The Ring Nitrogen Is Bonded Directly To Two Ring Carbons Of The Same Cyclo Which Carbons Are Members Of One Cyclo Only (e.g., Cyclopenta(c)pyrroles, Etc.) Patents (Class 548/515)
  • Patent number: 9540324
    Abstract: Compounds that selectively negatively modulate NMDA receptors containing an NR1/NR2B subunit, pharmaceutical compositions comprising the compounds, and methods of treating a disease using the compounds are disclosed.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: January 10, 2017
    Assignee: LUC THERAPEUTICS, INC.
    Inventors: David R. Anderson, Robert A. Volkmann, Frank S. Menniti
  • Patent number: 9447052
    Abstract: This invention relates to methods of making a compound of formula (I) and intermediates for same the compounds of formula (I) being useful for treating cardiovascular and inflammatory diseases such as atherosclerosis.
    Type: Grant
    Filed: May 17, 2011
    Date of Patent: September 20, 2016
    Assignee: Glaxo Group Limited
    Inventors: Kevin Stuart Cardwell, Claire Frances Crawford, Suzanne Helen Davies, Charles Edward Wade
  • Patent number: 9393204
    Abstract: Methods and compositions are provided for formulating and administering bicifadine and related compounds to treat or prevent functional impairment and disabilities associated with acute pain, chronic pain, and neuropathic disorders.
    Type: Grant
    Filed: June 2, 2013
    Date of Patent: July 19, 2016
    Assignee: EBI Life Sciences, Inc.
    Inventors: Arnold S. Lippa, Warren Stern, Johnson Lim
  • Patent number: 9133117
    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: October 24, 2013
    Date of Patent: September 15, 2015
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott C. Malcolm, Michael C. Hewitt
  • Patent number: 9133159
    Abstract: The invention provides novel 1-heteroaryl-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 but not limited to depression and anxiety.
    Type: Grant
    Filed: April 3, 2013
    Date of Patent: September 15, 2015
    Assignee: NEUROVANCE, INC.
    Inventors: Phil Skolnick, Zhengming Chen
  • 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: 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: 8952179
    Abstract: Industrial synthesis process for the compound of formula (I):
    Type: Grant
    Filed: December 11, 2013
    Date of Patent: February 10, 2015
    Assignee: Les Laboratories Servier
    Inventors: Nicolas Robert, Jean-Michel Lerestif, Jean-Pierre Lecouve, Marina Gaillard, Loic Meunier, Philippe Letellier, Mathieu Boiret
  • 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: 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
  • Publication number: 20140323689
    Abstract: Process for the preparation of a viral protease inhibitor and intermediates useful in its preparation.
    Type: Application
    Filed: April 21, 2014
    Publication date: October 30, 2014
    Applicant: DIPHARMA FRANCIS S.r.I.
    Inventors: Anna IULIANO, Varsha Ravindra JUMDE, Emanuele ATTOLINO, Maurizio TADDEI
  • Patent number: 8859784
    Abstract: The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M?, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
    Type: Grant
    Filed: November 11, 2011
    Date of Patent: October 14, 2014
    Assignee: Codexis, Inc.
    Inventors: Jack Liang, James Lalonde, Jun Zhu, John M. Gruber, John D. Munger, Jr.
  • Patent number: 8796470
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein ?, R1, R2, R3, and R4 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: August 5, 2014
    Assignee: AbbVie Inc.
    Inventors: Xenia B. Searle, Ming C. Yeung, Michael R. Schrimpf
  • Patent number: 8772313
    Abstract: The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: July 8, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
  • Patent number: 8765801
    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: February 3, 2012
    Date of Patent: July 1, 2014
    Assignee: Euthymics Bioscience, Inc.
    Inventors: Eric J. Hagen, Kevin Halloran
  • Publication number: 20140179638
    Abstract: The present invention relates to 9-aminomethyl substituted tetracycline compounds represented by formula (I), or pharmaceutically acceptable salt, prodrug, solvate or isomer thereof, as well as a method for preparing these compounds and a pharmaceutical composition comprising the same. The present invention relates also to a use of these compounds in the preparation of a medicament for the treatment and/or prophylaxis of tetracycline drug-sensitive disease. wherein, R2a, R2b, R3, R4a, R4b, R5, R6a, R6b, R7, R8, R9a, R9b, R10, R11, R12, R13a and R13b are each independently as defined in the description.
    Type: Application
    Filed: July 26, 2012
    Publication date: June 26, 2014
    Applicant: KBP BIOSCIENCES CO., LTD.
    Inventors: Hui Zhang, Yanyan Dong
  • Publication number: 20140179922
    Abstract: The present invention relates to a process for the preparation of Lurasidone or a pharmaceutically acceptable salt thereof, a compound useful for the treatment of schizophrenia and bipolar disorder. The present invention further relates to processes for the preparation of Lurasidone intermediates, and to certain novel intermediates obtained by such processes.
    Type: Application
    Filed: June 13, 2012
    Publication date: June 26, 2014
    Applicant: MAPI PHARMA LTD.
    Inventors: Ehud Marom, Michael Mizhiritskii, Susanna Tchilibon, Shai Rubnov
  • Publication number: 20140163240
    Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.
    Type: Application
    Filed: July 18, 2013
    Publication date: June 12, 2014
    Inventors: Jerry A. Murry, Edwin G. Corley, Feng Xu, Bryon Simmons
  • Publication number: 20140107175
    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 re-uptake 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: Application
    Filed: October 24, 2013
    Publication date: April 17, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Liming SHAO, Fengjiang Wang, Scott C. Malcolm, Michael C. Hewitt
  • Publication number: 20140107318
    Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
    Type: Application
    Filed: December 17, 2013
    Publication date: April 17, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Gerald J. Tanoury, Minzhang Chen, John E. Cochran, Valdas Jurkauskas
  • Publication number: 20140100374
    Abstract: Industrial synthesis process for the compound of formula (I):
    Type: Application
    Filed: December 11, 2013
    Publication date: April 10, 2014
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Nicolas ROBERT, Jean-Michel Lerestif, Jean-Pierre Lecouve, Marina Gaillard, Loic Meunier, Philippe Letellier, Mathieu Boiret
  • Patent number: 8691865
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Grant
    Filed: May 24, 2011
    Date of Patent: April 8, 2014
    Assignee: AbbVie Inc.
    Inventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
  • Publication number: 20140094616
    Abstract: Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.
    Type: Application
    Filed: May 17, 2012
    Publication date: April 3, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tetsuya Ikemoto, Leopold Mpaka Lutete, Toshiaki Aikawa
  • Patent number: 8664408
    Abstract: Industrial synthesis process for, and crystalline form I of, the compound of formula (I): and also crystalline form I of the associated free base. Medicinal products containing the same which are useful in the treatment of disorders of the histaminergic system.
    Type: Grant
    Filed: June 6, 2012
    Date of Patent: March 4, 2014
    Assignee: Les Laboratoires Servier
    Inventors: Nicolas Robert, Jean-Michel Lerestif, Jean-Pierre Lecouve, Marina Gaillard, Philippe Letellier, Mathieu Boiret, Julie Meunier
  • Publication number: 20140058116
    Abstract: The present invention relates to synthetic processes useful in the preparation of compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease and have application in the treatment of conditions caused by HCV. In particular, the present invention relates to novel oxidation processes useful for preparing compounds of Formula (I) and related compounds, including pharmaceutically acceptable salts, hydrates and solvates thereof, and including stereoisomers thereof.
    Type: Application
    Filed: May 2, 2012
    Publication date: February 27, 2014
    Inventors: Ji Xie, George Wu, Joseph Lamberson, Marc Poirier, Frank Chen
  • Publication number: 20140005165
    Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A 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, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
  • Publication number: 20130345439
    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: May 5, 2013
    Publication date: December 26, 2013
    Inventors: Phil SKOLNICK, Anthony Basile, Zhengming Chen, Joseph W. Epstein
  • Publication number: 20130345279
    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: Application
    Filed: May 31, 2013
    Publication date: December 26, 2013
    Inventor: ERIC J. HAGEN
  • Patent number: 8592608
    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 uptake 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: December 15, 2009
    Date of Patent: November 26, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Liming Shao, Fengjiang Wang, Scott C. Malcolm, Michael C. Hewitt
  • Patent number: 8586765
    Abstract: A process for preparing 3-amino-3-cyclobutylmethyl-2-hydroxypropionamide of the Formula I: or a salt thereof involves providing a compound of the Formula VI described herein in a solution comprising predominately dimethylsulfoxide (DMSO) and converting this compound directly to the compound of the Formula VIII described herein without working up or isolating the intermediate compound of the Formula VII described herein.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: November 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuan Dong, Jeonghan Park, Eugene John Vater
  • Publication number: 20130253029
    Abstract: The present invention relates to novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to processes for the synthesis of novel compounds of Formula I, their pharmaceutically acceptable derivatives, tautomeric forms, isomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention further provides pharmaceutical compositions comprising compounds of Formula I and methods of treating or preventing one or more disorders of the central and/or peripheral nervous system, preferably by modulating neurological and/or psychiatric targets (GPCR and/or non-GPCR).
    Type: Application
    Filed: September 27, 2011
    Publication date: September 26, 2013
    Applicant: Panacea Biotec Ltd
    Inventors: Rajesh Jain, Sanjay Trehan, Jagattaran Das, Nishan Singh, Sudhir Kumar Sharma
  • Patent number: 8529882
    Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: September 10, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Robert Edward Babine, Shu Hui Chen, Ivan Collado, Cristina Garcia-Paredes, John Irvin Glass, Ling Jin, Jason Eric Lamar, Raymond Samuel Parker, III, Nancy June Snyder, Xicheng David Sun, Deqi Guo, Yvonne Yee Mai Yip, Q. May Wang, Frantz Victor, Mark Joseph Tebbe, Robert B. Perni, Luc Farmer
  • Patent number: 8524760
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: April 10, 2012
    Date of Patent: September 3, 2013
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Publication number: 20130197011
    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: Application
    Filed: July 27, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Riccardo GIOVANNINI, Barbara BERTANI, Marco FERRARA, Iain LINGARD, Rocco MAZZAFERRO, Holger ROSENBROCK
  • Publication number: 20130172276
    Abstract: The invention relates to compounds and processes useful for the preparation of protease inhibitors, particularly serine protease inhibitors. The protease inhibitors are useful for treatment of HCV infections.
    Type: Application
    Filed: February 14, 2013
    Publication date: July 4, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: VERTEX PHARMACEUTICALS INCORPORATED
  • Publication number: 20130150578
    Abstract: The present invention relates to novel hypoglycemic compounds of formula (1) and pharmaceutically acceptable salts thereof.
    Type: Application
    Filed: April 1, 2011
    Publication date: June 13, 2013
    Applicant: CADILA PHARMACEUTICALS LIMITED
    Inventors: Bakulesh Mafatlal Khamar, Chandan Singh, Rajiv Indravadan Modi
  • Patent number: 8461196
    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: February 3, 2012
    Date of Patent: June 11, 2013
    Inventors: Phil Skolnick, Anthony Basile, Zhengming Chen, Joseph W. Epstein
  • Publication number: 20130096277
    Abstract: A process for preparing enantioselectively a compound of formula I-1a or I-1b: over a compound of formulas I-2-I-7:
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventor: Vertex Pharmaceuticals Incorporated
  • Patent number: 8420122
    Abstract: The present invention provides a method of continuous precipitation and isolation of an amorphous solid particulate form of 3-[2-(3-tert-Butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dimethyl-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid (2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide having controlled physical properties. The present invention provides also pharmaceutical formulations comprising the precipitated compound.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: April 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dimitrios Zarkadas, Vincenzo Liotta, Christopher Stanley Pridgen, Wing-Kee Philip Cho, Zhihui Qiu
  • Publication number: 20130072456
    Abstract: The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: October 26, 2012
    Publication date: March 21, 2013
    Applicant: Laboratorios del Dr. Esteve, S.A.
    Inventor: Laboratorios del Dr. Esteve, S.A.
  • Patent number: 8372990
    Abstract: The present invention relates to substituted bicyclic tetrahydropyrrole compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: April 30, 2007
    Date of Patent: February 12, 2013
    Assignee: Laboratorios Del Dr. Esteve S.A.
    Inventors: Miguel Angel Pericas-Brondo, Antonio Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobés, Carmen Garcia Granda
  • Publication number: 20130028843
    Abstract: The present invention relates to the crystal structure of the serine protease kallikrein 7 and to the use of this crystal structure in drug discovery. The present invention also relates to compounds binding specifically to this active site of kallikrein 7.
    Type: Application
    Filed: October 10, 2012
    Publication date: January 31, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Publication number: 20130012705
    Abstract: Disclosed are new dicycloazaalkane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and the uses for treatment especially for dipeptidyl peptidase inhibitor (DPP-IV), in which each substitute group of general formula (I) is as defined in specification.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 10, 2013
    Applicant: Jiangsu Hansoh Pharmaceutical Co., Ltd.
    Inventors: Peng Cho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li, Fanglong Yang, Jianghong Fu, Lin Wang, Guangyuan Shen, Dongliang Guan
  • Publication number: 20120316214
    Abstract: Industrial synthesis process for, and crystalline form I of, the compound of formula (I): and also crystalline form I of the associated free base. Medicinal products containing the same which are useful in the treatment of disorders of the histaminergic system.
    Type: Application
    Filed: June 6, 2012
    Publication date: December 13, 2012
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Nicolas ROBERT, Jean-Michel LERESTIF, Jean-Pierre LECOUVE, Marina GAILLARD, Loïc MEUNIER, Philippe LETELLIER, Mathieu BOIRET, Julie Meunier
  • Publication number: 20120302619
    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: February 3, 2012
    Publication date: November 29, 2012
    Inventors: Phil SKOLNICK, Anthony Basile, Zhengming Chen, Joseph W. Epstein
  • Publication number: 20120294935
    Abstract: The present invention provides a method of continuous precipitation and isolation of an amorphous solid particulate form of 3-[2-(3-tert-Butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dimethyl-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid (2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide having controlled physical properties. The present invention provides also pharmaceutical formulations comprising the precipitated compound.
    Type: Application
    Filed: May 25, 2012
    Publication date: November 22, 2012
    Inventors: Dimitrios Zarkadas, Vincenzo Liotta, Christopher Stanley Pridgen, Wing-Kee Philip Cho, Zhihui Qiu
  • Publication number: 20120289709
    Abstract: The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, wherein A, M, M?, and R5 are as described herein, and to biocatalytic processes for their preparation, and to the enzymes used in those processes.
    Type: Application
    Filed: May 7, 2012
    Publication date: November 15, 2012
    Applicant: CODEXIS, INC.
    Inventors: James Lalonde, Tao Li, Jack Liang, Benjamin Mijts, Roger Sheldon, George S.K. Wong, Aleksey Zaks
  • Publication number: 20120282219
    Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 3, 2012
    Publication date: November 8, 2012
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: ROBERT EDWARD BABINE, SHU HUI CHEN, IVAN COLLADO, CRISTINA GARCIA-PAREDES, JOHN IRVIN GLASS, DEQI GUO, LING JIN, JASON ERIC LAMAR, RAYMOND SAMUEL PARKER, III, NANCY JUNE SNYDER, XICHENG DAVID SUN, MARK JOSEPH TEBBE, FRANTZ VICTOR, Q. MAY WANG, YVONNE YEE MAI YIP, ROBERT B. PERNI, LUC FARMER
  • Patent number: 8198463
    Abstract: The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (1S,2R,5R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII.
    Type: Grant
    Filed: April 9, 2010
    Date of Patent: June 12, 2012
    Assignee: Schering Corporation
    Inventors: George Wu, Frank X. Chen, Paitoon Rashatasakhon, Jeffrey M. Eckert, George S. K. Wong, Hong-Chang Lee, Nolan C. Erickson, Jennifer Ann Vance, Peter C. Nirchio, Juergen Weber, David Jieh-Shyh Tsai, Nanfei Zou
  • Publication number: 20120142940
    Abstract: The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (?)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence.
    Type: Application
    Filed: February 3, 2012
    Publication date: June 7, 2012
    Inventors: Jerry A. MURRY, Edward G. Corley, Feng Xu, Bryon Simmons