Spiro Patents (Class 514/212.02)
  • Patent number: 10226471
    Abstract: The present invention relates to methods for weight management that utilize modified-release dosage forms comprising (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts and crystalline forms thereof. The present invention further relates to (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine salts, crystalline forms thereof and modified-release dosage forms comprising them.
    Type: Grant
    Filed: February 10, 2017
    Date of Patent: March 12, 2019
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Zezhi Jesse Shao, Anthony C. Blackburn, Andrew J. Grottick, Michael E. Morgan, Jaimie Karyn Rueter, Anna Shifrina, Scott Stirn, Libo Yang, Woo Hyun Yoon
  • Patent number: 10118929
    Abstract: The present disclosure relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present disclosure also relates to pharmaceutical compositions containing the fluorinated compounds of the disclosure, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: November 6, 2018
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Takeru Furuya, Ben C. Askew
  • Patent number: 9943525
    Abstract: A composition for reducing cell senescence including a Rho-kinase inhibitor and method of treating a cell senescence-related symptom in mammals.
    Type: Grant
    Filed: July 30, 2015
    Date of Patent: April 17, 2018
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Joontae Park, Hyuntae Kang, Chulwon Jung, Kobong Choi, Sangchul Park, Hyojei Choi
  • Patent number: 9850203
    Abstract: Described herein are compounds that are autotaxin inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with autotaxin activity.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: December 26, 2017
    Assignee: PHARMAKEA, INC.
    Inventors: John Howard Hutchinson, David Lonergan, Fei Huang, Martin Rowbottom, Imelda Calderon
  • Patent number: 9718796
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.
    Type: Grant
    Filed: January 12, 2012
    Date of Patent: August 1, 2017
    Assignees: VENTIRX PHARMACEUTICALS, INC., ARRAY BIOPHARMA, INC.
    Inventors: James Jeffry Howbert, Robert Hershberg, Laurence E. Burgess, Hong Woon Yang
  • Patent number: 9676781
    Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: May 19, 2015
    Date of Patent: June 13, 2017
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Georg Dahmann, Kai Gerlach, Roland Pfau, Wolfgang Wienen, Annette Schuler-Metz, Sandra Handschuh, Herbert Nar
  • Patent number: 9527840
    Abstract: The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound.
    Type: Grant
    Filed: February 11, 2016
    Date of Patent: December 27, 2016
    Assignees: Purdue Pharma L.P., Shionogi & Co. Ltd.
    Inventors: Kouki Fuchino, R. Richard Goehring, Bin Shao, Yoshiyuki Taoda, Naoki Tsuno, John William Frank Whitehead, Jiangchao Yao
  • Patent number: 9505739
    Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: November 29, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Hao Wu
  • Patent number: 9403777
    Abstract: Provided are compounds that are capable of modulating the activity of the influenza A virus via interaction with the M2 transmembrane protein. Also provided are methods for treating an influenza A-affected disease state or infection comprising administering a composition comprising one or more compounds that have been identified as being capable of interaction with the M2 protein.
    Type: Grant
    Filed: September 25, 2013
    Date of Patent: August 2, 2016
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Jun Wang
  • Patent number: 9365521
    Abstract: Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: June 14, 2016
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Anthony C. Blackburn, Yun Shan, Anna Shifrina, Scott Stirn
  • Patent number: 9309262
    Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thienylindole azepines. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: April 12, 2016
    Assignee: ABT Holding Company
    Inventors: Michael Robarge, Michelle Zawadski, John Harrington
  • Patent number: 9242964
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, infectious disease, inflammatory disorder, graft rejection, and graft-verses-host disease.
    Type: Grant
    Filed: September 3, 2013
    Date of Patent: January 26, 2016
    Assignees: VENTIRX PHARMACEUTICALS, INC., ARRAY BIOPHARMA, INC.
    Inventors: James Jeffry Howbert, Gregory Dietsch, Robert M. Hershberg, Laurence E. Burgess, George A. Doherty, C. Todd Eary, Robert D. Groneberg, Zachary Jones
  • Patent number: 9133120
    Abstract: The invention relates to fluorinated fentanyl derivatives that function as opioid receptor agonists, which activate target opioid receptors in a pH-dependent manner, and are thus selective for the receptors in inflamed (acidic) milieu; uses thereof and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: September 15, 2015
    Assignees: CHARITÉ—UNIVERSITÄTSMEDIZIN BERLIN, KONRAD-ZUSE-INSTITUT
    Inventors: Christoph Stein, Marcus Weber, Christian Zöllner, Olga Scharkoi
  • Patent number: 9073827
    Abstract: The present invention provides a method for producing a compound represented by general formula (1) (wherein R1, R2, R3, R10-R14, A1-A3, n1 and n2 are as defined in the description), which is characterized by reacting a compound represented by general formula (2) (wherein R10-R14, A1-A3, n1, n2 and B are as defined in the description) with a diamine compound represented by general formula (3) (wherein R1-R3 are as defined in the description). The present invention is a method for producing a diamine compound, which is useful for the formation of a ruthenium-diamine complex, under mild conditions, said method being able to be put in industrial practice.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: July 7, 2015
    Assignee: TAKASAGO INTERNATIONAL CORPORATION
    Inventors: Taichiro Touge, Tomohiko Hakamata, Hideki Nara
  • Publication number: 20150148333
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: June 6, 2013
    Publication date: May 28, 2015
    Inventors: Brian K. Albrecht, Victor S. Gehling, Alexander M. Taylor, Rishi G. Vaswani
  • Publication number: 20150104384
    Abstract: The present invention relates to certain amido-benzyl sulfoxide and sulfone compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: April 16, 2015
    Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Janet Gunzner-Toste, Bingsong Han, Jian Lin, Xiongcai Liu, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Mark Zak, Yamin Zhang, Guiling Zao, Xiaozhang Zheng, Po-Wai Yuen
  • Publication number: 20150099737
    Abstract: The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
    Type: Application
    Filed: December 12, 2014
    Publication date: April 9, 2015
    Applicant: NOVARTIS AG
    Inventors: Christopher Thomas BRAIN, Young Shin CHO, John William GIRALDES, Bharat LAGU, Julian Roy LEVELL, Michael Joseph LUZZIO, Lawrence Blas PEREZ, Yaping WANG, Fan YANG
  • Publication number: 20150099738
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Application
    Filed: June 30, 2014
    Publication date: April 9, 2015
    Inventors: Mark L. BEHNKE, Alfredo C. CASTRO, Lawrence K. CHAN, Catherine A. EVANS, Louis GRENIER, Michael J. GROGAN, Yves LEBLANC, Tao LIU, Stephane PELUSO, Daniel A. SNYDER, Thomas T. TIBBITTS
  • Publication number: 20150038490
    Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
  • Publication number: 20150018339
    Abstract: Compounds having the general formula II, III, or IV wherein R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle or a radical of an optionally substituted cyclic or acyclic tertiary amine or isoindoline-1,3-dione: R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate, optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Application
    Filed: February 21, 2014
    Publication date: January 15, 2015
    Inventors: Christopher R. MCCURDY, Christophe Mesangeau, Bonnie Ann Avery, Ahmed Hassan Amin Abdelazeem, Frederick T. Chin, Jacques Henri Poupaert
  • Publication number: 20150005292
    Abstract: There is described a method for increasing the maximal tolerated close and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT3 receptor antagonist, a dopamine antagonist, a H1-receptor antagonist, a cannabinoid agonist, aprepitant or casopitant as an antiemetic agent and (b) an acetylcholine esterase inhibitor are also described.
    Type: Application
    Filed: September 18, 2014
    Publication date: January 1, 2015
    Applicant: CHASE PHARMACEUTICALS CORPORATION
    Inventors: Thomas N. CHASE, Kathleen E. CLARENCE-SMITH
  • Publication number: 20140371206
    Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: June 24, 2014
    Publication date: December 18, 2014
    Applicant: Constellation Pharmaceuticals, Inc.
    Inventors: Brian K. Albrecht, James Edmund Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael Charles Hewitt, Yves Leblanc, Christopher G. Nasveschuk, Alexander M. Taylor, Rishi G. Vaswani
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Patent number: 8865701
    Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: February 20, 2010
    Date of Patent: October 21, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20140275019
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • Patent number: 8809381
    Abstract: A compound useful for treating subjects in need of therapy involving sigma receptors or for alleviation of affects resulting from drug abuse having the general formula I in which R1 can be a radical of an optionally substituted C-4 to C-7 N-containing heterocycle such as, for example, radicals of optionally substituted piperidines, optionally substituted piperazines, optionally substituted tetrahydropyridines, optionally substituted azepanes, tertiary amines (cyclic or acyclic), isoindoline-1,3-dione, or optionally substituted tetrahydroisoquinolones (aromatically substituted): R2,3,4,5,6 can each independently be any one or combinations of the following moieties, cyano, nitro, acyl, alkyl, amido, azido, isothiocyanate, isocyanate optionally substituted anilino, halogens, ethers, sulfonamides, thioacyl, nitro, aromatic, heterocyclic, olefinic, acetylene, deuterium, or tritium; Y can be either CH, CH2, O, S, OCH2, N—R, N—Ar, C—R, C—Ar; Z can be either H, O, S, S—R or NR.
    Type: Grant
    Filed: August 18, 2008
    Date of Patent: August 19, 2014
    Assignees: The University of Mississippi, L'Universite Catholique de Louvain
    Inventors: Christopher R. McCurdy, Christophe Mesangeau, Sanju Narayanan, Rae Reiko Matsumoto, Jacques Henri Poupaert
  • Patent number: 8778925
    Abstract: The present invention relates to pyridine and pyrimidine based compounds, pharmaceutical compositions comprising these compounds and their potential use as therapeutic agents for the treatment and/or prevention of cancer.
    Type: Grant
    Filed: October 6, 2009
    Date of Patent: July 15, 2014
    Assignee: Cancer Research Technology Ltd.
    Inventors: Edward McDonald, Julian Blagg, Mark Pichowicz, Simon Ross Crumpler
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Publication number: 20140187534
    Abstract: A compound of the following general formula [I]: wherein each symbol has the same meaning as defined herein, or a pharmaceutically acceptable salt thereof, or a solvate thereof, and a pharmaceutical use of the same in treating organ transplant rejection, graft versus host reaction after transplantation, autoimmune disease, allergic disease and chronic myeloproliferative disease.
    Type: Application
    Filed: November 12, 2013
    Publication date: July 3, 2014
    Applicant: Japan Tobacco Inc.
    Inventors: Satoru Noji, Makoto Shiozaki, Tomoya Miura, Yoshinori Hara, Hiroshi Yamanaka, Katsuya Maeda, Akimi Hori, Masafumi Inoue, Yasunori Hase
  • Publication number: 20140187530
    Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
    Type: Application
    Filed: November 27, 2013
    Publication date: July 3, 2014
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Fenglei Zhang, Brian W. Metcalf
  • Patent number: 8765735
    Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: July 1, 2014
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
  • Publication number: 20140178503
    Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 26, 2014
    Publication date: June 26, 2014
    Applicant: Auspex Pharmaceuticals, Inc.
    Inventors: Ronald C. Newbold, Chengzhi Zhang
  • Publication number: 20140179682
    Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.
    Type: Application
    Filed: June 8, 2012
    Publication date: June 26, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140128371
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
  • Publication number: 20140128375
    Abstract: Compounds of formula I: (wherein variables A1, m, R1, R2, R3, R4 and Z are as described herein) which are antagonists of CGRP receptors and which are 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: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Inventors: Ian M. Bell, Harold B. Selnick
  • Publication number: 20140080801
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. 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: Application
    Filed: November 18, 2013
    Publication date: March 20, 2014
    Applicant: Genentech, Inc.
    Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
  • Publication number: 20140066432
    Abstract: Provided are compositions and methods useful for modulation of signaling through the Toll-like receptors TLR7 and/or TLR8. The compositions and methods have use in treating or preventing disease, including cancer, autoimmune disease, fibrotic disease, cardiovascular disease, infectious disease, inflammatory disorder, graft rejection, or graft-versus-host disease.
    Type: Application
    Filed: January 12, 2012
    Publication date: March 6, 2014
    Inventors: James Jeffry Howbert, Robert Hershberg, Laurence E. Burgess, Hong Woon Yang
  • Publication number: 20140066428
    Abstract: The present invention relates to compounds defined by formula I wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.
    Type: Application
    Filed: November 5, 2013
    Publication date: March 6, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Stephan-Georg MUELLER, Christopher John BROWN, Alexander HEIFETZ, Bernd NOSSE, Juergen PRESTLE, Natacha PREVOST, Klaus RUDOLF, Stefan SCHEUERER, Marcus SCHINDLER, Dirk STENKAMP, Leo THOMAS, Heather TYE
  • Patent number: 8637501
    Abstract: Novel MCH-1 receptor antagonists are disclosed. These compounds are used in the treatment of various disorders, including obesity, anxiety, depression, non-alcoholic fatty liver disease, and psychiatric disorders. Methods of making these compounds are also described in the present invention.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: January 28, 2014
    Assignee: Albany Molecular Research, Inc.
    Inventors: Peter R. Guzzo, Matthew David Surman, James Francis Grabowski, Jr., Emily Elizabeth Freeman
  • Publication number: 20140005174
    Abstract: Disclosed are the CCR2 antagonists of Formula I: I or pharmaceutically acceptable salt thereof wherein R7, A, X, B, and n are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.
    Type: Application
    Filed: March 14, 2012
    Publication date: January 2, 2014
    Inventors: Anilkumar G. Nair, Joseph A. Kozlowski, Jose S. Duca, Stuart B. Rosenblum
  • Publication number: 20130331369
    Abstract: The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of a disorder or a disease mediated by the ghrelin receptor.
    Type: Application
    Filed: August 8, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Ameet Vijay Ambarkhane, Gurdip Bhalay, Martin Beckett, James Dale, Ahmed Hamadi, Alessandro Mazzacani, Jeffrey McKenna, Christopher Thomson
  • Publication number: 20130302282
    Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.
    Type: Application
    Filed: October 21, 2011
    Publication date: November 14, 2013
    Applicant: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Patent number: 8575149
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 5, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Jeffrey Smith, Brian Smith
  • Patent number: 8575148
    Abstract: This invention concerns spiro azepane-ox-azolidinones as voltage gated Kv1.3 potassium channel blockers, pharmaceutical compositions containing these compounds, methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in the treatment of diabetes, psoriasis, obesity, transplant rejection and inflammatory neuropathies, including T-cell mediated autoimmune diseases such as rheumatoid arthritis and multiple sclerosis. The compounds have formula (1): wherein R1, R2, (R3)n, and (R4)m have the meanings given in the specification.
    Type: Grant
    Filed: December 10, 2009
    Date of Patent: November 5, 2013
    Assignee: Abbott Healthcare Products B.V.
    Inventors: Pieter Smid, Michael Mlinaric, Konrad F. Koehler, Sara Nuñez Garcia, Elmar Wegener, Josephus H. M. Lange
  • Patent number: 8546379
    Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: October 1, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Brian Smith, Jeffrey Smith
  • Patent number: 8546378
    Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.
    Type: Grant
    Filed: March 12, 2012
    Date of Patent: October 1, 2013
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
  • Publication number: 20130231327
    Abstract: Substituted spiro-amide compounds corresponding to formula I in which R5 through R8, D, X, Y and Z have defined meanings, processes for preparing such spiro-amide compounds, pharmaceutical compositions containing such compounds, and methods of using such spiro-amide compounds for treating and/or inhibiting disorders or disease states mediated at least in part by the bradykinin 1 receptor.
    Type: Application
    Filed: April 15, 2013
    Publication date: September 5, 2013
    Applicant: Gruenenthal GmbH
    Inventor: Gruenenthal GmbH
  • Publication number: 20130225558
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. 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: Application
    Filed: February 18, 2011
    Publication date: August 29, 2013
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20130131042
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Application
    Filed: August 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu