Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
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Patent number: 7071196Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.Type: GrantFiled: August 8, 2003Date of Patent: July 4, 2006Assignee: SmithKline Beecham CroporationInventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
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Patent number: 7071197Abstract: N,N-Disubstituted diazocycloalkanes of the formula I (R1=halogen, R2=(C3–C8)-cycloalkyl, R3=(C1–C4)-alkoxy or (C1–C4)-haloalkoxy group, m is 1 or 2 and n is 1 or 2, have affinity for serotonergic receptors. These compounds and their enantiomers, diastereoisomers, N-oxides, polymorphs, solvates and pharmaceutically acceptable salts are useful in the treatment of patients with neuromuscular dysfunction of the lower urinary tract and diseases related to 5-HT1A receptor.Type: GrantFiled: June 16, 2003Date of Patent: July 4, 2006Assignee: Recordati S.A.Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 7067501Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.Type: GrantFiled: May 20, 2004Date of Patent: June 27, 2006Assignee: H. Lundbeck A/SInventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
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Patent number: 7056922Abstract: A compound of the formula wherein D, E, F, G, L, T, W, X, Y, Z, U, A, R1, R2, R3, R4, R5, R6 R7 are as defined in the specification, pharmaceutical compositions thereof, and methods of use to treat diseases and as D3 receptor modulators.Type: GrantFiled: July 29, 2003Date of Patent: June 6, 2006Assignee: Pfizer IncInventors: Anton F. J. Fliri, Anthony R. Reinhold
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Patent number: 7037914Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: September 23, 2002Date of Patent: May 2, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 7030122Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including serotonin receptors and dopamine receptors. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, Tourette's syndrome, psychiatric disorders, stroke, and senile dementia.Type: GrantFiled: March 27, 2003Date of Patent: April 18, 2006Assignee: Sepracor Inc.Inventors: James R. Hauske, Joanne M. Holland, Heike S. Radeke
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Patent number: 7019007Abstract: The invention provides compounds of Formula (I): wherein: R1–R4, A, D, and L have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 27, 2002Date of Patent: March 28, 2006Assignee: Syntex (U.S.A.) LLCInventors: Daisy Joe Du Bois, Beihan Wang
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Patent number: 7001907Abstract: This invention relates to peptide-containing ?-ketoamide inhibitors of cysteine and serine proteases, methods for making these compounds, and methods for using the same.Type: GrantFiled: October 14, 2003Date of Patent: February 21, 2006Assignee: Cephaon, Inc.Inventors: Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
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Patent number: 7001908Abstract: A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.Type: GrantFiled: April 16, 2003Date of Patent: February 21, 2006Assignees: Avera Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: Alexander Glenn Godfrey, Daniel Timothy Kohlman, John Cunningham O'Toole, Yao-Chang Xu, Tony Yantao Zhang
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Patent number: 6969713Abstract: The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapyType: GrantFiled: December 18, 2000Date of Patent: November 29, 2005Assignee: AstraZeneca ABInventors: Premji Meghani, Colin Bennion
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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: 6951860Abstract: The invention involves the identification of a family of compounds which block calcium channels. The compounds can be formulated in pharmaceutical carriers and administered to subjects. The compounds are useful for treating disorders associated with calcium channel activity, such as, cardiovascular diseases, for example hypertension, congestive heart failure, arrhythmia and angina.Type: GrantFiled: October 31, 2001Date of Patent: October 4, 2005Assignee: Massachusetts College of PharmacyInventors: Ahmed S. Mehanna, Jinyung T. Kim
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Patent number: 6951861Abstract: The invention relates to piperazine derivatives, to processes for their preparation, to pharmaceutical compositions containing them, and to their medical use. The novel compounds are antagonists of tachykinins, including substance P and other neurokinins.Type: GrantFiled: October 5, 2000Date of Patent: October 4, 2005Assignee: SmithKline Beechan CorporationInventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini, Mauro Corsi, Sergio Melotto
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Patent number: 6916816Abstract: Disclosed are compounds of formula (I) wherein: L is (a) optionally substituted by replacement of one or more of the hydrogen atoms on the phenanthrene ring system by one or more groups other than hydrogen; A is CH2, SO2 or C?O; X is CO2H, PO3H2, PO2H2, PO2HR5, PO2HOR5, SO3H, SO2H, or tetrazole; and R1, R2, R3, R4 and R5 are independently selected from H, alkyl, alkenyl, alkynyl, aryl and aralkyl; or a pharmaceutically acceptable acid salt or base addition salt or an in vivo hydrolysable ester or amide thereof.Type: GrantFiled: December 18, 2000Date of Patent: July 12, 2005Assignees: The Board of Regents of the University of Nebraska, The University of BristolInventors: Daniel T. Monaghan, David E. Jane, Heong Wai Tse
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Patent number: 6906073Abstract: The invention provides compounds of Formula (I): wherein: R1-R4, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.Type: GrantFiled: November 29, 2002Date of Patent: June 14, 2005Assignee: Roche Palo Alto LLCInventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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Patent number: 6906074Abstract: A 2-phenylpiperazine derivative represented by the formula (I) or a pharmaceutically acceptable salt, hydrate, or complex thereof: wherein each of X1 and X3 is oxygen or two hydrogen atoms, X2 O, NH, NCH3, or CH2, n is an integer of 0 or 1, R1 is hydrogen or lower alkyl and R2 is hydrogen, cyano, tetrazolyl, aminotriazolyl , mesyl, t-butoxycarbonyl, or a lower alkyl which may be optionally substituted, R3 is hydrogen, halogen, lower alkyl or lower alkoxy, each of R4 and R5 is hydrogen, lower alkoxy or trifluoromethyl, and a broken line indicates a single or double bond. The derivative may be used as a tachykinin antagonist in the treatment of diseases of the digestive system, nervous system and respiratory system, inflammation, allergy, carcinoid syndrome, chronic pain, headache, Crohn disease, depression and vomiting.Type: GrantFiled: February 20, 2003Date of Patent: June 14, 2005Assignee: Nippon Zoki Pharmaceutical Co., Ltd.Inventors: Takashi Ogino, Yukari Konishi, Kunihiko Higashiura, Kazuhito Furukawa
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Patent number: 6903120Abstract: New 3-substituted 4-(phenyl-N-alkyl)-piperazine and 4-(phenyl-N-alkyl)-piperidine compounds of Formula (1), wherein X N, CH, or C, however X may only be C when the compound comprises a double bond at the dotted line; R1 is OSO2CF3, OSO2CH3, SOR3, SO2R3, COR3, NO2, or CONHR3 and when X is CH or C R1 may also be CF3, CN, F, Cl, Br, or I; R2 is a C1-C4 alkyl, an allyl, CH2SCH3, CH2CH2OCH3, CH2CH2CH2F, CH2CF3, 3,3,3-trifluoropropyl, 4,4,4,-trifluorobutyl, or —(CH2)—R4; R3 is a C1-C3 alkyl CF3, or N(R2)2; R4 is a C3-C6 cycloalkyl, 2-tetrahydrofurane or 3-tetra-hydrofurane, as well as pharmaceutically acceptable salts thereof are disclosed.Type: GrantFiled: December 22, 2000Date of Patent: June 7, 2005Assignee: A. Carlsson Research ABInventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
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Patent number: 6894053Abstract: Compounds of the formula have a long duration of action and are useful for the treatment of chronic diseases resulting from the dysfunction of the serotonergic 5-HT1A system, such as schizophrenia and other psychotic disorders such as paranoia and mano-depressive illness.Type: GrantFiled: December 12, 2003Date of Patent: May 17, 2005Assignee: WyethInventors: Wayne E. Childers, Michael G. Kelly, Lee E. Schechter, Sharon J. Rosenzweig-Lipson
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Patent number: 6894052Abstract: Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.Type: GrantFiled: July 31, 1998Date of Patent: May 17, 2005Assignee: Recordati S.A. Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 6887876Abstract: Benzamidine derivatives are useful delta-opioid receptor modulators, agonists useful as analgesics and 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: December 11, 2001Date of Patent: May 3, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Ellen W. Baxter, Samuel O. Nortey, Allen B. Reitz
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Patent number: 6887878Abstract: A compound having the following formula I: where R1 is an alkyl group or an alkenyl group, X represents R2 is selected from the group consisting of a halogen (o, m, p) group such as F, Cl, Br or I, —NH2, —NO2 and a hydrogen group, R3 is a hydrogen group or OH. The compound has pharmacologically ?2-adrenergic/5-HT2A antagonist activity, 5-HT re-uptake activity, and anti-oxidant activity. The compound is produced by preparing 4-epoxy isoeugenol, mixing piperazine dissolved in methanol with the 4-epoxy isoeugenol to reflux at 100° C. for approximately 2 to approximately 6 hours, removing the methanol, passing the mixture through a silica gel column chromatography after the removing step, eluting the passed mixture with n-hexane and ethyl acetate, drying the eluted mixture, and crystallizing the dried mixture with methanol.Type: GrantFiled: June 30, 2003Date of Patent: May 3, 2005Assignees: Ing-Jun Chen, Syn-Rech Chem & Phan Co., LtdInventor: Ing-Jun Chen
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Patent number: 6881738Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.Type: GrantFiled: July 18, 2002Date of Patent: April 19, 2005Assignees: Medical College of Georgia Research Institute, University of Georgia Research Foundation, IncInventors: Jerry J. Buccafusco, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
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Patent number: 6878707Abstract: Compounds of formula (I) wherein R2—C, R3—C, R4—C or R5—C may be replaced by N; and wherein n is 1, 2 or 3; R1 is aryl, heteroaryl or (aryl or heteroaryl)-lower alkoxy; R2, R3, R4 and R5 are independently hydrogen, lower alkyl, lower alkoxy, halo, trifluoromethyl or cyano; R6 is (i) or (ii) m is 1, 2 or 3; R7 is hydrogen, lower alkyl (aryl or heteroaryl)-lower alkyl, lower alkoxy, (aryl or heteroaryl)-lower alkoxy, hydroxy, oxo, lower alkylenedioxy or lower alkanoyloxy; W is O, S or NR8; R8 is —CORa, (iii), —COORd, —SO2Re, hydrogen, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Ra, Rd and Re are independently optionally substituted lower alkyl, cycloalkyl, adamantyl, aryl, heteroaryl or (aryl or heteroaryl)-lower alkyl; Rb and Rc are independently hydrogen, cycloalkyl, optionally substituted lower alkyl, aryl, heteroaryl or (aryl or heteroaryl) lower alkyl; or Rb and Rc together represent lower alkylene; and pharmaceutically acceptable salts thereof; and enantiType: GrantFiled: January 16, 2001Date of Patent: April 12, 2005Assignee: Novartis AGInventor: Gary Michael Ksander
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Patent number: 6864262Abstract: The present invention provides a compound of the formula (I) and the pharmaceutically acceptable salts and solvates thereof, which is useful for treating bladder over-activity or urinary incontinence.Type: GrantFiled: November 16, 2001Date of Patent: March 8, 2005Assignee: Eli Lilly and CompanyInventors: John Mehnert Schaus, Dennis Charles Thompson, Karl Bruce Thor
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Patent number: 6858624Abstract: This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R1, R2, and R3 are as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of nicotine addiction/withdrawal and CNS disorders.Type: GrantFiled: November 27, 2002Date of Patent: February 22, 2005Assignees: Pfizer, Inc., Pfizer Products, Inc.Inventors: Anne E. Hagen, R. Scott Obach
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Publication number: 20040266785Abstract: A compound having the following formula I: 1Type: ApplicationFiled: June 30, 2003Publication date: December 30, 2004Inventor: Ing-Jun Chen
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Publication number: 20040266786Abstract: Isoeugenol derivative compounds having the moiety 1Type: ApplicationFiled: June 30, 2003Publication date: December 30, 2004Inventor: Ing-Jun Chen
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Publication number: 20040259861Abstract: A medicament for inhibiting sodium/calcium exchange system which comprises as an active ingredient a substance selected from the group consisting of an aminobenzenesulfonic acid derivative represented by the following general formula (I) and a salt thereof, and a hydrate thereof and a solvate thereof: 1Type: ApplicationFiled: July 14, 2004Publication date: December 23, 2004Inventor: Naoya Satoh
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Publication number: 20040254196Abstract: The present invention relates to cinnamaldehyde derivatives inhibiting growth of tumor cell and regulating cell cycle, the method for preparation and the pharmaceutical composition thereof. The cinnamaldehyde derivatives of the present invention can be effectively used as a cell cycle regulator or a cancer cell growth inhibitor, since it has an ability to regulate cell cycle by holding the cells in G2/M stage of the cell division and has activity to inhibit cancer cell growth.Type: ApplicationFiled: May 28, 2004Publication date: December 16, 2004Inventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong Cho Han, Sangku Lee, Jong Han Kim, Sung-Gyu Choi, Mi-Young Lee, Sun Bok Jeon
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Patent number: 6831080Abstract: There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken tType: GrantFiled: May 31, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Li-Quang Sun, Jie Chen, Huan He, Alexandre L'Heureux, Pierre Dextraze, Jean-Paul Daris, Gene G. Kinney, Steven I. Dworetzky, Piyasena Hewawasam
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Patent number: 6831084Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection, the compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.Type: GrantFiled: November 6, 2000Date of Patent: December 14, 2004Assignee: WyethInventors: Wayne E. Childers, Jr., Horace Fletcher, III, Magid A. Abou-Gharbia, John P. Yardley
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Patent number: 6828324Abstract: This invention provides compounds and methods using them to provide neuroprotection and prevent or limit processes of neurodegeneration in mammals, including Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, AIDS dementia, retinal disease, diabetic peripheral neuropathy, multiple sclerosis, stroke, acute thromboembolic stroke, focal ischemia, global ischemia, transient ischemic attack, ischemia resulting from surgery, head trauma, spinal trauma, hypoxia, fetal hypoxia, and neuroprotection. The compounds having the structure: wherein X is —CH2— or a bond; Y is —(CH2)m— or —(CH2)—O—(CH2)—; m 0 or 1; n is 0 or 1; R1 and R2 are independently selected from optionally substituted aryl or heteroaryl; the optical isomers and the pharmaceutically acceptable salts thereof.Type: GrantFiled: February 20, 2004Date of Patent: December 7, 2004Assignee: WyethInventors: Wayne E. Childers, Jr., Horace Fletcher, III, Magid A. Abou-Gharbia, John P. Yardley
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Patent number: 6825202Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: August 9, 2002Date of Patent: November 30, 2004Assignee: Syntex (U.S.A.) LLCInventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
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Publication number: 20040235830Abstract: The invention relates to substituted cyclohexane derivates of formula (I), a method for the production thereof and the use thereof in medicaments, particularly for preventing and/or treating cardiovascular diseases, diseases of the urogenital tract and cerebrovascular diseases.Type: ApplicationFiled: April 22, 2004Publication date: November 25, 2004Inventors: Susanne Rohrig, Andreas Stolle, Julio C. Castro-Palomino, Helmut Haning, Gabriele Handke-Erguden, Noemi Daviu-Folguera, Holger Paulsen, Josef Pernerstorfer, Stephan-Nicholas Wirtz, Henning Steinhagen, Wolfgang Thielemann, Erwin Bischoff, Ulrich Ebbinghaus-Kintscher, Peter Ellinghaus, Joachim Hutter, Thomas Krahn, Frank Wunder, Klemens Lustig, Joachim Schuhmacher, Frank Sussmeier
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Publication number: 20040235827Abstract: This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general formula (I): 1Type: ApplicationFiled: March 31, 2004Publication date: November 25, 2004Inventors: Bharat Lagu, Kenneth Rupert, Michael Wachter
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Publication number: 20040235855Abstract: This invention is directed to heterocyclyl-substituted anilino phospholipase C inhibitor compounds useful in treating or ameliorating an inflammatory disorders and/or restenosis of the general formula (I): 1Type: ApplicationFiled: March 31, 2004Publication date: November 25, 2004Inventors: Bharat Lagu, Meng Pan, Kenneth Rupert, Michael Wachter
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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: 20040229869Abstract: Novel mercaptophenyl naphthyl methane compounds, their pharmaceutically acceptable salts and compositions comprised thereof are useful for the prevention or treatment of various medical indications associated with estrogen dependent diseases or syndromes related to osteoporosis, bone loss, bone formation, cardiovascular disorders, neurodegenerative disorders, menopausal disorders, physiological disorders, diabetes disorders, prostatic carcinoma, cancer of breast, cancer of uterus, cancer of the cervix and cancer of the colon, threatened or habitual abortion, obesity, ovarian development or function, post-partum lactation and depression.Type: ApplicationFiled: March 26, 2004Publication date: November 18, 2004Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCHInventors: Sangita, Atul Kumar, Man Mohan Singh, Girish Kumar Jain, Puvvada Sri Ramanchandra Murthy, Suprabhat Ray
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Publication number: 20040229872Abstract: The use of substituted cyclohexan-1,4-diamine compounds in pharmaceutical compositions and for the treatment of diarrhea or irritable bowel diseases or as immunotherapeutic agents or peripheral analgesics, especially for treating burn pains, peripheral operation pains, pains generated by inflammation of soft tissues or inflammatory arthropathies, especially rheumatisms.Type: ApplicationFiled: November 10, 2003Publication date: November 18, 2004Applicant: Gruenenthal GmbHInventors: Elmar Josef Friderichs, Bernd Sundermann, Claudia Hinze, Babette-Yvonne Koegel
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Publication number: 20040229883Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: April 8, 2004Publication date: November 18, 2004Inventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
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Patent number: 6818644Abstract: The present invention relates to substituted piperazine derivatives of general formula wherein Ra, Rb, Rc Rf, Rg and m, n and X are defined as in claim 1, the isomers and salts thereof, particularly the physiologically acceptable salts thereof, which are valuable inhibitors of the microsomal triglyseride-transfer protein (MTP), medicaments containing these compounds and their use, as well as the preparation thereof.Type: GrantFiled: July 1, 2002Date of Patent: November 16, 2004Assignee: Boehringer Ingelheim Pharm GmbH & Co, KGInventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
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Publication number: 20040214822Abstract: 4-aminocyclohexanol compounds, processes for their preparation, pharmaceutical formulations comprising these compounds and the use of substituted 4-aminocyclohexanol compounds for the preparation of pharmaceutical formulations and for the treatment of diverse indications, including, without limitation, pain.Type: ApplicationFiled: January 16, 2004Publication date: October 28, 2004Applicant: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Stephan Wnendt
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Publication number: 20040214832Abstract: Disclosed are piperazine derivatives, their manufacture and use as inhibitors of renin.Type: ApplicationFiled: March 26, 2004Publication date: October 28, 2004Inventors: Cuiman Cai, Emma Hazel Clay, Dennis M. Downing, Jeremy John Edmunds, Daniel Dale Holsworth, Tingsheng Li, Noel Aaron Powell
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Publication number: 20040204422Abstract: The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I 1Type: ApplicationFiled: April 14, 2003Publication date: October 14, 2004Applicant: Abbott GmbH & Co. KG.Inventors: Wilfried M. Braje, Andreas Haupt, Wilfried Lubisch, Roland Grandel, Karla Drescher, Herve Geneste, Liliane Unger, Daryl R. Sauer
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Publication number: 20040198727Abstract: The invention provides compositions and methods to inhibit the cell cycle G2 checkpoint, in particular the DNA-damage-induced G2 checkpoint, in mammalian cells including human cells. Specifically, the invention provides compositions and methods to sensitize cells to DNA-damaging agents by abrogating the cell cycle G2 checkpoint. Compounds of the invention are used to treat proliferative disorders such as cancer. The invention provides compositions and methods for selectively sensitizing G1 checkpoint impaired cancer cells to DNA-damaging agents and treatments.Type: ApplicationFiled: June 6, 2003Publication date: October 7, 2004Inventors: Takumi Kawabe, Hidetaka Kobayashi
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Publication number: 20040180892Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.Type: ApplicationFiled: February 18, 2004Publication date: September 16, 2004Applicant: Encysive Pharmaceuticals Inc.Inventors: Chengde Wu, C. Eric Anderson, Huong Bui, Daxin Gao, Jamal Kassir, Wen Li, Junmei Wang, Robert V. Market
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Publication number: 20040180899Abstract: The invention relates to new phthalazine derivatives of formula (I), wherein R1 and R2: a) are independently in each case a lower alkyl; b) together form a bridge of subformula (I*), wherein the bond is achieved via the two terminal C atoms and m is 0 to 4; or c) together form a bridge of subformula (I**), wherein one or two of the ring members T1, T2, T3 and T4 are nitrogen, and the others are in each case CH, and the bond is achieved via atoms T1 and T4; A, B, D, E and T are independently N or CH subject to the proviso that at least one and not more than three of these radicals are N; X is imino, oxa, or thia; Y is hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or unsubstituted or substituted cycloalkyl; and wherein the bonds characterized in subformula (I*) by a wavy line are either single or double bonds; to an N-oxide of a compound of formula I; a tautomer or mixture of tautomers of a compound of formula (I) of an N-oxide thereof; and a pharmaceutically acceptable sType: ApplicationFiled: March 29, 2004Publication date: September 16, 2004Inventors: Guido Bold, Paul William Manley
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Publication number: 20040176393Abstract: The invention is a pharmaceutical composition comprising an MMP inhibitor and a statin, said composition being useful for treating vascular diseases.Type: ApplicationFiled: April 22, 2003Publication date: September 9, 2004Inventors: Roger Schofield Newton, Bruce David Roth
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Patent number: 6784183Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.Type: GrantFiled: June 29, 2001Date of Patent: August 31, 2004Assignee: Les Laboratoires ServierInventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
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Publication number: 20040162287Abstract: Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.Type: ApplicationFiled: November 10, 2003Publication date: August 19, 2004Applicant: GRUENENTHAL GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Babette-Yvonne Koegel
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Patent number: 5125102Abstract: A digitally trunked radio repeater system provides substantial improvements in timeliness of channel acquisition and channel drop, and in reliability of critical control signalling. The system uses a much higher digital signalling rate than is typically found in prior art systems, and uses a control channel to convey digital channel request and assignment messages between the central site and mobile transceivers. The mobile radio transceivers transmit channel requests on the control channel (if no response is received, the mobile retries during a retry time window which increases in duration in dependence on the number of retries). The mobile transceiver switches to a working channel in response to an assignement message received on the control channel. Subaudible digital signals transmitted on the control channel and on active working channels allow late entry, shifting to higher priority calls, and other advanced functions.Type: GrantFiled: January 3, 1990Date of Patent: June 23, 1992Assignee: Ericsson GE Mobile Communications Inc.Inventors: Jeffrey S. Childress, Marc A. Dissosway, Gerald M. Cooper, Houston H. Hughes, III