Abstract: The present invention provides adamantyl-diamide derivatives of formula (I): wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.
Type:
Grant
Filed:
July 17, 2009
Date of Patent:
May 24, 2011
Assignee:
H. Lundbeck A/S
Inventors:
Hermogenes N. Jimenez, Guiying Li, Dario Doller, Michel Grenon, Andrew D. White, Gil Ma, Maojun Guo
Abstract: The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes.
Type:
Application
Filed:
December 10, 2008
Publication date:
May 19, 2011
Inventors:
Scott Allen, William C. Blackwell, III, Eric Boros, Jon L. Collins, Don Hertzog, Xi Liang, John Ray, Steven Michael Reister, Vicente Samano, Ron Sherrill
Abstract: Provided herein are hepatitis C virus entry inhibitor oxoacetamide compounds, pharmaceutical compositions thereof, and methods for their use in treatment or prevention of hepatitis C virus infection in a subject in need thereof.
Type:
Application
Filed:
November 18, 2010
Publication date:
May 19, 2011
Inventors:
James E. MacDonald, McKelvy F. Jeffrey, Flossie Wong-Staal
Abstract: Disclosed are compounds of formula (I) and compositions of the present invention which are inhibitors of the sodium proton exchanger isoform-1 (NHE-I). Also disclosed are methods of using and making the same.
Type:
Application
Filed:
June 24, 2009
Publication date:
May 19, 2011
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Joerg Martin Bentzien, Stephen James Boyer, Jennifer Burke, Anne Bettina Eldrup, Xin Guo, John David Huber, Thomas Martin Kirrane, Fariba Soleymanzadeh, Alan David Swinamer
Abstract: The present invention provides compounds Formula (I) that are gamma secretase modulators and are therefore useful for the treatment of diseases treatable by modulation of gamma secretase such as Alzheimer's disease. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
Type:
Application
Filed:
May 4, 2009
Publication date:
May 19, 2011
Inventors:
Kaustav Biswas, Jian J. Chen, James R. Falsey, Vijay Keshav Gore, Qingyian Liu, Vu Van Ma, Stephanie J. Mercede, Robert M. Rzasa, Christopher M. Tegley, Jiawang Zhu
Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
Type:
Application
Filed:
January 13, 2009
Publication date:
May 19, 2011
Inventors:
Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
Abstract: The present invention relates to compounds of formula (I) comprising a lactam or a lactam derivative moiety, processes for preparing them, pharmaceutical compositions comprising said compounds and their uses as pharmaceuticals.
Abstract: Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.
Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
Type:
Application
Filed:
July 13, 2009
Publication date:
May 12, 2011
Inventors:
Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2). The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 and TYK2 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
Type:
Application
Filed:
July 1, 2009
Publication date:
May 12, 2011
Inventors:
Kevin Wilson, Gabriela de Almeida, Andrew Haidle, Kaleen Konrad, Michelle Machacek, Ann Zabierek
Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
Type:
Application
Filed:
January 18, 2011
Publication date:
May 12, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
James C. Barrow, Kelly-Ann S. Bieber, Rowena V. Cube, Mamio Christa Mattern, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; R3; R4; R5, R13, R16, X and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and thrombin and can in general be applied in conditions in which an undesired activity of factor Xa and/or thrombin are present or for the cure or prevention of which an inhibition of factor Xa and thrombin are intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
Abstract: The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. More specifically, the invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention.
Type:
Grant
Filed:
May 19, 2008
Date of Patent:
May 10, 2011
Assignee:
Kinex Pharmaceuticals, LLC
Inventors:
David G. Hangauer, Jr., Daniel Coughlin, Jonathan Gale, Jeremy A. Cody, Debasis Patra, Grant J. Palmer, Paul K. Isbester, Jonathon Salsbury
Abstract: A compound, its pharmaceutically acceptable salt, a composition containing the same and method of treatment that can provide analgesia and/or reduce inflammation are disclosed. A contemplated compound has a structure that corresponds to Formula A, wherein G, W, Q, Z, D, E, F, K, Y, d, e, f, k, n, m, and circle B and all R groups are defined within.
Type:
Application
Filed:
October 30, 2009
Publication date:
May 5, 2011
Inventors:
Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
Abstract: The present invention relates to aralkyl piperidine derivatives, compositions containing the same, and their uses in the preparation of antalgic or ataractic medicament. The said derivatives are a free base of the compound represented by the following formula or a salt thereof. The pharmacological experiments show that they display favorable antalgic, ataractic activity and low side effects.
Type:
Application
Filed:
June 20, 2008
Publication date:
May 5, 2011
Applicants:
NHWA PHARMA. CORPORATION, SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY
Inventors:
Jianqi Li, Guan Wang, Guisen Zhang, Yanqin Ma, Wenhua Ji, Yuan Zhang, Lin Guo
Abstract: This invention is in the field of pharmaceutical agents and specifically relates to compounds, compositions, uses and methods for treating cancer, by—combining VEGF(R) inhibitors and inhibitors of HGF/SF:c-Met.
Type:
Application
Filed:
May 14, 2009
Publication date:
May 5, 2011
Inventors:
Teresa L. Burgess, Angela Coxon, Isabelle Dussault, Paula Kaplan-Lefko, Anthony J. Polverino, Darrin Beaupre
Abstract: The invention relates to compositions comprising 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts. The invention provides an efficient process for the synthesis of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide and its mesylate and dihydrochloride salts and methods for modulating one or more components of a kinase cascade using the compositions of the invention. The present invention also provides a novel polymorph of the mesylate salt of 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide (Form A), characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure.
Type:
Grant
Filed:
May 19, 2009
Date of Patent:
May 3, 2011
Assignee:
Kinex Pharmaceuticals, LLC
Inventors:
David G. Hangauer, Jr., Debasis Patra, Jeremy A. Cody, Grant J. Palmer, Paul K. Isbester, Jonathon Salsbury
Abstract: This invention is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I) to processes for their preparation; to pharmaceutical compositions comprising them; and to their use in therapy.
Type:
Application
Filed:
February 12, 2007
Publication date:
April 28, 2011
Inventors:
Bernat Vidal Juan, Juan Francisco Caturla Javaloyes, Wenceslao Lumeras Amador, Laura Vidal Gispert
Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
Type:
Application
Filed:
August 3, 2010
Publication date:
April 28, 2011
Applicant:
ABBOTT LABORATORIES
Inventors:
Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
Abstract: The invention relates to a topical composition and a method for treating psoriasis. The topical composition comprises one or more compound that inhibits the production of IL-12 and IL-23.
Type:
Application
Filed:
February 6, 2009
Publication date:
April 28, 2011
Applicant:
Synta Pharmaceuticals Corporation
Inventors:
Suresh R. Babu, Yumiko Wada, Jianhua Shen, Nhung Nguyen
Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, m and n are defined as in the specification, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
Type:
Application
Filed:
April 20, 2010
Publication date:
April 28, 2011
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Tobias Wunberg, Siegfried Schneider, Lars Van Der Veen
Abstract: The present invention relates to compounds of formula (I) comprising a cyclobutoxy group, processes for preparing them, pharmaceutical compositions comprising said compounds and their use as pharmaceuticals, useful for the treatment and prevention of diseases or pathological conditions of the central nervous system including mild-cognitive impairments, Alzheimer's disease, learning and; memory disorders, cognitive disorders, attention deficit disorder, attention-deficit hyperactivity disorder, Parkinson's disease, schizophrenia, dementia, depression, epilepsy, seizures, convulsions, sleep/wake and arousal/vigilance disorders such as hypersomnia and narcolepsy, pain and/or obesity.
Type:
Application
Filed:
June 2, 2009
Publication date:
April 28, 2011
Applicant:
UCB PHARMA, S.A.
Inventors:
Sylvain Celanire, Laurent Provins, Frederic Denonne, Anne Valade
Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
Type:
Application
Filed:
October 26, 2010
Publication date:
April 28, 2011
Applicant:
H. LUNDBECK A/S
Inventors:
Hao Zhou, Guiying Li, Dario Doller, Gil Ma
Abstract: The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
Type:
Grant
Filed:
May 12, 2005
Date of Patent:
April 26, 2011
Assignee:
ChemoCentryx, Inc.
Inventors:
Solomon Ungashe, John Jessen Wright, Andrew Pennell
Abstract: The present invention provides novel organic compounds of Formula I: methods of use, and pharmaceutical compositions thereof.
Type:
Application
Filed:
June 12, 2009
Publication date:
April 21, 2011
Inventors:
Robin Burgis, Michael Paul Capparelli, Lucian Dipietro, Gabriel G. Gamber, Charles Francis Jewell, JR., Erik Meredith, Karl Miranda, Lauren G. Monovich, Chang Rao, Nicolas Soldermann, Taeyoung Yoon, Qingming Zhu
Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.
Type:
Application
Filed:
December 6, 2010
Publication date:
April 21, 2011
Inventors:
Janet L. GUNZNER, Daniel Sutherlin, Mark S. Stanley, Liang Bao, Georgette M. Castanedo, Rebecca L. Lalonde, Shumei Wang, Mark E. Reynolds, Scott J. Savage, Kimberly Malesky, Michael S. Dina
Abstract: The invention provides a method for modulating the activity of the hedgehog signaling pathway. In particular, the invention provides a method for inhibiting aberrant growth states resulting from phenotypes such as Ptc loss-of-function, hedgehog gain-of-function, smoothened gain-of-function or Gli gain-of-function, comprising contacting a cell with a sufficient amount of a compound of Formula I.
Type:
Grant
Filed:
July 24, 2007
Date of Patent:
April 19, 2011
Assignee:
IRM LLC
Inventors:
Dai Cheng, Dong Han, Wenqi Gao, Jiqing Jiang, Shifeng Pan, Yongqin Wan, Qihui Jin
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Grant
Filed:
October 15, 2007
Date of Patent:
April 19, 2011
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Doris Riether, David Smith Thomson, Renee M. Zindell
Abstract: The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.
Type:
Application
Filed:
April 5, 2007
Publication date:
April 14, 2011
Applicant:
Santhera Pharmaceuticals (Schweiz) AG
Inventors:
Michael Soeberdt, Holger Deppe, Philipp Weyermann, Stephan Bulat, Andreas Von Sprecher, Achim Feurer, Cyrille Lescop, Marco Hennebohle, Sonja Nordhoff
Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.
Type:
Application
Filed:
October 6, 2010
Publication date:
April 14, 2011
Inventors:
David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
Type:
Application
Filed:
April 15, 2009
Publication date:
April 7, 2011
Inventors:
Erik Verner, Sriram Balasubramanian, Joseph J. Buggy
Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
Type:
Application
Filed:
December 7, 2010
Publication date:
March 31, 2011
Applicant:
DAC S.r.I.
Inventors:
Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
Type:
Application
Filed:
November 30, 2010
Publication date:
March 24, 2011
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Malcolm TAYLOR, Chandana CHOWDHURY, Christopher Francis PALMER, Nigel BLUMIRE
Abstract: The invention relates to a process for preparing a pharmaceutical tablet composition which comprises an active pharmaceutical ingredient of formula I wherein the definitions are described in claim 1, or pharmaceutically acceptable acid addition salts thereof and a water soluble poloxamer in which the compound of formula I and the water soluble poloxamer are processed by hot melt extrusion, and then the hot melt extrudate is mixed with other ingredients to form a tablet, that is optionally coated with a composition comprising an immediate release film coating system and purified water. The invention also relates to such pharmaceutical compositions and hot melt extrudates.
Type:
Application
Filed:
November 29, 2010
Publication date:
March 24, 2011
Inventors:
Hashim A. Ahmed, Susanne Page, Navnit Hargovindas Shah
Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
Type:
Grant
Filed:
May 3, 2010
Date of Patent:
March 15, 2011
Assignee:
Abbott Laboratories
Inventors:
Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
Abstract: Disclosed is a compound having a strong affinity to serotonin-4 receptors, which is useful as an enterokinesis-promoting agent or a digestive tract function-improving agent. Specifically, disclosed is a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. Also specifically disclosed is a pharmaceutical composition containing a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. [In Formula (1), Ar represents a group represented by Formula (Ar-1) or Formula (Ar-2).
Abstract: The present invention relates to novel carboxamide compounds of the formula I and their use for the manufacture of a medicament. The carboxamide compounds are prodrugs of inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity.
Type:
Application
Filed:
December 29, 2008
Publication date:
March 10, 2011
Applicant:
Abbott GmbH & Co. KG
Inventors:
Wilfried Hornberger, Helmut Mack, Andreas Kling, Achim Moeller, Barbara Vogg, Jürgen Delzer, Gisela Backfisch, Armin Beyerbach
Abstract: The present invention provides a novel benzene derivative or thiophene derivative useful as a VAP-1 inhibitor, or a medicament for the prophylaxis or treatment of a VAP-1 associated disease and the like, namely, a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat obesity and other histamine H3 receptor-related diseases.
Type:
Grant
Filed:
February 22, 2005
Date of Patent:
March 8, 2011
Assignee:
Eli Lilly and Company
Inventors:
Lisa Selsam Beavers, Robert Alan Gadski, Philip Arthur Hipskind, Cynthia Darshini Jesudason, Karen Lynn Lobb, Richard Todd Pickard, Craig William Lindsley
Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
December 10, 2008
Date of Patent:
March 8, 2011
Assignee:
AstraZeneca AB
Inventors:
Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
Abstract: The present invention relates to 3,4-substituted piperidinyl-based renin inhibitor compounds bearing at 4-position oxopyridine and having the formula (I). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
Type:
Application
Filed:
May 4, 2009
Publication date:
March 3, 2011
Inventors:
Austin Chih-Yu Chen, Daniel Dube, Pierre-Andre Fournier, Erich L. Grimm, Patrick Lacombe, Sebastien Laliberte, Dwight MacDonald, D. Bruce MacKay, Daniel James McKay, Tom Yao-Hsiang Wu, Louis-Charles Campeau, Jeremy Peter Scott, Nadine Bremeyer
Abstract: The invention relates to compounds and composition for the treatment and prevention of cancer. The invention also covers all diseases that may be treated by selective modulation of levels of reactive oxygen species in diseased cells versus normal cells. Methods for the preparation and administration of such compositions are also disclosed.
Type:
Application
Filed:
September 2, 2010
Publication date:
March 3, 2011
Applicant:
CANTHERA THERAPEUTICS, INC.
Inventors:
Michael Andrew Foley, Robert Gould, Peter Elliott, Anna Mandinova, Sam Lee
Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
Type:
Application
Filed:
March 10, 2008
Publication date:
February 24, 2011
Applicant:
The Scripps Research Institute
Inventors:
Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
Abstract: The invention relates to pyrrolidine derivatives of formula wherein R1, R2, R3, n, and o are defined in the specification and to pharmaceutically active acid-addition salts thereof. Compounds of formula I have a high affinity simultaneously to both the NK1 and the NK3 receptors (dual NK1/NK3 receptor antagonists), useful in the treatment of schizophrenia.
Abstract: The present invention comprises a new class of compounds capable of modulating the c-kit receptor and, accordingly, useful for treatment of c-kit mediated diseases, including various inflammatory, fibrotic and/or mast cell mediated diseases such as mastocytosis. The compounds have a general Formula I wherein A1-3, R1 and R3-6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of c-kit mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.
Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
Type:
Application
Filed:
April 22, 2009
Publication date:
February 17, 2011
Applicant:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventors:
Masato Yoshida, Nobuki Sakauchi, Ayumu Sato
Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
Type:
Grant
Filed:
May 24, 2006
Date of Patent:
February 15, 2011
Assignee:
Merck Serono SA
Inventors:
Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
Type:
Application
Filed:
October 7, 2010
Publication date:
February 10, 2011
Applicant:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
Inventors:
Masato YOSHIDA, Nobuki Sakauchi, Ayumu Sato