Additional Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 546/126)
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Patent number: 10350199Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: August 3, 2016Date of Patent: July 16, 2019Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
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Patent number: 9815829Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is C1-C4alkyl, C1-C4haloalkyl or C3-C6cycloalkyl; each R2 is independently bromo, chloro, fluoro or trifluoromethyl; R3 is hydrogen; R4 is hydrogen, halogen, methyl, halomethyl or cyano; or R3 and R4 together form a bridging 1,3-butadiene group; R5 is chlorodifluoromethyl or trifluoromethyl; n is 2 or 3; by reacting a compound of formula (II) wherein A1, A2, R1, R2, R3, R4, R5 and n is as defined under formula (I) above, with hydroxylamine, a base and a chiral catalyst, characterized in that the chiral catalyst is a dimeric chiral catalyst of formula (III) wherein R6, R7, R8, R9, R10 and X are as defined in claim 1.Type: GrantFiled: August 4, 2015Date of Patent: November 14, 2017Assignee: Syngenta Participations AGInventors: Tomas Smejkal, Helmars Smits
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Patent number: 9346755Abstract: While methodologies for the Kinetic Resolution of alcohols are well established, no analogous direct methods exist for the highly selective, direct catalytic Kinetic Resolution of thiols (i.e., R—SH). The present invention relates to a method for resolving stereoisomeric mixtures of thiols. In particular, the present invention relates to purely organocatalytic mediated resolution of enantiomeric mixtures of thiols without the need for enzymes. Also disclosed are some novel catalysts. Such catalysts may comprise a cinchona alkaloid-derived moiety.Type: GrantFiled: September 25, 2014Date of Patent: May 24, 2016Assignee: THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH, NEAR DUBLIN TRINITY COLLEGE, UNIVERSITY OF DUBLINInventors: Stephen Joseph Connon, Aldo Peschiulli, Barbara Procuranti
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Publication number: 20150148344Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula I wherein R1, R2, R3, R4, R7, W, X, and Z are as described herein.Type: ApplicationFiled: November 21, 2014Publication date: May 28, 2015Inventors: Kerim Babaoglu, Britton K. Corkey, Robert H. Jiang, David Sperandio, Hai Yang
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Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
Publication number: 20150079028Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.Type: ApplicationFiled: August 5, 2013Publication date: March 19, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTDInventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo -
Patent number: 8962653Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: October 1, 2013Date of Patent: February 24, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
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Patent number: 8946429Abstract: While methodologies for the Kinetic Resolution of alcohols are well established, no analogous direct methods exist for the highly selective, direct catalytic Kinetic Resolution of thiols (i.e., R—SH). The present invention relates to a method for resolving stereoisomeric mixtures of thiols. In particular, the present invention relates to purely organocatalytic mediated resolution of enantiomeric mixtures of thiols without the need for enzymes. Also disclosed are some novel catalysts. Such catalysts may comprise a cinchona alkaloid-derived moiety.Type: GrantFiled: December 7, 2010Date of Patent: February 3, 2015Assignee: The Provost, Fellows, Foundation Scholars, and the other Members of the Board, of the College of the Holy and Undivided Trinity of Queen Elizabeth, Near DublinInventors: Stephen Joseph Connon, Aldo Peschiulli, Barbara Procuranti
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Publication number: 20150030683Abstract: In certain embodiments the methods of preventing or delaying the onset of a pre-Alzheimer's condition and/or cognitive dysfunction, and/or ameliorating one or more symptoms of a pre-Alzheimer's cognitive dysfunction, and/or preventing or delaying the progression of a pre-Alzheimer's condition or cognitive dysfunction to Alzheimer's disease, and/or of promoting the processing of amyloid precursor protein (APP) by the non-amyloidogenic pathway are provided. In certain embodiments the methods involve administering, or causing to be administered, to a subject in need thereof certain formulations comprising or more active agent(s) selected from the group consisting of tropisetron disulfiram, honokiol, nimetazepam, and/or derivatives or analogs thereof.Type: ApplicationFiled: February 15, 2013Publication date: January 29, 2015Inventors: Varghese John, Dale E. Bredesen, Stelios Tzannis
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Publication number: 20150010632Abstract: Aerosol formulations of granisetron useful for pulmonary delivery are provided. The formulations are useful in the reduction, elimination or prevention of nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. Also provided are novel methods to treat chemotherapy-induced nausea and vomiting (CINV), radiation-induced nausea and vomiting (RINV), and post-operative nausea and vomiting (PONV) using the inhalation formulations.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Applicant: Luxena Pharmaceuticals, Inc.Inventors: George Lu, Xiaodong Li
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Publication number: 20140364451Abstract: In various embodiments, compositions and methods are provided for treatment and/or prevention of amyloidogenic diseases. In certain embodiments, the methods entail administering an effective amount of a tropinol ester to a subject in need thereof for prophylactic or therapeutic effect. The methods are particularly useful for prophylactic and therapeutic treatment of Alzheimer's disease. In certain embodiments, methods of reducing the risk, lessening the severity, or delaying the progression or onset of a disease characterized by beta-amyloid deposits in the brain of a mammal are also provided. In certain embodiments, methods of directly or indirectly inhibiting the C-terminal cleavage of APP resulting in the formation of APP-C31 peptide and APPneo (AP-P664) in a mammal are provided.Type: ApplicationFiled: August 1, 2012Publication date: December 11, 2014Applicant: BUCK INSTITUTE FOR RESEARCH ON AGINGInventors: Varghese John, Dale E. Bredesen
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Patent number: 8859535Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: GrantFiled: June 19, 2012Date of Patent: October 14, 2014Assignee: Novartis AGInventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
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Publication number: 20140303143Abstract: Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Mark E. Layton, Joseph E. Pero, Hannah Fiji, Michael J. Kelly, III, Pablo de Leon, Michael A. Rossi, Kevin F. Gilbert, Anthony J. Roecker, Zhijian Zhao, Swati I P. Mercer, Scott Wolkenberg, James Mulhearn, Lianyun Zhao, Dansu Li
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Patent number: 8853241Abstract: The invention relates to biaryl substituted azabicyclic alkane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: January 27, 2011Date of Patent: October 7, 2014Assignee: AbbVie Inc.Inventors: Jianguo Ji, Tao Li, Kevin B. Sippy, Chih-Hung Lee, Murali Gopalakrishnan
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Publication number: 20140275020Abstract: This invention relates to compounds of Formula I having the following general structure: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 25, 2012Publication date: September 18, 2014Inventors: Shawn P. Walsh, Alexander Pasternak, Zhi-Cai Shi, Brian Cato
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Patent number: 8835457Abstract: The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma.Type: GrantFiled: June 14, 2013Date of Patent: September 16, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: John W. Lampe, Paul S. Watson, David J. Slade
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Patent number: 8815956Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.Type: GrantFiled: August 10, 2012Date of Patent: August 26, 2014Assignee: Senomyx, Inc.Inventors: Catherine Tachdjian, Xiao-Qing Tang, Donald S. Karanewsky, Guy Servant, Xiaodong Li, Feng Zhang, Qing Chen, Hong Zhang, Timothy James Davis, Vincent Darmohusodo, Melissa Sue Wong, Victor Selchau
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Publication number: 20140235669Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: April 28, 2014Publication date: August 21, 2014Applicant: ANIONA APSInventors: Dan PETERS, Gordon MUNRO, Elsebet Ostergaard NIELSEN, Karin Sandager NIELSEN
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Publication number: 20140221341Abstract: A compound of formula (I): wherein: M is hydrogen or a pharmaceutically acceptable salt-forming cation; Y is OR1 or NR2R3, and R1, R2, R3 and M are as defined herein. Also, methods of treating bacterial infection, pharmaceutical compositions, molecular complexes and processes for preparing compounds.Type: ApplicationFiled: April 15, 2014Publication date: August 7, 2014Applicant: NAEJA PHARMACEUTICAL INC.Inventors: Samarendra N. MAITI, Dai NGUYEN, Jehangir KHAN, Rong LING
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Patent number: 8785640Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: July 17, 2013Date of Patent: July 22, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Patent number: 8785639Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: December 1, 2010Date of Patent: July 22, 2014Assignee: AbbVie Inc.Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
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Publication number: 20140163063Abstract: The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: October 1, 2013Publication date: June 12, 2014Applicant: THERAVANCE, INC.Inventors: Daniel Marquess, Paul R. Fatheree, S. Derek Turner, Daniel D. Long, Seok-Ki Choi, Adam A. Goldblum, Daniel Genov
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Patent number: 8748457Abstract: The present invention is related to novel 2-Amino-2-[8-(dimethyl carbamoyl)-8-aza-bicyclo[3.2.1]oct-3-yl]-exo-ethanoyl derivatives of the general formula (A), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods of making of the above compounds, and their use as Dipeptidyl Peptidase-IV (DPP-IV) Inhibitors, which are useful in the treatment or prevention of diseases particularly Type II diabetes, other complications related to diabetes and other pathogenic conditions in which DPP IV enzyme is involved.Type: GrantFiled: September 1, 2009Date of Patent: June 10, 2014Assignee: Lupin LimitedInventors: Neelima Sinha, Prathap Nair, Navnath Karche, Nabendu Saha, Rajan Goel, Rajender Kumar Kamboj
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Publication number: 20140135306Abstract: The invention relates to compounds of formula (I): as defined in the application. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of MDM2 and/or MDM4, or variants thereof.Type: ApplicationFiled: June 19, 2012Publication date: May 15, 2014Applicant: Novartis AGInventors: Nicole Buschmann, Pascal Furet, Philipp Holzer, Joerg Kallen, Keiichi Masuya, Stefan Stutz
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Patent number: 8703758Abstract: The present invention provides to a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification.Type: GrantFiled: April 26, 2011Date of Patent: April 22, 2014Assignee: Takeda Pharmaceutical Company LimitedInventors: Tohru Yamashita, Makoto Kamata, Hideki Hirose, Masataka Murakami, Takuya Fujimoto, Zenichi Ikeda, Tsuneo Yasuma, Ikuo Fujimori, Ryo Mizojiri, Tomoya Yukawa
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Publication number: 20140094450Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicant: SANOFIInventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
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Patent number: 8658671Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.Type: GrantFiled: April 13, 2010Date of Patent: February 25, 2014Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
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Publication number: 20140051679Abstract: The present teachings provide a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: October 12, 2012Publication date: February 20, 2014Applicant: UNIVERISTY HEALTH NETWORKSInventors: Heinz W. Pauls, Radoslaw Laufer, Yong Liu, Sze-Wan Li, Bryan T. Forrest, Yunhui Lang, Narendra Kumar B. Patel, Louise G. Edwards, Grace Ng, Peter B. Sampson, Miklos Feher, Donald E. Awrey
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Patent number: 8633218Abstract: The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene derivatives useful as monoamine neurotransmitter re-uptake inhibitors. 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: November 16, 2009Date of Patent: January 21, 2014Assignee: Aniona APSInventors: Dan Peters, David Spencer Jones, Elsebet Østergaard Nielsen
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Patent number: 8609690Abstract: The present invention relates to compounds defined by formula (I) wherein the groups R1 and R2 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: GrantFiled: August 21, 2009Date of Patent: December 17, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Bradford S. Hamilton, Frank Himmelsbach, Stefan Peters
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Publication number: 20130331349Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).Type: ApplicationFiled: November 30, 2011Publication date: December 12, 2013Inventors: David C. Tully, Paul Vincent Rucker, Phillip B. Alper, Daniel Mutnick, Donatella Chianelli
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Patent number: 8592395Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: GrantFiled: July 23, 2010Date of Patent: November 26, 2013Assignee: GlaxoSmithKline LLCInventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
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Publication number: 20130303570Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: July 17, 2013Publication date: November 14, 2013Inventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20130295049Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 30, 2012Publication date: November 7, 2013Applicant: ENANTA PHARMACEUTICALS, INCInventor: ENANTA PHARMACEUTICALS, INC
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Publication number: 20130281485Abstract: The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma.Type: ApplicationFiled: June 14, 2013Publication date: October 24, 2013Inventors: John W. Lampe, Paul S. Watson, David J. Slade
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Patent number: 8513282Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: GrantFiled: October 23, 2009Date of Patent: August 20, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T. D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D. J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20130190351Abstract: This invention relates to bicyclic amide compounds, pharmaceutical compositions and methods for use in the prevention and treatment of a variety of conditions and/or disease states including cerebral insufficiency, through the enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors as defined herein. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in other disorders wherein a deficiency in neurotrophic factors is implicated, as well as other disorders as described herein.Type: ApplicationFiled: July 25, 2012Publication date: July 25, 2013Applicant: CORTEX PHARMACEUTICALS, INC.Inventors: Rudolf Mueller, Leslie Street
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Patent number: 8476295Abstract: The present invention is directed to synthetic bridged bicyclic compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. The method comprises administering to a subject a therapeutically effective amount of a Rho kinase inhibitory compound of Formula I, wherein said amount is effective to influence the actomyosin interactions, for example, by leading to cellular relaxation and alterations in cell-substratum adhesions. In one embodiment, the method treats increased intraocular pressure, such as primary open-angle glaucoma.Type: GrantFiled: December 10, 2010Date of Patent: July 2, 2013Assignee: InspireInventors: John W. Lampe, Paul S. Watson, David J. Slade
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Publication number: 20130137873Abstract: The invention relates to a family of fluorescent compounds that comprise a bridged polycyclo moiety. The compounds can be chemically linked to biomolecules, such as proteins, nucleic acids, and therapeutic small molecules. The compounds can be used for imaging in a variety of medical, biological and diagnostic applications, and are particularly useful for the in vivo imaging of regions of interest within a mammal.Type: ApplicationFiled: July 13, 2012Publication date: May 30, 2013Inventor: Nara Narayanan
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Patent number: 8410271Abstract: This invention relates to chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. 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: November 10, 2009Date of Patent: April 2, 2013Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Jorgen Scheel-Kruger, Elsebet Ostergaard Nielsen
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Patent number: 8404849Abstract: The present invention relates to the process for producing modulators of cystic fibrosis transmembrane conductance regulator (CFTR).Type: GrantFiled: May 20, 2011Date of Patent: March 26, 2013Assignee: Vertex PharmaceuticalsInventors: Lifang Sun, Khisal Ahmed Alvi, Caroline Joyce Decker, Yongmin Li
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Patent number: 8389727Abstract: The present invention relates to substantially crystalline and solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide (Form A-HCl, Form B, Form B-HCl, or any combination of these forms), pharmaceutical compositions thereof, and methods of treatment therewith.Type: GrantFiled: October 21, 2010Date of Patent: March 5, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Beili Zhang, Mariusz Krawiec, Brian Luisi, Ales Medek
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Publication number: 20130041046Abstract: The present invention includes compounds having structural formula (I), or salts or solvates thereof. These compounds are useful as sweet flavor modifiers. The present invention also includes compositions comprising the present compounds and methods of enhancing the sweet taste of compositions.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Applicant: SENOMYX, INC.Inventors: Catherine TACHDJIAN, Xiao Qing TANG, Donald S. KARANEWSKY, Guy SERVANT, Xiaodong LI, Feng ZHANG, Qing CHEN, Hong ZHANG, Timothy James DAVIS, Vincent DARMOHUSODO, Melissa Sue WONG, Victor SELCHAU
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Publication number: 20130040985Abstract: The present application discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the application discloses the use of these compounds, a method for therapy and to pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: January 14, 2011Publication date: February 14, 2013Applicant: NEUROSEARCH A/SInventors: Dan Peters, Gordon Munro, Elsebet Østergaard Nielsen, Karin Sandager Nielsen
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Publication number: 20130040986Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: October 15, 2012Publication date: February 14, 2013Inventors: Hayley Binch, Lev T.D. Fanning, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa
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Publication number: 20120295877Abstract: The present invention relates to compounds of Formula (I) and (Ia) useful in the treatment of CCR5-related diseases and disorders, for example, the prevention or treatment of an HIV infection, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS).Type: ApplicationFiled: July 23, 2010Publication date: November 22, 2012Inventors: Maosheng Duan, Wieslaw Mieczyslaw Kazmierski, Matthew Tallant
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Publication number: 20120276050Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.Type: ApplicationFiled: March 16, 2010Publication date: November 1, 2012Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
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Publication number: 20120238600Abstract: The present invention discloses and claims a series of substituted tropinone benzylamines of formula (I): The compounds of this invention are inhibitors of ?-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted tropinone benzylamines.Type: ApplicationFiled: June 5, 2012Publication date: September 20, 2012Applicant: SANOFIInventors: Yong Mi CHOI-SLEDESKI, Guyan LIANG, Patrick Wai-Kwok SHUM
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Publication number: 20120225884Abstract: The present invention relates to compounds of formula I hetaryl I, hetaryl II, R1, R2, R3, Y, m, and o or to pharmaceutically active acid addition salts thereof. The present compounds of formula I are modulators for amyloid beta and thus, they may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Karlheinz Baumann, Luke Green, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20120214817Abstract: The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.Type: ApplicationFiled: April 30, 2012Publication date: August 23, 2012Inventors: Bruce E Maryanoff, William A. Kinney, Edward C. Lawson, Diane K. Luci, Nikolay Marchenko, Sergey Sviridov, Shyamali Ghosh
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Publication number: 20120208841Abstract: The present invention relates to modulators of cystic fibrosis transmembrane conductance regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating diseases using modulators of CFTR.Type: ApplicationFiled: April 4, 2012Publication date: August 16, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Hayley Binch, Lev T.D. Fanning, Dennis Hurley, Urvi Sheth, Alina Silina, Xiaoqing Yang, Martyn Botfield, Peter D.J. Grootenhuis, Fredrick Van Goor, Mehdi Michel Djamel Numa