The Other Cyclo In The Bicyclo Ring System Is Also Six-membered (e.g., Naphthyridines, Etc.) Patents (Class 546/122)
  • Publication number: 20140243302
    Abstract: Novel bridged bicyclic compounds are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antibacterial agents. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating bacterial infections and associated diseases and conditions.
    Type: Application
    Filed: June 26, 2012
    Publication date: August 28, 2014
    Applicants: MERCK SHARP & DOHME CORPORATION, KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Yasumichi Fukuda, David E. Kaelin, JR., Sheo B. Singh
  • Publication number: 20140243346
    Abstract: The present invention provides heterocyclic derivatives which activate the IP receptor. 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. Pharmaceutical compositions comprising such derivatives are also encompassed. Examples of compounds of the invention include the compounds according to Formula Ia, or a pharmaceutically acceptable salt thereof, and the compounds of the examples.
    Type: Application
    Filed: April 30, 2014
    Publication date: August 28, 2014
    Applicant: NOVARTIS AG
    Inventors: Steven John CHARLTON, Catherine LEBLANC, Stephen Carl McKEOWN
  • Patent number: 8815849
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Grant
    Filed: July 26, 2011
    Date of Patent: August 26, 2014
    Assignee: Janssen R&D Ireland
    Inventors: Koen Vandyck, Wim Gaston Verschueren, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8815893
    Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: January 10, 2011
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
  • Publication number: 20140235647
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
  • Patent number: 8802697
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 12, 2014
    Assignee: Blueprint Medicines Corporation
    Inventors: Neil Bifulco, Jr., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Publication number: 20140221371
    Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 7, 2014
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Franciso Javier Garcia-Ladona, Wolfgang Wernet
  • Publication number: 20140221410
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 7, 2014
    Applicant: SCIFLUOR LIFE SCIENCES, LLC
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Publication number: 20140221348
    Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.
    Type: Application
    Filed: March 17, 2014
    Publication date: August 7, 2014
    Applicant: Basilea Pharmaceutica AG
    Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
  • Publication number: 20140213595
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: September 4, 2013
    Publication date: July 31, 2014
    Applicant: ABBVIE INC.
    Inventors: David A. DEGOEY, Pamela L. DONNER, Warren M. KATI, Charles W. HUTCHINS, Allan C. KRUEGER, John T. RANDOLPH, Christopher E. MOTTER, Preethi KRISHNAN, Neeta C. MISTRY, Tami J. PILOT-MATIAS, Sachin V. PATEL, Xiaoyan LI, Todd N. SOLTWEDEL, Lissa T. NELSON
  • Publication number: 20140200227
    Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: January 14, 2014
    Publication date: July 17, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
  • Publication number: 20140200216
    Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
    Type: Application
    Filed: January 14, 2014
    Publication date: July 17, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
  • Patent number: 8778977
    Abstract: The present invention provides pyridinonyl PDK1 inhibitors and methods of treating cancer using the same.
    Type: Grant
    Filed: July 2, 2007
    Date of Patent: July 15, 2014
    Assignee: Sunesis Pharmaceuticals, Inc.
    Inventors: Kenneth Egnard Lind, Kathy Cao, Edward Yin-shiang Lin, Thinh Ba Nguyen, Bradley T. Tangonan, Daniel A. Erlanson, Kevin Guckian, Robert Lowell Simmons, Wen-cherng Lee, Lihong Sun, Stig Hansen, Nuzhat Pathan, Lei Zhang
  • Publication number: 20140187559
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: December 26, 2013
    Publication date: July 3, 2014
    Applicant: BLUEPRINT MEDICINES CORPORATION
    Inventor: Chandrasekhar V. Miduturu
  • Publication number: 20140179667
    Abstract: This invention relates to compounds of general formula (I) in which R1, R2, U, V, L, M, R5, m, X, Y and Z are as defined herein, and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
    Type: Application
    Filed: December 18, 2013
    Publication date: June 26, 2014
    Applicant: PFIZER INC.
    Inventors: Martin Paul EDWARDS, Robert Arnold KUMPF, Pei-Pei KUNG, Indrawan James MCAPLINE, Sacha NINKOVIC, Eugene Yuanjin RUI, Scott Channing SUTTON, John Howard TATLOCK, Martin James WYTHES, Luke Raymond Zehnder
  • Publication number: 20140179675
    Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
    Type: Application
    Filed: February 28, 2014
    Publication date: June 26, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
  • Publication number: 20140171429
    Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.
    Type: Application
    Filed: January 20, 2012
    Publication date: June 19, 2014
    Applicant: ABBVIE INC.
    Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
  • Publication number: 20140171451
    Abstract: 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: Application
    Filed: August 10, 2012
    Publication date: June 19, 2014
    Applicant: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans, Eric Pierre Alexandre Arnoult
  • Publication number: 20140170066
    Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.
    Type: Application
    Filed: February 24, 2014
    Publication date: June 19, 2014
    Applicants: Merck & Co., Inc., Visen Medical, Inc.
    Inventors: Milind Rajopadhye, Guojie Ho, Bohumil Bednar, Le T. Duong, Paul J. Coleman
  • Publication number: 20140163038
    Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the Fab1 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: Application
    Filed: August 10, 2012
    Publication date: June 12, 2014
    Inventors: Jerôme Emile Georges Guillemont, David Francis Alain Lançois, Magali Madeleine Simone Motte, Anil Koul, Wendy Mia Albert Balemans
  • Publication number: 20140163001
    Abstract: Provided is a heterocyclic compound having an ROR?t inhibitory activity.
    Type: Application
    Filed: July 27, 2012
    Publication date: June 12, 2014
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Atsuko Ochida, Yoshiyuki Fukase, Yoshihide Tomata, Ayumu Sato, Shotaro Miura, Kazuko Yonemori, Ryokichi Koyama
  • Publication number: 20140148461
    Abstract: The present invention relates to compounds of the formula I and their salts etc. which are inhibitors of phosphodiesterase type 10A and to their use for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.
    Type: Application
    Filed: November 22, 2013
    Publication date: May 29, 2014
    Inventors: Hervé GENESTE, Sean Colm TURNER, Michael OCHSE, Karla DRESCHER, Lawrence A. BLACK, Katja JANTOS
  • Publication number: 20140142302
    Abstract: A 1,5-naphthyridine derivative represented by Formula [1] (in which R1, R2, R3, R4 and R5 represent a hydrogen atom, -L-Z (in which Z represents a non-aromatic heterocyclic group or the like; and L represents a single bond or the like), or the like, R6 represents -L-Z or the like, R7 and R8 represent a hydrogen atom or the like, and Q represents an oxygen atom or the like), or a salt thereof has an excellent inhibitory activity with respect to the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway, and is useful for treatments such as prophylactic treatments and therapeutic treatments of diseases in which the PI3K-AKT pathway and the Ras-Raf-MEK-ERK pathway are involved.
    Type: Application
    Filed: January 28, 2014
    Publication date: May 22, 2014
    Applicant: FUJIFILM Corporation
    Inventors: Hidetomo FURUYAMA, Hideki KURIHARA, Kentarou FURUYA, Takahiro TERAO, Shinichirou SEKINE, Daisuke NAKAGAWA
  • Publication number: 20140142108
    Abstract: 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: Application
    Filed: May 30, 2013
    Publication date: May 22, 2014
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 8729081
    Abstract: 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: Grant
    Filed: October 12, 2009
    Date of Patent: May 20, 2014
    Assignee: VM Discovery Inc.
    Inventor: Jay Jie-Qiang Wu
  • Publication number: 20140128365
    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: enantiomers, diastereomers, solvates, salts, tautomers or prodrugs thereof wherein, A, W, X, Y and R1 are defined herein.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 8, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Shung C. Wu, David S. Yoon
  • Patent number: 8710074
    Abstract: In one aspect, the invention relates to dihydronaphthyridinyl(organo)methanone analogs, 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: Grant
    Filed: January 12, 2012
    Date of Patent: April 29, 2014
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Jason Manka, Jon Jacobs, Ya Zhou, José Manuel Bartolomé-Nebreda, Gregor James MacDonald, Susana Conde-Ceide, Eric S. Dawson
  • Publication number: 20140113931
    Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 24, 2014
    Applicant: Portola Pharmaceuticals, Inc.
    Inventor: Portola Pharmaceuticals, Inc.
  • Publication number: 20140107110
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: October 1, 2013
    Publication date: April 17, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Patent number: 8697867
    Abstract: Cyclic amine compounds represented by formula (1) or salts thereof or N-oxides thereof, wherein Cy1 represents an unsubstituted or substituted aromatic ring; X represents oxygen, sulfur, unsubstituted or substituted nitrogen, sulfinyl, or sulfonyl; R1a and R2a, R1a and R4a, R2a and R3a, or R3a and R4a form saturated rings together; R1a, R1b, R2a, R2b, R3a, R3b, R4a, R4b, and R5 which do not form the saturated rings are each independently hydrogen, hydroxyl, halogen, unsubstituted or substituted amino, nitro, or an organic group; Cy2 represents an unsubstituted or substituted aromatic ring with a proviso that Cy2 is an unsubstituted or substituted heteroaromatic ring when R1a and R2a form a saturated ring together and Cy1 is an unsubstituted or substituted phenyl, and Cy2 is a substituted pyridin-2-yl having one or more cyano as a substituent when Cy1 is an unsubstituted or substituted phenyl and Cy2 is a pyridin-2-yl.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: April 15, 2014
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Isami Hamamoto, Jun Takahashi, Makio Yano, Masahiro Kawaguchi, Daisuke Hanai, Takao Iwasa
  • Patent number: 8691986
    Abstract: Azetidine and piperidine compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds and intermediates thereof. Provided herein also are methods of treating cognitive disorders or diseases treatable by inhibition of PDE10, such as Huntington's Disease, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: June 14, 2013
    Date of Patent: April 8, 2014
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Jian J. Chen, Michael J. Frohn, Matthew R. Kaller, Qingyian Liu, Thomas T. Nguyen, Alexander J. Pickrell, Wenyuan Qian, Robert M. Rzasa, Wenge Zhong
  • Publication number: 20140094456
    Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: April 3, 2014
    Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
  • Publication number: 20140094488
    Abstract: The invention relates to the compounds of general formula (I): Preparation process and therapeutic use.
    Type: Application
    Filed: May 16, 2012
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Alain BRAUN, Olivier DUCLOS, Gilbert LASSALLE, Franz LORGE, Valerie MARTIN, Olaf RITZELER, Aurelie STRUB
  • Patent number: 8685981
    Abstract: Compounds exhibiting an osteogenesis-promoting action having the general formula (I) or a pharmacologically acceptable salt thereof: wherein A is selected from among a 3- to 10-membered heterocyclyl group, B is selected from among an amino group, and X is selected from N and CH.
    Type: Grant
    Filed: July 14, 2011
    Date of Patent: April 1, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Osamu Kanno, Katsuyoshi Nakajima, Kazumasa Aoki, Ryoichi Tanaka, Shimpei Hirano, Kiyoshi Oizumi, Daigo Asano
  • Publication number: 20140088076
    Abstract: The invention provides novel compounds having the general formula: wherein X1 is N or N+O?, and one of X2, X3 and X4 is N or N+—O? and the remainder of X2, X3 and X4 is C. R2, R3, R4, R5, R6. A, B and Y are as described herein. Additionally compositions compounds of Formula I and methods of use are further described herein.
    Type: Application
    Filed: October 31, 2013
    Publication date: March 27, 2014
    Applicant: Genentech, Inc.
    Inventors: Joseph P. Lyssikatos, Lewis J. Gazzard, Emily Hanan, Samuel S. Kintz, Hans Edward Purkey
  • Publication number: 20140088100
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: July 11, 2013
    Publication date: March 27, 2014
    Applicant: BLUEPRINT MEDICINES
    Inventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Patent number: 8680159
    Abstract: Substituted benzamide compounds corresponding to formula (I) in which R5, R6, R7, R8, a, b, c, d, t, D and X have defined meanings, a process for their preparation, pharmaceutical compositions comprising such compounds, and a method of using such compounds to treat pain and other conditions mediated at least in part via the bradykinin 1 receptor.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: March 25, 2014
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Stefan Schunk, Ruth Jostock, Jean De Vry, Christa Kneip, Tieno Germann, Michael Engels
  • Patent number: 8680278
    Abstract: The present invention is directed to a process for enantioselectively preparing substituted piperidine alkanoic acid integrin antagonist compounds.
    Type: Grant
    Filed: October 30, 2008
    Date of Patent: March 25, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: William A. Kinney, Christopher A. Teleha, Shyamali Ghosh, Bruce E. Maryanoff, Gabriela Grasa, Antonio Zanotti-Gerosa, Jonathan Alan Medlock
  • Patent number: 8673920
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: March 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
  • Publication number: 20140066453
    Abstract: Compounds having the formula I wherein R2, X and Z as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
    Type: Application
    Filed: August 27, 2013
    Publication date: March 6, 2014
    Applicants: Genentech, Inc., Array BioPharma Inc.
    Inventors: Jim Blake, Huifen Chen, Mark Chicarelli, John Gaudino, Lewis Gazzard, Sam Kintz, Pete Mohr, Kirk Robarge, Jacob Schwarz, Aihe Zhou
  • Patent number: 8664379
    Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: March 4, 2014
    Assignee: Gilead Sciences, INc.
    Inventors: Matthew Abelman, Nancy Chu, Robert H. Jiang, Kwan Leung, Jeff Zablocki
  • Publication number: 20140057893
    Abstract: 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: Application
    Filed: April 5, 2012
    Publication date: February 27, 2014
    Applicant: 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
  • Patent number: 8658669
    Abstract: Bridged bicyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 25, 2014
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Sacha Holland, Joane Litvak, Dane Goff, Jing Zhang, Thilo J. Heckrodt
  • Publication number: 20140046067
    Abstract: The invention relates to novel alicyclic N,N?-substituted diazabicyclo[3.3.1]nonane derivatives of general formula (I) which act as allosteric AMPA receptor modulators, and to drugs based thereon which can be used for treating Alzheimer's, Parkinson's and other neurodegenerative diseases.
    Type: Application
    Filed: April 10, 2012
    Publication date: February 13, 2014
    Inventors: Maxim Eduardovich Zapolsky, Nokilai Serafimovich Zefirov, Vladimir Alexandrovich Palyulin, Mstislav Igorevich Lavrov
  • Publication number: 20140038960
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: October 4, 2013
    Publication date: February 6, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Publication number: 20140038943
    Abstract: Certain biphenyic compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 10, 2013
    Publication date: February 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Nicholas I. Carruthers, Wenying Chai, Jill A. Jablonowski, Chandravadan R. Shah, Brock T. Shireman, Devin M. Swanson, Vi Tran, Victoria Wong
  • Publication number: 20140031348
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: July 9, 2013
    Publication date: January 30, 2014
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
  • Patent number: 8637513
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved.
    Type: Grant
    Filed: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Publication number: 20140024646
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, Z1 and Z2 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: July 16, 2013
    Publication date: January 23, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Chaozhong Cai, David F. MCCOMSEY, Zhihua Sui, Fu-An Kang
  • Patent number: 8633319
    Abstract: The present invention relates to a compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast and/or basophil cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, chronic spontaneous urticaria and autoimmune conditions.
    Type: Grant
    Filed: April 27, 2011
    Date of Patent: January 21, 2014
    Assignee: Glaxo Group Limited
    Inventors: Francis Louis Atkinson, Michael David Barker, Clement Douault, Neil Stuart Garton, John Liddle, Vipulkumar Kantibhai Patel, Alexander George Steven Preston, David Matthew Wilson