Polycyclo Ring System Which Contains The Seven-membered Hetero Ring As One Of The Cyclos Patents (Class 514/211.09)
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Patent number: 8604019Abstract: The invention relates to the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and X are as defined in the description and claims, which are useful for the treatment or prophylaxis of RSV infection.Type: GrantFiled: October 10, 2012Date of Patent: December 10, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Chungen Liang, Lisha Wang, Hongying Yun, Xiufang Zheng
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Publication number: 20130317005Abstract: Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management.Type: ApplicationFiled: August 31, 2011Publication date: November 28, 2013Inventors: Anthony C. Blackburn, Yun Shan, Anna Shifrina, Scott Stirn
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Patent number: 8569284Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.Type: GrantFiled: August 1, 2010Date of Patent: October 29, 2013Assignee: The Trustees Of The University Of PennsylvaniaInventors: William F. DeGrado, Jun Wang
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Publication number: 20130281512Abstract: The present invention relates to 1,4-benzothiazepine derivatives and their use to treat conditions, disorders and diseases associated with ryanodine receptors (RyRs) that regulate calcium channel functioning in cells. The invention also discloses pharmaceutical compositions comprising the compounds and uses thereof to treat diseases and conditions associated with RyRs, in particular cardiac, musculoskeletal and central nervous system (CNS) disorders.Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Applicants: ARMGO Pharma, Inc., LES LABORATOIRES SERVIERInventors: Jiaming YAN, Sandro BELVEDERE, Yael WEBB, Mark BERTRAND, Nicole VILLENEUVE
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Patent number: 8557738Abstract: The present invention provides a nitrogen-containing heterocyclic compound represented by formula (I) and salt thereof (wherein, R1 to R6 each independently represents a hydrogen atom, unsubstituted or substituted C1-20 alkyl group and the like, R1 and R2, R3 and R4, or R5 and R6 may together form an unsubstituted or substituted 5- to 8-membered ring, A-B, in which A represents a carbon atom and B represents a nitrogen atom, represents the formula: C?N and the like, Y represents an oxygen atom and the like, X and X? each independently represent an unsubstituted or substituted C1-20 alkyl group and the like, m represents an integer of 0 to 2, and n represents an integer of 0 to 4), and a fungicide for agricultural and horticultural use that contains at least one of these compounds as an active ingredient thereof, demonstrates reliable effects and can be used safely.Type: GrantFiled: August 10, 2009Date of Patent: October 15, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Akira Mitani, Jun Inagaki, Raito Kuwahara, Masahiro Yokoyama, Kotaro Shibayama, Motoaki Sato
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Publication number: 20130267496Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: May 23, 2013Publication date: October 10, 2013Applicant: GILEAD CONNECTICUT, INC.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
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Publication number: 20130261101Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: April 1, 2013Publication date: October 3, 2013Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
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Publication number: 20130261106Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.Type: ApplicationFiled: April 2, 2013Publication date: October 3, 2013Applicant: SANOFIInventors: Jean-Christophe CARRY, Fabienne CHATREAUX, Stephanie DEPRETS, Olivier DUCLOS, Vincent LEROY, Sergio MALLART, Dominique MELON-MANGUER, Maria MENDEZ-PEREZ, Fabrice VERGNE
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Publication number: 20130261105Abstract: This invention relates to novel pyrazolopyrimidines and their use as metabotropic glutamate 5 receptor antagonists (mGlu5 receptor antagonists), pharmaceutical compositions containing the same, and methods of using the same as agents for treatment or amelioration of mGlu5 receptor mediated disorders.Type: ApplicationFiled: March 27, 2013Publication date: October 3, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk GOTTSCHLING, Heiner EBEL, Doris RIETHER, Bernd WELLENZOHN
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Publication number: 20130237520Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: April 23, 2013Publication date: September 12, 2013Applicant: GILEAD CONNECTICUT, INC.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J.M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
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Publication number: 20130236541Abstract: The present invention relates to a combination comprising a substance with inhibiting effect on the ileal bile acid transport system (I BAT) and at least one other active substance selected from an IBAT inhibitor; an enteroendocrine peptide or enhancer thereof; a dipeptidyl peptidase-IV inhibitor; a biguanidine; an incretin mimetic; a thiazolidinone; a PPAR agonist; a HMG Co-A reductase inhibitor; a bile acid binder; and a TGR5 receptor modulator; wherein the IBAT inhibitor compound and the at least one other active substance are administered simultaneously, sequentially or separately.Type: ApplicationFiled: November 8, 2011Publication date: September 12, 2013Applicant: Albireo ABInventors: Per-Göran Gillberg, Hans Graffner, Ingemar Starke
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Publication number: 20130237521Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: ApplicationFiled: April 23, 2013Publication date: September 12, 2013Applicant: GILEAD CONNECTICUT, INC.Inventors: Scott A. MITCHELL, Kevin S. CURRIE, Peter A. BLOMGREN, Jeffrey E. KROPF, Seung H. LEE, Jianjun XU, Douglas G. STAFFORD, James P. HARDING, Antonio J. M. BARBOSA, JR., Zhongdong ZHAO, David M. ARMISTEAD, Soumya MITRA
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Publication number: 20130237524Abstract: Disclosed embodiments concern polycyclic alkaloid compounds and methods for their use and synthesis. Particular embodiments concern polycyclic alkaloids having a fused, six-membered ring, while other embodiments concern polycyclic alkaloids having a fused, five-membered ring. Methods for making the polycyclic alkaloids are disclosed, as well as methods for their use as prophylactics or treatments for certain diseases. Also disclosed are pharmaceutical compositions comprising the polycyclic alkaloids and their use.Type: ApplicationFiled: March 7, 2013Publication date: September 12, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Donald G. Payan, Sylvia Braselmann
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Publication number: 20130196974Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R10, A, Q, X and Y are as defined in the specification and claims, and their use as a pharmaceutical for the treatment or prophylaxis of respiratory syncytial virus disease.Type: ApplicationFiled: July 30, 2012Publication date: August 1, 2013Inventors: Li Chen, Lichun Feng, Song Feng, Lu Gao, Tao Guo, Mengwei Huang, Chungen Liang, Yongfu Liu, Lisha Wang, Jason Christopher Wong, Jim Zhen Wu, Xihan Wu, Hongying Yun, Xiufang Zheng
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Publication number: 20130190288Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, A, X1, X2, X3, X4, R1, R2, R3a, R3b, R4a and R4b 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: Genentech, Inc.
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Patent number: 8481525Abstract: The invention is directed to a compound represented by the following structural formula and pharmaceutically acceptable salts thereof: Compounds represented by this structural formula are kinase inhibitors and are therefore disclosed herein for the treatment of cancer. Definitions for the variables in the structural formula are provided herein.Type: GrantFiled: April 6, 2010Date of Patent: July 9, 2013Assignee: University of Health NetworkInventors: Peter Brent Sampson, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Heinz W. Pauls, Louise G. Edwards, Miklos Feher, Narendra Kumar B. Patel, Guohua Pan
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Patent number: 8481524Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.Type: GrantFiled: March 31, 2010Date of Patent: July 9, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Lauffer, Pan Li, Nathan Waal, Kira Mcginty, Qing Tang, Steven Ronkin, Luc Farmer, Dean Shannon, Dylan Jacobs
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Patent number: 8466144Abstract: The present invention relates to generally to the cytoprotective activity of mixed muscarinic inhibition/PARP modulation and in particular to the use of dual inhibitors of M1 muscarinic receptor and poly(ADP-ribose) polymerase (PARP) as neuroprotective medicaments, particularly as medicaments for the prevention and/or treatment of neurological diseases. Particularly preferred compounds are condensed diazepinones, e.g. condensed benzodiazepinones such as pirenzepine or compounds which are metabolized to condensed benzodiazepinones such as olanzapine.Type: GrantFiled: July 18, 2005Date of Patent: June 18, 2013Assignee: Proteosys AGInventor: André Schrattenholz
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Publication number: 20130116237Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: October 10, 2012Publication date: May 9, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Publication number: 20130116213Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: June 20, 2011Publication date: May 9, 2013Applicant: HANMI SCIENCE CO., LTD.Inventors: Mi Young Cha, Seok Jong Kang, Mi Ra Kim, Ju Yeon Lee, Ji Young Jeon, Myoung Gi Jo, Eun Joo Kwak, Kwang Ok Lee, Tae Hee Ha, Kwee Hyun Suh, Maeng Sup Kim
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Publication number: 20130108573Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: May 2, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Publication number: 20130109671Abstract: Provided herein are methods of treating or ameliorating a pediatric cholestatic liver disease by non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a pediatric liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising non-systemically administering to an individual in need thereof a therapeutically effective amount of a pediatric formulation comprising an ASBTI or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: May 2, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Lumena Pharmaceuticals, Inc.
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Patent number: 8431564Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: July 27, 2010Date of Patent: April 30, 2013Assignee: Merck Sharp & Dohme B.V.Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20130090328Abstract: The invention relates to the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and X are as defined in the description and claims, which are useful for the treatment or prophylaxis of RSV infection.Type: ApplicationFiled: October 10, 2012Publication date: April 11, 2013Applicant: Hoffmann-La Roche IncInventor: Hoffmann-La Roche Inc
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Publication number: 20130079333Abstract: The present invention provides 4H,6H-5-oxa-2,3,10b-triaza-benzo[e]azulenes of the formula wherein R1 and R2 are as defined herein and which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments.Type: ApplicationFiled: August 23, 2012Publication date: March 28, 2013Inventors: Cosimo Dolente, Patrick Schnider
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Patent number: 8399452Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.Type: GrantFiled: October 26, 2007Date of Patent: March 19, 2013Assignees: Methylgene Inc., EnVivo PharmaceuticalsInventors: Robert Déziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Publication number: 20130059807Abstract: Provided herein are methods of utilizing bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents for the treatment of obesity, diabetes, and inflammatory gastrointestinal conditions.Type: ApplicationFiled: February 22, 2012Publication date: March 7, 2013Applicant: Satiogen Pharmaceuticals, Inc.Inventors: Bronislava Gedulin, Andrew A. Young, Howard E. Greene
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Publication number: 20130053343Abstract: Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis.Type: ApplicationFiled: November 2, 2010Publication date: February 28, 2013Applicant: The Trustees of Columbia University in th City ofInventors: Donald Landry, Shi-Xian Deng
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Publication number: 20130034536Abstract: Provided herein are methods and compositions comprising bile acid transport inhibitors and/or enteroendocrine peptide enhancing agents and/or FXR agonists for the treatment of pancreatitis or prevention of pancreatitis.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Lumena Pharmaceuticals, Inc.Inventor: Bronislava GEDULIN
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Publication number: 20130029938Abstract: Compounds of Formula I and methods for treating metabolic disorders are disclosed.Type: ApplicationFiled: April 27, 2011Publication date: January 31, 2013Applicant: GlaxoSmithKline LLCInventors: Christopher Joseph Aquino, Jon Loren Collins, David John Cowan, Yulin Wu
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Publication number: 20130017273Abstract: The present invention relates to pyrrolopyrazines compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein.Type: ApplicationFiled: June 22, 2012Publication date: January 17, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Simon Everitt, Michael Paul Mortimore, Jean-Damien Charrier, Somhairle MacCormick, Pierre-Henri Storck, Ronald Knegtel, Joanne Pinder, Steven John Durrant
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Publication number: 20130012494Abstract: The present invention provides cyclopropyl-fused-1,3-thiazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.Type: ApplicationFiled: June 29, 2012Publication date: January 10, 2013Inventor: Thomas Woltering
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Publication number: 20130005706Abstract: The present disclosure relates to compounds that are sodium channel inhibitors 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 Y, Z, n, R1 and R3 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 29, 2012Publication date: January 3, 2013Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Publication number: 20120316153Abstract: The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the use of such benzazepine derivatives for therapeutic purposes.Type: ApplicationFiled: May 10, 2012Publication date: December 13, 2012Applicants: Abbott Laboratories, Abbott GmbH & Co., KGInventors: Wilhelm Amberg, Udo Lange, Michael Ochse, Frauke Pohlki, Berthold Behl, Mario Mezler, Willfried Hornberger, Charles W. Hutchins
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Publication number: 20120258953Abstract: The invention is directed to Compounds of Formula (I): the invention provides compounds that inhibit, regulate, and/or modulate P13K and/or mTOR that are useful in the treatment of hyperproliferative diseases, such as cancer, in mammals. This invention also provides methods of making the compound methods of using such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: May 25, 2010Publication date: October 11, 2012Applicant: Exelixis, Inc.Inventors: Naing Aay, Arlyn Arcalas, Joerg Bussenius, Charles Steven Defina, Larisa Dubenko, Jason R. Harris, Eileen E. Jackson-Ugueto, Angie Inyoung Kim, Jean-Claire Limun Manalo, Michael Pack, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang, Owen Joseph Bowles, Jeffry Kimo Curtis
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Patent number: 8283346Abstract: The described invention relates to novel human immunodeficiency virus protease inhibitors, pharmaceutical compositions containing at least one such inhibitor, methods of preparing such inhibitors, and methods of utilizing such inhibitors to treat HIV and HIV-related disorders.Type: GrantFiled: November 10, 2009Date of Patent: October 9, 2012Assignee: The Trustees of the Stevens Institute of TechnologyInventors: A. K. Ganguly, Dipshikha Biswas, Sesha Sridevi Alluri, Danielle Caroccia, Chih-Hung Wang, Eun Hee Kang
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Publication number: 20120245139Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: June 4, 2012Publication date: September 27, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Publication number: 20120232057Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: September 13, 2012Inventors: George W. GRIESGRABER, Tushar A. KSHIRSAGAR, Azim A. CELEBI, Sarah J. SLANIA, Michael E. DANIELSON, Michael J. RICE, Joshua R. WURST
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Patent number: 8263588Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: April 4, 2008Date of Patent: September 11, 2012Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Patent number: 8263587Abstract: The invention provides a novel benzoxazepine compound of the general formula (I): wherein R1 and R2 are as defined in the specification; or a stereoisomer, a geometric isomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, or a polymorph thereof; a process for its preparation; and a pharmaceutical composition including an effective amount of the compound. The compounds are useful in the treatment of insulin resistance and clinical conditions associated therewith.Type: GrantFiled: November 1, 2007Date of Patent: September 11, 2012Assignee: Piramal Healthcare LimitedInventors: Swati Bal-Tembe, Bansi Lal, Satish Namdeo Sawant, Anagha Suhas Kulkarni
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Publication number: 20120225858Abstract: The present invention relates to 1,4 Thiazepines/Sulfones of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Hans Hilpert, Mark Rogers-Evans, Didier Rombach
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Publication number: 20120220568Abstract: This invention is directed to a compound of formula I, wherein R1, R2, R4, R5, R6, R7, R8 and n are as defined herein, or a pharmaceutically acceptable salt thereof; a pharmaceutical composition containing a compound of formula I, a process of preparation of a compound of formula I, a method of treatment of a disorder or condition such as depression, mood disorders, schizophrenia, anxiety disorders, Alzheimer's disease, attention-deficit hyperactivity disorder (ADHD), psychotic disorders, cognitive disorders, sleep disorders, obesity, dizziness, epilepsy, motion sickness, respiratory diseases, allergy, allergy-induced airway responses, allergic rhinitis, nasal congestion, allergic congestion, congestion, hypotension, cardiovascular disease, diseases of the GI tract, hyper and hypo motility and acidic secretion of the gastro-intestinal tract that may be treated by antagonizing histamine H3 receptors, the method comprising administering to a mammal in need of such treatment a compound of formula I as descriType: ApplicationFiled: March 9, 2012Publication date: August 30, 2012Inventors: Travis T. Wager, Ramalakshmi Y. Chandrasekaran, Todd William Butler
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Publication number: 20120220567Abstract: The present invention relates to certain 4,5-dihydro-3H-spiro[benzo[b]-[1,4]oxazepine compounds of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, m, n, o, and p are as herein described. In addition, the invention relates to compositions comprising at least one such compound, and methods of using the compounds for treating or preventing disorders such as non-insulin dependent (Type 2) diabetes, insulin resistance, hyperglycemia, a lipid disorder, obesity, fatty liver disease, or a skin disorder.Type: ApplicationFiled: July 21, 2010Publication date: August 30, 2012Inventors: Gerald W. Shipps, JR., Zhiwei Yang, Yongqi Deng, Robert E. West, JR., Dineshwar P. Sinha
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Patent number: 8247403Abstract: Compounds represented by the general formula (I): wherein each symbol is as defined in the description [with the proviso that 9-chloro-7-(1,1-dimethylethyl)-2,3,4,5-tetrahydro-1,4-benz-oxazepine and N-[[(5S)-2-oxo-3-(2,3,4,5-tetrahydro-1,4-benz-oxazepin-7-yl)-5-oxazolidinyl]methyl]acetamide are excluded], salts of the same, and prodrugs thereof have selective activation effect on serotonin 5-HT2C receptor and are useful as preventive and therapeutic agents for lower urinary tract diseases, obesity, and/or pelvic organ prolapse.Type: GrantFiled: March 6, 2008Date of Patent: August 21, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Junya Shirai, Takahiro Matsumoto, Izumi Kamo
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Patent number: 8242103Abstract: Bridged bicyclic sulphamides of formula (I) are disclosed for treatment of cancer.Type: GrantFiled: May 16, 2006Date of Patent: August 14, 2012Assignee: Merck Sharp & Dohme LimitedInventors: Huw David Lewis, Timothy Harrison, Mark Steven Shearman
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Publication number: 20120202790Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein n1, n2, n3, n4, A, B, D, E, G, Y, Z, R1 and R2 are defined herein.Type: ApplicationFiled: November 4, 2011Publication date: August 9, 2012Inventors: John M. Fevig, Dean A. Wacker
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Publication number: 20120202756Abstract: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.Type: ApplicationFiled: October 5, 2011Publication date: August 9, 2012Inventors: Richard Franklin, Martin Quibell, Robert G. Tyson, Bernard T. Golding
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Publication number: 20120184528Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: May 11, 2010Publication date: July 19, 2012Applicants: ADDEX PHARMA S.A., JANSSEN PHARMACEUTICALS, INCInventors: Jose Maria Cic-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
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Publication number: 20120184527Abstract: The present invention relates to novel triazolo[4,3-a]pyridine derivatives of Formula (I) wherein all radicals are as defined in the claims. The compounds according to the invention are positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (“mGluR2”), which are useful for the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which the mGluR2 subtype of metabotropic receptors is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds for the prevention or treatment of neurological and psychiatric disorders and diseases in which mGluR2 is involved.Type: ApplicationFiled: May 11, 2010Publication date: July 19, 2012Applicants: ADDEX PHARMA S.A., JANSSEN PHARMACEUTICALS, INCInventors: Jose Maria Cic-Nunez, Ana Isabel De Lucas Olivares, Andres Avelino Trabanco-Suarez, Gregor James MacDonald
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Patent number: 8222245Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: December 19, 2008Date of Patent: July 17, 2012Assignee: Glaxo Group LimitedInventors: Emmanuel Hubert Demont, Jag Paul Heer, John Skidmore, Ian David Wall, Jason Witherington, Thomas Daniel Heightman, David Nigel Hurst, Christopher Norbert Johnson