The Additional Hetero Ring Is Five-membered Patents (Class 546/280.4)
-
Patent number: 8614234Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: GrantFiled: September 3, 2010Date of Patent: December 24, 2013Assignee: Allergan, Inc.Inventors: Xialing Guo, Zhen Zhu
-
Publication number: 20130331387Abstract: Disclosed is a compound of formula (I), wherein Z, m and R1-R6 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: ApplicationFiled: February 22, 2012Publication date: December 12, 2013Applicant: Lupin LimitedInventors: Neelima Sinha, Gourhari Jana, Sachchidanand Sachchidanand, Sanjay Pralhad Kurhade, Navnath Popat Karche, Anil Kashiram Hajare, Ajay Ramchandra Tilekar, Venkata P. Palle, Rajender Kumar Kamboj
-
Publication number: 20130331328Abstract: Small molecule inhibitors of AGBL2 are provided, as well as methods of using the inhibitors to treat or prevent cancer and neurologic disorders.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: GEORGETOWN UNIVERSITYInventors: Stephen W. Byers, Sivanesan Dakshanamurthy, Ziad Sahab
-
Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
-
Publication number: 20130324501Abstract: Derivatives of 1-phenyl-2-pyridinyl alkyl alcohols according to formula (I) are useful as inhibitors of the phosphodiesterase 4 (PDE4) enzyme.Type: ApplicationFiled: June 4, 2013Publication date: December 5, 2013Inventors: Elisabetta ARMANI, Carmelida Capaldi, Laura Carzaniga, Oriana Esposito
-
Publication number: 20130324550Abstract: The invention relates to compounds of formula I: where X, HAr, a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: August 9, 2013Publication date: December 5, 2013Applicant: THERAVANCE, INC.Inventors: Eric L. Stangeland, Lori Jean Patterson, Sheila Zipfel
-
Publication number: 20130310378Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).Type: ApplicationFiled: April 23, 2013Publication date: November 21, 2013Applicants: AbbVie Inc., AbbVie Deutschland GmbH & Co KGInventors: AbbVie Deutschland GmbH & Co KG, AbbVie Inc.
-
Publication number: 20130273569Abstract: The present invention provides dye compounds optimally excited at about 400 nm and have a Stokes shift of at least about 80 nm. These dyes find use in detection of analyte in a sample and the preparation of dye-conjugates.Type: ApplicationFiled: February 26, 2013Publication date: October 17, 2013Inventor: LIFE TECHNOLOGIES CORPORATION
-
Publication number: 20130267700Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, 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 cardiovascular disorders.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
-
Patent number: 8552033Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.Type: GrantFiled: December 17, 2008Date of Patent: October 8, 2013Assignee: SANOFIInventors: Stephanie Hachtel, Juergen Dedio, Stephen Shimshock, Carolina Lanter
-
Publication number: 20130245255Abstract: An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells useful for improvement in the efficiency of gene transfer into hematopoietic stem cells for gene therapy useful for treatment of various disorders is provided. An expansion agent for hematopoietic stem cells and/or hematopoietic progenitor cells containing a compound represented by the formula (I) (wherein X, Y, Z, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof, which can expand hematopoietic stem cells and/or hematopoietic progenitor cells.Type: ApplicationFiled: May 2, 2013Publication date: September 19, 2013Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Taito NISHINO, Shunsuke IWAMOTO, Katsuaki MIYAJI
-
Publication number: 20130231344Abstract: 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: ApplicationFiled: January 4, 2013Publication date: September 5, 2013Applicant: CalciMedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Patent number: 8518973Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: GrantFiled: April 18, 2012Date of Patent: August 27, 2013Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
-
Publication number: 20130210836Abstract: The present invention relates to a compound of formula (I): wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.Type: ApplicationFiled: July 19, 2011Publication date: August 15, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wenderborn
-
Publication number: 20130197013Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.Type: ApplicationFiled: July 27, 2011Publication date: August 1, 2013Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
-
Publication number: 20130190356Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genetech, Inc.
-
Patent number: 8492410Abstract: The present invention relates to novel pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: February 6, 2013Date of Patent: July 23, 2013Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha-Bin Im
-
Publication number: 20130178632Abstract: One aspect of the present invention relates to ligands for transition metals. A second aspect of the present invention relates to the use of catalysts comprising these ligands in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The subject methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition metal-catalyzed: aryl amination reactions; aryl amidation reactions; Suzuki couplings; and Sonogashira couplings. In certain embodiments, the invention relates to catalysts and methods of using them that operate in aqueous solvent systems.Type: ApplicationFiled: February 15, 2013Publication date: July 11, 2013Applicant: Massachusetts Institute of TechnologyInventor: Massachusetts Institute of Technology
-
Patent number: 8481549Abstract: 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: GrantFiled: January 18, 2011Date of Patent: July 9, 2013Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Robert Murray McKinnell
-
Publication number: 20130172339Abstract: A compound of formula (I), wherein A is S, O or a double bond, and L is a substituted thiazolyl, phenyl or pyridyl. The compound is useful for the treatment of inflammation and cancer.Type: ApplicationFiled: September 19, 2011Publication date: July 4, 2013Applicant: KANCERA ABInventors: Styrbjorn Bystrom, Charles Hedgecock, Evert Homan, Thomas Lundback, Jessica Martinsson, Meral Sari, Katarina Farnegardh, Mattias Jonsson
-
Publication number: 20130165451Abstract: 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: July 19, 2012Publication date: June 27, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Gary Bohnert, Nha Vo, Qinglin Che, Zhiqiang Xia, Lijun Sun
-
Publication number: 20130158034Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: Amgen Inc.Inventors: James BROWN, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. Horne, Matthew R. KALLER, Qingyian LIU, Holger MONENSCHEIN, Thomas T. NGUYEN, Nobuko NISHIMURA, Wenge ZHONG
-
Publication number: 20130137684Abstract: The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.Type: ApplicationFiled: June 1, 2011Publication date: May 30, 2013Applicant: THE UNIVERSITY OF QUEENSLANDInventors: Mark Leslie Smythe, Jack Urquhart Flanagan
-
Publication number: 20130131321Abstract: The present invention relates to the use for affinity purification of an antibody or an fragment of an antibody, of a ligand-substituted matrix comprising a support material and at least one ligand covalently bonded to the support material, the ligand being represented by formula (I) wherein Sp is a spacer group; v is 0 or 1; Am is an amide group —NR1—C(O)—, and wherein either NR1 is attached to Ar1 and —C(O)— is attached to Ar2, or —C(O)— is attached to Ar1 and NR1 is attached to Ar2; and R1 is hydrogen or C1 to C4 alkyl, preferably hydrogen or methyl; and more preferably hydrogen; Ar1 is a divalent 5- or 6-membered substituted or unsubstituted aromatic ring; Ar2 is 5- or 6-membered heterocyclic aromatic ring which is (a) attached to a further 5- or 6-membered aromatic ring via a single bond; or (b) fused to a further 5- or 6-membered aromatic ring as part of a multicyclic ring system; or (c) attached to at least one substituent selected from C1 to C4 alkyl; C2 to C4 alkenyl; C2 to C4 alkynyl; aType: ApplicationFiled: August 3, 2011Publication date: May 23, 2013Applicant: GRAFFINITY PHARMACEUTICALS GMBHInventors: Holger Bittermann, Klaus Burkert, Marc Arnold, Oliver Keil, Thomas Neumann, Inge Ott, Kristina Schmidt, Daniel Schwizer, Renate Sekul
-
Publication number: 20130096161Abstract: The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: July 8, 2011Publication date: April 18, 2013Applicant: N30 PHARMACEUTICALS, INC.Inventors: Xicheng Sun, Jian Qiu
-
Publication number: 20130079313Abstract: The invention relates to inhibitors of the phosphodiesterase 4 (PDE4) enzyme. More particularly, the invention relates to compounds that are derivatives of 1-phenyl-2-pyridinyl alkyl alcohols, methods of preparing such compounds, compositions containing them and therapeutic use thereof.Type: ApplicationFiled: September 26, 2012Publication date: March 28, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
-
Publication number: 20130065880Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: ApplicationFiled: November 9, 2012Publication date: March 14, 2013Applicant: Allergan, Inc.Inventor: Allergan, Inc.
-
Publication number: 20130042918Abstract: Compounds of Formula (I): Wherein: R1 and R2 are independently selected from the group consisting of optionally substituted C1-C20 alkyl, optionally substituted C3-C8 cycloalkyl, optionally substituted aromatic, and optionally substituted heteroaromatic groups or R1 and R2 together with the nitrogen atom to which they are attached comprise an optionally substituted saturated or unsaturated ring which may optionally contain further heteroatoms selected from the group consisting of O, N and S, and may optionally be further fused to one or more other rings; Ar is selected from the group consisting of optionally substituted aromatic and optionally substituted heteroaromatic groups; L is a linker which is a direct bond or is selected from the group consisting of optionally substituted C2 alkenylene and optionally substituted C2 alkynylene; T is independently selected from the group consisting of: R3, R4 and R9 are independently selected from the group consisting of hydrogen, optionally substitutedType: ApplicationFiled: May 5, 2011Publication date: February 21, 2013Inventors: Richard Evans, Akhil Gupta, Abdelselam Saeed Ali
-
Publication number: 20130040992Abstract: The present invention relates to substituted 2,6-diamino-3,5-dicyano-4-arylpyridines of the formula (I) wherein the definitions of substituent groups R1-R7 are as provided in the specification and claims, to a pharmaceutical composition containing such a compound, to a process for preparation of such materials, and to their use as medicaments for the treatment of cardiovascular disorders and diabetes.Type: ApplicationFiled: August 13, 2012Publication date: February 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Rosentreter, Thomas Krämer, Andrea Vaupel, Walter Hübsch, Nicole Diedrichs, Thomas Krahn, Klaus Dembowsky, Johannes-Peter Stasch
-
Patent number: 8372649Abstract: The present invention describes the development of a end-capped bipyridine compound having formula A and the zinc complex having formula B. The assay having formula 1 can be used to estimate and quantify the amount of zinc ions by monitoring the fluorescence changes. The assay with formula 1 can be use to image and detect Zn2+ ions in MCF7 cell lines. The zinc complex of formula 2 and 4 can be used as a fluorescent sensor for cyanide anions using analyte replacement protocol. The assay with formula 2 is selective only to cyanide anions even in the presence of other competing anions. The assay with formula 3 having bright green solid state emission is used for the preparation of formula 4. The orange fluorescent powder of assay with formula 4 is used for the selective detection of CN? ions in aqueous solution.Type: GrantFiled: March 15, 2012Date of Patent: February 12, 2013Assignee: Council of Scientific & Industrial ResearchInventors: Ajayaghosh Ayyapanpillai, Sreejith Sivaramapanicker, Divya P Kizhumuri, Jayamurthy Purushothaman
-
Patent number: 8372991Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1 and R4 are defined herein, 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: GrantFiled: March 17, 2011Date of Patent: February 12, 2013Assignee: Calcimedica, Inc.Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Publication number: 20130012708Abstract: A compound represented by the formula (1): wherein A is a nitrogen atom or CR4, B is an oxygen atom, a sulfur atom or NR9 (provided that when A is a nitrogen atom, B is not NH), R1 is a C2-14 aryl group, L1 is a bond, CR10R11, an oxygen atom, a sulfur atom or NR12, X is OR13, SR13 or NR14NR15, R2 is a hydrogen atom, a formyl group, a C1-10 alkyl group or the like, L2 is a bond or the like, L3 is a bond, CR17R18, an oxygen atom, a sulfur atom or NR19, L4 is a bond, CR20R21, an oxygen atom, a sulfur atom or NR22, Y is an oxygen atom, a sulfur atom or NR23, and R3 is a C2-14 aryl group, a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: September 13, 2012Publication date: January 10, 2013Applicant: Nissan Chemical Industries LimitedInventors: Shingo Owada, Shunsuke Iwamoto, Kazufumi Yanagihara, Katsuaki Miyaji, Takanori Nakamura, Norihisa Ishiwata, Yutaka Hirokawa
-
Publication number: 20120316195Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 16, 2010Publication date: December 13, 2012Applicant: NOVARTIS AGInventors: Martin Allan, Sylvie Chamoin, Qi-Ying Hu, Hidetomo Imase, Julien Papillon
-
Patent number: 8324133Abstract: The present invention relates to 2-pyridyl-methylene-carboxamide derivatives of formula (I) in which the substituents are as in the description, their process of preparation, 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: GrantFiled: May 11, 2006Date of Patent: December 4, 2012Assignee: Bayer Cropscience AGInventors: Stéphanie Gary, Brian Hill, Joseph Perez, Rachel Rama, Gilbert Spica, Jean-Pierre Vors
-
Publication number: 20120295930Abstract: The present invention relates to an improved process for the preparation of cis-nucleoside derivative of formula-1 involving chlorination of the compound of formula-2 followed by reaction with compound of formula-3 in presence of a base to get compound of formula-4, reacting the compound of formula-4 with an alkyl halide (RiX) to get a quaternary ammonium salt then with cytosine derivative of formula-5 to provide the compound of formula-6, optionally de-protecting the compound of formula-6 to the compound of formula-7, reducing compound of formula-7 with metal catalyst in presence of a buffer solution, then adding an organic acid to get the compound of formula-8, and converting the compound of formula-8 to cis-nucleoside derivative of formula-1. The present invention further relates to novel cis-nucleoside derivative of formula-8. The present invention also relates to a pharmaceutical composition comprising cis-nucleoside derivative of formula-1 with excipients.Type: ApplicationFiled: February 1, 2011Publication date: November 22, 2012Inventors: Shankar Rama, Sarat Chandra Srikanth Gorantla, Lakshmana Rao Vadali, Venkata Bala Kishore Sarma Inupakutika, Srinivas Rao Dasari, Nagaraju Mittapelly, Santosh Kumar Singh, Debashish Datta
-
Patent number: 8309554Abstract: Hypoxia activated drug compounds having a structure of formula (I) are useful in the treatment of cancer and other hyperproliferative diseases.Type: GrantFiled: May 14, 2009Date of Patent: November 13, 2012Assignee: Threshold PharmaceuticalsInventors: Jason Lewis, Mark Matteucci, Tao Chen, Hailong Jiao
-
Publication number: 20120283272Abstract: 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: July 19, 2012Publication date: November 8, 2012Applicant: Synta Pharmaceuticals Corp.Inventors: Shoujun Chen, Junyi Zhang, Jun Jiang, Gary Bohnert, Nha Vo, Qinglin Che, Zhiqiang Xia, Lijun Sun
-
Patent number: 8247437Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: GrantFiled: June 8, 2011Date of Patent: August 21, 2012Assignee: Merck Serono SAInventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
-
Publication number: 20120209005Abstract: Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1 is an aryl group fused to a saturated ring or the like, A, B, L1, R2, L2, L3, Y, L4, R3 and X are defined in the description), a tautomer, prodrug or a pharmaceutically acceptable salt of the compound or a solvate thereof.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Applicant: Nissan Chemical Industries, Ltd.Inventors: Yukihiro Shigeta, Shingo Umezawa, Shunsuke Iwamoto, Takanori Nakamura
-
Publication number: 20120202817Abstract: A compound having the following formula [I] or a pharmaceutically acceptable salt thereof: wherein A is an aromatic five-membered heterocycle which optionally is fused with a cycloalkane ring; B is an alkylene; R1 and R2 are hydrogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, heterocycle, amino, alkylamino, arylamino or acyl, or R1 and R2 join together to form a heterocycle; X and Y are hydrogen, halogen, hydroxyl, alkoxy, aryloxy, alkyl, cycloalkyl, aryl, mercapto, alkylthio, arylthio, carboxyl, an ester of carboxyl, an amide of carboxyl, cyano or nitro; p is 0, 1 or 2; and q is 0 or 1. The compound is useful for treating diseases in which angiogenesis or augmentation of vascular permeability is involved.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takahiro Honda, Hisashi Tajima, Yoshimasa Sasabuchi, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto, Masakazu Ban
-
Publication number: 20120202795Abstract: The present invention relates to a series of 2,3,5-substituted pyridone derivatives of formula I: wherein R, R1, R2, R3 and R4 are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5?-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.Type: ApplicationFiled: April 18, 2012Publication date: August 9, 2012Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Philip M. WEINTRAUB, Paul R. EASTWOOD, Shujaath MEHDI, David W. STEFANY, Kwon Yon MUSICK, Neil MOORCROFT, Sungtaek LIM, John Z. JIANG, Hartmut RUTTEN, Stefan PEUKERT, Uwe SCHWAHN
-
Publication number: 20120196900Abstract: Disclosed are compounds of the formula I: wherein R1, R2, V, W, X, Y and Z can be as defined herein. The compounds can be used in the treatment of disorders mediated by the cannabinoid receptors.Type: ApplicationFiled: April 16, 2012Publication date: August 2, 2012Inventors: Bob M. Moore, II, Steven Gurley, Suni Mustafa
-
Publication number: 20120196884Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).Type: ApplicationFiled: June 14, 2010Publication date: August 2, 2012Applicant: BIOTIE THERAPIES CORPORATIONInventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
-
Publication number: 20120196905Abstract: Methods and small molecule compounds for smoking and CNS disease harm reduction are provided.Type: ApplicationFiled: August 5, 2011Publication date: August 2, 2012Applicant: HUMAN BIOMOLECULAR RESEARCH INSTITUTEInventor: John R. CASHMAN
-
Patent number: 8232297Abstract: Compounds of a certain formula I, in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, as well as salts thereof are novel effective HDAC inhibitors.Type: GrantFiled: September 8, 2006Date of Patent: July 31, 2012Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Rolf-Peter Hummel, Martin Feth, Matthias Müller, Thomas Bär, Jürgen Volz
-
Patent number: 8227495Abstract: The present disclosure provides 2,4-disubstituted thiazoles of the general structure shown below that are agonists of G-protein coupled receptor (IC-GPCR2). Also, provided are compositions comprising these compounds as well as methods for using these compounds in a variety of applications including diabetes and metabolic disorders.Type: GrantFiled: August 14, 2009Date of Patent: July 24, 2012Assignee: Metabolex Inc.Inventors: Xin Chen, Peng Cheng, L. Edward Clemens, Jeffrey D. Johnson, Jingyuan Ma, Alison Murphy, Imad Nashashibi, Christopher J. Rabbat, Jiangao Song, Maria E. Wilson, Yan Zhu, Zuchun Zhao
-
Publication number: 20120183496Abstract: 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: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
-
Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
-
Patent number: 8207196Abstract: The present invention relates to treatment and/or prevention of one or more metabolic disorders utilizing fatostatin A and/or a derivative and/or analog thereof. In other aspects, the compound for treatment and/or prevention of one or more metabolic disorders utilizes an A-B-C tripartite structure, wherein A, B, and C are identical or non-identical structures and are described in detail herein. In specific aspects, the metabolic disorder includes obesity or diabetes, for example.Type: GrantFiled: February 1, 2008Date of Patent: June 26, 2012Assignee: Baylor College of MedicineInventors: Motonari Uesugi, Salih J. Wakil, Lutfi Abu-Elheiga, Qian Mao, Shinji Kamisuki, Akira Kugimiya
-
NOVEL SUBSTITUTED PICOLINIC ACIDS, SALTS AND ACID DERIVATIVES THEREOF, AND USE THEREOF AS HERBICIDES
Publication number: 20120157314Abstract: The present invention relates to novel, herbicidally active picolinic acid derivatives of the formula (I) and to processes for preparation thereof. The present invention further provides for the use thereof as a herbicide, especially as a herbicide for selective control of weed plants in useful plant crops, and as a plant growth regulator alone or in combination with safeners and/or in a mixture with other herbicides.Type: ApplicationFiled: October 21, 2011Publication date: June 21, 2012Applicant: BAYER CROPSCIENCE AGInventors: Hartmut AHRENS, Marco BRÜNJES, Hansjörg DIETRICH, Elmar GATZWEILER, Isolde HÄUSER-HAHN, Stefan LEHR, Dirk SCHMUTZLER