Quinolines (including Hydrogenated) Patents (Class 514/253.06)
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Patent number: 7074796Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6Type: GrantFiled: June 27, 2002Date of Patent: July 11, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Patent number: 7071192Abstract: The present invention concerns compounds of formula (I), prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof wherein -a1=a2-a3=a4-represents a radical of formula —CH?CH—CH?CH—; —N—CH—CH?CH—; —CH?N—CH?CH—; —CH?CH—N?CH—; —CH?CH—CH?N—; wherein each hydrogen atom may optionally be substituted; Q is a radical of formulae (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), wherein Alk is C1-6alkanediyl; Y1 is a bivalent radical of formula —NR2— or —CH(NR2R4)—; X1 is NR4, S, S(?O), S(?O)2, O, CH2, C(?O), CH(?CH2), CH(OH), CH(CH3), CH(OCH3), CH(SCH3), CH(NR5aR5b), CH2—NR4 or NR4—CH2; X2 is a direct bond, CH2, C(?O), NR4, C1-4alkyl-NR4, NR4—C1-4alkyl, t is 2 to 5; u is 1 to 5; v is 2 or 3; and whereby each hydrogen in Alk and in (b-3), (b-4), (b-5), (b-6), (b-7) and (b-8), may optionally be replaced by R3: provided that when R3 is hydroxy or C1-6alkyloxy, then R3 cannot replace a hydrogen atom in the a position relative to a nitrogen atom; G is a diType: GrantFiled: June 20, 2000Date of Patent: July 4, 2006Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Jean Fernand Armand Lacrampe, Jérôme Emile Georges Guillemont, Marc Gaston Venet, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7067513Abstract: The invention relates to a novel group of phenylpiperazines having interesting pharmacological properties such as a high affinity for the dopamine D2 receptor and/or the serotonin reuptake site, and the ability to treat conditions related to disturbances in the dopaminergic and/or the serotonergic systems such as aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition, disturbances of memory, Parkinson's disease, schizophrenia, and psychotic disorders. The invention relates to a group of novel phenylpiperazine derivatives of the formula (I): wherein: X is a group of formula 1, 2, 3, 4, 5, 6, or 7 as defined in the text, m has the value 2 to 6; n has the value 0–2; R5 and R6 are independently H or alkyl (1–3C); or R5+R6 represent a group —(CH2)—p wherein p has the value 3–5, and R7 is alkyl (1–3C), alkoxy (1–3C), halogen or cyano; or R6+R7 (R7 at position 7 of the indole group) represent a group —(CH2)q wherein q has the value 2–4, and salts thereof.Type: GrantFiled: August 22, 2000Date of Patent: June 27, 2006Assignee: Solvay Pharmaceuticals B.V.Inventors: Roelof Van Hes, Johannes A. M. Van der Heijden, Cornelis G Kruse, Jacobus Tipker, Martinus T. M Tulp, Gerben M Visser, Bernard J Van Vliet
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Patent number: 7056923Abstract: Compounds of the following formula: where m, n, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: December 9, 2003Date of Patent: June 6, 2006Assignee: Schering AktiengesellschaftInventors: Judi Bryant, Brad Buckman, Imadul Islam, Raju Mohan, Michael Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 7041664Abstract: Disclosed are compounds of the formula: or pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, wherein R1, R2, R3, X, Q1 and Q2 are defined herein, which compounds are ligands for neurokinin receptors, in particular NK-3 receptors, and are therefor useful in the treatment of a wide range of diseases or disorders including, but not limited to depression, anxiety, psychosis, obesity, pain, Parkinson's disease, Alzheimer's disease, neurodegenerative diseases, movement disorders, respiratory diseases, inflammatory diseases, neuropathy, immune disorders, migraine, biliary disfunction, and dermatitis.Type: GrantFiled: June 14, 2004Date of Patent: May 9, 2006Assignee: Neurogen CorporationInventors: Jun Yuan, George Maynard, Alan Hutchison
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Patent number: 7037913Abstract: This invention provides compounds of Formula I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.Type: GrantFiled: March 20, 2003Date of Patent: May 2, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Owen B. Wallace, Nicholas A. Meanwell, John F. Kadow, Zhongxing Zhang, Zhong Yang
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Patent number: 7026314Abstract: Provided herein is a compound of the formula (I) wherein said compound is useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating, disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B antagonists. Also provided herein are processes for making compounds of Formula (I) and intermediate compounds.Type: GrantFiled: January 15, 2002Date of Patent: April 11, 2006Assignee: AstraZeneca ABInventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Patent number: 7009051Abstract: The present invention relates to compounds of the formula I wherein R1, R2, R3, X and Y are defined as in the specification. Those compounds are 5HT7 partial agonists and are useful in the treatment of several disorders of the central nervous system.Type: GrantFiled: July 10, 2003Date of Patent: March 7, 2006Assignee: Pfizer IncInventors: Willard M. Welch, Vinod Parikh
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Patent number: 6995156Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: September 22, 2004Date of Patent: February 7, 2006Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 6960580Abstract: The present invention relates to nitrogen-containing heterocyclic quinoline compounds and pharmaceutically acceptable salts thereof which have inhibitory activity on the phosphorylation of kinases, which inhibits the activity of such kinases. The invention is also related to a method of inhibiting kinases and treating disease states in a mammal by inhibiting the phosphorylation of kinases. More particularly, the present invention provides nitrogen-containing heterocyclic compounds and pharmaceutically acceptable salts thereof which inhibit phosphorylation of a PDGF receptor to hinder abnormal cell growth and cell wandering, and a method for preventing or treating cell-proliferative diseases such as arteriosclerosis, vascular reobstruction, cancer and glomerulosclerosis.Type: GrantFiled: March 8, 2002Date of Patent: November 1, 2005Assignee: Millennium Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Anjali Pandey
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Patent number: 6953801Abstract: Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: May 21, 2002Date of Patent: October 11, 2005Assignee: Neurogen CorporationInventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
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Patent number: 6949552Abstract: There are provided a therapeutic preparation for anxiety neurosis or depression which comprises a MC4 receptor antagonist as an effective ingredient; and a piperazine derivative represented by Formula [1]: [wherein Ar1 is a phenyl group, a substituted phenyl group, a naphthyl group or a substituted naphthyl group; Ar2 is a naphthyl group, a substituted naphthyl group, a quinolyl group, a group represented by the formula: (wherein R4 is a hydrogen atom or a halogen atom; and X—Y is CH—NH, CH—O, CH—S or N—O) or a group represented by the formula: (wherein R5 is a hydrogen atom, a hydroxyl group or a C1-10 alkoxy group); R1 is a hydrogen atom, a C1-10 alkyl group, a C3-8 cycloalkyl group, a C3-10 alkenyl group, a phenyl group, a 1-cyanoethyl group, a pyrimidin-2-yl group or an amidyl group; R2 and R3 are the same or different, and are each a hydrogen atom or a C1-10 alkyl group; A-B is N—CH2, CH—CH2, C(OH)—CH2 or C?CH; T1 is a single bond, —N(R6)— (wherein R6 is a hydrogen atom or a C1-10 alkyl groupType: GrantFiled: June 27, 2001Date of Patent: September 27, 2005Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Atsuro Nakazato, Shigeyuki Chaki, Taketoshi Okubo, Shin-ichi Ogawa, Takaaki Ishii
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Patent number: 6936611Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: January 12, 2004Date of Patent: August 30, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson, Peter Robert Guzzo, Michael John Mayer
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Patent number: 6916812Abstract: Novel piperazine and homopiperazine derivatives are agonists of melanocortin receptor(s) and are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of the melanocortin receptors. The compounds of the present invention are therefore useful for treatment or prevention of diseases and disorders such as obesity, diabetes, and sexual dysfunction.Type: GrantFiled: October 4, 2002Date of Patent: July 12, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Graham S. Poindexter, Guanglin Luo, Ling Chen
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Patent number: 6911442Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt and/or N-oxide thereof: corresponding novel medicaments, pharmaceutical compositions and/or methods ofType: GrantFiled: June 13, 2000Date of Patent: June 28, 2005Assignee: SmithKline Beecham p.l.c.Inventors: David Thomas Davies, Roger Edward Markwell, Neil David Pearson, Andrew Kenneth Takle
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Patent number: 6903103Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): wherein: X represents carbonyl, sulphonyl or sulphoxide, G1, G2 and G3 are as defined in the description, T represents a fused phenyl group or a fused pyridyl group, R1 represents hydrogen, linear or branched (C1-C6)alkyl, aryl or aryl-(C1-C6)alkyl in which the alkyl moiety is linear or branched, R2a and R2b, which are the same or different, are as defined in the description, R3 represents aryl or heteroaryl-A as defined in the description, each of which groups may optionally be substituted, Y represents aryloxy, heteroaryloxy or heteroaryl-B as defined in the description, each of which groups may optionally be substituted, its isomers, its hydrates, its solvates and addition salts thereof with a pharmaceutically aType: GrantFiled: February 20, 2003Date of Patent: June 7, 2005Assignee: Les Laboratories ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6890926Abstract: The invention relates to novel quinoline derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for treating tumors.Type: GrantFiled: July 20, 2001Date of Patent: May 10, 2005Assignee: Zentaris AGInventors: Peter Emig, Eckhard Günther, Jürgen Schmidt, Bernd Nickel, Bernhard Kutscher
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Patent number: 6872723Abstract: An antibacterial formulation suitable for injection into animals containing approximately 2-10% w/v difloxacin HCl, L-arginine base, propylene glycol, ethanol and/or benzyl alcohol, and water. The formulation is a solution having a pH of form 9 to 10. The formulation produces little or no tissue damage or irritation at the injection site.Type: GrantFiled: January 17, 2003Date of Patent: March 29, 2005Assignee: WyethInventor: Henderik W. Frijlink
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Patent number: 6861432Abstract: This invention relates to new piperazine derivatives of general formula I, in which V, W, n, R, R?, i, j, Y and Z have the meaning that is indicated in the description. The compounds according to the invention are distinguished by a diazacycloalkane substituent. They have at their disposal a special action with respect to the action that destabilizes the androgen receptor and can be used, for example, for treating prostrate cancer.Type: GrantFiled: November 22, 2002Date of Patent: March 1, 2005Assignee: Schering AktiengesellschaftInventors: Arwed Cleve, Christoph Huwe, Volker Schulze, Helmut Morack, Dieter Zopf, Jens Hoffmann, Andreas Reichel
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Patent number: 6861424Abstract: Compounds of the following formula (I): where a, b, R1, R2, R3, R4 and R6 are described herein, are useful as inhibitors of platelet adenosine diphosphate. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: GrantFiled: June 5, 2002Date of Patent: March 1, 2005Assignee: Schering AktiengesellschaftInventors: Judi A. Bryant, Brad O. Buckman, Imadul Islam, Raju Mohan, Michael M. Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Patent number: 6855711Abstract: Use of a compound of formula (I), wherein R1 is H or hydrocarbyl; R2 is a hydrophobic radical; R3 is 3-(C2-C6)acyl-4-hydroxyphenyl, 3-hydroxyimino (C2-C6)-alkyl-4-hydroxyphenyl, or COOZ, wherein Z is H, (C1-C6) alkyl, aryl, aryl or ar(C1-C6) alkyl; and n is 1-20; and of a compound of formula (II), wherein R4 is (C1-C6) alkyl, cyano (C1-C6) alkyl, (C1-C6) alkoxy (C1-C6) alkyl or —CH2NR7R8, wherein R7 and R8, the same or different, is each H or (C1-C6) alkyl, or together with the N atom form a saturated or unsaturated 5-7 membered ring optionally containing a further heteroatom selected from N, O or S, the further N atom being optionally substituted, and either R5 is H and R6 is (C2-C6) acyl or hydroxyimino (C2-C6) alkyl, or R5 and R6 together with the phenyl ring form a quinoline, a 1,2,3,4-tetrahydroquinoline or a perhydroquinoline ring, for the preparation of pharmaceutical compositions for the treatment of Parkinson's disease or stroke.Type: GrantFiled: June 7, 2000Date of Patent: February 15, 2005Assignees: Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.Inventors: Rivka Warshawsky, Moussa B. H. Youdim, Dorit Ben-Shachar, Abraham Warshawsky
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Patent number: 6838461Abstract: Compounds of the formula I in which R1, R2, R4 and R5 have the meanings indicated in claim 1, are potent 5-HT2A antagonists and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkingson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia, nervous anorexia, premenstrual syndrome and/or for positively affecting compulsive behavior (obsessive-compulsive disorder, OCD).Type: GrantFiled: July 7, 2000Date of Patent: January 4, 2005Assignee: Merck Patent GmbHInventors: Henning Boettcher, Christoph Seyfried
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Patent number: 6835731Abstract: Tertiary amines containing a multiplicity of heteroaromatic substituents are useful as chemokine receptor modulators.Type: GrantFiled: September 17, 2001Date of Patent: December 28, 2004Assignee: 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, Rosaria Maria Di Fluri
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Publication number: 20040259858Abstract: Compounds of formula I 1Type: ApplicationFiled: July 22, 2004Publication date: December 23, 2004Inventors: Michael G. Klug, Patrizio Mattei, Werner Mueller, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger, Jean-Marc Plancher
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Patent number: 6821967Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc, Rf, Rg, X, m and n are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyceride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: October 9, 2002Date of Patent: November 23, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Publication number: 20040229880Abstract: Compounds of the formula: 1Type: ApplicationFiled: February 18, 2004Publication date: November 18, 2004Applicant: WyethInventors: Diane Harris Boschelli, Margaret Maria Zaleska, Frank Charles Boschelli, Kim Timothy Arndt
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Patent number: 6809093Abstract: Compounds, compositions, and methods for treating multidrug resistance are disclosed. Suitable compounds are 2-substituted heterocyclic compounds.Type: GrantFiled: December 19, 2000Date of Patent: October 26, 2004Assignee: H. Lee Moffitt Cancer & Research Institute, Inc.Inventors: Charles Raymond Degenhardt, David Joseph Eickhoff
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Publication number: 20040209884Abstract: Compounds of formula (I) 1Type: ApplicationFiled: May 10, 2004Publication date: October 21, 2004Inventors: Chih-Hung Lee, Erol K. Bayburt, Stanley DiDomenico, Irene Drizin, Arthur R. Gomtsyan, John R. Koenig, Richard J. Perner, Robert G. Schmidt, Sean C. Turner, Tammie K. White, Guo Zhu Zheng
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Patent number: 6803369Abstract: A method of modulating the activity of a aberrant cell topoisomerase enzyme involving contacting the enzyme with a compound that inhibits enzyme-mediated cleavage of a polynucleotide substrate with which the enzyme is in complex. Pharmaceutical compositions containing such compounds may be used to treat neoplasias or to inhibit the growth of certain cancer cells. Screening methods can be employed to identify other compounds for these uses.Type: GrantFiled: July 25, 2001Date of Patent: October 12, 2004Assignees: SmithKline Beecham Corporation, SmithKlineBeecham p.l.c.Inventors: Symon G. Erskine, Michael Gwynn, Neil David Pearson, Edwina Imogen Wilding
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Publication number: 20040176388Abstract: Piperazine derivatives of formula (I) processes for their preparation, pharmaceutical compositions containing them and to their use in therapy as 5-HT1B antagonists. W,Y,Ra-Re are so defined in the application.Type: ApplicationFiled: March 17, 2004Publication date: September 9, 2004Applicant: SmithKline Beecham p.I.c.Inventors: Howard Marshall, Mervyn Thompson, Paul Adrian Wyman
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Patent number: 6784181Abstract: The present invention is directed to a compound of general formula (I), wherein R1 is selected from phenyl, pyridinyl, thiophenyl, furanyl, imidazolyl; each phenyl ring and heteroaromatic ring optionally and independently being further substituted by 1, 2 or 3 substituents selected from straight and branched C1-C6 alkyl, NO2, CF3, C1-C6 alkoxy, chloro, fluoro, bromo, and iodo, as well as their pharmaceutically acceptable salts. The invention includes pharmaceutical compositions comprising these compounds and the use of the compounds in therapy, in particular in the management of pain.Type: GrantFiled: October 21, 2002Date of Patent: August 31, 2004Assignee: AstraZeneca ABInventors: William Brown, Christopher Walpole, Niklas Plobeck
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Publication number: 20040162282Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: December 9, 2003Publication date: August 19, 2004Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subhabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Publication number: 20040157849Abstract: Compounds of formula (I) 1Type: ApplicationFiled: August 5, 2003Publication date: August 12, 2004Inventors: Chih-Hung Lee, Erol K. Bayburt, Stanley DiDomenico, Irene Drizin, Arthur R. Gomtsyan, John R. Koenig, Richard J. Perner, Robert G. Schmidt, Sean C. Turner, Tammie K. White, Guo Zhu Zheng
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Patent number: 6770650Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: August 29, 2001Date of Patent: August 3, 2004Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Donald Roy Hirschfeld, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Publication number: 20040142926Abstract: Compounds of the formula I: 1Type: ApplicationFiled: September 10, 2003Publication date: July 22, 2004Inventors: Deborah Ann Evrard, Dahui Zhou, Gary Paul Stack, Aranapakam Madumbai Venkatesan, Amedeo A. Failli, Susan Christman Croce
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Publication number: 20040138227Abstract: The present invention relates to a phenoxypropylamine compound of the formula (I) 1Type: ApplicationFiled: December 22, 2003Publication date: July 15, 2004Inventors: Akira Nishiyama, Masahiro Bougauchi, Takanobu Kuroita, Masanori Minoguchi, Yasunori Morio, Kouji Kanzaki
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Publication number: 20040138228Abstract: Compounds of the formula (I) 1Type: ApplicationFiled: November 17, 2003Publication date: July 15, 2004Applicant: AstraZeneca Canada Inc.Inventors: Edward Roberts, Niklas Plobeck, Claes Wahlestedt
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Publication number: 20040138203Abstract: Compounds of the formula I 1Type: ApplicationFiled: December 15, 2003Publication date: July 15, 2004Inventors: Gerd Steiner, Kurt Schellhaas, Laszlo Szabo, Berthold Behl, Francisco Javier, Lilliane Unger
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Publication number: 20040138229Abstract: Compounds of the following formula: 1Type: ApplicationFiled: December 9, 2003Publication date: July 15, 2004Applicant: Schering AktiengesellschaftInventors: Judi Bryant, Brad Buckman, Imadul Islam, Raju Mohan, Michael Morrissey, Guo Ping Wei, Wei Xu, Shendong Yuan
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Publication number: 20040132740Abstract: The present invention relates to a novel antifungal molecule 2-(3,4-dimethyl-2,5-dihydro-1H-pyrrol-2-yl)-1-methylethyl pentanoate of formula (I) from a plant Dutura metel a process for isolation and characterization of the molecule and a pharmaceutical composition essentially comprising the molecule as a antifungal agent (I).Type: ApplicationFiled: February 2, 2004Publication date: July 8, 2004Inventor: Farouk Hussni Al-Hajjar
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Publication number: 20040110750Abstract: Compounds of formula (I′) wherein the two OH— substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in claims, exhibit COMT enzyme inhibiting activity so that they are useful as COMT inhibitors.Type: ApplicationFiled: March 31, 2003Publication date: June 10, 2004Inventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Patent number: 6747029Abstract: A method of inhibiting motor hyperactivity in a mammal exhibiting the symptoms of attention deficit-hyperactivity disorder (ADHD) includes administering to a mammal a dopamine D4 receptor-selective antagonist.Type: GrantFiled: March 12, 2002Date of Patent: June 8, 2004Assignee: The McLean Hospital CorporationInventors: Ross J. Baldessarini, Kehong Zhang, Frank I. Tarazi
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Publication number: 20040097518Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: 1Type: ApplicationFiled: November 24, 2003Publication date: May 20, 2004Inventors: Carlos Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Maria Gerard Nadler
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Publication number: 20040082566Abstract: The present invention relates to pyrrolidine sulfonamides, pharmaceutical compositions containing them and their use as urotensin II antagonists.Type: ApplicationFiled: September 26, 2003Publication date: April 29, 2004Inventors: Dashyant Dhanak, Steven D Knight, Jian Jin, Ralph A Rivera, Anthony Sapienza
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Publication number: 20040082571Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: ApplicationFiled: June 11, 2003Publication date: April 29, 2004Applicant: ChemoCentryx, Inc.Inventors: Andrew M.K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Publication number: 20040082590Abstract: The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.Type: ApplicationFiled: July 11, 2003Publication date: April 29, 2004Inventors: Karin Briner, Christopher William Doecke, Vincent Mancuso, Michael John Martinelli, Timothy Ivo Richardson, Roger Ryan Rothhaar, Qing Shi, Chaoyu Xie
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Publication number: 20040082591Abstract: Provided herein is a compound having the formula (I) wherein said compounds are useful for the treatment of psychiatric disorders including but not limited to depression, generalized anxiety, eating disorders, dementia, panic disorder, and sleep disorders. The compounds may also be useful in the treatment of gastrointestinal disorders, cardiovascular regulation, motor disorders, endocrine disorders, vasospasm and sexual dysfunction. The compounds are 5HT1B and 5HT1D antagonists.Type: ApplicationFiled: July 16, 2003Publication date: April 29, 2004Inventors: Marc Chapdelaine, Timothy Davenport, Markus Haeberlein, Carey Horchler, John McCauley, Edward Pierson, Daniel Sohn
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Publication number: 20040082589Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: 1Type: ApplicationFiled: October 23, 2003Publication date: April 29, 2004Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Marie Gerard
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Publication number: 20040077657Abstract: Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).Type: ApplicationFiled: July 17, 2003Publication date: April 22, 2004Inventors: Henning Bottcher, Gerd Bartoszyk, Jurgen Harting, Christoph van Amsterdam, Christoph Seyfried
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Publication number: 20040077631Abstract: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3-7C) methyl, benzyl or m-phenyl benzyl.Type: ApplicationFiled: August 15, 2003Publication date: April 22, 2004Inventors: Marcel P.M. van Aar, Stefanus J. Schouten, Jan Zorgdrager, Michiel C. Heslinga