Patents Examined by Jeffrey Murray
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Patent number: 8912210Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. 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 CGRP is involved.Type: GrantFiled: November 10, 2011Date of Patent: December 16, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
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Patent number: 8703780Abstract: 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: GrantFiled: June 18, 2012Date of Patent: April 22, 2014Assignee: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 8697698Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2?are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 28, 2012Date of Patent: April 15, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Patent number: 8697710Abstract: The present invention relates to optionally substituted 3-amino-4,5-dihydro-(1H or 2H)-pyrazolo[3,4-d]pyrimidin-6(7H)-ones and their 4-imino or 4-thioxo derivatives, e.g., 3-amino-4-(thioxo or imino)-4,5-dihydro-2H-pyrazolo[3,4-d]pyrimidin-6(7H)-ones, 3-amino-4-(thioxo or imino)-4,5-dihydro-2H-pyrazolo[3,4-d]pyrimidin-6(7H)-ones, 3-amino-4-(thioxo or imino)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6(7H)-ones, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.Type: GrantFiled: December 7, 2009Date of Patent: April 15, 2014Assignee: Intra-Cellular Therapies, Inc.Inventors: Peng Li, Jun Zhao, Hailin Zeng, Lawrence Wennogle
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Patent number: 8697711Abstract: Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, 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: GrantFiled: May 23, 2012Date of Patent: April 15, 2014Assignee: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 8691819Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: GrantFiled: October 14, 2009Date of Patent: April 8, 2014Assignee: PRISM BioLab CorporationInventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
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Patent number: 8691825Abstract: The instant invention provides for substituted fused pyrimidine compounds of Formula A 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 29, 2010Date of Patent: April 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Qi Chen, Mingxiang Cui, Bin Hu, Shuangxi Hu, Zhifa Pu, Philip E. Sanderson, Richard Soll, Xue Tang, Jiabing Wang, Yongjin Yan, Jinfeng Yao, Hongjie Zhang
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Patent number: 8691546Abstract: Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, 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: GrantFiled: May 15, 2012Date of Patent: April 8, 2014Assignee: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 8691827Abstract: The present invention is directed to amino tetrahydro-pyridopyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: August 5, 2010Date of Patent: April 8, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
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Patent number: 8685987Abstract: This invention relates to novel substituted [1,2,4]triazolo[1,5-a]pyrimidines and their use as modulators of potassium channels. In other aspects the invention relates to the use of these compounds, in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: GrantFiled: March 30, 2010Date of Patent: April 1, 2014Assignee: Ataxion, Inc.Inventors: Ulrik Svane Sørensen, Birgitte L. Eriksen, Charlotte Hougaard, Dorte Strøbæk, Palle Christophersen
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Patent number: 8685988Abstract: The present invention relates to certain pyrrolopyrimidine derivatives, pharmaceutical compositions containing them, and methods of using them, including methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.Type: GrantFiled: June 13, 2013Date of Patent: April 1, 2014Assignee: Acea Biosciences, Inc.Inventors: Xiao Xu, Xiaobo Wang, Long Mao, Li Zhao, Biao Xi
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Patent number: 8674095Abstract: Provided herein are pyrido[2,3-D]pyrimidin-7(8H)-one compounds and compositions useful as PAK inhibitors. Also provided herein are methods of utilizing these compounds for the treatment of neuropsychiatric conditions. The compounds modulate dendritic spine morphology and/or synaptic function.Type: GrantFiled: December 18, 2009Date of Patent: March 18, 2014Assignee: Afraxis Holdings, Inc.Inventors: David Campbell, Sergio G. Durón, Benedikt Vollrath, Warren Wade
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Patent number: 8663961Abstract: Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, 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: GrantFiled: May 15, 2012Date of Patent: March 4, 2014Assignee: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 8664260Abstract: A method of making a bacteriochlorin is carried out by condensing a pair of compounds of Formula II to produce the bacteriochlorin, wherein R is an acetal or aldehyde group. The condensing may be carried out in an organic solvent, preferably in the presence of an acid. The bacteriochlorins are useful for a variety of purposes such as active agents in photodynamic therapy, luminescent compounds in flow cytometry, solar cells, light harvesting arrays, and molecular memory devices.Type: GrantFiled: April 10, 2012Date of Patent: March 4, 2014Assignee: North Carolina State UniversityInventors: Han-Je Kim, Jonathan S. Lindsey
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Patent number: 8658653Abstract: Disclosed herein are compounds, including compounds having the structure of Formula (A), (B), (C), and (D), as described in further detail herein, 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: GrantFiled: January 30, 2012Date of Patent: February 25, 2014Assignee: Pharmacyclics, Inc.Inventors: Lee Honigberg, Erik Verner, Zhengying Pan
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Patent number: 8653087Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, X1, X2, X3, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or anomalous cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 8, 2009Date of Patent: February 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Andreas Mantoulidis, Georg Dahmann, Peter Ettmayer, Christian Klein, Steffen Steurer, Irene Waizenegger, Stephan Karl Zahn
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Patent number: 8653085Abstract: Drug delivery systems have been developed based on the formation of diketopiperazine carboxylate salts and microparticles containing the same. The systems may further comprise a bioactive agent. Related methods for making and using the biologically active agent delivery compositions are also provided. In certain embodiments, the pharmaceutically acceptable salts described can be formed by removal of solvent by methods including distillation, evaporation, spray drying or lyophilization.Type: GrantFiled: August 22, 2012Date of Patent: February 18, 2014Assignee: Mankind CorporationInventors: Andrea Leone-Bay, Destardi Moye-Sherman, Bryan R. Wilson
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Patent number: 8653268Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X1, X2, X3, X4, X5, X6, X7, R1, and Q1 are defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.Type: GrantFiled: January 11, 2013Date of Patent: February 18, 2014Assignee: OSI Pharmaceuticals, LLCInventors: Mark J. Mulvihill, Radoslaw Laufer, An-Hu Li, Arno G. Steinig
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Patent number: 8648076Abstract: The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use.Type: GrantFiled: July 26, 2006Date of Patent: February 11, 2014Assignee: Hybrigenics SAInventors: Philippe Guedat, Guillaume Boissy, Catherine Borg-Capra, Frédéric Colland, Laurent Daviet, Etienne Formstecher, Xavier Jacq, Jean-Christophe Rain, Rémi Delansorne, Stefania Vallese, Matteo Colombo
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Patent number: 8642606Abstract: Compounds of Formula I: and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on one or more protein kinases, including a Zeta-chain-associated protein kinase 70 (ZAP-70), and any mutations thereof. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with increased expression of ZAP-70 cancer, B-cell chronic lymphocytic leukemia, aggressive B-cell chronic lymphocytic leukemia, an allergy-related disease or an allergic inflammation.Type: GrantFiled: September 23, 2011Date of Patent: February 4, 2014Assignee: Plexxikon Inc.Inventors: Prabha N. Ibrahim, Chao Zhang