The Additional Hetero Ring Is 1,3-diazine (including Hydrogenated) Patents (Class 540/601)
  • Patent number: 9834548
    Abstract: In one aspect, the invention provides a compound according to formula I, as well as tautomers, pharmaceutically acceptable salts, and hydrates thereof. Pharmaceutical compositions, methods of inhibiting Janus kinases (JAKs), and methods for treating a condition or disorder mediated at least in part by JAK kinase activity are also described.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: December 5, 2017
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Qing Xu, Yonghong Song, Anjali Pandey
  • Patent number: 9809569
    Abstract: The present invention provides a method of efficiently producing an optically active 6-(3-aminopiperidin-1-yl)-2,4-dioxo -1,2,3,4-tetrahydropyrimidine derivative. The optically active piperidine-3-carboxamide or a derivative thereof, which is obtained by subjecting 1,4,5,6-tetrahydropyridine -3-carboxamide or a derivative thereof to an asymmetric reduction in the presence of a catalyst, is used as an intermediate.
    Type: Grant
    Filed: March 13, 2015
    Date of Patent: November 7, 2017
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Masatoshi Yamada, Sayuri Hirano, Ryoji Tsuruoka, Mitsuhisa Yamano
  • Publication number: 20150148327
    Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: June 17, 2013
    Publication date: May 28, 2015
    Applicant: Merck Canada Inc.
    Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
  • Patent number: 9006232
    Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: April 14, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
  • Publication number: 20150065478
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: November 11, 2014
    Publication date: March 5, 2015
    Inventors: Patrick Rene Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Publication number: 20150051195
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Publication number: 20150045339
    Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).
    Type: Application
    Filed: October 16, 2014
    Publication date: February 12, 2015
    Applicant: FUJIFILM CORPORATION
    Inventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
  • Patent number: 8921357
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: December 30, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Patent number: 8916554
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: December 23, 2014
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Publication number: 20140336374
    Abstract: The present invention relates to a process for the production of novel antagonists for CCR2 (CC chemokine receptor 2) and intermediates thereof.
    Type: Application
    Filed: July 29, 2014
    Publication date: November 13, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN
  • Publication number: 20140328805
    Abstract: The present invention provides for compounds of Formula I and embodiments and salts thereof for the treatment of diseases (e.g., neurodegenerative diseases). R1, R2, R3, X1, X2, A and Cy variable in Formula all have the meaning as defined herein.
    Type: Application
    Filed: May 1, 2014
    Publication date: November 6, 2014
    Applicant: GENENTECH, INC.
    Inventors: Anthony Estrada, Alan G. Olivero, Snahel Patel, Michael Siu
  • Publication number: 20140296201
    Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A compound is represented by Structural Formula (IA) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (IA) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.
    Type: Application
    Filed: June 16, 2014
    Publication date: October 2, 2014
    Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Randy S. Bethiel, John J. Court, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Dylan H. Jacobs, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Tiansheng Wang, M. Woods Wannamaker, Randal Byrn, Yi Zhou, Chao Lin, Min Jiang, Steven Jones, Ursula A. Germann, Francesco G. Salituro, Ann Dak-Yee Kwong
  • Patent number: 8822451
    Abstract: 4-amido-pyrimidine compounds, derivatives and compositions thereof, and synthetic methods described herein are useful for modulating ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: May 22, 2006
    Date of Patent: September 2, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Anna R. Hazlewood, Peter D. J. Grootenhuis, Ashvani Kumar Singh, Thomas Cleveland, Frederick F. Van-Goor
  • Publication number: 20140243290
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 28, 2014
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Sathesh Bhat, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Jean-Francois Fournier, Jacques Yves Gauthier, Jonathan Grimm, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon D. Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Matthew L. Maddess, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Alessia Petrocchi, Michael H. Reutershan, Joel S. Robichaud, Eric T. Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hyun Chong Woo, Hua Zhou
  • Publication number: 20140162999
    Abstract: PIM kinase inhibitor compound having a structure as represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts of the compounds as represented by Formula I. The compounds significantly inhibit the Pim kinase activity and are used to prepare drugs to treat PIM kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 12, 2014
    Applicant: Jikai Biosciences, Inc.
    Inventor: Yu GE
  • Publication number: 20140162983
    Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.
    Type: Application
    Filed: June 10, 2012
    Publication date: June 12, 2014
    Applicant: Merck Patent GmbH
    Inventors: Brian L. Hodous, Lesley Liu-Bujalski, Reinaldo Jones, Donald Bankston, Theresa L. Johnson, Igor Mochalkin, Ngan Nguyen, Hui Qiu, Andreas Goutopoulos, Nadia Brugger
  • Patent number: 8680092
    Abstract: A compound represented by formula (I): (wherein the symbols are the same as defined in the description), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof, and medicinal use thereof. The compound represented by formula (I) has CXCR4 antagonistic activity. It is hence useful as, e.g., a preventive and/or therapeutic agent for CXCR4-mediated diseases such as inflammatory/immunologic diseases (e.g., rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, and rejection reactions of transplanted organs), allergic diseases, infections diseases (e.g., human immunodeficiency virus infection and acquired immunologic deficiency syndrome), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease, metabolic diseases, cancer diseases (e.g., cancer, cancer metastasis) or as an agent for regeneration therapy.
    Type: Grant
    Filed: February 24, 2006
    Date of Patent: March 25, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Ochiai, Akira Ohhata, Yoshikazu Takaoka, Shiro Shibayama
  • Patent number: 8623863
    Abstract: The present invention is directed to disubstituted azepan and oxazepan amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 15, 2009
    Date of Patent: January 7, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Mark E. Fraley, John D. Schreier
  • Publication number: 20130345197
    Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: June 3, 2013
    Publication date: December 26, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
  • Publication number: 20130345180
    Abstract: There are provided compounds of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as indicated in claim 1, useful in disorders where ZAP-70 and/or Syk inhibition plays a role or caused by a malfunction of signal cascades connected with FAK.
    Type: Application
    Filed: March 15, 2013
    Publication date: December 26, 2013
    Applicant: NOVARTIS AG
    Inventor: Novartis AG
  • Patent number: 8609852
    Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
    Type: Grant
    Filed: July 26, 2012
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao
  • Publication number: 20130331377
    Abstract: The present invention provides a diaminopyrimidine derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, a pharmaceutical composition comprising the same, and a use thereof. The diaminopyrimidine derivative or its pharmaceutically acceptable salt functions as a 5-HT4 receptor agonist, and therefore can be usefully applied for preventing or treating dysfunction in gastrointestinal motility, one of the gastrointestinal diseases, such as gastroesophageal reflux disease (GERD), constipation, irritable bowel syndrome (IBS), dyspepsia, post-operative ileus, delayed gastric emptying, gastroparesis, intestinal pseudo-obstruction, drug-induced delayed transit, or diabetic gastric atony.
    Type: Application
    Filed: February 24, 2012
    Publication date: December 12, 2013
    Applicant: YUHAN CORPORATION
    Inventors: Hyun-Joo Lee, Dong-Hoon Kim, Tae-Kyun Kim, Young-Ae Yoon, Jae-Young Sim, Myung-Hun Cha, Eun-Jung Jung, Kyoung-Kyu Ahn, Tai-Au Lee
  • Publication number: 20130324517
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.
    Type: Application
    Filed: July 24, 2013
    Publication date: December 5, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN, Stefan SCHEUERER, Silke HOBBIE, Frank BUETTNER
  • Publication number: 20130303506
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 14, 2013
    Applicant: Janssen Pharmaceutical N.V.
    Inventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Patent number: 8580781
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Grant
    Filed: April 29, 2008
    Date of Patent: November 12, 2013
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Patent number: 8551984
    Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: October 8, 2013
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Michael D. Altman, Brian M. Andresen, Kenneth L. Arrington, Jason Burch, Kaleen Konrad Childers, Bernard Cote, Maria Emilia Di Francesco, Anthony Donofrio, Kristina Dupont-Gaudet, John Michael Ellis, Christian Fischer, Daniel Guay, David Joseph Guerin, Andrew M. Haidle, Solomon Kattar, Sandra Lee Knowles, Chaomin Li, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Brendan M. O'Boyle, Ryan D. Otte, Michael H. Reutershan, Eric Romeo, Adam J. Schell, Tony Siu, Kerrie B. Spencer, Brandon M. Taoka, B. Wesley Trotter, Hua Zhou
  • Publication number: 20130210810
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: December 18, 2012
    Publication date: August 15, 2013
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Publication number: 20130184260
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: March 5, 2013
    Publication date: July 18, 2013
    Inventor: Merck Patent Gesellschaft Mit Beschrankter Haftung
  • Patent number: 8420630
    Abstract: The present invention relates to trisubstituted pyrimidines of formula (I) wherein 0Ra to Re are defined as in claim 1, which are suitable for the treatment of illnesses characterized by excessive or abnormal cell proliferation, the use thereof for preparing a pharmaceutical composition with the abovementioned properties, and processes for the preparation thereof.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: April 16, 2013
    Assignees: Boehringer Ingelheim Pharma GmbH & Co. KG, Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Georg Dahmann, Frank Himmelsbach, Bernd Krist, Martin Lenter, Alexander Pautsch, Gisela Schnapp, Martin Steegmaier, Helmut Wittneben, Anthony S. Prokopowicz, Walter Spevak, Andreas Schoop, Steffen Steurer
  • Publication number: 20130059830
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 16, 2011
    Publication date: March 7, 2013
    Inventors: Fa-Xiang Ding, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Cangming Yang
  • Patent number: 8377924
    Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 21, 2010
    Date of Patent: February 19, 2013
    Assignee: Rigel Pharmaceuticals Inc.
    Inventors: Rajinder Singh, Huí Li, Haoran Zhao, Rao Kolluri, Kin Tso, John Ramphal, Shihai Gu, Carlos Valdez, Jing Zhang, Emily Stauffer, Matthew Duncton, Salvador Alvarez
  • Publication number: 20120264704
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Application
    Filed: October 26, 2007
    Publication date: October 18, 2012
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Metin Akbaba, Mario Jeske
  • Publication number: 20120258959
    Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.
    Type: Application
    Filed: June 12, 2012
    Publication date: October 11, 2012
    Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
  • Publication number: 20120252790
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: May 15, 2012
    Publication date: October 4, 2012
    Inventors: Patrick René Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
  • Patent number: 8258129
    Abstract: The present invention encompasses compounds of general formula (1) wherein X and R1 to R3 are as defined in the disclosure, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: July 5, 2007
    Date of Patent: September 4, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Harald Engelhardt, Gerd Bader, Guido Boehmelt, Ralph Brueckner, Thomas Gerstberger, Maria Impagnatiello, Daniel Kuhn, Otmar Schaaf, Heinz Stadtmueller, Irene Waizenegger, Andreas Zoephel
  • Publication number: 20120208797
    Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Application
    Filed: August 11, 2010
    Publication date: August 16, 2012
    Applicants: SANOFI, MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
  • Publication number: 20120156219
    Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.
    Type: Application
    Filed: February 22, 2012
    Publication date: June 21, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Hiromu HABASHITA, Masaya KOKUBO, Shiro SHIBAYAMA, Hideaki TADA, Tatsuya TANIHIRO
  • Publication number: 20120129840
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Application
    Filed: August 5, 2010
    Publication date: May 24, 2012
    Applicant: KATHOLIEKE UNIVERSITEIT LEUVEN
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Publication number: 20120121727
    Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Kai THEDE, Ingo FLAMME, Felix OEHME, Jens-Kerim ERGÜDEN, Friederike STOLL, Joachim SCHUHMACHER, Hanno WILD, Peter KOLKHOF, Hartmut BECK, Jörg KELDENICH, Metin AKBABA, Mario JESKE
  • Publication number: 20120088750
    Abstract: The present invention provides a compound of the following formula and salts thereof: Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
    Type: Application
    Filed: October 7, 2011
    Publication date: April 12, 2012
    Applicant: BIOTA EUROPE LTD.
    Inventors: James T. PALMER, Christopher James LUNNIS, Daniel A. OFFERMANN, Lorraine Claire AXFORD, Michael BLAIR, Dale MITCHELL, Nicholas PALMER, Christopher STEELE, John ATHERALL, David WATSON, David HAYDON, Lloyd CZAPLEWSKI, David DAVIES, Ian COLLINS
  • Patent number: 8153625
    Abstract: The compound represented by formulae (I) and (II), the salt thereof, the N-oxide thereof or the solvate thereof, or the prodrug thereof and the pharmaceutical composition comprising thereof have a CXCR4-regulating effect, and they are effective in treatment and prevention of various inflammatory disease, various allergic disease, acquired immunodeficiency syndrome infection with human immunodeficiency virus, or agents for regeneration therapy. (wherein ring A represents a nitrogen-containing heterocyclic group which may have a substituent(s); ring B represents a homocyclic group which may have a substituent(s) or a heterocyclic group which may have a substituent(s); and Y represents a hydrocarbon group which may have a substituent(s), a heterocyclic group which may have a substituent(s), an amino group which may be protected, a hydroxyl group which may be protected or a mercapto group which may be protected; T represents ring A or an amino group which may be protected.).
    Type: Grant
    Filed: May 10, 2010
    Date of Patent: April 10, 2012
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hiromu Habashita, Masaya Kokubo, Shiro Shibayama, Hideaki Tada, Tatsuya Tanihiro
  • Patent number: 8138339
    Abstract: The present invention is directed to 2-cycloalkylamino-4-arylamino-benzamide compounds of formula I pharmaceutically acceptable salts thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as cardiovascular disease, inflammatory disease, autoimmune disease and cell proliferative disorder.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: March 20, 2012
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Qing Xu, Mukund Mehrotra, Jack W. Rose, Wolin Huang, Chandrasekar Venkataramani, Anjali Pandey
  • Publication number: 20120053164
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD. Formula (I), wherein A is selected from among a single bond, ?CH—, —CH2—, —O—, —S—, and —NH—; wherein n is 1, 2 or 3; wherein Z is C or N, the other variables are as defined in the claims, as well as in form of their acid addition salts with pharmacologically acceptable acids.
    Type: Application
    Filed: December 17, 2009
    Publication date: March 1, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Thomas Trieselmann, Patrick Tielmann, Stefan Scheuerer, Silke Hobbie, Frank Buettner
  • Publication number: 20120028952
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: January 24, 2011
    Publication date: February 2, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Siegfried SCHNEIDER, Dirk KESSLER, Lars van der VEEN, Tobias WUNBERG
  • Publication number: 20110306602
    Abstract: The present invention relates to inhibitors of general Formula (I) of cyclin-dependent kinases and therapeutic applications thereof. Furthermore, the invention relates to compounds for preventing and/or treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.
    Type: Application
    Filed: April 24, 2008
    Publication date: December 15, 2011
    Inventors: Philipp Wabnitz, Heike Schauerte, Hans Allgeier, Lutz Zeitlmann, Anke Mueller, Martin Augustin, Michael A. Pleiss, Gabriele Stumm, Axel Choidas, Bert Klebl, Gerhard Mueller, Wilfried Schwab, Joelle Le, Jackie Macritchie, Don Simpson
  • Publication number: 20110263570
    Abstract: The present invention relates to Pyriraidine Derivatives of formula (I), compositions comprising a Pyrimidine Derivative, and methods of using the Pyrimidine Derivatives for treating or preventing obesity, diabetes, a diabetic complication, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G protein-coupled receptor (GPCR) in a patient.
    Type: Application
    Filed: December 21, 2009
    Publication date: October 27, 2011
    Applicant: Schering Corporation
    Inventors: Bernard R. Neustadt, Andrew Stamford, Jinsong Hao, Charles Lee Jayne, Yan Xia
  • Publication number: 20110245156
    Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.
    Type: Application
    Filed: December 9, 2009
    Publication date: October 6, 2011
    Applicant: CYTOKINE PHARMASCIENCES, INC.
    Inventor: Thais M. Sielecki-Dzurdz
  • Publication number: 20110207715
    Abstract: The present invention is directed to disubstituted azepan and oxazepan amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: October 15, 2009
    Publication date: August 25, 2011
    Inventors: Christopher D. Cox, Mark E. Fraley, John D. Schreier
  • Patent number: RE43481
    Abstract: To provide a compound which has an anticoagulation action based upon inhibition of activated blood coagulation factor X and is useful as an anticoagulant or an agent for prevention and treatment of diseases caused by thrombus or embolus. A diazepan derivative such as 4-[(3-carbamimidoylphenylamino)methyl]-3-[4-(4-methyl-1,4-diazepan-1-yl)benzoylamino]benzoic acid and 3-hydroxy-4?-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide or a salt thereof is an effective ingredient.
    Type: Grant
    Filed: September 3, 2008
    Date of Patent: June 19, 2012
    Assignee: Astellas Pharma Inc.
    Inventors: Fukushi Hirayama, Hiroyuki Koshio, Tsukasa Ishihara, Norio Seki, Shunichiro Hachiya, Keizo Sugasawa, Ryota Shiraki, Yuji Koga, Yuzo Matsumoto, Takeshi Shigenaga, Souichirou Kawazoe
  • Patent number: RE44205
    Abstract: Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, cycloalkenyl, or heteroaryl; X is alkylene or —C(O)CH2—; Y is —N(R2)CH2CH2N(R)3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—NH—, or optionally substituted ?m and n are 2-3, and Q is nitrogen or optionally substituted carbon; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl, R6—C(O)—, R6—SO2—, R6—OC(O)—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)—, ?phenyl-CH(OH)—, or phenyl-C(?NOR2)—; or when Q is CH, phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl or substituted phenyl; and R2, R3, R6, R7, and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them; also disclosed are a processes for preparing intermediates useful for preparing comp
    Type: Grant
    Filed: April 6, 2012
    Date of Patent: May 7, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Bernard R. Neustadt, Neil Lindo, William J. Greenlee, Deen Tulshian, Lisa S. Silverman, Yan Xia, Craig D. Boyle, Samuel Chackalamannil