Four Or More Ring Nitrogens In The Tricyclo Ring System Patents (Class 544/251)
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Publication number: 20140350036Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.Type: ApplicationFiled: January 11, 2013Publication date: November 27, 2014Inventors: Robert Vince, Abbas Raza, Christine Dreis
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Patent number: 8894989Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly(ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radiosensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.Type: GrantFiled: June 19, 2012Date of Patent: November 25, 2014Assignee: Eisai Inc.Inventors: Weizheng Xu, Greg Delahanty, Ling Wei, Jie Zhang
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Publication number: 20140335048Abstract: This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1): or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.Type: ApplicationFiled: July 25, 2014Publication date: November 13, 2014Applicant: ONCOCEUTICS, INC.Inventors: Martin STOGNIEW, Joshua E. ALLEN
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Publication number: 20140329800Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.Type: ApplicationFiled: December 13, 2012Publication date: November 6, 2014Inventors: Daxin Gao, Heping Yang, Yajun Yu
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Publication number: 20140323726Abstract: Provided herein are synthetic methods for preparing a compound of formula (I): Also provided herein are synthetic methods for preparing a compound of formula (XIII): The disclosure also provides useful intermediates, derivatives, prodrugs, and pharmaceutically acceptable salts, solvates and hydrates of the formula (I) and formula (XIII) compounds. These compounds are useful for treating diseases associated with molybdenum cofactor deficiency.Type: ApplicationFiled: February 17, 2012Publication date: October 30, 2014Applicant: ALEXION PHARMA INTERNATIONAL SÀRLInventors: Xiangtian Long, Danmei Dai, Andreas Brunner, Derek Kevin Watt, Keith Clinch, Sylvia Myrna Baars, Rachel Anne Dixon, Gillian Mary Little, Cyrille Abel Sébastien Landreau, Nicolas Georges Rene Proisy
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Publication number: 20140315888Abstract: The present invention relates to novel heterocyclic compounds useful in preparing drugs for treatment of diseases associated with various functions of the histamine 4 receptor. Especially, the said drugs are useful for treatment of inflammatory diseases, allergy, pain, nasal polyps, rhinitis, chronic sinusitis, nasal congestion, nasal itch, asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis, eczema, pruritus, itchy skin, urticaria, idiopathic chronic urticaria, scleroderma, conjunctivitis, keratoconjunctivitis, ocular inflammation, dry eye, cardiac dysfunction, arrhythmia, atherosclerosis, multiple sclerosis, inflammatory bowel disease (including colitis, Crohn's disease, ulcerative colitis), inflammatory pain, neuropathic pain, osteoarthritic pain, autoimmune thyroid disease, immune-mediated (also known as type I) diabetes, lupus, post-operative adhesions, vestibular disorders and cancer.Type: ApplicationFiled: September 28, 2012Publication date: October 23, 2014Applicant: C&C RESEARCH LABORATORIESInventors: Pil Su Ho, Dong Oh Yoon, Sun Young Han, Won Il Lee, Jung Sook Kim, Woul Seong Park, Sung Oh Ahn, Hye Jung Kim
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Patent number: 8853220Abstract: The present invention relates to methods for synthesizing energetic compounds and intermediates thereof. Specifically, the present invention relates to methods for synthesizing adamantanes and intermediates that are useful in such synthesis. Synthesized intermediates are useful in the synthesis of bicyclic and tricyclic substituted adamantanes. Examples of various intermediates are: acyclic 2-nitromalonaldehyde intermediates, 2,6,9-tri-substituted-4,8-dinitro-2,6,9-triazabicyclo[3.3.1]nona-3,7-dienes and 2,6-dinitro-4,8,9,10-tetra-aza-4,8,9,10-tetra-substituted adamantanes. Intermediates synthesized according to the methods of the present invention are useful toward the synthesis of tetraaza-adamantanes, which can serve as precursors to potentially superior new high-energy-density compounds (HEDCs). The tricyclic intermediate compound has a structure of Formula III: where R is one of a benzyl, 4-methoxybenzyl, acetyl, nitro, formyl, allyl, and a carboethoxyl group.Type: GrantFiled: February 25, 2011Date of Patent: October 7, 2014Assignee: The United States of America as Represented by the Secretary of the NavyInventors: Alfred G. Stern, Craig J. Diamond
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Patent number: 8846703Abstract: To provide a crystal of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90. The present invention provides a crystal of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a medicament comprising the same, an anticancer agent comprising the same, and the like.Type: GrantFiled: February 21, 2013Date of Patent: September 30, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Yasusi Ueda, Nobuyuki Suzuki, Hitoshi Ohki
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Patent number: 8846701Abstract: The present invention relates to pyrazolo-quinazolines, characterized by an ortho-substituted-arylamino, heterocyclylamino- or C3-C7 cycloalkylamino residue at 8 position and an aryl, heterocyclyl or C3-C7 cycloalkyl as substituent of a carboxamide at 3 position of the molecule framework. The compounds of this invention modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular MPS1/TTK. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds.Type: GrantFiled: June 17, 2009Date of Patent: September 30, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Marina Caldarelli, Mauro Angiolini, Riccardo Colombo, Teresa Disingrini, Stefano Nuvoloni, Helena Posteri, Matteo Salsa, Marco Silvagni
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Patent number: 8841312Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: GrantFiled: December 18, 2008Date of Patent: September 23, 2014Assignee: Amgen Inc.Inventors: Richard V. Connors, Dai Kang, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang, Dustin L. McMinn, Jeffrey T. Mihalic, Jeffrey Deignan
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Publication number: 20140275131Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Inventors: Peng LI, Hailin ZHENG, Jun ZHAO, Lawrence P. WENNOGLE
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Publication number: 20140275130Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; 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. The compounds of this invention have the formula I: Additionally, the compounds of this invention have the formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: September 18, 2014Inventors: Jean-Damien Charrier, Chris Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, David Kay, Ronald Knegtel, Francoise Pierard, Joanne Pinder, Pierre-Henri Storck
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Publication number: 20140275023Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Inventors: Nivedita Namdev, Jianqiang Wang
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Publication number: 20140271527Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.Type: ApplicationFiled: November 1, 2012Publication date: September 18, 2014Applicant: Serina Therapeutics, Inc.Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
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Publication number: 20140249137Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: October 31, 2013Publication date: September 4, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis, Harmon J. Zuccola
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Publication number: 20140249143Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline LLCInventors: Anna Lindsey Banka, Janos Botyanszki, Eric Gregory Burroughs, John George Catalano, Wendy Huang Chern, Hamilton D. Dickson, Margaret J. Gartland, Robert Hamatake, Hans Hofland, Jesse Daniel Keicher, Christopher Brooks Moore, John Bradford Shotwell, Matthew David Tallant, Jean-Philippe Therrien, Shihyun You
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Patent number: 8815880Abstract: To provide a hydrochloride of a tricyclic pyrazolopyrimidine compound inhibiting the effect of HSP90 and a crystal thereof. The present invention provides a hydrochloride of 2-{4-amino-2-[(3-chloro-4-methoxy-5-methylpyridin-2-yl)methyl]-2,7-dihydro-6-thia-1,2,3,5-tetraazabenzo[cd]azulen-8-yl}-N-methylacetamide which inhibits the ATPase activity of HSP90 and which has antitumor activity, a crystal thereof, a medicament comprising the same, an anticancer agent comprising the same, and the like.Type: GrantFiled: February 21, 2013Date of Patent: August 26, 2014Assignee: Daiichi Sankyo Company, LimitedInventors: Shinji Matuura, Hisaki Kajino, Tomoyuki Nagai, Keijiro Kobayashi
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Patent number: 8809355Abstract: The present invention relates to novel compounds of the general formula (I) having anxiolytic, anticonvulsant, sedative-hypnotic and myorelaxant conditions as well as anxiogenic, somnolytic and convulsant conditions in mammals, including humans, as GABAA receptor modulator.Type: GrantFiled: April 2, 2009Date of Patent: August 19, 2014Assignee: Innovationspatent Sverige ABInventors: Mogens Peter Cherly Nielsen, Tommy Liljefors, Jakob Alexander Nilsson, Olov A Sterner
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Publication number: 20140212459Abstract: The invention relates to 10H-benzo[g]pteridine-2,4-dione derivatives, to the production thereof, and to the use thereof.Type: ApplicationFiled: June 22, 2012Publication date: July 31, 2014Inventors: Tim Maisch, Andreas Späth
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Publication number: 20140200220Abstract: The present disclosure relates to 10H-benzo[g]pteridine-2,4-dione derivatives, to the production thereof, and to the use thereof.Type: ApplicationFiled: June 22, 2012Publication date: July 17, 2014Inventors: Tim Maisch, Andreas Spath
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Publication number: 20140200344Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.Type: ApplicationFiled: August 10, 2012Publication date: July 17, 2014Applicant: Nissan Chemical Industries, Ltd.Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
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Publication number: 20140194396Abstract: The present invention relates to PDEI inhibitory compounds of Formula I as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 11, 2012Publication date: July 10, 2014Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hlilin Zheng, Jun Zhao, Lawrence P. Wennogle
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Publication number: 20140194414Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 10, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Publication number: 20140187774Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclisation conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).Type: ApplicationFiled: December 9, 2013Publication date: July 3, 2014Inventors: Jean-Damien Charrier, Steven Durrant, David Kay
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Patent number: 8765775Abstract: The invention relates to compounds of formula 1, tautomers and salts thereof, wherein R1, R2, R3, R4, and R5 have the meanings indicated in the specification. These compounds are receptor tyrosine kinase EphB4 inhibitors useful for the treatment of angiogenesis dependent cancers and intraocular neovascular syndromes. The invention further relates to a method termed ALTA (anchor-based library tailoring) of selecting compounds from a large compound library for screening as EphB4 inhibitors by computational procedures.Type: GrantFiled: January 23, 2009Date of Patent: July 1, 2014Assignee: Universitaet ZuerichInventors: Danzhi Huang, Peter Kolb, Karine Lafleur, Cristina Nevado, Amedeo Caflisch
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Publication number: 20140171412Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: NOVARTIS AGInventors: Mahbub AHMED, Alexander ASHALL-KELLY, Graham Charles BLOOMFIELD, Louisa GUERITZ, Jeffrey MCKENNA, Joseph MCKENNA, Simon MUTTON, Rakesh PARMAR, Jon SHEPERD, Paul WRIGHT
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Publication number: 20140171456Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine and dipyrazolopyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrrolo[3,2-e]pyrimidine or dipyrazolopyrimidine compounds.Type: ApplicationFiled: July 20, 2012Publication date: June 19, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: Zhaoyang Meng, Arshad Siddiqui, Panduranga Abdulla P. Reddy, Mehul F. Patel, Yang Nan
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Publication number: 20140148421Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng LI, Jun ZHAO, Hailin ZHENG, Lawrence WENNOGLE
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Patent number: 8735386Abstract: Compounds of general formula (I) wherein the groups R1 to R3 and X are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.Type: GrantFiled: July 20, 2011Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Matthias Treu
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Publication number: 20140128403Abstract: Use of 10H-benzo[g]pteridine-2,4-dione derivatives as photosensitizers in the inactivation of microorganisms.Type: ApplicationFiled: June 22, 2012Publication date: May 8, 2014Inventors: Tim Maisch, Andreas Späth
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Patent number: 8710065Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: GrantFiled: February 28, 2012Date of Patent: April 29, 2014Assignee: AbbVie Inc.Inventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Publication number: 20140113920Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: July 2, 2012Publication date: April 24, 2014Applicant: MERCK SHARP & DOHME CORP.Inventor: Wen-Lian Wu
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Patent number: 8691832Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: December 1, 2011Date of Patent: April 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Duane A. Burnett, Zhiqiang Zhao, David Cole, Hubert Josien, Dmitri A. Pissarnitski, Thavalakulamgar Sasikumar, Wen-Lian Wu, Martin Domalski
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Patent number: 8686139Abstract: The present invention relates to organic electronic devices that include an organic semiconducting material. The organic electronic devices may include organic light-emitting diodes, field-effect transistors, sensors, photodetectors, organic solar cells, organic thin-film transistors, organic integrated circuits, organic field-quench devices, organic light-emitting transistors, light-emitting electrochemical cells, or organic laser diodes.Type: GrantFiled: November 23, 2010Date of Patent: April 1, 2014Assignee: Novaled AGInventors: Andrea Lux, Omrane Fadhel, Josef Salbeck, Manfred Kussler
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Patent number: 8664207Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.Type: GrantFiled: December 7, 2009Date of Patent: March 4, 2014Assignee: Intra-Cellular Therapies, Inc.Inventors: Peng Li, Jun Zhao, Hailin Zheng, Lawrence Wennogle
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Patent number: 8664233Abstract: The invention relates to compounds of general formula 1 to processes for the production thereof, to pharmaceutical preparations containing said compounds and/or physiologically compatible salts and/or solvates which can be produced therefrom as well as to the pharmaceutical use of said compounds, the salts or solvates thereof as inductors of apoptosis in the case of non-solid malignant tumors of the hematopoietic system, in particular in the case of leukemias and lymphomas, more particularly in the case of leukemic B lymphocytes.Type: GrantFiled: December 21, 2007Date of Patent: March 4, 2014Assignee: The Medicines Company (Leipzig) GmbHInventors: Claudia Reichelt, Alexander Schulze, Mohammed Daghish, Friedrich-Alexander Ludwig, Jochen Heinicke, Konrad Herrmann, Maj Schuster, Sven Letschert, Kenneth Mugridge, Joseph DeAngelo
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Patent number: 8653097Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: October 15, 2009Date of Patent: February 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Publication number: 20140045833Abstract: The present invention relates to a novel family of inhibitors of protein kinases of Formula (1) wherein X is selected from CH2, O, S(0)n, or NR6; and process for their production and pharmaceutical compositions thereof. In particular, the present invention relates to inhibitors of the members of the Tec, Src, Btk and Lck protein kinase families.Type: ApplicationFiled: April 3, 2012Publication date: February 13, 2014Applicant: PHARMASCIENCE INC.Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith
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Patent number: 8648078Abstract: The present invention relates to novel crystalline, water-soluble salts of a plk inhibitor. Such crystal salts are for example L-tartrate, succinate, phosphate, mesylate, maleate, L-malate, hydrochloride, fumarate (half mole of counterion), fumarate, citrate (half mole of counterion), benzenesulfonate and L-aspartate (half mole of counterion). New crystal forms of the base as well as solvates and hydrates of such new salt forms, a process for their preparation, their utility in therapy and to the pharmaceutical compositions containing them are also claimed and described in the present application.Type: GrantFiled: July 22, 2010Date of Patent: February 11, 2014Assignee: Nerviano Medical Sciences S.R.L.Inventors: Massimo Zampieri, Italo Beria, Annalisa Airoldi, Ilaria Candiani, Riccardo Frigerio
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Publication number: 20140038988Abstract: The present invention relates to novel heterocyclically fused diaryldihydropyrimidine derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: October 7, 2013Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, SONJA ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG
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Patent number: 8637666Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclization conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).Type: GrantFiled: March 20, 2012Date of Patent: January 28, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jean-Damien Charrier, Steven Durrant, David Kay
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Publication number: 20140023614Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.Type: ApplicationFiled: March 21, 2012Publication date: January 23, 2014Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
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Publication number: 20140018343Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Patent number: 8629272Abstract: The present invention relates to compounds having the general formula (I) with the definitions of X1-X3, Y1, Y2, L1, R1 and R2 given below and/or solvates, hydrates, esters and pharmaceutically acceptable salts thereof. Furthermore, the invention relates to the use of said compounds for modulating of the Wnt signalling pathway activity and their use as a medicament, preferably for the treatment of cancer.Type: GrantFiled: June 25, 2010Date of Patent: January 14, 2014Assignee: Deutsches KrebsforschungszentrumInventors: Florian Fuchs, Daniel Gilbert, Corinna Koch, Rajendra-Prasad Maskey, Sandra Steinbrink, Michael Boutros
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Patent number: 8623885Abstract: Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.Type: GrantFiled: March 21, 2012Date of Patent: January 7, 2014Assignee: Amgen Inc.Inventors: Xiaoqi Chen, Kang Dai, Jason Duquette, Michael W. Gribble, Jr., Justin N. Huard, Kathleen S. Keegan, Zhihong Li, Sarah E. Lively, Lawrence R. McGee, Mark L. Ragains, Xianghong Wang, Margaret F. Weidner, Jian Zhang
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Patent number: 8618121Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain tricyclic compounds (referred to herein as TC compounds), and especially certain 9H-pyrimido[4,5-b]indole, 9H-pyrido[4?,3?:4,5]pyrrolo[2,3-d]pyridine, and 9H-1,3,6,9-tetraaza-fluorene compounds, which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or TS inhibitor; (d) a microtubule targeted agent; and (e) ionising radiation.Type: GrantFiled: July 1, 2008Date of Patent: December 31, 2013Assignee: Cancer Research Technology LimitedInventors: Ian Collins, John Charles Reader, Suki Klair, Jane Scanlon, Glynn Addison, Michael Cherry
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Patent number: 8614220Abstract: Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: GrantFiled: December 17, 2007Date of Patent: December 24, 2013Assignee: Nerviano Medical Sciences S.r.l.Inventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ron Ferguson, Helena Posteri, Barbara Valsasina
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Patent number: 8614221Abstract: The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: March 10, 2010Date of Patent: December 24, 2013Assignees: Merck Sharp & Dohme Corp., MSD K.K.Inventors: Weiming Fan, Thomas F. N. Haxell, Matthew G. Jenks, Nobuhiko Kawanishi, Shuliang Lee, Hao Liu, Michael J. Malaska, Joseph A. Moore, III, Yoshio Ogino, Yu Onozaki, Bharathi Pandi, Michael R. Peel, Toshihiro Sakamoto, Tony Siu
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Publication number: 20130338134Abstract: The present invention relates to tricyclic compounds, 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: ApplicationFiled: June 12, 2013Publication date: December 19, 2013Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
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Publication number: 20130338139Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: ApplicationFiled: June 18, 2013Publication date: December 19, 2013Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse