Additional Hetero Ring Other Than The Six-membered Hetero Rings Patents (Class 514/333)
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Publication number: 20140228340Abstract: Compounds of the formula I, in which R1, R2, 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: August 13, 2012Publication date: August 14, 2014Applicant: MERCK PATENT GMBHInventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
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Publication number: 20140228394Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Novartis AGInventors: Mark Gary BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
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Publication number: 20140228386Abstract: The present invention provides compounds of Formula (I), or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: April 27, 2012Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: Mark Gary Bock, Christoph Gaul, Venkateshwar Rao Gummadi, Saumitra Sengupta
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Publication number: 20140228363Abstract: The present invention provides a compound of formula (I): as further described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: April 22, 2014Publication date: August 14, 2014Applicant: NOVARTIS AGInventors: Matthew Burger, Yu Ding, Wooseok Han, Gisele Nishiguchi, Alice Rico, Robert Lowell Simons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Publication number: 20140220154Abstract: What is described is a method of preventing or treating heterotopic ossification, vascular calcification, and pathologic mineralization, comprising administering an drug, wherein the drug is an antagonist of the Hedgehog (Hh) pathway. For example the antagonist consists of arsenic trioxide, sodium arsenite, phenylarsine, GANT-58, GANT-61, zerumbone vismodegib (GDC-0449, Genentech), bevacizumab, gemcitabine, nab-paclitaxel, FOLFIR, FOLFOX, RO4929097, cixutumumab, cisplatin, etoposide, LDAC, decitabine, daunorubicin, cytarabin, rosiglitazone, goserelin, leuprolide, capecitabine, fluorouracil, leucovorin, oxaliplatin, irinotecan, diclofenac, BMS-833923 (XL139), IPI-926—Infinity Pharmaceuticals, Inc., LDE225, LEQ506—Novartis Pharmaceuticals, TAK-441 Millennium Pharmaceuticals, Inc., and PF-04449913—Pfizer, alone or in combination therapy.Type: ApplicationFiled: June 28, 2012Publication date: August 7, 2014Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human ServiceInventors: Jean Regard, Yingzi Yang
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Publication number: 20140221332Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: August 7, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat
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Publication number: 20140221362Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Publication number: 20140221346Abstract: 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: January 9, 2014Publication date: August 7, 2014Applicant: Gilead Sciences, Inc.Inventors: Randall L. HALCOMB, Yunfeng Eric HU, Qi LIU, Jennifer R. ZHANG
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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: 8796247Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.Type: GrantFiled: January 24, 2012Date of Patent: August 5, 2014Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
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Patent number: 8796314Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: January 28, 2010Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
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Patent number: 8796001Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: August 5, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
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Patent number: 8796310Abstract: The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: GrantFiled: April 30, 2012Date of Patent: August 5, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Eric Thomas Romeo, Michelle R. Machacek, Benjamin Wesley Trotter, Thomas Allen Miller, Brian Michael Andresen, Neville John Anthony, Brandon M. Taoka, Yuan Liu
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Publication number: 20140213568Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: January 22, 2014Publication date: July 31, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Publication number: 20140213448Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: ApplicationFiled: March 28, 2014Publication date: July 31, 2014Applicant: DOW AGROSCIENCES LLCInventors: Ann M. Buysse, Noormohamed M. Niyaz, David A. Demeter, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, Akshay Patny, Negar Garizi, Paul R. LePlae, JR., Frank Wessels, Ronald Ross, JR., Carl DeAmicis, Peter Borromeo
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Patent number: 8791139Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and a plurality of processes for their preparation.Type: GrantFiled: June 14, 2011Date of Patent: July 29, 2014Assignee: Bayer Cropscience AGInventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Christian Funke, Eva-Maria Franken, Olga Malsam, Arnd Voerste, Ulrich Görgens, Tetsuya Murata
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Patent number: 8785489Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: GrantFiled: October 13, 2009Date of Patent: July 22, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Bennett Farmer, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Patent number: 8785468Abstract: Provided herein are compounds of formula I: wherein A, B, X, R1, R2 and subscript n are as defined in the following disclosure. Compositions comprising the compounds are also provided, as well as methods for their use, for example, in treatment of type 2 diabetes and type 2 diabetes-related conditions.Type: GrantFiled: February 12, 2010Date of Patent: July 22, 2014Assignee: Amgen Inc.Inventors: Xiaohui Du, Zice Fu, Jonathan B. Houze, XianYun Jiao, Yong-Jae Kim, Leping Li, Jinqian Liu, Mike Elias Lizarzaburu, Julio C. Medina, Wang Shen, Simon Turcotte, Ming Yu
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Patent number: 8779154Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 25, 2007Date of Patent: July 15, 2014Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
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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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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8778955Abstract: The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of I?B kinase comprising administering such compounds.Type: GrantFiled: June 6, 2007Date of Patent: July 15, 2014Assignee: Sanofi-Aventis Deutschland GmbHInventors: Olaf Ritzeler, Gerhard Jaehne
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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: 20140194443Abstract: The invention relates to pyrazolyl-based carboxamide compounds useful as ICRAC inhibitors, to pharmaceutical compositions containing these compounds and to these compounds for the use in the treatment and/or prophylaxis of diseases and/or disorders, in particular inflammatory diseases and/or inflammatory disorders.Type: ApplicationFiled: January 10, 2014Publication date: July 10, 2014Applicant: Grünenthal GmbHInventors: Sonja Nordhoff, Sebastian Wachten, Achim Kless, Felix Voss, Stefanie Ritter
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Publication number: 20140194407Abstract: The present invention relates to a novel antiplatelet agent and a novel compound which is an active ingredient for the agent. The present invention provides the antiplatelet agent comprising a compound represented by the formula I: wherein, X is N, or CR1d, Xb1-Xb5 are the same or different, and are nitrogen or carbon, R1a-R1d are the same or different, and are hydrogen, an optionally substituted alkyl, an optionally substituted alkoxy, an optionally substituted alkylthio, an alkenyl, a cycloalkyl, a halogen, cyano, or hydroxyl or optionally substituted by 1 or 2 alkylamino, R2 is an optionally substituted aryl or an optionally substituted heteroaryl, R3 is an optionally substituted aryl or an optionally substituted heteroaryl, or pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: February 25, 2014Publication date: July 10, 2014Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hiroshi SATO, Kazutoshi YOKOYAMA, Kazushi SATO
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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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3-(BENZOIMIDAZOL-2-YL)-INDAZOLE INHIBITORS OF THE WNT SIGNALING PATHWAY AND THERAPEUTIC USES THEREOF
Publication number: 20140194441Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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: January 8, 2014Publication date: July 10, 2014Applicant: Samumed, LLCInventors: Sunil Kumar KC, John Hood -
Patent number: 8772304Abstract: The present invention relates to compounds of formula (IA), (IB) and (IC): and pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: October 26, 2011Date of Patent: July 8, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Stephane De Lombaert, Weimin Liu, Ho Yin Lo, Peter Allen Nemoto
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Patent number: 8772320Abstract: An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. The present invention provides a nicotinamide derivative represented by the following formula (I) (wherein R1 represents a halogen atom; R2 represents a C1-12 alkyl group, a C2-12 alkenyl group, a C2-12 alkynyl group, a C3-8 cycloalkyl group, an aryl group, an ar-C1-6 alkyl group or a heterocyclic group, each optionally having at least one substituent; R3 represents an aryl group or a heterocyclic group each optionally having at least one substituent; and R4 and R5 each independently represent a hydrogen atom; and R2 and R4 may form a cyclic amino group optionally having at least one substituent together with the nitrogen atom to which they bind) or a salt thereof, and a pharmaceutical composition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.Type: GrantFiled: December 28, 2012Date of Patent: July 8, 2014Assignee: FUJIFILM CorporationInventors: Hideyasu Fujiwara, Kimihiko Sato, Shinsuke Mizumoto, Yuichiro Sato, Hideki Kurihara, Yohei Kubo, Hiyoku Nakata, Yasutaka Baba, Takashi Tamura, Hidenobu Kuniyoshi, Shinji Hagiwara, Mari Yamamoto
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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: 8772289Abstract: N-Thio-anthranilamid compounds of formula (I) wherein A is A1 wherein the variables and the indices are as defined per the description, processes for preparing the compounds I, pesticidal compositions comprising compounds I, use of compounds I for the control of insects, acarids or nematodes, and methods for treating, controlling, preventing or protecting animals against infestation or infection by parasites by use of compounds of formula I.Type: GrantFiled: November 20, 2012Date of Patent: July 8, 2014Assignee: BASF SEInventors: Thomas Schmidt, Michael Puhl, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Franz-Josef Braun, Toni Bucci, Henry Van Tuyl Cotter, David G. Kuhn, Hassan Oloumi-Sadeghi
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Patent number: 8765789Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 27, 2012Date of Patent: July 1, 2014Assignee: MSD K.K.Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
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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: 20140179742Abstract: Described herein are methods and compositions for killing or preventing the growth of microbes. It has been discovered that a class of porphyrins can kill or prevent the growth of microbes. The porphyrins can be used in a number of different applications where microbes grow.Type: ApplicationFiled: December 12, 2013Publication date: June 26, 2014Applicant: Frontier Scientific, Inc.Inventors: Glenn PRESTWICH, Jerry C. BOMMER, Charles TESTA
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Publication number: 20140179702Abstract: 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.Type: ApplicationFiled: October 15, 2013Publication date: June 26, 2014Inventors: Andreas Kling, Katja Jantos, Helmut Mack, Achim Möller, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen
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Patent number: 8759376Abstract: Compounds of Formula (I), pharmaceutical compositions comprising compounds of Formulae (I a) or (VII) and a method of treating a subject with an inflammatory cytokine-mediated disorder comprising administering to the subject a compound of Formulae (I a) or (VIIa). The variables of Formulae (I), (I a), (VII) and (VII a) are described herein.Type: GrantFiled: September 27, 2010Date of Patent: June 24, 2014Assignee: The Feinstein Institute for Medical ResearchInventors: Yousef Al-Abed, Kevin J. Tracey
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Patent number: 8759539Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: GrantFiled: November 11, 2009Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
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Publication number: 20140171437Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: December 6, 2013Publication date: June 19, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
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Publication number: 20140171446Abstract: The invention relates to certain compounds or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: May 3, 2012Publication date: June 19, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Gary Bohnert, Jun Jiang, Zhiqiang Xia
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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: 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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Patent number: 8748627Abstract: The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.Type: GrantFiled: February 15, 2007Date of Patent: June 10, 2014Assignee: AbbVie Inc.Inventors: Yu Gui Gu, Moshe Weitzberg, Xiangdong Xu, Richard F. Clark, Tianyuan Zhang, Qun Li, Todd M. Hansen, Hing Sham, Bruce A. Beutel, Heidi S. Camp, Xiaojun Wang
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Patent number: 8748433Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: GrantFiled: April 25, 2011Date of Patent: June 10, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Publication number: 20140155381Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.Type: ApplicationFiled: July 27, 2012Publication date: June 5, 2014Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
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Publication number: 20140155401Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine 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: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
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Publication number: 20140155370Abstract: The invention generally relates to the field of nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to new substituted-heterocyclic azole compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, pulmonary fibrosis, hepatic fibrosis, glomerulonephritis, and other renal disorders, and for the treatment of viral infections (both acute and chronic).Type: ApplicationFiled: June 28, 2013Publication date: June 5, 2014Inventors: Sharon Shacham, Michael Kauffman, Vincent P. Sandanayaka, Sharon Shechter
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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: 20140155379Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: ApplicationFiled: December 20, 2013Publication date: June 5, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Patent number: 8741932Abstract: The present invention relates to compounds of formula (I), wherein Ra, Rb, Rc, Rd, Re and Rf are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PI3K), mammalian target of rapamycin (mTOR), Signal transducer and activator of transcription 3 (STAT 3), tumor necrosis factor-? (TNF-?), interleukin-6 (IL-6) or a combination thereof particularly in the treatment of cancer and inflammation.Type: GrantFiled: November 4, 2010Date of Patent: June 3, 2014Assignee: Piramal Enterprises LimitedInventors: Sanjay Kumar, Sivaramakrishnan Hariharan, Mandar Bhonde, Nilesh Dagia, Rajiv Sharma, Pallavi Hanmantrao Mane, Pramod Bhaskar Kumar
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Publication number: 20140148461Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: November 22, 2013Publication date: May 29, 2014Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS