The Additional Hetero Ring Also Contains Nitrogen Patents (Class 548/518)
Ring carbon of each of the two nitrogen containing hetero rings is bonded directly to chalcogen (e.g., both rings may be bonded to the same oxygen atom or to different oxygen atoms, etc.) (Class 548/519)
Ring nitrogens of the two nitrogen containing hetero rings are bonded directly to the same atom or chain, which chain may include a ring (Class 548/523)
  • INSECTICIDAL ARYLPYRROLINES
    Publication number: 20110003690
    Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.
    Type: Application
    Filed: January 29, 2009
    Publication date: January 6, 2011
    Applicant: BAY CROPSCIENCE AG
    Inventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
  • Non-covalent complexes comprising carbon nanotubes
    Patent number: 7858648
    Abstract: The present invention relates to the use of a carbon nanotube comprising positive and/or negative charges, the charges being carried by at least one charge-carrying group, the charge carrying group being covalently bound to the surface of the carbon nanotube, for the manufacture of a complex between the carbon nanotube and at least one charged molecule, the bond between the carbon nanotube and the charged molecule being essentially electrostatic, and the charged molecule comprising at least one negative charge if the carbon nanotube comprises positive charges and/or at least one positive charge if the carbon nanotube comprises negative charges.
    Type: Grant
    Filed: June 6, 2005
    Date of Patent: December 28, 2010
    Assignees: Centre National de la Recherche Scientifique (C.N.R.S.), University of London, The School of Pharmacy, Universita degli Studi di Trieste
    Inventors: Alberto Bianco, Davide Pantarotto, Kostas Kostarelos, Maurizio Prato
  • Anti-Viral Compounds
    Publication number: 20100317568
    Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.
    Type: Application
    Filed: June 10, 2010
    Publication date: December 16, 2010
    Applicant: ABBOTT LABAORATORIES
    Inventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Todd N. Soltwedel, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Michael J. Lavin, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi
  • Beverage Preservative System Containing Pimaricin-Povidone Complex
    Publication number: 20100310722
    Abstract: The present invention provides a beverage preservative system comprising a Pimaricin-providone complex for use in beverages products. The present invention is further directed to beverage products comprising the beverage preservative systems. The beverage preservative system prevents spoilage by microorganisms in a beverage within a sealed container for a period of at least 16 weeks.
    Type: Application
    Filed: June 2, 2010
    Publication date: December 9, 2010
    Applicant: PepsiCo, Inc.
    Inventor: Richard T. Smith
  • Histamine H3 receptor inhibitors, preparation and therapeutic uses
    Patent number: 7846950
    Abstract: The present invention provides novel compounds with histamine-H3 receptor antagonist or inverse agonist activity. In particular, the invention provides a compound of Formula I, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the compounds, methods of treatment employing these compounds and compositions, and intermediates and methods for making these compounds. The invention provides methods of using compounds and pharmaceutical compositions to treat obesity, cognitive deficiences, narcolepsy, and other histamine H3 receptor-related diseases.
    Type: Grant
    Filed: October 11, 2005
    Date of Patent: December 7, 2010
    Assignee: Eli Lilly and Company
    Inventors: Cynthia Darshini Jesudason, Freddie Craig Stevens
  • N-benzoyl- and N-benzylpyrrolidin-3-ylamines as histamine-3 antagonists
    Patent number: 7842715
    Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
    Type: Grant
    Filed: May 18, 2007
    Date of Patent: November 30, 2010
    Assignee: Wyeth LLC
    Inventors: Derek Cecil Cole, Magda Asselin, Joseph Raymond Stock, Jin-In Kim
  • Polymorphic Forms Of A 3-Pyrrole Substituted 2-Indolinone
    Publication number: 20100286410
    Abstract: The invention relates to new crystalline polymorphic forms of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide (i.e., sunitinib base), including Form I, Form II, and Form IV, processes for preparing crystalline polymorphic forms of sunitinib base, and pharmaceutically acceptable salts of new crystalline polymorphic forms of sunitinib base and pharmaceutical compositions comprising new crystalline polymorphic forms of sunitinib base, salts of new crystalline polymorphic forms of sunitinib base and mixtures thereof.
    Type: Application
    Filed: December 12, 2008
    Publication date: November 11, 2010
    Applicant: Medichem, S.A.
    Inventors: Stephen Benedict David Winter, Bernardino Mangion
  • 3,4-SUBSTITUTED PYRROLIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE
    Publication number: 20100280009
    Abstract: The present invention is directed to 3,4-substituted pyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: December 10, 2008
    Publication date: November 4, 2010
    Inventors: Shawn J. Stachel, Thomas Steele, Alessia Petrocchi
  • Inhibitors of phosphodiesterase type-IV
    Patent number: 7825147
    Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.
    Type: Grant
    Filed: August 30, 2004
    Date of Patent: November 2, 2010
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Venkata P. Palle, Sarala Balachandran, Mohammad Salman, Gagan Kukreja, Nidhi Gupta, Abhijit Ray, Sunanda G. Dastidar
  • 2-(4-oxo-4H-quinazolin-3-yl)acetamides and their use as vasopressin V3 antagonists
    Patent number: 7807686
    Abstract: The present invention relates to 2-(4-oxo4H-quinazolin-3-yl) acetamicle derivatives of formula (I), and to their use as vasopressin V3 antagonists, particularly for the treatment of depression.
    Type: Grant
    Filed: March 10, 2006
    Date of Patent: October 5, 2010
    Assignee: N.V. Organon
    Inventors: Jeffrey Letourneau, Christopher Riviello, Koc-Kan Hoc, Jui-Hsiang Chan, Michael Ohlmeyer, Patrick Jokiel, Irina Neagu, John Richard Morphy, Susan Elizabeth Napier
  • Fused bicyclic-substituted amines as histamine-3 receptor ligands
    Patent number: 7807697
    Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands and methods for using such compounds and compositions.
    Type: Grant
    Filed: January 29, 2008
    Date of Patent: October 5, 2010
    Assignee: Abbott Laboratories
    Inventors: Marlon D. Cowart, Yi-Yin Ku, Sou-Jen Chang, Dilinie P. Fernando, Timothy A. Grieme, Robert J. Altenbach
  • Substituted prolinamides, manufacturing, and the use thereof as medicaments
    Patent number: 7807693
    Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, L, E, G, J, M, R3, R4, R5 and R13 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures, and the salts thereof.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: October 5, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Kai Gerlach, Georg Dahmann, Herbert Nar, Roland Pfau, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
  • Azetidines as MEK Inhibitors for the Treatment of Proliferative Diseases
    Publication number: 20100249096
    Abstract: Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: May 5, 2010
    Publication date: September 30, 2010
    Applicant: EXELIXIS, INC.
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Aminoalkylazole derivatives as histamine-3 antagonists
    Patent number: 7803825
    Abstract: The present invention provides a compound of formula Ia: and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor.
    Type: Grant
    Filed: July 15, 2008
    Date of Patent: September 28, 2010
    Assignee: Wyeth LLC
    Inventors: Jonathan Laird Gross, Albert Jean Robichaud, Marla Jean Williams, Alessandro Mazzacani
  • 2-Heterocycle-substituted indole derivatives for treating diabetes and associated conditions
    Patent number: 7799820
    Abstract: Disclosed is a compound represented by the formula (I) below, which has a glucokinase-activating effect and is thus useful for treatment of diabetes or obesity, or a pharmaceutically acceptable salt thereof. In the formula, R1 represents an aryl or the like; R11 represents an aryl or the like; R2 represents a formyl or the like, R3 represents a C1-6 alkyl or the like; R3 represents a hydrogen atom or the like; Z1 represents —O— or the like; Z2 represents —O— or the like; Y1-Y4 respectively represent a carbon atom or a nitrogen atom; ring A represents a heteroaryl group; X represents a carbon atom or the like; m represents an integer of 0-2; and q represents an integer of 0-2.
    Type: Grant
    Filed: September 29, 2006
    Date of Patent: September 21, 2010
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Keiji Takahashi, Yoshio Ogino, Teruyuki Nishimura
  • PYRROLIDINE COMPOUNDS
    Publication number: 20100234431
    Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, X, Y, and Z are as defined herein. Also disclosed is a method for inhibiting actively of fibroblast activation protein or for treating cancer or inflammation conditions with such a compound.
    Type: Application
    Filed: February 19, 2010
    Publication date: September 16, 2010
    Applicant: National Health Research Institutes
    Inventors: Weir-Tong Jiaang, Xin Chen
  • IAP BIR domain binding compounds
    Patent number: 7795298
    Abstract: Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I: or a salt thereof, in which R1, R2, R100, R200, A, A1, B, B1, BG, n, Q and Q1 are substituents described. Also disclosed is the use of compounds of Formula 1 to treat proliferative disorders.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: September 14, 2010
    Assignee: Aegera Therapeutics, Inc.
    Inventors: Alain Laurent, Kim Hewitt, Stephen Morris, Patrick Bureau, Alain Boudreault, Scott Jarvis, James Jaquith
  • Crystal form of 2-methyl-3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone
    Patent number: 7790731
    Abstract: The present invention is directed to a form I crystal of 2-methyl 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone that is useful for example in the treatment of sleep disorders or various sleep disorder-associated diseases.
    Type: Grant
    Filed: February 13, 2006
    Date of Patent: September 7, 2010
    Assignee: Banyu Pharmaceutical Co. Ltd.
    Inventors: Akio Kanatani, Nagaaki Sato, Tsuyoshi Nagase, Shigeru Tokita
  • Pyrroloquinoxalinone inhibitors of poly(ADP-ribose)polymerase
    Patent number: 7790721
    Abstract: Compounds of formula I where X is a bond; A1 and A2, together with the atoms to which they are attached, is pyrrole; and A3 and A4, together with the atoms to which they are attached, are benzene; are poly(ADP-ribose)polymerase inhibitors. The compounds of formula I are useful for the treatment of diseases such as cancer.
    Type: Grant
    Filed: December 27, 2007
    Date of Patent: September 7, 2010
    Assignee: Abbott Laboratories
    Inventors: Vincent L. Giranda, Julie M Miyashiro, Thomas D Penning, Keith W. Woods
  • IAP BIR DOMAIN BINDING COMPOUNDS
    Publication number: 20100221261
    Abstract: Disclosed is an isomer, enantiomer, diastereoisomer or tautomer of a compound represented by Formula I or II or a salt thereof, in which R1, R2, R3, R100, R200, R300, A, A1, BG, Q and Q1 are substituents described herein. Also disclosed is the use of compounds of Formula I and II to treat proliferative disorders such as cancer.
    Type: Application
    Filed: November 17, 2009
    Publication date: September 2, 2010
    Applicant: Aegera Therapeutics, Inc.
    Inventors: Alain Boudreault, James Jaquith, Patrick Bureau, John W. Gillard, Alain Laurent
  • NOVEL ISOPHTHALATES AS BETA-SECRETASE INHIBITORS
    Publication number: 20100222581
    Abstract: There is provided a series of substituted isophthalates of formula (I) or a stereoisomer thereof; or a pharmaceutically acceptable salt thereof, wherein W, R3, R5 and R6 as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
    Type: Application
    Filed: May 14, 2010
    Publication date: September 2, 2010
    Inventors: Lorin A. Thompson, III, Kenneth M. Boy, Jianliang Shi, John E. Macor
  • 2-Oxo-1-pyrrolidine derivatives, processes for preparing them and their uses
    Publication number: 20100222576
    Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula I, wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.
    Type: Application
    Filed: February 17, 2010
    Publication date: September 2, 2010
    Inventors: Edmond Differding, Benoît Kenda, Bénédicte Lallemand, Alain Matagne, Philippe Michel, Patrick Pasau, Patrice Talaga
  • Cyanoguanidine-based azole compounds useful as malonyl-CoA decarboxylase inhibitors
    Patent number: 7786145
    Abstract: The present invention provides methods for the use of compounds as depicted by structure I, pharmaceutical compositions containing the same, and methods for the prophylaxis, management and treatment of metabolic diseases and diseases modulated by MCD inhibition. The compounds disclosed in this invention are useful for the prophylaxis, management and treatment of diseases involving in malonyl-CoA regulated glucose/fatty acid metabolism pathway. In particular, these compounds and pharmaceutical composition containing the same are indicated in the prophylaxis, management and treatment of cardiovascular diseases, diabetes, cancer and obesity.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: August 31, 2010
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Jie Fei Cheng, Bin Liu, Thomas Arrhenius, Mark E. Wilson, Alex M. Nadzan, Gary D. Lopaschuk, Jason R. Dyck, Rossy Serafimov
  • Pesticidal arylpyrrolidines
    Publication number: 20100216792
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: October 14, 2009
    Publication date: August 26, 2010
    Applicant: Bayer CropScience AG
    Inventors: Ulrich Görgens, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
  • REFINED ROUTES TO CHLORIN BUILDING BLOCKS
    Publication number: 20100204465
    Abstract: A method of making chlorins comprises the steps of reacting (e.g. condensing) a dipyrrin western half intermediate with an eastern half intermediate to form a tetrahydrobilene, and then cyclizing the tetrahydrobilene to form a chlorin. Intermediates including tetrahydrobilenes useful in such reactions are also described.
    Type: Application
    Filed: January 25, 2010
    Publication date: August 12, 2010
    Inventors: Jonathan S. Lindsey, Masahiko Taniguchi, Doyoung Ra, Guoning Mo, Thiagarajan Balasubramanian
  • Aryl Sulfonamides Useful for Modulation of the Progesterone Receptor
    Publication number: 20100204228
    Abstract: In one embodiment, compounds of the following structure are described, wherein R1 to R7 are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.
    Type: Application
    Filed: April 15, 2010
    Publication date: August 12, 2010
    Applicant: Wyeth LLC
    Inventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
  • Salt and polymorphs of a DPPIV inhibitor
    Patent number: 7772264
    Abstract: The invention is concerned with (S)-1-{[2-(5-Methyl-2-phenyl-oxazol-4-yl)-ethylamino]-acetyl}-pyrrolidine-2-carbonitrile mesylate and crystalline polymorphs of this compound. This compound and its polymorphic forms exhibits superior properties compared to the previously known compounds and can be used as medicament for the treatment of disorders which are associated with DPP-IV.
    Type: Grant
    Filed: March 16, 2006
    Date of Patent: August 10, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stefan Abrecht, Andre Gerard Bubendorf, Stephan Goetzoe, Olaf Grassmann, Francois Montavon, Regina Moog, Franziska Rohrer, Armin Ruf, Michelangelo Scalone, Urs Schwitter, Shaoning Wang
  • FUNCTIONALIZED EXPANDED PORPHYRINS
    Publication number: 20100197031
    Abstract: Disclosed are functionalized expanded porphyrins that can be used as spectrometric sensors for high-valent actinide cations. The disclosed functionalized expanded porphyrins have the advantage over unfunctionalized systems in that they can be immobilized via covalent attachment to a solid support comprising an inorganic or organic polymer or other common substrates. Substrates comprising the disclosed functionalized expanded porphyrins are also disclosed. Further, disclosed are methods of making the disclosed compounds (immobilized and free), methods of using them as sensors to detect high valent actinides, devices that comprise the disclosed compounds, and kits.
    Type: Application
    Filed: June 23, 2008
    Publication date: August 5, 2010
    Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Jonathan L. Sessler, Patricia J. Pantos
  • Pharmaceutical Compositions As Inhibitors of Dipeptidyl Peptidase-IV (DPP-IV)
    Publication number: 20100190822
    Abstract: The present invention relates to compounds which inhibit dipeptidyl peptidase IV (DPP-IV) and are useful for the prevention or treatment of diabetes, especially type II diabetes, as well as hyperglycemia, Syndrome X, hyperinsulinemia, obesity, atherosclerosis, and various immunomodulatory diseases.
    Type: Application
    Filed: March 19, 2010
    Publication date: July 29, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: David J. Madar, Stevan W. Djuric, Melissa J. Michmerhuizen, Hana A. Kopecka, Xiaofeng Li, Kenton L. Longenecker, Zhonghua Pei, Daisy Pireh, Hing L. Sham, Kent D. Stewart, Bruce G. Szczepankiewicz, Paul E. Wiedeman, Hong Yong
  • Tetrahydropteridines useful as inhibitors of protein kinases
    Patent number: 7763629
    Abstract: The present invention relates to compounds useful as inhibitors of protein kinase, represented by Structural Formula (I): wherein the variables in Structural Formula (I) are as described herein. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: July 27, 2010
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, David Kay, Ronald Knegtel
  • SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF
    Publication number: 20100173897
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
  • SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF
    Publication number: 20100173949
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
  • SUBSTITUTED N-PHENYL-BIPYRROLIDINE UREAS AND THERAPEUTIC USE THEREOF
    Publication number: 20100173908
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine ureas of formula (I). Wherein R, R1, R2, R3, R4 and R5 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted N-phenyl-bipyrrolidine ureas and intermediates therefor.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
  • SUBSTITUTED N-PHENYL-PYRROLIDINYLMETHYLPYRROLIDINE AMIDES AND THERAPEUTIC USE THEREOF
    Publication number: 20100173898
    Abstract: The present invention discloses and claims a series of substituted N-phenyl-pyrrolidinylmethylpyrrolidine amides of formula (I). Wherein R, R1, R2, R3 and R4 are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this invention also discloses methods of preparation of substituted pyrrolidinylmethylpyrrolidine amides and intermediates therefor.
    Type: Application
    Filed: March 15, 2010
    Publication date: July 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Werngard CZECHTIZKY, Zhongli GAO, William J. HURST, Lothar SCHWINK, Siegfried STENGELIN
  • Taxol Derivatives With Antitumor Activity
    Publication number: 20100168420
    Abstract: Taxol derivatives or their salts having the formula as following: Wherein, R1, R2, Z1, Z2, Z3 and Z4 are defined as the description. Their preparation methods and their use as antitumor agent are also disclosed.
    Type: Application
    Filed: January 5, 2007
    Publication date: July 1, 2010
    Inventor: Piaoyang Sun
  • METHOD FOR PRODUCING OPTICALLY ACTIVE AMINES
    Publication number: 20100160636
    Abstract: The present invention provides a method for producing chiral amines, comprising asymmetric transfer hydrogenation of imine compounds in the presence of a hydrogen donor compound and an iridium(III) complex having a chiral prolinamide compound as a ligand. The present invention is useful for production of chiral amines in an efficient manner in terms of their optical and chemical yields.
    Type: Application
    Filed: June 30, 2008
    Publication date: June 24, 2010
    Inventor: Sadayuki Maeda
  • HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
    Publication number: 20100160406
    Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods and intermediates for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
    Type: Application
    Filed: March 28, 2006
    Publication date: June 24, 2010
    Inventors: Philip Arthur Hipskind, Takako Takakuwa, Cynthia Darshini Jesudason, Robert Alan Gadski, William Joseph Hornback, Richard Todd Pickard, Lisa Selsman Beavers
  • Bicyclic pyrazolo-heterocycles
    Patent number: 7741350
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Grant
    Filed: October 20, 2009
    Date of Patent: June 22, 2010
    Assignee: Cara Therapeutics, Inc.
    Inventor: Robert Zhiyong Luo
  • Pharmacological uses of azetidine derivatives
    Patent number: 7741316
    Abstract: A method of treating or preventing Alzheimer's disease, Parkinson's Disease and/or schizophrenia, this method comprising administering to a patient in need of such treatment a compound of formula: in which R, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: November 12, 2004
    Date of Patent: June 22, 2010
    Assignee: Aventis Pharma S.A.
    Inventors: Daniel Achard, Herve Bouchard, Jean Bouquerel, Bruno Filoche, Serge Grisoni, Augustin Hittinger, Michael R. Myers
  • Substituted Pyrrolidine-2-Carboxamides
    Publication number: 20100152190
    Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, R5, R6 and R7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: February 9, 2010
    Publication date: June 17, 2010
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Jing Zhang, Zhuming Zhang
  • Substituted thiophene carboxamides, process for their preparation and their use as medicaments
    Patent number: 7732466
    Abstract: The present invention relates to new substituted thiophene-2-carboxylic acid amides of general formula wherein A, and R1 to R8c are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: May 10, 2005
    Date of Patent: June 8, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Roland Pfau, Henning Priepke, Kai Gerlach, Wolfgang Wienen, Annette Schuler-Metz, Herbert Nar, Sandra Handschuh, Georg Dahmann
  • Aryl sulfonamides useful for modulation of the progesterone receptor
    Patent number: 7723332
    Abstract: In one embodiment, compounds of the following structure are described, wherein R1to R7are described herein. Also provided are methods for preparing these compounds and methods of contraception; treating or preventing fibroids; treating or preventing uterine leiomyomata; treating or preventing endometriosis, dysfunctional bleeding, and polycystic ovary syndrome; treating or preventing hormone-dependent carcinomas; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; and treating cycle-related symptoms using the compounds described herein.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: May 25, 2010
    Assignee: Wyeth LLC
    Inventors: Casey Cameron McComas, Andrew Fensome, Michael Anthony Marella
  • Synthesis of porphyrins designed for attachment to electroactive surfaces via one or more carbon tethers
    Patent number: 7718794
    Abstract: Porphyrin compounds having a surface attachment group coupled thereto at the 5 position are described. The surface attachment group has the formula: wherein R is —CHCH2 or —CCH and Ar is an aromatic group. Methods and intermediates useful for making such compounds are also described.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: May 18, 2010
    Assignees: North Carolina State University, ZettaCore, Inc.
    Inventors: Jonathan S. Lindsey, Robert S. Loewe
  • Pyrrolidin-3-yl compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7714021
    Abstract: The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: June 10, 2005
    Date of Patent: May 11, 2010
    Assignee: Merck & Co., Inc.
    Inventor: Craig A. Coburn
  • Amino acid and peptide conjugates of arylalkylic acids for cosmetic use
    Publication number: 20100099727
    Abstract: The invention provides novel compounds of general formula I wherein R1, R2 and R3 are independently hydrogen, OR4, C1-C6 alkyl or C2-C6 alkenyl, R4 is hydrogen, C1-C6 alkyl or C2-C6 alkenyl, —N-(AA) represents the residue of an amino acid or of a peptide which is bonded over the N-terminus of the amino acid or the peptide and the peptide is composed of 2 to 6, that means 2, 3, 4, 5 or 6, amino acids, wherein the C-terminus of the amino acid or the peptide is optionally esterified with a C1-C16 hydrocarbon moiety and n is an integer of 1 to 5. The compounds are in particular useful for cosmetic applications.
    Type: Application
    Filed: November 27, 2009
    Publication date: April 22, 2010
    Applicant: DSM IP ASSETS B.V.
    Inventors: Jochen Klock, Philippe Emmandel Maillan, Juergen H. Vollhardt, Raphael Beumer
  • Histamine H3 receptor agents, preparation and therapeutic uses
    Patent number: 7696234
    Abstract: The present invention discloses novel compounds of Formula I or pharmaceutically acceptable salts thereof which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using these compositions to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: April 13, 2010
    Assignee: Eli Lilly and Company
    Inventors: Lisa Selsam Beavers, Robert Alan Gadski, Cynthia Darshini Jesudason, Richard Todd Pickard, Freddie Craig Stevens
  • METHODS AND INTERMEDIATES FOR SYNTHESIS OF SELECTIVE DPP-IV INHIBITORS
    Publication number: 20100087658
    Abstract: Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.
    Type: Application
    Filed: March 5, 2008
    Publication date: April 8, 2010
    Applicant: Phenomix Corporation
    Inventors: David Alan Campbell, Emília P.T. Leitão, Zhen-Ping Wu, Peng Wang
  • Antibacterial agents
    Patent number: 7691850
    Abstract: Compounds of formula (I) and derivatives thereof: compositions containing them, their preparation and their use as antibacterials.
    Type: Grant
    Filed: June 15, 2005
    Date of Patent: April 6, 2010
    Assignee: Glaxo Group Limited
    Inventors: William Henry Miller, Israil Pendrak, Mark Andrew Seefeld
  • FAP inhibitors
    Publication number: 20100081701
    Abstract: The present invention concerns compounds, according to general formula (I), which find utility preferably for the treatment of cancer.
    Type: Application
    Filed: August 31, 2006
    Publication date: April 1, 2010
    Inventor: David Michael EVANS
  • FLUORESCENT ISOTOPE TAGS AND THEIR METHOD OF USE
    Publication number: 20100081203
    Abstract: The present invention provides novel reactive fluorescent compounds that incorporate stable isotopic (deuterium, 13-carbon, 15-nitrogen, 18-oxygen) substitutions. The invention includes the use of these compounds, in combination with non-isotopically substituted analogs, for the purification, identification and relative quantification of proteins, peptides, saccharides, metabolites, and other biologically important compounds by combining liquid chromatography (LC) and mass spectrometry (MS). Fluorescent labeling of target compounds in this manner provides orders-of-magnitude sensitivity enhancement over traditional stable isotope labels, and also affords the possibility of simultaneous multiplexed analysis due to the multiwavelength nature of different fluorophores.
    Type: Application
    Filed: June 19, 2009
    Publication date: April 1, 2010
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Brian Agnew, Kyle Richard Gee