Ring Nitrogen In The Polycyclo Ring System Patents (Class 546/198)
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Patent number: 8785631Abstract: Novel raw material compounds are provided that are useful for producing novel cycloalkane carboxamide derivatives having cathepsin K inhibitory action. An oxazolone derivative represented by formula (I): [wherein, R1 represents a substituted or unsubstituted alkyl group, substituted or unsubstituted alkenyl group, substituted or unsubstituted alkynyl group, substituted phenyl group, substituted or unsubstituted naphthyl group or substituted or unsubstituted heterocyclic group, and ring A represents a saturated cyclic alkylidene group having 6 to 7 carbon atoms].Type: GrantFiled: January 10, 2007Date of Patent: July 22, 2014Assignee: Seikagaku CorporationInventors: Tsuneo Koji, Hisatomo Kunii, Nobuo Kobayashi
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Publication number: 20140187583Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.Type: ApplicationFiled: May 18, 2012Publication date: July 3, 2014Applicant: RAQUALIA PHARMA INC.Inventors: Toyoharu Numata, Hirohide Noguchi, Nobuaki Waizumi, Takashi Kojima
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Publication number: 20140179927Abstract: A method for preparation of iloperidone is provided which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride with 1-[4-(3-chloropropoxyl)-3-methoxyphenyl]ethyl ketone in an inorganic alkaline aqueous solution. A crystallization method of iloperidone is also provided which comprises adding seed crystal to the iloperidone solution in ethyl acetate, and then iloperidone crystal is obtained with high purity by controlling the temperature and the stirring speed.Type: ApplicationFiled: February 26, 2014Publication date: June 26, 2014Applicant: Zhejiang Huahai Pharmaceutical Co., Ltd.Inventors: Shiwei Zhou, Feng Jian
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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: 8754097Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: August 22, 2012Date of Patent: June 17, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Publication number: 20140148440Abstract: The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.Type: ApplicationFiled: November 15, 2010Publication date: May 29, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Rambabu Namala, Adi Reddy Dwarampudi, Laxman Kota, Murlimohan Gampa, Padmavathi Kodru, Taraka Naga Vinaykumar Tiriveedhi, Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad, Venkateswarlu Jasti
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Patent number: 8735576Abstract: Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance.Type: GrantFiled: August 5, 2013Date of Patent: May 27, 2014Assignee: Biotie Therapies, Inc.Inventors: Thomas R. Malefyt, Lesley Pickford
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Publication number: 20140135310Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.Type: ApplicationFiled: June 29, 2012Publication date: May 15, 2014Applicant: Adamed Sp. z o.o.Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
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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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Patent number: 8703758Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.Type: GrantFiled: April 26, 2011Date of Patent: April 22, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
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Publication number: 20140100248Abstract: The present invention relates to new heterocyclic compounds as modulators of sphingolipid signaling and uses thereof of as pharmaceutically active agents, suitable for treating proliferative, degenerative, infectious, and other diseases.Type: ApplicationFiled: April 2, 2012Publication date: April 10, 2014Applicants: UNIVERSITÄT BERN, JOHANN WOLFGANG GOETHE-UNIVERSITÄTInventors: Holger Stark, Aleksandra Zivkovic, Andrea Huwiler, Josef Pfeilschifter
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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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Publication number: 20140073622Abstract: To develop an antibiotic having a novel mechanism of action, the present inventors have searched for a compound that has weak cytotoxicity, the physical property of high solubility in water, the effect of inhibiting both DNA gyrase GyrB and topoisomerase IV ParE subunits, and sufficient antibacterial activity. As a result, the present inventors have completed the present invention by finding that a compound of the present invention represented by the general formula (1), a pharmacologically acceptable salt thereof, and a prodrug thereof have desirable properties. The present invention provides a pharmaceutical composition (particularly, a preventive or therapeutic composition for infectious disease) comprising a compound represented by the formula (1), a pharmacologically acceptable salt thereof, or a prodrug thereof as an active ingredient.Type: ApplicationFiled: September 13, 2013Publication date: March 13, 2014Applicant: Daiichi Sankyo Company, LimitedInventors: Tsuyoshi Soneda, Hiroshi Takeshita, Yoshiko Kagoshima, Yuko Yamamoto, Takafumi Hosokawa, Toshiyuki Konosu, Nobuhisa Masuda, Takuya Uchida, Issei Achiwa, Junichi Kuroyanagi, Tetsunori Fujisawa, Aki Yokomizo, Tetsuji Noguchi
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Publication number: 20140066412Abstract: 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: November 6, 2013Publication date: March 6, 2014Inventors: 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. Selerstad
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Publication number: 20140045829Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one 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: October 8, 2013Publication date: February 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: MARK E. LAYTON, Michael J. Kelly
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Publication number: 20140045811Abstract: 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 18, 2013Publication date: February 13, 2014Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
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Publication number: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
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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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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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Publication number: 20140011796Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.Type: ApplicationFiled: September 12, 2013Publication date: January 9, 2014Applicant: AMGEN INC.Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
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Publication number: 20140011996Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed. Specifically, a series of compounds containing N-piperidinyl acetamide derivatives as shown in formula (1).Type: ApplicationFiled: August 29, 2013Publication date: January 9, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Ramesh Kaul, Yanbing Ding, Yongbao Zhu, Lingyun Zhang, Nagasree Chakka, MIchael Edward Grimwood, Jason Tan, Yuanxi Zhou
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Publication number: 20140005191Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 9, 2011Publication date: January 2, 2014Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEacher, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Patent number: 8614232Abstract: An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.Type: GrantFiled: September 14, 2012Date of Patent: December 24, 2013Assignee: Novartis AGInventors: Dierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
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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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Publication number: 20130324556Abstract: A compound of formula (I) or a pharmaceutically acceptable salt, solvate, or hydrate thereof Wherein Y, Z, R3, U, R4, m and n are as defined in the claims.Type: ApplicationFiled: January 27, 2012Publication date: December 5, 2013Inventors: Joe William Boyd, Paul Meo, Michael Higginbottom, Iain Simpson, David Mark Mountford, Edward Daniel Savory
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Patent number: 8598179Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 17, 2010Date of Patent: December 3, 2013Assignee: SanofiInventors: Marc Nazaré, Gernot Zech, Jochen Goerlitzer, Melitta Just, Tilo Weiss, Gerhard Hessler, Werngard Czechtizky, Sven Ruf
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Publication number: 20130317219Abstract: Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance.Type: ApplicationFiled: August 5, 2013Publication date: November 28, 2013Applicant: Biotie Therapies, Inc.Inventors: Thomas R. Malefyt, Lesley Pickford
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Patent number: 8580968Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: GrantFiled: March 1, 2012Date of Patent: November 12, 2013Assignee: AbbVie Inc.Inventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
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Publication number: 20130289067Abstract: Inhibitors of HIV-1 protease and compositions containing them are described. Use of the inhibitors and compositions containing them to treat HIV, AIDS, and AIDS-related diseases is described.Type: ApplicationFiled: June 27, 2013Publication date: October 31, 2013Inventors: Arun K. GHOSH, Bruno D. Chapsal, Hiroaki Mitsuya
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20130261308Abstract: Disclosed is a process for the synthesis of iloperidone starting from 4-hydroxy-3-methoxy acetophenone (acetovanillone), 1-chloro-3-bromo propane and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, using a one-pot method. Said process is performed without any intermediate isolation, and is particularly advantageous from the environmental standpoint and in terms of yields, productivity and the purity of the product obtained, both in the reaction mixture and in the crystal isolated.Type: ApplicationFiled: March 28, 2013Publication date: October 3, 2013Applicant: PROCOS. S.p.A.Inventors: Piergiorgio BETTONI, Jacopo ROLETTO, Paolo Paissoni
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Publication number: 20130261108Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).Type: ApplicationFiled: November 30, 2011Publication date: October 3, 2013Applicant: IRM LLCInventors: David C. Tully, Agnes Vidal, Daniel Mutnick, Phillip B. Alper
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Publication number: 20130261154Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, J, Z, and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 12, 2011Publication date: October 3, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Mary Ann Hanagan, Gilles Seburyamo
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Patent number: 8536198Abstract: The present application describes modulators of MIP-1 of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein m, Q, T, W, Z, R1, R3, R4, R5, R5a and R5b, are as set forth above. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using the modulators are disclosed.Type: GrantFiled: July 23, 2008Date of Patent: September 17, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Joseph B. Santella, John Hynes, Daniel S. Gardner
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Publication number: 20130231329Abstract: The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.Type: ApplicationFiled: September 27, 2011Publication date: September 5, 2013Applicant: BIOPROJETInventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stéphane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Patent number: 8524742Abstract: A method of treating or curing a disease caused by or associated with elevated levels of TNF in a patient including administering to the patient 5H-thioeno(3,4-c)pyrrole-4,6-dione derivatives.Type: GrantFiled: May 9, 2012Date of Patent: September 3, 2013Assignee: Tianjin Hemay Bio-Tech Co., Ltd.Inventor: Hesheng Zhang
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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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Patent number: 8501938Abstract: Provided are compounds of formula I or II that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods oftreating patients suffering from or susceptible to at least one symptom of abuse of dependence on, or withdrawal from at least one substance.Type: GrantFiled: June 16, 2010Date of Patent: August 6, 2013Assignee: Biotie Therapies, Inc.Inventors: Thomas R. Malefyt, Leslie Pickford
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Publication number: 20130196960Abstract: The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy.Type: ApplicationFiled: February 9, 2011Publication date: August 1, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
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Publication number: 20130190501Abstract: The present invention relates to processes for the preparation of 4?-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3?-methoxyacetophenone and intermediates thereof. The present invention also provides a process for purifying 4?-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3?-methoxyacetophenone to obtain the purity greater than about 98.0 area % to about 99.0 area % as measured by HPLC, preferably greater than about 99.0 area % to about 99.5 area %, more preferably greater about 99.5 area % to about 99.9 area %. individual impurities lower than about 0.15 area %, preferably lower than about 0.1% and total impurities lower than about 0.5 area % by HPLC.Type: ApplicationFiled: July 18, 2011Publication date: July 25, 2013Applicant: SYMED LABS LIMITEDInventors: Dodda Mohan Rao, Pingili Krishna Reddy, Buthukuri Venkat Reddy
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Patent number: 8492405Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like. A glucokinase activator containing a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof or a prodrug thereof.Type: GrantFiled: October 17, 2007Date of Patent: July 23, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Yasufumi Miyamoto
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Publication number: 20130184284Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: ApplicationFiled: July 16, 2012Publication date: July 18, 2013Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu, Scott A. Bolton, Laxman Pasunoori, Sunil Kumar Mandal, Philip M. Sher
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Publication number: 20130172365Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: ApplicationFiled: September 16, 2011Publication date: July 4, 2013Applicant: ADAMED SP. Z.O.O.Inventors: Marcin Kolaczkowski, Piotr Kowalski, Jolanta Jaskowska, Monika Marcinkowska, Katarzyna Mitka, Adam Bucki, Anna Wesolowska, Maciej Pawlowski
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Publication number: 20130165432Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: ApplicationFiled: February 21, 2013Publication date: June 27, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130165422Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.Type: ApplicationFiled: November 29, 2012Publication date: June 27, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130150366Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: ASTRAZENECA, INTELLECTUAL PROPERTYInventor: AstraZeneca, Intellectual Property
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Publication number: 20130150408Abstract: This invention relates to novel substituted dioxopiperidinyl phthalimide derivatives and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an immunomodulatory agent.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: CONCERT PHARMACEUTICALS, INC.Inventor: Concert Pharmaceuticals, Inc.
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Patent number: 8455520Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: July 11, 2008Date of Patent: June 4, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
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Patent number: 8445480Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.Type: GrantFiled: June 16, 2008Date of Patent: May 21, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Julianne A. Hunt, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
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Publication number: 20130109649Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 25, 2012Publication date: May 2, 2013Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha