Bicyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos (e.g., Octahydroindoles, Etc.) Patents (Class 548/452)
Plural ring hetero atoms in the bicyclo ring system, or ring nitrogen is shared by the two cyclos of the bicyclo ring system (Class 548/453)
Additional polycyclo heterocyclic ring system attached directly or indirectly to the bicyclo ring system by nonionic bonding (Class 548/454)
Additional hetero ring, attached directly or indirectly to the bicyclo ring system by nonionic bonding (Class 548/465)
The bicyclo ring system consists of the five-membered hetero ring and a benzene ring (e.g., indole, etc.) (Class 548/469)
Chalcogen bonded directly to ring carbon of the five-membered hetero ring (e.g., adrenochrome, etc.) (Class 548/512)
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.) (Class 548/515)
Two double bonds between ring members of the five-membered hetero ring (e.g., 4,5,6,7-tetrahydroindoles, etc.) (Class 548/516)
  • Method for the synthesis of a ramipril intermediate
    Patent number: 8263784
    Abstract: The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.
    Type: Grant
    Filed: October 27, 2009
    Date of Patent: September 11, 2012
    Assignee: DSM Sinochem Pharmaceuticals Netherlands B.V.
    Inventors: Ben De Lange, Dennis Heemskerk
  • Dendrimer conjugates
    Patent number: 8252834
    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.
    Type: Grant
    Filed: March 12, 2009
    Date of Patent: August 28, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: James R. Baker, Jr., Xue-min Cheng, Thommey P. Thomas, Baohua Mark Huang
  • Crystal forms of saxagliptin and processes for preparing same
    Patent number: 8236847
    Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: August 7, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
  • Bisulfite purification of an alpha-keto amide
    Patent number: 8222427
    Abstract: This disclosure relates to novel processes useful in the purification of keto-amide, ketone and aldehyde compounds, which are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease and have application in the treatment of conditions caused by HCV. The processes of this disclosure relate to purification via a bisulfite adduct. In particular, this disclosure relates to processes useful in the purification of the keto-amide compound of Formula I, (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]-amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: July 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: George S. K. Wong, Jeonghan Park, Tetsuo Iwama, Anantha R. Sudhakar
  • ENANTIO- AND STEREO-SPECIFIC SYNTHESES OF BETA-AMINO-ALPHA- HYDROXY AMIDES
    Publication number: 20120178942
    Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.
    Type: Application
    Filed: July 27, 2010
    Publication date: July 12, 2012
    Inventors: John Traverse, William M. Leong, Steven P. Miller, Jennifer Albaneze-Walker, Thomas J. Hunter, Lijun Wang, Hongbiao Liao, Ashok Arasappan, Scott T. Trzaska, Randi M. Smith, Azzeddine Lekhal, Stephane L. Bogen, Jianshe Kong, Frank Bennett, F. George Njoroge, Marc Poirier, Shen-Chun Kuo, Yonggang Chen, Kenneth S. Matthews, Patrice Demonchaux, Amadeo Ferreira
  • Process for producing cyclic N-hydroxy imide compounds
    Patent number: 8217182
    Abstract: A cyclic polycarboxylic acid anhydride, a polycarboxylic acid, or a mixture of them is allowed to react with hydroxylamine or a salt thereof in an organic solvent under dewatering conditions to yield a corresponding cyclic N-hydroxyimide compound. The cyclic polycarboxylic acid anhydride can be, for example, succinic anhydride or glutaric anhydride. The polycarboxylic acid can be, for example, succinic acid, glutaric acid, or adipic acid. In this process, the reaction is preferably carried out using an organic solvent capable of undergoing azeotropy with water as all or part of a reaction solvent while removing water from the reaction system by azeotropy with the organic solvent. This process produces a cyclic N-hydroxyimide compound in a good yield from any of a cyclic polycarboxylic acid anhydride and a polycarboxylic acid.
    Type: Grant
    Filed: July 28, 2009
    Date of Patent: July 10, 2012
    Assignee: Daicel Chemical Industries, LTD.
    Inventor: Yasuteru Kajikawa
  • Small molecule inhibition of PDZ-domain interaction
    Patent number: 8211934
    Abstract: Novel compounds that have been found effective in inhibiting PDZ domain interactions, and particularly interactions of PDZ domains in MAGIs with the oncogenic (tumor suppressor) protein PTEN and interactions between the PDZ domain in the Dishevelled (Dvl) protein and other proteins such as the Frizzled (Fz) protein, have the general formula (I) or (III). The invention also includes combinatorial libraries, arrays and methods for screening and studying proteins using such compounds. Compounds of the invention have produced apoptosis in certain cell lines that overexpress the Dishevelled protein (Dvl), inhibiting Wnt signaling.
    Type: Grant
    Filed: August 4, 2010
    Date of Patent: July 3, 2012
    Assignee: The Regents of the University of California
    Inventors: Rodney Kiplin Guy, Naoaki Fujii, Liang You, David M. Jablons
  • Nitroreductase enzymatic substrates
    Patent number: 8211662
    Abstract: The present invention relates to an enzyme substrate for detecting nitroreductase activity of formula (I) below: in which X is S, NX1, O or NX1-CO; R1 is nothing or a substituent selected from Cl, CH3, Br, F, I, alkyl, aryl and carboxyl; R2 is nothing or a substituent selected from Cl, O—CH2—O, O—CH3, F, diethylenediamine-CH3, NR3R4, Br, I, alkyl, aryl, carboxyl, NO2 and R3 and R4 are independently H or an alkyl group containing from 1 to 4 carbon atoms; and X1 is selected from H, CH3, C2H4Ph, OH, alkyl and aryl.
    Type: Grant
    Filed: May 29, 2008
    Date of Patent: July 3, 2012
    Assignee: Biomerieux
    Inventors: Olivier Fabrega, Arthur James, Vindhya Lakshika Salwatura, Sylvain Orenga, Stephen Stanforth
  • Angiotensin II receptor antagonists
    Patent number: 8207208
    Abstract: A compound having the structure R—Y wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2)(C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is Y1 is selected from the group consisting of —C(O)—O— and —P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: May 6, 2009
    Date of Patent: June 26, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • Tetrahydroindole derivatives for treatment of alzheimer's disease
    Patent number: 8203004
    Abstract: Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: November 3, 2006
    Date of Patent: June 19, 2012
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: Frank Burkamp, Graham David Checksfield, Stephen Robert Fletcher, Stephen John Lewis, Edward Giles Mciver, Paul Joseph Oakley, Martin Richard Teall
  • Process for the preparation of 6,6-dimethyl-3-azabicyclo-[3.3.0]-hexane compounds and enantiomeric salts thereof
    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
  • HCV protease inhibitors and uses thereof
    Patent number: 8188137
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: May 29, 2012
    Assignee: Avila Therapeutics, Inc.
    Inventors: Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh
  • Stereomerically Pure Fused Bicyclic Proline Compounds Useful for Preparing Hepatitis C Protease Inhibitors
    Publication number: 20120130087
    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: November 11, 2011
    Publication date: May 24, 2012
    Applicant: CODEXIS, INC.
    Inventors: Benjamin Mijts, Sheela Muley, Jack Liang, Lisa M. Newman, Xiyun Zhang, James Lalonde, Michael D. Clay, Jun Zhu, John M. Gruber, Jeffrey Colbeck, John D. Munger, JR., Jagadeesh Mavinahalli, Roger Sheldon
  • Derivatives of azabicyclo octane, the method of making them and the uses thereof as inhibitors of dipeptidyl peptidase IV
    Patent number: 8178575
    Abstract: Derivatives of azabicyclo octane presented by formula (I), the method of making them, and the compositions containing the same and the uses thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV), wherein the substitutes in formula (I) have the same meanings as what is mentioned in the descriptions.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: May 15, 2012
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hansoh Pharmaceutical Co., Ltd.
    Inventors: Pengcho Tang, Zhigang Lin, Hejun Lü, Fuqiang Zhao, Li Li
  • Synthesis of thieno[3,4-b]thiophene, thieno[3,4-b]furan, related compounds and their derivatives and use thereof
    Patent number: 8168671
    Abstract: Inexpensive and facile methods of preparing fused heterocycles such as thieno[3,4-b]thiophene, thieno[3,4-b]furan, related compounds, and their derivatives are disclosed. Also disclosed are regioregular polymers prepared from the fused heterocycles.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: May 1, 2012
    Assignee: The University of Connecticut
    Inventor: Gregory A. Sotzing
  • 2-AZA-BICYCLO[2.2.1]HEPTANE COMPOUNDS AND USES THEREOF
    Publication number: 20120094995
    Abstract: This invention relates to 2-aza-bicyclo[2.2.1]heptane compounds (and salts thereof), the process for making such a compound and pharmaceutical compositions comprising such a compound. The invention also relates to the use of the compounds for modulating the glycine transporter 1 (GlyT1) and for the treatment of psychosis, cognitive disorders, bipolar disorders, depression disorders, anxiety disorders, post-traumatic stress disorders and pain.
    Type: Application
    Filed: January 27, 2010
    Publication date: April 19, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Jeffrey Scott Albert, Donald Andisik, Cristobal Alhambra, Todd Andrew Brugel, Glen E Ernst, William Frietze, Lindsay Hinkley, Jeffrey Gilbert Varnes, Xia Wang, Hui Xiong
  • CRYSTAL FORMS OF SAXAGLIPTIN
    Publication number: 20120088808
    Abstract: The present invention relates to novel polymorphic forms of Saxagliptin Hydrochloride. The present invention also relates to methods of making polymorphic forms of Saxagliptin Hydrochloride.
    Type: Application
    Filed: April 9, 2010
    Publication date: April 12, 2012
    Applicant: SANDOZ AG
    Inventors: Arthur Pichler, Josef Wieser, Christoph Langes, Milica Vukicevic
  • POLYMORPHS OF SAXAGLIPTIN HYDROCHLORIDE AND PROCESSES FOR PREPARING THEM
    Publication number: 20120083517
    Abstract: The invention provides polymorphs of Saxagliptin hydrochloride, processes for preparing polymorphs of Saxagliptin hydrochloride, and pharmaceutical compositions of polymorphs of Saxagliptin hydrochloride.
    Type: Application
    Filed: October 4, 2011
    Publication date: April 5, 2012
    Inventors: Marina Marinkovic, Marina Ratkaj, Oliver Frankovic, Tina Mundorfer
  • N-[(2-AZABICYCLO[2.1.1]HEX-1-YL)-ARYL-METHYL]-BENZAMIDE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    Publication number: 20120071536
    Abstract: The invention relates to N-[(2-aza-bicyclo[2.2.1]hex-1-yl)-aryl-methyl]-benzamide derivatives of the general formula (I) where: R is a hydrogen atom or a (C1-C6)alkyl group, (C3-C7)-cycloalkyl, optionally substituted by one or more fluorine, (C3-C7)-cycloalkyl, (C2-C4)alkenyl, phenyl, (C1-C6)alkoxy, hydroxy; R1 is phenyl or naphtyl optionally substituted by one or more halogen, (C1-C6)alkyl, (C1-C6)alkoxy, halo-(C1-C6)alkyl, NR4R5, (C1-C6)alkylthio, (C1-C6)alkyl-SO2, phenyl or heteroaryl; R2 is one or more hydrogen or halogen atoms, halo-(C1-C6)alkyl, (C1-C6)alkyl, (C3-C7)cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)alkyl; R3, R4 and R5 are independently a hydrogen atom or a (C1-C6)alkyl group; R6 is a (C1-C6)alkyl group; R3 and R4 as well as R3 and R6 may form, together with the atoms having them, a 5- or 6-member ring; R4 and R5 may form together a ring selected from azetidine, pyrrolidine, piperidine, morpholine, thiomorpholine, piperazine, azepine, optionally substituted by a (C1-C6)alkyl group.
    Type: Application
    Filed: February 9, 2010
    Publication date: March 22, 2012
    Applicant: SANOFI
    Inventors: Gihad Dargazanli, Genevieve Estenne-Bouhtou, Abdel-Kader Mafroud
  • Hydroxymethyl ether hydroisoindoline tachykinin receptor antagonists
    Patent number: 8124633
    Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.
    Type: Grant
    Filed: April 7, 2008
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao
  • Amorphous form of an L-arginine salt of perindopril and processes for preparation thereof
    Patent number: 8101646
    Abstract: In illustrative embodiments, there is provided an amorphous form of L-arginine salt of perindopril which may be particularly suitable for pharmaceutical applications, and processes for preparing said form.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: January 24, 2012
    Assignee: Apotex Pharmachem Inc.
    Inventors: Gamini Weeratunga, Carlos B. Zetina-Rocha
  • Processes for the preparation of 4-oxo-octahydro-indole-1-carbocyclic acid methyl ester and derivatives thereof
    Patent number: 8084487
    Abstract: The present invention relates to a process for the production of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester enantiomers and of 1-carbalkoxy-4-ketoperhydroindole enantiomers.
    Type: Grant
    Filed: August 10, 2009
    Date of Patent: December 27, 2011
    Assignee: Novartis AG
    Inventors: Ernst Kuesters, Murat Acemoglu, Philipp Lustenberger, Gottfried Sedelmeier, Beat Schmitz, Gerhard Penn
  • NOVEL POLYMORPHIC FORMS OF PERINDOPRIL (L)-ARGININE AND PROCESS FOR THE PREPARATION THEREOF
    Publication number: 20110301357
    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: Application
    Filed: June 22, 2009
    Publication date: December 8, 2011
    Applicant: MATRIX LABORATORIES LTD
    Inventors: Ramakoteswara Rao Jetti, Chetan Kanaiyalal Raval, Aggi Ramireddy Bommareddy, Debashish Datta
  • Tricyclic angiotensin II agonists
    Patent number: 8067418
    Abstract: There is provided compounds of formula I, wherein the dotted line, X1, X2, X3, A, Y1, Y2, Y3, Y4, Z1, Z2, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: November 29, 2011
    Assignee: Vicore Pharma AB
    Inventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
  • Trans-3-aza-bicyclo[3.1.0]hexane derivatives
    Patent number: 8063099
    Abstract: The invention relates to novel trans-3-aza-bicyclo[3.1.0]hexane derivatives of formula (I), wherein A, B, n and R1 are as described in the description, and to the use of such compounds, or of pharmaceutically acceptable salts of such compounds, as medicaments, especially as orexin receptor antagonists.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: November 22, 2011
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, David Lehman, Thierry Sifferlen, Daniel Trachsel
  • SAXAGLIPTIN INTERMEDIATES, SAXAGLIPTIN POLYMORPHS, AND PROCESSES FOR PREPARATION THEREOF
    Publication number: 20110275687
    Abstract: The invention provides Saxagliptin Schiff bases, polymorphs of Saxagliptin and (1S,3S,5S)-2-[(2S)-2-propan-2-ylideneamino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, processes for preparing Saxagliptin hydrates, and pharmaceutical compositions thereof.
    Type: Application
    Filed: May 5, 2011
    Publication date: November 10, 2011
    Inventors: Marina RATKAJ, Tomislav BILJAN, Marina MARINKOVIC
  • METAL COORDINATED COMPOSITIONS
    Publication number: 20110275792
    Abstract: A metal coordination complex of a biologically active moiety and a metal is disclosed. The complex confers to the biologically active moiety an improved performance which can include potency, stability, absorbability, targeted delivery, and combinations thereof.
    Type: Application
    Filed: July 15, 2011
    Publication date: November 10, 2011
    Inventor: Thomas Piccariello
  • PPAR active compounds
    Patent number: 8053463
    Abstract: Compounds are described that are active on at least one of PPAR?, PPAR?, and PPAR?, which are useful for therapeutic and/or prophylactic methods involving modulation of at least one of PPAR?, PPAR?, and PPAR?, wherein the compounds have the formula: wherein: X2 and X3 are independently CH or N; and one of X1 and X4 is N or CR4 and the other of X1 and X4 is N or CH.
    Type: Grant
    Filed: March 5, 2008
    Date of Patent: November 8, 2011
    Assignee: Plexxikon Inc.
    Inventors: Jack Lin, Byunghun Lee, Shenghua Shi, Chao Zhang, Dean R. Artis, Prabha N. Ibrahim, Weiru Wang, Rebecca Zuckerman
  • Hepatitis C Virus Inhibitors
    Publication number: 20110269956
    Abstract: The present disclosure relates to methods for making compounds useful in the treatment of Hepatitis C virus (HCV) infection.
    Type: Application
    Filed: October 29, 2010
    Publication date: November 3, 2011
    Inventors: Shawn K. Pack, Steven Tymonko, Bharat P. Patel, Kenneth J. Natalie, JR., Makonen Belema
  • METHOD FOR THE SYNTHESIS OF A RAMIPRIL INTERMEDIATE
    Publication number: 20110263871
    Abstract: The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril.
    Type: Application
    Filed: October 27, 2009
    Publication date: October 27, 2011
    Inventors: Ben De Lange, Dennis Heemskerk
  • Nitric Oxide Releasing Prodrugs of Therapeutic Agents
    Publication number: 20110263526
    Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.
    Type: Application
    Filed: April 22, 2011
    Publication date: October 27, 2011
    Applicant: PIRAMAL LIFE SCIENCES LIMITED
    Inventor: Apparao SATYAM
  • Hepatitis C virus inhibitors
    Patent number: 8044087
    Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: October 25, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Alan Xiangdong Wang, Ramkumar Rajamani, Paul Michael Scola
  • ENANTIOSELECTIVE PROCESS FOR CYCLOALKENYL ?-SUBSTITUTED ALANINES
    Publication number: 20110257408
    Abstract: A process for preparing an enantiomerically enriched cycloalkene-substituted alanine compound having the structure: by asymmetrically hydrogenating a dehydro amino acid compound having the structure: in a suitable reaction media in the presence of a catalyst having a transition metal moiety complexed to a chiral phosphine ligand to prepare enantiomerically enriched cycloalkene substituted alanine compounds having the structure of Formula (IA) or (IB), which are key intermediates for the ACE inhibitors ramipril and perindolpril:
    Type: Application
    Filed: April 20, 2011
    Publication date: October 20, 2011
    Applicant: Chiral Quest, Inc.
    Inventors: Zijun Liu, Sanhui Lin, Wenge Li, Jingyang Zhu, Xinjun Liu, Xiaojuan Zhang, Hui Lu, Fei Xiong, Zhongwei Tian
  • Tetrahydrofuro[3,2-b] pyrrol-3-one intermediates
    Patent number: 8039641
    Abstract: The present invention relates to a process for preparing a compound of formula (Ia), (Ib), (Ic) or (Id), or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof, said process comprising the steps of: (A) (i) treating a compound of formula (IVa), where R48 is alkyl or tosyl, with an oxidizing agent to form a compound of formula (Va); and (ii) converting said compound of formula (Va) to a compound of formula (Ia) or (Ic); or (B) (i) treating a compound of formula (IVb), where R48 is alkyl or tosyl, with an oxidizing agent to form a compound of formula (Vb); and (ii) converting said compound of formula (Vb) to a compound of formula (Ib) or (Id).
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: October 18, 2011
    Assignee: Amura Therapeutics Limited
    Inventors: Martin Quibell, James Nally, Lee Patient, Yikang Wang, Claudio Dagostin, John Paul Watts
  • Polymorphic form of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,3-dihydro-1h-pyrrolizin-5-ylacetic acid
    Patent number: 8034837
    Abstract: The present invention relates to a new crystalline modification of 6-(4-chlorophenyl)-2,2-dimethyl-7-phenyl-2,S-dihydro-1H-pyrrolizin-S-ylacetic acid which is referred to as polymorph B. It has a peak in the solid state 13C-NMR spectrum (with adamantane as external reference standard; CH group d=29.45 ppm) in the range from 179.8 to 180.2 ppm and can be processed directly to a pharmaceutical formulation.
    Type: Grant
    Filed: March 20, 2006
    Date of Patent: October 11, 2011
    Assignee: Merckle GmbH
    Inventors: Wolfgang Albrecht, Thomas Kammermeier, Hans-Gunter Striegel, Philipp Merckle, Stefan Laufer
  • 6-SUBSTITUTED SULFONYL AZABICYCLO[3.2.1]OCTANES USEFUL TO INHIBIT 11Beta-HYDROXYSTEROID DEHYDROGENASE TYPE-1
    Publication number: 20110237559
    Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: August 12, 2008
    Publication date: September 29, 2011
    Applicant: Schering Corporation
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
  • 2-arylindole derivatives as nPGES-1 inhibitors
    Patent number: 8017644
    Abstract: A 2-arylindole compound substituted in position 5, of formula (I): in which X, Y, Z, W, A, R and R? have the meanings given in the description, a pharmaceutical composition comprising it, and also intermediate compounds and a preparation process therefor.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: September 13, 2011
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
    Inventors: Maria Alessandra Alisi, Nicola Cazzolla, Barbara Garofalo, Guido Furlotti, Caterina Maugeri, Rosella Ombrato, Isabella Coletta, Lorenzo Polenzani, Giorgina Mangano, Beatrice Garrone, Angelo Guglielmotti
  • Fluorescent diketopyrrolopyrroles
    Patent number: 8008507
    Abstract: The present invention relates to fluorescent diketopyrrolopyrroles of the formula (I), or (III), a process for their preparation and their use for the preparation of inks, colorants, pigmented plastics for coatings, non-impact-printing material, color filters, cosmetics, polymeric ink particles, toners, as fluorescent tracers, in color changing media, in solid dye lasers, EL lasers and electroluminescent devices. A luminescent device comprising a compound, or composition according to the present invention is high in the efficiency of electrical energy utilization and high in luminance.
    Type: Grant
    Filed: November 30, 2005
    Date of Patent: August 30, 2011
    Assignee: BASF SE Ludwigshafen
    Inventors: Hiroshi Yamamoto, Hidetaka Oka, Mathias Düggeli
  • SUBSTITUTED BICYCLIC AMINES FOR THE TREATMENT OF DIABETES
    Publication number: 20110207737
    Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.
    Type: Application
    Filed: November 11, 2009
    Publication date: August 25, 2011
    Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
  • Addition salts of angiotensin-converting enzyme inhibitors with no donor acids, a process for their preparation and pharmaceutical compositions containing them
    Patent number: 7981920
    Abstract: Compounds of formula (I): (A)m·(B)n??(I) wherein A represents an angiotensin-converting enzyme inhibitor compound containing at least one salt-forming basic function, B represents a compound containing at least one salt-forming acid function and at least one NO donor group, m represents the number of acid functions of B that have been converted to a salt and n represents the number of basic functions of A that have been converted to a salt, the bond or bonds between A and B being of the ionic type. Medicinal products containing the same which are useful in treating cardiovascular pathologies.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: July 19, 2011
    Assignee: Les Laboratoires Servier
    Inventors: Guillaume De Nanteuil, Bernard Portevin, Philippe Gloanec, Jean-Gilles Parmentier, Alain Benoist, Tony Verbeuren, Alain Rupin, Christine Courchay, Serge Simonet
  • Process for the synthesis of an ACE inhibitor
    Patent number: 7973173
    Abstract: A process for the synthesis of trandolapril which comprises condensing N—[I—(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride with trans octahydro-1H-indole-2-carboxylic acid in a first organic solvent comprising a water immiscible inert organic solvent and in the presence of a base, and isolating trandolapril from a second organic solvent. N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride may also be condensed with (2S,3aR,7aS) octahydro-1H-indole-2-carboxylic acid in a first organic solvent and in the presence of a base, and trandolapril isolated. There is also provided a process for the resolution of racemic trans octahydro-1H-indole-2-carboxylc acid.
    Type: Grant
    Filed: July 5, 2006
    Date of Patent: July 5, 2011
    Assignee: Cipla Limited
    Inventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Manjinder Singh Phull, Ashwini Sawant, Dilip Ramdas Birari
  • Process of making 3-aminopentanenitrile
    Patent number: 7973174
    Abstract: A process for making 3-aminopentanenitrile from a crude 2-pentenenitrile (“crude 2PN”) comprising 2-pentenenitrile, 2-methyl-2-butenenitrile, and 2-methyl-3-butenenitrile includes contacting the crude 2PN with an ammonia-containing fluid and water. The ammonia-containing fluid can include at least one reactant selected from the group consisting of ammonia, aqueous ammonia, and ammonium hydroxide.
    Type: Grant
    Filed: October 18, 2005
    Date of Patent: July 5, 2011
    Assignee: Invista North America S.A.R.L.
    Inventor: Ronald L. Amey
  • PROCESSES FOR THE PREPARATION OF 4-OXO-OCTAHYDRO-INDOLE-1-CARBOCYCLIC ACID METHYL ESTER AND DERIVATIVES THEREOF
    Publication number: 20110144352
    Abstract: The present invention relates to a process for the production of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester enantiomers and of 1-carbalkoxy-4-ketoperhydroindole enantiomers.
    Type: Application
    Filed: August 10, 2009
    Publication date: June 16, 2011
    Applicant: NOVARTIS AG
    Inventors: Ernst Kuesters, Murat Acemoglu, Philipp Lustenberger, Gottfried Sedelmeier, Beat Schmitz, Gerhard Penn
  • Pharmaceutical intermediate for synthesizing ACE inhibitors and the use thereof
    Patent number: 7960558
    Abstract: The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.
    Type: Grant
    Filed: May 11, 2007
    Date of Patent: June 14, 2011
    Assignee: Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Márta Porcs-Makkay, Gyula Simig, Tibor Mezei, Angéla Veressné Pandur, Gyula Lukács
  • NOVEL PEPTIDES AS NS3-SERINE PROTEASE INHIBITORS OF HEPATITIS C VIRUS
    Publication number: 20110117057
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Application
    Filed: December 20, 2010
    Publication date: May 19, 2011
    Applicants: SCHERING CORPORATION, DENDREON CORPORATION
    Inventors: Anil K. Saksena, Viyyoor Moopil Girijavallabhan, Raymond G. Lovey, Edwin Jao, Frank Bennett, Jinping L. McCormick, Haiyan Wang, Russell E. Pike, Stephane L. Bogen, Tin-Yau Chan, Yi-Tsung Liu, Zhaoning Zhu, F. George Njoroge, Ashok Arasappan, Tejal Parekh, Ashit K. Ganguly, Kevin X. Chen, Srikanth Venkatraman, Henry A. Vaccaro, Patrick A. Pinto, Bama Santhanam, Scott Jeffrey Kemp, Odile Esther Levy, Marguerita Lim-Wilby, Susan Y. Tamura, Wanli Wu, Siska Hendrata, Yuhua Huang
  • Polymorphic and pseudopolymorphic forms of trandolaprilat, pharmaceutical compositions and methods for production and use
    Patent number: 7943655
    Abstract: The present invention provides novel polymorphic and pseudopolymorphic forms of Trandolaprilat, including crystalline Trandolaprilat Form A, crystalline Trandolaprilat Form B, crystalline Trandolaprilat Form C, crystalline Trandolaprilat Form D, crystalline Trandolaprilat Form E, and mixtures thereof. The invention also provides novel methods for producing Trandolaprilat, pharmaceutically acceptable salts of Trandolaprilat, and polymorphic and pseudopolymorphic forms of Trandolaprilat, pharmaceutical compositions including one or more novel Trandolaprilat compounds and methods for treating high blood pressure and/or cardiac insufficiency using one or more novel Trandolaprilat compounds.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: May 17, 2011
    Assignee: Universitat Zurich
    Inventor: Thomas Bader
  • Crystal forms of saxagliptin and processes for preparing same
    Patent number: 7943656
    Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: May 17, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
  • SELECTIVE HYDROXAMIC ACID BASED MMP-12 AND MMP-13 INHIBITORS
    Publication number: 20110112076
    Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
    Type: Application
    Filed: July 13, 2009
    Publication date: May 12, 2011
    Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
  • Dipeptidyl Peptidase-IV Inhibitors
    Publication number: 20110112051
    Abstract: The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes.
    Type: Application
    Filed: January 13, 2011
    Publication date: May 12, 2011
    Applicant: Alantos Pharmaceuticals Holding, Inc.
    Inventors: Heiko KROTH, Tim Feuerstein, Frank Richter, Jürgen Boer, Michael Essers, Bert Nolte, Matthias Schneider, Matthias Hochguertel, Fritz-Frieder Frickel, Arthur Taveras, Christoph Steeneck
  • Pleuromutilin derivatives as antimicrobials
    Patent number: RE43390
    Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
    Type: Grant
    Filed: October 27, 1998
    Date of Patent: May 15, 2012
    Assignees: GlaxoSmithKline LLC, SmithKline Beecham Limited
    Inventors: Valerie Joan Berry, Steven Dabbs, Colin Henry Frydrych, Eric Hunt, Francis Dominic Sanderson, Gary Woodnutt