Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazole Ring Patents (Class 548/200)
  • Patent number: 9580732
    Abstract: A method including the steps a) providing a primary alcohol of the formula HO—(CH2)x—R1, where R1 is —OH, —SH, —NH2 or —COOR2; x is at least 3; and R2 is H, alkyl or aryl, b) oxidizing the primary alcohol by contacting it with an NAD(P)+-dependent alcohol dehydrogenase, and c) contacting the oxidation product of step a) with a transaminase, where the NAD(P)+-alcohol dehydrogenase and/or the transaminase is a recombinant or isolated enzyme. A whole cell catalyst for carrying out the method. The use of such a whole cell catalyst for oxidizing a primary alcohol.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: February 28, 2017
    Assignee: Evonik Degussa GmbH
    Inventors: Markus Pötter, Thomas Haas, Jan Christoph Pfeffer, Arne Skerra, Wolfgang Kroutil, Alexandra Lerchner, Johann H. Sattler, Steffen Schaffer, Katharina Christin Tauber
  • Patent number: 9255072
    Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: February 9, 2016
    Assignee: National Health Rsearch Institutes
    Inventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
  • Patent number: 9168249
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: February 4, 2015
    Date of Patent: October 27, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
  • Patent number: 9085585
    Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: July 21, 2015
    Assignee: Cerenis Therapeutics Holding SA
    Inventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Otto Geoffroy, Ronald Barbaras
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Publication number: 20150141646
    Abstract: In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Applicant: Concortis Biosystems, Corp., a wholly owned subsidary of Sorrento Therapeutics, Inc,
    Inventors: Zhenwei Miao, Yufeng Hong, Tong Zhu
  • Publication number: 20150105392
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Publication number: 20150099766
    Abstract: The invention relates to compounds of the general formula (I), in which the radicals A1, A2, A3, A4, Lm, Q, R1, T and U have the meaning given in the description and to the use of the compounds for controlling animal pests. In addition, the invention relates to processes and intermediates for the preparation of the compounds according to formula (I).
    Type: Application
    Filed: December 15, 2014
    Publication date: April 9, 2015
    Inventors: Michael MAUE, Isabelle ADELT, Wolfgang GIENCKE, Markus HEIL, Peter JESCHKE, Bernd-Wieland KRÜGER, Friedrich August MÜHLTHAU, Alexander SUDAU, Klaus RAMING, Ulrich EBBINGHAUS-KINTSCHER, Martin ADAMCZEWSKI, Arnd VOERSTE, Ulrich GÖRGENS, Tobias KAPFERER, Mark Wilhelm DREWES, Angela BECKER, Eva-Maria FRANKEN
  • Patent number: 8993567
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: March 31, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
  • Publication number: 20150087823
    Abstract: The present invention relates to a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical agent containing the compound as an active ingredient. The trans-2-decenoic acid derivative or a pharmaceutically acceptable salt, which is the compound of the present invention, is specifically represented by the general formula (I): wherein X is a substituent such as a 1-pyrrolidyl, a 3-thiazolizyl, or a piperidino, and the compound is highly useful as a pharmaceutical agent, such as a prophylactic or therapeutic agent for a peripheral nerve disorder induced by administration of an anticancer agent, a prophylactic or therapeutic agent for neurodegenerative diseases or mental diseases such as dementia, Alzheimer's disease, Parkinson's disease, diabetic neuropathy, depression, glaucoma, or autistic disorder spectrum, a therapeutic or repairing agent for spinal cord injury, analgesics against various pain diseases, or the like.
    Type: Application
    Filed: April 26, 2013
    Publication date: March 26, 2015
    Inventors: Munekazu Iinuma, Shoei Furukawa, Mitsuru Naiki, Tomonori Matsumoto, Kunihiko Higashiura
  • Patent number: 8987258
    Abstract: The present invention relates to novel chromenone analog sirtuin modulator compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions and treatment methods and combination therapies thereof for use in increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity.
    Type: Grant
    Filed: September 29, 2009
    Date of Patent: March 24, 2015
    Inventors: Christopher Oalmann, Robert B. Perni, Chi B. Vu
  • Patent number: 8987312
    Abstract: The invention provides a series of -?ketoheterocyclic compounds, for example, compounds of formula (I). The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula (I), useful intermediates for the preparation of compounds of formula (I), and methods of using compounds of formula (I) and compositions thereof.
    Type: Grant
    Filed: July 8, 2009
    Date of Patent: March 24, 2015
    Assignee: The Scripps Research Institute
    Inventor: Dale L. Boger
  • Publication number: 20150079028
    Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
    Type: Application
    Filed: August 5, 2013
    Publication date: March 19, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD
    Inventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo
  • Patent number: 8975254
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 10, 2015
    Assignee: Orion Corporation
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Patent number: 8946233
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: January 16, 2014
    Date of Patent: February 3, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8946432
    Abstract: Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: February 3, 2015
    Assignee: Lupin Limited
    Inventors: Neelima Sinha, Navnath Popat Karche, Girish Dhanraj Hatnapure, Anil Kashiram Hajare, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150005320
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 1, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Patent number: 8921364
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: December 30, 2014
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
  • Patent number: 8921370
    Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
    Type: Grant
    Filed: December 22, 2011
    Date of Patent: December 30, 2014
    Assignee: H. Lundbeck A/S
    Inventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
  • Patent number: 8921571
    Abstract: Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: December 30, 2014
    Assignee: The Ohio State University
    Inventors: Michael K. Chan, Tomasz Fekner, Xin Li, Marianne Lee, Manoj Nair, Jennifer Jo Ottensen
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140348850
    Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.
    Type: Application
    Filed: August 15, 2014
    Publication date: November 27, 2014
    Inventors: Edward P. Feener, Allen Clermont
  • Patent number: 8895552
    Abstract: Provided is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. (In the formula, A is C6-10 arylene, etc.; R1a, R1b and R1c each independently is a hydrogen atom, a halogen atom, a C1-4 alkyl group, a C1-4 alkoxy group, etc.; R2 is an optionally substituted C6-10 aryl group, an optionally substituted 5- to 12-membered monocyclic or polycyclic heteroaryl group, an optionally substituted C7-16 aralkyl group, etc.; m is 0, etc.; n is an integer of 0 to 2.
    Type: Grant
    Filed: September 2, 2011
    Date of Patent: November 25, 2014
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Yoshihiro Horiuchi, Hiroaki Fujiwara, Hitoshi Suda, Izumi Sasaki, Mitsutaka Iwata, Kiyoto Sawamura
  • Patent number: 8877741
    Abstract: 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: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8865751
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: October 21, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Philip Collier
  • Publication number: 20140302069
    Abstract: Heterocyclic compounds that modulate C3a receptors and their use in the treatment or prevention of inflammatory diseases, infectious diseases, cancers, metabolic disorders, obesity, type 2 diabetes, metabolic syndrome and associated cardiovascular diseases are described. The use of the compounds in stimulating or suppressing an immune response is also described together with pharmaceutical compositions comprising the compounds or their pharmaceutically acceptable salts.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 9, 2014
    Inventors: David Fairlie, Robert C. Reid
  • Publication number: 20140303157
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: August 27, 2012
    Publication date: October 9, 2014
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Publication number: 20140275178
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of degenerative diseases and disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: September 18, 2014
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Craig C. BEESON, Christopher C. LINDSEY, Yuri K. PETERSON, Baerbel ROHRER
  • Publication number: 20140275543
    Abstract: A method for stabilization of potent alkanone-heterocyclic flavorants in dry powder form is provided. Coordination of alkanone-heterocyclic flavorants to transition metal salts results in the formation of stable crystalline complexes, which upon hydration release the free flavorant. Food and topping products containing the stabilized alkanone-heterocyclic flavorant are provided as are methods for stabilizing the alkanone-heterocyclic flavorant.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Keith R. Cadwallader, Ming-Chih Fang
  • Patent number: 8835472
    Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: August 17, 2011
    Date of Patent: September 16, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Gerald Juergen Roth, Martin Fleck, Niklas Heine, Joerg Kley, Thorsten Lehmann-Lintz, Heike Neubauer, Bernd Nosse
  • Publication number: 20140256771
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Publication number: 20140248299
    Abstract: 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: Application
    Filed: May 9, 2014
    Publication date: September 4, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Gary Bohnert, Shoujun Chen, Yu Xie
  • Patent number: 8822512
    Abstract: The disclosure features crystalline tripeptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 2, 2014
    Assignee: Onyx Therapeutics, Inc.
    Inventors: Pasit Phiasivongsa, Louis C. Sehl
  • Patent number: 8822466
    Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Noëlle Gauvry, Steve Nanchen
  • Patent number: 8815920
    Abstract: A substituted amide compound is useful as an active ingredient of a pharmaceutical composition, in particular a pharmaceutical composition for treating diseases caused by lysophosphatidic acid (LPA). The compound is of a formula: In this formula, A is an optionally substituted aryl, etc.; B is an optionally substituted 5-membered aromatic hetero ring group; X is a single bond or —(CRX1RX2)n—; n is 1, 2, 3, or 4; RX1 and RX2 are hydrogen, etc.; Y1 to Y5 are each CRY or N; each RY is hydrogen, etc.; R1 and R2 are hydrogen, etc.; m is 1, 2, or 3; R3 is hydrogen, etc.; and R4 is an optically substituted lower alkyl, etc.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: August 26, 2014
    Assignee: Astellas Pharma Inc.
    Inventors: Eiji Kawaminami, Tatsuhisa Takahashi, Takatoshi Kanayama, Yuta Fukuda, Hiroyuki Kaizawa, Yutaka Kondoh, Ryushi Seo, Kazuyuki Kuramoto, Kazuhiko Take, Kazuyuki Sakamoto
  • Patent number: 8815903
    Abstract: 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 benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 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], or 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: Grant
    Filed: January 24, 2012
    Date of Patent: August 26, 2014
    Assignees: Kissei Pharmaceutical Co., Ltd., Kyorin Pharmaceutical Co., Ltd.
    Inventors: Kazuya Tatani, Atsushi Kondo, Tatsuhiro Kondo, Naohiro Kawamura, Shigeki Seto, Yasushi Kohno
  • Publication number: 20140228416
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: September 12, 2013
    Publication date: August 14, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Publication number: 20140221383
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 7, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Publication number: 20140206691
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 27, 2014
    Publication date: July 24, 2014
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 8785442
    Abstract: The present invention relates to a compound as antagonist of LPA receptor, and a pharmaceutical composition comprising the same. The present invention also relates to the use of the compound and the composition, and a method of using the compound to treat, prevent or diagnose diseases, disorders or conditions associated with one or more of the LPA receptors.
    Type: Grant
    Filed: January 30, 2011
    Date of Patent: July 22, 2014
    Assignee: Curegenix, Inc.
    Inventors: Songzhu An, Chufang Li, Guisheng Zhou, Chen Huang
  • Patent number: 8759333
    Abstract: 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 Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Patent number: 8759533
    Abstract: 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 Q and Z are defined herein.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: June 24, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Peter J. Connolly, Mark J. Macielag, Bin Zhu
  • Publication number: 20140171474
    Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions
    Type: Application
    Filed: February 19, 2014
    Publication date: June 19, 2014
    Inventors: Philippe DESBORDES, Ralf DUNKEL, Stephanie GARY, Marie-Claire GROSJEAN-COURNOYER, Benoit HARTMANN, Philippe RINOLFI, Jean-Pierre VORS, Rachel RAMA
  • Patent number: 8754209
    Abstract: Disclosed are novel indazole derivatives represented by the following Chemical Formula 1 or pharmaceutically acceptable salts, hydrates or solvates thereof, and pharmaceutical compositions for the prevention or treatment of proliferative diseases, containing the same as an active ingredient. Having potent inhibitory effect against protein kinase, such as b-raf, KDR, Fms, Tie2, SAPK2a and Ret, inducing diseases caused by abnormal cell proliferation, the novel indazole derivatives can be used for the prevention or treatment of diseases caused by abnormal cell proliferation.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: June 17, 2014
    Assignees: Korea Institute of Science and Technology, Korea Research Institute of Chemical Technology, Korea Research Institute of Bioscience and Biotechnology
    Inventors: Tae Bo Sim, Jung Beom Son, Hwan Kim, Dong Sik Park, Hwan Geun Choi, Young Jin Ham, Jung Mi Hah, Kyung Ho Yoo, Chang Hyun Oh, So Ha Lee, Jae Du Ha, Sung Yun Cho, Byoung Mog Kwon, Dong Cho Han
  • Publication number: 20140162998
    Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 12, 2014
    Applicant: Jikai Biosciences, Inc.
    Inventor: Yu GE
  • Patent number: 8748471
    Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.
    Type: Grant
    Filed: November 27, 2012
    Date of Patent: June 10, 2014
    Assignee: Bayer CropScience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
  • Publication number: 20140155433
    Abstract: Disclosed is a compound of formula (I): wherein ‘D’, ‘E’, ‘m’, ‘n’ and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the ?7 subtype, in a subject in need thereof, as well as analogues, prodrugs, isotopically substituted analogs, metabolites, pharmaceutically acceptable salts, polymorphs, solvates, isomers, clathrates, and co-crystal thereof, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds and analogues. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
    Type: Application
    Filed: July 2, 2012
    Publication date: June 5, 2014
    Applicant: LUPIN LIMITED
    Inventors: Neelima Sinha, Navnath Popat Karche, Girish Dhanraj Hatnapure, Anil Kashiram Hajare, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20140148600
    Abstract: The present invention relates to thiazole compounds of formula I, the method for preparation and use thereof. More specifically, the present invention relates to novel derivatives of natural product largazole, the method for preparing them and their uses for treatments against tumor and multiple sclerosis as inhibitors of histone deacetylase.
    Type: Application
    Filed: May 7, 2012
    Publication date: May 29, 2014
    Inventors: Fajun Nan, Fei Chen, Yangming Zhang, Jia Li, Yubo Zhou, Mingbo Su, Jian DING, Linghua Meng, Xin Xie, Shixian Wang
  • Publication number: 20140135333
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 16, 2014
    Publication date: May 15, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • Patent number: 8722901
    Abstract: Heteroaryl compounds, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or disorders mediated by Diacylglycerol acyltransferase (DGAT) enzyme, particularly DGAT-1 is described.
    Type: Grant
    Filed: November 1, 2010
    Date of Patent: May 13, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma, Kishorkumar Shivajirao Kadam, Shivaji Sadashiv Kandre