Carbocyclic Ring Bonded Directly To The Piperazine Ring Patents (Class 514/255.03)
  • Patent number: 7071196
    Abstract: 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: Grant
    Filed: August 8, 2003
    Date of Patent: July 4, 2006
    Assignee: SmithKline Beecham Croporation
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini
  • Patent number: 7071197
    Abstract: 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: Grant
    Filed: June 16, 2003
    Date of Patent: July 4, 2006
    Assignee: Recordati S.A.
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
  • Patent number: 7067501
    Abstract: The invention provides compounds of the formula wherein the substituents are as defined in the application. The compounds are valuable glycine transport inhibitors.
    Type: Grant
    Filed: May 20, 2004
    Date of Patent: June 27, 2006
    Assignee: H. Lundbeck A/S
    Inventors: Garrick P. Smith, Gitte Mikkelsen, Kim Andersen, Daniel Greve, Thomas Ruhland, Stephen P. Wren
  • Patent number: 7056922
    Abstract: 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: Grant
    Filed: July 29, 2003
    Date of Patent: June 6, 2006
    Assignee: Pfizer Inc
    Inventors: Anton F. J. Fliri, Anthony R. Reinhold
  • Patent number: 7037914
    Abstract: 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: Grant
    Filed: September 23, 2002
    Date of Patent: May 2, 2006
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
  • Patent number: 7030122
    Abstract: One aspect of the present invention relates to novel heterocyclic compounds. A second aspect of the present invention relates to the use of the novel heterocyclic compounds as ligands for various cellular receptors, including 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: Grant
    Filed: March 27, 2003
    Date of Patent: April 18, 2006
    Assignee: Sepracor Inc.
    Inventors: James R. Hauske, Joanne M. Holland, Heike S. Radeke
  • Patent number: 7019007
    Abstract: 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: Grant
    Filed: November 27, 2002
    Date of Patent: March 28, 2006
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Daisy Joe Du Bois, Beihan Wang
  • Patent number: 7001907
    Abstract: 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: Grant
    Filed: October 14, 2003
    Date of Patent: February 21, 2006
    Assignee: Cephaon, Inc.
    Inventors: Sankar Chatterjee, John P. Mallamo, Ron Bihovsky, Gregory J. Wells
  • Patent number: 7001908
    Abstract: 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: Grant
    Filed: April 16, 2003
    Date of Patent: February 21, 2006
    Assignees: Avera Pharmaceuticals, Inc., Eli Lilly and Company
    Inventors: Alexander Glenn Godfrey, Daniel Timothy Kohlman, John Cunningham O'Toole, Yao-Chang Xu, Tony Yantao Zhang
  • Patent number: 6969713
    Abstract: 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 therapy
    Type: Grant
    Filed: December 18, 2000
    Date of Patent: November 29, 2005
    Assignee: AstraZeneca AB
    Inventors: Premji Meghani, Colin Bennion
  • Patent number: 6953801
    Abstract: 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: Grant
    Filed: May 21, 2002
    Date of Patent: October 11, 2005
    Assignee: Neurogen Corporation
    Inventors: Alan Hutchison, Linda M. Gustavson, John M. Peterson, Dario Doller, Timothy M. Caldwell, Taeyoung Yoon, Wallace C. Pringle, Yiping Shen, Cheryl Steenstra
  • Patent number: 6951860
    Abstract: 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: Grant
    Filed: October 31, 2001
    Date of Patent: October 4, 2005
    Assignee: Massachusetts College of Pharmacy
    Inventors: Ahmed S. Mehanna, Jinyung T. Kim
  • Patent number: 6951861
    Abstract: 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: Grant
    Filed: October 5, 2000
    Date of Patent: October 4, 2005
    Assignee: SmithKline Beechan Corporation
    Inventors: Giuseppe Alvaro, Romano Di Fabio, Riccardo Giovannini, Giuseppe Guercio, Yves St-Denis, Antonella Ursini, Mauro Corsi, Sergio Melotto
  • Patent number: 6916816
    Abstract: 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: Grant
    Filed: December 18, 2000
    Date of Patent: July 12, 2005
    Assignees: The Board of Regents of the University of Nebraska, The University of Bristol
    Inventors: Daniel T. Monaghan, David E. Jane, Heong Wai Tse
  • Patent number: 6906073
    Abstract: 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: Grant
    Filed: November 29, 2002
    Date of Patent: June 14, 2005
    Assignee: Roche Palo Alto LLC
    Inventors: Daisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
  • Patent number: 6906074
    Abstract: 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: Grant
    Filed: February 20, 2003
    Date of Patent: June 14, 2005
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Takashi Ogino, Yukari Konishi, Kunihiko Higashiura, Kazuhito Furukawa
  • Patent number: 6903120
    Abstract: 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: Grant
    Filed: December 22, 2000
    Date of Patent: June 7, 2005
    Assignee: A. Carlsson Research AB
    Inventors: Clas Sonesson, Ingela Marianne Svan, Anders Kristoffer Lilja, Liselott Lilja Rönnqvist, Jenny Maria Carlberg, Susanna Waters, Nicholas Waters, Joakim Tedroff, Bengt Andersson
  • Patent number: 6894053
    Abstract: 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: Grant
    Filed: December 12, 2003
    Date of Patent: May 17, 2005
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Michael G. Kelly, Lee E. Schechter, Sharon J. Rosenzweig-Lipson
  • Patent number: 6894052
    Abstract: 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: Grant
    Filed: July 31, 1998
    Date of Patent: May 17, 2005
    Assignee: Recordati S.A. Chemical and Pharmaceutical Company
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
  • Patent number: 6887876
    Abstract: 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: Grant
    Filed: December 11, 2001
    Date of Patent: May 3, 2005
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Ellen W. Baxter, Samuel O. Nortey, Allen B. Reitz
  • Patent number: 6887878
    Abstract: 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: Grant
    Filed: June 30, 2003
    Date of Patent: May 3, 2005
    Assignees: Ing-Jun Chen, Syn-Rech Chem & Phan Co., Ltd
    Inventor: Ing-Jun Chen
  • Patent number: 6881738
    Abstract: 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: Grant
    Filed: July 18, 2002
    Date of Patent: April 19, 2005
    Assignees: Medical College of Georgia Research Institute, University of Georgia Research Foundation, Inc
    Inventors: Jerry J. Buccafusco, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
  • Patent number: 6878707
    Abstract: 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 enanti
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: April 12, 2005
    Assignee: Novartis AG
    Inventor: Gary Michael Ksander
  • Patent number: 6864262
    Abstract: 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: Grant
    Filed: November 16, 2001
    Date of Patent: March 8, 2005
    Assignee: Eli Lilly and Company
    Inventors: John Mehnert Schaus, Dennis Charles Thompson, Karl Bruce Thor
  • Patent number: 6858624
    Abstract: 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: Grant
    Filed: November 27, 2002
    Date of Patent: February 22, 2005
    Assignees: Pfizer, Inc., Pfizer Products, Inc.
    Inventors: Anne E. Hagen, R. Scott Obach
  • Publication number: 20040266785
    Abstract: A compound having the following formula I: 1
    Type: Application
    Filed: June 30, 2003
    Publication date: December 30, 2004
    Inventor: Ing-Jun Chen
  • Publication number: 20040266786
    Abstract: Isoeugenol derivative compounds having the moiety 1
    Type: Application
    Filed: June 30, 2003
    Publication date: December 30, 2004
    Inventor: Ing-Jun Chen
  • Publication number: 20040259861
    Abstract: 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: 1
    Type: Application
    Filed: July 14, 2004
    Publication date: December 23, 2004
    Inventor: Naoya Satoh
  • Publication number: 20040254196
    Abstract: 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: Application
    Filed: May 28, 2004
    Publication date: December 16, 2004
    Inventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong Cho Han, Sangku Lee, Jong Han Kim, Sung-Gyu Choi, Mi-Young Lee, Sun Bok Jeon
  • Patent number: 6831080
    Abstract: 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 t
    Type: Grant
    Filed: May 31, 2002
    Date of Patent: December 14, 2004
    Assignee: Bristol-Myers Squibb Company
    Inventors: 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
  • Patent number: 6831084
    Abstract: 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: Grant
    Filed: November 6, 2000
    Date of Patent: December 14, 2004
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Jr., Horace Fletcher, III, Magid A. Abou-Gharbia, John P. Yardley
  • Patent number: 6828324
    Abstract: 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: Grant
    Filed: February 20, 2004
    Date of Patent: December 7, 2004
    Assignee: Wyeth
    Inventors: Wayne E. Childers, Jr., Horace Fletcher, III, Magid A. Abou-Gharbia, John P. Yardley
  • Patent number: 6825202
    Abstract: 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: Grant
    Filed: August 9, 2002
    Date of Patent: November 30, 2004
    Assignee: Syntex (U.S.A.) LLC
    Inventors: Jacob Berger, Robin Douglas Clark, Shu-Hai Zhao
  • Publication number: 20040235830
    Abstract: 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: Application
    Filed: April 22, 2004
    Publication date: November 25, 2004
    Inventors: 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
  • Publication number: 20040235827
    Abstract: 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): 1
    Type: Application
    Filed: March 31, 2004
    Publication date: November 25, 2004
    Inventors: Bharat Lagu, Kenneth Rupert, Michael Wachter
  • Publication number: 20040235855
    Abstract: 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): 1
    Type: Application
    Filed: March 31, 2004
    Publication date: November 25, 2004
    Inventors: Bharat Lagu, Meng Pan, Kenneth Rupert, Michael Wachter
  • Patent number: 6821967
    Abstract: 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: Grant
    Filed: October 9, 2002
    Date of Patent: November 23, 2004
    Assignee: Boehringer Ingelheim Pharma KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Publication number: 20040229869
    Abstract: 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: Application
    Filed: March 26, 2004
    Publication date: November 18, 2004
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Sangita, Atul Kumar, Man Mohan Singh, Girish Kumar Jain, Puvvada Sri Ramanchandra Murthy, Suprabhat Ray
  • Publication number: 20040229872
    Abstract: 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: Application
    Filed: November 10, 2003
    Publication date: November 18, 2004
    Applicant: Gruenenthal GmbH
    Inventors: Elmar Josef Friderichs, Bernd Sundermann, Claudia Hinze, Babette-Yvonne Koegel
  • Publication number: 20040229883
    Abstract: Disclosed are compounds of the formula: 1
    Type: Application
    Filed: April 8, 2004
    Publication date: November 18, 2004
    Inventors: Rajagopal Bakthavatchalam, Andrew Thurkauf, Alan Hutchison
  • Patent number: 6818644
    Abstract: 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: Grant
    Filed: July 1, 2002
    Date of Patent: November 16, 2004
    Assignee: Boehringer Ingelheim Pharm GmbH & Co, KG
    Inventors: Thorsten Lehmann-Lintz, Armin Heckel, Leo Thomas, Michael Mark
  • Publication number: 20040214822
    Abstract: 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: Application
    Filed: January 16, 2004
    Publication date: October 28, 2004
    Applicant: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Stephan Wnendt
  • Publication number: 20040214832
    Abstract: Disclosed are piperazine derivatives, their manufacture and use as inhibitors of renin.
    Type: Application
    Filed: March 26, 2004
    Publication date: October 28, 2004
    Inventors: Cuiman Cai, Emma Hazel Clay, Dennis M. Downing, Jeremy John Edmunds, Daniel Dale Holsworth, Tingsheng Li, Noel Aaron Powell
  • Publication number: 20040204422
    Abstract: The invention relates to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula I 1
    Type: Application
    Filed: April 14, 2003
    Publication date: October 14, 2004
    Applicant: Abbott GmbH & Co. KG.
    Inventors: Wilfried M. Braje, Andreas Haupt, Wilfried Lubisch, Roland Grandel, Karla Drescher, Herve Geneste, Liliane Unger, Daryl R. Sauer
  • Publication number: 20040198727
    Abstract: 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: Application
    Filed: June 6, 2003
    Publication date: October 7, 2004
    Inventors: Takumi Kawabe, Hidetaka Kobayashi
  • Publication number: 20040180892
    Abstract: The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
    Type: Application
    Filed: February 18, 2004
    Publication date: September 16, 2004
    Applicant: Encysive Pharmaceuticals Inc.
    Inventors: Chengde Wu, C. Eric Anderson, Huong Bui, Daxin Gao, Jamal Kassir, Wen Li, Junmei Wang, Robert V. Market
  • Publication number: 20040180899
    Abstract: 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 s
    Type: Application
    Filed: March 29, 2004
    Publication date: September 16, 2004
    Inventors: Guido Bold, Paul William Manley
  • Publication number: 20040176393
    Abstract: The invention is a pharmaceutical composition comprising an MMP inhibitor and a statin, said composition being useful for treating vascular diseases.
    Type: Application
    Filed: April 22, 2003
    Publication date: September 9, 2004
    Inventors: Roger Schofield Newton, Bruce David Roth
  • Patent number: 6784183
    Abstract: Compounds of formula (I): and medicinal products containing the same which are useful as dual &agr;2/5-HT2c antagonists.
    Type: Grant
    Filed: June 29, 2001
    Date of Patent: August 31, 2004
    Assignee: Les Laboratoires Servier
    Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Anne Dekeyne, Mauricette Brocco
  • Publication number: 20040162287
    Abstract: Substituted cyclohexane-1,4-diamine compounds, methods for production thereof, pharmaceutical compositions comprising these compounds and methods of treatment using these compounds.
    Type: Application
    Filed: November 10, 2003
    Publication date: August 19, 2004
    Applicant: GRUENENTHAL GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Werner Englberger, Babette-Yvonne Koegel
  • Patent number: 5125102
    Abstract: 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: Grant
    Filed: January 3, 1990
    Date of Patent: June 23, 1992
    Assignee: Ericsson GE Mobile Communications Inc.
    Inventors: Jeffrey S. Childress, Marc A. Dissosway, Gerald M. Cooper, Houston H. Hughes, III