The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/368)
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Publication number: 20140179922Abstract: The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.Type: ApplicationFiled: June 13, 2012Publication date: June 26, 2014Applicant: MAPI PHARMA LTD.Inventors: Ehud Marom, Michael Mizhiritskii, Susanna Tchilibon, Shai Rubnov
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Publication number: 20140171442Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.Type: ApplicationFiled: July 31, 2012Publication date: June 19, 2014Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
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Patent number: 8741892Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: November 30, 2012Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf, Bernd Wellenzohn
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Publication number: 20140142114Abstract: The present invention relates to novel anthelmintic compounds of formula (I) below: wherein Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X1, X2, X3, X4, X5, X6, X7 and X8 are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.Type: ApplicationFiled: November 19, 2013Publication date: May 22, 2014Applicant: Merial LimitedInventors: Charles Q. Meng, Alan Long, Scot Huber, Srinivas Reddy Gurrala, Douglas Edward Wilkinson, Gregory Pacofsky
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Patent number: 8729085Abstract: A preparation for oral administration comprising: a pregelatinized starch comprising N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]-(2R,3R)-2,3-tetramethylene-butyl]-(1?R,2?S,3?R,4?S)-2,3-bicyclo[2,2,1]-heptanedicarboxyimide hydrochloride (lurasidone) represented by the formula (1) as an active ingredient; a water-soluble excipient; and a water-soluble polymeric binder, the preparation exhibiting an invariant level of elution behavior even when the content of its active ingredient is varied.Type: GrantFiled: May 26, 2006Date of Patent: May 20, 2014Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventor: Kazuyuki Fujihara
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Patent number: 8716277Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: May 6, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Klaus Rudolf, Daniel Bischoff, Georg Dahmann, Matthias Grauert, Raimund Kuelzer, Bernd Wellenzohn
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Publication number: 20140113911Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases.Type: ApplicationFiled: April 6, 2012Publication date: April 24, 2014Applicant: NHWA PHARMA CORPORATIONInventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xin Liu, Song Zhao, Shicheng Liu, Minquan Yu, Heng Zhang, Xinghua Liu
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Publication number: 20140107129Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: December 11, 2013Publication date: April 17, 2014Applicant: Galderma Research & DevelopmentInventors: Laurence CLARY, Sandrine CHAMBON, Laurent CHANTALAT, Carine ROSIGNOLI, Olivier ROYE, Jean-Claude PASCAL, Marlene SCHUPPLI-NOLLET
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Patent number: 8691805Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: May 1, 2013Date of Patent: April 8, 2014Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Patent number: 8680090Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: GrantFiled: July 8, 2013Date of Patent: March 25, 2014Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Patent number: 8673920Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: April 27, 2010Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
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Patent number: 8653069Abstract: The present invention discloses an aralkyl substituted piperidine or piperazine derivative and the use of the derivative in preparation of medicaments for treating schizophrenia and correlative psychoneuroses. It is shown by pharmacological tests that the derivative of the present invention has better antischizophrenic effect and less toxicity. Said derivative is a free base or salt of the compound having the following general formula.Type: GrantFiled: July 28, 2008Date of Patent: February 18, 2014Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.Inventors: Jianqi Li, Shaoping Peng, Wangping Cai, Kai Gao
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Publication number: 20140039190Abstract: Compounds of general formula A useful as potential anticancer agents against human cancer cell lines and a process for the preparation thereof.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Inventors: Ahmed Kamal, Adla Mallareddy, Paidakula Suresh, Rajesh V., C., R., N., C. Shetti, Harish Chandra Pal, Ajit Kumar Saxena
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Publication number: 20140031548Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.Type: ApplicationFiled: September 30, 2013Publication date: January 30, 2014Inventors: Nobuyuki AE, Yuji Fujiwara
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Patent number: 8637498Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (Ia) and Formula (Ib) as follows: wherein Y, Z, and n are defined herein; and wherein Yb and Zb are as defined herein.Type: GrantFiled: September 27, 2011Date of Patent: January 28, 2014Assignee: Janssen Pharmaceutica, NVInventors: Peter J. Connolly, Mark J. Macielag, Mark E. McDonnell, Bin Zhu
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Publication number: 20140024656Abstract: The present invention belongs to the medicinal chemistry field, and specifically discloses a [1,3,4]oxadiazole derivative with the structure of general formula (I) and pharmaceutically acceptable salt thereof. The compound can be used to prepare a medicine for preventing or treating a disease of the central nervous system.Type: ApplicationFiled: April 1, 2012Publication date: January 23, 2014Applicant: HUAZHONG UNIVERSITY OF SCIENCE & TECHNOLOGY NHWA PHARMA CORPORATIONInventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xiaojun Feng, Song Zhao, Shicheng Liu, Minquan Yu, Yu Lan, Yinli Qiu
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Patent number: 8633196Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 22, 2013Date of Patent: January 21, 2014Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marlène Schuppli-Nollet
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Publication number: 20140011799Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 8, 2013Publication date: January 9, 2014Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Patent number: 8614318Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: GrantFiled: July 24, 2006Date of Patent: December 24, 2013Assignee: AbbVie Inc.Inventors: Milan Bruncko, Hong Ding, Steven Elmore, Aaron Kunzer, Christopher L. Lynch, William McClellan, Cheol-Min Park, Andrew Petros, Xiaohong Song, Xilu Wang, Noah Tu, Michael Wendt, Alexander R. Shoemaker, Michael J. Mitten
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Patent number: 8604037Abstract: A compound of formula: wherein Ar1, A, R3, x, and m are as disclosed herein and Ar2 is a benzothiazolyl, benzooxazolyl, or benzoimidazolyl group or a pharmaceutically acceptable salt thereof (a “Benzoazolylpiperazine Compound”), compositions comprising a Benzoazolylpiperazine Compound, and methods for treating or preventing pain, UI, an ulcer, IBD, IBS, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, stroke, a seizure, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia, or depression in an animal comprising administering to an animal in need thereof an effective amount of a Benzoazolylpiperazine Compound are disclosed.Type: GrantFiled: August 18, 2011Date of Patent: December 10, 2013Assignee: Purdue Pharma, L.P.Inventors: Qun Sun, Laykea Tafesse, Sam Victory
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Patent number: 8586737Abstract: The present invention relates to a novel process for preparing quaternary ammonium salt derivatives.Type: GrantFiled: April 26, 2011Date of Patent: November 19, 2013Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Nobuyuki AE, Yuji Fujiwara
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Publication number: 20130296335Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: March 29, 2013Publication date: November 7, 2013Inventors: Bradley P. MORGAN, Erica A. KRAYNACK, Pu-Ping LU, Alex MUCI, David J. MORGANS
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Publication number: 20130289277Abstract: The present invention relates to a medicament comprising lurasidone or a pharmaceutically acceptable acid addition salt thereof for treating pervasive developmental disorders and a method of the treatment thereof.Type: ApplicationFiled: March 14, 2013Publication date: October 31, 2013Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventor: Tsuyoshi TSUJIMURA
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Patent number: 8557810Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: January 24, 2012Date of Patent: October 15, 2013Assignee: Ambit Biosciences CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Patent number: 8552001Abstract: Sulfoxide derivatives of the formula Ia to Im as described, and pharmaceutically usable salts, solvates, enantiomers, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for the treatment of tumors.Type: GrantFiled: September 14, 2010Date of Patent: October 8, 2013Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Publication number: 20130252953Abstract: The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.Type: ApplicationFiled: November 29, 2011Publication date: September 26, 2013Inventors: Zee-Fen Chang, Jim-Min Fang, Chun-Mei Hu, Ming-Tyng Yeh
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Publication number: 20130245022Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
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Publication number: 20130217680Abstract: This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 24, 2011Publication date: August 22, 2013Inventors: Alexander Pasternak, Reynalda K. deJesus, Yuping Zhu, Lihu Yang, Shawn Walsh, Haifeng Tang, Dooseop Kim, Barbara Pio, Aurash Shahripour, Kevin Belyk
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Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Publication number: 20130184278Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.Type: ApplicationFiled: November 20, 2012Publication date: July 18, 2013Applicant: Abbott LaboratoriesInventor: Abbott Laboratories
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Publication number: 20130183753Abstract: The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: KYOTO UNIVERSITYInventor: Kyoto University
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Publication number: 20130178481Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.Type: ApplicationFiled: March 4, 2013Publication date: July 11, 2013Inventors: Mark T Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Patent number: 8481547Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: July 9, 2013Assignee: Janssen Pharmaceutica NVInventors: Alfonzo D. Jordan, Renee L. DesJarlais, Dennis J. Hlasta, Michael H. Parker, Carsten Schubert, Kimberly White
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Publication number: 20130172364Abstract: Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis.Type: ApplicationFiled: September 29, 2011Publication date: July 4, 2013Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Eliezer Falb, Jeffrey Sterling, Yaacov Herzig, Raphael Nudelman, Konstantin Ulanenko
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Publication number: 20130172363Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Galderma Research & Development
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Publication number: 20130158042Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Annekatrin HEIMANN, Georg DAHMANN, Marc GRUNDL, Stephan Georg MUELLER, Bernd WELLENZOHN
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Publication number: 20130158002Abstract: The present invention is directed to 5-substituted 1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxide and 1,3-dihydro[1,2,5]thiadiazolo[3,4-b]pyridine 2,2,-dioxide derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: February 28, 2011Publication date: June 20, 2013Inventors: Mark E. Layton, Michael J. Kelly, Timothy J. Hartingh
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Publication number: 20130158011Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130143870Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: November 30, 2012Publication date: June 6, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Patent number: 8455476Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: June 4, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130137679Abstract: The present invention relates to novel functionally selective ligands of dopamine D2 receptors, FIG. 1 including agonists, antagonists, and inverse agonists. The invention further relates to the use of these compounds for treating central nervous system disorders related to D2 receptors.Type: ApplicationFiled: July 1, 2011Publication date: May 30, 2013Inventors: Jian Jin, Bryan Roth, Stephen Frye
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Patent number: 8445477Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica, NVInventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20130123239Abstract: The invention relates to compounds of Formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: June 22, 2011Publication date: May 16, 2013Inventor: Noriyuki Kurose
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Patent number: 8435977Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, W and are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica, NVInventors: Chris Flores, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang
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Publication number: 20130096089Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: September 7, 2012Publication date: April 18, 2013Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Patent number: 8420632Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: June 28, 2010Date of Patent: April 16, 2013Assignee: Galderma Research & DeveloplmentInventors: Laurence Clary, Sandrine Chambon, Laurent Chantalat, Carine Rosignoli, Olivier Roye, Jean-Claude Pascal, Marléne Schuppli
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Patent number: 8415341Abstract: Disclosed are compounds, compositions and methods for treating diseases, syndromes, conditions and disorders that are affected by the inhibition of MGL, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, r, R2 and Z are defined herein.Type: GrantFiled: April 22, 2010Date of Patent: April 9, 2013Assignee: Janssen Pharmaceutica, NVInventors: Kristen Chevalier, Jose Clemente, Scott Dax, Chris Flores, Li Liu, Mark Macielag, Mark McDonnell, Marina Nelen, Erica Nulton, Stephen Prouty, Matthew Todd, Sui-Po Zhang, Bin Zhu
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Patent number: 8410111Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.Type: GrantFiled: August 21, 2012Date of Patent: April 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Patent number: 8410268Abstract: The present invention relates to a process for preparing Ziprasidone of formula I, or a pharmaceutically acceptable salt or a solvate or a hydrate thereof; comprising the steps of reacting 1-(1,2-benzisothiazol-3-yl) piperazine of formula II or its salt: with 5-(2-haloethyl)-6-chloro-oxindole of formula III: wherein X is leaving groups like fluoro, chloro, bromo, iodo or sulphonyl; in the presence of a dispersing agent and a base in a solvent to form ziprasidone of formula I; and optionally converting the ziprasidone formed into a pharmaceutically acceptable acid addition salts of ziprasidone; or a solvate or a hydrate thereof.Type: GrantFiled: March 9, 2009Date of Patent: April 2, 2013Assignee: Alkem Laboratories LimitedInventors: Shashiprabha, Kanakamajalu Shridhara, Debkiron Mukherjee, Padmashree Badraje, K Sundarraja Rao, Kuppuswamy Nagarajan
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Patent number: 8404691Abstract: There is provided compounds that inhibit interaction between murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity. Compounds include imidazothiazole derivatives that can inhibit interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity.Type: GrantFiled: July 15, 2011Date of Patent: March 26, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Kouichi Uoto, Yuuichi Sugimoto, Hiroyuki Naito, Masaki Miyazaki, Keisuke Yoshida, Masashi Aonuma