The Additional Ring Is A Six-membered Hetero Ring Consisting Of One Nitrogen And Five Carbon Atoms Patents (Class 514/318)
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Patent number: 8754097Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: August 22, 2012Date of Patent: June 17, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Patent number: 8754107Abstract: The present invention is directed to novel aminopyrrolidines of formula I pharmaceutically acceptable salts thereof, metabolites thereof, isomers thereof, stereoisomers thereof or pro-drugs thereof, wherein the variables are as defined herein. The compounds of formula (I) are useful as chemokine receptor antagonists and as such would be useful in treating certain conditions and diseases, especially inflammatory conditions and diseases and proliferative disorders and conditions, for example, cancers.Type: GrantFiled: November 16, 2007Date of Patent: June 17, 2014Assignee: AbbVie Inc.Inventors: Dawn M. George, Richard W. Dixon, Michael Friedman, Adrian D. Hobson, Biqin Li, Lu Wang, Xiaoyun Wu, Neil Wishart
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Patent number: 8754226Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R6, R6a, R7, R9, R9a, and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: GrantFiled: May 13, 2011Date of Patent: June 17, 2014Assignee: Array BioPharma Inc.Inventors: Thomas Daniel Aicher, Josef Roland Bencsik, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt, Ajay Singh, Timothy M. Turner, David A. Mareska, Steven Armen Boyd
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Publication number: 20140162983Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.Type: ApplicationFiled: June 10, 2012Publication date: June 12, 2014Applicant: Merck Patent GmbHInventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
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Publication number: 20140163024Abstract: Compounds of the formula Ia or Ib: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, Y, Z, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 10, 2013Publication date: June 12, 2014Applicant: GENENTECH, INC.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Simon Gaines, Jonathan Killen, Stuart Ward
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Patent number: 8748613Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.Type: GrantFiled: December 28, 2012Date of Patent: June 10, 2014Assignee: Chiesi Farmaceutici S.p.A.Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
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Patent number: 8748420Abstract: Pyridinylcarboxylic acid derivatives of the formula (I) in which the symbols A, X, Y1, Y2, Y3, L1, L2, RG and R1 are each as defined in the description, and also salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: GrantFiled: November 8, 2013Date of Patent: June 10, 2014Assignee: Bayer CropScience AGInventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Nicola Rahn, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
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Patent number: 8748459Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HTlF receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.Type: GrantFiled: February 1, 2012Date of Patent: June 10, 2014Assignee: Eli Lilly and CompanyInventors: Michael Philip Cohen, Daniel Timothy Kohlman, Sidney Xi Liang, Frantz Victor, Yao-Chang Xu, Bai-Ping Ying, DeAnna Piatt Zacherl, Deyi Zhang
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Publication number: 20140155391Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.Type: ApplicationFiled: December 5, 2013Publication date: June 5, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Elisabetta ARMANI, Gabriele Amari, Oriana Esposito, Laura Carzaniga, Carmelida Capaldi
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Publication number: 20140155377Abstract: The present invention relates to 3-cycloalkylaminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as modulators of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Amy Qi Han, Darius J. Robinson, Changsheng Zheng, Anlai Wang, Yingxin Zhang
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Publication number: 20140155410Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R11, R12, R13, Q, Z, and p are as described herein. Compounds of the present invention are useful for the treatment of cancers.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: GlaxoSmithKline LLCInventors: Jerry Leroy Adams, Thomas H. Faitg, Neil W. Johnson, Jiri Kasparec, Hong Lin, Mark Mellinger, Xin Peng, Ren Xie
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Patent number: 8742115Abstract: This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.Type: GrantFiled: October 6, 2011Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Markus Frank, Hans Haeberle, Manuel Henry, Thorsten Pachur, Marco Santagostino, Uwe Stertz, Thomas Trebing, Ulrike Werthmann
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Publication number: 20140148477Abstract: The present invention provides an animal ectoparasite-controlling agent and a method for preventing or treating infection in animals caused by parasites by using the controlling agent. An animal ectoparasite-controlling agent exhibiting excellent insecticidal activity, and a method for preventing or treating infection in animals caused by parasites by using the controlling agent are obtained by using a compound having a pyrazole ring at the 4-position of the piperidine ring as an active ingredient.Type: ApplicationFiled: July 19, 2012Publication date: May 29, 2014Applicant: OTSUKA AGRITECHNO CO., LTD.Inventors: Yasuhiro Endo, Yuichi Shirai
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Publication number: 20140148457Abstract: Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: April 12, 2012Publication date: May 29, 2014Applicant: MERCK PATENT GMBHInventors: Srinivasa R. Karra, Wolfgang Staehle, Eike Staub, Margarita Wucherer-Plietker
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Publication number: 20140148467Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: February 3, 2014Publication date: May 29, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Patent number: 8735426Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a process for the producing such compounds, and the use thereof to treat or inhibit pain and/or various other disorders or conditions.Type: GrantFiled: April 11, 2008Date of Patent: May 27, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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Publication number: 20140142097Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseasesType: ApplicationFiled: April 11, 2012Publication date: May 22, 2014Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
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Publication number: 20140142139Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.Type: ApplicationFiled: November 15, 2013Publication date: May 22, 2014Inventors: Bruce A. Ellsworth, Jun Shi, William R. Ewing, Elizabeth A. Jurica, Andres S. Hernandez, Ximao Wu
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Publication number: 20140142085Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: July 5, 2012Publication date: May 22, 2014Applicant: Gilead Sciences, Inc.Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
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Publication number: 20140142083Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: April 13, 2012Publication date: May 22, 2014Applicant: EPIZYME, INC.Inventors: Kevin Wayne Kuntz, Richard Chesworth, Kenneth William Duncan, Heike Keilhack, Natalie Warholic, Christine Klaus, Sarah K. Knutson, Timothy James Nelson Wigle, Masashi Seki
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Patent number: 8729084Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, L, m, n, o, p, R2, R3, R3, R4 and R5 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: GrantFiled: May 4, 2011Date of Patent: May 20, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl
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Patent number: 8729069Abstract: The invention relates to compounds of structural formula (Ia): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, X4, X6, X10, R1, Y, Z, L, and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 28, 2010Date of Patent: May 20, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Gary Bohnert, Shoujun Chen, Yu Xie
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Publication number: 20140135307Abstract: This invention relates to co-crystals and salts of CCR3 inhibitors of formula 1, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases related with the CCR3-receptor.Type: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Markus FRANK, Hans HAEBERLE, Manuel HENRY, Thorsten PACHUR, Marco SANTAGOSTINO, Uwe STERTZ, Thomas TREBING, Ulrike WERTHMANN
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Publication number: 20140135305Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: December 12, 2013Publication date: May 15, 2014Applicant: PTC THERAPEUTICS, INC.Inventors: Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
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Publication number: 20140135329Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 20, 2013Publication date: May 15, 2014Inventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Publication number: 20140135301Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: January 22, 2014Publication date: May 15, 2014Applicant: Chiesi Farmaceutici S.p.A.Inventors: Maurizio Delcanale, Elisabetta Armani, Gabriele Amari
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Publication number: 20140135361Abstract: The present invention provides inhibitors of allergy, and allergic reactions specifically compounds of the present invention are described by the following chemical Formula I: A method for treating an allergic reaction, or allergy diseases or disorders includes administering a therapeutically effective composition comprising a compound of Formula I or a pharmaceutically acceptable salt, solvate or prodrug thereof and a pharmaceutically acceptable carrier, vehicle or excipient to a subject in need thereof.Type: ApplicationFiled: June 27, 2012Publication date: May 15, 2014Inventors: Tongjun Lin, Jun XIN
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Patent number: 8722663Abstract: The present invention provides a novel compound having an excellent antitumor effect. The compound of the present invention is represented by the following general formula (1) wherein R1 and R2 are aryl or the like; A is lower alkylene; Ring X is optionally substituted arylene; E is bond or lower alkenylene; Ring Y is optionally substituted heterocycloalkylene containing one or more nitrogen atoms, one of which is attached to the adjacent carbonyl group; G is —NH-G2-, —N(lower alkyl)-G2-, —NH—CH2-G2-, —N(lower alkyl)-CH2-G2- or —CH2-G2-, [wherein G2 binds to R2, G2-R2 is bond-R2, phenylene-G3-R2, phenylene-G4-O—R2, phenylene-G5-NH—R2, phenylene-G6-N(lower alkyl)-R2 or quinolinediyl-O—R2, the phenylene of said phenylene-containing groups being optionally substituted with one or more substituents; G3-R2 is —O-lower alkylene-R2 or the like; G4-O— is lower alkylene-O— or the like; G5 is lower alkylene; G6 is lower alkylene].Type: GrantFiled: January 28, 2011Date of Patent: May 13, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hideki Takasu, Shigekazu Fujita, Shinya Ohtsuka, Toshiyuki Hirose, Yosuke Sato, Satoshi Yamada, Keisuke Miyajima, Koji Sakai, Yutaka Kojima, Kazuo Sekiguchi, Yasuo Yanagihara, Takashi Suzuki, Hideo Tanaka, Kazuhisa Sugiyama, Mitsuhiro Okuno, Takumi Sumida
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Patent number: 8722930Abstract: A compound of formula (I) wherein R1 to R15, P1, P2, A, B and Q are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as matriptase inhibitors and are useful in the treatment of matriptase dependent conditions, particularly cancer.Type: GrantFiled: May 18, 2010Date of Patent: May 13, 2014Assignee: Orion CorporationInventors: Rajeev Goswami, Anil Kumar Vuppala, Ramesh Veludandi, Ramesh Sistla, Chakshusmathi Ghadiyaram, Muralidhara Ramachandra
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Patent number: 8722681Abstract: This invention provides thiazolylpiperazine derivatives, and N-sulfonyl heterocyclic derivatives including phenyl- and benzyl-thiazolylpiperidine derivatives, and pharmaceutically acceptable salts thereof, which are useful active ingredients for administration in a method for the treatment of an ?-synucleopathy such as Parkinson's disease, diffuse Lewy body disease, traumatic brain injury, amyotrophic lateral sclerosis, Niemann-Pick disease, Hallervorden-Spatz syndrome, Down syndrome, neuroaxonal dystrophy, multiple system atrophy and Alzheimer's disease. This invention also provides methods for making such derivatives, and pharmaceutical compositions including such derivatives together with pharmaceutically acceptable excipients.Type: GrantFiled: February 5, 2010Date of Patent: May 13, 2014Assignee: NV reMYNDInventors: Gerard Griffioen, Veronica Rojas De La Parra, Annick Lauwers
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Publication number: 20140128427Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
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Publication number: 20140128393Abstract: The present invention relates to methods of treating cancer by administering the EZH2 inhibitor compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: October 15, 2013Publication date: May 8, 2014Applicant: EPIZYME, INC.Inventors: Sarah K. Knutson, Natalie Warholic, Heike Keilhack
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Publication number: 20140128406Abstract: 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: ApplicationFiled: June 27, 2012Publication date: May 8, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Fredrik Emil Malcolm Cederbaum
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Publication number: 20140128363Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Inventors: Matthew Frank Brown, Ye Che, Anthony Marfat, Michael Joseph Melnick, Justin Ian Montgomery, Usa Reilly
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Publication number: 20140128432Abstract: The present invention relates to diagnostic, therapeutic and prognostic methods for thyroid cancers. In one embodiment, the present invention provides a method for treating a an anaplastic thyroid cancer (ATC) patient comprising the step of administering to the patient an effective amount of an anaplastic lymphoma kinase (ALK) inhibitor. In another embodiment, a method for diagnosing ATC in patient comprises the step of performing an assay on a biological sample from the patient to identify the presence or absence of a C3592T and/or a G3602A mutation in exon 23 of the ALK gene according to SEQ ID NO:6, wherein the presence of either of both of the mutations correlates with a diagnosis of ATC in the patient.Type: ApplicationFiled: May 7, 2012Publication date: May 8, 2014Inventors: Michael Mingzhao Xing, Murugan Avaniyapuram Kannan
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Publication number: 20140128376Abstract: 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: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: Genentech, Inc.Inventor: Xiaojing Wang
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Publication number: 20140128397Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.Type: ApplicationFiled: January 20, 2012Publication date: May 8, 2014Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
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Patent number: 8716283Abstract: The invention, in some aspects, relates to compounds and compositions useful for inhibiting Type III secretion systems in pathogenic bacteria, such as Yersinia Pestis. In some aspects, the invention relates to methods for discovering inhibitors of the Type III secretion system and uses of such inhibitors in the treatment and prevention of disease.Type: GrantFiled: April 1, 2009Date of Patent: May 6, 2014Assignees: University of Massachusetts, President and Fellows of Harvard CollegeInventors: Jon Goguen, Ning Pan, Kyungae Lee
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Patent number: 8716312Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Publication number: 20140121210Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.Type: ApplicationFiled: January 8, 2014Publication date: May 1, 2014Applicant: HELSINN HEALTHCARE SAInventors: Silvina GARCIA RUBIO, Claudio PIETRA, Claudio GIULIANO, Zhigang LI
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Publication number: 20140120112Abstract: The invention provides compositions and methods of predicting a subject's risk of developing age-related macular degeneration (AMD) and methods of treating, delaying, or preventing the development and progression of AMD.Type: ApplicationFiled: December 19, 2013Publication date: May 1, 2014Inventor: Kameran Lashkari
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Publication number: 20140121195Abstract: Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: ApplicationFiled: October 17, 2013Publication date: May 1, 2014Applicant: ChemoCentryx, Inc.Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
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Publication number: 20140121166Abstract: Provided are materials and methods for the prevention and treatment of Juvenile Neuronal Ceroid Lipofuscinosis comprising administration of an effective amount of at least one of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor. In some embodiments, the methods comprise administration of an effective amount of each of a hemi-channel inhibitor and a phosphodiesterase-4 inhibitor. Also provided are pharmaceutical compositions comprising a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor, as well as kits comprising at least one effective dose of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor or a combination of both.Type: ApplicationFiled: October 29, 2013Publication date: May 1, 2014Applicant: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKAInventor: Tammy Kielian
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Patent number: 8710048Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: GrantFiled: April 23, 2012Date of Patent: April 29, 2014Assignee: Novartis AGInventors: James C. Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M. Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith B. Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
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Patent number: 8710049Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: GrantFiled: July 16, 2012Date of Patent: April 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
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Publication number: 20140113892Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4-P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: May 10, 2013Publication date: April 24, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Patent number: 8703934Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: November 17, 2007Date of Patent: April 22, 2014Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süβmeier, Joerg Keldenich
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Patent number: 8703721Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: GrantFiled: May 12, 2011Date of Patent: April 22, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Publication number: 20140107122Abstract: The present invention relates to substituted benzene compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Inventors: Kevin Wayne Kuntz, John Emmerson Campbell, Masashi Seki