Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/233.8)
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Publication number: 20150031694Abstract: The invention provides compounds of formula (I): wherein R1-R7 and W have any of the values defined in the specification, and salts thereof. The compounds have good solubility and are useful for treating bacterial infections.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Inventors: Edmond J. LaVoie, Ajit Parhi, Yongzheng Zhang, Daniel S. Pilch, Malvika Kaul
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Publication number: 20150030588Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase a and/or a receptor tyrosine kinase (RTK) in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or an RTK in a subject. In yet another aspect, a method of inhibiting phosphorylation of Akt (S473) in a cell is set forth.Type: ApplicationFiled: November 12, 2012Publication date: January 29, 2015Inventors: Katayoun Jessen, Xin Guo, Pingda Ren, Christian Rommel, Yi Liu
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Publication number: 20150011541Abstract: The present invention relates to compounds having a pipecolate sulfonamide scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said pipecolate sulfonamide compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 8, 2015Inventors: Ranganath Gopalakrishnan, Felix Hausch
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Publication number: 20150011528Abstract: Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.Type: ApplicationFiled: September 21, 2012Publication date: January 8, 2015Applicant: YUHAN CORPORATIONInventors: Youn Hur, Dong-Hyun Kim, Eun-Kyung Kim, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Se-Woong Oh, Dong-Kyun Kim, Kyoung-Kyu Ahn
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Publication number: 20150005284Abstract: Compounds of the formula I in which R1, R2 and X have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: January 3, 2013Publication date: January 1, 2015Applicant: Merck Patent GmbHInventors: Hans Michael Eggenweiler, Guenter Hoelzemann, Dieter Dorsch
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Publication number: 20150004181Abstract: The present patent application concerns new ligands of the H4-receptor, their process of preparation and their therapeutic use.Type: ApplicationFiled: June 27, 2014Publication date: January 1, 2015Inventors: Isabelle BERREBI-BERTRAND, Xavier BILLOT, Thierry CALMELS, Marc CAPET, Denis DANVY, Stéphane KRIEF, Olivier LABEEUW, Jeanne-Marie LECOMTE, Nicolas LEVOIN, Xavier LIGNEAU, Philippe ROBERT, Jean-Charles SCHWARTZ
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Publication number: 20150005299Abstract: The present invention relates to substituted pyrrole compounds and compositions comprising substituted pyrrole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted pyrrole compound of the invention, or a pharmaceutical composition comprising such a compound.Type: ApplicationFiled: July 2, 2014Publication date: January 1, 2015Inventors: Dinesh U. Chimmanamada, Weiwen Ying
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Publication number: 20140378450Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Novartis AGInventors: Giorgio CARAVATTI, Robin Alec FAIRHURST, Pascal FURET, Clive MCCARTHY, Heinrich RUEEGER, Frank Hans SEILER, Frédéric STAUFFER
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Patent number: 8912177Abstract: A method of treating polycystic kidney disease in a subject comprises administering to the subject an effective amount of a compound represented by Structural Formula (1): or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 3, 2008Date of Patent: December 16, 2014Assignee: Genzyme CorporationInventors: Thomas A. Natoli, Oxana Ibraghimov-Beskrovnaya, John P. Leonard, Nelson S. Yew, Seng H. Cheng
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Patent number: 8906852Abstract: This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions.Type: GrantFiled: April 8, 2011Date of Patent: December 9, 2014Assignee: MethylGene Inc.Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frédéric Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
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Patent number: 8906902Abstract: The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: GrantFiled: March 21, 2013Date of Patent: December 9, 2014Assignee: Biota Europe LimitedInventors: Christopher James Lunniss, James T. Palmer, Gary Robert William Pitt, David Davies, Lorraine Claire Axford
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Publication number: 20140350009Abstract: Topical formulations and method of using the same are provided. The topical formulation comprises a pyrazolylbenzothiazole derivative of the following formula (1) wherein X, R1, R2, R3 and R4 are described herein.Type: ApplicationFiled: May 6, 2014Publication date: November 27, 2014Applicant: Dermira (Canada), Inc.Inventors: Zaihui Zhang, Timothy S. Daynard, Shisen Wang, Xinyao Du, Gregory B. Chopiuk, Jun Yan, Jianxin Chen, Serguei V. Sviridov
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Publication number: 20140336108Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Xialing Guo, Zhen Zhu
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Publication number: 20140336174Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: ApplicationFiled: April 17, 2014Publication date: November 13, 2014Applicant: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
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Patent number: 8883784Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: August 12, 2013Date of Patent: November 11, 2014Assignee: AbbVie Inc.Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
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Publication number: 20140322195Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: October 24, 2012Publication date: October 30, 2014Inventors: Matthew Voss, Hiroki Sone, Samuel Chackalamannil, Munetaka Ohkouchi
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Publication number: 20140315801Abstract: This invention relates to methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions using compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to the methods of treatment which utilize compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling.Type: ApplicationFiled: June 18, 2014Publication date: October 23, 2014Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frederic Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
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Patent number: 8865712Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: GrantFiled: December 20, 2013Date of Patent: October 21, 2014Assignee: Novartis AGInventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sebastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
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Patent number: 8859529Abstract: This invention relates to compounds of the Formula (I) as described herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: GrantFiled: September 22, 2009Date of Patent: October 14, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Ling Tong, Michael K. C. Wong, Brian J. Lavey, Joseph A. Kozlowski, Lei Chen, Razia K. Rizvi, Aneta Maria Kosinski, De-Yi Yang, Guowei Zhou, Kristen E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
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Publication number: 20140303154Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: June 19, 2014Publication date: October 9, 2014Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20140275003Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: NOVARTIS AGInventors: Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
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Publication number: 20140256712Abstract: Provided herein are multicyclic compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: March 12, 2014Publication date: September 11, 2014Applicants: Psychogenics Inc., Sunovion Pharmaceuticals Inc.Inventors: Liming SHAO, John Emmerson CAMPBELL, Michael Charles HEWITT, Una CAMPBELL, Taleen G. HANANIA
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Publication number: 20140235647Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: September 27, 2012Publication date: August 21, 2014Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
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Publication number: 20140228352Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: March 24, 2014Publication date: August 14, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
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Publication number: 20140219989Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: July 3, 2012Publication date: August 7, 2014Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
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Publication number: 20140213538Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: January 15, 2014Publication date: July 31, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
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Patent number: 8791111Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in Claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: September 19, 2008Date of Patent: July 29, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Publication number: 20140200197Abstract: The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 9, 2013Publication date: July 17, 2014Inventors: JOHN A. MCCAULEY, CHRISTIAN BEAULIEU, DAVID J. BENNETT, CHRISTOPHER J. BUNGARD, RONALD K. CHANG, SHELDON CRANE, THOMAS J. GRESHOCK, LI HAO, KATE HOLLOWAY, JESSE J. MANIKOWSKI, DANIEL MCKAY, CARMELA MOLINARO, OSCAR MIGUEL MORADEI, PHILIPPE G. NANTERMET, CHRISTIAN NADEAU, TUMMANAPALLI SATYANARAYANA, WILLIAM SHIPE, SANJAY KUMAR SINGH, VOUY LINH TRUONG, SIVALENKA VIJAYARADHI, PETER D. WILLIAMS, CATHERINE M. WISCOUNT
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Publication number: 20140200215Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: March 12, 2013Publication date: July 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8772285Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: GrantFiled: October 25, 2012Date of Patent: July 8, 2014Assignee: High Point Pharmaceuticals, LLCInventors: Florencio Zaragoza Dorwald, Inge Thoger Christensen
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Patent number: 8765746Abstract: This invention provides compounds of formula I-A or I-B: wherein HY, G1, G2, R2, R12, W1, W2, n, and Ring A are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: October 13, 2011Date of Patent: July 1, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Hong Myung Lee, Todd B. Sells, Zhan Shi, Leo R. Takaoka, Stepan Vyskocil, Tianlin Xu
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Publication number: 20140179632Abstract: This invention relates to methods for inhibiting kinase activity and/or inhibiting angiogenesis and/or treating a disease responsive to inhibition of kinase activity and/or treating a cell proliferative disease and/or treating an ophthalmic disease, condition or disorder treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions comprising administering novel compounds that inhibit protein tyrosine kinase activity.Type: ApplicationFiled: February 28, 2014Publication date: June 26, 2014Applicant: MethylGene Inc.Inventors: Michael Mannion, Stephane Raeppel, Stephen William Claridge, Frederic Gaudette, Lijie Zhan, Ljubomir Isakovic, Oscar Mario Saavedra, Tetsuyuki Uno, Masashi Kishida, Arkadii Vaisburg
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Publication number: 20140178360Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.Type: ApplicationFiled: February 27, 2014Publication date: June 26, 2014Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Mann-Yan KUO, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
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Publication number: 20140162998Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating 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: ApplicationFiled: February 10, 2014Publication date: June 12, 2014Applicant: Jikai Biosciences, Inc.Inventor: Yu GE
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Publication number: 20140155379Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.Type: ApplicationFiled: December 20, 2013Publication date: June 5, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
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Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as Janus kinase inhibitors
Patent number: 8741895Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: GrantFiled: May 8, 2013Date of Patent: June 3, 2014Assignee: Incyte CorporationInventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks -
Publication number: 20140142097Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseasesType: ApplicationFiled: April 11, 2012Publication date: May 22, 2014Applicant: Merck Patent GmbHInventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
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Patent number: 8729075Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: GrantFiled: February 7, 2013Date of Patent: May 20, 2014Assignee: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas Natoli
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Publication number: 20140135305Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: December 12, 2013Publication date: May 15, 2014Applicant: PTC THERAPEUTICS, INC.Inventors: Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
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Patent number: 8710048Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: GrantFiled: April 23, 2012Date of Patent: April 29, 2014Assignee: Novartis AGInventors: James C. Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M. Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith B. Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
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Publication number: 20140113005Abstract: The present disclosure relates to pyrazine compounds of formula I: wherein L, n, R1, and R2 are as described in the specification. These compounds are useful as inhibitors of ATR protein kinase. The disclosure also relates to pharmaceutically acceptable compositions comprising the compounds of the disclosure; methods of treating of various diseases, disorders, and conditions using the compounds of the disclosure; processes for preparing the compounds of the disclosure; intermediates for the preparation of the compounds of the disclosure; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors.Type: ApplicationFiled: January 16, 2013Publication date: April 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20140107117Abstract: The present invention relates to substituted thienyl- and furanyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thienyl and furanyl-isoquinolinones and to their use in treating various diseases and disorders.Type: ApplicationFiled: December 13, 2013Publication date: April 17, 2014Inventors: Roberto Pellicciari, Flavio Moroni
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Publication number: 20140107116Abstract: The present invention is related to the use of benzothiazole derivatives for the manufacture of a medicament for the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). G is an unsubstituted or substituted pyrimidinyl group. L is an unsubstituted or substituted C1-C6-alkoxy, or an amino group, or an unsubstituted or a substituted 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S (e.g. a piperazine, a piperidine, a morpholine, a pyrrolidine). R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl or C1-C6-alkoxy, unsubstituted or substituted aryl, halogen, cyano or hydroxy.Type: ApplicationFiled: October 8, 2013Publication date: April 17, 2014Applicant: MERCK SERONO SAInventors: Pascale GAILLARD, Jean-Pierre GOTTELAND
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Publication number: 20140100223Abstract: The invention relates to compounds of Formula I or a pharmaceutically acceptable salt, ester or prodrug thereof:Type: ApplicationFiled: September 26, 2013Publication date: April 10, 2014Applicants: PRESIDENT & FELLOWS OF HARVARD COLLEGE, THE BROAD INSTITUTE, INC.Inventors: Mahmud Hussain, Daisuke Ito, Jason Law, Matthias Leiendecker, Ke Liu, Benito Munoz, Stuart Schreiber, Alykhan Shamji, Andrew Stern
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Patent number: 8680090Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: GrantFiled: July 8, 2013Date of Patent: March 25, 2014Assignee: Bristol-Myers Squibb CompanyInventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
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Publication number: 20140080826Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of 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 compounds of the present invention.Type: ApplicationFiled: September 25, 2013Publication date: March 20, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
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Publication number: 20140080825Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 21, 2013Publication date: March 20, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20140080804Abstract: The invention provides novel substituted 6-arylamino pyridone carboxamides represented by Formula I, or a pharmaceutically acceptable salt, solvate, poly-morph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.Type: ApplicationFiled: November 1, 2011Publication date: March 20, 2014Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Shixin Wang, Rong Yu, Wei Hu, Zhi Liang, Xijie Liu, Quan Hu
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Publication number: 20140073584Abstract: The invention relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as PI-3 kinase.Type: ApplicationFiled: September 30, 2013Publication date: March 13, 2014Applicant: SIGNALRX PHARMACEUTICALS, INC.Inventors: Guillermo A. Morales, Kevin Weber, Jessica Newblom, Joseph R. Garlich
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Publication number: 20140073640Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: August 12, 2013Publication date: March 13, 2014Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao