Ring Nitrogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/340)
-
Publication number: 20130085148Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: ApplicationFiled: September 30, 2012Publication date: April 4, 2013Applicant: ENDO PHARMACEUTICALS INC.Inventor: Endo Pharmaceuticals Inc.
-
Publication number: 20130085147Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: November 7, 2012Publication date: April 4, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
-
Patent number: 8410145Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of Formula (I), to insecticidal, acaricidal, molluscicidal or nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc or nematode pests.Type: GrantFiled: December 18, 2008Date of Patent: April 2, 2013Assignee: Syngenta Crop Protection LLCInventors: Pierre Joseph Marcel Jung, Peter Renold
-
Publication number: 20130079313Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: September 26, 2012Publication date: March 28, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
-
Publication number: 20130079362Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: ApplicationFiled: August 21, 2012Publication date: March 28, 2013Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
-
Patent number: 8404676Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: October 1, 2008Date of Patent: March 26, 2013Assignee: Merck Serono SAInventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
-
Patent number: 8404726Abstract: A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPAR?. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.Type: GrantFiled: April 18, 2007Date of Patent: March 26, 2013Assignee: Nippon Chemiphar Co. Ltd.Inventors: Shogo Sakuma, Nobutaka Mochiduki, Rie Takahashi, Masatoshi Ushioda, Tomio Yamakawa, Seiichiro Masui
-
Patent number: 8404722Abstract: The present invention relates generally to compounds represented in Formula (I), pharmaceutical compositions comprising them and methods of treating of diseases or disorders such as cancer.Type: GrantFiled: March 13, 2009Date of Patent: March 26, 2013Assignee: Amgen Inc.Inventors: Matthew Brown, Michael G. Johnson
-
Publication number: 20130072490Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 29, 2010Publication date: March 21, 2013Applicant: Amira Pharmaceuticals INC.Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
-
Publication number: 20130072461Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: November 13, 2012Publication date: March 21, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventor: Synta Pharmaceuticals Corp.
-
Patent number: 8399494Abstract: The present invention is directed to 2,5-disubstituted phenyl carboxamide 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: October 26, 2009Date of Patent: March 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Jeffrey M. Bergman, Paul J. Coleman, Anthony J. Roecker, John D. Schreier
-
Patent number: 8399493Abstract: The present invention relates to methods for treating or controlling schizophrenia in a mammal using compounds having the Formula (I), wherein M1 and M2 are defined in the application.Type: GrantFiled: September 16, 2005Date of Patent: March 19, 2013Assignees: Janssen Pharmaceuticals, Inc., Addex Pharmaceuticals S.A.Inventors: Christelle Martine Bolea, Vanthea Nhem, Terry Patrick Finn, Emmanuel Christian Le Poul, Jean-Philippe Francois Christian Rocher, Robert Johannes Lutjens
-
Patent number: 8399492Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: November 11, 2011Date of Patent: March 19, 2013Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
-
Publication number: 20130065842Abstract: Heterocyclic compounds, and pharmaceutical compositions thereof, are disclosed as ROR?t modulators that have a formula represented by the following: and wherein n1, n2, R1, R2, R3, and R4 are as described herein. These compounds may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, inflammatory conditions, autoimmune disorders, cancer, and graft-versus-host disease.Type: ApplicationFiled: March 11, 2011Publication date: March 14, 2013Inventors: Dan Littman, Jun R. Huh, Wenwei Huang, Ruili Huang
-
Publication number: 20130065911Abstract: The present invention relates to compounds of the formula wherein R1 to R3 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 10, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Stephan Roever
-
Publication number: 20130065907Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Stephan Roever, Uwe Grether
-
Patent number: 8394837Abstract: The present invention is directed to 2,3,4,6-substituted pyridyl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: November 18, 2005Date of Patent: March 12, 2013Assignee: Merck, Sharp & Dohme, Corp.Inventors: Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, James C. Barrow, Shaun R. Stauffer, Joseph P. Vacca, Keith P. Moore, Shawn J. Stachel, Mattahew G. Stanton
-
Publication number: 20130059883Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: March 7, 2013Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
-
Patent number: 8389546Abstract: The present application relates to compounds and methods for treating pain and other conditions related to TRPV3.Type: GrantFiled: July 1, 2011Date of Patent: March 5, 2013Assignee: Hydra Biosciences, Inc.Inventors: Magdalene M. Moran, Jayhong A. Chong, Christopher Fanger, Amy Ripka, Glenn R. Larsen, Xiaoguang Zhen, Dennis John Underwood, Manfred Weigele
-
Patent number: 8389549Abstract: A compound of Formula: (I) or a pharmaceutically acceptable derivative thereof, where Ar1, Ar2, X, R3, and m are as disclosed herein. Compounds of Formulae (I)-(V) and pharmaceutically acceptable derivatives thereof; compositions comprising an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof; and methods for treating or preventing pain, UI, an ulcer, IBD, or IBS in an animal comprising administering to an animal in need thereof an effective amount of a compound of Formulae (I)-(V) or a pharmaceutically acceptable derivative thereof are disclosed herein.Type: GrantFiled: April 25, 2008Date of Patent: March 5, 2013Assignee: Purdue Pharma L.P.Inventor: Laykea Tafesse
-
Patent number: 8389550Abstract: The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 17, 2010Date of Patent: March 5, 2013Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLCInventors: Bernd Buettelmann, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20130053361Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: July 5, 2012Publication date: February 28, 2013Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
-
Publication number: 20130053416Abstract: 3-Heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals The present invention relates to compounds of the formula I, wherein Ht, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: July 26, 2012Publication date: February 28, 2013Applicant: SANOFIInventors: Sven RUF, Josef PERNERSTORFER, Thorsten SADOWSKI, Georg HORSTICK, Herman SCHREUDER, Christian BUNING, Klaus WIRTH
-
Patent number: 8383822Abstract: The invention relates to novel substituted oxazolidinones, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.Type: GrantFiled: June 7, 2008Date of Patent: February 26, 2013Assignee: Bayer Intellectual Property GmbHInventors: Swen Allerheiligen, Marcus Bauser, Dirk Heimbach, Stefan Heitmeier, Mark Jean Gnoth, Christoph Gerdes, Georges Von Degenfeld, Susanne Röhrig, Ulrich Rester, Elke Dittrich-Wengenroth, Uwe Saatmann, Adrian Tersteegen, Joachim Krüger, Holger Paulsen
-
Patent number: 8383660Abstract: Dibenzyl amine compounds and derivatives of Formula I, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.Type: GrantFiled: January 3, 2007Date of Patent: February 26, 2013Assignee: Pfizer Inc.Inventors: George Chang, Ravi S. Garigipati, Bruce Lefker, David A. Perry
-
Publication number: 20130045964Abstract: Disclosed are compounds of Formula (I) or stereoisomers, salts, or prodrugs thereof, wherein: Q is, or R1 is phenyl substituted with zero to 3 substituents; and R1, R2, R3, R4, R5, and G are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: April 21, 2011Publication date: February 21, 2013Inventors: Robert J. Cherney, Yanlei Zhang
-
Patent number: 8377942Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.Type: GrantFiled: December 17, 2009Date of Patent: February 19, 2013Assignee: Novartis AGInventors: Steve Nanchen, Noëlle Gauvry, Francois Pautrat
-
Patent number: 8377971Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutically acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.Type: GrantFiled: August 1, 2007Date of Patent: February 19, 2013Assignee: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai
-
Patent number: 8377938Abstract: The invention provides acid addition salts of the compounds represented by formula (1) or (2), or crystals thereof, and processes for preparing the same. The salts or crystals have HGFR inhibitory activity and excellent physical properties (solubility, safety, etc.) and are therefore useful as anti-tumor agents, angiogenesis inhibitors and inhibitors for metastasis for a various types of tumor.Type: GrantFiled: February 14, 2008Date of Patent: February 19, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Tomohiro Matsushima, Shuji Shirotori, Keiko Takahashi, Atsushi Kamada, Kazunori Wakasugi, Takahisa Sakaguchi
-
Publication number: 20130040950Abstract: There are provided inter alia multisubstituted aromatic compounds useful for the inhibition of thrombin, which compounds include substituted pyrazolyl or substituted triazolyl. There are additionally provided pharmaceutical compositions. There are additionally provided methods of treating and preventing a disease or disorder, which disease or disorder is amenable to treatment or prevention by the inhibition of thrombin.Type: ApplicationFiled: September 28, 2012Publication date: February 14, 2013Applicant: VERSEON CORPORATIONInventor: VERSEON CORPORATION
-
Publication number: 20130039944Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: April 20, 2011Publication date: February 14, 2013Applicant: Kineta, Inc.Inventors: Shawn P. Iadonato, Kristin Bedard
-
Patent number: 8372807Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: GrantFiled: May 20, 2010Date of Patent: February 12, 2013Assignee: Ardea Biosciences, Inc.Inventors: Martha De La Rosa, Jean-Luc Girardet, Karen Watson
-
Patent number: 8372867Abstract: The present invention relates to novel aryl isoxazoline derivatives having excellent insecticidal activity as insecticides and represented by the formula: and their use as insecticides and acarizides.Type: GrantFiled: March 28, 2008Date of Patent: February 12, 2013Assignee: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Katsuhiko Shibuya, Eiichi Shimojo, Ulrich Görgens, Andreas Turberg, Thomas Bach
-
Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
-
Publication number: 20130035331Abstract: The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors.Type: ApplicationFiled: January 12, 2011Publication date: February 7, 2013Applicant: AB SCIENCEInventors: Alain Moussy, Abdellah Benjahad, Jason Martin, Emmanuel Chevenier, Didier Pez, Franck Sandrinelli, Willy Picoul
-
Publication number: 20130035339Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).Type: ApplicationFiled: September 13, 2012Publication date: February 7, 2013Applicant: Gilead Sciences, IncInventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
-
Publication number: 20130029845Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 30, 2012Publication date: January 31, 2013Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip LAHM, Wesley Lawrence SHOOP, Ming XU
-
Publication number: 20130030000Abstract: The present invention is directed to a composition useful for the treatment of a FAAH mediated disease, disorder or conditions comprising a FAAH inhibitor and a second activation, comprising a selected imidazole or oxazole FAAH inhibitor and a second active agent. The compositions will be useful in the treatment of a wide range of disease, disorder, or conditions including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease. In another aspect the invention discloses herein is directed to compositions useful in the treatment of neuropathic and nociceptive pain, said compositions comprising etoricoxib.Type: ApplicationFiled: January 25, 2011Publication date: January 31, 2013Inventors: Harry R. Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo, Terence G. Hamill, Wenping Li, Darrell Arthur Henze
-
Patent number: 8357703Abstract: The present invention is concerned with novel isoxazoles of formula I wherein X, R1, R2, R3 and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as therapeutics.Type: GrantFiled: May 3, 2010Date of Patent: January 22, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
-
Publication number: 20130018066Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: July 17, 2012Publication date: January 17, 2013Applicant: Schering Corporation & Pharmacopeia Drug Discovery Inc.Inventors: Zhaoning Zhu, Brian A. McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew Stamford, William J. Greenlee, Robert Mazzola, John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter, Michelle L. Morris, Huizhong Gu, Gang Qian, Dawit Tadesse
-
Publication number: 20130018055Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, A1, A2 and n are as described herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: January 17, 2012Publication date: January 17, 2013Inventors: Johannes Aebi, Alfred Binggeli, Cornelia Hertel, Anish Ashok Konkar, Holger Kuehne, Bernd Kuhn, Hans P. Maerki, Haiyan Wang
-
Publication number: 20130018048Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 4, 2011Publication date: January 17, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
-
Publication number: 20130012526Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: April 18, 2011Publication date: January 10, 2013Applicant: Merck Sharp & Dohme Corp.Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
-
Publication number: 20130012547Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.Type: ApplicationFiled: March 11, 2011Publication date: January 10, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Pierre Joseph Marcel Jung, Peter Danko, Christopher Richard Ayles Godfrey, Peter Renold, Ottmar Franz Hueter
-
Publication number: 20130012546Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: December 28, 2010Publication date: January 10, 2013Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
-
Publication number: 20130005719Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: June 19, 2012Publication date: January 3, 2013Applicant: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
-
Publication number: 20130005735Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
-
Publication number: 20130005776Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: ApplicationFiled: July 30, 2012Publication date: January 3, 2013Applicant: VIAMET PHARMACEUTICALS, INC.Inventors: William J. Hoekstra, Robert J. Schotzinger, Stephen W. Rafferty
-
Publication number: 20130005730Abstract: The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: January 3, 2013Inventors: Piaoyang Sun, Mikhajlovich Antonov Dmitry, Xiao Xiong Zhou
-
Publication number: 20130005672Abstract: According to the present invention, a plant disease control agent having a superior control effect on plant diseases at a low dose is provided. The plant disease control agent of the present invention includes at least one selected from tetrazolyl oxime derivatives represented by formula (I) and salts thereof, and at least one selected from the group consisting of imidacloprid, triflumizole, spinosad, hydroxy isoxazole, thiophanate-methyl, tricyclazole, clothianidin, benomyl, acetamiprid and salts thereof. In formula (I), X represents a C1-6 alkyl group or the like; n represents an integer of 0 to 5; Y represents a C1-6 alkyl group; Z represents a group represented by NHC(?O)-Q; Q represents a C1-8 alkoxy group or the like; R represents a halogen atom; m represents an integer of 0 to 3.Type: ApplicationFiled: March 14, 2011Publication date: January 3, 2013Inventor: Ichirou Urihara