Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
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Patent number: 12227500Abstract: The present invention provides, inter alia, a compound having the structure: Also provided are compositions containing a pharmaceutically acceptable carrier and one or more compounds according to the present invention. Further provided are methods for treating or ameliorating the effects of a disorder in a subject, methods of suppressing the toxicity of endoplasmic reticulum (ER) stress in a subject, methods of treating or ameliorating the effects of a disease involving axon degeneration in a subject, and methods for treating or ameliorating the effects of a neurodegenerative disease.Type: GrantFiled: September 1, 2020Date of Patent: February 18, 2025Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Brent R. Stockwell, Hynek Wichterle, Pieter Bos, Arie Zask, Sebastian Thams, Emily Rhodes Lowry
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Patent number: 12215110Abstract: Disclosed is a process for the preparation of certain intermediates, e.g. a process for preparing a compound of formula (I) wherein, R1, R2 and X1 are as defined in the description, and which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.Type: GrantFiled: May 20, 2020Date of Patent: February 4, 2025Assignee: Janssen Pharmaceutica NVInventors: Philip James Pye, Andras Horvath, Cheng Yi Chen, Yuanyuan Yuan, Jinxiong Su, Shuo Wang, Simon Albert Wagschal
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Patent number: 11827641Abstract: The invention relates to compounds of formula (I): or a salt or solvate thereof, wherein the variables are as described herein. Compounds of formula (I) and pharmaceutical compositions thereof are antagonists of toll-like receptors such as TLR7, TLR8 and/or TLR9 that are useful for inhibiting immune response and treating diseases associated with undesirable immune response.Type: GrantFiled: May 20, 2022Date of Patent: November 28, 2023Assignee: DYNAVAX TECHNOLOGIES CORPORATIONInventors: Albert Frederick Candia, III, Richard Thomas Beresis, Robert L. Coffman
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Patent number: 11370792Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: GrantFiled: December 14, 2016Date of Patent: June 28, 2022Assignee: Raze Therapeutics, Inc.Inventors: Nello Mainolfi, Mikel P. Moyer, Eddine Saiah, Cristina Lecci, Robert David Matthew Pace, Heather Tye, Julia Vile
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Patent number: 11066410Abstract: A compound and/or a pharmaceutically acceptable salt thereof has the following formula A: These compounds can be PIKfyve kinase inhibitors.Type: GrantFiled: March 23, 2018Date of Patent: July 20, 2021Assignee: 3100 Central Expressway LLCInventors: Sergei Romanov, Robert Greenhouse, Nikolai Sepetov
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Patent number: 10760078Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: GrantFiled: December 19, 2018Date of Patent: September 1, 2020Assignee: SAREPTA THERAPEUTICS, INC.Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Patent number: 10039283Abstract: The present invention relates to novel substituted pyrazolyl-nicotin(thio)amide derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms, in crop protection and in the protection of materials.Type: GrantFiled: March 31, 2015Date of Patent: August 7, 2018Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Christophe Dubost, Cyril Montagne, Ulrike Wachendorff-Neumann, Phillipp Winter, Strphane Brunet, Jean-Pierre Vors, Pierre-Yves Coqueron, Joerg Greul
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Patent number: 9969738Abstract: Novel compounds of Formula I and their use in therapeutic treatments.Type: GrantFiled: March 28, 2014Date of Patent: May 15, 2018Assignee: OGEDA SAInventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
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Patent number: 9695166Abstract: In one aspect this invention relates generally to compounds of Formula: and sub-formulas thereof, or a tautomer of each thereof, a pharmaceutically acceptable salt of each thereof, or a pharmaceutically acceptable solvate of each of the foregoing, where X1, L1, L3, and R3 are described herein.Type: GrantFiled: May 4, 2015Date of Patent: July 4, 2017Assignee: Global Blood Therapeutics, Inc.Inventors: Zhe Li, Qing Xu, Chul Yu, Calvin Yee, Stephen L. Gwaltney, II, Brian W. Metcalf, Steven Richards, Matthew A. Lardy, Lina Setti, Hing Sham
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Patent number: 9469664Abstract: Oligonucleotide analogs comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: GrantFiled: June 6, 2014Date of Patent: October 18, 2016Assignee: Sarepta Therapeutics, Inc.Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Publication number: 20150133447Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R3, X3 to X6 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: November 4, 2014Publication date: May 14, 2015Inventor: Harald ENGELHARDT
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Publication number: 20150126502Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: January 14, 2015Publication date: May 7, 2015Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
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Publication number: 20150126508Abstract: Provided are a pteridine ketone derivative used as an EGFR, BLK, and FLT3 inhibitor and applications thereof. Specifically, provided are a compound of the following formula I, a pharmaceutical composition containing the compound of the formula I, and use of compound in preparing medicine for treating diseases mediated by EGFR, BLK, or FLT3 or inhibiting EGFR, BLK, and FLT3.Type: ApplicationFiled: April 2, 2013Publication date: May 7, 2015Inventors: Honglin Li, Yufang Xu, Zhenjiang Zhao, Xiaofeng Liu, Wei Zhou, Fang Bai, Mengzhu Xue, Lei Zhang, Youli Zhang
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Patent number: 9023385Abstract: A method of treating a patient to improve liver functioning includes providing a drug composed of at least one of pharmaceutical 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine and a pharmaceutically acceptable salt thereof; and administering the drug to the patient in a manner and dosage effective to improve liver functioning. The 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine can inhibit the activated hepatic stellate cells from synthesizing and expressing collagens and other extracellular matrix proteins including MMPs and TIMPs, and so it can inhibit liver fibrosis. In the liver, it can inhibit collagen synthesis and expression, and therefore reverse and treat hepatitis and liver cirrhosis effectively.Type: GrantFiled: December 2, 2013Date of Patent: May 5, 2015Assignee: Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd.Inventors: Ka Ho Kenneth Lee, Ruohan Chen, Zhibo Hou, Quanwei Pan
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Publication number: 20150105382Abstract: The present invention relates to a purine compound useful as a kinase inhibitor.Type: ApplicationFiled: May 7, 2014Publication date: April 16, 2015Applicant: VERASTEM, INC.Inventors: DiZhong Chen, Meredith Williams
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Publication number: 20150094305Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: September 25, 2014Publication date: April 2, 2015Inventors: Donna ROMERO, Craig E. MASSE, Shaughnessy ROBINSON, Jeremy Robert GREENWOOD, Geraldine C. HARRIMAN
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Publication number: 20150094295Abstract: The present disclosure provides compounds of Formula (IA) and or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: September 6, 2013Publication date: April 2, 2015Inventors: Tim Owens, Erik Verner
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Patent number: 8993580Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating lipid kinases such PI3 kinases, tyrosine kinases and protein kinases such as mTOR. For example, the invention provides compounds of Formula: Also provided in the present invention are methods of using these compositions to modulate these kinases especially for therapeutic applications.Type: GrantFiled: March 16, 2009Date of Patent: March 31, 2015Assignee: Intellikine LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan
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Publication number: 20150087643Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.Type: ApplicationFiled: October 10, 2014Publication date: March 26, 2015Applicant: Advinus Therapeutics Private LimitedInventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
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Publication number: 20150087644Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
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Patent number: 8987257Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, to their preparation, to their medical use, in particular to their use in the treatment of cancer and neurodegenerative disorders, and to medicaments comprising them.Type: GrantFiled: January 30, 2012Date of Patent: March 24, 2015Assignee: Novartis AGInventors: Branko Radetich, Bing Yu, Yanyi Zhu
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Patent number: 8987280Abstract: Compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: GrantFiled: January 29, 2009Date of Patent: March 24, 2015Assignees: Genentech, Inc., F. Hoffmann-La Roche AGInventors: Jennafer Dotson, Tim Heffron, Alan Olivero, Daniel P. Sutherlin, Shumei Wang, Bing-Yan Zhu, Irina Chuckowree, Adrian Folkes, Nan Chi Wan
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Publication number: 20150073140Abstract: Oligonucleotide analogues comprising modified intersubunit linkages and/or modified 3? and/or 5?-end groups are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects.Type: ApplicationFiled: June 6, 2014Publication date: March 12, 2015Applicant: Sarepta Therapeutics, Inc.Inventors: Gunnar J. Hanson, Alexander Charles Rudolph, Bao Zhong Cai, Ming Zhou, Dwight D. Weller
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Patent number: 8969551Abstract: The present invention provides a useful morpholino nucleic acid derivative for synthesizing a morpholino nucleic acid oligomer. The present invention provides a compound represented by the following general formula (1) or a salt thereof. Here, R1 represents hydrogen, trityl and so on. R2 represents an amide or an imine. R3 represents a hydroxy group which may be protected by trialkylsilyl and so on, or a group represented by the following general formula (5): (wherein X represents O or S, Y represents dialkylamino or alkoxy, and Z represents chlorine).Type: GrantFiled: September 29, 2011Date of Patent: March 3, 2015Assignee: Nippon Shinyaku Co., Ltd.Inventor: Toshihiro Ueda
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Publication number: 20150051202Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: February 14, 2013Publication date: February 19, 2015Applicant: Merck Patent GmbHInventors: Kai Schiemann, Carl Deutsch, Guenter Hoelzemann, Daniel Kuhn, Ansgar Wegener, Dominique Swinnen, Horacio Comas
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Publication number: 20150038503Abstract: The present invention provides novel 6-substituted [1,2,4]triazolo[4,3-b]pyridazines that are agonists of Rev-Erb. These compounds, and pharmaceutical compositions comprising the same, are suitable means for treating any disease wherein the activation of Rev-Erb has therapeutic effects, for instance in inflammatory and circadian rhythm-related disorders or cardiometabolic diseases.Type: ApplicationFiled: September 27, 2012Publication date: February 5, 2015Applicant: GENFITInventors: Maryline Bourotte, Jean-Francois Delhomel, Mathieu Dubernet, Marie-Helene Gouy
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Publication number: 20150031672Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: October 10, 2014Publication date: January 29, 2015Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20150025058Abstract: Compounds of the formula I in which R1, R2 and R4 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupusType: ApplicationFiled: January 22, 2013Publication date: January 22, 2015Applicant: MERCK PATENT GMBHInventors: Carl Deutsch, Daniel Kuhn, Tatjana Ross, Lars Burgdorf
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Publication number: 20150018349Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. 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: ApplicationFiled: March 27, 2014Publication date: January 15, 2015Applicant: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Publication number: 20150018336Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Inventors: Wei Chen, David J. Loury
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Publication number: 20150011545Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: July 15, 2014Publication date: January 8, 2015Applicant: AstraZeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle Laurae LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
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Publication number: 20140378431Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Guenter Hoelzemann, Kai Schiemann, Ansgar Wegener
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Patent number: 8912178Abstract: The 4-urea-phenyl substituted 6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine derivatives are potent and selective inhibitors of mTOR kinase and are useful in treating disorders related to abnormal mTOR activities such as cancer, immune disorders, cardiovascular disease, ocular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.Type: GrantFiled: May 18, 2011Date of Patent: December 16, 2014Assignee: Xcovery Holdings Company, LLCInventor: Congxin Liang
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Publication number: 20140364423Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: August 26, 2014Publication date: December 11, 2014Inventors: Wei-Sheng Huang, Ranny M. Thomas
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Publication number: 20140364410Abstract: The present disclosure provides compounds of Formula (IA) and/or pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BTK, and are potentially useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer, inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and/or pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: August 20, 2014Publication date: December 11, 2014Inventors: Tim OWENS, Erik VERNER
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Publication number: 20140316132Abstract: Provided are modulators of TLRs of Formula II: pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventors: Manoj C. Desai, Randal L. Halcomb, Paul Hrvatin, Hon Chung Hui, Ryan McFadden, Paul A. Roethle, Hong Yang
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Patent number: 8865896Abstract: A method for producing adenine compound (1): wherein m and n are independently an integer of 2 to 5, R1 is C1-6 alkyl group, R2 and R3 are the same or different, and hydrogen atom, or C1-6 alkyl group, or R2 and R3 are combined with an adjacent nitrogen atom to form pyrrolidine, morpholine, piperidine, piperazine, etc., and R4 is C1-3 alkyl group, which comprises a step of reacting compound (2): and compound (3): in the presence of a boron-containing reducing agent.Type: GrantFiled: January 16, 2009Date of Patent: October 21, 2014Assignees: Astrazeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Kazuki Hashimoto, Wataru Katoda, Kazuhiko Takahashi, Ayumu Kurimoto
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Publication number: 20140303366Abstract: Provided is a method of treating myasthenia gravis in a patient by administering to the patient an effective amount of a skeletal muscle troponin activator, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 7, 2014Publication date: October 9, 2014Inventors: Aaron Hinken, Fady Malik, Malar Pannirselvam, Alan Russell
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Publication number: 20140303161Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 9, 2013Publication date: October 9, 2014Inventor: Principia Biopharma, Inc.
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Publication number: 20140296207Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: June 11, 2014Publication date: October 2, 2014Inventors: Pingda REN, Yi LIU, Liansheng LI, Troy Edward WILSON
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Publication number: 20140296233Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicants: Sanofi, Celgene Avilomics Research, Inc.Inventors: Laura Akullian D'Agostino, Robert Tjin Tham Sjin, Deqiang Niu, Joseph John McDonald, Zhendong Zhu, Haibo Liu, Hormoz Mazdiyasni, Russell C. Petter, Juswinder Singh, Matthieu Barrague, Alexandre Gross, Mark Munson
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Publication number: 20140296216Abstract: A compound of formula (I) or (II) and use of the compound in the preparation of drugs for treating cancer are disclosed. The study shows that the compounds can inhibit the growth of many kinds of tumor cells, can be used for targeting epidermal growth factor receptor (EGFR), and particularly can inhibit tumor cells with single or multiple mutations of EGFR (T790M). Therefore, the compound can be used as EGFR inhibitor to treat cancer and has a relatively large application value.Type: ApplicationFiled: December 21, 2011Publication date: October 2, 2014Applicant: GUANGZHOU INSTITUTE OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCESInventors: Ke Ding, Shaohua Chang, Shilin Xu, Lianwen Zhang, Zhengchao Tu, Jian Ding, Meiyu Geng, Yi Chen
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Patent number: 8846909Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.Type: GrantFiled: May 24, 2011Date of Patent: September 30, 2014Assignee: University of RochesterInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth
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Patent number: 8846673Abstract: Compounds having the formula (I), and enantiomers, and diastereomers, pharmaceutically-acceptable salts, thereof, (I) are useful as kinase modulators, including Btk modulation, wherein A1, A2, A3, R4 are as defined herein.Type: GrantFiled: August 11, 2010Date of Patent: September 30, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Bin Jiang, Zhonghui Lu
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Publication number: 20140288046Abstract: The invention relates to a compound of formula (I) wherein A, R1 and R2 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: April 11, 2014Publication date: September 25, 2014Applicant: HOFFMANN-LA ROCHE INC.Inventors: Jean-Michel Adam, Caterina Bissantz, Uwe Grether, Atsushi Kimbara, Matthias Nettekoven, Stephan Roever, Mark Rogers-Evans
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Publication number: 20140287031Abstract: The present invention provides for methods and pharmaceutical compositions comprising inhibitors of mTorC1 and/or mTorC2. In some aspects, the invention provides for treatment regimens resulting in enhanced treatment efficacy and better tolerability.Type: ApplicationFiled: November 21, 2012Publication date: September 25, 2014Applicant: INTELLIKINE, LLCInventors: Yi Liu, Lynne Bui, Michael Martin, Troy Edward Wilson, Christian Rommel
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Publication number: 20140275024Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
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Publication number: 20140275528Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: HYDRA BIOSCIENCES, INC.Inventors: Bertrand L. Chenard, Randall J. Gallaschun, Spencer David Kimball
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Publication number: 20140275071Abstract: Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: HYDRA BIOSCIENCES, INC.Inventors: Bertrand L. Chenard, Randall J. Gallaschun
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Patent number: 8835420Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.Type: GrantFiled: July 8, 2013Date of Patent: September 16, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace