Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/350)
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Publication number: 20140155395Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: ApplicationFiled: February 4, 2014Publication date: June 5, 2014Applicant: Janssen Pharmaceutica, NVInventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
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Publication number: 20140148430Abstract: Certain imidazopyridines (I) 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: ApplicationFiled: November 26, 2012Publication date: May 29, 2014Applicant: Gilead Connecticut, Inc.Inventors: Peter A. Blomgren, Kevin S. Currie, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Aaron C. Schmitt, Jianjun Xu, Zhongdong Zhao
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Publication number: 20140142108Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R1d, R2a, R2b, X1, X2, 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: ApplicationFiled: May 30, 2013Publication date: May 22, 2014Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20140142098Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: November 11, 2013Publication date: May 22, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald ENGELHARDT, Davide GIANNI, Christian SMETHURST
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Publication number: 20140142298Abstract: The present invention embodiments relate to a compound with formula (V?) The invention also relates in certain embodiments to the synthesis method for compound (V?) and its use for the preparation of 1,4,7-triazacyclononane (tacn) and N- and/or C-functionalized derivatives thereof, particularly compounds with formula (I) The invention also relates in certain embodiments to metallic complexes comprising a ligand with formula (I) and a metal and their use for imaging.Type: ApplicationFiled: November 13, 2013Publication date: May 22, 2014Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE BOURGOGNEInventors: Franck Denat, Pauline Desogere, Claire Bernhard, Yoann Rousselin, Frederic Boschetti
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Publication number: 20140142085Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.Type: ApplicationFiled: July 5, 2012Publication date: May 22, 2014Applicant: Gilead Sciences, Inc.Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-hung Chou, Randall L. Halcomb, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
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Patent number: 8729081Abstract: The present invention provides compounds which antagonize epsilon protein kinase C (PKC?). These compounds have a structural formula (Ia), (Ic) or (II). The present invention also provides pharmaceutical compositions containing these compounds and methods of treating various diseases, conditions, and/or symptoms by using these compounds.Type: GrantFiled: October 12, 2009Date of Patent: May 20, 2014Assignee: VM Discovery Inc.Inventor: Jay Jie-Qiang Wu
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Patent number: 8729095Abstract: A compound of the general formula (I): [wherein, R1 represents a halogen atom, or the like, R2 represents a hydrogen atom, or the like, R3 and R4, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, R5 represents a hydrogen atom, a halogen atom, or the like, R6 represents a hydrogen atom, a halogen atom, or the like, R7 and R8, each independently, represent a hydrogen atom, a halogen atom, or the like, R9 and R10, each independently, represent a hydrogen atom, a C1-4 alkyl group, R11 and R12, each independently, represent a hydrogen atom, a C1-4 alkyl group, or the like, X represents an oxygen atom, a group —CH2—, or the like, Y represents a nitrogen atom, a group ?CH—, or the like, and Z represents a nitrogen atom, or the like] or a pharmacologically acceptable salt thereof, which has an excellent suppressive action on platelet aggregation, and is useful for prevention and/or treatment of thromboembolism.Type: GrantFiled: August 27, 2010Date of Patent: May 20, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Tatsuya Nishi, Masashi Hasegawa, Yumi Nakamoto, Yuichi Ochiai, Ryoko Kitazawa, Hiroshi Susaki
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Publication number: 20140135319Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: December 13, 2011Publication date: May 15, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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Publication number: 20140128374Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides of the foregoing; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds, salts or N-oxides, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), ADHD, impulsivity, compulsive gambling, overeating, autism spectrum disorder, MCI, age-related cognitive decline, dementia, RLS, Parkinson's disease, Huntington's chorea, anxiety, depression, MDD, TRD, and bipolar disorder.Type: ApplicationFiled: November 5, 2013Publication date: May 8, 2014Applicant: PFIZER INCInventors: JENNIFER ELIZABETH DAVOREN, AMY BETH DOUNAY, IVAN VIKTOROVICH EFREMOV, DAVID LAWRENCE FIRMAN GRAY, SCOT RICHARD MENTE, STEVEN VICTOR O'NEIL, BRUCE NELSEN ROGERS, CHAKRAPANI SUBRAMANYAM, LEI ZHANG
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Publication number: 20140128607Abstract: There is provided salts and polymorphs of sitagliptin, processes for the preparation thereof, and pharmaceutical compositions comprising the same.Type: ApplicationFiled: December 5, 2013Publication date: May 8, 2014Applicants: Dr. Reddy's Laboratories, Inc., 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: 8716291Abstract: Provided are compounds of Formula I and compounds of Formula II: and pharmaceutically acceptable salts thereof, and methods for their use.Type: GrantFiled: September 12, 2012Date of Patent: May 6, 2014Assignee: Cytokinetics, Inc.Inventors: Aaron Hinken, Fady Malik, Malar Pannirselvam, Alan Russell
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Patent number: 8716312Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: GrantFiled: November 17, 2009Date of Patent: May 6, 2014Assignee: Merck Sharp & Dohme CorporationInventors: Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
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Publication number: 20140121200Abstract: Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.Type: ApplicationFiled: June 7, 2012Publication date: May 1, 2014Applicant: HUTCHISON MEDIPHARMA LIMITEDInventors: Wei-Guo Su, Wei Deng, Jianguo Ji
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Publication number: 20140113898Abstract: The invention relates to bisarylsulfone and dialkylarylsulfone compounds (e.g., compounds according to any of Formulas (I)-(IX) or compounds (1)-(227) of Tables 4 and 5) useful in treating conditions associated with calcium channel function, and particularly conditions associated with N-type calcium channel activity. The invention also relates to pharmaceutical compositions that include these bisarylsulfone compounds, as well methods for the treatment of conditions such as cardiovascular disease, epilepsy, cancer and pain.Type: ApplicationFiled: November 4, 2011Publication date: April 24, 2014Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan A. Pajouhesh, Richard Holland, Yuanxi Zhou, Yongbao Zhu, Michael Edward Grimwood, Navjot Chahal
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Patent number: 8703759Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, R4, and R5 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: GrantFiled: June 30, 2011Date of Patent: April 22, 2014Assignee: Gilead Sciences, Inc.Inventors: Tetsuya Kobayashi, Dmitry Koltun, Gregory Notte, Eric Parkhill, Jeff Zablocki
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Patent number: 8703946Abstract: In one aspect, the invention relates to substituted pyrazolo[1,5-a]pyrazine compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: December 7, 2011Date of Patent: April 22, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Carrie K. Jones, Shaun R. Stauffer, José Manuel Bartolome-Nebreda, Gregor James McDonald, Susana Conde-Ceide, Han Min Tong
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Patent number: 8697699Abstract: Imidazopyrazines of Formula I and pharmaceutically acceptable salts and mixtures thereof, are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle are also provided. 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 disclosed. These diseases include cancer (e.g., B-cell lymphoma and leukemia), autoimmune diseases, inflammatory diseases, acute inflammatory reactions, and allergic disorders. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for determining the presence or absence of Syk kinase in a sample.Type: GrantFiled: January 4, 2012Date of Patent: April 15, 2014Assignee: Gilead Connecticut, Inc.Inventors: Scott A. Mitchell, Peter A. Blomgren, Joseph Raker
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Publication number: 20140094456Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: ApplicationFiled: March 13, 2013Publication date: April 3, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8686135Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: GrantFiled: April 30, 2013Date of Patent: April 1, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Patrick Anthony Jokiel, Juan Antonio Gamboa, Philip Pye, William Wei-Hwa Leong, Anusuya Choudhury
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Publication number: 20140086870Abstract: New pyrazole derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: February 18, 2011Publication date: March 27, 2014Inventors: Jordi Bach Taña, Lluis Miquel Pages Santacana, Joan Taltavull Moll, Paul Robert Eastwood, Jacob Gonzalez Rodrigues, Victor Giulio Matassa
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Patent number: 8680098Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.Type: GrantFiled: February 25, 2011Date of Patent: March 25, 2014Assignee: Janssen Pharmaceutica, NVInventors: Mark R. Player, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
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Publication number: 20140081026Abstract: 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: ApplicationFiled: May 4, 2012Publication date: March 20, 2014Applicant: CHEMO IBERICA S.A.Inventors: Marcello Rasparini, Roberto Rocco Tufaro, Cosima Minelli
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Patent number: 8673908Abstract: Provided is a kynurenine production inhibitor comprising a nitrogen-containing heterocyclic compound represented by formula (I): (wherein R50 and R51 may be the same or different and each represent a hydrogen atom or the like, G1 and G2 may be the same or different and each represent a nitrogen atom or the like, X represents formula (III): (wherein m1 and m2 may be the same or different and each represent an integer of 0 or 1, Y represents an oxygen atom or the like, and R6 and R7 may be the same or different and each represent a hydrogen atom or the like), R1 represents optionally substituted lower alkyl or the like, R2 represents a hydrogen atom or the like, and R3 represents optionally substituted lower alkyl or the like), and the like.Type: GrantFiled: November 9, 2009Date of Patent: March 18, 2014Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Nobuyoshi Amishiro, Yuichi Fukuda, Keisuke Kimpara, Motoya Mie, Hisashi Tagaya, Takeshi Takahashi
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Patent number: 8674098Abstract: Compositions containing neurogenic agents for inhibition of neuron death and inducing proliferation of neural cells are disclosed.Type: GrantFiled: January 17, 2013Date of Patent: March 18, 2014Assignee: Neuralstem, Inc.Inventors: Judith Kelleher-Andersson, Karl K. Johe
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Patent number: 8674097Abstract: The present invention relates to compounds of formula (I) wherein X, Y, Z, R1, R2, R3 are as defined in claim 1, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention of diabetes, metabolic syndrome, obesity, cancer, inflammation.Type: GrantFiled: August 24, 2012Date of Patent: March 18, 2014Assignee: Merck Patent GmbHInventors: Daniel Cravo, Sophie Hallakou-Bozec, Franck Lepifre
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Patent number: 8673905Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of AML.Type: GrantFiled: March 9, 2012Date of Patent: March 18, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Michael Soth
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Publication number: 20140073640Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: August 12, 2013Publication date: March 13, 2014Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
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Publication number: 20140073626Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.Type: ApplicationFiled: May 16, 2012Publication date: March 13, 2014Applicant: Principia BiopharmaInventors: David Michael Goldstein, Kenneth Albert Brameld, Erik Verner
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Publication number: 20140073791Abstract: The present invention relates to pharmaceutically acceptable acid addition salts of sitagliptin, in particular anti-oxidant acid addition salts of sitagliptin and a process for its preparation. The present invention also provides a pharmaceutical composition using the pharmaceutically acceptable acid addition salts of sitagliptin.Type: ApplicationFiled: October 12, 2012Publication date: March 13, 2014Applicant: LAURUS LABS PRIVATE LIMITEDInventors: Venkata Sunil Kumar Indukuri, Seeta Ramanjaneyulu Gorantla, Vamsee Krishna Muppidi, Satyanarayana Chava
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Patent number: 8669256Abstract: The invention relates to compounds according to general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of cancer.Type: GrantFiled: May 23, 2011Date of Patent: March 11, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Brigitte Johanna Bernita Folmer, de Adrianus Petrus Antonius Man, Elisabeth Sophia Gernette, Rita Corte Real Goncalves Azevedo, Hemen Ibrahim
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Publication number: 20140066420Abstract: The present invention relates to wherein each symbol is as defined in the specification. The compound of the present invention has a superior RBP4-lowering action, and is useful as a medicament for the prophylaxis or treatment of disease and condition mediated by increased RBP4.Type: ApplicationFiled: October 16, 2013Publication date: March 6, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Shizuo KASAI, Tomohiro KAKU, Masahiro KAMAURA
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Publication number: 20140066426Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: ApplicationFiled: August 29, 2013Publication date: March 6, 2014Inventors: Stefan SCHUNK, Melanie REICH, Henning STEINHAGEN, Nils DAMANN, Michael HAURAND, Achim KLESS, Philip SKONE, Richard HAMLYN, Robert KIRBY, Marc ROGERS, Kathy SUTTON
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Publication number: 20140057893Abstract: 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.Type: ApplicationFiled: April 5, 2012Publication date: February 27, 2014Applicant: 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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Patent number: 8658794Abstract: The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.Type: GrantFiled: February 3, 2011Date of Patent: February 25, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Adrianus Petrus Antonius de Man, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Hans Cornelis Andreas Raaijmakers, Jacobus Cornelis Henricus Maria Wijkmans
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Patent number: 8658649Abstract: The invention is directed to a compound of formula (I): and the prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs. Such a compound has valuable pharmaceutical properties, in particular the ability to inhibit protein kinases.Type: GrantFiled: March 10, 2009Date of Patent: February 25, 2014Assignee: SanofiInventors: Timothy A. Gillespy, Paul Eynott, Elizabeth M. Allen, Kin T. Yu, Asher Zilberstein
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Patent number: 8658646Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: August 31, 2012Date of Patent: February 25, 2014Assignee: Hoffmann-LaRoche Inc.Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
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Publication number: 20140051856Abstract: The present invention discloses new salts of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine i.e. gentisate, adipate and trifluoro acetic acid salts. The invention also describes the new. crystalline and amorphous forms of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine gentisate. The present invention also discloses novel crystalline salt form of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine hydrochloride and novel crystalline and amorphous salt forms of besylate and process for their preparation and isolation.Type: ApplicationFiled: March 2, 2012Publication date: February 20, 2014Applicant: CADILA HEALTHCARE LIMITEDInventors: Bipin Pandey, Mayank Ghanshyambhai Dave, Himanshu M. Kothari, Bhavin Shriprasad Shukla
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Patent number: 8653268Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.Type: GrantFiled: January 11, 2013Date of Patent: February 18, 2014Assignee: OSI Pharmaceuticals, LLCInventors: Mark J. Mulvihill, Radoslaw Laufer, An-Hu Li, Arno G. Steinig
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Patent number: 8653078Abstract: The present invention relates to a method of controlling plants or inhibiting plant growth which comprises applying to the plants or to the locus thereof a herbicidally effective amount of a compound of formula (I) wherein R1, R2, R3, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to intermediates used in the preparation of compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to certain novel pyridopyridines.Type: GrantFiled: December 21, 2012Date of Patent: February 18, 2014Assignee: Syngenta LimitedInventors: Matthew Robert Cordingley, V, Michael Drysdale Turnbull, Neil Brian Carter, Patrick Jelf Crowley
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Publication number: 20140045814Abstract: The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: August 9, 2013Publication date: February 13, 2014Applicant: Incyte CorporationInventors: Liang Lu, Chunhong He, Wenqing Yao
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Publication number: 20140045831Abstract: The invention relates to bicyclic heterocycle compounds of formula (I): or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2, R3, A, W, U and V are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: April 20, 2012Publication date: February 13, 2014Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Ildiko Maria Buck, Gianni Chessari, Steven Howard, David Charles Rees, Alison Jo-Anne Woolford
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Publication number: 20140045687Abstract: The present invention relates to the use of dithiine-dicarboximide compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel dithiine-dicarboximides, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.Type: ApplicationFiled: April 10, 2012Publication date: February 13, 2014Applicant: BASF SEInventors: Wassilios Grammenos, Nadege Boudet, Richard Riggs, Jochen Dietz, Egon Haden, Marcus Fehr
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Patent number: 8648075Abstract: The present invention is to provide an oxopyrazine derivative having an excellent herbicidal activity and besides exhibiting high safety for useful crops and the like, or a salt thereof, and a herbicide containing the same. The present invention relates to an oxopyrazine derivative represented by formula [I]: wherein X1 represents an oxygen atom or a sulfur atom; X2 represents CH or N(O)m; m represents an integer of 0 or 1; R1 represents a hydrogen atom, a C1-C12 alkyl group and the like; R2 represents a halogen atom, a cyano group and the like; R3 is a hydroxyl group, a halogen atom and the like; A1 represents C(R4R5); A2 represents C(R6R7) or C?O; A3 represents C(R8R9); R4 to R9 represent a hydrogen atom or an alkyl group, or a salt thereof, and a herbicide containing these compounds.Type: GrantFiled: January 17, 2013Date of Patent: February 11, 2014Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Ryuji Tamai, Minoru Ito, Masami Kobayashi, Takashi Mitsunari, Yuki Nakano
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Publication number: 20140038955Abstract: Heteroaryl amide analogues 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: October 2, 2013Publication date: February 6, 2014Applicant: H. Lundbeck A/SInventors: David C. IHLE, Qin GUO, Kevin HODGETTS, Jun YUAN
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Patent number: 8642617Abstract: The present invention relates to pyridopyrazinone derivatives of formula (I), wherein X, Y, Z1 W, A and R1 are as defined in claim 1, as insulin secretion stimulators. The invention also relates to the preparation and use of these pyridopyrazinone derivatives for the prophylaxis and/or treatment of diabetes and pathologies associated.Type: GrantFiled: January 25, 2012Date of Patent: February 4, 2014Assignee: Merck Patent GmbHInventors: Gérard Botton, Eric Valeur, Micheline Kergoat, Christine Charon, Samer Elbawab
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Patent number: 8642281Abstract: Coelenterazine analogues with different luminescence properties from conventional ones and coelenteramide analogues with different fluorescence properties from conventional ones have been desired. The invention provides coelenterazine analogues modified at the 8-position of coelenterazine and coelenteramide analogues modified at the 2- or 3-position of coelenteramide.Type: GrantFiled: April 5, 2011Date of Patent: February 4, 2014Assignees: JNC Corporation, National University Corporation Tokyo Medical and Dental UniversityInventors: Satoshi Inouye, Yuiko Sahara, Takamitsu Hosoya
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Publication number: 20140031339Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A1, A2, L1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. 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: ApplicationFiled: July 16, 2013Publication date: January 30, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael Jason BURKE, Thomas Martin KIRRANE, JR., Chuk Chui MAN, Daniel Richard MARSHALL, Anil Kumar PADYANA, Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Roger John SNOW, Ronald John SORCEK, Hidenori TAKAHASHI, Steven John TAYLOR, Michael Robert TURNER, Erick Richard Roush YOUNG, Qiang ZHANG, Yunlong ZHANG, Renee M. ZINDELL
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Publication number: 20140024058Abstract: There has been a need for coelenterazine analogs that exhibit luminescence properties different from those of known coelenterazine analogs. The present invention provides the compound represented by general formula (1).Type: ApplicationFiled: August 22, 2013Publication date: January 23, 2014Applicants: Tokyo Institute Of Technology, JNC CorporationInventors: Satoshi INOUYE, Yuiko Sahara, Rie Iimori, Takamitsu Hosoya
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Patent number: 8624026Abstract: Disclosed are a novel, simple and low-cost method for preparing sitagliptin of formula (I), as DPP-IV (dipeptidyl peptidase IV) inhibitor, which is useful in treating type 2 diabetes mellitus and key intermediates used in said preparation of sitagliptin:Type: GrantFiled: October 19, 2010Date of Patent: January 7, 2014Assignee: Hanmi Science Co., LtdInventors: Nam Du Kim, Ji Yeon Chang, Dong Jun Kim, Hyun Seung Lee, Jae Hyuk Jung, Young Kil Chang, Gwan Sun Lee