Ring Nitrogen In The Polycyclo Ring System Patents (Class 546/200)
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Publication number: 20120058996Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, are useful as kinase modulators, including Btk modulation.Type: ApplicationFiled: November 9, 2011Publication date: March 8, 2012Inventors: Qingjie Liu, Douglas G. Batt, George V. DeLucca, Qing Shi, Andrew J. Tebben
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Publication number: 20120053159Abstract: Provided herein are lenalidomide, which is enriched with isotopes such as deuterium. Pharmaceutical compositions comprising the isotopes-enriched compounds, and methods of using such compounds are also provided.Type: ApplicationFiled: February 9, 2010Publication date: March 1, 2012Inventors: George W. Muller, Hon-Wah Man
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Patent number: 8124606Abstract: Disclosed are compounds of the following formula: in which R1, R2, R5, R6, R7, R11, X, and m are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: March 4, 2011Date of Patent: February 28, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20120046316Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: ApplicationFiled: October 3, 2011Publication date: February 23, 2012Applicant: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Publication number: 20120039804Abstract: The compounds of the invention are modulators of cannabinoid receptors CB1 or CB2. The compounds can be used for the prevention or treatment of, e.g., pain, cancer, skin diseases, weight-associated disorders, chemical addictions, psychiatric disorders, neurodegenerative disorders, bone diseases, and inflammatory diseases. The compounds of the invention can further be used to study these diseases and disorders, as well as cannabinoid receptor biology, by coupling the compounds to, e.g., imaging agents.Type: ApplicationFiled: June 6, 2011Publication date: February 16, 2012Inventors: Philippe Diaz, Fanny Diaz, Ravil Rashitovich Petrov
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Publication number: 20120029020Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: ApplicationFiled: September 22, 2011Publication date: February 2, 2012Applicant: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Publication number: 20120022106Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: ApplicationFiled: September 22, 2011Publication date: January 26, 2012Applicant: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Publication number: 20120020884Abstract: An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Harry John Wadsworth, Bo Shan, Dennis O'shea, Joanna Marie Passmore, William John Trigg, Amanda Ewan
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Patent number: 8093391Abstract: This invention relates to an improved and scalable process for the preparation of substantially pure palonosetron and its acid addition salts, in particular hydrochloride (I) which comprises of, (a) converting intermediate (IIa) as such or as its freebase (II) to a crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) via hydrogenation under pressure with an appropriately chosen hydrogenation catalyst in an suitable organic solvent. (b) making the resulting crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) substantially free from (II) or (IIa) via halogenation reaction.Type: GrantFiled: January 5, 2010Date of Patent: January 10, 2012Assignee: Sterling Biotech Research CenterInventors: Sugata Chatterjee, Ajay Singh Rawat, Anil V. Pawar, Jetti Rajanikanth, Penigandla Venkateswarlu
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Publication number: 20110311483Abstract: Compounds of Formulae I-1 to I-9 are disclosed, which are modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders.Type: ApplicationFiled: March 29, 2011Publication date: December 22, 2011Applicant: IRONWOOD PHARMACEUTICALS, INC.Inventors: James JIA, Regina GRAUL, Bo PENG, Colleen HUDSON, Joel MOORE, Ara MERMERIAN
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Patent number: 8080566Abstract: The present invention relates to carbazole compounds, pharmaceutical compositions comprising them, and methods which may be useful as inhibitors of H1R and/or H4R for the treatment or prevention of inflammatory, autoimmune, allergic, and ocular diseases.Type: GrantFiled: June 11, 2009Date of Patent: December 20, 2011Assignee: Kalypsys, IncInventors: Mehmet Kahraman, Allen J. Borchardt, Robert L. Davis, Stewart A. Noble, James W. Malecha
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Publication number: 20110305661Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.Type: ApplicationFiled: October 5, 2009Publication date: December 15, 2011Inventors: John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
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Publication number: 20110288127Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: ApplicationFiled: May 26, 2011Publication date: November 24, 2011Applicant: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Publication number: 20110281870Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 24, 2011Publication date: November 17, 2011Applicant: ABBOTT LABORATORIESInventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
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Publication number: 20110280808Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 18, 2011Publication date: November 17, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Patent number: 8058443Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: December 15, 2008Date of Patent: November 15, 2011Assignee: Celgene CorporationInventors: Manohar T. Saindane, Louise M. Cameron
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Publication number: 20110263649Abstract: The present invention relates to a novel crystalline form of lenalidomide having formula (I) and chemically known as 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione. The present invention further relates to a process for the preparation of said novel form and its use in pharmaceutical preparations for the treatment of autoimmune disease, inflammation, inflammatory disease and diseases such as cancer, in particular the management of multiple myeloma.Type: ApplicationFiled: November 2, 2009Publication date: October 27, 2011Applicant: GENERICS [UK] LIMITEDInventors: Priyanka Bhosale, Vinayak Gore, Ashok Pehere, Vinay Shukla
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Publication number: 20110224440Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.Type: ApplicationFiled: May 27, 2011Publication date: September 15, 2011Inventors: Chuansheng Ge, George W. Muller, Roger Chen, Manohar Tukaram Saindane
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Patent number: 8012997Abstract: The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-? in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.Type: GrantFiled: July 23, 2009Date of Patent: September 6, 2011Assignee: Celgene CorporationInventors: Michael J. Robarge, Roger Shen-Chu Chen, George W. Muller, Hon-Wah Man
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Patent number: 8008298Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables Q1, R, and X are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: February 20, 2009Date of Patent: August 30, 2011Assignee: Roche Palo AltoInventors: Joe Timothy Bamberg, Daisy Joe DuBois, Todd Richard Elworthy, Robert Than Hendricks, Johannes Cornelius Hermann, Alam Jahangir, Rama K. Kondru, Remy Lemoine, Yan Lou, Timothy D. Owens, David Bernard Smith, Michael Soth, Hanbiao Yang
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Patent number: 8008327Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 23, 2009Date of Patent: August 30, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Darren DiSalvo, Daniel Kuzmich, Can Mao, Hossein Razavi, Christopher Ronald Sarko, Alan David Swinamer, David Smith Thomson, Qiang Zhang
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Patent number: 8008326Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.Type: GrantFiled: July 21, 2005Date of Patent: August 30, 2011Assignee: Richter Gedeon Vegyeszeti Gyar Rt.Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
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Patent number: 8008299Abstract: This invention is directed to a compound of Formula (I): and forms thereof, wherein A, B, E, G, X and L2 are as defined herein and their use as urotensin II receptor antagonists.Type: GrantFiled: June 5, 2008Date of Patent: August 30, 2011Assignee: Janssen Pharmaceutica, N.V.Inventors: William A. Kinney, Edward C. Lawson, Shyamali Ghosh, Diane K. Luci, David F. McComsey
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Publication number: 20110207719Abstract: A series of novel anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, wherein said application includes a pharmaceutical composition containing said derivatives for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.Type: ApplicationFiled: February 25, 2010Publication date: August 25, 2011Inventor: Hsu-Shan HUANG
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Patent number: 8003664Abstract: The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 23, 2010Date of Patent: August 23, 2011Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Roland Gendron, Adam A. Goldblum, Daniel D. Long, Daniel Marquess, S. Derek Turner, Seok-Ki Choi
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Publication number: 20110172270Abstract: 1,4-disubstituted piperidine compounds of general formula (I) wherein the substituents are defined in claim 1 that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: ApplicationFiled: January 6, 2011Publication date: July 14, 2011Applicant: LABORATORIOS DEL DR. ESTEVE S.AInventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
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Patent number: 7977357Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: July 23, 2008Date of Patent: July 12, 2011Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
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Publication number: 20110166155Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: ApplicationFiled: January 6, 2011Publication date: July 7, 2011Inventors: Bradford VAN WAGENEN, Radhakrishnan UKKIRAMAPANDIAN, Joshua CLAYTON, Ian EGLE, James R. EMPFIELD, Methvin ISAAC, Fupeng MA, Abdelmalik SLASSI, Gary STEELMAN, Rebecca URBANEK, Sally WALSH
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Publication number: 20110160180Abstract: Compounds of Formulae (I), or pharmaceutically acceptable salts thereof: wherein R1, R2 and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: August 15, 2008Publication date: June 30, 2011Applicant: ASTRAZENECA ABInventors: Sara Beha, William Brown, Shawn Johnstone, Ziping Liu, Daniel Pagé, Miroslaw Tomaszewski, Zhong-yong Wei, Shi Yi Yue
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Patent number: 7956082Abstract: The present invention creates an indole derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the generic formula (I) wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a 3- to 8-membered nitrogen-containing non-aromatic heterocyclic ring etc.; R1, R2, R3, R4 and R5 are independently a hydrogen atom or a halogen atom etc.; R6 is C2-C4 alkyloxy etc.; R7 is independently a halogen atom etc.; R8 is independently C1-C4 alkyl etc.; R9 is carboxy etc.; Y is a single bond etc.; M is sulfonyl etc.; L1, L2 and L3 are a single bond or alkylene optionally containing one or two heteroatoms etc.; n is 0 etc.; q is 0 etc.; a pharmaceutically acceptable salt or hydrate thereof.Type: GrantFiled: July 20, 2006Date of Patent: June 7, 2011Assignee: Shionogi & Co., LtdInventors: Akira Kugimiya, Michitaka Shichijo, Yoshiharu Hiramatsu, Natsuki Ishizuka
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Publication number: 20110086836Abstract: 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: ApplicationFiled: April 5, 2007Publication date: April 14, 2011Applicant: Santhera Pharmaceuticals (Schweiz) AGInventors: Michael Soeberdt, Holger Deppe, Philipp Weyermann, Stephan Bulat, Andreas Von Sprecher, Achim Feurer, Cyrille Lescop, Marco Hennebohle, Sonja Nordhoff
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Patent number: 7915260Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: GrantFiled: January 10, 2007Date of Patent: March 29, 2011Inventors: Bruce E. Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20110065750Abstract: The present invention provides for new crystalline and amorphous forms of 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione, and methods of making the same.Type: ApplicationFiled: September 17, 2010Publication date: March 17, 2011Applicant: ScinoPharm Taiwan Ltd.Inventors: Chen-Tung CHEN, Inze Lin
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Publication number: 20110064698Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The present invention relates to novel antiviral compounds represented herein above, pharmaceutical compositions comprising such compounds, and methods for the treatment or prophylaxis of viral (particularly HCV) infection in a subject in need of such therapy with said compounds.Type: ApplicationFiled: September 10, 2010Publication date: March 17, 2011Inventors: Yat Sun Or, Xiaowen Peng, Ce Wang, Lu Ying, Yao-Ling Qiu
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Patent number: 7893066Abstract: The present invention discloses pyrido[2,3-B]pyrazinones having the structure of Formula I for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.Type: GrantFiled: April 9, 2008Date of Patent: February 22, 2011Assignee: Gilead Palo Alto, Inc.Inventors: Dmitry Koltun, Jeff Zablocki, Eric Parkhill, Andrei Glushkov, Natalya Vasilevich, Timur Zilbershtein, Alexey Ivanov, Jeffrey Chisholm
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Patent number: 7888510Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.Type: GrantFiled: July 29, 2004Date of Patent: February 15, 2011Assignee: Laboratorios del Dr. Esteve S.A.Inventors: Antoni Jover Torrens, Josep Mas Prio, Alberto Dordal Zueras, Maria Angeles Fisas Escasany, Helmut-Heinrich Buschmann
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Publication number: 20110034512Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: April 23, 2009Publication date: February 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Darren Disalvo, Daniel Kuzmich, Can Mao, Hossein Razavi, Christopher Sarko, Alan David Swinamer, David Smith Thomson, Qiang Zhang
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Publication number: 20110034440Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.Type: ApplicationFiled: April 10, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
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Publication number: 20110021567Abstract: Processes for the preparation of substantially pure lenalidomide. The application also relates to an enriched, substantially pure, and pure amorphous form of lenalidomide and solid dispersions containing amorphous lenalidomide.Type: ApplicationFiled: March 11, 2009Publication date: January 27, 2011Applicants: DR. REDDY'S LABORATORIES LTD., DR. REDDY'S LABORATORIES, INC.Inventors: Surya Narayana Devarakonda, Sesha Reddy Yarraguntla, Vamsi Krishna Mudapaka, Rajasekhar Kadaboina, Veerender Murki, Amarendhar Manda, Venkata Rao Badisa, Naresh Vemula, Rama Seshagiri Rao Pulla, Venu Nalivela
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Patent number: 7875621Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions containing compounds of formula (I) wherein R1, R3, L, X, Y and Z have defined meanings.Type: GrantFiled: June 28, 2005Date of Patent: January 25, 2011Assignee: Janssen Pharmaceutica NVInventors: Marcel Jozef Maria Van Der Aa, Albertus Henricus Maria Theresia Van Heertum, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijin Leopold Wouters
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Publication number: 20110015228Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: ApplicationFiled: September 27, 2010Publication date: January 20, 2011Inventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller, Manohar T. Saindane, Louise M. Cameron
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Publication number: 20100324017Abstract: An object of the present invention is to provide a novel and excellent agent for treating or preventing dementia, schizophrenia and the like, based on the 5-HT5A receptor modulating action. It was confirmed that a compound characterized by a structure that a tricyclic hetero ring having a pyrrole ring at the center and guanidine are bonded via a carbonyl group has a potent 5-HT5A receptor modulating action and an excellent pharmacological action based thereon, and thus, it was found that the compound can be an excellent agent for treating or preventing dementia, schizophrenia, bipolar disorder, or attention deficit hyperactivity disorder, particularly for memory-related functional disorders such as cognitive impairments including dementia and schizophrenia, thereby completing the present invention.Type: ApplicationFiled: February 6, 2008Publication date: December 23, 2010Inventors: Isao Kinoyama, Satoshi Miyamoto, Hiroaki Hoshii, Takehiro Miyazaki, Mayako Yamazaki
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Patent number: 7855217Abstract: Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed.Type: GrantFiled: December 15, 2008Date of Patent: December 21, 2010Assignee: Celgene CorporationInventors: Markian S. Jaworsky, Roger Shen-Chu Chen, George W. Muller
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Publication number: 20100311747Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.Type: ApplicationFiled: May 20, 2008Publication date: December 9, 2010Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lu, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
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Publication number: 20100311745Abstract: Novel 1,3-dihydroisoindole derivatives of the formula (I), in which R1-R3 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: July 28, 2008Publication date: December 9, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Hans Michael Eggenweiler, Christian Sirrenberg, Hans Peter Buchstaller
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Patent number: 7842704Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: December 11, 2007Date of Patent: November 30, 2010Assignee: Theravance, Inc.Inventors: Mathai Mammen, Sarah Dunham
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Patent number: 7842808Abstract: The present invention relates to compounds of Formula (I) as antagonists of calcitonin gene-related peptide receptors (“CGRP-receptor”), pharmaceutical compositions comprising them, methods for identifying them, methods of treatment using them and their use in therapy for treatment of neurogenic vasodilation, neurogenic inflammation, migraine and other headaches, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), and other conditions the treatment of which can be effected by the antagonism of CGRP-receptors.Type: GrantFiled: January 5, 2007Date of Patent: November 30, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Prasad V. Chaturvedula, Ling Chen, Rita Civiello, Andrew P. Degnan, Gene M. Dubowchik, Xiaojun Han, Xiang Jun J. Jiang, Guanglin Luo, John E. Macor, Graham S. Poindexter, George O. Tora
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Publication number: 20100292215Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: March 27, 2007Publication date: November 18, 2010Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
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Publication number: 20100292219Abstract: The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R1-R12 in Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.Type: ApplicationFiled: February 26, 2008Publication date: November 18, 2010Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Atul Agarwal, Xiangzhu Wang, Dawei Chen, Suoming Zhang, Avinash Phadke
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Patent number: 7829712Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I) where x, y, G, J, K, L, M, Q, W, V, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: GrantFiled: September 20, 2005Date of Patent: November 9, 2010Assignee: Xenon Pharmaceuticals Inc.Inventors: Rajender Kamboj, Zaihui Zhang, Jianmin Fu, Serguei Sviridov, Sultan Chowdhury, Vishnumurthy Kodumuru