1,3,4-oxadiazoles (including Hydrogenated) Patents (Class 548/143)
  • Publication number: 20120196861
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Application
    Filed: January 27, 2012
    Publication date: August 2, 2012
    Applicant: 4SC Discovery GmbH
    Inventors: Johann LEBAN, Stefan TASLER, Roland BAUMGARTNER, Wael SAEB, Carine CHEVRIER
  • Publication number: 20120196862
    Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.
    Type: Application
    Filed: January 27, 2012
    Publication date: August 2, 2012
    Applicant: 4SC Discovery GmbH
    Inventors: Johann LEBAN, Stefan TASLER, Wael SAEB, Carine CHEVRIER
  • Publication number: 20120184544
    Abstract: The present invention relates to substituted benzamide derivatives of the general Formula I and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites, and polymorphs and can be useful for treating disease states mediated by glucokinase. Compounds disclosed herein can be used for reducing blood glucose levels and for increasing insulin secretion for treating type II diabetes. The invention also relates to processes for the preparation of the compounds of invention, pharmaceutical compositions containing the compounds, and their use.
    Type: Application
    Filed: July 22, 2010
    Publication date: July 19, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Rajendra Kharul, Makul R. Jain, Pankaj R. Patel
  • Patent number: 8217065
    Abstract: The present invention provides compounds of the following structure; A-Q-B—C-D that are useful for treating conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Grant
    Filed: December 9, 2010
    Date of Patent: July 10, 2012
    Assignee: Novartis AG
    Inventors: Young-Shin Kwak, Gary Mark Coppola
  • Publication number: 20120165540
    Abstract: A process is described for the preparation of 3-alkylsulfinylbenzoyl derivatives of the formula (IIIa) by reaction of 3-alkylsulfinylbenzoic acids of the formula (Ib) with compounds of the formula (II) in the presence of a chlorinating agent and a base. In the formulae specified above, Y is a radical such as pyrazolyl and cyclohexanedionyl. R1, R2 and R3 are radicals such as halogen, nitro, cyano and alkyl.
    Type: Application
    Filed: December 22, 2011
    Publication date: June 28, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Mark James FORD, Jan Peter SCHMIDT, Helmut KOHLHEPP
  • Patent number: 8207204
    Abstract: The present invention relates to substituted triazole compounds of the formula (I): and salts thereof, to pharmaceutical compositions containing them and their use in medicine. In particular, the invention relates to compounds for inhibiting SCD activity, such as diseases related to elevated lipid levels, cardiovascular disease, diabetes, obesity, metabolic syndrome, skin disorders such as acne, diseases or conditions related to cancer and the treatment of symptoms linked to the production of the amyloid plaque-forming A?42 peptide such as Alzheimer's disease and the like.
    Type: Grant
    Filed: November 7, 2008
    Date of Patent: June 26, 2012
    Assignee: GlaxoSmithKline LLC
    Inventors: Anne Marie Jeanne Bouillot, Alain Laroze
  • Publication number: 20120149704
    Abstract: The invention relates to disubstituted benzamide derivatives of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers, prodrugs, metabolites and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating type II diabetes using the compounds of the invention.
    Type: Application
    Filed: June 21, 2010
    Publication date: June 14, 2012
    Applicant: CADILA HEALTHCARE LIMITED
    Inventor: Rajendra Kharul
  • Publication number: 20120136003
    Abstract: The present invention relates to compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Tables 1-2 or encompassed by formulas I-IV) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 20, 2010
    Publication date: May 31, 2012
    Inventors: Michael Geoffrey Neil Russell, Kevin James Doyle
  • Publication number: 20120101131
    Abstract: The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts and esters thereof, wherein Q, W, X, R1-R5 and n are defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are antagonists at the CRTH2 receptor and may be useful in treating diseases and disorders associated with that receptor such as asthma.
    Type: Application
    Filed: January 2, 2012
    Publication date: April 26, 2012
    Inventors: Li Chen, Fariborz Firooznia, Paul Gillespie, Yun He, Tai-An Lin, Sung-Sau So, HongYing Yun, Zhenshan Zhang
  • Publication number: 20120095012
    Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.
    Type: Application
    Filed: December 30, 2009
    Publication date: April 19, 2012
    Applicant: Elara Pharmaceuticals GmbH
    Inventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
  • Patent number: 8153682
    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 A, B, G, Y, R1, R2, R3, and R4 are defined herein.
    Type: Grant
    Filed: July 18, 2008
    Date of Patent: April 10, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Shawn T. Branum, Raymond W. Colburn, Scott L. Dax, Christopher M. Flores, Michele C. Jetter, Yi Liu, Donald Ludovici, Mark J. Macielag, Jay M. Matthews, James J. McNally, Laura M. Reaney, Ronald K. Russell, Ning Qin, Christopher Teleha, Kenneth M. Wells, Scott C. Youells, Mark A. Youngman
  • Patent number: 8153670
    Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Grant
    Filed: January 5, 2009
    Date of Patent: April 10, 2012
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
  • Publication number: 20120077806
    Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.
    Type: Application
    Filed: September 23, 2011
    Publication date: March 29, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey W. Perry, Roderick J. Sorenson, Mary X. O'Riordan, Yafei Jin
  • Publication number: 20120077847
    Abstract: The present invention is directed to ?-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
    Type: Application
    Filed: September 26, 2011
    Publication date: March 29, 2012
    Inventors: Michael N. Greco, Margery A. Connelly, Shyamali Ghosh, Dennis J. Hlasta, Edward C. Lawson, Eric Strobel, Michele A. Weidner-Wells, Hong Ye
  • Patent number: 8143405
    Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: September 19, 2007
    Date of Patent: March 27, 2012
    Assignee: Merck, Sharp & Dohme Corp
    Inventor: Shaun R. Stauffer
  • Publication number: 20120071513
    Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.
    Type: Application
    Filed: November 28, 2011
    Publication date: March 22, 2012
    Applicant: COMPASS PHARMACEUTICALS LLC
    Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
  • Publication number: 20120053165
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Application
    Filed: March 2, 2010
    Publication date: March 1, 2012
    Applicant: Pfizer Inc.
    Inventors: Martin Patrick Allen, Christopher William Am Ende, Michael Aaron Brodney, Amy Beth Dounay, Douglas Scott Johnson, Martin Youngjin Pettersson, Jacob Bradley Schwartz, Tuan Phong Tran
  • Publication number: 20120040984
    Abstract: The invention relates to compounds of the formula (I) either (i) in the state of a base or an acid addition salt, or (ii) in the state of an acid or a base addition salt, as well as to a method for preparing same and to the therapeutic applications thereof.
    Type: Application
    Filed: January 27, 2010
    Publication date: February 16, 2012
    Applicant: SANOFI
    Inventors: Eykmar Fett, Patrick Mougenot, Claudie Namane, Eric Nicolai, Christophe Philippo
  • Patent number: 8110588
    Abstract: This invention relates to novel 1,2,3-triazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: February 7, 2012
    Assignee: Neurosearch A/S
    Inventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters, Gunnar M. Olsen, Tino Dyhring
  • Patent number: 8110566
    Abstract: Disclosed herein are compounds of formula I in which R1, R2, R3, R4, R5, A, X, Y are as described in the specification, their use in pharmaceutical compositions and in methods of treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Grant
    Filed: April 30, 2010
    Date of Patent: February 7, 2012
    Assignee: AstraZeneca AB
    Inventors: Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Bjorn Christian Ingvar Lofberg, Joachim Persson
  • Publication number: 20120028969
    Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.
    Type: Application
    Filed: July 25, 2011
    Publication date: February 2, 2012
    Applicant: NOVARTIS AG
    Inventors: David Weninger BARNES, Gregory Raymond BEBERNITZ, Kevin CLAIRMONT, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Stephanie Kay DODD, Christoph GAUL, Hatice Belgin GULGEZE EFTHYMIOU, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Kai LIN, Justin Yik Ching MAO, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Liansheng SU
  • Publication number: 20120022083
    Abstract: Compounds, particularly compounds having activity as modulators of cadherin-mediated cell adhesion having the following structure: or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein R1, R2, R3, R4, R5, R6, A, X, Y, Z, m and n are as defined herein. Methods associated with preparation and use of the same, as well as pharmaceutical compositions containing the same, are also disclosed.
    Type: Application
    Filed: February 9, 2011
    Publication date: January 26, 2012
    Applicant: ADHEREX TECHNOLOGIES, INC.
    Inventors: Mukur Gupta, Brian Huber, Orest W. Blaschuk
  • Publication number: 20120010189
    Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 12, 2012
    Applicant: AstraZeneca AB
    Inventors: Susanne Doris Margit Bökman-Winiwarter, Marlene FREDENWALL, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
  • Publication number: 20120004270
    Abstract: This invention provides compounds as described herein or pharmaceutically acceptable salte thereof, pharmaceutical compositions comprising a compound as described herein or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor using the compounds or compositions described herein, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) using the compounds and compositions described herein and processes for making compounds described herein and intermediates useful in the preparation of same.
    Type: Application
    Filed: July 1, 2011
    Publication date: January 5, 2012
    Applicant: Radius Health, Inc.
    Inventor: Chris P. Miller
  • Patent number: 8084478
    Abstract: Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein R1, R2 and R3 are each independently selected from hydrogen, fluoro, chloro, cyano, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: December 27, 2011
    Assignee: AsstraZeneca AB
    Inventors: Roger John Butlin, Alleyn Thomas Plowright
  • Publication number: 20110306637
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: May 20, 2011
    Publication date: December 15, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • Publication number: 20110301208
    Abstract: Novel classes of viral and fungal inhibitors are disclosed. These compounds are useful in treating, preventing, and/or ameliorating viral infections such as, for example, Hepatitis C Virus, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus, and fungal infections such as, for example, candidiasis.
    Type: Application
    Filed: September 23, 2009
    Publication date: December 8, 2011
    Applicants: WICHITA STATE UNIVERSITY, GEORGETOWN UNIVERSITY
    Inventors: Radhakrishnan Padmanabhan, William C. Groutas, Brent E. Korba
  • Publication number: 20110301203
    Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 8, 2011
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Philip Stewart Turnbull, Rodolfo Cadilla, Andrew Larkin, Huiquiang Zhou, Eugene L. Stewart, Katherine Stetson, Darryl Lynn McDougald, Amarjit Sab Randhawa, John A. Ray
  • Patent number: 8067448
    Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: November 29, 2011
    Assignee: Radius Health, Inc.
    Inventor: Chris P. Miller
  • Publication number: 20110285274
    Abstract: An organic material for an organic light emitting diode (OLED) display, and an OLED display are provided, and the organic material includes an anthracene derivative includes at least deuterium.
    Type: Application
    Filed: April 29, 2011
    Publication date: November 24, 2011
    Applicant: Samsung Mobile Display Co., Ltd.
    Inventors: Yuji Hamada, Kwan-Hee Lee
  • Publication number: 20110275797
    Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 10, 2011
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
  • Publication number: 20110269761
    Abstract: The invention relates to substituted aryl-sulphonylglycine derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as in the specification and claims, which are suitable for preparing a pharmaceutical composition for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Application
    Filed: April 17, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Elke Langkopf, Frank Himmelsbach, Juergen Mack, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Publication number: 20110253994
    Abstract: A compound for an organic optoelectronic device, an organic optoelectronic device including the same, and a display device including the same, the compound for an organic optoelectronic device being represented by the following Chemical Formula 1:
    Type: Application
    Filed: June 29, 2011
    Publication date: October 20, 2011
    Inventors: Hyung-Sun Kim, Ho-Jae Lee, Sung-Hyun Jung, Young-Sung Park, Eun-Sun Yu, Mi-Young Chae, Young-Hoon Kim, Ja-Hyun Kim
  • Publication number: 20110251193
    Abstract: Novel classes of 1,2-benzisothiazolinone and isoindolinone compounds and compositions are disclosed. These compounds and compositions are useful in treating, preventing, and/or ameliorating viral, yeast, and fungal infections such as, for example, Hepatitis C Virus, Flavivirus infections, Aspergillus fumigatus, and candidiasis.
    Type: Application
    Filed: September 23, 2009
    Publication date: October 13, 2011
    Applicants: WICHITA STATE UNIVERSITY, GEORGETOWN UNIVERSITY
    Inventors: Richard A. Calderone, William C. Groutas, Brent E. Korba
  • Patent number: 8026260
    Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: September 27, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G Stanton, Paul Tempest, David J. Witter
  • Publication number: 20110224267
    Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
    Type: Application
    Filed: August 17, 2010
    Publication date: September 15, 2011
    Applicant: Radius Health,Inc.
    Inventor: Chris P. Miller
  • Patent number: 8008298
    Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: August 30, 2011
    Assignee: Roche Palo Alto
    Inventors: Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
  • Patent number: 8008301
    Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine—H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds.
    Type: Grant
    Filed: November 2, 2009
    Date of Patent: August 30, 2011
    Assignee: Eli Lilly and Company
    Inventors: Lisa Selsam Beavers, Don Richard Finley, Terry Patrick Finn, Robert Alan Gadski, Philip Arthur Hipskind, William Joseph Hornback, Cynthia Darshini Jesudason, Richard Todd Pickard, Takako Takakuwa, Grant Mathews Vaught
  • Patent number: 8003800
    Abstract: The invention relates to thiophene derivatives of formula (I)/their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunosuppressive agents wherein: A represents *—CO—CH?CH—, *—CO—CH2CH2—, *—CO—CH2—NH—, wherein the asterisks indicate the bond that is linked to the thiophene group of Formula (I), and R1-R3 are as defined in the claims.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: August 23, 2011
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jörg Velker
  • Patent number: 8003805
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein W, R1, R2, R7, R8, R9 and R10 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals. Also disclosed is a method of using such compounds in the treatment of hyperproliferative diseases in mammals, and pharmaceutical compositions containing such compounds.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: August 23, 2011
    Assignee: Array BioPharma Inc.
    Inventors: Eli M. Wallace, Joseph P. Lyssikatos, Allison L. Marlow, T. Brian Hurley
  • Patent number: 8003676
    Abstract: Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein: n is 1, 2 or 3 and each R is independently selected from fluoro, chloro, cyano, methyl, ethyl, methoxy, ethoxy, trifluoromethyl, trifluoromethoxy and difluoromethoxy; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicaments.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: August 23, 2011
    Assignee: AstraZeneca AB
    Inventors: Craig Johnstone, Alleyn Plowright
  • Patent number: 8003675
    Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: August 23, 2011
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Toshihiro Nagata, Atsushi Kogure, Isao Kaneko, Norihisa Yonekura, Ryo Hanai
  • Publication number: 20110178087
    Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.
    Type: Application
    Filed: March 30, 2011
    Publication date: July 21, 2011
    Applicant: Compass Pharmaceuticals LLC.
    Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
  • Patent number: 7981910
    Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: October 16, 2006
    Date of Patent: July 19, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sherman T. Waddell, James M. Balkovec, Nancy J. Kevin, Xin Gu
  • Patent number: 7977671
    Abstract: The present invention relates to a compound having an oxadiazole ring structure having a substituted pyridyl group connected thereto, represented by the following general formula (1). According to the present invention, it becomes possible to provide an organic compound having excellent characteristic of high stability in a thin film state, and the emission efficiency and durability of conventional organic EL devices can be remarkably improved.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: July 12, 2011
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Tetsuzo Miki, Makoto Nagaoka, Shuichi Hayashi, Yoshio Taniguchi, Musubu Ichikawa
  • Publication number: 20110160207
    Abstract: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 30, 2011
    Inventors: Stephen T. Wrobleski, Jagabandhu Das, T.G. Murali Dhar, Alaric J. Dyckman, John Hynes, Katerina Leftheris, James Lin, Shuqun Lin
  • Patent number: 7968157
    Abstract: A discotic nematic material comprising a compound of R1—H1—Ar—H2—R wherein Ar represents a substituted or unsubstituted aromatic hydrocarbon ring; H1 and H2 represent an aromatic hetero ring; and R1 and R2 represent a substituent having from 1 to 30 carbon atoms. The discotic nematic material contains a discotic liquid-crystal compound having a smaller number of side branches and capable of expressing an ND phase.
    Type: Grant
    Filed: February 6, 2007
    Date of Patent: June 28, 2011
    Assignee: Fujifilm Corporation
    Inventor: Makoto Takahashi
  • Publication number: 20110139654
    Abstract: Novel oxadiazole derivatives of the formula (I), in which R, R?, Y, X1, X2 and X3 have the meanings indicated in claim 1, are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, in general in all types of fibroses, inflammatory processes, tumours and tumour diseases.
    Type: Application
    Filed: July 9, 2009
    Publication date: June 16, 2011
    Inventors: Markus Klein, Norbert Beier, Florian Lang
  • Patent number: 7960544
    Abstract: Indoles that have activity as inhibitors of FAAH are described as are indoles and indole derivatives that have activity as inhibitors of DAO.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: June 14, 2011
    Assignee: Ironwood Pharmaceuticals, Inc.
    Inventors: Wilmin Bartolini, Brian M. Cali, Barbara Chen, Yueh-Tyng Chien, Mark G. Currie, G. Todd Milne, James Philip Pearson, John Jeffrey Talley, Jane Yang, Craig Zimmerman, Charles Kim, Kevin Sprott, Timothy Barden, Regina Lundigran, Ara Mermerian
  • Patent number: 7956074
    Abstract: The present invention is concerned with isoxazol-4-yl-oxadiazole derivatives of formula wherein R1, R2, and R3, are as defined in the specification and pharmaceutically acceptable acid addition salts thereof. This class of compounds has high affinity and selectivity for GABA A ?5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 13, 2009
    Date of Patent: June 7, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Bernd Buettelmann, Bo Han, Henner Knust, Andreas Koblet, Andrew Thomas