Additional Hetero Ring Patents (Class 514/422)
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Publication number: 20140336174Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: ApplicationFiled: April 17, 2014Publication date: November 13, 2014Applicant: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
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Publication number: 20140336158Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.Type: ApplicationFiled: July 25, 2014Publication date: November 13, 2014Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
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Publication number: 20140329802Abstract: The purpose is to provide a compound which has an intestinal phosphate transporter (NPT-IIb) inhibitory action and is useful as an active ingredient of an agent for treating and/or preventing hyperphosphatemia. A tetrahydrobenzothiophene compound of the following formula (I) has NPT-IIb inhibitory action and can be used as an agent for treating and/or preventing hyperphosphatemia: wherein, R1 represents —O-lower alkyl, -lower alkylene-phenyl, or the like; R2 and R3 are the same as or different from each other and represent H, lower alkyl, cycloalkyl, aryl, heteroaryl or the like, or, R2 and R3 may be combined with a nitrogen atom to which they bind to form 5- to 7-membered saturated cyclic amino; R4's are the same as or different from each other and represent halogen, lower alkyl; and n represents 0 to 2.Type: ApplicationFiled: March 28, 2014Publication date: November 6, 2014Applicant: Astellas Pharma Inc.Inventors: Shunichiro HACHIYA, Masanori Miura, Yoshimasa Imamura, Daisuke Kaga, Ippei Sato, Hiroyuki Moritomo, Koji Kato, Kazuhiro Terai, Yoh Terada
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Publication number: 20140328896Abstract: Provided are methods and compositions for enhancing the gastrointestinal health of an animal in need thereof by administering a gastrointestinal health maintaining or improving amount of a composition comprising an effective amount of lactic acid. The administered composition may also comprise one or more prebiotic, probiotic, symbiotic, anti bacterial, or anti-diarrhea agents.Type: ApplicationFiled: December 29, 2011Publication date: November 6, 2014Applicant: HILL'S PET NUTRITION, INC.Inventors: Dennis Jewll, Luis J. Montelongo, Sarah Martinez, Lynda Melendez
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Publication number: 20140329796Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Ajinomoto Co., Inc.Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
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Publication number: 20140329823Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Applicant: TETRALOGIC PHARMACEUTICALS CORPORATIONInventors: Stephen M. Condon, Matthew G. Laporte, Yijun DENG, Susan R. Rippin
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Publication number: 20140323502Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula I: as defined in the specification. The invention is also directed to compositions containing and uses of the compounds of formula I.Type: ApplicationFiled: February 13, 2014Publication date: October 30, 2014Inventors: Anton Franz Joseph Fliri, Randall James Gallaschun, Christopher John O'Donnell, Jacob Bradley Schwarz, Barbara Eileen Segelstein
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Patent number: 8871798Abstract: This disclosure relates to compounds of formula I: wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.Type: GrantFiled: October 16, 2012Date of Patent: October 28, 2014Assignee: SanofiInventors: Karl Schoenafinger, Henning Steinhagen, Bodo Scheiper, Uwe Heinelt, Volkmar Herrmann, Matthias Herrmann
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Patent number: 8871753Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.Type: GrantFiled: April 23, 2009Date of Patent: October 28, 2014Assignee: Incyte CorporationInventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
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Publication number: 20140309208Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are disclosed that are represented by general formula (I). Also disclosed, are pharmaceutical compositions including these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated pathologies.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
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Patent number: 8853196Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: GrantFiled: August 3, 2012Date of Patent: October 7, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
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Patent number: 8853255Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: April 25, 2013Date of Patent: October 7, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Eric L. Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam D. Hughes, Lori Jean Patterson
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Patent number: 8853126Abstract: The present invention relates to compositions for controlling plant pests containing the compound of the formula (I) in a mixture with specified fungicidally active compounds.Type: GrantFiled: February 29, 2012Date of Patent: October 7, 2014Assignee: Bayer AktiengesellschaftInventors: Christoph Eredelen, Wolfram Andersch, Klaus Stenzel, Astrid Mauler-Machnik, Wolfgang Kraemer
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Publication number: 20140296254Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds are described that correspond to general formula (I). Also described, are pharmaceutical compositions that include these compounds and methods of using these compounds and compositions for the treatment of chemokine-mediated diseases.Type: ApplicationFiled: October 26, 2012Publication date: October 2, 2014Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Branislav Musicki, Jerôme Aubert, Jean-Guy Boiteaux, Laurence Clary, Patricia Rossio, Marlène Schuppli-Nollet
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Publication number: 20140296287Abstract: Disclosed herein are methods of treating a patient suffering from a cognitive disorder using compounds of Formulas 1 and 2 wherein the variables have the meaning disclosed in the specificationType: ApplicationFiled: March 18, 2014Publication date: October 2, 2014Applicant: Allergan, Inc.Inventors: John E. Donello, Fabien J. Schweighoffer, Lauren M. Luhrs
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Publication number: 20140294873Abstract: The invention provides a screening assay for selecting inhibitors of NFAT:Transcription factor interactions. The invention also provides compositions and methods for inhibiting immune response in a subject.Type: ApplicationFiled: November 8, 2012Publication date: October 2, 2014Applicant: Children Medical Center CorporationInventors: Srimoyee Ghosh, Anjana Rao, Patrick G. Hogan
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Publication number: 20140294851Abstract: Base-labile crosslinkers, base-labile conjugates comprising such crosslinkers, methods of their synthesis and use are disclosed.Type: ApplicationFiled: April 1, 2013Publication date: October 2, 2014Inventor: MARK QUANG NGUYEN
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Patent number: 8846655Abstract: 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, R2, R3, Ra, and Y are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: September 30, 2014Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Haiyan Bian, Chaozhong Cai, Bart L. DeCorte, Li Liu, Mark J. Macielag, Scott L. Dax, Philip M. Pitis, Peter J. Connolly, Wei He
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Patent number: 8846674Abstract: The invention provides methods for treating ophthalmic disorders comprising at least one nitric oxide enhancing prostaglandin compound or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The nitric oxide enhancing prostaglandin compounds comprise at least one heterocyclic nitric oxide donor group and/or at least one nitroxide group.Type: GrantFiled: October 18, 2011Date of Patent: September 30, 2014Assignee: Nicox, S.A.Inventor: David S. Garvey
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Publication number: 20140288144Abstract: A compound of formula (I): R?—O-A-O—R??, in which R? and R? are a hydrogen atom or a monovalent radical of formula (IIa), or a monovalent radical of formula (IIb), it being understood that at least one of the radicals R? or R? is not a hydrogen atom and that, when none of the radicals R? and R? is a hydrogen atom, R? and R? are identical, and in which A is a divalent radical of formula (III): —CH(X1)-[C(X2)(X3)]p-CH(X4) in which X1, X2, X3 and X4 are identical or different and are either a hydrogen atom or a methyl radical or an ethyl radical, and p is an integer greater than or equal to 1 and less than or equal to 6. Also the method for preparing the compound of formula (I) and to the use thereof in cosmetics and as a drug.Type: ApplicationFiled: October 12, 2012Publication date: September 25, 2014Applicant: Societe D'Exploitation de Produits Pour Les Industries Chimiques SeppicInventors: Sandy Dumont, Jerome Guilbot, Stephanie Garcel, Laetitia Cattuzzato
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Publication number: 20140288065Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
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Publication number: 20140287988Abstract: Provided herein are compositions, which include an active pharmaceutical ingredient and macrogol 15 hydroxystearate, and methods for using the same for treating diseases or disorder.Type: ApplicationFiled: December 9, 2013Publication date: September 25, 2014Applicant: ALLERGAN, INC.Inventors: ANURADHA V. GORE, KEVIN S. WARNER, CHETAN P. PUJARA, RICHARD S. GRAHAM, AJAY P. PARASHAR, MU-LAN LEE, ROBERT S. JORDAN, SUKHON LIKITLERSUANG
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Publication number: 20140288106Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.Type: ApplicationFiled: June 3, 2014Publication date: September 25, 2014Applicant: SanofiInventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
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Publication number: 20140286931Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 5, 2014Publication date: September 25, 2014Inventor: Chengzhi Zhang
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Publication number: 20140275020Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
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Publication number: 20140275203Abstract: The present invention is for method of treating metabolic bone disease, new compounds and pharmaceutical compositions comprising the active ingredients having inhibition effects on osteoclast differentiation. The pharmaceutical composition comprising new compounds according to the present invention can be used as medicines for treating metabolic bone diseases such as bone metastatic cancer, solid cancer bone metastasis, musculoskeletal complication by solid cancer bone metastasis, hypercalcemia by malignant tumor, multiple myeloma, primary bone tumor, osteoporosis, rheumatoid arthritis, osteoarthritis, periodontal disease, inflammatory resorption of alveolar bone, inflammatory resorption of bone, and Paget's disease.Type: ApplicationFiled: June 2, 2014Publication date: September 18, 2014Applicant: Metacine, Inc.Inventors: Bae Keun PARK, Sung-Hwa YOON, Ju-Young PARK, Sung Hoon PARK
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Publication number: 20140275068Abstract: The present invention provides neuronal gap junction blocking compounds according to formula (I) or a hydrate, solvate, or pharmaceutically acceptable salt thereof: wherein the integers Q, R2, A, R1, Z1, Z2, and Z3 are as defined in claim 1. The compounds are useful for the treatment or prevention of a range of conditions including, e.g., migraine, epilepsy, non-epileptic seizures, brain injury, and cardiovascular disease.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Proximagen LimitedInventors: Edward Savory, Daniel Hill, Oldrich Kocian
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Publication number: 20140275008Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Qing Xu, Zhe Li
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Publication number: 20140275005Abstract: The present disclosure relates to a series of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and formula (Ib). wherein R1, R2, R3, R4, X, m, l, n, p and s are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure relates to methods of preparation of substituted phenyl cycloalkyl pyrrolidine (piperidine) spirolactams and amides of formula (Ia) and (Ib), and intermediates therefor.Type: ApplicationFiled: May 5, 2014Publication date: September 18, 2014Applicant: SanofiInventor: Zhongli GAO
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Publication number: 20140275079Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
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Publication number: 20140256712Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: March 12, 2014Publication date: September 11, 2014Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
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Patent number: 8822523Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; X is methine or nitrogen; A is R5 is hydrogen, halogen, -?-C1-C6alkyl, -?-C3-C7cycloalkyl or -?-aryl; R6 is hydrogen, halogen, -?-C1-C6alkyl, -?-C3-C7cycloalkyl or -?-aryl; and agrochemically acceptable salts/isomers/structural isomers/stereoisomers/diastereoisomers/enantiorners/tautorriers and N-oxides of those compounds are suitable for use as microbiocides.Type: GrantFiled: February 16, 2012Date of Patent: September 2, 2014Assignee: Syngenta Participations AGInventors: Harald Walter, Daniel Stierli
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Patent number: 8822526Abstract: A novel pharmaceutical combination comprising a cytotoxic antineoplastic agent selected from a the group consisting of paclitaxel, docetaxel, doxorubicin and gemcitabine or a pharmaceutically acceptable salt thereof and at least one cyclin dependent kinase (CDK) inhibitor; wherein the said combination exhibits synergistic effects when used in the treatment of cancer. The invention also relates to a method for the treatment of cancer, using a therapeutically effective amount of the said combination.Type: GrantFiled: May 15, 2007Date of Patent: September 2, 2014Assignee: Piramal Enterprises LimitedInventors: Maggie Rathos, Kalpana Joshi, Harshal Khanwalkar, Somesh Sharma
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Publication number: 20140243324Abstract: The present invention relates to uses of small molecule mimetics of hematopoietic growth factors. In particular the present invention relates to uses of small molecule mimetics of erythropoietin.Type: ApplicationFiled: November 17, 2011Publication date: August 28, 2014Applicant: LIGAND PHARMACEUTICALS INCORPORATEDInventors: Reid P. Bissonnette, Andrew R. Hudson, Keith B. Marschke, Deepa Rungta, Lin Zhi
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Patent number: 8815869Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, n, R1, X and Y are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: March 10, 2011Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Irene Drizin, George Doherty, Pramila A. Bhatia, Andrew O. Stewart
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Patent number: 8815871Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.Type: GrantFiled: March 11, 2013Date of Patent: August 26, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Muneaki Kurimura, Shinichi Taira, Takahiro Tomoyasu, Nobuaki Ito, Kuninori Tai, Noriaki Takemura, Takayuki Matsuzaki, Yasuhiro Menjo, Shin Miyamura, Yohji Sakurai, Akihito Watanabe, Yasuyo Sakata, Takumi Masumoto, Kohei Akazawa, Haruhiko Sugino, Naoki Amada, Satoshi Ohashi, Tomoichi Shinohara, Hirofumi Sasaki, Chisako Morita, Junko Yamashita, Satoko Nakajima
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Publication number: 20140235681Abstract: Disclosed herein is method of treating glaucoma or ocular hypertension comprising administering a prostaglandin agonist and a second therapeutically active agent to a mammal in need thereof, wherein said second therapeutically active agent is selected from: ?-Blockers, Adrenergic Agonists, non-selective adrenergic agonists, ?2-selective adrenergic agonists, Carbonic Anhydrase Inhibitors, Cholinergic Agonists, direct acting cholinergic agonists, chlolinesterase inhibitors, Glutamate Antagonists, Ca2+ channel blockers, Prostamides, Prostaglandins, Cannabinoids, and combinations thereof. Compositions and medicaments containing a combination of these two active agents are also disclosed.Type: ApplicationFiled: December 6, 2013Publication date: August 21, 2014Applicant: ALLERGAN, INC.Inventors: SCOTT M. WHITCUP, ROBERT M. BURK, DAVID W. OLD, YARIV DONDE, WHA-BIN IM, MARK A. HOLOBOSKI
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Publication number: 20140228321Abstract: The present invention provides compounds of Formula (I): (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 24, 2012Publication date: August 14, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Heather Finlay, Ji Jiang, John Lloyd, Carol Hui Hu, Zulan Pi, George O. Tora, James Neels, Jon J. Hangeland, Todd J. Friends
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Publication number: 20140228416Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: September 12, 2013Publication date: August 14, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8802665Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: GrantFiled: February 14, 2013Date of Patent: August 12, 2014Assignee: Genentech, Inc.Inventors: David Banner, Wolfgang Haap, Thomas Luebbers, Jens-Uwe Peters
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Patent number: 8802692Abstract: This invention is based on the discovery that the administration of a sphingosine-1-phosphate receptor antagonist (S1P) and at least one chemotherapeutic agent selected from the the group of antimicrotubule agents provides an unexpectedly superior treatment for cancer. Antimicrobial agents such as the taxane compounds are known in the art, for example, paclitaxel (available as TAXOL® from Bristol-Myers Squibb, Princeton, N.J.), docetaxel (available as TAXOTERE® from Sanofi-aventis, Bridgewater, N.J.) and the like and other compounds that act as antimicrotubule agents, such as Vincristine (ONCOVIN®, VINCASAR PFS®, VCR), Vinblastin (VELBAN®, VELSAR®) and Vinorelbine, and similar compounds. The present invention also provides methods of modulating the growth of selected cell populations, such as cancer cells, by administering a therapeutically effective amount of at least one sphingosine-1-phosphate 1 (S1P1R) receptor antagonists, and at least one antimicrotubule agent.Type: GrantFiled: October 16, 2009Date of Patent: August 12, 2014Assignee: Exelixis, Inc.Inventors: Geetha Shankar, Frauke Bentzien, Peter Lamb, David Matthews
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Patent number: 8802716Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.Type: GrantFiled: June 25, 2013Date of Patent: August 12, 2014Assignee: TetraLogic Pharmaceuticals CorporationInventors: Stephen M. Condon, Matthew G. LaPorte, Yijun Deng, Susan R. Rippin
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Publication number: 20140219915Abstract: Disclosed herein is a method for coupling a first compound having the formula (I) with a second compound that contains a carbonyl group. Also disclosed herein are compounds that can be formed by this method, and uses for such compounds.Type: ApplicationFiled: July 6, 2012Publication date: August 7, 2014Applicants: AUSTRALIAN NUCLEAR SCIENCE AND TECHNOLOGY ORGANISATION, THE AUSTRALIAN NATIONAL UNIVERSITYInventors: Suzanne Virginia Smith, Eskender Mume, Gary James Perkins
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Publication number: 20140221349Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias ECKHARDT
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Publication number: 20140221342Abstract: Provided herein is a method of treating an allergic inflammatory disease selected from asthma, dermatitis, allergic rhinitis, urticaria, anaphylaxis, angioedemea, allergies, contact hypersensitivity, drug hypersensitivity, and allergic conjunctivitis in a mammal, comprising administering a therapeutically effective amount of a compound of Formula I or a pharmaceutically acceptable salt thereof, to said mammal in need thereof, wherein A1, A2, W, L, G, R7a, R7b, R8, R9 and R10 are as defined herein.Type: ApplicationFiled: March 31, 2014Publication date: August 7, 2014Applicant: Array BioPharma Inc.Inventors: Laurence E. Burgess, Christopher T. Clark, Adam Cook, Christopher P. Corrette, Robert Kirk DeLisle, George A. Doherty, Kevin W. Hunt, Todd T. Romoff, Ganghyeok Kim
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Publication number: 20140213588Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments. The disclosure also provides a novel method of treating diseases or conditions related to the activity of endothelial lipase by use of compounds according to Formula (II): as defined in the specification and compositions comprising any of the compounds.Type: ApplicationFiled: September 26, 2012Publication date: July 31, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Patent number: 8791102Abstract: This disclosure relates to sphingosine-1-phosphate (S1P) receptor antagonists, compositions comprising the S1P receptor antagonists and methods for using and processes for making the S1P receptor antagonists. In particular, this disclosure relates to sphingosine-1-phosphate 1 (S1P1) receptor antagonists, compositions comprising the S1P1 receptor antagonist and methods for using the S1P1 receptor antagonist, such as in the treatment of cancer, and processes for making the S1P1 receptor antagonists.Type: GrantFiled: October 16, 2009Date of Patent: July 29, 2014Assignee: Exelixis, Inc.Inventors: Mohamed Abdulkader Ibrahim, Joon Won Jeong, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Gary L. Lewis, Robin Tammie Noguchi, John M. Nuss
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Patent number: 8778835Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: July 5, 2007Date of Patent: July 15, 2014Assignee: Bayer Cropscience AGInventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel
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Publication number: 20140194480Abstract: The present invention provides a method for controlling termites comprising applying a liquid formulation comprising a compound of formula I to a location where termite control is needed or is expected to be needed, wherein the compound of formula (I) is wherein X is optionally substituted aryl, optionally substituted heterocyclyl, or a group selected from X1 to X5 cycle A is aryl or heteroaryl; cycle B is a saturated or partially unsaturated heterocyclyl; cycle C is aryl or heteroaryl; R1, R2, R3, R4, R5, R6 and R8 are independently hydrogen or an organic radical; R7 is haloalkyl; G is oxygen or sulfur; L is O, NH, NR1, CR3R4; n is 0, 1, 2, 3, 4 or 5; o is 0, 1, 2, 3, 4 or 5; p is 1, 2, 3, 4 or 5. The invention also relates to methods for protecting man-made structures from termites using the compounds of formula I as well as termite baits comprising the compound of formula I.Type: ApplicationFiled: August 27, 2012Publication date: July 10, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Mark Hoppe, Myriem El Qacemi, Jerome Yves Cassayre
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Publication number: 20140194425Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: N30 Pharmaceuticals, Inc.Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu