The Other Cyclo In The Bicyclo Ring System Is A Pyridine Ring (including Hydrogenated) (e.g., Pyrido[2,3-d]pyrimidine, Etc.) Patents (Class 514/264.1)
  • Patent number: 10829487
    Abstract: The present invention encompasses compounds of formula (I) wherein the groups R1 to R4, A and p have the meanings given in the claims and specification, their use as inhibitors of SOS1, pharmaceutical compositions which contain compounds of this kind and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: November 10, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Juergen Ramharter, Christiane Kofink, Heinz Stadtmueller, Tobias Wunberg
  • Patent number: 10800783
    Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R2A, R2B, R3, R4, R5A, R5B, R6, R7, R8, R9, p, q and r are as defined herein, 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: Grant
    Filed: January 17, 2019
    Date of Patent: October 13, 2020
    Assignee: Pfizer Inc.
    Inventors: Douglas Carl Behenna, Ping Chen, Kevin Daniel Freeman-Cook, Robert Louis Hoffman, Mehran Jalaie, Asako Nagata, Sajiv Krishnan Nair, Sacha Ninkovic, Martha Alicia Ornelas, Cynthia Louise Palmer, Eugene Yuanjin Rui
  • Patent number: 10781178
    Abstract: The present application provides compounds useful in methods of treating neurological disorders such as Alzheimer's disease, and cancer such as prostate cancer. Also provided herein are radiolabeled compounds useful for imaging techniques, and techniques for diagnosis and monitoring of treatment of neurological disorders and cancer. An exemplary radiolabeled compound provided herein is useful as a radiotracer for positron emission tomography or single-photon emission computed tomography. Methods for preparing radiolabeled compounds and methods for preparing unlabeled compounds are also provided.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: September 22, 2020
    Assignee: The General Hospital Corporation
    Inventors: Neil Vasdev, Huan Steven Liang
  • Patent number: 10745420
    Abstract: The present invention relates to tetrahydropyrido[4,3-d]pyrimidine based compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
    Type: Grant
    Filed: August 13, 2019
    Date of Patent: August 18, 2020
    Assignees: Board of Regents, The University of Texas System, ChemPartner Corporation
    Inventors: Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Michael Garrett Johnson, Sarah Lively
  • Patent number: 10632126
    Abstract: The present disclosure relates to bicyclic heterocycles of Formula (I?), and pharmaceutical compositions of the same, that are inhibitors of the FGFR3 and/or FGFR4 enzyme and are useful in the treatment of FGFR-associated diseases.
    Type: Grant
    Filed: February 15, 2019
    Date of Patent: April 28, 2020
    Assignee: Incyte Corporation
    Inventors: Alexander Sokolsky, Liangxing Wu, Wenqing Yao
  • Patent number: 10618902
    Abstract: The present invention provides substituted pyrido[2,3-d]pyrimidine compounds useful as inhibitors of protein kinases, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 28, 2018
    Date of Patent: April 14, 2020
    Assignees: Celgene CAR LLC, Sanofi
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson, Darren Harvey, Andrew Scholte, Sachin Maniar
  • Patent number: 10457682
    Abstract: Disclosed are small molecules and pharmaceutical compositions comprising them that can be used in treating diseases associated with the major histocompatibility complex (MHC) molecule MR1.
    Type: Grant
    Filed: October 20, 2017
    Date of Patent: October 29, 2019
    Inventors: David Lewinsohn, Melanie Harriff, Aaron Nilsen, Haihong Jin, Erin Adams, Cara Froyd, Curtis McMurtrey, William Hildebrand
  • Patent number: 10421765
    Abstract: The present invention relates to tetrahydropyrido[4,3-d]pyrimidine based compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.
    Type: Grant
    Filed: May 25, 2018
    Date of Patent: September 24, 2019
    Assignees: Board of Regents, The University of Texas System, ChemPartner Corporation
    Inventors: Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Michael Garrett Johnson, Sarah Lively
  • Patent number: 10377738
    Abstract: This invention relates to pyridone derivatives, processes for their preparation, phamaceutical compositions, and their use in therapy.
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: August 13, 2019
    Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANY
    Inventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 10300067
    Abstract: A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof
    Type: Grant
    Filed: February 12, 2018
    Date of Patent: May 28, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Shinichi Aoki, Masanori Asai, Takahiro Asai, Hiroyoshi Yamanaka, Suguru Dohi
  • Patent number: 10233188
    Abstract: This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R2A, R2B, R3, R4, R5A, R5B, R6, R7, R8, R9, p, q and r are as defined herein, 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: Grant
    Filed: July 31, 2017
    Date of Patent: March 19, 2019
    Assignee: Pfizer Inc.
    Inventors: Kevin Daniel Freeman-Cook, Robert Louis Hoffman, Asako Nagata, Sacha Ninkovic
  • Patent number: 10196391
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3, Q, U, W, Z, X and Y are as described herein, compositions including the compounds and methods of using the compounds. These compounds are HbsAg inhibitors and are useful as medicaments for the treatment or prophylaxis of HBV infection.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: February 5, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Zhanling Cheng, Min Wang, Song Yang
  • Patent number: 9949979
    Abstract: The invention relates to new uses of PI3K inhibitors, wherein said inhibitors have an inhibitory action on the PI3K isoform delta for the treatment of immunopathology in a subject suffering from a disease or disorder selected from malaria, leishmaniasis, trypanosomiasis, toxoplasmosis and/or neurocysticercosis, via functional inhibition of TLR9 of the infected subject.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: April 24, 2018
    Assignee: Novartis AG
    Inventors: Nigel Graham Cooke, Paulo Antonio Fernandes Gomes Dos Santos, Pascal Furet, Christina Hebach, Klemens Hoegenauer, Gregory Hollingworth, Christoph Kalis, Ian Lewis, Alexander Baxter Smith, Nicolas Soldermann, Frederic Stauffer, Ross Strang, Frank Stowasser, Nicola Tuffilli, Anette Von Matt, Romain Wolf, Frederic Zecri
  • Patent number: 9889136
    Abstract: A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: February 13, 2018
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Shinichi Aoki, Masanori Asai, Takahiro Asai, Hiroyoshi Yamanaka, Suguru Dohi
  • Patent number: 9820989
    Abstract: The present invention relates to a method of treating ophthalmic diseases and conditions, e.g. diabetic retinopathy, age-related macular degeneration, retinopathy of prematurity, etc., in a subject comprising administering to said subject a therapeutically effective amount of at least one compound of formula I or a prodrug, pharmaceutically acceptable salt, racemic mixtures or enantiomers of said compound. The compounds of formula I are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.
    Type: Grant
    Filed: June 17, 2016
    Date of Patent: November 21, 2017
    Assignee: ALLERGAN, INC.
    Inventors: Clarence E. Hull, III, Thomas C. Malone
  • Patent number: 9663524
    Abstract: The present invention provides compounds of formula I-h: useful as inhibitors of protein kinases, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 30, 2017
    Assignees: Celgene CAR LLC, Sanofi
    Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson, Darren Harvey, Andrew Scholte, Sachin Maniar
  • Patent number: 9655854
    Abstract: This invention relates to sustained release dosage forms comprising {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, or a pharmaceutically acceptable salt thereof, and doses and methods related thereto.
    Type: Grant
    Filed: August 6, 2014
    Date of Patent: May 23, 2017
    Assignee: Incyte Corporation
    Inventors: Krishnaswamy Yeleswaram, Bhavnish Parikh, Dilip P. Modi, Trupti Sheth
  • Patent number: 9540371
    Abstract: In one aspect, the invention relates to 3-benzylquinazolin-4(3H)-one analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor 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: April 28, 2014
    Date of Patent: January 10, 2017
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Shaun R. Stauffer, Joseph David Panarese
  • Patent number: 9464080
    Abstract: The present invention relates to the cosmetic use, as agent for preventing and/or treating an aesthetic defect in the skin and/or its appendages that is associated with an imbalance in the differentiation and/or proliferation of the cells of an epidermis, of an effective amount of at least one compound represented by one of the general formulae, (Ia) or (Ib)
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: October 11, 2016
    Assignee: L'Oreal
    Inventors: Xavier Marat, Benoit Muller, Agnès Thomas-Collignon, Dominique Bernard
  • Patent number: 9399021
    Abstract: Disclosed are novel pharmaceutical compositions containing N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: July 26, 2016
    Assignee: Novartis AG
    Inventors: Douglas J. DeMarini, Francisco Henriquez, Ngocdiep T. Le, Lihong Wang
  • Patent number: 9315449
    Abstract: The present invention relates to substituted pyrazole compounds, methods for their discovery, and their research and therapeutic uses, and pharmaceutical Formulations thereof. In particular, the present invention provides substituted pyrazole compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.
    Type: Grant
    Filed: November 12, 2010
    Date of Patent: April 19, 2016
    Assignees: DUKE UNIVERSITY, CHAPERONE THERAPEUTICS, INC
    Inventors: Dennis J Thiele, Daniel W Neef, Jose S Mendoza
  • Patent number: 9206173
    Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: December 8, 2015
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
  • Patent number: 9181243
    Abstract: The present invention relates to a crystalline Form M of trametinib dimethyl sulfoxide solvate. Comparing with the prior art, Form M is a more stable crystalline form with better particle size distribution and good flowability and is non-hygroscopic. Therefore, it is more suitable for formulation. The present invention also relates to pharmaceutical compositions thereof, methods of making and using thereof.
    Type: Grant
    Filed: June 30, 2014
    Date of Patent: November 10, 2015
    Assignee: Hangzhou Pushai Pharmaceutical Technology Co. Ltd.
    Inventors: Chenyang Hu, Xiaoxia Sheng, Xiaohong Sheng
  • Patent number: 9155706
    Abstract: Disclosed are novel pharmaceutical compositions containing N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2, 4, 7-trioxo-3, 4, 6, 7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide dimethyl sulfoxide solvate, methods of using the compositions in therapy and processes for preparing the same.
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: October 13, 2015
    Assignee: Novartis AG
    Inventors: Douglas J. DeMarini, Francisco Henriquez, Ngocdiep T. Le, Lihong Wang
  • Publication number: 20150148356
    Abstract: The present invention relates to the cosmetic use, as agent for preventing and/or treating an aesthetic defect in the skin and/or its appendages that is associated with an imbalance in the differentiation and/or proliferation of the cells of an epidermis, of an effective amount of at least one compound represented by one of the general formulae, (Ia) or (Ib)
    Type: Application
    Filed: June 5, 2013
    Publication date: May 28, 2015
    Inventors: Xavier Marat, Benoit Muller, Agnès Thomas-Collignon, Dominique Bernard
  • Publication number: 20150133424
    Abstract: The present disclosure is related to heteroaryl compounds as MEK inhibitors. These compounds include heteroaryl compounds of formula I, their pharmaceutically acceptable salts, combinations with suitable medicament and pharmaceutical compositions thereof. The present disclosure also includes processes of preparation of the compounds and their use in methods of treatment.
    Type: Application
    Filed: March 11, 2013
    Publication date: May 14, 2015
    Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
  • Publication number: 20150126533
    Abstract: Disclosed are methods for the treatment of non-BRAFV600E mutant melanoma in patients in need of such treatment. The methods comprise administering to such a patient a MEK inhibitor such as (R)-3-(2,3-dihydroxypropyl)-6-fluoro-5-((2-fluoro-4-iodophenyl)amino)-8-methylpyrido[2,3-d]pyrimidine-4,7(3H,8H)-dione (TAK-733) and a RAF inhibitor selected from N-{7-cyano-6-[4-fluoro-3-({[3-(trifluoromethyl)phenyl]acetyl}amino)phenoxy]-1,3-benzothiazol-2-yl}cyclopropanecarboxamide (TAK-632) and (R)-2-(1-(6-amino-5-chloropyrimidine-4-carboxamido)ethyl)-N-(5-chloro-4-(trifluoromethyl)pyridin-2-yl)thiazole-5-carboxamide (MLN2480). Also disclosed are medicaments for use in the treatment of such melanoma.
    Type: Application
    Filed: March 29, 2013
    Publication date: May 7, 2015
    Inventors: Takeo Arita, Shuntarou Tsuchiya
  • Patent number: 9023858
    Abstract: The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: May 5, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Matsunaga, Hideo Suzuki, Kouhei Asano, Hidekazu Tokuhara, Takeshi Yamamoto, Rei Okamoto
  • Publication number: 20150111869
    Abstract: The invention provides combinations comprising a MEK inhibitor (such as GDC-0973 or GDC-0623), or a pharmaceutically acceptable salt thereof and an ERK inhibitor (such as GDC-0994). The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.
    Type: Application
    Filed: August 29, 2014
    Publication date: April 23, 2015
    Applicant: Genentech, Inc.
    Inventors: Marcia Belvin, John Moffat, Mark Merchant
  • Publication number: 20150111904
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. melanoma.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Patent number: 9006255
    Abstract: Compounds of the formula I in which R, X, L2 and A1-A6 have the meanings indicated in Claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.
    Type: Grant
    Filed: September 22, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Patent GmbH
    Inventor: Markus Klein
  • Publication number: 20150094321
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.
    Type: Application
    Filed: May 6, 2014
    Publication date: April 2, 2015
    Applicant: GlaxoSmithKline LLC
    Inventors: Melissa DUMBLE, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie LaQuerre
  • Publication number: 20150079154
    Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.
    Type: Application
    Filed: July 9, 2012
    Publication date: March 19, 2015
    Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBH
    Inventors: Lars Zender, Ramona Rudalska, Daniel Dauch
  • Publication number: 20150072955
    Abstract: The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
    Type: Application
    Filed: October 14, 2014
    Publication date: March 12, 2015
    Applicant: Resverlogix Corp.
    Inventor: Henrik C. Hansen
  • Publication number: 20150072974
    Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.
    Type: Application
    Filed: May 9, 2013
    Publication date: March 12, 2015
    Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
  • Patent number: 8962637
    Abstract: The present invention relates to substituted aromatic bicyclic compounds containing pyrimidine and pyridine rings of formula (I) having the structure as well as pharmaceutically acceptable salts thereof. The compounds of the present invention are useful as tyrosine kinase inhibitors, preferably SRC family kinases (SFKs) inhibitors, in particular as multi SFK/JAK. kinases inhibitors and even preferably as dual c-SRC/JAK kinases inhibitors, thereby inhibiting the STAT3 activation and therefore abnormal growth of particular cell types. Notably, the compounds of the present invention are useful for the treatment or inhibition of certain diseases that are the result of deregulation of STAT3.
    Type: Grant
    Filed: January 14, 2013
    Date of Patent: February 24, 2015
    Assignees: Debiopharm S.A., Aurigene Discovery Technologies Ltd.
    Inventors: Andrès Mc Allister, Maximilien Murone, Saumitra Sengupta, Shankar Jayaram Shetty
  • Patent number: 8957062
    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. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: February 17, 2015
    Assignee: 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: 8952018
    Abstract: A novel combination comprising the MEK inhibitor N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethyl; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, with a B-Raf inhibitor, particularly N-{3-[5-(2-Amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same and methods of using such combinations and compositions in the treatment of conditions in which the inhibition of MEK and/or B-Raf is beneficial, eg. cancer.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: February 10, 2015
    Assignee: GlaxosmithKline LLC
    Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
  • Publication number: 20150023955
    Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods.
    Type: Application
    Filed: September 15, 2014
    Publication date: January 22, 2015
    Applicant: THE ROCKEFELLER UNIVERSITY
    Inventors: Sohail Tavazoie, Nora Pencheva
  • Publication number: 20150018352
    Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.
    Type: Application
    Filed: March 7, 2013
    Publication date: January 15, 2015
    Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
  • Publication number: 20140364392
    Abstract: The present invention is directed to the provision of a multi-dose topical ophthalmic composition containing a 1H-indole-1-carboxamide and use thereof for treatment of ophthalmic disease. More specifically the present invention is directed to a multi-dose aqueous ophthalmic composition (e.g., a solution, a suspension, an emulsion or the like) containing a 1H-indole-1-carboxamide (e.g., N-(1-methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6-((methylamino) methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide) and use thereof for treatment of an ophthalmic disease at the back of the eye such as age related macular degeneration (AMD).
    Type: Application
    Filed: May 30, 2014
    Publication date: December 11, 2014
    Applicant: Novartis AG
    Inventors: Malay Ghosh, Christopher Michael Adams, Stephanie Kay Dodd, Stephen Hedrick Poor
  • Publication number: 20140357617
    Abstract: The invention relates to novel heterocyclic acrylamide compounds (I), to the preparation of the compounds and intermediates used therein, to the use of the compounds as antibacterial medicaments and pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: August 20, 2014
    Publication date: December 4, 2014
    Applicant: FAB PHARMA S.A.S.
    Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
  • Publication number: 20140349995
    Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Christopher Michael ADAMS, Veronique DARSIGNY, Alec Nathanson FLYER, Christine Fang GELIN, Timothy Brian HURLEY, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Erik MEREDITH, Chang RAO, Michael H. SERRANO-WU, Catherine Fooks SOLOVAY
  • Publication number: 20140350020
    Abstract: The present application relates to novel fused pyrimidines and triazines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Application
    Filed: July 5, 2011
    Publication date: November 27, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
  • Publication number: 20140329798
    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: November 9, 2012
    Publication date: November 6, 2014
    Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
  • Publication number: 20140323506
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, or a pharmaceutically acceptable salt thereof, and N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy;-2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, to a human in need thereof.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Tona M. GILMER, Rakesh KUMAR, Li Liu
  • Publication number: 20140315808
    Abstract: A method of treating a disease or condition in which up-regulating GAGs is therapeutically beneficial is disclosed. The method comprises locally administering to a subject a therapeutically effective amount of an agent capable of down-regulating activity or expression of a component of the renin-angiotensin system.
    Type: Application
    Filed: June 30, 2014
    Publication date: October 23, 2014
    Inventors: Talia WEINSTEIN, Uzi GAFTER, Zvi NEVO, Dror ROBINSON, Zoharia EVRON
  • Publication number: 20140315902
    Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of 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: Application
    Filed: April 18, 2014
    Publication date: October 23, 2014
    Inventors: Yaping Sun, Liang Lu, Wenqing Yao, Jincong Zhuo, Liangxing Wu, Meizhong Xu, Ding-Quan Qian, Chunhong He, Fenglei Zhang
  • Patent number: 8865213
    Abstract: Disclosed herein are multiparticulate modified release pharmaceutical compositions comprising: (a) a first portion comprising an active ingredient, at least one surfactant and at least one release modifying agent and (b) a second portion comprising an active ingredient and optionally a release modifying agent. Particularly, the active ingredient in the first portion is a calcium channel blocker and the modified release composition is in the form of a multiparticulate tablet.
    Type: Grant
    Filed: December 29, 2010
    Date of Patent: October 21, 2014
    Assignees: USV Limited, Indicus Pharma LLC
    Inventors: Nitin Vadilal Sheth, Sunil Suresh Jog, Santosh Sadashiv Chothe, Sampada Hemant Tupe
  • Patent number: RE47739
    Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.
    Type: Grant
    Filed: July 27, 2018
    Date of Patent: November 26, 2019
    Assignee: Warner-Lambert Company LLC
    Inventors: Mark Barvian, Richard John Booth, John Quinn, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Lawrence Toogood, Scott Norman Vanderwel, Hairong Zhou