1,2-diazoles (including Hydrogenated) Patents (Class 546/275.4)
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Publication number: 20130131349Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.Type: ApplicationFiled: January 18, 2013Publication date: May 23, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Sumitomo Chemical Company, Limited
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Publication number: 20130131348Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.Type: ApplicationFiled: January 18, 2013Publication date: May 23, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: SUMITOMO CHEMICAL COMPANY, LIMITED
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Publication number: 20130131119Abstract: The present invention relates to fungicidal N-[(het)arylethyl)] pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: June 1, 2011Publication date: May 23, 2013Inventors: Jurgen Benting, Christoph Braun, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Thomas Knobloch, Ruth Meissner, Ulrike Wachendorf-Neumann, Lothar Willms
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Publication number: 20130131347Abstract: The present invention relates to a process for preparing 1-pyridyl-substituted pyrazoles, comprising the reaction of acetyleneketones with pyridylhydrazine derivatives to give 1-pyridyl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-pyridyl-substituted trihalomethylpyrazoles, and the further processing thereof.Type: ApplicationFiled: January 11, 2013Publication date: May 23, 2013Applicant: Bayer Intellectual Property GmbHInventors: Sergii PAZENOK, Norbert LUI, Harry BLASCHKE
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Publication number: 20130123281Abstract: Compositions and methods which modulate diseases and disorders related to transducin ?-like protein 1 (TBL1) activity, including but not limited to cancer, inflammation, and bone related diseases.Type: ApplicationFiled: November 12, 2012Publication date: May 16, 2013Applicant: BETA CAT PHARMACEUTICALS, LLCInventors: Hariprasad M. Vankayalapati, Stephen Horrigan
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Publication number: 20130123260Abstract: The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of rhinovirus infection, methods of treating or preventing rhinovirus infection employing said compounds or pharmaceutical composition comprising the same. The disclosure also relates to compounds of formula (I) for use in the treatment or prophylaxis of exacerbation of respiratory disorders (such as asthma, COPD, bronchitis and/or cystic fibrosis) by rhinovirus infection.Type: ApplicationFiled: June 17, 2011Publication date: May 16, 2013Applicant: RESPIVERT LIMITEDInventors: Catherine Elisabeth Charron, Kazuhiro Ito, William Garth Rapeport
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Publication number: 20130123265Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Frank King, Yazhong Pei, Jeffrey P. Whitten
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Publication number: 20130123500Abstract: Provided is a novel compound represented by formula [I] or a pharmaceutically acceptable salt thereof having antagonistic activity against group II metabolism-type glutamic acid (m-Glu) receptors. The compound or pharmaceutically acceptable salt thereof is useful as a prophylactic or therapeutic agent for diseases such as new mood disorders (depressive and bipolar disorders), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, post-traumatic stress disorder, specific phobias, and acute stress disorder), schizophrenia, Alzheimer's disease, cognitive dysfunction, dementia, drug dependence, convulsions, tremors, pain, sleep disorders, and the like.Type: ApplicationFiled: July 29, 2011Publication date: May 16, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto
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Publication number: 20130116228Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: August 2, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
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Patent number: 8436001Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: April 6, 2011Date of Patent: May 7, 2013Assignee: F. Hoffmann-La Roche AGInventor: Xiaojing Wang
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Patent number: 8436023Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: June 9, 2011Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
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Patent number: 8436024Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R6, R7, L, X and Y are as defined in the specification; together with processes and intermediates for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.Type: GrantFiled: October 1, 2010Date of Patent: May 7, 2013Assignee: Astrazeneca ABInventors: Andiappan Murugan, Lena Kristina Bergstrom, Anna Kristoffersson, Martin Lindsjö, Peter Olof Sjö, Mark David Ashton, Jon Meigh
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Publication number: 20130109566Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: ApplicationFiled: October 24, 2012Publication date: May 2, 2013Applicant: Dow Agrosciences LLCInventor: Dow AgroSciences LLC
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Publication number: 20130109686Abstract: The present invention is directed to isoindolone 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: June 27, 2011Publication date: May 2, 2013Inventors: Douglas C. Beshore, Scott D. Kuduk, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20130102607Abstract: Medicinal use The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of respiratory syncitial virus (RSV) infection in particular viral exacerbation of a respiratory disorder such as bronchitis, asthma, COPD and/or cystic fibrosis, methods of treating or preventing RSV infection employing said compounds or pharmaceutical composition comprising the same.Type: ApplicationFiled: June 17, 2011Publication date: April 25, 2013Applicant: Respivert LimitedInventors: Lindsey Cass, Kazuhiro Ito, William Garth Rapeport, Peter Strong
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Publication number: 20130096144Abstract: The present invention provides isoindolinone and pyrrolopyridinone derivatives, as well as their compositions and methods of use, that inhibit the activity of the serine/threonine kinase, Akt, and are useful in the treatment of diseases related to the activity of Akt including, for example, cancer and other diseases.Type: ApplicationFiled: October 12, 2012Publication date: April 18, 2013Applicant: Incyte CorporationInventor: Incyte Corporation
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Publication number: 20130096161Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: July 8, 2011Publication date: April 18, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu
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Patent number: 8420824Abstract: The disclosure relates to a compound of formula (I): and salts thereof; wherein Ar, L, A, X, R1, R2, R3, R4a, R4b, and R5 are as defined in the disclosure; compositions comprising said compounds, methods for their preparation, intermediates thereto, and the use thereof, particularly as drugs.Type: GrantFiled: June 9, 2011Date of Patent: April 16, 2013Assignee: SanofiInventors: Kirsten Bjergarde, Mark Dodson, Jacques Mauger, Anil Nair, Marcel Patek, Michel Tabart
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Patent number: 8420823Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: GrantFiled: April 17, 2009Date of Patent: April 16, 2013Assignee: MSD K.K.Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Patent number: 8420642Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4 and D have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: GrantFiled: August 13, 2008Date of Patent: April 16, 2013Assignee: Merck Patent GmbHInventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Christine Charon, Daniel Cravo
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Publication number: 20130090358Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: ApplicationFiled: November 29, 2012Publication date: April 11, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Publication number: 20130084346Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.Type: ApplicationFiled: February 28, 2011Publication date: April 4, 2013Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman
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Patent number: 8410278Abstract: A method is disclosed for preparing a non-hydratable crystal form from a hydratable crystal form of 3-bromo-1-(3-chloro-2-pyridinyl)-N-[4-cyano-2-methyl-6-[(methylamino)-carbonyl]phenyl]-1H-pyrazole-5-carboxamide (Compound 1).Type: GrantFiled: November 11, 2009Date of Patent: April 2, 2013Assignee: E I du Pont de Nemours and CompanyInventor: Matthew Richard Oberholzer
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Patent number: 8410141Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which have excellent insecticidal activity and which can thus be used as an insecticide.Type: GrantFiled: May 18, 2010Date of Patent: April 2, 2013Assignee: Bayer Cropscience AGInventors: Tetsuya Murata, Yasushi Yoneta, Hidetoshi Kishikawa, Jun Mihara, Daiei Yamazaki, Mamoru Hatazawa, Norio Sasaki, Kei Domon, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Masashi Ataka, Ulrich Görgens
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Patent number: 8410106Abstract: The present invention constitutes new hydrazine-substituted anthranilic acid derivatives of the general formula (I), in which R1, R2, R3, R4, R5, R6, Qx, A, Qy and n have the definitions indicated in the description, application thereof as insecticides and acaricides for controlling animal pests, alone and in combination with further agents for activity boosting, and a number of processes for their preparation.Type: GrantFiled: February 8, 2011Date of Patent: April 2, 2013Assignee: Bayer Cropscience AGInventors: Rüdiger Fischer, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christoph Grondal, Achim Hense, Arnd Voerste
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Publication number: 20130079302Abstract: The present invention relates to fungicidal N-[(het)arylalkyl)]pyrazolecarboxamide or thiocarboxamide and their heterosubstituted analogues, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: June 1, 2011Publication date: March 28, 2013Inventors: Jurgen Benting, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jorg Greul, Hiroyuki Hadano, Ruth Meissner, Ulrike Wachendorff-Neumann
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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
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Publication number: 20130079513Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: BASF SEInventor: BASF SE
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Patent number: 8399436Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: GrantFiled: April 22, 2010Date of Patent: March 19, 2013Assignee: Glaxo Group LimitedInventors: David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
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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
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Patent number: 8399490Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.Type: GrantFiled: July 14, 2008Date of Patent: March 19, 2013Assignee: Syngenta Crop Protection LLCInventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, André Jeanguenat, Andrew Edmunds, André Denis Stoller
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Patent number: 8399679Abstract: The present invention relates to a process for preparing 1-aryl-substituted pyrazoles, comprising the reaction of alkoxy enones and enamino ketones with arylhydrazine derivatives to give 1-aryl-substituted dihydro-1H-pyrazoles, the further reaction thereof with elimination of water to give 1-aryl-substituted trihalomethylpyrazoles, and the further processing thereof.Type: GrantFiled: September 14, 2012Date of Patent: March 19, 2013Assignee: Bayer CropScience AGInventors: Sergii Pazenok, Norbert Lui
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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
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Publication number: 20130065876Abstract: The present invention relates to compounds of formula I, wherein R1 to R5 are defined in the description and claims, and to pharmaceutically acceptable salts thereof. The present invention relates also to the manufacture of said compounds, pharmaceutical compositions containing them and methods for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Uwe Grether, Paul Hebeisen, Peter Mohr, Fabienne Ricklin, Stephan Roever
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Publication number: 20130065918Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, A and B 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: March 8, 2012Publication date: March 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Jehrod Burnett Brenneman, John D. Huber, Brian Christopher Raudenbush, Christopher Ronald Sarko
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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
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Patent number: 8394838Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (III): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.Type: GrantFiled: April 9, 2008Date of Patent: March 12, 2013Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshihiko Nokura, Hiroshi Ikegami, Markus Jachmann
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Publication number: 20130059860Abstract: The present invention is directed to naphthalene carboxamide 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 Alzheimers 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: May 23, 2011Publication date: March 7, 2013Inventors: Douglas C. Beshore, Chirstina Ng Dimarco, Scott D. Kuduk
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Publication number: 20130060025Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 12, 2012Publication date: March 7, 2013Inventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
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Publication number: 20130053419Abstract: Compounds which are sulfonamido 3,4-diarylpyrazole derivatives, or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is their use as prodrugs.Type: ApplicationFiled: January 19, 2011Publication date: February 28, 2013Inventors: Maurizio Pulici, Chiara Marchionni, Gabriella Traquandi
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Patent number: 8377970Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: GrantFiled: October 6, 2010Date of Patent: February 19, 2013Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
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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
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Publication number: 20130040995Abstract: There is provided inter alia a compound of formula (I): wherein R1, J, Ar, L, X, R3 and R4 are as defined in the specification, for use in the treatment of inflammatory disorders.Type: ApplicationFiled: April 8, 2011Publication date: February 14, 2013Inventors: John King-Underwood, Kazuhiro Ito, Peter Strong, William Garth Rapeport, Catherine Elisabeth Charron, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
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Publication number: 20130040962Abstract: There is provided a compound of formula (I): wherein: J represents (A): or (B): compositions comprising same, processes for preparing said compounds and use thereof in treatment, particularly in the treatment of inflammatory disease, such as asthma, COPD and 15 rheumatoid arthritis.Type: ApplicationFiled: April 8, 2011Publication date: February 14, 2013Inventors: John King-Underwood, Peter John Murray, Jonathan Gareth Williams, Ildiko Buck, Stuart Thomas Onions
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Publication number: 20130040983Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.Type: ApplicationFiled: January 7, 2011Publication date: February 14, 2013Inventors: Jean-Michel Vernier, Patrick O'Connor, William Ripka, David Matthews, Anthony Pinkerton, Pierre-Yves Bounaud, Stephanie Hopkins
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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
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Patent number: 8367844Abstract: The present invention relates to heterocyclic compounds of formula I which have microbiocidal activity, in particular fungicidal activity as well as methods of using the compounds of formula (I) to control microbes: wherein A is x-C(R10R11)—C(?O)—, x-C(R12R13)—C(?S)—, x-O—C(?O)—, x-O—C(?S)—, x-N(R14)—C(?O)—, x-N(R15)—C(?S)—, x-C(R16R17)—SO2— or X—N?C(R30)—, in each case x indicates the bond that is connected to R1; T is CR18 or N; Y1, Y2, Y3, and Y4 are independently CR19 or N; Q is O or S; n is 1 or 2; p is 1 or 2, providing that when n is 2, p is 1.Type: GrantFiled: August 6, 2010Date of Patent: February 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Laura Quaranta, Mathias Stephan Respondek
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Patent number: 8367687Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrazole compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.Type: GrantFiled: December 8, 2008Date of Patent: February 5, 2013Assignees: Novartis AG, Astex Therapeutics Ltd.Inventors: Christopher Thomas Brain, Moo Sung, Young Shin Cho, Ying Hou
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Publication number: 20130029990Abstract: There are provided inter alia compounds of formula (I): wherein R1, R2a, R2b, R3, R4, L, X, R5 and R6 are as defined in the description for use in the treatment of inflammatory diseases.Type: ApplicationFiled: April 1, 2011Publication date: January 31, 2013Inventors: John King-Underwood, George Hardy, Peter John Murray, Jonathan Gareth Williams, Stuart Thomas Onions
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Publication number: 20130029948Abstract: Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases.Type: ApplicationFiled: May 21, 2012Publication date: January 31, 2013Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: Jeffrey Roger Roppe, Timothy Andrew Parr, John Howard Hutchinson