Bicyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/412)
  • Patent number: 10328054
    Abstract: Provided herein are compounds of the formula (I), as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment or prevention of mGluR5 mediated disorders, such as acute and/or chronic neurological disorders, cognitive disorders and memory deficits, as well as acute and chronic pain.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: June 25, 2019
    Assignee: Hua Medicine (Shanghai) Ltd.
    Inventors: Li Chen, Yuejiao Duan, Jin She, Chengde Wu
  • Patent number: 10316045
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: June 11, 2019
    Assignee: PFIZER INC.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Patent number: 10273244
    Abstract: The disclosure provides compounds having formula (I), wherein the substituents are as defined herein. The compounds are useful for modulating the dopamine D3 receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: April 30, 2019
    Assignee: INDIVIOR UK LIMITED
    Inventors: Fabrizio Micheli, Susanna Cremonesi, Teresa Semeraro, Luca Tarsi
  • Patent number: 10092544
    Abstract: The invention relates to a composition comprising melatonin, a metabolite or derivative thereof and coenzyme Q10 and to use thereof for the production of a pharmaceutical or cosmetic composition for the treatment of the skin, said composition potentiating the movement of both molecules into the mitochondrion and facilitating percutaneous absorption, in which both the melatonin and the CoQ10 can reach all of the strata of the skin.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: October 9, 2018
    Assignee: Universidad de Granada
    Inventors: Germaine Escames Rosa, Darío Acuña Castroviejo, Luis Carlos López Garcia
  • Patent number: 9895335
    Abstract: The present invention relates to compositions comprising a 4-nitrooxybutan-1-ol alkyl ester as nitric oxide donor. More specifically, the invention relates to compositions comprising 4-nitrooxybutan-1-ol alkyl ester as a nitric oxide donor and an ophthalmic drug, useful in controlling elevated intraocular pressure associated with glaucoma or ocular hypertension associated with other diseases or conditions. The invention is also directed to methods of controlling intraocular pressure utilizing said compositions.
    Type: Grant
    Filed: July 7, 2014
    Date of Patent: February 20, 2018
    Assignee: NICOX SCIENCE IRELAND
    Inventors: Ennio Ongini, Nicoletta Almirante, Laura Storoni, Elena Bastia
  • Patent number: 9850204
    Abstract: Provided herein are bicyclic compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders. Compounds provided herein inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations containing the compounds are also provided.
    Type: Grant
    Filed: September 10, 2015
    Date of Patent: December 26, 2017
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott C. Malcolm, Michael C. Hewitt
  • Patent number: 9770436
    Abstract: The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3, 4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: September 26, 2017
    Assignee: EUTHYMICS BIOSCIENCE, INC.
    Inventors: Eric J. Hagen, Kevin Halloran
  • Patent number: 9725412
    Abstract: The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form ? and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form ? with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process.
    Type: Grant
    Filed: July 29, 2015
    Date of Patent: August 8, 2017
    Assignee: Mylan Laboratories Limited
    Inventors: Ramakoteswara Rao Jetti, Chetan Kanaiyalal Raval, Aggi Ramireddy Bommareddy, Debashish Datta
  • Patent number: 9605002
    Abstract: The invention provides a series of 5,5-heteroaromatic compounds, syntheses thereof, compositions thereof, and methods of using such compounds and compositions. Various embodiments provide methods of killing and/or inhibiting the growth of M. tuberculosis and/or M. avium, and methods of treating, preventing, and/or ameliorating M. tuberculosis and/or M. avium infections in a subject. In various embodiments, the 5,5-heteroaromatic compound is N-(4-(4-chlorophenoxy)benzyl)-2,6-dimethylimidazo[2,1-b]thiazole-5-carboxamide.
    Type: Grant
    Filed: July 18, 2013
    Date of Patent: March 28, 2017
    Assignee: UNIVERSITY OF NOTRE DAME DU LAC
    Inventors: Garrett Moraski, Marvin J. Miller
  • Patent number: 9585870
    Abstract: The present disclosure relates to the use of pharmaceutical agents to manipulate serotonin in animal mammary glands. Use of the serotonin agents results in increased PTHrP levels, resulting in the release of calcium from the bone, which improves lactation.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: March 7, 2017
    Assignees: UNIVERSITY OF CINCINNATI, WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Nelson Horseman, Laura Hernandez Baumgard
  • Patent number: 9585877
    Abstract: A method of administering an effective amount of (R)-7-chloro-N-(quinuclidin-3-yl)benzo[b]thiophene-2-carboxamide, or a pharmaceutically acceptable salt thereof, to a patient in need thereof.
    Type: Grant
    Filed: May 6, 2013
    Date of Patent: March 7, 2017
    Assignee: Forum Pharmaceuticals, Inc.
    Inventors: Dana C. Hilt, Gerhard Koenig
  • Patent number: 9566264
    Abstract: The present disclosure relates to novel methods of treating pain comprising administering to a human in need thereof an effective amount of (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and/or pharmaceutically acceptable salt form, substantially free of the corresponding (?) enantiomer, wherein the human is a heavy drinker and/or binge drinker and/or wherein the human has compromised liver function and/or wherein the human is a codeine non-responder. The present disclosure also relates to a method of treating pain comprising concurrently or sequentially administering to a patient in need thereof an effective amount of (a) (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and/or pharmaceutically acceptable salt form, and (b) acetaminophen. The present disclosure also relates to a method of treating pain comprising simultaneously or sequentially administering to a patient in need thereof an effective amount of (a) (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: February 14, 2017
    Assignee: EUTHYMICS BIOSCIENCE, INC.
    Inventors: Frank Bymaster, Anthony McKinney
  • Patent number: 9233083
    Abstract: Therapeutic compositions and methods for treatment of late-onset Gaucher disease are described herein. The compositions comprise compounds having activity as pharmacological chaperones for mutant forms of the beta-glucocerebrosidase. Methods of treatment involve providing therapeutically effective amounts of such compositions to subjects in need thereof.
    Type: Grant
    Filed: April 17, 2014
    Date of Patent: January 12, 2016
    Assignees: The Hospital for Sick Children, McMaster University
    Inventors: Don J. Mahuran, Michael B. Tropak, Justin D. Buttner, Jan E. Blanchard, Eric D. Brown
  • Patent number: 9199933
    Abstract: Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: December 1, 2015
    Inventor: Ramamohan Rao Davuluri
  • Patent number: 9139521
    Abstract: The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: September 22, 2015
    Assignee: EUTHYMICS BIOSCIENCE, INC.
    Inventors: Eric J. Hagen, Kevin Halloran
  • Patent number: 9067931
    Abstract: The invention relates to novel 2-heteroaryl carboxamides and to the use thereof for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.
    Type: Grant
    Filed: April 25, 2014
    Date of Patent: June 30, 2015
    Assignee: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Joachim Luithle, Frank-Gerhard Boess, Christina Erb, Frank-Thorsten Hafner, Katrin Schnizler, Timo Flessner, Marja Van Kampen, Franz-Josef Van Der Staay
  • Publication number: 20150148399
    Abstract: The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
    Type: Application
    Filed: September 23, 2014
    Publication date: May 28, 2015
    Inventors: Phil SKOLNICK, Anthony BASILE, Zhengming CHEN, Joseph W. Epstein
  • Patent number: 9034319
    Abstract: A method of treating a cancer of the central nervous system in a subject in need thereof is provided. The method comprising administering to the subject a therapeutically effective amount of an agent which reduces blood glutamate levels and enhances brain to blood glutamate efflux to thereby treat the cancer of the central nervous system in the subject.
    Type: Grant
    Filed: May 26, 2008
    Date of Patent: May 19, 2015
    Assignee: Yeda Research and Development Co. Ltd.
    Inventors: Vivian I. Teichberg, Angela Ruban-Matuzani
  • Publication number: 20150126493
    Abstract: The invention provides bicyclic sulfone compounds, pharmaceutical compositions, methods of inhibiting RORy activity, reducing the amount of iL-17 in a subject, and treating immune disorders and inflammatory disorders using such bicyclic sulfone compounds. Another aspect of the invention provides a method of treating a subject suffering from a medical disorder. The method comprises administering to the subject a therapeutically effective amount of one or more bicyclic sulfone compounds described herein. In certain other embodiments, the disorder is rheumatoid arthritis.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 7, 2015
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Vladimir Simov, Willam D. Thomas, Peter L. Toogood, Chad A. Van Huis
  • Patent number: 9023885
    Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: March 8, 2013
    Date of Patent: May 5, 2015
    Assignee: Natrogen Therapeutics International, Inc.
    Inventors: Longgui Wang, Xiao Mei Liu, Lian Mo, Simon K. Mencher, James P. McCarron, Jr.
  • Patent number: 9012489
    Abstract: Substituted phenyl-3-aza-bicyclo[3.1.0]hex-3-yl-methanones which are glycine transporter-1 (GlyT1) inhibitors. These are useful for the treatment of schizophrenia, Alzheimer's Disease and other neurological and psychiatric disorders.
    Type: Grant
    Filed: July 27, 2012
    Date of Patent: April 21, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Riccardo Giovannini, Barbara Bertani, Marco Ferrara, Iain Lingard, Rocco Mazzaferro, Holger Rosenbrock
  • Publication number: 20150105375
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • Patent number: 9006283
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: April 14, 2015
    Assignee: Acumen Pharmaceuticals, Inc.
    Inventors: Grant A. Krafft, Todd Pray, William F. Goure
  • Publication number: 20150094345
    Abstract: The present invention is related to a pharmaceutical formulation containing ramipril with improved stability, which comprises ramipril and a desintegrant directly granulated with a binder.
    Type: Application
    Filed: February 17, 2012
    Publication date: April 2, 2015
    Applicant: EGIS GYOGYSZERGYAR ZRT.
    Inventors: Andras Feher, Zsolt Zsigmond, György Újfalussy, Péter Tonkanagy, György Morovjan
  • Publication number: 20150087626
    Abstract: There is described a novel group of cyclic amine derivative compounds, having an EP4 receptor antagonistic activity and specifically pharmaceutical compounds which are useful for the treatment or alleviation of Prostaglandin E mediated diseases. The present invention therefore relates to novel compounds which are selective antagonists of the EP4 subtype of PGE2 receptors with analgesic and antinflammatory activity, processes for their preparation, pharmaceutical compositions containing them and their use as medicaments, inter alia for the treatment or alleviation of Prostaglandin E mediated diseases such as acute and chronic pain, osteoarthritis, inflammation-associated disorder as arthritis, rheumatoid arthritis, cancer, migraine and endometriosis.
    Type: Application
    Filed: July 4, 2011
    Publication date: March 26, 2015
    Inventors: Manuela Borriello, Sabrina Pucci, Luigi Piero Stasi, Lucio Rovati
  • Publication number: 20150087686
    Abstract: It comprises a cocrystal of saxagliptin hydrochloride and a compound selected from the group consisting of saxagliptin, glycolic acid, malonic acid, and urea; or a solvate thereof, or a hydrate thereof. It also comprises a salt of saxagliptin with glycolic acid 1:1 hydrate. It also comprises their preparation processes, as well as their use as antidiabetics.
    Type: Application
    Filed: April 24, 2013
    Publication date: March 26, 2015
    Applicant: ENANTIA, S.L.
    Inventors: Nicolas Tesson, Montserrat Trilla Castaño, Lydia Cárdenas Romaña, Llorenç Rafecas Jané
  • Publication number: 20150087628
    Abstract: K-Ras is the most frequently mutated oncogene in human cancer. Disclosed herein are compositions and methods for modulating K-Ras and treating cancer.
    Type: Application
    Filed: April 10, 2013
    Publication date: March 26, 2015
    Inventors: Jonathan Ostrem, Ulf Peters, Kevan M. Shokat
  • Publication number: 20150080448
    Abstract: Combination between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}-benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an NMDA glutamatergic receptor antagonist. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and neurodegenerative diseases.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Aurore SORS, Caryn Trocme-Thibierge, Annette Merdes
  • Publication number: 20150080379
    Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
    Type: Application
    Filed: November 26, 2014
    Publication date: March 19, 2015
    Inventors: Caryn TROCME-THIBIERGE, Aurore SORS, Florence KEIME-GUIBERT
  • Publication number: 20150080382
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: June 24, 2014
    Publication date: March 19, 2015
    Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
  • Publication number: 20150080325
    Abstract: This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein (I), Q, J, L and Z are as defined in the specification.
    Type: Application
    Filed: April 1, 2014
    Publication date: March 19, 2015
    Applicant: EnVivo Pharmaceuticals, Inc.
    Inventors: Kathryn Rogers, Holger Patzke
  • Publication number: 20150080378
    Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
    Type: Application
    Filed: November 25, 2014
    Publication date: March 19, 2015
    Inventors: Caryn TROCME-THIBIERGE, Aurore Sors, Florence Keime-Guibert
  • Publication number: 20150080447
    Abstract: A composition including as an active ingredient an extract of a plant of the family Mesembryanthemaceae with mesembrenol and mesembrenone as the two major alkaloids present. The invention also relates to the use of the composition as a PDE4 inhibitor and as a serotonin-uptake inhibitor, preferably applied in formulations for the use of the composition as a dual serotonin-uptake inhibitor and PDE4 inhibitor. The invention extends to compositions, such as pharmaceutical compositions or compositions used as dietary supplements, the total alkaloid content of which includes at least 80% (w/w) combined content of mesembrenol and mesembrenone, less than 5% (w/w) mesembrine, and at least 7% (w/w) mesembranol.
    Type: Application
    Filed: July 15, 2014
    Publication date: March 19, 2015
    Inventors: Nigel Gericke, Alan Harvey, Alvaro Viljoen, Deon Hofmeyr
  • Patent number: 8980935
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 27, 2013
    Date of Patent: March 17, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Patent number: 8980338
    Abstract: A composition including as an active ingredient an extract of a plant of the family Mesembryanthemaceae with mesembrenol and mesembrenone as the two major alkaloids present. The invention also relates to the use of the composition as a PDE4 inhibitor and as a serotonin-uptake inhibitor, preferably applied in formulations for the use of the composition as a dual serotonin-uptake inhibitor and PDE4 inhibitor. The invention extends to compositions, such as pharmaceutical compositions or compositions used as dietary supplements, the total alkaloid content of which includes at least 80% (w/w) combined content of mesembrenol and mesembrenone, less than 5% (w/w) mesembrine, and at least 7% (w/w) mesembranol.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: March 17, 2015
    Assignee: H.L. Hall & Sons Limited
    Inventors: Nigel Gericke, Alan Harvey, Alvaro Viljoen, Deon Hofmeyr
  • Publication number: 20150050335
    Abstract: The present disclosure relates to methods for making extended-release formulations of water-soluble active pharmaceutical ingredients such as metformin HCl. In one aspect, the disclosure provides a method that includes adding an aqueous solution of an active pharmaceutical ingredient to an agitated mixture of one or more release-modifying polymers and optionally one or more binders in one or more organic solvents, the one or more organic solvents together being an antisolvent for the active pharmaceutical ingredient, water being sufficiently soluble in the one or more organic solvents such that the water added as part of the aqueous solution dissolves in the mixture, the addition thereby precipitating the active pharmaceutical ingredient; separating the active pharmaceutical ingredient and the one or more release-modifying polymers and, if present, the one or more binders from the one or more organic solvents to yield co-processed particles; and drying the co-processed particles.
    Type: Application
    Filed: February 28, 2013
    Publication date: February 19, 2015
    Inventors: Deniz Erdemir, Shih-Ying Chang, Divyakant Desai, San Kiang
  • Publication number: 20150031737
    Abstract: The present invention provides a stabilized controlled-release pharmaceutical composition comprising gliclazide and sodium citrate as stabilizing agent; and process for the preparation of said pharmaceutical composition.
    Type: Application
    Filed: February 23, 2013
    Publication date: January 29, 2015
    Inventors: Ravindra Agarwal, Ajay Kumar Dobhal, Ravi Kochhar
  • Patent number: 8940785
    Abstract: Association between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an acetylcholinesterase inhibitor. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and with neurodegenerative diseases.
    Type: Grant
    Filed: May 1, 2012
    Date of Patent: January 27, 2015
    Assignee: Les Laboratoires Servier
    Inventors: Caryn Trocme-Thibierge, Aurore Sors, Florence Keime-Guibert
  • Publication number: 20150005277
    Abstract: The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Application
    Filed: June 21, 2014
    Publication date: January 1, 2015
    Inventors: Zhiwei Wang, Yunhang Guo
  • Publication number: 20150005260
    Abstract: The present invention relates to methods and kits for detecting diastolic dysfunction in subjects without clinical signs of heart failure.
    Type: Application
    Filed: January 2, 2013
    Publication date: January 1, 2015
    Inventors: Faiez Zannad, Patrick Rossignol
  • Publication number: 20150005359
    Abstract: The present disclosure relates to novel methods of treating pain comprising administering to a human in need thereof an effective amount of (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and/or pharmaceutically acceptable salt form, substantially free of the corresponding (?) enantiomer, wherein the human is a heavy drinker and/or binge drinker and/or wherein the human has compromised liver function and/or wherein the human is a codeine non-responder. The present disclosure also relates to a method of treating pain comprising concurrently or sequentially administering to a patient in need thereof an effective amount of (a) (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, in free and/or pharmaceutically acceptable salt form, and (b) acetaminophen. The present disclosure also relates to a method of treating pain comprising simultaneously or sequentially administering to a patient in need thereof an effective amount of (a) (1R,5S)-(+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.
    Type: Application
    Filed: July 1, 2014
    Publication date: January 1, 2015
    Inventors: Frank BYMASTER, Anthony MCKINNEY
  • Patent number: 8921409
    Abstract: Combination between 4-{3-[cis-hexahydrocyclopenta[c]pyrrol-2(1H)-yl]propoxy}-benzamide of formula (I): or an addition salt thereof with a pharmaceutically acceptable acid or base, and an NMDA glutamatergic receptor antagonist. Medicinal products containing the same which are useful in the treatment of cognitive disturbances associated with cerebral ageing and neurodegenerative diseases.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: December 30, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Aurore Sors, Caryn Trocme-Thibierge, Annette Merdes
  • Patent number: 8912199
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: December 16, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
  • Patent number: 8906911
    Abstract: Disclosed herein are chemokine receptor antagonists of formula (I) wherein R1, R2, and R3 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 9, 2014
    Assignee: AbbVie Inc.
    Inventors: Michael D. Meyer, Xueqing Wang, Tao Guo, Robert Guo Ping Wei, Lijuan Jane Wang
  • Patent number: 8901157
    Abstract: The present invention discloses compositions and a method of improving the pharmacokinetics of pharmaceutical agents (or pharmaceutically acceptable salts, esters, and prodrugs thereof) which are metabolized by cytochrome P450 monoxygenase comprising coadministering ritonavir or a pharmaceutically acceptable salt, ester, and prodrug thereof.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: December 2, 2014
    Assignee: AbbVie Inc.
    Inventors: Dale J. Kempf, Kennan C. Marsh
  • Publication number: 20140343037
    Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
  • Publication number: 20140343065
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 20, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Riccardo GIOVANNINI, Yunhai CUI, Henri DOODS, Marco FERRARA, Stefan JUST, Raimund KUELZER, Iain LINGARD, Rocco MAZZAFERRO, Klaus RUDOLF
  • Patent number: 8883852
    Abstract: Provided herein are methods, for reducing, preventing, mitigating and treating damage caused by radiation. The methods comprise delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation or to mitigate apoptosis. The compounds comprise glyburide or other sulfonylurea hypoglycemic compounds or potassium channel inhibitors.
    Type: Grant
    Filed: October 21, 2009
    Date of Patent: November 11, 2014
    Assignee: University of Pittburgh—Of the Commonwealth System of Higher Education
    Inventors: Michael Epperly, Joel Greenberger, Jianfei Jiang, Valerian Kagan, John Lazo, Peter McDonald
  • Publication number: 20140329836
    Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: December 5, 2013
    Publication date: November 6, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
  • Patent number: 8877798
    Abstract: The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.
    Type: Grant
    Filed: May 5, 2013
    Date of Patent: November 4, 2014
    Assignee: Neurovance, Inc.
    Inventors: Phil Skolnick, Anthony Basile, Zhengming Chen, Joseph W. Epstein