At 4- Or 6-position Patents (Class 544/319)
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Patent number: 8481550Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: GrantFiled: August 24, 2011Date of Patent: July 9, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Publication number: 20130172557Abstract: 2,6-Dihalo-5-alkoxy-4-substituted-pyrimidines, 2,6-dihalo-5-alkoxy-4-pyrimdine carbaldehydes, and derivatives of each are useful intermediates in forming potent herbicides that demonstrate a broad spectrum of weed control. These compounds are disclosed, as are methods of forming and using these compounds.Type: ApplicationFiled: December 28, 2012Publication date: July 4, 2013Applicant: DOW AGROSCIENCES LLCInventor: DOW AGROSCIENCES LLC
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Publication number: 20130172312Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Inventors: Bernd NOSSE, Martin FLECK, Niklas HEINE, Gerald Juergen ROTH
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Publication number: 20130165422Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.Type: ApplicationFiled: November 29, 2012Publication date: June 27, 2013Applicant: SANOFIInventor: SANOFI
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Patent number: 8471013Abstract: The present invention provides a process for reacting between a phenol derivative and an aromatic substrate under phenolate forming conditions comprising the following steps: (a) reacting a phenol derivative with a base in a polar organic solvent to obtain a phenolate salt, wherein water is removed form the reaction mixture during the reaction, (b) adding the aromatic substrate to the reaction mixture obtained in step (a), (c) heating the reaction mixture of step (b) to a temperature in the range of 80° to 1300° C., preferably, 90° to 1000° C. for 2 to 7 hours to obtain a phenoxy substituted aromatic substrate, (d) removing the solvent from the mixture of step (c) and optionally further isolating an purifying the phenoxy substituted aromatic substrate. Optionally, the removal of water during step (a) is in conjunction with partial removal of the organic solvent.Type: GrantFiled: December 16, 2007Date of Patent: June 25, 2013Assignee: Makhteshim Chemical Works, Ltd.Inventors: David Ovadia, Raya Sturkovich, David Leonov
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Publication number: 20130158054Abstract: The present invention relates to novel crystalline polymorphic and amorphous forms of the compound (E)-2-{2-[6-(2-cyanophenoxy)pyrimidin-4-yloxy]phenyl}-3-methoxy-acrylate (azoxystrobin). Infrared Raman spectra, X-ray powder diffraction pattern and differential scanning calorimetry thermogram of two polymorphs “A” and “B” are provided. Further, the present invention also provides methods for preparing the novel polymorphic forms “A” and “B”, as well as processes for producing mixtures of the polymorphs, and a process for preparing amorphous azoxystrobin. Yet further, the present invention provides anti-fungal compositions comprising the novel crystalline polymorphs “A” and “B” or amorphous azoxystrobin, which are useful for controlling and combating fungi grown on agricultural and horticultural crops and up-land, and methods of using the same as pesticidal agents for combating fungi on agricultural and horticultural crops.Type: ApplicationFiled: December 6, 2012Publication date: June 20, 2013Applicant: MAKHTESHIM CHEMICAL WORKS, INC.Inventor: Makhteshim Chemical Works, Inc.
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Publication number: 20130158021Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.Type: ApplicationFiled: October 26, 2012Publication date: June 20, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
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Publication number: 20130158053Abstract: Crystalline forms of the p38 kinase inhibitor 3-[5-chloro-4-[(2,4-difluorobenzyl)oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide is provided. Also provided are combinations and pharmaceutical compositions comprising the crystalline forms, and methods for the prophylaxis and/or treatment of a p38 kinase-mediated condition comprising administering to a subject a therapeutically effective amount of the crystalline forms.Type: ApplicationFiled: November 6, 2012Publication date: June 20, 2013Applicant: Pharmacia & Upjohn Company LLCInventor: Pharmacia & Upjohn Company LLC
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Publication number: 20130150388Abstract: Disclosed are chemical entities which are inhibitors of Nedd8-activating enzyme (NAE), namely, the compound {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate and pharmaceutically acceptable salts thereof; solid state forms thereof; and prodrugs thereof. Also disclosed are methods of using the chemical entities to treat disorders such as cancer.Type: ApplicationFiled: August 23, 2012Publication date: June 13, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Ashley Sue McCarron, Todd B. Sells, Matthew Stirling, Stephen G. Stroud
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Publication number: 20130150356Abstract: The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The 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 voltage gated sodium channels are involved.Type: ApplicationFiled: August 9, 2011Publication date: June 13, 2013Applicant: RAQUALIA PHARMA INC.Inventors: Mikiko Morita, Shuzo Watanabe
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Publication number: 20130150372Abstract: This invention relates to novel phenyl amide or pyridyl amide derivatives of the formula wherein A1, A2, B1, B2 and R1 to R11 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and can be used as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: February 15, 2013Publication date: June 13, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Patent number: 8461168Abstract: A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula (I) wherein R is CONH2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H2N CH?C(R)CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula (I) is transferred into an acid addition salt, and the transformation of a compound of formula (II) wherein R is CONH2 into a compound of formula (II) wherein R is CN by treatment with POCI3.Type: GrantFiled: April 8, 2010Date of Patent: June 11, 2013Assignee: DSM IP Assets B.V.Inventors: Reinhard Karge, Jan Schütz
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Patent number: 8455489Abstract: Novel compositions and methods of using substituted pyrimidines which have the general formula: (I).Type: GrantFiled: November 9, 2004Date of Patent: June 4, 2013Assignee: Exelixis, Inc.Inventors: Richard Martin, Raju Mohan, Peter Ordentlich
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Publication number: 20130137868Abstract: The present invention provides novel salts of raltegravir, processes for their preparation and pharmaceutical compositions comprising them. The present invention also provides crystalline sodium salt of raltegravir, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of amorphous sodium salt of raltegravir. The present invention further provides a process for the preparation of raltegravir potassium crystalline form H1.Type: ApplicationFiled: May 25, 2010Publication date: May 30, 2013Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
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Publication number: 20130137635Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.Type: ApplicationFiled: February 9, 2011Publication date: May 30, 2013Applicant: LEXICON PHARMACEUTICALS, INC.Inventor: Arthur Thomas Sands
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Publication number: 20130137675Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.Type: ApplicationFiled: August 9, 2011Publication date: May 30, 2013Inventors: Takahiko Taniguchi, Shinkichi Suzuki, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
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Publication number: 20130137671Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.Type: ApplicationFiled: May 23, 2012Publication date: May 30, 2013Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Publication number: 20130137865Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.Type: ApplicationFiled: August 11, 2011Publication date: May 30, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto, Hideaki Amada, Hiroki Urabe, Rie Nishikawa, Shuhei Kashiwa ASHIWA
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Publication number: 20130121919Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.Type: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
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Publication number: 20130123287Abstract: Providing a novel control agent for soft rot and a novel control method for the same. A compound having no antibacterial activity against Erwinia carotovora but having a control activity against fungi on soil surface, specifically containing, as the active ingredient, a fungicide comprising any of a strobilurin compound such as azoxystrobin and kresoxim-methyl, an azole compound such as triflumizol, cyazofamid, amisulbrom, and thiophanate-methyl, a carboxamide compound such as penthiopyrad and boscalid, a sulfonamide compound such as flusulfamide, an organic chlorine compound such as chlorothalonil, a dicarboximide compound such as pro-cymidone and iprodione, a phenylpyrrole compound such as fludioxonil, an anilinopyrimidine compound such as mepanipyrim, and a guanidine compound such as iminoctadine is the control agent for plant soft rot, which is applied to plant cultivation soil.Type: ApplicationFiled: July 21, 2011Publication date: May 16, 2013Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Koji Sugimoto, Hiroyuki Hayashi
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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: 20130123284Abstract: Provided herein are compounds useful for kinase inhibition.Type: ApplicationFiled: March 24, 2011Publication date: May 16, 2013Applicant: AMITECH THERAPEUTIC SOLUTIONS INCInventors: Lee Daniel Arnold, Eric A. Murphy
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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: 20130109660Abstract: This disclosure relates to novel HIV integrase inhibitors their derivatives, pharmaceutically acceptable salts thereof. This disclosure also provides compositions comprising a compound of this disclosure and the use of such compositions in methods of treating HIV infections.Type: ApplicationFiled: July 13, 2011Publication date: May 2, 2013Applicant: CONCERT PHARMACEUTICALS INC.Inventor: Roger Tung
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Patent number: 8431578Abstract: Compounds of formula (I) in free or salt or solvate form, where T1, T2, and T3 have the meanings as indicated in the specification, are useful for treating inflammatory or obstructive airways, pulmonary hypertension, pulmonary fibrosis, liver fibrosis, muscle diseases and systemic skeletal disorders. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: GrantFiled: January 9, 2009Date of Patent: April 30, 2013Assignee: Novartis AGInventors: Peter Hunt, Catherine Leblanc, Robert Alexander Pulz, Nikolaus Johannes Stiefl
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Publication number: 20130102568Abstract: [PROBLEMS] The present invention provides a novel alkoxyimino derivative or a salt thereof, as well as to a pest control agent containing the derivative or salt thereof as an active ingredient, which shows an excellent pest control effect on a wide range of pests in the agricultural and horticultural field and is also capable of controlling resistant pests. [MEANS FOR SOLVING PROBLEMS] The novel alkoxyimino derivative is characterized by being represented by general formula [I] (in the formula, X, R1, R2 and Q are as defined in the specification) and the post control agent is characterized by containing as an active ingredient the alkoxyimino derivative or a salt thereof.Type: ApplicationFiled: June 21, 2011Publication date: April 25, 2013Applicant: Kumiai Chemical Industry Co., Ltd. and Ihara Chemical Industry Co., Ltd.Inventors: Shunichirou Fukumoto, Daisuke Shikama, Keiji Toriyabe, Toshihiro Nagata, Masaaki Komatsu, Takeshi Matsuda, Yuki Nakano
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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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Patent number: 8426591Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.Type: GrantFiled: November 23, 2009Date of Patent: April 23, 2013Assignee: Dow AgroSciences, LLC.Inventors: Katherine A. Guenthenspberger, Thomas L. Siddall
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Patent number: 8426419Abstract: The present invention relates to tyrosine kinase inhibitors that contain a zinc-binding moiety and their use in the treatment of tyrosine related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.Type: GrantFiled: January 20, 2011Date of Patent: April 23, 2013Assignee: Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Stephen Gould, Haixiao Zhai
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Publication number: 20130096147Abstract: The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.Type: ApplicationFiled: December 7, 2012Publication date: April 18, 2013Inventors: Ana KWOKAL, Lilach Hedvati, Revital Burstein, Adi Yeori, Rinat Moshkovits-Kaptsan
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Publication number: 20130096005Abstract: 2-(Substituted phenyl)-6-amino-5-alkoxy, thioalkoxy and aminoalkyl-4-pyrimidinecarboxylic acid and its derivatives are potent herbicides demonstrating broad spectrum of weed control.Type: ApplicationFiled: December 5, 2012Publication date: April 18, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
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Patent number: 8410122Abstract: The present invention relates to Bicyclic Heterocycle Derivatives, compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a GPCR in a patient.Type: GrantFiled: December 21, 2009Date of Patent: April 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew Stamford, Hong Liu
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Publication number: 20130079360Abstract: The present invention includes new salts of Raltegravir and crystalline forms thereof, pharmaceutical compositions containing the salts or crystalline forms, methods of using the salts or crystalline forms or the compositions to treat HIV infection or to prepare medicament for treating HIV infection, and a process for preparing Raltegravir potassium.Type: ApplicationFiled: April 1, 2011Publication date: March 28, 2013Inventors: Ana Kwokal, Lilach Hedvati, Revital Burstein, Adi Yeori, Rinat Moshkovits-Kaptsan
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Publication number: 20130072427Abstract: Compounds of formula (I) that modulate the activity of the G-protein-coupled receptor GPR119 and their uses in the treatment of diseases linked to the modulation of the G-protein-coupled receptor GPR119 in animals are described herein.Type: ApplicationFiled: July 22, 2010Publication date: March 21, 2013Inventors: Cristiano Guimaraes, Vincent Mascitti, Kim F. McClure, Michael J. Munchhof, Ralph P. Robinson
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Publication number: 20130065858Abstract: The present invention provides compounds useful as inhibitors of Raf protein kinase. The present invention also provides compositions thereof, and methods of treating Raf-mediated diseases.Type: ApplicationFiled: October 22, 2012Publication date: March 14, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., MILLENNIUM PHARMACEUTICALS, INC.Inventors: MILLENNIUM PHARMACEUTICALS, INC., SUNESIS PHARMACEUTICALS, INC.
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Patent number: 8394809Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: March 12, 2013Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Patent number: 8389534Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: GrantFiled: October 14, 2009Date of Patent: March 5, 2013Assignee: The University of Tennessee Research FoundationInventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa, Patrick Allison
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Publication number: 20130053403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: ApplicationFiled: April 25, 2011Publication date: February 28, 2013Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Patent number: 8383639Abstract: The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: October 8, 2010Date of Patent: February 26, 2013Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Kevin Peese, Ira B. Dicker, Chen Li, Manoj Patel, Nicholas A. Meanwell, Michael A. Walker
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Publication number: 20130045948Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, W, X, G, R1, R2, R3, R4, m and n are as defined in the disclosure. Also disclosed are pharmaceutical compositions containing the compounds of Formula 1 and methods for treating a disease or condition mediated by fatty acid amide hydrolase activity comprising applying a therapeutically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 10, 2010Publication date: February 21, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Mei H. Dung, Robert James Pasteris
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Patent number: 8378118Abstract: The present invention discloses a novel thyroid like compounds of formula (I), wherein R1 R2, R3, R4 and Z are as defined in the specification, method for its preparation, composition containing such compounds and use of such compounds and composition as medicament. Further, compounds of formula (I) has significantly low binding affinity to thyroid receptors and thus considerably devoid of thyrotoxic effects. The invention also relates to the use of the compound of formula (I) for the preparation of a medicament for treating various disease conditions such as obesity, dyslipidemia, metabolic syndrome and co-morbidities associated with metabolic syndrome.Type: GrantFiled: January 10, 2012Date of Patent: February 19, 2013Assignee: Torrent Pharmaceuticals Ltd.Inventors: Laxmikant Chhipa, Shitalkumar Pukharaj Zambad, Ramesh Gupta, Davinder Tuli, Ashok Kasundra, Siralee Munshi, M. Amir Siddiqui, Subrat Kumar Bhattamisra, C. Dutt, Vijay Chauthaiwale
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Publication number: 20130040975Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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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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Patent number: 8372857Abstract: The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: June 21, 2010Date of Patent: February 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Matthew J. Clements, John S. Debenham, Jeffrey J. Hale, Christina Madsen-Duggan
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Publication number: 20130035485Abstract: In one embodiment the present invention encompasses 4-(2,6-dichloropyrimidin-4-yloxy)-3,5-dimethylbenzonitrile (“ETHER”), 4-(4,6-dichloropyrimidin-2-yloxy)-3,5-dimethyl-benzonitrile (“ETHER C-2 isomer”), mixtures and salts thereof of. The present invention encompasses the use of ETHER and salts thereof to prepare Etravirine and Etravirine intermediates, and salts thereof. In another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare debrometravirine (“DEBETV”) and salts thereof. In yet another embodiment the present invention encompasses the use of ETHER and salts thereof to prepare 4-(6-chloro-2-(4-cyanophenylamino)pyrimidin-4-yloxy)-3,5-dimethyl-benzonitrile (“ARCPBN”) and salts thereof.Type: ApplicationFiled: March 2, 2012Publication date: February 7, 2013Inventors: Irena KRIZMANIC, Jasna Dogan, Marina Marinkovic, Maja Sepelj
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Patent number: 8367682Abstract: The invention relates to new pyrimidine compounds of formula (1) wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (1) are useful in the control of parasites, in particular ectoparasites, in and on warmblooded animals.Type: GrantFiled: July 17, 2007Date of Patent: February 5, 2013Assignee: Novartis AGInventors: Noëlle Gauvry, François Pautrat, Jacques Bouvier, Jörg Früchtel, Beatrice Bapst, Sandra Schorderet Weber
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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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Patent number: 8362248Abstract: The present invention relates to certain substituted pyridinyl and pyrimidinyl derivatives of Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.Type: GrantFiled: July 6, 2006Date of Patent: January 29, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Juerg Lehmann
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Patent number: 8357798Abstract: Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.Type: GrantFiled: June 4, 2010Date of Patent: January 22, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin M. Belyk, Henry G. Morrison, Philip Jones, Vincenzo Summa, V. Brett Cooper, Amar J. Mahajan, Daniel J. Kumke, Hsien-Hsin Tung, Lawrence Wai, Vanessa Pruzinsky, Philip Pye, Remy Angelaud, Danny Mancheno