Polycyclo Ring System Having The 1,2-diazole Ring As One Of The Cyclos Patents (Class 546/275.7)
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Publication number: 20140336224Abstract: Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: November 13, 2014Inventors: Ping Lan, Kun Liu, Anthony Ogawa, Hong Shen, Christine Yang, Yuguang Wang, Richard Beresis, Changhe Qi
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Publication number: 20140336377Abstract: The present invention relates to arylamide 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: October 18, 2011Publication date: November 13, 2014Applicant: RAQUALIA PHARMA INC.Inventors: Tatsuya Yamagishi, Kiyoshi Kawamura, Yoshimasa Arano, Mikio Morita
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Patent number: 8883821Abstract: The present invention relates to a compound of following formula (I): or a pharmaceutically acceptable salt or solvate of same, a tautomer of same, or a stereoisomer or mixture of stereoisomers of same in any proportions, such as a mixture of enantiomers, notably a racemic mixture; as well as to the use of same as a drug, notably intended for the treatment of cancer, inflammation and neurodegenerative diseases such as Alzheimer's disease; to the use of same as a kinase inhibitor; to the pharmaceutical compositions comprising same; and to methods for the preparation of same.Type: GrantFiled: November 27, 2012Date of Patent: November 11, 2014Assignee: Pierre Fabre MedicamentInventors: El Bachir Kaloun, Karim Bedjeguelal, Rémi Rabot, Anna Kruczynski, Philippe Schmitt, Michel Perez, Nicolas Rahier
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Patent number: 8883801Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.Type: GrantFiled: August 22, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
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Patent number: 8883850Abstract: The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: May 23, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
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Publication number: 20140309225Abstract: The object of the present invention is to provide a compound and a pharmaceutical composition having excellent Syk inhibitory activity. According to the present invention, a nicotinamide derivative represented by the following formula (I) or a salt thereof is provided, wherein R1 is a substituent represented by the following formula (II-1), (III-1), or (IV-1) (wherein R3, R4, R5, n, and X1 have the same definitions as those described in the specification), and R2 is a pyridyl, indazolyl, phenyl, pyrazolopyridyl, benzisoxazolyl, pyrimidinyl, or quinolyl group, each of which optionally has at least one substituent.Type: ApplicationFiled: June 27, 2014Publication date: October 16, 2014Applicant: FUJIFILM CorporationInventors: Hideyasu FUJIWARA, Shinsuke MIZUMOTO, Yohei KUBO, Hiyoku NAKATA, Shinji HAGIWARA, Yasutaka BABA, Takashi TAMURA, Hidenobu KUNIYOSHI, Tomoyuki MASHIKO, Mari YAMAMOTO
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Publication number: 20140303164Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are 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: February 28, 2014Publication date: October 9, 2014Inventors: Gediminas BRIZGYS, Eda CANALES, Chien-Hung CHOU, Michael GRAUPE, Yunfeng Eric HU, John O. LINK, Qi LIU, Yafan LU, Roland D. SAITO, Scott D. SCHROEDER, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
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Publication number: 20140303186Abstract: The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.Type: ApplicationFiled: November 16, 2012Publication date: October 9, 2014Inventors: Yan Zhang, Min Zhang, Hoyin Lo
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Patent number: 8853207Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.Type: GrantFiled: April 12, 2012Date of Patent: October 7, 2014Assignee: Development Center for BiotechnologyInventors: Chu-Bin Liao, Chao-Cheng Chiang, Huei-Ru Yang, Yuan-Chun Liao, Paonien Chen
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Publication number: 20140296266Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are 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: February 28, 2014Publication date: October 2, 2014Inventors: Yunfeng Eric HU, John O. LINK, Qi LIU, Winston C. TSE, Jennifer R. ZHANG
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Patent number: 8846935Abstract: Herein are disclosed indazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: GrantFiled: May 5, 2011Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Celine Duquenne, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20140288090Abstract: The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), inhibit cdk5-mediated phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes or obesity. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.Type: ApplicationFiled: November 20, 2012Publication date: September 25, 2014Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Amy S. Ripka, Jeffrey O. Saunders
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Publication number: 20140288124Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: September 25, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
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Publication number: 20140274695Abstract: 4-Amino-6-(heterocyclic)picolinic acids and their derivatives; 6-amino-2-(heterocyclic)pyrimidine-4-carboxylates and their derivatives; and methods of using the same as herbicides.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: Dow AgroSciences LLCInventors: Joseph D. Eckelbarger, Jeffrey B. Epp, Stephen Craig Fields, Lindsey G. Fischer, Natalie C. Giampietro, Katherine A. Guenthenspberger, Christian T. Lowe, Jeff Petkus, Joshua Roth, Norbert M. Satchivi, Paul R. Schmitzer, Thomas L. Siddall, Nick X. Wang
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Publication number: 20140275074Abstract: The present invention is related to a compound represented by formula (I), wherein X1, X2, X3, X4, X5, R5, R6, R7, R8, n, p, q, ring A and ring B are as described in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 24, 2012Publication date: September 18, 2014Inventors: Kayoko Hata, Manami Masuda, Hiromi Nakai, Daisuke Taniyama, Hiroyuki Tobinaga, Yoshio Hato, Motohiro Fujiu
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Patent number: 8829195Abstract: The present invention relates to compounds of formula (I): in which Y, Y1, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: GrantFiled: May 13, 2013Date of Patent: September 9, 2014Assignee: Novartis AGInventors: Stephanie Kay Dodd, Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Patent number: 8829026Abstract: The present invention relates to sulfamoyl benzoic acid heterobicyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof or a prodrug thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders which are mediated via the TRPMb8 receptor.Type: GrantFiled: October 3, 2011Date of Patent: September 9, 2014Assignee: RaQualia Pharma Inc.Inventors: Kiyoshi Kawamura, Yuji Shishido, Masashi Ohmi
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Patent number: 8822447Abstract: The present invention is directed to substituted indazole compounds of formula (I) pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.Type: GrantFiled: April 21, 2011Date of Patent: September 2, 2014Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Marta C. Abad, Alan C. Gibbs, Gee-Hong Kuo, Lawrence C. Kuo, Fengbin Song, Zhihua Sui
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Patent number: 8816092Abstract: A compound represented by formula (1) or salt thereof and a production intermediate thereof are created. The compound exhibited an excellent antioxidation action in a microsome lipid peroxidation measuring system using a rat liver microsome. Therefore, the compound or salt thereof is useful as an antioxidant. The present invention also provides use of a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof for production of an antioxidant.Type: GrantFiled: May 26, 2011Date of Patent: August 26, 2014Assignee: Ube Industries, Ltd.Inventors: Masahiko Hagihara, Ken-ichi Komori, Hidetoshi Sunamoto, Hiroshi Nishida, Yasunori Tsuzaki, Akira Takama, Kazutaka Kido, Tomokazu Fujimoto, Takeshi Matsugi
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Publication number: 20140221347Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof are disclosed. Also disclosed are 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: January 9, 2014Publication date: August 7, 2014Applicant: Gilead Sciences, Inc.Inventors: Gediminas BRIZGYS, Chien-Hung CHOU, Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, John R. SOMOZA, Winston C. TSE, Jennifer R. ZHANG
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Patent number: 8791140Abstract: The present invention relates to crystalline polymorphic and amorphous form of 6-[2-(methylcarbamoyl)phenyl sulfanyl]-3-E-[2-(pyridin-2-yl)ethenyl]indazole and to methods for their preparation. The invention is also directed to pharmaceutical compositions containing at least one polymorphic form and to the therapeutic or prophylactic use of such polymorphic forms and compositions.Type: GrantFiled: March 25, 2008Date of Patent: July 29, 2014Assignee: Pfizer Inc.Inventors: Anthony Michael Campeta, Brian Patrick Chekal, Robert Alan Singer
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Patent number: 8785478Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: GrantFiled: April 11, 2013Date of Patent: July 22, 2014Assignee: Biota Scientific Management Pty Ltd.Inventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
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Publication number: 20140199263Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 16, 2012Publication date: July 17, 2014Inventors: Casey Cameron McComas, Nigel J. Liverton, Joerg Habermann, Uwe Koch, Frank Narjes, Peng Li, Xuanjia Peng, Richard Soll, Hao Wu, Anandan Palani, Xing Dai, Hong Liu, Shuwen He, Zhong Lai, Qun Dang, Nicolas Zorn
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Patent number: 8778977Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.Type: GrantFiled: July 2, 2007Date of Patent: July 15, 2014Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
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Publication number: 20140194470Abstract: The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt: in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH2, —CH(R?)—, —NH(R?)— or a heteroatom chosen from O and S, it being understood that R? represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO2—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; orType: ApplicationFiled: March 7, 2014Publication date: July 10, 2014Applicant: SANOFIInventors: Jean-Michel Altenburger, Valerie Fossey, Stephane Illiano, Geraldine Manette
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Publication number: 20140194469Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 5, 2013Publication date: July 10, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Patent number: 8771665Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: GrantFiled: December 16, 2011Date of Patent: July 8, 2014Assignee: Cocrystal Discovery, Inc.Inventors: Sam S K Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Patent number: 8765748Abstract: The present invention is directed to a compound is represented by Structural Formula (A): or a pharmaceutically acceptable salt thereof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 19, 2008Date of Patent: July 1, 2014Assignee: University Health NetworkInventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
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Publication number: 20140179676Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: ABBVIE INC.Inventors: Kevin P. Cusack, Thomas D. Gordon, Michael Z. Hoemann, David C. Ihle, Bin Li, Gloria Y. Lo Schiavo, Gagandeep K. Somal, Michael Friedman, Martin E. Hayes, Wouter Iwema Bakker
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Publication number: 20140171432Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted 3-aminopyridine derivative compounds, substituted 3-aminopyridazine derivative compounds, and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 19, 2013Publication date: June 19, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Toufike Kanouni, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Publication number: 20140162985Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: September 6, 2013Publication date: June 12, 2014Applicant: ABBVIE INC.Inventors: Andrew Burchat, Thomas D. Gordon, Kelly D. Mullen, David C. Ihle, Michael J. Morytko, Kevin P. Cusack, Gloria Y. Lo Schiavo, Lei Wang, Michael Friedman
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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: 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: 20140107073Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: ApplicationFiled: October 4, 2013Publication date: April 17, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
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Publication number: 20140107151Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.Type: ApplicationFiled: May 16, 2012Publication date: April 17, 2014Applicant: Principia Biophama Inc.Inventors: David Michael Goldstein, Kenneth Albert Brameld
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Patent number: 8685959Abstract: 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: GrantFiled: November 30, 2012Date of Patent: April 1, 2014Assignee: ChemoCentryx, Inc.Inventors: Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jay Powers, Ju Yang
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Publication number: 20140088094Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.Type: ApplicationFiled: November 8, 2011Publication date: March 27, 2014Applicants: Merck Sharp & Dohme Corp., Lycera CorporationInventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
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Publication number: 20140057920Abstract: This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 20, 2013Publication date: February 27, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thorsten OOST, Dennis FIEGEN, Christian GNAMM, Sandra HANDSCHUH, Stefan PETERS, Gerald Juergen ROTH
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Publication number: 20140057891Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl 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.Type: ApplicationFiled: November 4, 2013Publication date: February 27, 2014Applicant: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Patent number: 8658801Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: February 14, 2007Date of Patent: February 25, 2014Assignees: Syngenta Crop Protection, LLC, Syngenta LimitedInventors: Olivier Loiseleur, Patricia Durieux, Stephan Trah, Andrew Edmunds, André Jeanguenat, André Stoller, David John Hughes
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Publication number: 20140051660Abstract: 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, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui, Christopher Flores
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Publication number: 20140051688Abstract: 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, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui
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Publication number: 20140045815Abstract: Indazole-3-carboxamide compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole-3-carboxamide compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: ApplicationFiled: September 5, 2013Publication date: February 13, 2014Applicant: Samumed, LLCInventors: John Hood, Sunil Kumar KC
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Publication number: 20140045859Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 2, 2013Publication date: February 13, 2014Applicant: Takeda California, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
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Publication number: 20140038942Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.Type: ApplicationFiled: February 10, 2012Publication date: February 6, 2014Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
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Patent number: 8637513Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.Type: GrantFiled: October 23, 2008Date of Patent: January 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
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Publication number: 20140005227Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula (I) in which R1, R2, R3, R4, X, m and n have the meanings mentioned in the claims and the description, the tautomers thereof, the hydrates thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: December 8, 2011Publication date: January 2, 2014Applicant: ABBVIE Deutschland GmbH & Co. KGInventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Moller, Wilfried Hornberger, Yanbin Lao, Gisela Backfisch, Marjoleen Nijsen
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Patent number: 8580785Abstract: Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 14, 2006Date of Patent: November 12, 2013Assignee: Syngenta Crop Protection LLCInventors: André Jeanguenat, Roger Graham Hall, Olivier Loiseleur, Stephan Trah, Patricia Durieux, Andrew Edmunds, André Stoller
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Publication number: 20130296281Abstract: The invention relates to aryl and heteroaryl substituted compounds of Formula (I), and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein G, R1, and Z1-Z5 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: June 16, 2011Publication date: November 7, 2013Applicant: Purdue Pharma L.P.Inventors: Donald J. Kyle, Chiyou Ni, Laykea Tafesse, Jiangchao Yao
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Publication number: 20130289076Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.Type: ApplicationFiled: October 7, 2011Publication date: October 31, 2013Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal