Polycyclo Ring System Having The Additional Six-membered Hetero Ring As One Of The Cyclos Patents (Class 514/252.04)
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Publication number: 20120225885Abstract: The present invention relates to novel imidazole compounds, pharmaceutical compositions comprising the imidazole compounds and the use of these compounds for treating or preventing allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: November 12, 2010Publication date: September 6, 2012Inventors: Ashwin U. Rao, Anandan Palani, Robert G. Aslanian
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Patent number: 8258134Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: GrantFiled: March 9, 2009Date of Patent: September 4, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Steven Joseph Berthel, Nancy-Ellen Haynes, Robert Francis Kester, Lee Apostle McDermott, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Jefferson Wright Tilley
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Publication number: 20120220599Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: May 2, 2012Publication date: August 30, 2012Inventors: Dominik FEUERBACH, Konstanze HURTH, Timothy John RITCHIE
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Publication number: 20120208791Abstract: The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: June 12, 2009Publication date: August 16, 2012Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Maria Grazia Carr, Miles Stuart Congreve, Martyn Frederickson, Charlotte Mary Griffiths-Jones, Christopher Charles Frederick Hamlett, Andrew Madin, Christopher William Murray, Rajdeep Kaur Benning, Gordon Saxty, Emma Vickerstaffe, Brian John Williams, Marian Williams, Andrew James Woodhead, Steven John Woodhead, Eddy Jean Edgard Freyne, Tom Cornelis Hortense Govaerts, Patrick René Angibaud
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Publication number: 20120208820Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: ApplicationFiled: January 31, 2012Publication date: August 16, 2012Inventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120202822Abstract: The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer.Type: ApplicationFiled: October 12, 2010Publication date: August 9, 2012Inventors: Kurtis Earl Bachman, Joel David Greshock, Tona Gilmer, Sylvie Laquerre, Shannon Renae Morris
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Patent number: 8236796Abstract: The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3 -a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle oType: GrantFiled: April 2, 2009Date of Patent: August 7, 2012Assignees: Albany Molecular Research, Inc., Bristol-Myers Squibb CompanyInventors: Bruce F. Molino, Shuang Liu, Peter R. Guzzo, James P. Beck
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Patent number: 8236803Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: October 31, 2008Date of Patent: August 7, 2012Assignee: Novartis AGInventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
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Publication number: 20120196845Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: October 1, 2010Publication date: August 2, 2012Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
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Publication number: 20120184523Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: ApplicationFiled: March 22, 2012Publication date: July 19, 2012Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takbuchi, Yong Wang, Wei Xu
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Publication number: 20120178707Abstract: Methods for treating prostate cancer involving the administration of a compound that selectively inhibits pathological production of human vascular endothelial growth factor (VEGF) are described. Methods for treating benign prostatic hyperplasia involving the administration of a compound that selectively inhibits pathological production of human VEGF are also described. The compound may be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: July 12, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Charles M. Romfo, Marla L. Weetall
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Publication number: 20120157400Abstract: Methods for treating Kaposi's sarcoma involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, Langdon Miller, Marla L. Weetall
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Publication number: 20120157460Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.Type: ApplicationFiled: December 20, 2011Publication date: June 21, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Matthew D. SURMAN, Peter R. GUZZO, Emily FREEMAN, Alan J. HENDERSON
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Publication number: 20120157464Abstract: The invention concerns the use of azabicycloalkyl derivatives or pyrrolidine-2-one derivatives for the treatment, prevention or delay of progression of ataxia.Type: ApplicationFiled: July 21, 2010Publication date: June 21, 2012Inventors: Dominik Feuerbach, Baltazar Gomez-Mancilla
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Publication number: 20120157402Abstract: Methods for treating brain tumors involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Samit Hirawat, Harry H. Miao, langdon Miller, Marla Weetall
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Publication number: 20120157401Abstract: Methods for treating neurofibromatosis involving the administration of a compound that selectively inhibits pathological production of human VEGF are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: May 27, 2010Publication date: June 21, 2012Inventors: Liangxian Cao, Thomas W. Davis, Harry H. Miao, Langdon Miller, Marla Weetall
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Publication number: 20120142669Abstract: The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use thereof in therapy.Type: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Applicant: SANOFI-AVENTISInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, David Machnik, André Malanda
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Publication number: 20120142670Abstract: The invention relates to compounds of the general formula (I): Wherein X, Y, Z, Z1, Z2, Z3, Z4 and n are as defined herein. The invention also relates to a method for making the same and to the use thereof in therapy.Type: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Applicant: SANOFI-AVENTISInventors: Laurent Dubois, Yannick Evanno, Catherine Gille, David Machnik, André Malanda
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Patent number: 8193192Abstract: The present invention relates to compounds which bind to the NR1H4 receptor (FXR) and act as agonists or partial agonists of the NR1H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.Type: GrantFiled: August 29, 2007Date of Patent: June 5, 2012Assignee: Phenex Pharmaceuticals AGInventors: Claus Kremoser, Ulrich Deuschle, Ulrich Abel, Andreas Schulz
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Publication number: 20120135999Abstract: The present invention is directed to compounds and forms and pharmaceutical compositions thereof useful for treating a viral infection, or for affecting viral activity by modulating viral replication.Type: ApplicationFiled: April 5, 2010Publication date: May 31, 2012Applicant: PTC THERAPEUTICS, INC.Inventors: Malcolm Maccoss, F. George Njoroge, Amin Nomeir, Guangming Chen, Gary Mitchell Karp, William Jospeh Lennox, Chunshi Li, Christie Morrill, Steven D. Paget, Hongyu Ren, Nanjing Zhang, Xiaoyan Zhang
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Patent number: 8183238Abstract: Compounds of Formula X: wherein A, X, Y, Z, R5, R6a, and R6b are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other neurodegenerative and/or neurological disorders in mammals, including humans.Type: GrantFiled: June 16, 2010Date of Patent: May 22, 2012Assignee: Pfizer Inc.Inventors: Michelle M. Claffey, Amy B. Dounay, Matthew M. Hayward, Suobao Rong, Patrick R. Verhoest, Jamison B. Tuttle, Xinmin Gan
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Publication number: 20120108601Abstract: A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating crystalline compound (1) are provided.Type: ApplicationFiled: December 23, 2011Publication date: May 3, 2012Applicants: Gilead Sciences, Inc., Gerhard Puerstinger, K.U. Leuven Research & DevelopmentInventors: Eric D. Dowdy, Kenneth M. Kent, Norma J. Tom, Vahid Zia
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Publication number: 20120070413Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Inventors: Tae-Seong KIM, David Bauer, Steven Bellon, Alessadro Boezio, Shon Booker, Deborah Choquette, Derin C. D'Amico, Noel D'Angelo, Celia Dominguez, Ingrid M. Fellows, Julie Germain, Russell Graceffa, Jean-Christophe Harmange, Satoko Hirai, Daniel La, Matthew Lee, Longbin Liu, Mark H. Norman, Michele Potashman, Philip Roveto, Aaron C. Siegmund, Ning Xi, Kevin Yang
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Publication number: 20120065165Abstract: Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.Type: ApplicationFiled: November 2, 2009Publication date: March 15, 2012Applicant: ARGINETIX, INCInventors: Simon E. Aspland, Dan E. Berkowitz, Trinity Bivalacqua, Hunter Champion
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Publication number: 20120046298Abstract: The invention relates to compounds having general formula (I), wherein R is as defined herein. The invention also relates to acid addition salt, a hydrate or a solvate of compounds of formula (I). The invention further relates to the method of preparing said compounds and to the use of same in therapeutics.Type: ApplicationFiled: November 1, 2011Publication date: February 23, 2012Applicant: SANOFI-AVENTISInventors: Frederic GALLI, Odile LECLERC, Alistair LOCHEAD, Julien VACHE
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Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20120040949Abstract: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.Type: ApplicationFiled: August 11, 2011Publication date: February 16, 2012Inventors: Steven Joseph Berthel, Roland Joseph Billedeau, Christine E. Brotherton-Pleiss, Fariborz Firooznia, Stephen Deems Gabriel, Xiaochun Han, Ramona Hilgenkamp, Saul Jaime-Figueroa, Buelent Kocer, Francisco Javier Lopez-Tapia, Yan Lou, Lucja Orzechowski, Timothy D. Owens, Jenny Tan, Peter Michael Wovkulich
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Publication number: 20120028974Abstract: The present invention relates to a compound according to formula I, wherein R1, R2 and A are as defined herein, which exhibit PDE4 inhibitory activity and may be used in the treatment of inflammatory diseases or autoimmune diseases, in particular inflammatory or proliferative dermal diseases.Type: ApplicationFiled: December 18, 2009Publication date: February 2, 2012Applicant: LEO PHARMA A/SInventors: Simon Feldbaek Nielsen, Thomas Vifian, Anne Marie Horneman, Jesper Faergemann Lau
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Patent number: 8106054Abstract: A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections Methods of making and formulating crystalline compound (1) are provided.Type: GrantFiled: July 3, 2008Date of Patent: January 31, 2012Assignees: Gilead Sciences, Inc., K.U. Leuven Research & DevelopmentInventors: Eric D. Dowdy, Kenneth M. Kent, Norma J. Tom, Vahid Zia
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Publication number: 20120022074Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: ApplicationFiled: October 4, 2011Publication date: January 26, 2012Inventors: Dominik FEUERBACH, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Publication number: 20120022064Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases.Type: ApplicationFiled: February 5, 2010Publication date: January 26, 2012Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio Nakamura, Seiji Masuda, Aya Futamura
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Publication number: 20120010192Abstract: 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 R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Patent number: 8076340Abstract: The invention relates to compounds having general formula (I), wherein R is as defined herein. The invention also relates to acid addition salt, a hydrate or a solvate of compounds of formula (I). The invention further relates to the method of preparing said compounds and to the use of same in therapeutics.Type: GrantFiled: December 5, 2008Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Frederic Galli, Odile Leclerc, Alistair Lochead, Julien Vache
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Publication number: 20110301145Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: November 12, 2009Publication date: December 8, 2011Applicant: Gilead Connecticut INc.Inventors: Antonio J.M. Barbosa JR., Peter A. Blomgren, Kevin S. Currie, Seung Lee, Jeffrey Kropf, Scott A. Mithchell, Daniel Ortwine, William M. Rennells, Aaron C. Schmitt, Jianjun Xu, Wendy B. Young, Zhongdong Zhao, Pavel E. Zhichkin
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Publication number: 20110300103Abstract: Method for treating an HCV infection and inhibiting HCV replication with a compound of formula I wherein R1, R2, R3, R4, X1, X2, X3 and X4 and as defined hereinType: ApplicationFiled: August 18, 2011Publication date: December 8, 2011Applicant: Roche Palo Alto LLCInventors: Javier de Vicente Fidalgo, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas, Joshua Paul Gergely Taygerly
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Patent number: 8071595Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 24, 2009Date of Patent: December 6, 2011Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110281881Abstract: The present invention is concerned with substituted bicyclic heterocyclic compounds of Formula (I) wherein Het1, Het2, A1, A2, A3 and A4 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: February 2, 2010Publication date: November 17, 2011Inventors: Henricus, Jacobus, Maria Gijsen, Adriana Ingrid Velter, Gregor James MacDonald, Francois Paul Bischoff, Tongfei Wu, Sven, Franciscus, Anna Van Brandt, Michel Surkyn, Mirko Zaja, Serge, Maria, Aloysius Pieters, Didier Jean-Claude Berthelot, Michel, Anna, Josef De Cleyn, Daniel Oehlrich
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Publication number: 20110281869Abstract: The invention relates to novel tetrahydroisoquinoline derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including pharmaceutical compositions containing one or more of those compounds and their use as medicaments for the treatment or prevention of protozoal infections, such as especially malaria.Type: ApplicationFiled: May 18, 2009Publication date: November 17, 2011Inventors: Hamed Aissaoui, Christoph Boss, Olivier Corminboeuf, Marie-Celine Frantz
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Patent number: 8048885Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I) wherein the substituents are as defined in the specification and to processes for their production to pharmaceutical compositions comprising them and to their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and nemodegenerative disorders.Type: GrantFiled: March 26, 2010Date of Patent: November 1, 2011Assignee: Novartis AGInventors: Dominik Feuerbach, Mathias Frederiksen, Konstanze Hurth, Bernard Lucien Roy, Beatrix Wagner
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Publication number: 20110257169Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.Type: ApplicationFiled: May 19, 2011Publication date: October 20, 2011Applicant: NYCOMED GmbHInventor: Ulrich KAUTZ
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Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
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Publication number: 20110230458Abstract: The present invention provides phenyl-heteroaryl derivatives of Formula (I) and pharmaceutically acceptable salts thereof These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use of such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.Type: ApplicationFiled: February 15, 2011Publication date: September 22, 2011Applicant: TransTech Pharma, Inc.Inventors: Devi R. Gohimukkula, David Jones, Ghassan Qabaja, Jeff J. Zhu, Jeremy T. Cooper, William K. Banner, Kurt Sundermann, Muralidhar Bondlela, Mohan Rao, Pingzhen Wang, Raju B. Gowda, Robert C. Andrews, Suparna Gupta, Anitha Hari
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Publication number: 20110230457Abstract: The invention relates to substituted nitrogen containing bicyclic heterocycles of the formula (I) wherein Z is CH2 or N—R4 and X, R1, R2, R4, R6, R7 and n are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: ApplicationFiled: December 20, 2010Publication date: September 22, 2011Applicant: NOVARTIS AGInventors: Joerg BERGHAUSEN, Nicole BUSCHMANN, Pascal FURET, François GESSIER, Joanna HERGOVICH LISZTWAN, Philipp HOLTZER, Edgar JACOBY, Joerg KALLEN, Keiichi MASUYA, Carole PISSOT SOLDERMANN, Haixia REN, Stefan STUTZ
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Patent number: 8012968Abstract: This invention relates to new quinolone based compounds that exhibit prolyl hydroxylase inhibitory activity. This invention also relates to methods of increasing HIF levels or activity in a subject or treating a condition associated with HIF levels or activity in a subject by administering to the subject at least one quinolone based compound. This invention further involves assays for the detection of a hydroxyproline residue in a HIF molecule.Type: GrantFiled: February 10, 2010Date of Patent: September 6, 2011Assignee: Amgen Inc.Inventors: Jennifer R. Allen, Kaustav Biswas, Roland Burli, Jennifer Dao, Michael J. Frohn, Jennifer E. Golden, Randall W. Hungate, Robert Kurzeja, Stephanie J. Mercede, Kristine M. Muller, Susana C. Neira, Tanya A. N. Peterkin, Christopher M. Tegley, Violeta Yu
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Publication number: 20110212053Abstract: Provided are compounds according to Formula (I): or stereoisomer, prodrug, polymorph, or pharmaceutically acceptable salt forms thereof, wherein X, Y, R1, R6, R7, and R8 are as defined, and which compounds are effective inhibitors of PI3-kinase and/or other medically and clinically relevant kinases. Also provided are pharmaceutical compositions and methods of using the compounds and compositions as PI3-kinase and kinase inhibitors. More particularly, the compounds of the invention provide treatments and therapeutics for human diseases regulated by, or associated with, the activity of, PI3-kinases and/or protein kinases, or mutant or variant forms thereof.Type: ApplicationFiled: June 19, 2009Publication date: September 1, 2011Inventors: Dapeng QIAN, Amy Qi Han, Mark Hamilton, Eric Wang
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Publication number: 20110201615Abstract: Beta-carboline derivatives of structural formula (I) are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.Type: ApplicationFiled: October 19, 2009Publication date: August 18, 2011Inventors: Liangqin Guo, Jian Liu, Ravi P. Nargund, Alexander Pasternak, Lihu Yang, Zhixiong Ye
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Publication number: 20110190262Abstract: The present invention relates to compounds defined by formula I wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.Type: ApplicationFiled: November 14, 2008Publication date: August 4, 2011Applicant: Boehringer Ingelheim International GmbHInventors: Frank Himmelsbach, Matthias Eckhardt, Bradford S. Hamilton, Armin Heckel, Joerg Kley, Thorsten Lehmann-Lintz, Herbert Nar, Stefan Peters, Annette Schuler-Metz, Matthias Zentgraf
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Publication number: 20110190309Abstract: The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is a selected muscarinic receptor antagonist, and a second active ingredient which is a ?2-adrenoceptor agonist, or use in the treatment of respiratory diseases such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: May 12, 2009Publication date: August 4, 2011Inventors: Rhonan Ford, Andrew Mather, Antonio Mete, Katherine Wiley, Richard James Bull
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Publication number: 20110183976Abstract: 5- and 6-membered heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Also described is the treatment of neurological, neurodegenerative and psychiatric disorders including but not limited to those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 25, 2009Publication date: July 28, 2011Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20110172237Abstract: The invention provides named compounds of formula (I), wherein R4 is a N-substituted quinuclidine (I) pharmaceutical compositions containing them and a process for preparing the pharmaceutical compositions. Their use in therapy for’ the treatment of conditions mediated by M3 muscarinic receptors, such as chronic obstructive pulmonary disease is also disclosed.Type: ApplicationFiled: May 13, 2008Publication date: July 14, 2011Inventors: Richard James Bull, Elizabeth Anne Skidmore, Rhonan Lee Ford, Andrew Nigel Mather, Antonio Mete