Ring Nitrogen In The Polycyclo Ring System Patents (Class 546/198)
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Publication number: 20090318690Abstract: Disclosed is a compound represented by the general formula (I) or a salt thereof: wherein any one of R1, R2 and R3 represents a group represented by the formula: —(CH2)m-NR11R12 (wherein m is 1 or 2; and R11 and R12 independently represent a hydrogen atom or a C1-6 alkyl group or may, together with a nitrogen atom to which R11 and R12 are bound, form a 4- or 5-membered cyclic group); the remaining two or R1, R2 and R3 independently represent a group represented by the formula: —(O)n-R21 (wherein n is 0 or 1; and R21 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like); and R4 represents a C1-6 alkyl group which may have a substituent or the like.Type: ApplicationFiled: April 27, 2007Publication date: December 24, 2009Applicant: Eisai R&D Management Co., Ltd.Inventors: Atsushi Sasaki, Kohshi Ueno, Yuichi Suzuki, Shinichi Hamaoka, Daisuke Shimmyo, Yoshinori Takahashi, Toshiki Kurokawa, Yuji Kazuta, Hiroo Ogura, Tatsuto Fukushima
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Patent number: 7635696Abstract: The present invention relates to novel isoxazoline-indole derivatives according to Formula (I), a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, with a binding affinity towards dopamine receptors, in particular towards dopamine D2 and/or D3 receptors, with selective serotonin reuptake inhibition (SSRI) properties and showing an affinity for the 5-HT1A receptor, pharmaceutical compositions comprising the compounds according to the invention, the use thereof for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic disorders, most in particular schizophrenia and processes for their production, wherein the variables are further defined in the application.Type: GrantFiled: November 25, 2005Date of Patent: December 22, 2009Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, José Manuel Bartolomé-Nebreda, Manuel Jesus Alcázar-Vaca, Maria de las Mercedes Garcia-Martin, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20090298833Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.Type: ApplicationFiled: July 20, 2009Publication date: December 3, 2009Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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Publication number: 20090264405Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 30, 2006Publication date: October 22, 2009Inventors: Amjad Ali, Julianne A. Hunt, Florida Kallashi, Jennifer Kowalchick, Dooseop Kim, Cameron J. Smith, Peter J. Sinclair, Ramzi F. Sweis, Gayle E. Taylor, Christopher F. Thompson, Liya Chen, Nazia Quraishi
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Publication number: 20090264459Abstract: Compounds of formula (I) in free or a pharmaceutically acceptable salt form, wherein X1, L and Q have the meanings as indicated in the specification, are useful for treating obstructive or inflammatory airways diseases. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: June 28, 2007Publication date: October 22, 2009Inventors: Stephen Paul Collingwood, Robin Alec Fairhurst, Neil John Press
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Patent number: 7601734Abstract: An object of the present invention is to provide a cyclic amine compound which has a potent inhibitory effect on the binding of ?2C-adrenoceptor and is useful in preventing and treating disorders attributable to ?2C-adrenoceptor. The above-described object is solved by the following cyclic amine compound, etc., wherein X is O, S, SO, SO2 or NR2, etc.; R1 is a hydrogen atom, a cyano group, a carboxyl group, a C2-C13 alkoxycarbonyl group, a carbamoyl group, etc.; Ar1 and Ar2 are the same or different and each represent an aryl or heteroaryl group which may be substituted by 1 to 3 substituents and so on; ring B is a benzene ring may be substituted by 1 to 3 substituents and so on; n is an integer from 1 to 10; and p and q are the same or different and each represent an integer of 1 or 2.Type: GrantFiled: April 8, 2005Date of Patent: October 13, 2009Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Toshihito Kumagai, Toshio Nakamura, Yuri Amada, Yoshinori Sekiguchi
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Patent number: 7598359Abstract: A bis(indolestyryl) compound. The bis(indolestyryl) compound has formula (I): wherein A and B comprise benzene, naphthalene, or heterocyclic ring containing O, S, or N, R1 and R1? are H, halogen, C1-5 alkyl, nitro, ester, carboxyl, sulfo, sulfonamide, amide, sulfo ester, C1-3 alkoxy, amino, alkylamino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, R2, R2?, R3, and R3? comprise H, C1-6 alkyl, C6-18 aryl, C2-6 alkenyl, C3-6 cycloalkenyl, or C3-6 cycloalkyl, R4 is H, C1-5 alkyl, hydroxyl, halogen, or alkoxy, R5 and R5? comprise H, halogen, C1-5 alkyl, nitro, C1-3 alkoxy, amino, cyano, C1-6 alkylsulfonyl, or C2-7 alkoxy carbonyl, W comprises oxygen, sulfur, selenium, —NR, or —C(CH3)2, n is 1˜18 and Z1 and Z2 are different and comprise an anion or an anionic organometallic complex with +1 or +2 valence, wherein R bonded to nitrogen is C1-4 alkyl.Type: GrantFiled: September 1, 2005Date of Patent: October 6, 2009Assignee: Industrial Technology Research InstituteInventors: Shin-Shin Wang, Jong-Lieh Yang, Chii-Chang Lai, Hui-Ping Tsai, Wen-Ping Chu, Chien-Wen Chen, Chien-Liang Huang, Wen-Yih Liao, Ming-Chia Lee
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Patent number: 7598271Abstract: The invention relates to a compound, and pharmaceutically acceptable salts, having the formula I: wherein: R represents an alkyl or alkynyl group having 1-4 carbon atoms, or a phenyl group optionally substituted by C1-4 alkyl, alkylthio, alkoxy, halogen, nitro, acylamino, methylsulfonyl or methylenedioxy, or represents tetrahydronaphthyl, R1 represents hydrogen, trifluoro (C1-4) alkyl, alkyl or alkynyl, X represents hydrogen, alkyl having 1-4 carbon atoms, alkoxy, trifluoroalkyl, hydroxy, halogen, methylthio or aralkoxy, R2 represents: a C1-C10 alkyl group, a phenyl group optionally substituted by one or more of the following groups: a C1-C10 alkyl group, a halogen group, a nitro group, hydroxy group, and/or an alkoxy group.Type: GrantFiled: November 30, 1998Date of Patent: October 6, 2009Assignee: Noven Therapeutics, LLCInventors: Franciscus Bernardus Gemma Benneker, Frans Van Dalen, Jacobus Maria Lemmens, Theodorus Hendricus Antonium Peters, Frantisek Picha
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Publication number: 20090247509Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: ApplicationFiled: April 17, 2009Publication date: October 1, 2009Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: James A. Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M. Shutske, Joseph T. Strupczewski, Kenneth J. Bordeau, John G. Jurcak, Thaddeus R. Nieduzak, Sharon A. Jackson, Paul Angell, James P. Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
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Publication number: 20090209583Abstract: The present invention relates to 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives, their use as protease inhibitors, in particular as broad-spectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present 2-(substituted-amino)-benzothiazole sulfonamide compounds and derivatives with another anti-retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: ApplicationFiled: June 22, 2007Publication date: August 20, 2009Inventors: Herman De Kock, Tim Hugo Maria Jonckers, Paul Jozef Gabriel Maria Boonants, Stefaan Julien Last, Inge Dierynck, Judith Eva Baumeister, Gerben Albert Van ' T Klooster
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Publication number: 20090202920Abstract: The present invention provides an optical recording composition comprising at least one optical recording compound selected from the group consisting of cyanine compounds having specific structures and a holographic recording medium comprising a recording layer, wherein the recording layer comprises at least one optical recording compound selected from the group consisting of cyanine compounds having specific structures.Type: ApplicationFiled: February 10, 2009Publication date: August 13, 2009Applicant: FUJIFILM CorporationInventor: Hiroyuki SUZUKI
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Publication number: 20090203714Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: X is CH or N; and R4 is optionally substituted C3-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: August 13, 2009Applicant: Amura Therapeutics LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20090197927Abstract: The present invention relates to novel jasmonate derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for prevention and treatment of cancers.Type: ApplicationFiled: December 7, 2006Publication date: August 6, 2009Inventors: Max Herzberg, Adrian Harel, Christian Mang
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Patent number: 7569586Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4,R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: August 15, 2005Date of Patent: August 4, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, Yu-Hua Ji
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Publication number: 20090192170Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof (I), wherein: R3 is cyclopentyl or cyclohexyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: July 30, 2009Inventors: Martin Quibell, John Paul Watts
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Publication number: 20090186906Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, wherein: R3 is ten-butylmethyl, sec-butyl or tert-butyl; X is CH or N; and R4 is optionally substituted C1-8 alkyl or optionally substituted C3-8 cycloalkyl. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.Type: ApplicationFiled: January 8, 2009Publication date: July 23, 2009Inventors: Martin Quibell, John Paul Watts
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Publication number: 20090163485Abstract: The present invention relates to compounds of formula wherein Ar, Het, R1 and n are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. Compounds of formula I are orexin receptor antagonists and are useful in the treatment of sleep apnea, narcolepsy, insomnia, parasomnia, jet lag syndrome, circadian rhythms disorder and sleep disorders associated with neurological diseases.Type: ApplicationFiled: December 15, 2008Publication date: June 25, 2009Inventors: Henner Knust, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20090163517Abstract: This invention is concerned with compounds of the formula wherein X, A, B, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.Type: ApplicationFiled: February 23, 2009Publication date: June 25, 2009Inventors: Alfred Binggeli, Andreas Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
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Patent number: 7550469Abstract: The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: December 21, 2006Date of Patent: June 23, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: James A Hendrix, Joseph T Strupczewski, Kenneth Bordeau, Matthias Urmann, Gregory Shutske, Horst Hemmerle, John G Jurcak, Harpal Gill, Franz J Weiberth, Thaddeus Nieduzak, Sharon Anne Jackson, Xu-Yang Zhao, Paul Justin Mueller
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Publication number: 20090156640Abstract: A compound of the formula (I), (II), (III) or (IV) wherein Z, A, B, C, R, R1, R2, Q, and n are as described herein.Type: ApplicationFiled: February 23, 2009Publication date: June 18, 2009Inventors: Qun SUN, R. Richard Goehring, Donald Kyle, Zhengming Chen, Sam Victory, John Whitehead
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Patent number: 7544701Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: July 22, 2004Date of Patent: June 9, 2009Assignee: WyethInventors: Derek Cecil Cole, Ronald Charles Bernotas
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Publication number: 20090143353Abstract: A 1,6-?-glucan synthetase inhibitor is provided, having potent growth inhibition and having excellent safety. A compound is provided, capable of expressing in a wide spectral range and specifically or selectively, an antifungal effect based on its functional mechanism of 1,6-?-glucan synthesis inhibition. Also provided is a drug, especially an antifungal that contains the compound, its salt or their hydrate.Type: ApplicationFiled: August 16, 2006Publication date: June 4, 2009Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Katsuhiro Kawakami, Kazuo Kanai, Takao Horiuchi, Hiroshi Takeshita, Syozo Kobayashi, Yuichi Sugimoto, Issei Achiwa, Junichi Kuroyanagi
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Publication number: 20090130077Abstract: The invention relates to substituted benzothiazoles, benzoxazoles—and their counterparts having pyridine and pyrimidine rings replacing the benzene ring—that are PDE4 inhibitors useful for treating stroke, myocardial infarct, and cardiovascular inflammatory conditions, to pharmaceutical compositions comprising these compounds, and to methods for the treatment of stroke, myocardial infarct, and cardiovascular inflammatory conditions in a mammal. The compounds have general formula I: in which A and B are carbocycles or heterocycles.Type: ApplicationFiled: November 20, 2008Publication date: May 21, 2009Applicant: deCODE genetics ehfInventors: Jasbir Singh, Mark E. Gurney, Alex Burgin, Vincent Sandanayaka, Alexander Kiselyov, Munagala Rao
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Publication number: 20090124660Abstract: 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: ApplicationFiled: October 3, 2008Publication date: May 14, 2009Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Jie Fei Cheng, Mi Chen, Thomas Arrhenius, Mark E. Wilson, Gary D. Lopaschuk, Jason R. Dyck, Rossy Serafimov
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Publication number: 20090118272Abstract: A compound of Formula (I) an enantiomer, diastereomer or a pharmaceutically-acceptable salt thereof, wherein A is independently selected from: further wherein R1, R2, R3, R4, R5, R6, R7, and W are as described herein. Also disclosed is a compound of Formula (II) an enantiomer, diastereomer, or a pharmaceutically-acceptable salt thereof, wherein each of G, X and Y are independently CH or N, wherein at each occurrence at least one of G, X or Y is N and the other two of G, X or Y are CH; and B is independently selected from: further wherein R1, R2, R3, R4, R5, R8, R9 and Z are as described herein. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and Formula (II), and methods of treating conditions associated with the activity of p38 kinase.Type: ApplicationFiled: December 12, 2008Publication date: May 7, 2009Inventors: Chunjian Liu, Katerina Leftheris, James Lin
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Patent number: 7521445Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: March 5, 2007Date of Patent: April 21, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: James Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Joseph T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A. Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Francois Sabuco, Yulin Chiang, Nicola Collar
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Publication number: 20090093451Abstract: 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: ApplicationFiled: April 20, 2007Publication date: April 9, 2009Applicant: Smithkline Beecham CorporationInventor: Jakob Busch-Petersen
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Patent number: 7501418Abstract: The invention concerns fused heterocyclic isoxazoline derivatives of Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N-oxide form thereof, more in particular, tetrahydropyranoisoxazole, hexahydroisoxazolopyridine, tetrahydrothiopyrano isoxazole and hexahydrobenzoisoxazole derivatives fused to a heterocyclic ring system via the 6-membered ring of the bicyclic moiety as well as processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for treating depression, anxiety, movement disorders, psychosis, Parkinson's disease and body weight disorders including anorexia nervosa and bulimia, wherein the variables are defined as in Claim 1.Type: GrantFiled: August 13, 2003Date of Patent: March 10, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, José Manuel Bartolomé -Nebreda, Francisco Javier Fernández-Gadea, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Megens
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Publication number: 20090062259Abstract: The present invention relates to compounds according to formula (I), a process for preparing them, the intermediate compounds of the process and the use of the compounds in the manufacture of a medicament for use in treating diseases such as ARDS, pulmonary emphysema, bronchitis, bronchiectasis, COPD, asthma and rhinitis. The compounds are beta adrenoreceptor agonists.Type: ApplicationFiled: March 12, 2007Publication date: March 5, 2009Applicant: ASTRAZENECA ABInventors: Lilian Alcaraz, Andrew Lister, Garry Pairaudeau
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Publication number: 20090062261Abstract: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist. A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.Type: ApplicationFiled: February 21, 2007Publication date: March 5, 2009Applicant: SHIONOGI & CO., LTD.Inventors: Moriyasu Masui, Makoto Adachi, Hidenori Mikamiyama, Akira Matsumura, Naoki Tsuno
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Publication number: 20090054457Abstract: Disclosed are novel substituted heterocyclic derivatives having the structure of Formula I: The compounds are useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, diabetes, and myocardial infarction.Type: ApplicationFiled: October 27, 2008Publication date: February 26, 2009Inventors: Elfatih Elzein, Prabha Ibrahim, Venkata Palle, Kenneth Rehder, Jeffery Zablocki
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Publication number: 20090042854Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.Type: ApplicationFiled: January 19, 2007Publication date: February 12, 2009Inventors: Jianming Bao, Robert J. DeVita, Huagang Lu, Sander G. Mills, Gregori J. Morriello
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Publication number: 20090036444Abstract: The present invention relates to a fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.Type: ApplicationFiled: May 18, 2006Publication date: February 5, 2009Applicant: Japan Tobacco Inc.Inventors: Ryo Mizojiri, Shintaro Hirashima, Takahiro Oka, Kenta Aoki, Satoru Noji, Izuru Ando, Toshihiro Sato, Yasushi Niwa
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Publication number: 20090029986Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 29, 2007Publication date: January 29, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Publication number: 20090029977Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: ApplicationFiled: July 18, 2008Publication date: January 29, 2009Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20090030000Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: ApplicationFiled: May 1, 2008Publication date: January 29, 2009Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY. LTD.Inventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
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Patent number: 7476680Abstract: Compounds suitable for treating multidrug resistance and methods for their preparation and use are disclosed. The compounds are represented by the following formula: or an optical isomer, diastereomer, enantiomer or pharmaceutically acceptable salt thereof.Type: GrantFiled: June 22, 2006Date of Patent: January 13, 2009Assignee: H. Lee Moffitt Cancer Center & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Publication number: 20090012073Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: October 26, 2007Publication date: January 8, 2009Inventors: Clive Leslie BRANCH, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Patent number: 7470710Abstract: This invention relates to N-aroyl cyclic amine derivatives of formula (I), wherein X represents a bond, oxygen, NR3 or a group (CH2), wherein n represents 1, 2 or 3; Y represents CH2, CO, CH(OH), or CH2CH(OH); Het is an optionally substituted bicyclic heteroaryl group containing up to 4 heteroatoms selected from N, O and S; Ar2 represents an optionally substituted phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S and their use as pharmaceuticals, specifically as orexin receptor antagonists.Type: GrantFiled: June 25, 2002Date of Patent: December 30, 2008Assignee: SmithKline Beecham p.l.c.Inventors: Clive Leslie Branch, Wai Ngor Chan, Amanda Johns, Christopher Norbert Johnson, David John Nash, Riccardo Novelli, Jean-Pierre Pilleux, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Geoffrey Stemp
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Publication number: 20080312222Abstract: The present invention relates to new 4-benzylidene-piperidin derivatives of formula (I), useful as NMDA, in a particular NR2B subunit containing receptor antagonists and analgesica.Type: ApplicationFiled: July 21, 2005Publication date: December 18, 2008Inventors: Istvan Borza, Csilla Horvath, Sandor Farkas, Istvan Gyertyan, Jozsef Nagy, Sandor Kolok, Kornel Galgoczy, Katalin Saghy
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Patent number: 7462717Abstract: The invention concerns substituted tricyclic isoxazoline derivatives, more in particular tricyclic dihydrobenzopyranoisoxazoline, dihydroquinolinoisoxazoline, dihydronaphthalenoisoxazoline and dihydrobenzothiopyranoisoxazoline derivatives substituted on at least one of the C6- and C9-positions of the phenylpart of the tricyclic moiety with a selected radical, according to Formula (I) wherein X=CH2, N—R7, S or O, R1, R2, R14 and R15 are certain specific substituents, with the proviso that at least one of R14 and R15 is not hydrogen, Pir is preferably an optionally substituted piperidinyl or piperazinyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S; a process for their preparation, pharmaceutical compositions comprising themType: GrantFiled: August 19, 2003Date of Patent: December 9, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: José Ignacio Andrés-Gil, Manuel Jesús Alcázar-Vaca, Maria Encarnacion Matesanz-Ballesteros, Margaretha Henrica Maria Bakker, Antonius Adrianus Hendrikus Petrus Megens
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Publication number: 20080300275Abstract: The present invention provides compounds of formula (I) wherein e, R1, R2, R3, R4, R5, R4, R5, R6, R7, R7a, R7b, A, D, m and n are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 3, 2006Publication date: December 4, 2008Applicant: ASTRAZENECA ABInventors: Roger Bonnert, Alice Flaherty, Garry Pairaudeau, Michael Stocks
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Patent number: 7449482Abstract: 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: GrantFiled: July 28, 2004Date of Patent: November 11, 2008Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Jie Fei Cheng, Mi Chen, Thomas Arrhenius, Mark E. Wilson, Gary D. Lopaschuk, Jason R. Dyck, Rossy Serafimov
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Publication number: 20080255194Abstract: This invention relates to novel 1,2-benzisoxazol-3-yl compounds, their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an antagonist of both dopamine and serotonin receptors.Type: ApplicationFiled: April 14, 2008Publication date: October 16, 2008Applicant: CONCERT PHARMACEUTICALS INC.Inventor: Scott L. Harbeson
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Patent number: 7435744Abstract: The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more: (a) hydrogen atoms; (b) carbon atoms; (c) —CH? groups; (d) —CH2— groups; or (e) additional heteroatoms of the same or different type; or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C1-C4 alkyl, ?S or —SH groups; W: is —CO—, —CH2— or —CH2—(C1-C4 alkyl)-; X: is —CO—; Y: is —O—, C1-C4 alkylene, C1-C4 alkynylene, cycloalkylene, aminocarbonyl, —NH—, —N(C1-C4 alkyl)-, -C1-C4 alkylene-N(C1-C4 alkyl)-, —CH2O—, —CH(OH)— or —OCH2—; Z: is hydrogen, halogen, nitro, amino, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluoromethType: GrantFiled: January 21, 2004Date of Patent: October 14, 2008Assignee: Gedeon Richter Vegyeszeti Gyar RTInventors: Gyorgy Domány, Csilla Horváth, Gizella Bartáné Szalai, József Nagy, Sándor Kolok, Éva Kovácsné Bozó, István Borza, István Vágó, Attila Bielik, Györgyi Ignáczné Szendrei, György Keserü, Sándor Farkas
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Publication number: 20080214539Abstract: The invention includes benzisoxazole piperidine compositions and methods of using them for modulating sleep.Type: ApplicationFiled: April 26, 2006Publication date: September 4, 2008Inventors: Daniel Coughlin, James F. White, Kazumi Shiosaki, David G. Hangauer, Michael Solomon, Dale M. Edgar
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Patent number: 7419986Abstract: Compounds of the Formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as premenstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa and bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: August 31, 2006Date of Patent: September 2, 2008Assignee: WyethInventors: Dahui Zhou, Gary Paul Stack
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Publication number: 20080207690Abstract: This invention relates to compounds of the formula (I): wherein A, B, R1, R4, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.Type: ApplicationFiled: February 15, 2006Publication date: August 28, 2008Inventors: Hirohide Noguchi, Isao Sakurada, Chikara Uchida, Nobuaki Waizumi
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Patent number: 7408067Abstract: Compounds comprising an aza-cyclic portion and an aromatic portion linked via a sulphur atom are disclosed. The compounds disclosed are selective modulators of beta 4 subtype nicotinic acetylcholine receptors and are useful for the treatment of dysfunctions of the central and autonomic nervous systems.Type: GrantFiled: July 29, 2002Date of Patent: August 5, 2008Assignee: Merck + Co., Inc.Inventors: Peter Charles Astles, Stephen Richard Baker, Celine Bonnefous, Jean Michel Vernier, Martine Keenan, Adam Jan Sanderson
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Publication number: 20080176900Abstract: Taught are derivatives of 5H-thioeno(3,4-c)pyrrole-4,6-dione, their organic, and inorganic salts, methods of synthesis of these derivatives, and their application as active pharmaceutical-ingredients useful as inhibitors of TNF?, the derivative being represented by the general formula (I): in which R1 represents H, C1-6alkyl, OR4, OC(O)R5, NO2, NHC(O)R6, or NR7R8; R2 represents H, a halogen, or C1-6alkyl; R3 represents H, methyl, isopropyl, allyl, benzyl, CH2CO2(C1-6alkyl), or CH2(CH2)nR9; R4, R5, R6, R7, and R8 each independently and at each occurrence represents H, or C1-6alkyl; R9 represents H, C1-6alkyl, OH, OC1-6alkyl, NH2, NHC1-6alkyl, N(C1-6alkyl)2, or CO2(C1-6alkyl); and n represents 1, 2, 3, or 4.Type: ApplicationFiled: March 20, 2008Publication date: July 24, 2008Inventor: Hesheng ZHANG