The Additional Hetero Ring Is A Diazine Patents (Class 514/252.02)
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Patent number: 8431572Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: July 6, 2011Date of Patent: April 30, 2013Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Patent number: 8426412Abstract: This invention relates to certain novel 2-alkynyl-6-pyridin-2-yl-pyridazinones, 2-alkynyl-6-pyridin-2-yl-dihydropyridazinones, 2-alkynyl-6-pyrimidin-2-yl-pyridazinones and 2-alkynyl-6-pyrimidin-2-yl-dihydropyridazinones such as those illustrated in Formula I and to the use of these compounds for control of fungal pathogens of plants and mammals.Type: GrantFiled: April 8, 2009Date of Patent: April 23, 2013Assignee: Dow AgroSciences, LLC.Inventors: Martha Kelly, Ronald Ross, Jr., David H. Young
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Patent number: 8426413Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: GrantFiled: February 23, 2012Date of Patent: April 23, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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Publication number: 20130095193Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: September 4, 2012Publication date: April 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Joanne Pinder, Michael Edward O'Donnell, Ronald Marcellus Alphonsus Knegtel, Stephen Clinton Young, Philip Michael Reaper, Steven John Durrant, Heather Clare Twin, Christopher John Davis
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Patent number: 8420630Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.Type: GrantFiled: February 24, 2010Date of Patent: April 16, 2013Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG, Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
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Patent number: 8410105Abstract: The present invention relates to substituted pyridazinylamine derivatives of the formula I or pharmaceutically acceptable salts or hydrates thereof, wherein the substituents are defined as in the description, their preparation process, pharmaceutical compositions comprising them, and uses of the said compounds as picorna virus inhibitors for prevention and/or treatment of diseases caused by picorna viruses.Type: GrantFiled: November 15, 2010Date of Patent: April 2, 2013Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Song Li, Chunlai Mi, Zhibing Zheng, Guoming Zhao, Xinbo Zhou, Zehui Gong
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Publication number: 20130079338Abstract: 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 ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.Type: ApplicationFiled: September 24, 2012Publication date: March 28, 2013Applicant: BRISTOL-MYERS SQUIBB COMPANYInventor: Bristol-Myers Squibb Company
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Publication number: 20130079323Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.Type: ApplicationFiled: September 10, 2010Publication date: March 28, 2013Applicant: TRIUS THERAPEUTICS, INC.Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
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Publication number: 20130072496Abstract: The invention relates to chemical compounds, compositions and methods of making and using the same. In particular, the invention provides selected pyridazine compounds of the formula I wherein R1, R4, R5, R6, R7, R8, R9, R12, R13 ET R14 are independently hydrogen, hydroxyl, alkyl, alkenyl, alkynyl, alkylene, alkenylene, alkoxy, alkenyloxy, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloalkoxy, aryl, aryloxy, arylalkoxy, aroyl, heteroaryl, heterocyclic, acyl, acyloxy, amino, imino, azido, thiol, thioallyl, thioalkoxy, thioaryl, nitro, cyano, halo, sulfate, sulfonyl, sulfinyl, sulfonyl, sultanate, sulfoxide, silyl, silyloxy, silylalkyl, silylthio, =0, ?S, phosphonate, ureido, carboxyl, carbonyl, carbamoyl, or carboxamide; and X is optionally substituted pyrimidinyl or pyridazinyl, an isomer, a pharmaceutically acceptable salt, or derivative thereof.Type: ApplicationFiled: October 25, 2012Publication date: March 21, 2013Applicant: Northwestern UniversityInventor: Northwestern University
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Publication number: 20130072485Abstract: The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds.Type: ApplicationFiled: November 6, 2012Publication date: March 21, 2013Applicants: Dana-Farber Cancer Institute, Inc., Whitehead Institute for Biomedical ResearchInventors: Whitehead Institute for Biomedical Research, Dana-Farber Cancer Institute, Inc.
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Publication number: 20130065850Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) in order to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, as well as in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. The antiviral activity of enzyme inhibitors is demonstrated.Type: ApplicationFiled: April 3, 2012Publication date: March 14, 2013Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Josh MUNGER, Bryson BENNETT, Thomas SHENK, Joshua RABINOWITZ
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Publication number: 20130053362Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: February 28, 2013Applicants: INTELLKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20130045965Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: August 16, 2012Publication date: February 21, 2013Inventors: Christine E. Brotherton-Pleiss, Saul Jaime-Figueroa, Francisco Javier Lopez-Tapia, Yan Lou, Timothy D. Owens
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Patent number: 8372837Abstract: Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: July 15, 2009Date of Patent: February 12, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Dean A. Wacker, Karen A. Rossi, Ying Wang, Gang Wu
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Patent number: 8367668Abstract: Compounds of the formula (I), in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: May 2, 2008Date of Patent: February 5, 2013Assignee: Merck Patent Gesellschaft mit Beschränkter HaftungInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20130029978Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.Type: ApplicationFiled: December 24, 2010Publication date: January 31, 2013Inventors: Tomoyuki Kamino, Yoshitaka Maeda
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Publication number: 20130029999Abstract: Pyridazinyl compounds, compositions and related methods of use.Type: ApplicationFiled: October 1, 2012Publication date: January 31, 2013Applicant: NORTHWESTERN UNIVERSITYInventors: DANIEL MARTIN WATTERSON, LINDA J. VAN ELDIK, HEATHER BEHANNA, HANTAMALALA RALAY RANAIVO
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Publication number: 20130029984Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.
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Publication number: 20130023526Abstract: The present invention provides compound of Formula (I) biologically active metabolites, pro-drugs, isomers, stereoisomers, solvates, hydrates and pharmaceutically acceptable salts thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological conditions.Type: ApplicationFiled: April 30, 2012Publication date: January 24, 2013Applicant: Abbott LaboratoriesInventors: David J. Calderwood, Eric C. Breinlinger, Steven L. Swann, Venkata Srikanth Chitty, Subramanyah Seetharama Shastry Hosahalli, Subhendu Mukherjee, Siva Sanjeeva Rao Thunuguntla
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Publication number: 20130023499Abstract: Certain chemical entities chosen from compounds represented by Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: January 4, 2012Publication date: January 24, 2013Applicant: Gilead Connecticut, Inc.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, David M. ARMISTEAD, Joseph RAKER
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Publication number: 20130023494Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 5, 2011Publication date: January 24, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Sangdon Han, Daniel J. Buzard, Juerg Lehmann, Sanju Narayanan, Dawei Yue
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Publication number: 20130023502Abstract: The invention relates to new substituted pyridinyl-pyrimidines of formula 1 wherein ring A is a five-membered saturated or unsaturated carbocyclic ring which optionally comprises one, two or three heteroatoms each independently from each other selected from the group N, S and O, wherein R1, R2, R4, R3, R5 and R6 are defined as in claim 1 and wherein ring A is further optionally substituted by one or two further substituents and the pharmaceutically acceptable salts, diastereomers, enantiomers, racemates, hydrates and solvates of the aforementioned compounds.Type: ApplicationFiled: January 25, 2012Publication date: January 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GmbHInventors: Georg Dahmann, Dennis Fiegen, Martin Fleck, Matthias Hoffmann, Jasna Klicic, Stephen Peter East, Spencer Charles R. Napier, John Scott
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Publication number: 20130018053Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: ApplicationFiled: April 18, 2011Publication date: January 17, 2013Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
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Publication number: 20130012380Abstract: The present invention relates to pyridazine compounds of formulae I or II and the salts thereof, the N-oxides thereof and the salts of the N-oxides thereof, where the radical A is of the formula A, wherein # denotes the point of attachment to the remainder of formulae I or II, and wherein A1 is N or C—RA1, A2 is N or C—RA2, A3 is N or C—RA3, A4 is N or C—RA4 and A5 is N or C—RA5, provided that one or two of the variables A1, A2, A3, A4 or A5 is N; RA1, RA5, if present, are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-haloalkyl and the like; RA2, RA4, if present, are H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; RA3, if present, is H, halogen, CN, NO2, C1-C10-alkyl, C1-C10-haloalkyl and the like; where W is N or C—RW and V is N or C—RV, provided that one of the variables W or V is N; Rt and Rw, if present, are H, halogen, methyl, C1-haloalkyl and the like; Ru and Rv, if present, are H, halogen, C1-C4-alkyl, C1-C3-haloalkyl and the like; X1 is S, O or NR1a, wherein R1a is H, C1-C10-alkylType: ApplicationFiled: March 23, 2011Publication date: January 10, 2013Applicant: BASF SEInventors: Ronan Le Vezouet, Sebastian Soergel, Christian Defieber, Steffen Gross, Karsten Koerber, Wolfgang Von Deyn, Douglas D. Anspaugh, Deborah L. Culbertson
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Publication number: 20120329798Abstract: A combination of a BCR-ABL inhibitor and a hedgehog pathway inhibitor for the treatment of leukemia.Type: ApplicationFiled: August 28, 2012Publication date: December 27, 2012Inventors: Mhairi Copland, Marion Dorsch, David Irvine, Paul W. Manley, Stefan Peukert
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Publication number: 20120322795Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Zhidong CHEN, Stephane DE LOMBAERT, Michel Jose EMMANUEL, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Hidenori TAKAHASHI
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Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
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Publication number: 20120316176Abstract: The present invention relates to derivatives of 7,8-dihydro-1H-imidazo[2,1-b]purin-4(5H)-one, compositions thereof and methods of use thereof for treating or preventing pain or an inflammatory disease.Type: ApplicationFiled: December 16, 2010Publication date: December 13, 2012Inventors: Deen Tulshian, Michael F. Czarniecki, Julius Matasi, Stephanie N. Brumfield
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Patent number: 8329692Abstract: Compounds selected from the group according to Claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: July 4, 2008Date of Patent: December 11, 2012Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20120295896Abstract: The present invention relates to compounds of formula (I) and (IA): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: September 20, 2011Publication date: November 22, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin W. LIU, Pui Leng LOKE, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20120295908Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: August 3, 2012Publication date: November 22, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Oliver SCHADT, Dieter DORSCH, Frank STIEBER, Andree BLAUKAT
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Publication number: 20120295902Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: December 17, 2010Publication date: November 22, 2012Applicant: MERCK PATENT GMBHInventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Patent number: 8314103Abstract: The present invention relates to pyridyl derivatives capable of inhibiting phosphatidylinositol-3-kinase (PI3k), mammalian target of rapamycin (mTOR) and/or hypoxia inducible factor 1? (HIF-1?) mediated signaling. Also disclosed are processes for preparation of the pyridyl derivatives, and their use in the manufacture of pharmaceutical compositions for the treatment of clinical conditions caused by deregulation of signaling pathways selected from one or more of PI3K, mTOR and HIF-1? pathways. The pyridyl derivatives are also useful for the treatment of conditions or disorders mediated by TNF-?.Type: GrantFiled: August 6, 2008Date of Patent: November 20, 2012Assignee: Piramal Enterprises LimitedInventors: Sanjay Kumar, Kalpana Sanjay Joshi, Vijaykumar Deore, Mandar Ramesh Bhonde, Nilambari Nilkanth Yewalkar, Amol Arun Padgaonkar, Asha Adrian Kulkarni-Almeida, Maggie Joyce Rathos, Sapna Parikh, Nilesh Madhukar Dagia
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Publication number: 20120289507Abstract: The present invention relates generally to novel compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders. The present invention includes novel compounds, novel compositions, methods of their use and methods of their manufacture, where such compounds are generally pharmacologically useful as agents in therapies whose mechanism of action involve methods of inhibiting tumorigenesis, tumor growth and tumor survival using agents that inhibit the Hedgehog and Smo signaling pathway.Type: ApplicationFiled: July 20, 2012Publication date: November 15, 2012Applicant: NOVARTIS AGInventors: Feng HE, Stefan PEUKERT, Karen MILLER-MOSLIN, Naeem YUSUFF, Zhuoliang CHEN, Bharat LAGU
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Patent number: 8309537Abstract: Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.Type: GrantFiled: November 5, 2010Date of Patent: November 13, 2012Assignee: Aerpio Therapeutics Inc.Inventors: Joseph H. Gardner, Robert Shalwitz
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Publication number: 20120277206Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.Type: ApplicationFiled: May 11, 2012Publication date: November 1, 2012Applicant: Andrea Boesciences, Inc.Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
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Publication number: 20120277204Abstract: The present invention provides a compound which has the effect of PDE inhibition, and which is useful as a medicament for preventing or treating schizophrenia or so on. A compound of formula (I0), wherein R1 represents a substituent; R2 represents a hydrogen atom, or a substituent; R3 represents a hydrogen atom, or a substituent; Ring A represents an aromatic ring which can be substituted, and Ring B represents a 5-membered heteroaromatic ring which can be substituted, or a salt thereof.Type: ApplicationFiled: July 6, 2012Publication date: November 1, 2012Inventors: Takahiko TANIGUCHI, Akira Kawada, Mitsuyo Kondo, John F. Quinn, Jun Kunitomo, Masato Yoshikawa, Makoto Fushimi
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Publication number: 20120277205Abstract: The present invention relates to compounds corresponding to formula (I): in which: A represents a divalent aromatic radical; X represents a —CH— group or a nitrogen atom; R1 represents a (C1-C4)alkyl or a (C1-C4)alkoxy; R2 represents a group Alk; R3 represents a hydroxyl or a group —NR7R8; R4 represents a hydrogen atom, a halogen atom, a cyano, a phenyl, a group Alk, a group OAlk or a group —NR9R10; R5 represents a hydrogen atom, a halogen atom or a group Alk; R6 represents a hydrogen atom, a halogen atom, a cyano, a group —COOAlk or a —CONH2 group.Type: ApplicationFiled: September 13, 2011Publication date: November 1, 2012Applicant: SANOFIInventors: Alain Badorc, Christophe Boldron, Nathalie Delesque, Valérie Fossey, Gilbert Lassalle, Xavier Yvon
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Patent number: 8299253Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: December 22, 2006Date of Patent: October 30, 2012Assignee: University of Kentucky Research FoundationInventors: Peter Crooks, Linda Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha P Sumithran
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Publication number: 20120270856Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: ApplicationFiled: July 2, 2012Publication date: October 25, 2012Inventors: Tomoharu IINO, Akio OHNO, Norikazu OTAKE, Takuya SUGA, Masanori ASAI
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Publication number: 20120270871Abstract: Pyrrolopyridinylpyrimidin-2-ylamine derivatives of the formula (I), in which R1-R6 and R1 have the meanings indicated in claim 1, are inhibitors of cell proliferation/cell vitality and can be employed for the treatment of tumours.Type: ApplicationFiled: October 12, 2010Publication date: October 25, 2012Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Margarita Wucherer-Plietker, Christina Esdar, Brian Hodous
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Publication number: 20120264735Abstract: The present invention relates to pyridazin-4(1H)-one derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: December 14, 2010Publication date: October 18, 2012Inventors: Jonathan Young, Barbara Czako, Michael Altman, David Guerin, Michelle Martinez, Alexey Rivkin, Kevin Wilson, Kathryn Lipford, Catherine White, Laura Surdi, Stephanie Chichetti, Matthew H. Daniels, Sean P. Ahearn, Danielle Falcone, Ekundayo Osimboni
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Publication number: 20120264761Abstract: The present invention is directed to aminobenzoquinazolinone 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: December 13, 2010Publication date: October 18, 2012Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng DiMarco, Thomas J. Greshock
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Publication number: 20120258951Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: December 17, 2010Publication date: October 11, 2012Applicant: Mitsubishi Tanage Pharma CorporationInventors: Hiroshi Sato, Kazutoshi Yokoyama, Kazushi Sato
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Patent number: 8278304Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: March 12, 2009Date of Patent: October 2, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh
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Patent number: 8278316Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.Type: GrantFiled: March 9, 2010Date of Patent: October 2, 2012Assignee: Bristol-Myers Squibb CompanyInventor: Saleem Ahmad
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Publication number: 20120245162Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein.Type: ApplicationFiled: September 20, 2011Publication date: September 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20120245180Abstract: The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer.Type: ApplicationFiled: September 28, 2010Publication date: September 27, 2012Applicant: GlaxoSmithKline LLCInventors: Kurt R. Auger, Kurtis Earl Bachman, Tona M. Gilmer, James G. Greger, JR., Joel David Greshock, Sylvie Laquerre, Li Liu, Shannon Renae Morris
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Publication number: 20120245125Abstract: The invention relates to novel chemical compounds, compositions and methods of making and using the same. In particular, the invention provides pyridazine compounds and/or related heterocyclic derivatives, compositions comprising the same, and methods of making and using pyridazine compounds and/or related heterocyclic derivatives and compositions comprising the same, for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for, research, drug screening, and therapeutic applications.Type: ApplicationFiled: June 8, 2012Publication date: September 27, 2012Applicants: Northwestern UniversityInventors: D. Martin Watterson, Linda Van Eldik, Jacques Haiech, Marcel Hibert, Jean-Jacques Bourguignon, Anastasia Velentza, Wenhui Hu, Magdalena Zasadzki