novel sulfonamides of formula I wherein R1, R2, Ar, Hetaryl, m and n are as described in the description and claims. The compounds are orexin receptor antagonists, useful in the treatment of disorders, in which orexin pathways are involved.Type: ApplicationFiled: July 21, 2009Publication date: February 4, 2010Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: 7635775Abstract: Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.Type: GrantFiled: May 5, 2006Date of Patent: December 22, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Francine S. Grant, Sarah Bartulis, Louis Brogley, Michael S. Dappen, Ramesh Kasar, Mohammed A. Khan, Martin Neitzel, Michael A. Pleiss, Eugene D. Thorsett, John Tucker, Michael Ye, Jon E. Hawkinson
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Publication number: 20090306134Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: ApplicationFiled: September 30, 2008Publication date: December 10, 2009Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Publication number: 20090274632Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: August 19, 2008Publication date: November 5, 2009Applicant: Senomyx, Inc.Inventors: Xiaodong Li, Andrew Patron, Catherine Tachdjian, Hong Xu, Qing Li, Alexey Pronin, Guy Servant, Lan Zhang, Thomas Brady, Vincent Darmohusodo, Melissa Arellano, Victor Selchau, Brett Weylan Ching, Donald S. Karanewsky, Paul Brust, Jing Ling, Wen Zhao, Chad Priest