Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
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Publication number: 20150072974Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.Type: ApplicationFiled: May 9, 2013Publication date: March 12, 2015Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
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Patent number: 8975254Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 27, 2010Date of Patent: March 10, 2015Assignee: Orion CorporationInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Publication number: 20150065501Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: March 5, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
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Publication number: 20150065468Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.Type: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
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Patent number: 8969558Abstract: There is provided a process for preparation of sitagliptin of Formula II or a pharmaceutically acceptable salt thereof by deprotection of Formula IX.Type: GrantFiled: December 5, 2013Date of Patent: March 3, 2015Assignee: Dr. Reddy's Laboratories LimitedInventors: Pratap Reddy Padi, Babu Ireni, Srinivas Polavarapu, Shailaja Padamata, Kavitha Nerella, Vijaya Anand Ramasamy, Ranga Reddy Vangala
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Patent number: 8969345Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.Type: GrantFiled: August 3, 2012Date of Patent: March 3, 2015Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
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Patent number: 8969349Abstract: Provided herein are compounds of formula A-L-B, and pharmaceutically acceptable salts and stereoisomers thereof, wherein A is R1 and R2 together with the carbon atoms to which they are attached form a 1,2-phenylene ring optionally substituted with one or more R11; L is —C(R6)2—C(R6)2—; B is a heteroaromatic group defined herein; and -A1-A2- , A3, R11 and R6 are defined herein. Also disclosed are methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: GrantFiled: May 26, 2011Date of Patent: March 3, 2015Assignee: Sunovion Pharmaceuticals Inc.Inventors: John Emmerson Campbell, Michael Charles Hewitt, Philip Jones, Linghong Xie
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Publication number: 20150057283Abstract: Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis.Type: ApplicationFiled: March 28, 2014Publication date: February 26, 2015Applicant: CHOONGWAE PHARMA CORPORATIONInventors: Sung Hwan Moon, Jae Uk Chung, Sung Chan Lee, Masakatsu Eguchi, Michael Kahn, Kwang Won Jeong, Cu Nguyen
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Patent number: 8962835Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: GrantFiled: April 12, 2013Date of Patent: February 24, 2015Assignee: Gilead Connecticut, Inc.Inventors: Scott A. Mitchell, Kevin S. Currie, Peter A. Blomgren, Jeffrey E. Kropf, Seung H. Lee, Jianjun Xu, Douglas G. Stafford
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Publication number: 20150051213Abstract: The present invention provides sitagliptin 4-methylsalicylate, sitagliptin myristate, sitagliptin isophthalate, sitagliptin isonicotinide, sitagliptin adipate, their polymorphic form, processes for their preparation and pharmaceutical compositions thereof.Type: ApplicationFiled: June 26, 2012Publication date: February 19, 2015Inventors: Suresh Babu Jayachandra, Jigar Bhaskarbhai Shah, Sailu Chiguru
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Publication number: 20150051202Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: February 14, 2013Publication date: February 19, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Carl Deutsch, Guenter Hoelzemann, Daniel Kuhn, Ansgar Wegener, Dominique Swinnen, Horacio Comas
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Patent number: 8957062Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Publication number: 20150045326Abstract: The present invention relates to compounds of formula 1 or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, R4, R5, R6 and X? have the meanings as indicated in the specification, to their use as a medicament, to their use in the treatment of a disease selected from among respiratory diseases or complaints and allergic diseases of the airways, to pharmaceutical composition comprising at least one of said compound or a pharmaceutically acceptable salt thereof, as well as to medicament combinations containing one or more of said compounds or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 7, 2014Publication date: February 12, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dieter WIEDENMAYER, Armin HECKEL, Dieter HAMPRECHT
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Patent number: 8952010Abstract: A compound represented by the following formula (I) or a salt thereof: wherein R represents a hydrogen atom, a hydroxy group, or a halogen atom Ar1 represents a bicyclic heterocyclic group represented by the following formula: ?and Ar2 represents a bicyclic heterocyclic group represented by the following formulae:Type: GrantFiled: February 6, 2012Date of Patent: February 10, 2015Assignee: Daiichi Sankyo Company, LimitedInventors: Hiroaki Inagaki, Tetsunori Fujisawa, Masao Itoh, Aki Yokomizo, Toshifumi Tsuda, Saito Higuchi, Biswajit Das, Rita Katoch, Dilip J. Upadhyay
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Publication number: 20150037406Abstract: A novel crystalline form of sitagliptin sulfate is provided. In addition, a method for obtaining the crystalline form, pharmaceutical compositions comprising the novel crystalline form and the crystalline form for use as a medicament are provided.Type: ApplicationFiled: March 1, 2013Publication date: February 5, 2015Inventors: María del Carmen Bernabeu Martínez, Alicia Dobarro Rodríguez, Cristobal Galán Rodríguez
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Publication number: 20150038506Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), neurodegenerative diseases (e.g., Alzheimer's disease), metabolic diseases (e.g. diabetes), neurodevelopmental disorders (e.g. autism), or psychiatric disorders (e.g. schizophrenia or anxiety)) as well as methods of treating these diseases.Type: ApplicationFiled: October 17, 2014Publication date: February 5, 2015Applicants: Agency for Science, Technology and Research, University of BaselInventors: Kassoum Nacro, Stephane Baudouin, Peter Scheiffele
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Patent number: 8946203Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 5, 2013Date of Patent: February 3, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Steven Richard Brunette, Michael J. Burke, Suresh R. Kapadia, Thomas Martin Kirrane, Matthew Russell Netherton, Hossein Razavi, Sonia Rodriguez, Anjan Saha, Robert Sibley, Lana Louise Smith-Keenan, Hidenori Takahashi, Michael Robert Turner, Jiang-Ping Wu, Erick Richard Roush Young, Qiang Zhang, Qing Zhang, Renee M. Zindell
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Patent number: 8946224Abstract: The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state.Type: GrantFiled: November 11, 2011Date of Patent: February 3, 2015Assignee: Redx Pharma LimitedInventors: Mark Craighead, Ronald Palin, Neil Murray, Derek Lindsay
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Patent number: 8946223Abstract: This invention provides compounds of formula (I): wherein X1, X2, R1a, R1b, R1c, R1d, n, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: April 11, 2011Date of Patent: February 3, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Janice Chin, Kenneth M. Gigstad, He Xu
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Publication number: 20150031652Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: August 1, 2014Publication date: January 29, 2015Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20150025080Abstract: The present invention provides processes for the preparation of amorphous form of sitagliptin dihydrogen phosphate. It also provides a solid dispersion of sitagliptin dihydrogen phosphate, including in the amorphous form, and processes for its preparation.Type: ApplicationFiled: June 29, 2012Publication date: January 22, 2015Applicant: RANBAXY LABORATORIES LIMITEDInventors: Poonam Kaushik, Ram Thaimattam, Mohan Prasad, Sudershan Kumar Arora
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Publication number: 20150025081Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: September 17, 2014Publication date: January 22, 2015Inventors: Andreas Ritzen, Morten Langgard, Jan Kehler, Jacob Nielsen, John Paul Kilburn, Mohamed M. Farah
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Publication number: 20150025058Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupusType: ApplicationFiled: January 22, 2013Publication date: January 22, 2015Applicant: MERCK PATENT GMBHInventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
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Patent number: 8937069Abstract: The present invention provides compounds of formula (Ia) and (Ib) which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said compounds and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.Type: GrantFiled: January 11, 2013Date of Patent: January 20, 2015Assignee: Novartis AGInventors: Claire Adcock, Catherine Leblanc
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Patent number: 8937068Abstract: Pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: GrantFiled: November 10, 2006Date of Patent: January 20, 2015Assignee: Zentaris GmbHInventors: Irene Seipelt, Eckhard Claus, Eckhard Guenther, Tilmann Schuster, Michael Czech, Emmanuel Polymeropoulos
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Publication number: 20150018543Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: April 28, 2014Publication date: January 15, 2015Applicants: Institut Pasteur Korea, INSERM (Institut National de la Sante et de la Recherche Medicale)Inventors: Priscille BRODIN, Thierry CHRISTOPHE, Zaesung NO, Jaeseung KIM, Auguste GENOVESIO, Denis Philippe Cedric FENISTEIN, Heekyoung JEON, Fanny Anne EWANN, Sunhee KANG, Saeyeon LEE, Min Jung SEO, Eunjung PARK, Monica CONTRERAS DOMINGUEZ, Ji Youn NAM, Eun Hye KIM
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Patent number: 8933228Abstract: The present invention relates to respiratory formulations comprising a compound of formula (I): and use of said compounds and compositions in treatment, for example in the treatment of an inflammatory disease or a respiratory disorder, in particular an inflammatory mediated and/or virally mediated respiratory disorder such as asthma and COPD or the treatment or prevention of viral infection, for example infection by influenza virus, rhinovirus or RSV. The invention also extends to certain novel compounds of formula (I).Type: GrantFiled: June 17, 2011Date of Patent: January 13, 2015Assignee: Respivert, Ltd.Inventors: Peter John Murray, Stuart Thomas Onions, Jonathan Gareth Williams, Kevin Joly
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Publication number: 20150011555Abstract: The invention relates to salts of (7-(2,3-di-p-tolyl-7,8-dihydropyrido[2,3-b]pyrazin-5(6H)-yl)heptanoic acid which are useful for treating diseases affected by the activation of the IP receptor, pharmaceutical compositions that contain the salts and processes for preparing the salts are also described.Type: ApplicationFiled: January 11, 2013Publication date: January 8, 2015Applicant: NOVARTIS AGInventors: Catherine Leblanc, Stephen Carl McKeown, Anett Perlberg, Nicola Tufilli
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Publication number: 20150011557Abstract: The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis.Type: ApplicationFiled: September 7, 2012Publication date: January 8, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Wolfgang Staehle, Michael Busch, Dirk Wienke, Oliver Poeschke, Christa Burger
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Patent number: 8927738Abstract: This invention is directed to compounds of formula I having the structure which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: GrantFiled: June 24, 2013Date of Patent: January 6, 2015Assignee: H. Lundbeck A/SInventors: Ask Puschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morton Langgard
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Publication number: 20150005311Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.Type: ApplicationFiled: January 11, 2013Publication date: January 1, 2015Applicant: NOVARTIS AGInventors: Steven Carl Chatlton, Catherine Leblanc, Stephen Carl Mckeown
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Publication number: 20150005309Abstract: Compounds of formula (I) which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals.Type: ApplicationFiled: January 8, 2013Publication date: January 1, 2015Inventors: Lars Bärfacker, William Scott, Andrea Hägebarth, Stuart Ince, Hartmut Rehwinkel, Oliver Politz, Roland Neuhaus, Ulf Bömer
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Publication number: 20150005280Abstract: The present application relates to a series of substituted pyrazolo[1,5-a]pyridine compounds, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: December 12, 2012Publication date: January 1, 2015Applicant: DR. REDDY'S LABORATORIES LTD.Inventors: Pradip Kumar Sasmal, Shahadat Ahmed, Ganesh Prabhu, Ashok Tehim, Vidyadhar Paradkar, Marahanakuli Prasanna Dattatreya, Nanjegowda Jagadeesh Mavinahalli
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Publication number: 20150005293Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: September 9, 2014Publication date: January 1, 2015Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
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Patent number: 8921319Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.Type: GrantFiled: July 5, 2011Date of Patent: December 30, 2014Assignee: The Medicines Company (Leipzig) GmbHInventors: Torsten Steinmetzer, Sebastian Martin Saupe
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Patent number: 8921273Abstract: Substituted pyridazines of the formula I in which the variables are defined according to the description, processes and intermediates for preparing the compounds of the formula I and their N-oxides, their agriculturally suitable salts, compositions comprising them and their use as herbicides, and also methods for controlling unwanted vegetation.Type: GrantFiled: March 23, 2011Date of Patent: December 30, 2014Assignee: BASF SEInventors: Dschun Song, Julia Major, Johannes Hutzler, Trevor William Newton, Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Tao Qu, Frank Stelzer, Andree Van Der Kloet, Thomas Seitz, Thomas Ehrhardt, Klaus Kreuz, Klaus Grossmann, Anna Aleksandra Michrowska-Pianowska, Anja Simon, Ruediger Reingruber, Helmut Kraus, Hans Wolfgang Hoeffken, Thomas Mietzner
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Publication number: 20140378463Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor, processes for preparing them, pharmaceutical compositions comprising said derivatives and uses thereof. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients.Type: ApplicationFiled: January 11, 2013Publication date: December 25, 2014Applicant: NOVARTIS AGInventor: Catherine Leblanc
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Patent number: 8916559Abstract: A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 1 with fumaric acid or a hydrate thereof, where the molar ratio of the compound of formula 1 to fumaric acid is 1:0.6 to 1:1.3 is described.Type: GrantFiled: August 12, 2010Date of Patent: December 23, 2014Assignee: Sandoz AGInventors: Fritz Blatter, Katharina Reichenbächer
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Publication number: 20140371138Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
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Publication number: 20140371199Abstract: The present invention relates to certain compounds (e.g., imidazopyrazine, imidazopyridine, imidazopyridazine and imidazpyrimidine compounds) that act as inhibitors of the MAP kinase interacting kinases MNK2a, MNK2b, MNK1a, and MNK1b. The present invention further relates to pharmaceutical compositions comprising these compounds, and to the use of the compounds for the preparation of a medicament for the prophylaxis and treatment of diseases (e.g., proliferative diseases (e.g., cancer), inflammatory diseases, Alzheimer's disease), as well as methods of treating these diseases.Type: ApplicationFiled: April 1, 2013Publication date: December 18, 2014Applicant: Agency for Science, Technology and ResearchInventors: Kassoum Nacro, Athisayamani Jeyaraj Duraiswamy, Lohitha Rao
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Patent number: 8912189Abstract: The present invention provides new pyridopyrazine compounds of Formula (I) which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: GrantFiled: April 4, 2012Date of Patent: December 16, 2014Assignee: Aeterna Zentaris GmbHInventors: Matthias Gerlach, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
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Patent number: 8912181Abstract: A novel bicyclic compound having an HSP90 inhibitory effect and a carcinostatic effect. A pharmaceutical agent based on the HSP90 inhibitory effect and useful in the prevention and/or treatment of a disease involving HSP90, particularly cancer. The compound has a general formula (I) or is a salt thereof wherein at least one of X1, X2, X3, and X4 represents N or N-oxide and the rest thereof are each independently C—R2; any one or two of Y1, Y2, Y3, and Y4 represent C—R4 and the rest thereof are each independently CH or N; R1 represents an optionally substituted monocyclic or bicyclic unsaturated heterocyclic group having 1 to 4 heteroatoms selected from N, S, and O; R2 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon atoms etc.; R3 represents a hydrogen atom, —CO—R5 etc.Type: GrantFiled: January 6, 2012Date of Patent: December 16, 2014Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Makoto Kitade, Satoshi Yamashita, Shuichi Ohkubo
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Patent number: 8912327Abstract: A novel process is described for the synthesis of Sitagliptin, IUPAC name 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1 2,4-triazolo[4,3-a]pyrazine, of formula (I).Type: GrantFiled: May 4, 2012Date of Patent: December 16, 2014Assignee: Chemo Iberica, S.A.Inventors: Marcello Rasparini, Roberto Rocco Tufaro, Cosima Minelli
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Publication number: 20140364393Abstract: The present invention is directed to novel piperidinyl-carboxamide derivatives, pharmaceutical compositions containing them and their use as inhibitors of SCD1, useful in the treatment of obesity, type-II diabetes and other related metabolic disorders.Type: ApplicationFiled: December 5, 2012Publication date: December 11, 2014Inventors: Shyh-Ming Yang, Gee-Hong Kuo, Micheal D. Gaul, Thomas A. Rano
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Publication number: 20140364423Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Inventors: Wei-Sheng Huang, Ranny M. Thomas
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Publication number: 20140364414Abstract: Disclosed are compounds, compositions and methods for treating Type II diabetes. Such compounds are represented by Formula (I) as follows: wherein R1, R2, L, and Q are defined herein.Type: ApplicationFiled: June 9, 2014Publication date: December 11, 2014Applicant: JANSSEN PHARMACEUTICA, NVInventors: Mark R. Player, Sanath K. Meegalla, Carl R. Illig, Jinsheng Chen, Kenneth J. Wilson, Yu-Kai Lee, Daniel J. Parks, Hui Huang, Sharmila Patel, Tianbao Lu
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Patent number: 8907087Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions, comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: GrantFiled: June 26, 2013Date of Patent: December 9, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Sophie Perrin-Ninkovic, Roy L. Harris, John Sapienza, Graziella I. Shevlin, Patrick Papa, Branden Lee, Garrick Packard, Jingjing Zhao, Jennifer Riggs, Jason Parnes, Deborah Mortensen, Jan Elsner
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Patent number: 8906923Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.Type: GrantFiled: August 10, 2012Date of Patent: December 9, 2014Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
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Publication number: 20140356430Abstract: Provided herein are compositions of 7-(6-(2-hydroxypropan-2-yl)pyridin-3-yl)-1-((trans)-4-methoxycyclohexyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, solid forms, isotopologues and metabolites thereof, and methods of their use for the treatment of a disease, disorder, or condition.Type: ApplicationFiled: May 28, 2014Publication date: December 4, 2014Applicant: Signal Pharmaceuticals, LLCInventors: Marie Georges BEAUCHAMPS, Antonio Christian FERRETTI, Juan Antonio GAMBOA, Kevin KLOPFER, William Edward KONNECKE, Matthew Michael KREILEIN, Anil MENON, Amanda Nicole MIKLOS, John Fitzgerald TRAVERSE