Additional Hetero Ring Containing Patents (Class 546/135)
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Patent number: 7355046Abstract: This invention provides biphenyl derivatives of formula I: wherein R1, R2, R3, R4, R5, R6, R7, W, a, b and c are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The biphenyl derivatives of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity and therefore, such biphenyl derivatives are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.Type: GrantFiled: June 7, 2006Date of Patent: April 8, 2008Assignee: Theravance, Inc.Inventors: Mathai Mammen, Adam Hughes, Yan Chen
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Patent number: 7345058Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.Type: GrantFiled: March 31, 2006Date of Patent: March 18, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Paul Gillespie, Robert Alan Goodnow, Jr., Qiang Zhang
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Patent number: 7326786Abstract: Thiazolinone quinoline derivatives having no substitution on the quinoline ring active as CDK1 inhibitors which are useful as anti-proliferation agents such as for treating solid tumors.Type: GrantFiled: June 29, 2005Date of Patent: February 5, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Shaoqing Chen
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Patent number: 7312231Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: March 31, 2003Date of Patent: December 25, 2007Assignee: Almirall Prodesfarma AGInventors: Maria Antonia Buil Albero, Dolors Fernandez Forner, Maria Prat Quiñones
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Patent number: 7312335Abstract: One aspect of the present invention relates to quinine-based and quinidine-based catalysts. Another aspect of the invention relates to a method of preparing a derivatized quinine-based or quinidine-based catalyst comprising 1) reacting quinine or quinidine with base and a compound that has a suitable leaving group, and 2) converting the ring methoxy group to a hydroxy group. Another aspect of the present invention relates to a method of preparing a chiral, non-racemic compound from a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone, comprising the step of: reacting a prochiral electron-deficient alkene or azo compound or prochiral aldehyde or prochiral ketone with a nucleophile in the presence of a catalyst; thereby producing a chiral, non-racemic compound; wherein said catalyst is a derivatized quinine or quinidine.Type: GrantFiled: May 27, 2005Date of Patent: December 25, 2007Assignee: Brandeis UniversityInventors: Li Deng, Hongming Li
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Patent number: 7253285Abstract: Thiazolinone monosubstituted quinoline derivatives where the quinoline ring is mono-substituted at the 4 positions which derivatives demonstrates CDK1 antiproliferative activity and are useful as anti-cancer agents.Type: GrantFiled: August 29, 2005Date of Patent: August 7, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Li Chen, Shaoqing Chen, Jianping Lou, Achyutharao Sidduri
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Patent number: 7250515Abstract: Thiazolinone disubstituted quinoline derivatives where the quinoline ring is disubstituted at the 3, 4 positions which derivatives demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents.Type: GrantFiled: June 29, 2005Date of Patent: July 31, 2007Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Shaoqing Chen, Christophe Michoud
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Patent number: 7241773Abstract: Compounds of formula: or pharmaceutically acceptable salts, esters, amides, or prodrugs thereof, wherein: A and G are each independently N or N+—O?; m and n are each independently 0, 1, or 2; X1 and X3 are each independently O, S, and —N(R1)—; X2 is O, S, —N(R1)—, —N(Ar2)—and —N(R2)C(O)—; Ar1 is a six-membered aromatic ring; Ar2 is cyclohexyl or a mono- or bicyclic aromatic ring, and R13 is hydrogen, alkyl, or halogen, as defined herein. The compounds are useful in treating conditions or disorders prevented by or ameliorated by nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formulas (I) and (II) and methods for using such compounds and compositions.Type: GrantFiled: December 17, 2004Date of Patent: July 10, 2007Assignee: Abbott LaboratoriesInventors: Jianguo Ji, Tao Li
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Patent number: 7205318Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 16, 2004Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Tammy C. Wang, Gren Z. Wang, Timur Gungor
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Patent number: 7179818Abstract: This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: GrantFiled: October 14, 2003Date of Patent: February 20, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Robert E. Boyd, Allen B. Reitz
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Patent number: 7176217Abstract: An azabicyclo compound (I) or a salt thereof in accordance with the present invention has an excellent inhibiting action on matrix metalloproteases (MMPs) activity, and is useful for pharmaceutical, cosmetic and skin external compositions. wherein R is H, alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl, acyl, COOR1, carbamoyl or SO2R2 (wherein R1 and R2 each are alkyl, heteroalkyl, aryl, heteroaryl, arylalkyl or heteroarylalkyl); X is methylene, ethylene or propylene; and is a single bond or a double bond.Type: GrantFiled: November 13, 2002Date of Patent: February 13, 2007Assignee: Shiseido Co., Ltd.Inventors: Takuya Hiruma, Koji Kobayashi, Shinji Inomata
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Patent number: 7132432Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables L, Z0, R1, R4, R5, and R11 are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: June 2, 2004Date of Patent: November 7, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Jingwu Duan, Chu-Biao Xue, James Sheppeck, Bin Jiang, Lihua Chen
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Patent number: 7129261Abstract: The present invention provides analogues of duocarmycins that are potent cytotoxins. Also provided are peptidyl and disulfide linkers that are cleaved in vivo. The linkers are of use in forming prodrugs and conjugates of the cytotoxins of the invention as well as other diagnostic and therapeutic moieties. The invention provides prodrugs and conjugates of the duocarmycin analogues with the linker arms of the invention.Type: GrantFiled: May 31, 2002Date of Patent: October 31, 2006Assignee: Medarex, Inc.Inventors: Howard P. Ng, Danny P.C. McGee, Oliver L. Saunders, Valeri Martichonok, Guoxian Wu, Zhihong Li, Geoffrey T. Yarranton
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Patent number: 7115629Abstract: The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1–C4)-alkylthio, (C1–C4)-alkoxyl, (C1–C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1–C4)alkyl and (C1–C4)alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quaternary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.Type: GrantFiled: June 23, 2004Date of Patent: October 3, 2006Assignee: Laboratorios S.A.L.V.A.T., S.A.Inventors: Carles Farrerons Gallemi, Juan Lorenzo Catena Ruiz, Anna Fernandez Serrat, Ignacio José Miquel Bono, Dolors Balsa Lopez, José Ignacio Bonilla Navarro, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andrés Fernandez Garcia
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Patent number: 7115654Abstract: The invention provides compounds of Formula I and derivatives thereof, pharmaceutical compositions comprising a compound of Formula I, and methods of treatment utilizing such compounds and compositions: wherein: R1 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; L is a linker; R2 is chosen from optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, and optionally substituted heteroaralkyl; and or single stereoisomers, mixtures of stereoisomers, or the pharmaceutically acceptable salts, amides, or esters thereof.Type: GrantFiled: June 5, 2003Date of Patent: October 3, 2006Assignee: Sunesis Pharmaceuticals, Inc.Inventors: Darin Allen, Bruce Fahr, Johan Oslob, Brian C. Raimundo, Michael J. Romanowski
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Patent number: 7105538Abstract: Substituted 2-pyrrolidin-2-yl compounds corresponding to formula I a method for their production, pharmaceutical compositions containing them, and methods of using them, especially for treating pain and/or depression.Type: GrantFiled: February 28, 2005Date of Patent: September 12, 2006Assignee: Gruenenthal GmbHInventors: Hagen-Heinrich Hennies, Corinna Sundermann, Helmut Buschmann, Bernd Sundermann
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Patent number: 7091217Abstract: Compounds which modulate chemokine receptor activities are disclosed. These compounds are preferably tertiary amines comprising tetrahydroquinoline and benzimidazole.Type: GrantFiled: March 11, 2004Date of Patent: August 15, 2006Assignee: AnorMED, Inc.Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosaria Di Fluri
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Patent number: 7041685Abstract: The present invention is directed to substituted 3-aryl-5-aryl-[1,2,4]-oxadiazoles and analogs thereof, represented by the Formula I: wherein Ar1, Ar3, A, B and D are defined herein. The present invention also relates to the discovery that compounds having Formula I are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: June 10, 2002Date of Patent: May 9, 2006Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, John A. Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Jared Daniel Kuemmerle, Kristin P. Ollis
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Patent number: 7041693Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein L, Z0, R1, R4, R5, and R11 are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.Type: GrantFiled: October 2, 2003Date of Patent: May 9, 2006Assignee: Bristol-Myers Squibb CompanyInventor: James Sheppeck
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Patent number: 7022259Abstract: A liquid crystal compound with high helical twisting power, a method for preparing the same, and a liquid crystal composition containing the same. The liquid crystal compounds include cyclic group chain structures similar to the liquid crystal to serve as the core structure, and multi-ring structures of natural alcohol with optical activity, such as alcoholates of terpenol, borneol, cinchonidine, quinine, or derivatives thereof. As a result, the liquid crystal composition containing the liquid crystal compounds can filter out light of specific wavelengths from incident light due to optical activity and high helical twisting power thereof.Type: GrantFiled: September 30, 2003Date of Patent: April 4, 2006Assignee: Industrial Technology Research InstituteInventors: Dao-Hung Lee, Ding-Jen Chen, Kung-Lung Cheng
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Patent number: 7001900Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1–2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 21, 2006Assignee: Pfizer Inc.Inventors: Eric Jon Jacobsen, Jason K. Myers, Daniel Patrick Walker, Donn G. Wishka, Steven Charles Reitz, David W. Piotrowski, Brad A. Acker, Vincent E. Groppi, Jr.
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Patent number: 6984648Abstract: The present application describes novel cyclic ?-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa, and S(O)p, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease and/or as TNF-? inhibitors.Type: GrantFiled: February 13, 2004Date of Patent: January 10, 2006Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Zhonghui Lu, Thomas P. Maduskuie, Jr., Matthew E. Voss, Chu-Biao Xue, Jingwu Duan, Gregory Ott, Lihua Chen, Carl Decicco
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Patent number: 6958348Abstract: Disclosed is an anti-cancer compound represented by Structural Formula (I): The variables in Structural Formula (I) are described hereinbelow. Also disclosed is a pharmaceutical composition comprising a pharmaceutically acceptable carrier or diluent and a compound represented by Structural Formula (I) (preferably an effective amount). Also disclosed is a method of treating a subject with cancer by administering to the subject an effective amount of a compound represented by Structural Formula (I).Type: GrantFiled: August 29, 2002Date of Patent: October 25, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Mitsunori Ono, Guiqing Liang, David James, Hao Li, Zhi-Qiang Xia
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Patent number: 6953855Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.Type: GrantFiled: February 21, 2003Date of Patent: October 11, 2005Assignee: Targacept, Inc.Inventors: Anatoly A. Mazurov, Jozef Klucik, Lan Miao, Angela S. Seamans, Teresa Youngpeter Phillips, Jeffrey Daniel Schmitt, Craig Harrison Miller
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Patent number: 6927293Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: GrantFiled: August 26, 2002Date of Patent: August 9, 2005Assignee: Merck & Co., Inc.Inventors: Yuntae Kim, Barbara Hanney, Keith L. Spencer, George D. Hartman, Kenneth L. Arrington
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Patent number: 6916828Abstract: The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1-C4)-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1-C4)-alkyl and (C1-C4)-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quatemary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.Type: GrantFiled: June 25, 2001Date of Patent: July 12, 2005Assignee: Laboratorios S.A.L.V.A.T., S.A.Inventors: Carles Farrerons Gallemi, Juan Lorenzo Catena Ruiz, Anna Fernandez Serrat, Ignacio José Miquel Bono, Dolors Balsa Lopez, José Ignacio Bonilla Navarro, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andrés Fernandez Garcia
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Patent number: 6884807Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: November 28, 2001Date of Patent: April 26, 2005Assignee: Neurosearch, A/SInventors: Dan Peters, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Philip K. Ahring, Tino Dyhring Jørgensen
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Patent number: 6864265Abstract: Compounds that bind to chemokine receptors such as CXCR4 and CCR5 demonstrate protective effects against infection of cells by human immunodeficiency virus are disclosed. These compounds contain a tertiary amine[[s]] linked to a core nitrogen via an aromatic or heteroaromatic moiety.Type: GrantFiled: September 17, 2001Date of Patent: March 8, 2005Assignee: AnorMED, Inc.Inventors: Gary Bridger, Renato Skerlj, Al Kaller, Curtis Harwig, David Bogucki, Trevor R. Wilson, Jason Crawford, Ernest J. Mceachern, Bern Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis, Rosaria Maria Di Fluri
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Patent number: 6858613Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.Type: GrantFiled: February 14, 2003Date of Patent: February 22, 2005Assignee: Pfizer Inc.Inventors: Bruce N. Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka, Vincent E. Groppi, Jr.
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Publication number: 20040266816Abstract: A compound which is a carbamate of formula: 1Type: ApplicationFiled: July 10, 2002Publication date: December 30, 2004Inventors: Maria Antonia Buil Albero, Maria Dolors Fernandez Forner, Maria Prat Quinones
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Publication number: 20040242629Abstract: A compound which is a carbamate of formula: 1Type: ApplicationFiled: March 31, 2003Publication date: December 2, 2004Inventors: Maria Antonia Buil Albero, Dolors Fernandez Forner, Maria Prat Quinones
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Patent number: 6825181Abstract: Aminoisoquinoline derivatives of the following formulae or analogs thereof and pharmaceutically acceptable salts thereof are provided. These compounds have an excellent effect of inhibiting activated blood-coagulation factor X, and they are useful as anticoagulants or agents for preventing or treating thrombi or emboli.Type: GrantFiled: September 19, 2000Date of Patent: November 30, 2004Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Shingo Makino, Kazuyuki Sagi, Masaru Takayanagi, Takashi Kayahara, Shunji Takehana
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Patent number: 6821962Abstract: This invention is directed to quinoline/quinoxaline compounds which inhibit platelet-derived growth factor or p56lck tyrosine kinase activity, to pharmaceutical compositions comprising these compounds, and to the use of these compounds for treating a patient suffering from or subject to disorders/conditions involving cellular differentiation, proliferation, extracellular matrix production or mediator release and/or T cell activation and proliferation.Type: GrantFiled: February 6, 2003Date of Patent: November 23, 2004Assignee: Aventis Pharmaceuticals Inc.Inventors: Michael R. Myers, Wei He, Alfred P. Spada, Martin P. Maguire
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Publication number: 20040230057Abstract: An optical recording medium dye has the following structure (1): 1Type: ApplicationFiled: April 7, 2004Publication date: November 18, 2004Inventors: Chao-Nan Kuo, Sung-Kuei Chiang
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Publication number: 20040224977Abstract: The invention provides compounds of Formula I: 1Type: ApplicationFiled: June 10, 2004Publication date: November 11, 2004Inventors: Daniel Patrick Walker, Donn G. Wishka, Jeffrey W. Corbett, Mark R. Rauckhorst, David W. Piotrowski, Vincent E. Groppi
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Patent number: 6815451Abstract: The invention relates to novel 1,2,3,4-tetrahydroisoquinoline derivatives of formula (I) and related compounds and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as neurohormonal antagonists especially urotensin II antagonists.Type: GrantFiled: September 15, 2003Date of Patent: November 9, 2004Assignee: Actelion Pharmaceuticals Ltd.Inventors: Jörg Velker, Hamed Aissaoui, Christoph Binkert, Martine Clozel, Boris Mathys, Claus Mueller, Oliver Nayler, Michael Scherz, Thomas Weller
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Publication number: 20040220214Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.1]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.Type: ApplicationFiled: June 4, 2003Publication date: November 4, 2004Applicant: Targacept, Inc.Inventors: Merouane Bencherif, Craig Harrison Miller, Gregory D. Hawkins, Balwinder S. Bhatti
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Publication number: 20040157878Abstract: Radiolabeled ligands useful as probes for determining the relative abundance, receptor occupancy, and/or function of nicotinic acetylcholine receptors. The compounds of Formula I as described herein are labeled with a radioactive isotopic moiety such as 11C, 18F, 76Br, 123I or 125I. Disorders are diagnosed by administering to a mammal a detectably labeled compound and detecting the binding of that compound to the nAChR. The compounds that have been administered are detected using methods including, but not limited to, position emission topography and single-photon emission computed tomography. The present invention is useful in diagnosing a wide variety of diseases and disorders as discussed herein.Type: ApplicationFiled: December 5, 2003Publication date: August 12, 2004Inventors: Bruce Nelson Rogers, David W. Piotrowski, Vincent Edward Groppi, Eric Jon Jacobsen, Jason Kenneth Myers, Daniel Patrick Walker, Donn Gregory Wishka, Marc Bradley Skaddan
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Publication number: 20040147522Abstract: The invention discloses compounds that are selective &agr;7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.Type: ApplicationFiled: October 31, 2003Publication date: July 29, 2004Inventors: Erik Ho Fong Wong, Luz A. Cortes-Burgos, Bruce Nelson Rogers, David W. Piotrowski, Daniel Patrick Walker, Eric Jon Jacobsen, Brad A. Acker, Donn G. Wishka
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Publication number: 20040138253Abstract: The invention features quaternary ammonium compounds of formula I, described herein, and their use in treating asthma, chronic obstructive pulmonary disorder, allergic rhinitis, and infectious rhinitis.Type: ApplicationFiled: October 17, 2003Publication date: July 15, 2004Inventor: John Gregory Slatter
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Patent number: 6762200Abstract: The present invention provides medicinal compositions characterized by containing as the active ingredient either a compound represented by a general formula (1) or a pharmaceutically acceptable composite thereof, [wherein X represents oxygen or sulfur; R1 represents hydrogen, C1-4 alkyl, etc.; R2 represents, e.g., phenyl optionally substituted by A1; R3 represents, e.g., hydrogen, C1-4 alkyl optionally substituted by A2, or a group represented by either one of the following formulae; R represents oxygen, sulfur, or a group represented by a formula (N—G)], in particular, inhibitors of phospholipase A(2) activity; use of the compositions; and compounds represented by a general formula (1—1); wherein X, R1, R2, R3 and G1 are the same as defined in the description.Type: GrantFiled: September 25, 2002Date of Patent: July 13, 2004Assignee: Nippon Soda Co. Ltd.Inventors: Masae Takagi, Keiichi Ishimitsu, Tadayuki Nishibe
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Publication number: 20040132768Abstract: A compound according to formula (I) 1Type: ApplicationFiled: December 17, 2003Publication date: July 8, 2004Inventors: Maria Dolors Fernandez Forner, Maria Prat Quinones, Maria Antonia Buil Albero
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Patent number: 6756384Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.Type: GrantFiled: July 23, 2002Date of Patent: June 29, 2004Assignees: Novo Nordisk A/S, Boehringer Ingelheim International GmbHInventors: Knud Erik Andersen, Florencio Zaragoza Dorwald, Bernd Peschke, Ulla Grove Sidelmann, Klaus Rudolf, Dirk Stenkamp, Rudolf Hurnaus, Stephan Georg Muller, Bernd Krist, Birgitte Eriksen
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Patent number: 6750226Abstract: A compound according to formula (I) wherein: is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; which shows high affinity for muscarinic M3 receptors (Hm3).Type: GrantFiled: January 14, 2002Date of Patent: June 15, 2004Assignee: Almirall-Prodesfarma, S.A.Inventors: Dolors Fernandez Forner, Maria Prat Quiñones, Maria Antonia Buil Albero
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Publication number: 20040110789Abstract: This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: ApplicationFiled: October 14, 2003Publication date: June 10, 2004Inventors: Robert E. Boyd, Allen B. Reitz
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Publication number: 20040110229Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: ApplicationFiled: April 29, 2003Publication date: June 10, 2004Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Patent number: 6730418Abstract: Quinoline derivatives represented by formula (1) wherein two or more of substituents R1 to R7 are each a group of formula (2). In general formula (2), Q is a carbo- or hetero-aryl group; and the number (n) of double bonds is preferably 1 to 3. Use of such derivatives in an organic EL device provided with a layer of an organic compound and two electrodes sandwiching the layer as the organic compound gives devices emitting yellow to red light with high brightness and high efficiency. Further, doping a hole transport layer with such derivatives realizes organic EL devices capable of emitting lights of resultant colors (e.g., white) composed of lights from light-emitting and hole transport layers.Type: GrantFiled: June 13, 2002Date of Patent: May 4, 2004Assignee: Kabushiki Kaisha Toyota Chuo KenkyushoInventors: Makoto Mouri, Hisato Takeuchi, Hiromitsu Tanaka, Tomohiko Mori, Masahiko Ishii, Koji Noda, Shizuo Tokito
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Publication number: 20040063950Abstract: The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1-C4)-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1-C4)-alkyl and (C1-C4)-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quatemary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.Type: ApplicationFiled: July 28, 2003Publication date: April 1, 2004Inventors: Carles Farrerons Gallemi, Juan Lorenzo Catena Ruiz, Anna Fernandez Serrat, Ignacio Jose Miquel Bono, Dolors Balsa Lopez, Jose Ignacio Bonilla Navarro, Carmen Lagunas Arnal, Carolina Salcedo Roca, Andres Fernandez Garcia
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Publication number: 20040044026Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters.Type: ApplicationFiled: May 9, 2003Publication date: March 4, 2004Inventors: Dan Peters, Gunnar M. Olsen, Elsebet Ostergaard Nielsen, Philip K. Ahring, Tino Dyhring Jorgensen
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Patent number: RE39265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 9, 2000Date of Patent: September 5, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley