Spiro Patents (Class 548/300.7)
-
Patent number: 10294219Abstract: The present invention relates to a novel Ledipasvir (LDV) crystal form and a preparation method thereof. Specifically, disclosed is an LDV solvate. The solvate is a solvate formed by LDV and a solvent A and/or a solvent B, wherein the solvent A is acetonitrile or acetone; and the solvent B is methyl tertiary butyl ether (MTBE). Also disclosed are a preparation method and an application of the solvate. The solvate has a high purity, a good crystallization property, and better optical stability. The preparation method is simple and the process is stable. The solvate can significantly improve quality control and industrial applications of LDV-containing drugs.Type: GrantFiled: June 24, 2016Date of Patent: May 21, 2019Assignee: SHANGHAI FOREFRONT PHARMACEUTICAL CO., LTD.Inventors: Wei Li, Yi Ren, Chengjun Huang, Yanyan Zhu, Shaojun Fu, Gang Fu, Zhewen Wei
-
Patent number: 10118912Abstract: An improved process is provided for the preparation of Ledipasvir and its pharmaceutically acceptable salts or solvates thereof, which is useful as an antiviral agent. This disclosure also provides a process for the preparation of key intermediates of Ledipasvir.Type: GrantFiled: June 29, 2016Date of Patent: November 6, 2018Assignee: Optimus Drugs Private Ltd.Inventors: Dnyandev Ragho Rane, Srinivas Reddy Desi Reddy, Subbareddy Peketi, Srinivas Rao Velivela
-
Patent number: 9765087Abstract: 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.Type: GrantFiled: April 4, 2014Date of Patent: September 19, 2017Assignee: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Hui Cao, Lu Ying, Xuri Gao, Bin Wang, Yat Sun Or
-
Patent number: 9718807Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.Type: GrantFiled: August 4, 2016Date of Patent: August 1, 2017Assignee: GILEAD PHARMASSET LLCInventors: Robert William Scott, Justin Philip Vitale, Kenneth Stanley Matthews, Martin Gerald Teresk, Alexandra Formella, Jared Wayne Evans
-
Patent number: 9150587Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: GrantFiled: August 28, 2014Date of Patent: October 6, 2015Assignee: Janssen Pharmaceuticals, Inc.Inventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton
-
Patent number: 9056860Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.Type: GrantFiled: March 13, 2013Date of Patent: June 16, 2015Assignee: Gilead Pharmasset LLCInventors: Robert William Scott, Justin Philip Vitale, Kenneth Stanley Matthews, Martin Gerald Teresk, Alexandra Formella, Jared Wayne Evans
-
Publication number: 20150141659Abstract: Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.Type: ApplicationFiled: January 20, 2015Publication date: May 21, 2015Inventors: Erik Mogalian, Robert William Scott, Bing Shi, Fang Wang
-
Patent number: 9035054Abstract: The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns Dinitroxide-type Biradical polarizing agents characterized by a rigid linkage between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.Type: GrantFiled: October 30, 2013Date of Patent: May 19, 2015Assignee: UNIVERSITE D'AIX-MARSEILLEInventors: Oliver Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
-
Publication number: 20150099730Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including those mediated by inhibition of fatty acid synthase (FASN) enzyme, such as, cancer, obesity or related discorders, and liver related disorders. Such compounds are represented by formula (I) as follows: wherein L1, a, b, m, n, R1, R2, R3, R4, and R5 are defined herein.Type: ApplicationFiled: September 6, 2013Publication date: April 9, 2015Applicant: Janssen Pharmaceutica, NVInventor: Peter J. Connolly
-
Patent number: 8969588Abstract: Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2 -[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl -propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.Type: GrantFiled: March 13, 2013Date of Patent: March 3, 2015Assignee: Gilead Pharmasset LLCInventors: Robert William Scott, Fang Wang, Bing Shi, Erik Mogalian
-
Publication number: 20150045551Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia.Type: ApplicationFiled: March 29, 2013Publication date: February 12, 2015Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Shuhei Kashiwa, Takeshi Kuwada, Youichi Shimazaki
-
Patent number: 8921573Abstract: The present invention relates to processes and intermediates for the preparation of novel benzimidazole derivatives, especially in the synthesis of hepatitis C virus NS5A inhibitors.Type: GrantFiled: April 16, 2014Date of Patent: December 30, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Datong Tang, Guoyou Xu, Xiaowen Peng, Lu Ying, Ce Wang, Hui Cao, Jiang Long, In Jong Kim, Guoqiang Wang, Yao-Ling Qiu, Yat Sun Or
-
Publication number: 20140371455Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton
-
Publication number: 20140364429Abstract: Provided are compounds antiviral compounds represented by formula Ia and Ib: that are highly potent as HCV NS5A inhibitors, where the structural variables are as defined herein. These compounds are useful in, for example, inhibiting Hepatitis C virus and treating Hepatitis C virus infections.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Applicant: AB PHARMA LTD.Inventor: Zheng-Yun James ZHAN
-
Publication number: 20140323458Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.Type: ApplicationFiled: July 10, 2014Publication date: October 30, 2014Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
-
Publication number: 20140316143Abstract: The present invention relates to processes and intermediates for the preparation of novel benzimidazole derivatives, especially in the synthesis of hepatitis C virus NS5A inhibitors.Type: ApplicationFiled: April 16, 2014Publication date: October 23, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Datong Tang, Guoyou Xu, Xiaowen Peng, Lu Ying, Ce Wang, Hui Cao, Jiang Long, In Jong Kim, Guoqiang Wang, Yao-Ling Qiu, Yat Sun Or
-
Patent number: 8853416Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: GrantFiled: June 12, 2013Date of Patent: October 7, 2014Assignee: Janssen Pharmaceuticals, Inc.Inventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton
-
Patent number: 8846023Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 9, 2013Date of Patent: September 30, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
-
Publication number: 20140288050Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as pain, neurological disorders, psychiatric disorders, and neuromuscular disorders. Compounds provided herein modulate the activity of opioid receptor (e.g., ?-opioid receptor) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: November 7, 2012Publication date: September 25, 2014Inventors: Scott Malcolm, Carrie Bowen, Laurence Melnick, Linghong Xie
-
Publication number: 20140275006Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTDInventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
-
Patent number: 8834749Abstract: Disclosed are a photosensitive resin composition including (A) a binder resin including a cardo-based resin including a repeating unit represented by the following Chemical Formula 1, (B) a photopolymerizable monomer, (C) a photopolymerization initiator, (D) a colorant and (E) a solvent, and a light blocking layer using the same. In the above Chemical Formula 1, each substituent is the same as defined in the detailed description.Type: GrantFiled: July 22, 2013Date of Patent: September 16, 2014Assignee: Cheil Industries Inc.Inventors: Hyun-Moo Choi, Chang-Min Lee, Ji-Hye Kim, Kyung-Won Ahn, A-Rum Yu, Jae-Bum Yim, Hwan-Sung Cheon, Ju-Ho Jung
-
Patent number: 8778938Abstract: 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.Type: GrantFiled: June 3, 2011Date of Patent: July 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
-
Patent number: 8765731Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: GrantFiled: November 16, 2012Date of Patent: July 1, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: James A. Henderson, John Maxwell, Louis Vaillancourt, Mark Morris, Ronald Grey, Jr., Simon Giroux, Laval Chan Chun Kong, Sanjoy Kumar Das, Bingan Liu, Carl Poisson, Caroline Cadilhac, Monica Bubenik, T. Jagadeeswar Reddy, Guy Falardeau, Constantin Yannopoulos, Jian Wang, Oswy Z. Pereira, Youssef L. Bennani, Albert C. Pierce, Govinda Rao Bhisetti, Kevin M. Cottrell, Valerie Marone
-
Publication number: 20140134193Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.Type: ApplicationFiled: October 31, 2013Publication date: May 15, 2014Applicant: PFIZER INC.Inventors: Chakrapani SUBRAMANYAM, Frank Erich KOEHN, Kenneth John DIRICO, Alessandra S. EUSTAQUIO, Michael Eric GREEN, Haiyin HE, Min HE, Christopher John O'DONNELL, Sujiet PUTHENVEETIL, Anokha RATNAYAKE, Jesse Alexander TESKE, Hui Yu YANG
-
Patent number: 8722695Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizophrenia, substance abuse disorders, sleep disorders or epilepsy.Type: GrantFiled: December 6, 2010Date of Patent: May 13, 2014Assignee: Autifony Therapeutics LimitedInventors: Giuseppe Alvaro, Anne Décor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
-
Patent number: 8674113Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions. A, L, M, W, R1, R2, R3, R4, R6, R7, R9, Ra, Rb have meanings given in the description.Type: GrantFiled: December 8, 2011Date of Patent: March 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Henning Priepke, Henri Doods, Alexander Heim-Riether, Raimund Kuelzer, Roland Pfau, Klaus Rudolf, Dirk Stenkamp
-
Publication number: 20140058114Abstract: Process for preparing cis-alkoxy-substituted spirocyclic 1-H-pyrrolidine-2,4-dione derivatives and alkali metal salts and alkaline earth metal salts thereof.Type: ApplicationFiled: March 6, 2012Publication date: February 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Albert Schatterer, Thomas Himmler, Reiner Fischer
-
Publication number: 20140051656Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 31, 2013Publication date: February 20, 2014Applicant: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard L. Mackman, Hyung-Jung Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
-
Patent number: 8648193Abstract: The present invention relates to the field of organic chemistry and in particular to organic free radicals used as polarizing agents in the technique of Dynamic Nuclear Polarization (DNP), which involves transferring the polarization of electron spins to the nuclei of a compound whose Nuclear Magnetic Resonance (NMR) is being observed. It concerns dinitroxide-type biradical polarizing agents characterized by a rigid linkage between the nitroxide units that enables optimal orientation and distance to be maintained between the aminoxyl groups of said nitroxide units. This particular structure enables, at low temperatures and high fields, optimal transfer of polarization and optimal enhancement of NMR/MAS signals of the polarized nuclei of the compound studied.Type: GrantFiled: May 29, 2009Date of Patent: February 11, 2014Assignee: Universite d'Aix MarseilleInventors: Olivier Ouari, Hakim Karoui, Francois Le Moigne, Paul Tordo, Robert G. Griffin, Yoh Matsuki, Thorsten Maly
-
Publication number: 20140038954Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I, wherein variables A1, A3, A4, A5, A6, A8, R2, R7, X, Y and Z of Formula I are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to plaque formation and deposition, resulting from the activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits and impairments, schizophrenia and other central nervous system conditions and disorders. The invention further provides compounds of Formulas II and III, and of sub-formulas of Formulas I, II and III, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.Type: ApplicationFiled: February 13, 2012Publication date: February 6, 2014Applicant: AMGEN INC.Inventors: Oleg Epstein, Ryan White, Vinod F. Patel, Jason Human
-
Publication number: 20140018313Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 16, 2011Publication date: January 16, 2014Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
-
Publication number: 20140017195Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 9, 2013Publication date: January 16, 2014Inventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavole, Omar D. Lopez, Alain Martel, Nicolas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
-
Publication number: 20140005164Abstract: The present invention relates to novel compounds of formula (I): as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: ApplicationFiled: March 23, 2012Publication date: January 2, 2014Applicant: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Massimiliano Travagli, Giacomo Minetto, Lucia Cesari, Simone Galeazzi, Andrea Caricasole, Antonio Chiumiento, Massimiliano Salerno
-
Patent number: 8609859Abstract: A one pot process for the synthesis of Irbesartan comprising reacting 2-n-Butyl-1,3-Diazaspiro[4,4]Non-1-en-4-one (Formula III) and Bromomethyl Cyanobiphenyl (Formula IV) in the presence of base and water with the optional use of PTC to give formula II from which Irbesartan is obtained by reacting with sodium azide and triethylamine hydrochloride in the presence of a non polar solvent.Type: GrantFiled: November 19, 2009Date of Patent: December 17, 2013Assignee: CTX Life Sciences Pvt. Ltd.Inventors: Prakash Yashwant Kolhe, Rajesh Dilip Joshi, Bimal Kumar Srivastava, Nitin Jerambhai Patel, Sanket Sureshbhai Gajjar
-
Publication number: 20130324740Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.Type: ApplicationFiled: March 13, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Robert William Scott, Justin Philip Vitale, Kenneth Stanley Matthews, Martin Gerald Teresk, Alexandra Formella, Jared Wayne Evans
-
Patent number: 8574563Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 11, 2012Date of Patent: November 5, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
-
Patent number: 8569312Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, 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 conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: GrantFiled: April 4, 2013Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Anandan Palani, Michael Y. Berlin, Robert G. Aslanian
-
Patent number: 8563714Abstract: The present invention relates to bridged spiro[2.4]heptane derivatives of formula (I), wherein W, Y, Z, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds as ALX receptor and/or FPRL2 agonists for the treatment of inflammatory and obstructive airways diseases.Type: GrantFiled: May 17, 2010Date of Patent: October 22, 2013Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
-
Patent number: 8541595Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.Type: GrantFiled: November 3, 2009Date of Patent: September 24, 2013Assignee: Merch Sharp & Dohme Corp.Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
-
Patent number: 8492554Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: GrantFiled: November 15, 2012Date of Patent: July 23, 2013Assignee: GlaxoSmithKline LLCInventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Richard Martin Grimes, Wieslaw Mieczyslaw Kazmierski, Beth Adams Norton, Matthew Tallant
-
Publication number: 20130183269Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: January 7, 2013Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
-
Publication number: 20130157997Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein A, B, B?, X, Y, R1, R1?, R2, R2?, R3, R3?, R5, R5?, R6, m, n, or p are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: November 16, 2012Publication date: June 20, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
-
Publication number: 20130137877Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: July 19, 2012Publication date: May 30, 2013Applicant: Gilead Sciences, Inc.Inventors: Hongyan Guo, Darryl Kato, Thorsten A. Kirschberg, Hongtao Liu, John O. Link, Michael L. Mitchell, Jay P. Parrish, Jianyu Sun, James Taylor, Elizabeth M. Bacon, Eda Canales, Aesop Cho, Choung U. Kim, Jeromy J. Cottell, Manoj C. Desai, Randall L. Halcomb, Michael Graupe, Evan S. Krygowski, Scott E. Lazerwith, Qi Liu, Richard Mackman, Hyung-Jun Pyun, Joseph H. Saugier, James D. Trenkle, Winston C. Tse, Randall W. Vivian, Scott D. Schroeder, William J. Watkins, Lianhong Xu
-
Publication number: 20130121957Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: May 7, 2012Publication date: May 16, 2013Inventors: Qi Chen, Omar D. Lopez, John A. Bender, Gan Wang, Van N. Nguyen, John F. Kadow, Nicholas A. Meanwell, Makonen Belema
-
Publication number: 20130102604Abstract: The present invention relates to a compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 have the significance given in claim 1. The compound may be used, for example, for the treatment or prophylaxis of obesity, hyperglycemia, dyslipidemia, and type 1 or type 2 diabetes.Type: ApplicationFiled: December 10, 2012Publication date: April 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
-
Publication number: 20130072690Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: ApplicationFiled: November 15, 2012Publication date: March 21, 2013Applicant: GLAXOSMITHKLINE LLCInventor: GLAXOSMITHKLINE LLC
-
Patent number: 8361959Abstract: The present invention relates to compounds of the general formula: (I) wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: GrantFiled: September 30, 2009Date of Patent: January 29, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Andrew Stamford, Michael W. Miller, Duane Eugene DeMong, William J. Greenlee, Joseph A. Kozlowski, Brian J. Lavey, Michael K. C. Wong, Wensheng Yu, Xing Dai, De-Yi Yang, Guowei Zhou
-
Publication number: 20130012434Abstract: The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.Type: ApplicationFiled: March 22, 2011Publication date: January 10, 2013Inventors: Michael K. Wong, Brian J. Lavey, Wensheng Yu, Joseph A. Kozlowski, Duanc E. DeMong, Xing Dai, Andrew W. Stamford, Michael W. Miller, Guowei Zhou, De-Yi Yang, William J. Greenlee
-
Publication number: 20130004457Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Inventors: Carol Bachand, Makonen Bekema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
-
Patent number: 8344155Abstract: Disclosed are compounds of Formula III. Also disclosed are salts of the compounds, pharmaceutical composition comprising the compounds or salts, and methods for treating HCV infection by administration of the compounds or salts.Type: GrantFiled: August 26, 2010Date of Patent: January 1, 2013Assignee: GlaxoSmith Kline LLCInventors: Pingyun Chen, Ricky Couch, Maosheng Duan, Beth Adams Norton