Pyridine Ring Or Partially Hydrogenated Pyridine Ring Patents (Class 546/193)
Carbocyclic ring containing (Class 546/194)
  • Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase
    Publication number: 20100292266
    Abstract: Certain oxazolyl piperidine compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
    Type: Application
    Filed: May 25, 2007
    Publication date: November 18, 2010
    Inventors: Richard Apodaca, James Guy Breitenbucher, Alison L. Chambers, Mark Seierstad, Wei Xiao
  • PESTICIDAL COMPOSITIONS
    Publication number: 20100292253
    Abstract: This document discloses molecules having the following formula (“Formula I”):
    Type: Application
    Filed: May 4, 2010
    Publication date: November 18, 2010
    Applicant: DOW AGROSCIENCES LLC
    Inventors: Tony K. Trullinger, Ricky Hunter, Negar Garizi, Maurice C. H. Yap, Ann M. Buysse, Dan Pernich, Timothy C. Johnson, Kristy Bryan, Carl Deamicis, Yu Zhang, Noormohamed M. Niyaz, CaSandra L. McLeod, Ronald Ross, JR., Yuanming Zhu, Peter L. Johnson, Joseph D. Eckelbarger, Marshall H. Parker
  • HETEROCYCLIC AMIDE COMPOUNDS AS PROTEIN KINASE INHIBITORS
    Publication number: 20100286135
    Abstract: The present invention relates to novel heterocyclic amide compounds of Formula I: as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are compositions comprising said compounds, and methods for using said compounds for treating or preventing a proliferative disease, an anti-proliferative disorder, inflammation, arthritis, a neurological or neurodegenerative disease, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease or a fungal disease.
    Type: Application
    Filed: July 17, 2008
    Publication date: November 11, 2010
    Applicant: Schering Corporation Patent Department, K-6-1; 1990
    Inventors: Panduranga Adulla P. Reddy, Lianyun Zhao, Praveen k. Tadikonda, Tzu Tshin Wong, Shuyi Tang, Luis E. Torres, David F. Cauble, JR., Timothy J. Guzi, M. Arshad Siddiqui
  • PYRIDINE COMPOUND, PESTICIDAL COMPOSITION AND METHOD OF CONTROLLING PEST
    Publication number: 20100286148
    Abstract: A pyridine compound represented by the following general formula (1); the pyridine compound in which R1 is a C1-C3 fluoroalkyl group or a C1-C3 fluoroalkoxy group; the pyridine compound in which R2 is a hydrogen atom; the pyridine compound in which R2 is a group represented by Q; a pesticidal composition containing the pyridine compound as an active ingredient; and a method of controlling a pest including applying an effective amount of the pyridine compound to the pest or a place where the pest inhabits, are provided.
    Type: Application
    Filed: November 18, 2008
    Publication date: November 11, 2010
    Inventor: Hajime Mizuno
  • 2-Arylthiazole Derivatives as CXCR3 Receptor Modulators
    Publication number: 20100286191
    Abstract: The invention encompasses compounds of Formula I or pharmaceutically acceptable salts thereof, which are modulators of the CXCR3 chemokine receptor function useful for the treatment or prevention of pathogenic inflammatory processes, autoimmune diseases or graft rejection processes. Methods of use and pharmaceutical compositions are also encompassed.
    Type: Application
    Filed: December 8, 2006
    Publication date: November 11, 2010
    Inventors: Rachel G. Samuel, Conrad Santini
  • Pyrazole Derivatives
    Publication number: 20100280033
    Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases, particularly pyrazole compounds and derivatives are described which inhibit protein kinases. The organic compounds are useful in treating proliferative disease.
    Type: Application
    Filed: December 8, 2008
    Publication date: November 4, 2010
    Inventors: Christopher Thomas Brain, Moo Sung, Young Shin Cho, Ying Hou
  • PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS
    Publication number: 20100279998
    Abstract: The present invention relates to piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
    Type: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Ahmed ABOUABDELLAH, Antonio Almario Garcia, Christian Hoornaert, Jean Jeunesse
  • Compounds and methods for controlling fungi, bacteria and insects
    Patent number: 7820696
    Abstract: The present invention includes compounds of pyridinium salts and methods of their use for industrial uses. The present invention also relates to methods of controlling fungi and/or bacteria. The present invention may also be used to control insects.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: October 26, 2010
    Assignee: Mycosol, Inc.
    Inventors: Richard B. Klein, Jeffrey L. Selph, John J. Partridge, John Reinhard
  • THERAPEUTIC AGENTS USEFUL FOR TREATING PAIN
    Publication number: 20100256111
    Abstract: The invention provides a compound of formula (I): (where R1, Q, A and R2 are disclosed herein) or a pharmaceutically acceptable salt thereof (a “Pyridine-alkynyl Compound”); pharmaceutical compositions comprising an effective amount of a Pyridine-alkynyl Compound; and methods for treating or preventing a condition such as pain, urinary incontinence, an addictive disorder, Parkinson's disease, parkinsonism, anxiety, epilepsy, a seizure, stroke, a pruritic condition, psychosis, a cognitive disorder, a memory deficit, restricted brain function, Huntington's chorea, amyotrophic lateral sclerosis, dementia, retinopathy, a muscle spasm, a migraine, vomiting, dyskinesia or depression in an animal comprising administering to an animal in need thereof an effective amount of a Pyridine-alkynyl Compound.
    Type: Application
    Filed: May 24, 2010
    Publication date: October 7, 2010
    Applicant: Purdue Pharma L.P.
    Inventors: Donald J. Kyle, Qun Sun, Xiaoming Zhou
  • Piperidine carboxylic acid amide derivatives
    Patent number: 7799805
    Abstract: The invention relates to novel piperidine carboxylic acid amide derivatives and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of these novel compounds, pharmaceutical compositions comprising such compounds and especially the use of such compounds as inhibitors of renin.
    Type: Grant
    Filed: May 23, 2006
    Date of Patent: September 21, 2010
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Olivier Bezencon, Christoph Boss, Daniel Bur, Austin Chih-Yu Chen, Olivier Corminboeuf, Daniel Dube, Walter Fischli, Corinna Grisostomi, Lubos Remen, Sylvia Richard-Bildstein, Thierry Sifferlen, Michel Therien, Thomas Weller
  • SUBSTITUTED 1,2,4-OXADIAZOLES AND ANALOGS THEREOF AS CB2 RECEPTOR MODULATORS, USEFUL IN THE TREATMENT OF PAIN, RESPIRATORY AND NON-RESPIRATORY DISEASES
    Publication number: 20100227845
    Abstract: The present invention relates to compounds represented by Formula (I), Formula (II) and Formula (III) and pharmaceutically acceptable salts thereof. The present invention also provides pharmaceutical compositions comprising the instant compounds. This invention further provides methods to treat and prevent pain, respiratory and non-respiratory diseases.
    Type: Application
    Filed: October 14, 2008
    Publication date: September 9, 2010
    Inventors: Zhicai Wu, John C. Hartnett
  • FLUOROPYRROLIDINES HAVING DIPEPTIDYL PEPTIDASE ENZYME INHIBITORY ACTIVITY
    Publication number: 20100210838
    Abstract: The present invention relates to new, potent DPP-IV enzyme inhibitors of the general formula (I), which contain fluorine atoms.
    Type: Application
    Filed: February 1, 2010
    Publication date: August 19, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Peter Arányi, László Balázs, Imre Bata, Sándor Bátori, Éva Boronkay, Philippe Bovy, Károly Kánai, Zoltán Kapui, Edit Susán, Tibor Szabó, Lajos T. Nagy, Katalin Urbán-Szabó, Márton Varga
  • N-PIPERIDIN-4-YLMETHYL-AMIDE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
    Publication number: 20100204275
    Abstract: This invention relates to novel N-piperidin-4-ylmethyl amide derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy, and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: July 31, 2008
    Publication date: August 12, 2010
    Applicant: NeuroSearch A/S
    Inventors: Dan Peters, Birgitte L. Eriksen, John Paul Redrobe, Gordon Munro, Elsebet Østergaard Nielsen
  • PIPERIDINE DERIVATIVES
    Publication number: 20100197715
    Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: January 20, 2010
    Publication date: August 5, 2010
    Inventors: Sabine Kolczewski, Emmanuel Pinard, Henri Stalder
  • Potent and Selective Neuronal Nitric Oxide Synthase Inhibitors with Improved Membrane Permeability
    Publication number: 20100190230
    Abstract: Compounds and related compositions and methods as can be used to inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.
    Type: Application
    Filed: January 25, 2010
    Publication date: July 29, 2010
    Inventors: Richard B. Silverman, Fengtian Xue
  • Novel Substituted Piperidones as HSP Inducers
    Publication number: 20100190824
    Abstract: The present invention relates to novel compounds of formula (I) or (II), their pharmaceutically acceptable salts and their hydrates, solvates, stereoisomers, conformers, tautomers, polymorphs and prodrugs and also pharmaceutically acceptable compositions containing them Wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification. The compounds of the present invention are HSP inducers and by virtue of this effect, useful for the treatment of various diseases accompanying pathological stress. The present invention also relates to a process for the preparation of the said novel compounds. The invention also relates to the use of the above-mentioned compounds for the preparation of medicament for use as pharmaceuticals.
    Type: Application
    Filed: June 24, 2008
    Publication date: July 29, 2010
    Inventors: Prabhat Kumar, Anookh Mohanan, Navnath Argade, Chakradhar Hadole, Appaji Mandhare, Ramesh Gupta, Shailesh Deshpande, Prashant Jamadarkhana, Poonam Joshi
  • 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
  • Preparation of ketone amides
    Patent number: 7759487
    Abstract: The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1-(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry.
    Type: Grant
    Filed: January 5, 2006
    Date of Patent: July 20, 2010
    Assignee: Schering Corporation
    Inventors: Shen-Chun Kuo, David Jieh-Shyh Tsai, Hongbiao Liao
  • ANTIBACTERIAL PIPERDINE DERIVATIVES
    Publication number: 20100179150
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Application
    Filed: February 16, 2006
    Publication date: July 15, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Gregory Basarab, Brian Dangel, Paul Robert Fleming, Michael Barry Gravestock, Oluyinka Green, Sheila Irene Hauck, Pamela Hill, Kenneth Gregory Hull, George Mullen, Brian Sherer, Fei Zhou, Haihong Ni
  • Metalloproteinase inhibitors
    Patent number: 7754750
    Abstract: Compounds of the formula (I) wherein z is SO2 or SO, useful as metalloproteinase inhibitors, especially as inhibitors of MMP12.
    Type: Grant
    Filed: May 6, 2008
    Date of Patent: July 13, 2010
    Assignee: AstraZeneca AB
    Inventors: Anders Eriksson, Matti Lepistö, Michael Lundkvist, Magnus Munck Af Rosenschöld, Pavol Zlatoidsky
  • PIPERIDINE COMPOUNDS AND USES THEREOF - 596
    Publication number: 20100173909
    Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.
    Type: Application
    Filed: December 10, 2009
    Publication date: July 8, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Gregory BASARAB, Pamela HILL, Brian SHERER, Fei ZHOU
  • Novel Pyridine Derivatives, Processes for Preparing Them, Pharmaceutical Compositions Thereof
    Publication number: 20100168077
    Abstract: The present invention concerns 2-amino pyridine derivatives of formula 1 processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: March 31, 2008
    Publication date: July 1, 2010
    Applicant: UCB PHARMA, S.A.
    Inventor: Duncan Hannah
  • Benzimidazole-derivatives as factor Xa inhibitors
    Patent number: 7741341
    Abstract: The present invention relates to compounds of the formula I, wherein R0, R1, R2, Q, V, G and M are as defined herein. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: June 22, 2010
    Assignee: sanofi-aventis Deutschland GmbH
    Inventors: Marc Nazare, Michael Wagner, Volkmar Wehner, Hans Matter, Matthias Urmann, Kurt Ritter
  • Novel Heterocyclic Compounds
    Publication number: 20100152188
    Abstract: The present invention relates to novel compounds of the general formula (I), their derivatives, their analogs, their stereoisomers, their pharmaceutically acceptable salts and compositions. The present invention more particularly provides novel heterocyclic compounds of the general formula (I).
    Type: Application
    Filed: August 4, 2006
    Publication date: June 17, 2010
    Inventors: Akella Satya Surya Visweswara Srinivas, Kasinathan Mathiyazhagan, Duddu Savaraiah Sharada, Thanasekaran Ponpandian, Kulasekharan Revathy, Gaddam Om Reddy, Mani Kamarai, Sriram Raiagopal
  • NOVEL HETEROAROMATIC DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS
    Publication number: 20100144756
    Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Application
    Filed: July 10, 2008
    Publication date: June 10, 2010
    Inventors: Christelle Boléa, Sylvain Calanire
  • Heteerocyclyl-substituted thiazoles as crop protection agents
    Publication number: 20100137245
    Abstract: Heterocyclyl-substituted thiazoles of the formula (I), in which the symbols have the meanings given in the description, and also to the agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Application
    Filed: September 29, 2009
    Publication date: June 3, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Pierre CRISTAU, Nicola Rahn, Stefan Herrmann, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting, Pierre Wasnaire, Sebstian Hoffmann
  • N-linked heterocyclic antagonists of P2Yreceptor useful in the treatment of thrombotic conditions
    Patent number: 7728008
    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: June 26, 2006
    Date of Patent: June 1, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer Qiao, Tammy C. Wang, James C. Sutton, Timur Gungor
  • NOVEL 3-AMINO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H, 6H) CARBALDEHYDE DERIVATIVES
    Publication number: 20100130501
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: (A) and (B) wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Application
    Filed: February 4, 2008
    Publication date: May 27, 2010
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Isonipecotamides for the treatment of integrin-mediated disorders
    Patent number: 7718673
    Abstract: The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: May 18, 2010
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Michael J. Costanzo, William J. Hoekstra, Bruce E. Maryanoff
  • LACTAM-CONTAINING COMPOUNDS AND DERIVATIVES THEREOF AS FACTOR XA INHIBITORS
    Publication number: 20100119510
    Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.
    Type: Application
    Filed: January 22, 2010
    Publication date: May 13, 2010
    Applicant: Bristol-Myers Squibb Company
    Inventors: Donald J.P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y.S. Lam, Stephanie L. Koch
  • Chemical compounds
    Patent number: 7709500
    Abstract: The invention provides compounds of formula (I): wherein: X is CH2, O, S(O)2 or NR10; Y is a bond, CH2, NR35, CH2NH, CH2NHC(O), CH(OH), CH(NHCOR33), CH(NHSO2R34), CH2O or CH2S; Z is C(O), or when Y is a bond Z can also be S(O)2; R1 is optionally substituted aryl, optionally substituted heterocyclyl or C4-6 cycloalkyl fused to a benzene ring; and R2, R3, R4, R5, R6, R7 and R8, R9, R10, R32, R33, R34 and R35 are as defined herein; are modulators of chemokine (especially CCR3) activity (for use in, for example, treating asthma). The invention also provides a process for making 4-(3,4-dichlorophenoxy)piperidine, which is useful as an intermediate for making certain compounds of the invention.
    Type: Grant
    Filed: February 17, 2003
    Date of Patent: May 4, 2010
    Assignee: AstraZeneca AB
    Inventors: Lilian Alcaraz, Mark Furber, Mark Purdie, Brian Springthorpe
  • PIPERIDINE GPCR AGONISTS
    Publication number: 20100105732
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
    Type: Application
    Filed: January 4, 2008
    Publication date: April 29, 2010
    Inventors: Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, John Keily, Simon Andrew Swain, Lisa Sarah Bertram
  • NOVEL BENZAMIDE DERIVATIVES AND PROCESS FOR THE PREPARTION THEREOF
    Publication number: 20100105727
    Abstract: The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT<sb>4</sb> receptor comprising the same, as an active ingredient. Benzamide derivatives of the present invention has superior affinity for 5-HT<sb>4</sb> receptors, capability to reduce the gastric evacuation time, capability to alleviate ventricular tachycardia, ventricular fibrillation, torsades de pointes and QT prolongation, and low toxicity. Therefore, benzamide derivatives of the present invention are therapeutically effective for digestive system diseases.
    Type: Application
    Filed: March 14, 2008
    Publication date: April 29, 2010
    Applicant: DONG-A-PHARM. CO., LTD.
    Inventors: Moo-Hi Yoo, Jae-Keol Rhee, Weon-Bin Im, Sung-Hak Choi, Eun-Jung Kim, Jung-Sang Park, Sun-Ho Choi, Tae-Kyoung Shon, Hyun-Jung Sung, Ja-Young Kim, Ju-Hee Shon
  • Indoles useful in the treatment of inflammation
    Patent number: 7705023
    Abstract: There is provided a compound of formula: (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: April 27, 2010
    Assignee: Biolipox AB
    Inventors: Kristofer Olofsson, Benjamin Pelcman, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
  • SRC FAMILY KINASE INHIBITORS
    Publication number: 20100099710
    Abstract: The invention relates to compounds of general formula (I) wherein X, A, R1 and R2 are as defined herein for use as antiinflammatory agents capable of modulating the activity of a protein tyrosine kinase of the Src family.
    Type: Application
    Filed: April 16, 2008
    Publication date: April 22, 2010
    Inventors: Lene Jensen, Jef Fensholdt
  • Arylamidine derivative, salt thereof, and antifungal containing these
    Patent number: 7700623
    Abstract: An arylamidine derivative represented by the general formula (wherein R1 represents optionally protected or substituted amidino; and R2 and R3 are the same or different and each represents hydrogen or halogeno) or a salt of the derivative. The derivative and salt have potent activity against fungi including ones having tolerance to azole type drugs and further have high safety and excellent properties in a repeated dose toxicity test. They are hence useful as an excellent antifungal.
    Type: Grant
    Filed: June 28, 2005
    Date of Patent: April 20, 2010
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Kazuya Hayashi, Kazuto Kunitani, Sayuri Uehara, Teiichi Morita
  • NK-1 and Serotonin Transporter Inhibitors
    Publication number: 20100087434
    Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating disorders associated with an excess or imbalance of tachykinins or serotonin or both.
    Type: Application
    Filed: November 13, 2009
    Publication date: April 8, 2010
    Inventors: Andrew P. Degnan, Kevin W. Gillman, Derek J. Denhart, Jonathan L. Ditta, Ramkumar Rajamani, Ying Han, George O. Tora
  • 1-isopropyl-2-oxo-1,2-dihydropyridine-3-carboxamide derivatives having 5-HTreceptor agonistic activity
    Patent number: 7691881
    Abstract: This invention provides a compound of formula (I): wherein R1 represents an alkyl group having from 1 to 4 carbon atoms or a halogen atom, R2 represents an alkyl group having from 1 to 4 carbon atoms, R3 represents a hydrogen atom or a hydroxy group, and A represents an oxygen atom or a group of the formula —C(R4)(R5)— (in which R4 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms and R5 represents a hydroxy group or an alkoxy group having from 1 to 4 carbon atoms) or a pharmaceutically acceptable salts thereof. These compounds have 5-HT4 receptor agonistic activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans.
    Type: Grant
    Filed: January 18, 2005
    Date of Patent: April 6, 2010
    Assignee: Pfizer Inc
    Inventors: Tomoki Kato, Kiyoshi Kawamura, Chikara Uchida
  • Azetidine derivatives as CCR-3 receptor antagonist
    Patent number: 7691841
    Abstract: Compounds of formula I in free or salt form, wherein Ar, X, Y and T have the meanings as indicated in the specification, are useful for treating a condition mediated by CCR-3, particularly an inflammatory or allergic condition such as an inflammatory or obstructive airways disease. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: April 6, 2010
    Assignee: Novartis AG
    Inventor: Darren M Legrand
  • SUBSTITUTED 4-AMINO-3,5-DICYANO-2-THIOPYRIDINES AND USE THEREOF
    Publication number: 20100069363
    Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
    Type: Application
    Filed: November 17, 2007
    Publication date: March 18, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Joerg Keldenich
  • IMIDAZOLE COMPOUNDS HAVING AN ANTIINFLAMMATORY EFFECT
    Publication number: 20100069436
    Abstract: The invention relates to imidazole derivatives of the Formula (I) in which the radicals R1, R2, R3, R4 and R5 have the meanings indicated in the description. The compounds of the invention have an immunomodulating and/or cytokine release-inhibiting effect and are therefore suitable for the treatment of disorders associated with an impairment of the immune system.
    Type: Application
    Filed: August 24, 2007
    Publication date: March 18, 2010
    Applicant: Merckle
    Inventors: Wolfgang Albrecht, Dominik Hauser, Stefan Laufer, Hans-Gunter Striegel, Karola Tollmann
  • NOVEL ALKYL SUBSTITUTED PIPERIDINE DERIVATIVES AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS
    Publication number: 20100056567
    Abstract: This invention relates to novel alkyl substituted piperidine derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.
    Type: Application
    Filed: November 9, 2009
    Publication date: March 4, 2010
    Inventors: Dan PETERS, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Jorgen Scheel-Krûger
  • INHIBITORS OF AKT ACTIVITY
    Publication number: 20100056523
    Abstract: Invented are novel 1H-imidazo[4,5-c]pyridin-2-yl compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
    Type: Application
    Filed: November 9, 2006
    Publication date: March 4, 2010
    Inventors: Dirk A. Heerding, Tammy J. Clark, Jack Dale Leber, Igor Safonov
  • PIPERIDINE GPCR AGONISTS
    Publication number: 20100048625
    Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of obesity and diabetes.
    Type: Application
    Filed: January 4, 2008
    Publication date: February 25, 2010
    Inventors: Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, John Keily, Simon Andrew Swain
  • Anabaseine derivatives, pharmaceutical compositions and method of use thereof
    Patent number: 7662965
    Abstract: Disclosed are novel anabaseine derivatives that act as agonists of the ?7 nAChR. Also disclosed are pharmaceutical compositions, methods of treating inflammatory conditions, methods of treating CNS disorders, methods for inhibiting cytokine release from mammalian cells and methods for the preparation of the novel compounds.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: February 16, 2010
    Assignee: Cornerstone Therapeutics, Inc.
    Inventors: Gregory J. Habgood, Daniel Elbaum
  • Benzoimidazole compounds
    Patent number: 7662966
    Abstract: Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
    Type: Grant
    Filed: August 26, 2008
    Date of Patent: February 16, 2010
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: James P. Edwards, Michael D. Hack, David E. Kindrachuk, Jennifer D. Venable
  • Pyridine, pyrimidine and pyrazine derivatives as gpcr agonists
    Publication number: 20100035897
    Abstract: Compounds of formula (I): R1-A-V—B—R2, wherein V is phenyl or a 6-membered heteroaryl ring containing up to three N-atoms, or pharmaceutically acceptable salts thereof, are agonists of GPR116 and are useful for the treatment of obesity, and for the treatment of diabetes.
    Type: Application
    Filed: December 30, 2005
    Publication date: February 11, 2010
    Inventors: Stuart Edward Bradley, Matthew Colin Thor Fyfe, Gerard Hugh Thomas
  • Pyridyltetrahydropyridines and Pyridylpiperidines, and Method of Manufacturing Them
    Publication number: 20100029947
    Abstract: The present invention provides pyridine derivatives useful as intermediates of drugs and agricultural chemicals, electrophotographic receptors, dyes and so on. More specifically, the invention relates to novel pyridyltetrahydropyridines and novel pyridylpiperidines, and further to a method of manufacturing pyridine derivatives through reaction between bipyridine derivatives and benzyl halide or benzyloxycarbonyl halide and subsequent reduction of the resultant reaction products with the aid of palladium catalysts, platinum catalysts, ruthenium catalysts or rhodium catalysts.
    Type: Application
    Filed: October 9, 2009
    Publication date: February 4, 2010
    Inventors: Hirokazu Kuwabara, Takayuki Sonoda, Hiromitsu Saitoh, Hidehiro Arai
  • Heterocyclic compounds and methods of use
    Patent number: 7652051
    Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.
    Type: Grant
    Filed: August 24, 2005
    Date of Patent: January 26, 2010
    Assignee: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTOR INHIBITORS
    Publication number: 20100016343
    Abstract: The present invention provides compounds and compositions, methods of making them, and methods of using them to modulate ?7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system.
    Type: Application
    Filed: July 16, 2009
    Publication date: January 21, 2010
    Applicants: WYETH, SIENA BIOTECH S.P.A.
    Inventors: Chiara Ghiron, Michela Valacchi, Ugo Zanelli, Simon N. Haydar