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)
  • Compounds and methods for the treatment of pain and other diseases
    Patent number: 8530453
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: September 10, 2013
    Assignee: Aquilus Pharmaceuticals, Inc.
    Inventor: Irving Sucholeiki
  • HCV protease inhibitors and uses thereof
    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
  • Process For Preparing Dipeptidyl Peptidase IV Inhibitors And Intermediates Therefor
    Publication number: 20130204012
    Abstract: A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure prepared by subjecting an acid of the structure to reduce amination by treating the acid with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase/formate dehydrogenase enzyme concentrate (PDH/FDH) and without isolating treating the resulting amine of the structure 2 with di-tert-butyl dicarbonate to form the BOC-protected amine.
    Type: Application
    Filed: January 4, 2013
    Publication date: August 8, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventor: Bristol-Myers Squibb Company
  • Saxagliptin intermediates, saxagliptin polymorphs, and processes for preparation thereof
    Patent number: 8501960
    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: Grant
    Filed: May 5, 2011
    Date of Patent: August 6, 2013
    Assignee: Assia Chemical Industries Ltd.
    Inventors: Marina Ratkaj, Tomislav Biljan, Marina Marinkovic
  • ALKALOID AMINOESTER DERIVATIVES AND MEDICINAL COMPOSITION THEREOF
    Publication number: 20130196978
    Abstract: Alkaloid aminoester compounds which act as muscarinic receptor antagonists are useful for the prevention and/or treatment of a broncho-obstructive or inflammatory diseases.
    Type: Application
    Filed: March 14, 2013
    Publication date: August 1, 2013
    Applicant: Chiesi Farmaceutici S.p.A.
    Inventor: Chiesi Farmaceutici S.p.A.
  • Isoindolones derivatives as MEK kinase inhibitors and methods of use
    Patent number: 8492427
    Abstract: The invention relates to isoindolones of formula, (I) with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
    Type: Grant
    Filed: July 1, 2009
    Date of Patent: July 23, 2013
    Assignee: Genentech, Inc.
    Inventors: Emanuela Gancia, Robert Andrew Heald, Philip Jackson, Stephen Price
  • DIAMINOCYCLOHEXANE COMPOUNDS AND USES THEREOF
    Publication number: 20130184262
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.
    Type: Application
    Filed: July 16, 2012
    Publication date: July 18, 2013
    Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
  • CANNABINOID RECEPTOR MODULATORS
    Publication number: 20130178457
    Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).
    Type: Application
    Filed: July 5, 2012
    Publication date: July 11, 2013
    Applicant: LUPIN LIMITED
    Inventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
  • DELTA CRYSTALLINE FORM OF THE ARGININE SALT OF PERINDOPRIL, A PROCESS FOR ITS PREPARATION, AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT
    Publication number: 20130178464
    Abstract: Delta crystalline form of the compound of formula (I): characterised by its X-ray powder diffraction diagram. Medicinal products containing the same which are useful in the treatment of cardiovascular diseases.
    Type: Application
    Filed: January 3, 2013
    Publication date: July 11, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventor: LES LABORATOIRES SERVIER
  • PROCESS FOR THE PREPARATION OF THE L-ARGININE SALT OF PERINDOPRIL
    Publication number: 20130178635
    Abstract: Process for the preparation of the compound of formula (I):
    Type: Application
    Filed: January 3, 2013
    Publication date: July 11, 2013
    Applicant: LES LABORATOIRES SERVIER
    Inventor: Les Laboratoires Servier
  • POLYMORPHS OF SAXAGLIPTIN HYDROCHLORIDE AND PROCESSES FOR PREPARING THEM
    Publication number: 20130158091
    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: February 15, 2013
    Publication date: June 20, 2013
    Inventors: Marina MARINKOVIC, Marina RATKAJ, Oliver FRANKOVIC, Tina MUNDORFER
  • 6-substituted sulfonyl azabicyclo[3.2.1]octanes useful to inhibit 11?-hydroxysteroid dehydrogenase type-I
    Patent number: 8466149
    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: Grant
    Filed: August 12, 2008
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
  • 1-benzyl-3-hydroxymethylindazole derivatives and use thereof in the treatment of diseases based on the expression of MCP-1, CX3CR1 and P40
    Patent number: 8461194
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
    Type: Grant
    Filed: March 5, 2009
    Date of Patent: June 11, 2013
    Assignee: Aziende Chimiche Riunite Angelini Francesco A. C. R. A. F. S. p. A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
  • COMPOUND LIBRARIES MADE THROUGH PHOSPHINE-CATALYZED ANNULATION/TEBBE/DIELS-ALDER REACTIONS
    Publication number: 20130143916
    Abstract: A method for producing libraries of structurally and stereochemically diverse molecules that can be screened for biological or chemical activity. A library of 91 heterocyclic compounds composed of 16 distinct scaffolds was synthesized through a sequence of phosphine-catalyzed ring-forming reactions, Tebbe reactions, Diels-Alder reactions, and, in some cases, hydrolysis to illustrate the methods. Three compounds inhibiting migration of human breast cancer cells are identified from the library.
    Type: Application
    Filed: November 9, 2012
    Publication date: June 6, 2013
    Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: THE REGENTS OF THE UNIVERSITY OF CALIF, Gabriel Fenteany
  • NOVEL COMPOUNDS AS DPP-IV INHIBITORS AND PROCESS FOR PREPARATION THEREOF
    Publication number: 20130137852
    Abstract: The present invention relates to process for preparation of novel compounds which are acting as inhibitors of dipeptidyl peptidase-IV enzyme and is depicted by the structural formula as given below: Formula VI. Which are useful in the treatment or prevention of diseases in which the dipeptidylpeptidase-IV enzyme is involved, such as diabetes and particularly type-2 diabetes.
    Type: Application
    Filed: August 3, 2011
    Publication date: May 30, 2013
    Applicant: Cadila Corporate Campus
    Inventors: Bakulesh Mafatlal Khamar, Nirav Kishorbhai Joshi, Chandan Hardhan Singh, Uday Rajaram Bapat, Bipin Dhanjibhai Gadhiya, Nirav Sureshbhai Sagar, Indravadan Ambalal Modi
  • Dendrimer conjugates
    Patent number: 8445528
    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: July 12, 2012
    Date of Patent: May 21, 2013
    Assignee: The Regents of the University of Michigan
    Inventors: James R. Baker, Jr., Xue-min Cheng, Thommey P. Thomas, Baohua Mark Huang
  • Beta-amino acid derivatives for treatment of diabetes
    Patent number: 8431602
    Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.
    Type: Grant
    Filed: December 23, 2008
    Date of Patent: April 30, 2013
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
  • Sterically bulky stabilizers
    Patent number: 8426636
    Abstract: A sterically bulky stabilizer that is associated non-covalently with a benzimidazolone pigment. The sterically bulky stabilizer compound includes an aromatic acid derivative, and the presence of the sterically bulky stabilizer limits an extent of particle growth and aggregation, to afford nanoscale pigment particles.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: April 23, 2013
    Assignees: Xerox Corporation, National Research Council of Canada
    Inventors: Rina Carlini, Darren Andrew Makeiff
  • Macrocyclic factor VIIa inhibitors useful as anticoagulants
    Patent number: 8420830
    Abstract: The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: April 16, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Nicholas Ronald Wurtz, Eldon Scott Priestley, Daniel L. Cheney, Peter W. Glunz, Xiaojun Zhang, Brandon Parkhurst, Vladimir Ladziata, Luciano Mueller
  • Polymorphs of Saxagliptin hydrochloride and processes for preparing them
    Patent number: 8410288
    Abstract: The invention provides polymorphs of Saxagliptin hydrochloride, processes for preparing polymorphs of Saxagliptin hydrochloride, and pharmaceutical compositions of polymorphs of Saxagliptin hydrochloride.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: April 2, 2013
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: Marina Marinković, Marina Ratkaj, Oliver Franković, Tina Mundorfer
  • Pyrrolopyrrole derivatives, their manufacture and use
    Patent number: 8404864
    Abstract: The present invention relates to compounds of the formula (I) wherein the substituents are as defined in claim 1, and their use as organic semiconductor in organic devices, like diodes, organic field effect transistors and/or a solar cells. The compounds of the formula I have excellent solubility in organic solvents. High efficiency of energy conversion, excellent field-effect mobility, good on/off current ratios and/or excellent stability can be observed, when said compounds are used in semiconductor devices or organic photovoltaic (PV) devices (solar cells).
    Type: Grant
    Filed: September 22, 2008
    Date of Patent: March 26, 2013
    Assignee: BASF SE
    Inventors: Zhimin Hao, Beat Schmidhalter, Jean-Luc Budry, Margherita Fontana, Mathieu Turbiez, Frank Bienewald, Mathias Düggeli, Oliver Frédéric Aebischer, Pascal Hayoz, Marta Fonrodona Turon
  • Heterocyclic amide derivatives as EP4 receptor antagonists
    Patent number: 8404736
    Abstract: The invention relates to compounds of Formula (I) (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including antagonism of Prostaglandin EP4 receptor as a therapeutic treatment.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: March 26, 2013
    Assignee: Beta Pharma Canada Inc.
    Inventor: Wei Yuan
  • Tetrahydroindoles having sphingosine-1-phosphate receptor activity
    Patent number: 8404863
    Abstract: Compounds are disclosed herein having the formula (I). Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: March 26, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard L. Beard
  • Substituted 7-azabicyclo[2.2.1]heptyl derivatives useful for making pharmaceutical compositions
    Patent number: 8389561
    Abstract: This invention provides 1-substituted-7-azabicyclo[2.2.1]heptyl derivatives, intermediates and methods for producing them, which are therapeutic agents useful for the prevention and treatment of central nervous system disorders and diseases mediated by a Nicotinic Acetylcholine Receptor such as Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy, pain, nicotine addiction and dementia.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: March 5, 2013
    Assignee: Universiteit Gent
    Inventors: Christian Stevens, Ann De Blieck, Thomas Heugebaert
  • Ink composition for jet printer
    Patent number: 8383743
    Abstract: Disclosed is an ink composition for jet printer, comprising a pigment, a film forming resin and an organic solvent, the film forming resin being an acrylic copolymer containing, as a monomer unit, at least one of compounds represented by the general formulas (1) and (2): wherein R1 represents a hydrogen atom or a methyl group; R2 represents an alkylene group having 2 to 12 carbon atoms which may be linear or branched; and R3 and R4 each independently represents a hydrogen atom, an alkyl group, an alkenyl group or an aryl group, and the sum of the number of carbon atoms of R3 and R4 is from 4 to 12, or R3 and R4 form a saturated or unsaturated hydrocarbon group which is a five-membered ring formed by combination of the R3 and R4; and wherein R1 represents a hydrogen atom or a methyl group; R2 represents an alkylene group having 2 to 12 carbon atoms which may be linear or branched; and X represents a group selected from the group consisting of groups represented by the general formulas (3) to (9).
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: February 26, 2013
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Akio Kumagai, Hiromichi Arakawa, Shigehiro Tanaka, Kazuhiro Kaneko, Yoshinosuke Shimamura
  • Angiotensin II receptor antagonists
    Patent number: 8367711
    Abstract: A compound having the structure 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 30, 2012
    Date of Patent: February 5, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Iyassu K. Sebhat, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • PROCESS FOR PREPARING SAXAGLIPTIN AND ITS NOVEL INTERMEDIATES USEFUL IN THE SYNTHESIS THEREOF
    Publication number: 20130023671
    Abstract: Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof.
    Type: Application
    Filed: May 24, 2012
    Publication date: January 24, 2013
    Applicant: APICORE, LLC
    Inventors: Ravishanker Kovi, KeshavRao Rapole, Ashish Naik, Jayaraman Kannapan, Murali Krishna Madala, Sanjay F. Thakor
  • METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF
    Publication number: 20130012723
    Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
    Type: Application
    Filed: August 31, 2012
    Publication date: January 10, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Truc Chi Vu, David B. Brzozowski, Rita Fox, Jollie Duaine Godfrey, JR., Ronald L. Hanson, Sergei V. Kolotuchin, John A. Mazzullo, Ramesh N. Patel, Jianji Wang, Kwok Wong, Jurong Yu, Jason J. Zhu, David R. Magnin, David J. Augeri, Lawrence G. Hamann
  • Nitrogenated 5-membered heterocyclic compound
    Patent number: 8349886
    Abstract: The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: April 15, 2009
    Date of Patent: January 8, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Indole and indazole derivatives having a cell-, tissue- and organ-preserving effect
    Patent number: 8349885
    Abstract: The present invention relates to a composition for preserving cells, tissues and organs, comprising as an active ingredient indole and indazole compounds of formula (1), or a pharmaceutically acceptable salt or isomer thereof, which are effective for preventing injury of organs, isolated cell systems or tissues caused by cold storage, transplant operation or post-transplantation reperfusion; a preservation method; and a preparation method of the composition.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: January 8, 2013
    Assignee: LG Life Sciences Ltd.
    Inventors: Soon Ha Kim, Hyoung Jin Kim, Chul Woong Chung, Heui Sul Park, Hyo Shin Kwak, Sung Ho Kim, Jin Gu Park
  • Indole derivatives as inhibitors of histone deacetylase
    Patent number: 8338416
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Grant
    Filed: March 16, 2007
    Date of Patent: December 25, 2012
    Assignee: Pharmacylics, Inc.
    Inventors: Joseph J. Buggy, Sriram Balasubramanian, Erik Verner, Vincent W. F. Tai, Chang-Sun Lee
  • N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
    Patent number: 8329718
    Abstract: The present invention provides novel ureas containing N-aryl or N-heteroaryl substituted heterocycles of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, D and W are as defined herein. These compounds are selective inhibitors of the human P2Y1 receptor which can be used as medicaments.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: December 11, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
  • FF-ATPase inhibitors and related methods
    Patent number: 8324258
    Abstract: The present invention relates to a family of guanidine-based F1F0-ATPase inhibitors, e.g., mitochondrial F1F0-ATPase inhibitors, methods for their discovery, and their use as therapeutic agents for treating certain disorders.
    Type: Grant
    Filed: September 11, 2008
    Date of Patent: December 4, 2012
    Assignee: The Regents of the University of Michigan
    Inventors: Gary D. Glick, Gina Ney
  • Method of differentiating hematopoietic stem cells into natural killer cells using YC-1 or IL-21
    Patent number: 8318491
    Abstract: The present invention relates to an agent for differentiating hematopoietic stem cells into natural killer cells and a method for the differentiation, more precisely an agent for differentiating hematopoietic stem cells into natural killer cells comprising YC-I [3-(5?-hydroxymethyl-2?-furyl)-1-benzylindazole] or IL-21 (Interleukin-21) as an active ingredient and a method for differentiating hematopoietic stem cells into natural killer cells using the same. The YC-I and IL-21 regulate the differentiation of hematopoietic stem cells into natural killer cells and increase the killing activity of NK cells. Therefore, the agent for NK cell differentiation of the present invention can be effectively used for cell therapy for the treatment of cancer by regulating the differentiation of hematopoietic stem cells into natural killer cells having tumor cell killing activity.
    Type: Grant
    Filed: October 2, 2007
    Date of Patent: November 27, 2012
    Assignee: Korea Research Institute of Bioscience and Biotechnology
    Inventors: Inpyo Choi, SukRan Yoon, Sohyun Yun, Jin Woong Chung
  • 4-hydroxythiobenzamide derivatives of drugs
    Patent number: 8314140
    Abstract: Derivatives of drugs are provided, said derivatives comprising the H2S-releasing moiety 4-hydroxythiobenzamide that is either covalently linked to the drug or forms a salt with the drug. The compounds of the present invention exhibit enhanced activity or reduced side effects or both.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: November 20, 2012
    Assignee: Antibe Therapeutics Inc.
    Inventors: John Wallace, Giuseppe Cirino, Vincenzo Santagada, Giuseppe Caliendo
  • Kallikrein 7 modulators
    Patent number: 8309596
    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: Grant
    Filed: June 26, 2008
    Date of Patent: November 13, 2012
    Assignee: Novartis AG
    Inventors: Stefanie Flohr, Stefan Andreas Randl, Nils Ostermann, Ulrich Hassiepen, Frederic Berst, Ursula Bodendorf, Bernd Gerhartz, Andreas Marzinzik, Claus Ehrhardt, Josef Gottfried Meingassner
  • CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME
    Publication number: 20120283181
    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: Application
    Filed: July 11, 2012
    Publication date: November 8, 2012
    Applicant: 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
  • AZABICYCLO[3.1.0]HEX-2-YL COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    Publication number: 20120283245
    Abstract: Compounds of formula: wherein: ALK represents an alkylene chain, W represents a group wherein R and R? are as defined in the description. Medicinal products containing the same which are useful in treating cognitive disorders associated with cerebral aging or with neurodegenerative diseases.
    Type: Application
    Filed: December 8, 2010
    Publication date: November 8, 2012
    Applicant: LES LABORATOIRES SERVIER
    Inventors: Patrick Casara, Anne-Marie Chollet, Alain Dhainaut, Jean-Michel Henlin, Pierre Lestage, Fany Panayi
  • Process For Preparing Dipeptidyl Peptidase IV Inhibitors And Intermediates Therefor
    Publication number: 20120276600
    Abstract: A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure prepared by subjecting an acid of the structure to reduce amination by treating the acid with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase/formate dehydrogenase enzyme concentrate (PDH/FDH) and without isolating treating the resulting amine of the structure 2 with di-tert-butyl dicarbonate to form the BOC-protected amine
    Type: Application
    Filed: June 14, 2012
    Publication date: November 1, 2012
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Michael Politino, Matthew M. Cadin, Paul M. Skonezny, Jason G. Chen
  • Bicyclic tetrahydropyrrole compounds
    Patent number: 8299113
    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: October 30, 2012
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Miguel Angel Pericas-Brondo, Antonio Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobes, Carmen Garcia Granda
  • 2-aza-bicyclo[3.1.0]hexane derivatives as orexin receptor antagonists
    Patent number: 8288435
    Abstract: The invention relates to novel 2-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: December 28, 2007
    Date of Patent: October 16, 2012
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Hamed Aissaoui, Christoph Boss, Markus Gude, Ralf Koberstein, Thierry Sifferlen, Daniel Trachsel
  • Process for the synthesis of (2S,3AR,7AS)-octahydro-1H-indole carboxylic acid as an intermediate for trandolapril
    Patent number: 8288565
    Abstract: A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.
    Type: Grant
    Filed: July 16, 2010
    Date of Patent: October 16, 2012
    Assignee: Abbott Laboratories
    Inventors: Sanjay R. Chemburkar, Rajarathnam E. Reddy, Douglas M. Reamer, John T. Pavlina, Stephen S. Ulrey, Brian J. Kotecki
  • Process for Preparing Azabicyclic Compounds
    Publication number: 20120259129
    Abstract: The present invention relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof.
    Type: Application
    Filed: March 9, 2012
    Publication date: October 11, 2012
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Narendra Bhalchandra Ambhaikar, Brian Richard Bear, Lev T. D. Fanning, Robert Hughes, Benjamin Littler
  • AGENT THAT MODULATES PHYSIOLOGICAL CONDITION OF PESTS, INVOLVED IN INSECT PEPTIDYL-DIPEPTIDASE A ACTIVITY
    Publication number: 20120258929
    Abstract: The present invention provides an agent that modulates physiological condition of pests, wherein the agent has an ability to modulate the activity of an insect peptidyl-dipeptidase A; a method for assaying pesticidal activity of a test substance, which comprises a step of measuring the activity of a peptidyl-dipeptidase A in a reaction system in which the peptidyl-dipeptidase A contacts with a test substance, and the like.
    Type: Application
    Filed: June 23, 2006
    Publication date: October 11, 2012
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Yasutaka Shimokawatoko, Marc Van De Craen, Irene Nooren, Sandra Turconi, Yann Naudet, Guy Nys, Jurgen Debaveye
  • PHARMACEUTICAL CO-CRYSTALS OF QUERCETIN
    Publication number: 20120258170
    Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.
    Type: Application
    Filed: March 19, 2012
    Publication date: October 11, 2012
    Applicant: Nutracryst Therapeutics Private Limited
    Inventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
  • Methods and compounds for producing dipeptidyl peptidase IV inhibitors and intermediates thereof
    Patent number: 8278462
    Abstract: Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: October 2, 2012
    Assignee: Bristol-Myers Squibb Company
    Inventors: Truc Chi Vu, David B. Brzozowski, Rita Fox, Jollie Duaine Godfrey, Jr., Ronald L. Hanson, Sergei V. Kolotuchin, John A. Mazzullo, Ramesh N. Patel, Jianji Wang, Kwok Wong, Jurong Yu, Jason J. Zhu, David R. Magnin, David J. Augeri, Lawrence G. Hamann
  • Red colour filter composition
    Patent number: 8273269
    Abstract: A composition, for producing dispersions, thermoplastic masses and/or color filters, comprising (a) a colorant of formula (1) wherein 20-100 mol % R1 are Br and 80-100 mol % R3 are H, especially of formula (Ib) and/or (Ic); (b) from 0 to 150% by weight, based on (a), of C. I. Pigment Red 144, 188, 190, 224, 242 or 2,4,6-trimethylphenylperylene diimide; (c) from 3 to 25% by weight, based on (a), of a di- or tri-azacyclopentylmethyl-substituted colorant (formulae given); (d) from 0 to 10% by weight, preferably from 0.01 to 8% by weight, based on the sum of (a) and (b), of an additionally sulfonated colorant of the same kernels as in (c); and (e) from 0 to 30% by weight, preferably from 3 to 25% by weight, especially from 5 to 20% by weight, based on (a), of a diketopyrrolopyrrole colorant substituted by at least one chain containing a plurality of nitrogen atoms (cf. formula (V)).
    Type: Grant
    Filed: May 5, 2009
    Date of Patent: September 25, 2012
    Assignee: BASF SE
    Inventors: Roman Lenz, Gerardus De Keyzer, Mathias Duggeli, Patrick Christopher Holzhuter
  • Substituted sulfonamide compounds
    Patent number: 8268814
    Abstract: Substituted sulfonamide compounds corresponding to formula I processes for the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds for treating and/or inhibiting pain or other conditions at least partly mediated by the bradykinin 1 receptor.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: September 18, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Melanie Reich, Ellen Klegraf, Stefan Oberboersch, Stefan Schunk, Ruth Jostock, Sabine Hees, Tieno Germann, Michael Engels
  • Dual alanyl aminopeptidase and dipeptidyl peptidase iv inhibitors for functionally influencing different cells and for treating immunological inflammatory, neuronal and other diseases
    Patent number: 8263636
    Abstract: The present invention relates to substances capable of specifically inhibiting Ala-p-nitroanilide-cleaving peptidases and Gly-Pro-p-nitroanilide-cleaving peptidases as well, for a use in the medical field. Furthermore, the invention relates to the use of at least one of such substances or of at least one pharmaceutical or cosmetic composition containing at least one such substance for a prophylaxis or a therapy of diseases, particularly for a prophylaxis and a therapy of diseases accompanied by an excessive immune response (autoimmune diseases, allergies, transplant rejections), of other chronic-inflammatory diseases, of neuronal diseases and cerebral damage, of skin diseases (inter alia acne, psoriasis), of tumor diseases and of specific virus infections (inter alia SARS).
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: September 11, 2012
    Assignees: IMTM GmbH, Keyneurotek Pharmaceuticals AG
    Inventors: Siegfried Ansorge, Ute Bank, Karsten Nordhoff, Michael Taeger, Frank Striggow
  • Cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV and method
    Patent number: RE44186
    Abstract: Dipeptidyl peptidase IV (DP 4) inhibiting compounds are provided having the formula where x is 0 or 1 and y is 0 or 1 (provided that x=1 when y=0 and x=0 when y=1); n is 0 or 1; X is H or CN; and wherein R1, R2, R3 and R4 are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, and other diseases as set out herein, employing such DP 4 inhibitor *or a combination of such DP 4 inhibitor and one or more of another antidiabetic agent such as metformin, glyburide, troglitazone, pioglitazone, rosiglitazone and/or insulin and/or one or more of a hypolipidemic agent and/or anti-obesity agent and/or other therapeutic agent.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: April 30, 2013
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jeffrey A. Robl, Richard B. Sulsky, David J. Augeri, David R. Magnin, Lawrence G. Hamann, David A. Betebenner