Hetero Ring Is Four-membered And Includes At Least One Ring Nitrogen Patents (Class 514/210.01)
  • Publication number: 20100087414
    Abstract: The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5 -difluorophenyl)methylsulfonamide.
    Type: Application
    Filed: December 11, 2009
    Publication date: April 8, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Philippe BOFFELLI, Michel DELTHIL, Luc GRONDARD, Maxime LAMPILAS, Joel MALPART, Stephane MUTTI, Lahlou NAIT-BOUDA, Joerg RIEKE-ZAPP
  • 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
  • Patent number: 7687489
    Abstract: A pharmaceutical composition for the treatment and/or prevention of cerebral ischemic diseases, which comprises two components, i.e. an astrocyte function-improving agent, preferably a compound represented by the formula (I): (wherein R6 is hydroxy, etc., (1) n is 1, R11 is hydrogen and R5 is (alkyl of which one carbon atom is substituted by fluorine)-CH2— or (2) n is 0 or 1, R11 is hydrogen, etc., and R5 is alkyl, etc.) and a thrombolytic agent, preferably tissue plasminogen activator, as active ingredients. The pharmaceutical composition of the present invention exhibits a synergistic therapeutic effect compared to independent administration of an astrocyte function-improving agent and a thrombolytic agent.
    Type: Grant
    Filed: May 24, 2007
    Date of Patent: March 30, 2010
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kaneyoshi Honjo, Narito Tateishi, Nobuo Katsube
  • Patent number: 7687493
    Abstract: The present invention relates to a novel method for the preparation of azetidine derivatives such as N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-quinol-6-ylmethylsulfonamide and the dihydrochloride thereof and N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: March 30, 2010
    Assignee: Aventis Pharma SA
    Inventors: Stephane Mutti, Michel Lavigne, Luc Grondard, Joel Malpart, Joerg Rieke-Zapp, Veronique Crocq-Stuerga
  • Publication number: 20100075941
    Abstract: An alkyl ether derivative represented by the following general formula [1] or its salt: wherein R1 and R2 represent each a substituent such as hydrogen, halogeno or alkyl; R3 represents alkylamino, amino or hydroxyl; the ring A represents a 5- or 6-membered aromatic heterocycle or a benzene ring; m and n are each an integer of from 1 to 6; and p is an integer of from 1 to 3; shows an effect of protecting retinal nerve cells and, therefore, is useful as a preventive and/or a remedy for retinal nerve diseases such as glaucoma, diabetic retinopathy, retinal artery obstruction, retinal venous obstruction, macular degeneration and retinopathy of prematurity.
    Type: Application
    Filed: August 17, 2009
    Publication date: March 25, 2010
    Applicant: Toyama Chemical Co., Ltd.
    Inventors: Tatsuo KIMURA, Noboru IWAKAMI, Akihito SAITOH
  • Patent number: 7678808
    Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.
    Type: Grant
    Filed: May 8, 2007
    Date of Patent: March 16, 2010
    Assignee: BrainCells, Inc.
    Inventors: Carrolee Barlow, Todd Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
  • Publication number: 20100063021
    Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.
    Type: Application
    Filed: August 20, 2007
    Publication date: March 11, 2010
    Inventors: Robert J. Davies, Jingwang Xu
  • Patent number: 7666860
    Abstract: A melt-formulated, multiparticulate, oral dosage form containing clavulanic acid and/or at least one physiologically acceptable salt thereof and at least one sucrose fatty acid ester and optionally further physiologically acceptable auxiliary substances; a process for producing such a dosage form, combination dosage forms with ?-lactam antibiotics, and the pharmaceutical use thereof, e.g., for treating bacterial infections.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: February 23, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Iris Ziegler, Johannes Bartholomaeus, Dieter Schateikis
  • Publication number: 20100022501
    Abstract: The invention concerns injectable or orally deliverable binary or ternary formulations of azetidine derivatives. The azetidine derivatives used in the inventive pharmaceutical compositions can be represented by the general formulae (Ia) or (Ib), wherein Ar is an aromatic or heteroaromatic group optionally substituted by one or more among (C1-C4)alkyl, halogen, NO2, CN, (C1-C4) alkoxy or OH.
    Type: Application
    Filed: October 5, 2009
    Publication date: January 28, 2010
    Applicant: AVENTIS PHARMA SA
    Inventors: Maria-Teresa PERACCHIA, Gilbert GAUDEL, Sophie COTE
  • Publication number: 20100016272
    Abstract: The present invention relates to heteroarylacrylamides of the formula I, in which Het, X, Ra, Rb, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.
    Type: Application
    Filed: June 17, 2009
    Publication date: January 21, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Hartmut STROBEL, Paulus WOHLFART, Heinz-Werner KLEEMANN, Gerhard ZOLLER, David William WILL
  • Publication number: 20090318406
    Abstract: The present invention relates to novel oxindole derivatives of general formula (I), in which the substituents R1, R2, A, B and Y are as defined in claim 1, medicinal products containing them and use thereof for the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
    Type: Application
    Filed: August 24, 2007
    Publication date: December 24, 2009
    Applicant: ABBOTT GMBH & CO. KG
    Inventors: Herve Geneste, Thorsten Oost, Astrid Netz, Charles W. Hutchins, Wolfgang Wernet, Wolfgang Lubisch, Liliane Unger, Wilfried Hornberger
  • Patent number: 7632820
    Abstract: Disclosed are compounds of the formulain which n is 0 or 1; X—Y is —CH?CH— or —CH2—CH2—; Z is —C(?O)—, —C(?S)— or —SO2—; R1 is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; and R2 is R3-Z-, R3—O-Z-, R4 or -Z-N(R6)(R7); Q is O or —N—R5; R3 and R4 are for example H, C1C12alkyl, C2-C12alkenyl, C2-C12alkynyl, C3-C12zcycloalkyl, C5-C12cycloalkenyl, aryl or heterocyclyl; R5 is for example H, C1-C8alkyl, hydroxy-C1-C8alkyl, C3-C8cycloalkyl, C2-C8alkenyl, C2-C8alkynyl, phenyl or benzyl; R6 and R7 are for example, H, unsubstituted or mono- to pentasubstituted C1-C12alkyl, unsubstituted or mono- to pentasubstituted C2-C12alkenyl or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof, in each case in free form or in salt form, are useful as pesticides.
    Type: Grant
    Filed: January 30, 2004
    Date of Patent: December 15, 2009
    Assignee: Merial Limited
    Inventors: Thomas Pitterna, Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Pierre Jung
  • Publication number: 20090306037
    Abstract: The present invention relates to pharmaceutical compositions comprising a combination of a particular dipeptidyl peptidase-IV (DPP-IV) inhibitor and a particular cannabinoid CB?1#191 receptor antagonist/inverse agonist, kits containing such combinations and methods of using such compositions for the treatment of diabetes, diabetes associated with obesity, diabetes-related disorders, obesity, and obesity-related disorders.
    Type: Application
    Filed: April 28, 2006
    Publication date: December 10, 2009
    Applicant: MERCK & CO., INC.
    Inventors: John M. Amatruda, Tung M. Fong, David E. Moller, Nancy A. Thornberry
  • Publication number: 20090291935
    Abstract: The present invention provides X-nitro compound, pharmaceutical compositions of X-nitro compounds and methods of using X-nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
    Type: Application
    Filed: April 23, 2009
    Publication date: November 26, 2009
    Applicant: RadioRx, Inc.
    Inventors: Mark D. BEDNARSKI, Lynn M. Oehler, Andrew C. Haaland, Susan J. Knox
  • Publication number: 20090281072
    Abstract: A compound which may be used for the prevention or treatment of respiratory diseases in which STAT 6 is concerned, particularly asthma, chronic obstructive pulmonary disease and the like is provided. A pyrimidine derivative or a salt thereof, which has an arylamino or arylethylamino group which may be substituted with a specified substituent, at the 2-position, amino group substituted with benzyl group or the like, at the 4-position, and carbamoyl group which may be substituted, at the 5-position, is provided.
    Type: Application
    Filed: September 22, 2008
    Publication date: November 12, 2009
    Applicant: Astellas Pharm Inc.
    Inventors: Shinya Nagashima, Hiroshi Nagata, Masashiro Iwata, Masaki Yokota, Hiroyuki Moritomo, Eiichi Nakai, Sadao Kuromitsu, Keiko Ohga, Makoto Takeuchi
  • Publication number: 20090281076
    Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.
    Type: Application
    Filed: April 11, 2007
    Publication date: November 12, 2009
    Inventors: Matthew Colin, Thor Fyfe, William Gattrell, Chrystelle Marie Rasamison
  • Publication number: 20090275524
    Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agents
    Type: Application
    Filed: May 7, 2009
    Publication date: November 5, 2009
    Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
  • Publication number: 20090264398
    Abstract: The present invention refers to a method for inducing tumor apoptosis by influencing the ROS (reactive oxygen species) signaling pathway in tumor cells. Increasing the level of ROS leads to the selective inactivation of a tumor cell catalase and subsequently to an apoptosis of these cells. The level of ROS can be increased by increasing the level of nitric oxide through inhibition of the enzymes nitric oxide dioxygenase or arginase. According to the present invention inhibitors of the nitric oxide dioxygenase or arginase can be used for the manufacture of a medicament for the treatment of cancer. The present invention further provides a method for identifying compounds which can be used for the treatment of cancer, wherein the method allows to specifically identify compounds which induce apoptosis through the ROS signaling pathway. The present invention also provides a kit for identifying compounds which induce tumor apoptosis by inactivating a catalase on the tumor cell surface.
    Type: Application
    Filed: August 7, 2007
    Publication date: October 22, 2009
    Applicant: Universitatsklinikum Freiburg
    Inventor: Georg Bauer
  • Publication number: 20090253669
    Abstract: Substituted sulfonamide compounds corresponding to the formula I: processes for the preparation thereof, pharmaceutical composition containing these compounds and the use of substituted sulfonamide compounds for the preparation of pharmaceutical compositions.
    Type: Application
    Filed: March 16, 2009
    Publication date: October 8, 2009
    Applicant: GRUENENTHAL GmbH
    Inventors: Stefan OBERBOERSCH, Melanie REICH, Bernd SUNDERMANN, Werner ENGLBERGER, Sabine HEES, Ruth JOSTOCK, Stefan SCHUNK, Edward BIJSTERVELD, Fritz THEIL
  • Publication number: 20090253670
    Abstract: The invention relates to novel amide derivatives that are positive allosteric modulators of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.
    Type: Application
    Filed: March 26, 2009
    Publication date: October 8, 2009
    Applicant: ABBOTT LABORATORIES
    Inventors: Michael R. Schrimpf, Kathleen H. Mortell, Diana L. Nersesian, Chih-Hung Lee, Bruce Clapham
  • Publication number: 20090203663
    Abstract: The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.
    Type: Application
    Filed: February 7, 2007
    Publication date: August 13, 2009
    Applicant: AstraZeneca AB
    Inventors: Jean Claude Arnould, Benedicte Delouvrie, Jason Grant Kettle
  • Publication number: 20090197857
    Abstract: The present invention provides novel substituted amino-azetidines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.
    Type: Application
    Filed: January 29, 2009
    Publication date: August 6, 2009
    Applicant: JENRIN DISCOVERY
    Inventors: John F. McElroy, Robert J. Chorvat
  • Publication number: 20090197856
    Abstract: Provided are compounds of Formula (I) or a pharmaceutically acceptable salt or solvate thereof. The compounds and compositions are useful for treating viral infections caused by the Flaviviridae family of viruses.
    Type: Application
    Filed: December 19, 2008
    Publication date: August 6, 2009
    Inventors: Salvador G. Alvarez, Janos Botyanszki, Joseph de los Angeles, Jiping Fu, Roger Fujimoto, Joshua Michael Gralapp, Ronald Conrad Griffith, Peichao Lu, Son Minh Pham, Christopher Don Roberts, Franz Ulrich Schmitz, Mohindra Seepersaud, Ruben Tommasi, Adam Christopher Villa, Sompong Wattanasin, Aregahagn Yifru, Rui Zheng, Xiaoling Zheng
  • Publication number: 20090186834
    Abstract: Various azetidinone, pyrrolidine, imidazolidine, and oxazolidine derivatives are described, as are pharmaceutical compositions containing these compounds and methods of treatment of diseases using these compounds. Other embodiments are also described.
    Type: Application
    Filed: March 24, 2006
    Publication date: July 23, 2009
    Applicant: MICROBIA, INC.
    Inventors: John Talley, Eduardo Martinez, Daniel Zimmer, Regina Lundrigan
  • Publication number: 20090170824
    Abstract: Compounds of formula I: are potent and selective antagonists of the human 5-HT2A receptor, and hence useful in treatment of a variety of adverse conditions of the CNS.
    Type: Application
    Filed: December 12, 2008
    Publication date: July 2, 2009
    Inventors: Jose Luis Castro Pineiro, Laura Catherine Cooper, Myra Gilligan, Alexander Charles Humphries, Peter Alen Hunt, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Monique Bodil Van Niel, Kevin Wilson
  • Patent number: 7544676
    Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: June 9, 2009
    Assignee: Adolor Corporation
    Inventors: Roland E. Dolle, Karin Worm
  • Patent number: 7544667
    Abstract: The present invention relates to novel hypocholesterolemic compounds of formula (I) useful in the treatment and prevention of atherosclerosis and for the reduction of cholesterol levels as well as to pharmaceutical compositions comprising said compounds alone or in combination with other active agents.
    Type: Grant
    Filed: September 15, 2004
    Date of Patent: June 9, 2009
    Assignee: Lipideon Biotechnology AG
    Inventors: Erick Carreira, Helmut Hauser, Lisbet Kvaerno, Tobias Ritter, Moritz Werder
  • Publication number: 20090093451
    Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Application
    Filed: April 20, 2007
    Publication date: April 9, 2009
    Applicant: Smithkline Beecham Corporation
    Inventor: Jakob Busch-Petersen
  • Patent number: 7511159
    Abstract: It is intended to provide compounds having EDG-5 antagonism. Because of having EDG-5 antagonism, compounds of the formula (I): wherein each symbol is as defined in the description; salts thereof, N-oxides thereof, solvates thereof or prodrugs thereof are useful as preventive and/or therapeutic agent for EDG-5 mediated diseases, for example, diseases caused by blood vessel contraction (e.g. cerebrovascular spasms disease, cardiovascular spasms diseases, coronary artery spasms disease, hypertension, pulmonary hypertension, renal diseases, myocardial infarction, angina pectoris, arrhythmia, portal hypertension, varicosity and the like), arteriosclerosis, pulmonary fibrosis, hepatic fibrosis, renal fibrosis, respiratory diseases (e.g. bronchial asthma, chronic obstructive pulmonary diseases and the like), nephropathy, diabetes, hyperlipemia and the like.
    Type: Grant
    Filed: December 24, 2004
    Date of Patent: March 31, 2009
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hiromu Habashita, Haruto Kurata, Shinji Nakade, Takeji Ono
  • Patent number: 7507842
    Abstract: The present invention provides cyclic nitro compound, pharmaceutical compositions of cyclic nitro compounds and methods of using cyclic nitro compounds and/or pharmaceutical compositions thereof to treat or prevent diseases or disorders characterized by abnormal cell proliferation, such as cancer, inflammation, cardiovascular disease and autoimmune disease.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: March 24, 2009
    Assignees: RadioRx, Inc., Alliant Techsystems Inc.
    Inventors: Lynn M. Oehler, legal representative, Susan Knox, Louis Cannizzo, Kirstin Warner, Robert Wardle, Stephen Velarde, Shoucheng Ning, Mark D. Bednarski
  • Patent number: 7504522
    Abstract: Compounds of formula (I) and their use in therapy, particularly for the treatment of a disorder mediated by CB1 receptors such as obesity: Formula (I) wherein: R1 and R2 are independently selected from aryl; and R3 is hydrogen or alkyl; or a pharmaceutically acceptable salt or prodrug thereof, wherein at least one of R1 and R2 has a non-hydrogen substituent in the ortho-position(s) thereof relative to the point of attachment to the [—CH—O—] group.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: March 17, 2009
    Assignee: Vernalis Research Limited
    Inventors: James Edward Paul Davidson, Claire Elizabeth Dawson, Kerry Harrison, Howard Langham Mansell, Robert Mark Pratt, Sukhjit Sohal, Victoria Jane Ruston
  • Publication number: 20090069284
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Application
    Filed: October 21, 2008
    Publication date: March 12, 2009
    Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
  • Patent number: 7494987
    Abstract: An agent for preventing/treating respiratory diseases contains, as an active ingredient, a compound represented by following Formula (I): wherein A is a group represented by L-W [wherein L is a bond or CH2; and W is O, SOn (wherein n is 0 to 2), or —NR7— (wherein R7 is hydrogen or lower alkyl)]; each of G1 and G2 is (CH2)r (wherein r is 0 to 2), provided that when n is 1, G1 and G2 may be bridged by lower alkylene; Y is a lower alkylene or (substituted) benzylidene; Z is a bond or O, provided that when Z is a bond, Y may form a 5- or 6-membered ring with carbon on the benzene ring; R1 is, for example, NO2, a lower alkoxycarbonyl, (substituted) carbamoyl, (protected) hydroxyl group, (protected) carboxyl, or (protected) N-hydroxycarbamoyl; each of R2 and R3 is hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy or NO2; each of R4 and R5 is, for example, hydrogen, halogen, (halogenated) lower alkyl, (halogenated) lower alkoxy, CN, or lower alkylsulfonyl; and R6 is hydrogen or lower alkyl
    Type: Grant
    Filed: November 25, 2003
    Date of Patent: February 24, 2009
    Assignee: Mochida Pharmaceutical Co., Ltd.
    Inventors: Yasushige Akada, Kazuyuki Matsuura
  • Publication number: 20090048224
    Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: September 5, 2008
    Publication date: February 19, 2009
    Applicants: Amgen, Inc., Array BioPharma, Inc.
    Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
  • Publication number: 20090048223
    Abstract: A compound represented by the formula (1) [A represents a nitrogen-containing saturated ring; m represents an integer of 0 to 2; n represents an integer of 1 to 4; G1 represents hydrogen atom, chlorine atom, hydroxyl group, an alkoxy group, or amino group; G2 represents a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; G3 represents hydrogen atom, a halogen atom, hydroxyl group, cyano group, carboxy group, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, an alkylthio group, an amino group, an alkoxycarbonyl group, an acyl group, an acyloxy group, an alkylsulfinyl group, an alkylsulfonyl group, or an aryl group; Y represents a single bond, or —C(R3)(R4)— (R3 and R4 represent hydrogen atom, or an alkyl group, or alkylene groups which combine together to form a saturated hydrocarbon ring group); G4 represents hydro
    Type: Application
    Filed: February 27, 2008
    Publication date: February 19, 2009
    Applicant: Asahi Kasei Pharma Corporation
    Inventors: Koki Matsubara, Atsushi Iesato, Akifumi Oomura, Koh Kawasaki, Rintaro Yamada, Minoru Seto
  • Publication number: 20090042851
    Abstract: The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.
    Type: Application
    Filed: July 21, 2008
    Publication date: February 12, 2009
    Applicant: SANOFI-AVENTIS
    Inventors: Pierre DESPEYROUX, Evelyne Fontaine, Gilles Courtemanche, Pierrick Rochard, Claudine Serradeil-Le Gal
  • Publication number: 20090036420
    Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.
    Type: Application
    Filed: July 28, 2008
    Publication date: February 5, 2009
    Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 7485651
    Abstract: Compounds and methods are provided for the alleviation or treatment of diseases or conditions in which modification of muscarinic m1 receptor activity has a beneficial effect. In the method, a therapeutically effective amount of a selective muscarinic m1 agonist compound is administered to a patient in need of such treatment.
    Type: Grant
    Filed: January 7, 2003
    Date of Patent: February 3, 2009
    Assignee: Acadia Pharmaceuticals, Inc.
    Inventors: Mark Brann, Terri Messier, Erika Currier, Kate Duggento, Tracy Spalding, Mikael Friberg, Niels Skjaerbaek
  • Publication number: 20090029962
    Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar, n and o are as defined herein and to their pharmaceutically acceptable active salts. Compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Application
    Filed: July 21, 2008
    Publication date: January 29, 2009
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
  • Patent number: 7473779
    Abstract: Novel derivatives of amidines of formula wherein the substituents are defined as in the specification which are useful for inhibiting activity on NO-synthase enzymes producing nitrogen mono oxide and/or trapping the reactive oxygen species (ROS) making them useful for treating various diseases.
    Type: Grant
    Filed: September 12, 2003
    Date of Patent: January 6, 2009
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
  • Publication number: 20080312205
    Abstract: The invention relates to a novel method for the synthesis of N-{1-[bis(4-chlorophenyl)methyl]azetidin-3-yl}-N-(3,5-difluorophenyl)methylsulfonamide.
    Type: Application
    Filed: August 20, 2008
    Publication date: December 18, 2008
    Applicant: SANOFI-AVENTIS
    Inventors: Philippe BOFFELLI, Michel DELTHIL, Luc GRONDARD, Maxime LAMPILAS, Joel MALPART, Stephane MUTTI, Lahlou NAIT-BOUDA, Joerg RIEKE-ZAPP
  • Patent number: 7465719
    Abstract: This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently:—O —C(?O)— or —C(?O)—O — or —C(?O)—; Cy is a cyclyl group and is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q2 is an acid leader group, and is independently: C1-8alkylene; and is optionally substituted; or: Q2 is an acid leader group, and is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or C1-7alkylene-C5-20ary
    Type: Grant
    Filed: January 19, 2004
    Date of Patent: December 16, 2008
    Assignee: Topotarget UK Limited
    Inventors: Paul W. Finn, Ivars Kalvinsh, Einars Loza, Aleksandrs Gutcaits, Irena Olutnika, Ludmila Serpionova, Vija Gailite, Rasma Bokaldere
  • Patent number: 7462629
    Abstract: The present invention relates to immunosuppressant, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG receptor mediated signal transduction.
    Type: Grant
    Filed: May 19, 2004
    Date of Patent: December 9, 2008
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Yi Fan, Wenqi Gao
  • Publication number: 20080293685
    Abstract: This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.
    Type: Application
    Filed: May 22, 2008
    Publication date: November 27, 2008
    Applicant: Chevron U.S.A. Inc.
    Inventors: Deyuan Kong, Frederick W. Lam, Steven F. Sciamanna, Earl Shelton, Shenggao Liu, Robert M. Carlson
  • Publication number: 20080293686
    Abstract: The present invention relates to novel formulations of azetidine derivatives for oral administration comprising at least one azetidine compound of formula (Ia) or (Ib): in a system comprising a Vitamin E d-?-tocopheryl polyethylene glycol 1000 succinate polymeric semi-solid material.
    Type: Application
    Filed: July 28, 2008
    Publication date: November 27, 2008
    Applicant: AVENTIS PHARMA S.A.
    Inventors: Maria-Teresa PERACCHIA, Sophie COTE, Valerie BOBINEAU
  • Publication number: 20080293684
    Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: July 26, 2005
    Publication date: November 27, 2008
    Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
  • Patent number: 7452879
    Abstract: The present invention provides methods of treating or preventing autoimmune diseases with 2,4-pyrimidinediamine compounds, as well as methods of treating, preventing or ameliorating symptoms associated with such diseases. Specific examples of autoimmune diseases that can be treated or prevented with the compounds include rheumatoid arthritis and/or its associated symptoms, systemic lups erythematosis and/or its associated symptoms and multiple sclerosis and/or its associated symptoms.
    Type: Grant
    Filed: October 5, 2006
    Date of Patent: November 18, 2008
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Hui Li, Somasekhar Bhamidipati, David Carroll, Catherine Sylvain, Jeffrey Clough, Holger Keim
  • Publication number: 20080280867
    Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ).
    Type: Application
    Filed: March 28, 2008
    Publication date: November 13, 2008
    Applicant: Abbott Laboratories
    Inventors: Vincent L. Giranda, Thomas D. Penning, Wolfgang Wernet, David J. Frost, Cherrie K. Donawho
  • Publication number: 20080234247
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including opiate receptors, other G-protein-coupled receptors, and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds as analgesics.
    Type: Application
    Filed: March 17, 2008
    Publication date: September 25, 2008
    Applicant: Sepracor, Inc.
    Inventors: Brian M. Aquila, James R. Hauske, Liming Shao
  • Publication number: 20080227767
    Abstract: Methods and compositions which are useful in the treatment of amyloidosis. In particular, methods and compositions are provided for inhibiting, preventing and treating amyloid deposition, e.g., in pancreatic islets, wherein the amyloidotic deposits are islet amyloid polypeptide (IAPP)-associated amyloid deposition or deposits. The methods of the invention involve administering to a subject a therapeutic compound which inhibits IAPP-associated amyloid deposits. Accordingly, the compositions and methods of the invention are useful for inhibiting IAPP-associated amyloidosis in disorders in which such amyloid deposition occurs, such as diabetes.
    Type: Application
    Filed: May 22, 2008
    Publication date: September 18, 2008
    Applicant: Neurochem (International) Limited
    Inventors: Walter A. Szarek, Donald F. Weaver, Xianqi Kong, Ajay Gupta, David Migneault