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)
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Patent number: 12195475Abstract: Disclosed herein are compounds of Formula (I?). Compounds of Formula (I?) inhibit, regulate and/or modulate kinase receptor, particularly Axl and Mer signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.Type: GrantFiled: June 13, 2023Date of Patent: January 14, 2025Assignee: Exelixis, Inc.Inventors: Lynne Canne Bannen, Minna Bui, Faming Jiang, Yong Wang, Wei Xu
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Patent number: 11173162Abstract: 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: GrantFiled: March 12, 2020Date of Patent: November 16, 2021Assignee: Incyte CorporationInventors: Alexander Sokolsky, Liangxing Wu, Wenqing Yao
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Patent number: 11174255Abstract: Identified compounds demonstrate protein kinase inhibitory activity. More specifically, the compounds having the structures below (I) are demonstrated to inhibit receptor interacting kinase 2 (RIPK2) and/or Activin-like kinase 2 (ALK2). Compounds that are either dual RIPK2/ALK2 inhibitors or that preferentially inhibit RIPK2 or ALK2 could provide therapeutic benefit.Type: GrantFiled: May 15, 2018Date of Patent: November 16, 2021Assignees: UNIVERSITY OF HOUSTON SYSTEM, TRUSTEES OF TUFTS COLLEGEInventors: Gregory Cuny, Sameer Nikhar, Alexei Degterev
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Patent number: 11083722Abstract: Provided herein is a combination therapy useful for the treatment breast cancer. The combination comprises an ER-alpha inhibitor and a CDK 4/6 inhibitor.Type: GrantFiled: March 16, 2018Date of Patent: August 10, 2021Assignee: EISAI R&D MANAGEMENT CO., LTD.Inventors: Craig D. Karr, Manav Korpal, Nathalie Rioux, Peter Gerard Smith
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Patent number: 10829487Abstract: 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: GrantFiled: December 20, 2018Date of Patent: November 10, 2020Assignee: Boehringer Ingelheim International GmbHInventors: Juergen Ramharter, Christiane Kofink, Heinz Stadtmueller, Tobias Wunberg
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Patent number: 10800783Abstract: 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: GrantFiled: January 17, 2019Date of Patent: October 13, 2020Assignee: 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
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Patent number: 10781178Abstract: 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: GrantFiled: February 9, 2016Date of Patent: September 22, 2020Assignee: The General Hospital CorporationInventors: Neil Vasdev, Huan Steven Liang
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Patent number: 10745420Abstract: 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: GrantFiled: August 13, 2019Date of Patent: August 18, 2020Assignees: Board of Regents, The University of Texas System, ChemPartner CorporationInventors: Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Michael Garrett Johnson, Sarah Lively
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Patent number: 10632126Abstract: 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: GrantFiled: February 15, 2019Date of Patent: April 28, 2020Assignee: Incyte CorporationInventors: Alexander Sokolsky, Liangxing Wu, Wenqing Yao
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Patent number: 10618902Abstract: 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: GrantFiled: August 28, 2018Date of Patent: April 14, 2020Assignees: Celgene CAR LLC, SanofiInventors: 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
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Patent number: 10457682Abstract: 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: GrantFiled: October 20, 2017Date of Patent: October 29, 2019Inventors: David Lewinsohn, Melanie Harriff, Aaron Nilsen, Haihong Jin, Erin Adams, Cara Froyd, Curtis McMurtrey, William Hildebrand
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Patent number: 10421765Abstract: 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: GrantFiled: May 25, 2018Date of Patent: September 24, 2019Assignees: Board of Regents, The University of Texas System, ChemPartner CorporationInventors: Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Michael Garrett Johnson, Sarah Lively
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Patent number: 10377738Abstract: This invention relates to pyridone derivatives, processes for their preparation, phamaceutical compositions, and their use in therapy.Type: GrantFiled: May 23, 2014Date of Patent: August 13, 2019Assignee: JANSSEN SCIENCES IRELAND UNLIMITED COMPANYInventors: David Craig McGowan, Pierre Jean-Marie Bernard Raboisson
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Patent number: 10300067Abstract: 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 thereofType: GrantFiled: February 12, 2018Date of Patent: May 28, 2019Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Shinichi Aoki, Masanori Asai, Takahiro Asai, Hiroyoshi Yamanaka, Suguru Dohi
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Patent number: 10233188Abstract: 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: GrantFiled: July 31, 2017Date of Patent: March 19, 2019Assignee: Pfizer Inc.Inventors: Kevin Daniel Freeman-Cook, Robert Louis Hoffman, Asako Nagata, Sacha Ninkovic
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Patent number: 10196391Abstract: 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: GrantFiled: June 30, 2017Date of Patent: February 5, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Zhanling Cheng, Min Wang, Song Yang
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Patent number: 9949979Abstract: 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: GrantFiled: December 14, 2012Date of Patent: April 24, 2018Assignee: Novartis AGInventors: 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
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Patent number: 9889136Abstract: 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 thereofType: GrantFiled: July 6, 2016Date of Patent: February 13, 2018Assignee: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Kazuhisa Minamiguchi, Shigeo Okajima, Shinichi Aoki, Masanori Asai, Takahiro Asai, Hiroyoshi Yamanaka, Suguru Dohi
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Patent number: 9820989Abstract: 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: GrantFiled: June 17, 2016Date of Patent: November 21, 2017Assignee: ALLERGAN, INC.Inventors: Clarence E. Hull, III, Thomas C. Malone
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Patent number: 9663524Abstract: 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: GrantFiled: March 14, 2014Date of Patent: May 30, 2017Assignees: Celgene CAR LLC, SanofiInventors: 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
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Patent number: 9655854Abstract: 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: GrantFiled: August 6, 2014Date of Patent: May 23, 2017Assignee: Incyte CorporationInventors: Krishnaswamy Yeleswaram, Bhavnish Parikh, Dilip P. Modi, Trupti Sheth
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Patent number: 9540371Abstract: 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: GrantFiled: April 28, 2014Date of Patent: January 10, 2017Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Shaun R. Stauffer, Joseph David Panarese
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Patent number: 9464080Abstract: 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: GrantFiled: June 5, 2013Date of Patent: October 11, 2016Assignee: L'OrealInventors: Xavier Marat, Benoit Muller, Agnès Thomas-Collignon, Dominique Bernard
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Patent number: 9399021Abstract: 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: GrantFiled: December 11, 2013Date of Patent: July 26, 2016Assignee: Novartis AGInventors: Douglas J. DeMarini, Francisco Henriquez, Ngocdiep T. Le, Lihong Wang
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Patent number: 9315449Abstract: 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: GrantFiled: November 12, 2010Date of Patent: April 19, 2016Assignees: DUKE UNIVERSITY, CHAPERONE THERAPEUTICS, INCInventors: Dennis J Thiele, Daniel W Neef, Jose S Mendoza
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Patent number: 9206173Abstract: 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: GrantFiled: May 27, 2010Date of Patent: December 8, 2015Assignee: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
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Patent number: 9181243Abstract: 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: GrantFiled: June 30, 2014Date of Patent: November 10, 2015Assignee: Hangzhou Pushai Pharmaceutical Technology Co. Ltd.Inventors: Chenyang Hu, Xiaoxia Sheng, Xiaohong Sheng
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Patent number: 9155706Abstract: 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: GrantFiled: December 11, 2013Date of Patent: October 13, 2015Assignee: Novartis AGInventors: Douglas J. DeMarini, Francisco Henriquez, Ngocdiep T. Le, Lihong Wang
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Publication number: 20150148356Abstract: 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: ApplicationFiled: June 5, 2013Publication date: May 28, 2015Inventors: Xavier Marat, Benoit Muller, Agnès Thomas-Collignon, Dominique Bernard
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Publication number: 20150133424Abstract: 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: ApplicationFiled: March 11, 2013Publication date: May 14, 2015Inventors: Bhavesh Dave, Rakesh Kumar Banerjee, Samiron Phukan, Abhijit Datta Khoje, Rajkumar Hangarge, Jitendra Sambhaji Jadhav, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20150126533Abstract: 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: ApplicationFiled: March 29, 2013Publication date: May 7, 2015Inventors: Takeo Arita, Shuntarou Tsuchiya
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Patent number: 9023858Abstract: 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: GrantFiled: July 22, 2011Date of Patent: May 5, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuyuki Matsunaga, Hideo Suzuki, Kouhei Asano, Hidekazu Tokuhara, Takeshi Yamamoto, Rei Okamoto
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Publication number: 20150111904Abstract: 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: ApplicationFiled: December 22, 2014Publication date: April 23, 2015Inventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
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Publication number: 20150111869Abstract: 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: ApplicationFiled: August 29, 2014Publication date: April 23, 2015Applicant: Genentech, Inc.Inventors: Marcia Belvin, John Moffat, Mark Merchant
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Patent number: 9006255Abstract: 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: GrantFiled: September 22, 2011Date of Patent: April 14, 2015Assignee: Merck Patent GmbHInventor: Markus Klein
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Publication number: 20150094321Abstract: 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: ApplicationFiled: May 6, 2014Publication date: April 2, 2015Applicant: GlaxoSmithKline LLCInventors: Melissa DUMBLE, Tona Gilmer, Rakesh Kumar, Peter F. Lebowitz, Shannon Renae Morris, Sylvie LaQuerre
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Publication number: 20150079154Abstract: 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: ApplicationFiled: July 9, 2012Publication date: March 19, 2015Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBHInventors: Lars Zender, Ramona Rudalska, Daniel Dauch
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Publication number: 20150072974Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and neurological disorders, including, but not limited to, e.g., psychosis, schizophrenia, depression, movement disorders, and Parkinson's disease.Type: ApplicationFiled: May 9, 2013Publication date: March 12, 2015Inventors: Phillip G. Jones, Robert Lew, Kerry L. Spear, Linghong Xie
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Publication number: 20150072955Abstract: 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: ApplicationFiled: October 14, 2014Publication date: March 12, 2015Applicant: Resverlogix Corp.Inventor: Henrik C. Hansen
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Patent number: 8962637Abstract: 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: GrantFiled: January 14, 2013Date of Patent: February 24, 2015Assignees: Debiopharm S.A., Aurigene Discovery Technologies Ltd.Inventors: Andrès Mc Allister, Maximilien Murone, Saumitra Sengupta, Shankar Jayaram Shetty
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Patent number: 8957062Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Patent number: 8952018Abstract: 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: GrantFiled: March 5, 2014Date of Patent: February 10, 2015Assignee: GlaxosmithKline LLCInventors: Melissa Dumble, Rakesh Kumar, Sylvie Laquerre, Peter Lebowitz
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Publication number: 20150023955Abstract: The present invention discloses novel agents and methods for diagnosis and treatment of melanoma. Also disclosed are related arrays, kits, and screening methods.Type: ApplicationFiled: September 15, 2014Publication date: January 22, 2015Applicant: THE ROCKEFELLER UNIVERSITYInventors: Sohail Tavazoie, Nora Pencheva
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Publication number: 20150018352Abstract: 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: ApplicationFiled: March 7, 2013Publication date: January 15, 2015Inventors: Thomas Dineen, Charles Kreiman, Matthew Weiss, Stephanie Geuns-Meyer
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Publication number: 20140364392Abstract: 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: ApplicationFiled: May 30, 2014Publication date: December 11, 2014Applicant: Novartis AGInventors: Malay Ghosh, Christopher Michael Adams, Stephanie Kay Dodd, Stephen Hedrick Poor
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Publication number: 20140357617Abstract: 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: ApplicationFiled: August 20, 2014Publication date: December 4, 2014Applicant: FAB PHARMA S.A.S.Inventors: Vincent Gerusz, Sonia Escaich, Mayalen Oxoby, Alexis Denis
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Publication number: 20140349995Abstract: 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: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: 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
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Publication number: 20140350020Abstract: 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: ApplicationFiled: July 5, 2011Publication date: November 27, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li, Walter Kroh, Lars Bärfacker
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Patent number: RE47739Abstract: The present invention provides substituted 2-aminopyridines useful in treating cell proliferative disorders.Type: GrantFiled: July 27, 2018Date of Patent: November 26, 2019Assignee: Warner-Lambert Company LLCInventors: Mark Barvian, Richard John Booth, John Quinn, III, Joseph Thomas Repine, Derek J. Sheehan, Peter Lawrence Toogood, Scott Norman Vanderwel, Hairong Zhou
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Patent number: RE48731Abstract: The invention relates to dihydronaphthyridines and related compounds; compositions comprising an effective amount of a dihydronaphthyridine or a related compound; and methods for treating or preventing proliferative diseases comprising the administration of an effective amount of a dihydronaphthyridine or a related compound.Type: GrantFiled: April 17, 2019Date of Patent: September 14, 2021Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Michael D. Kaufman, Peter A. Petillo