Unsaturated Ring Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/144)
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Patent number: 6608082Abstract: Methods for treating erectile dysfunction using tetrahydroisoquinoline aromatic amines that function as melanocortin receptor ligands.Type: GrantFiled: May 6, 1999Date of Patent: August 19, 2003Assignee: Lion Bioscience AGInventors: Amaresh Basu, Timothy C. Gahman, Beverly E. Girten, Michael C. Griffith, Curtis C. Hecht, John S. Kiely, Sandra R. Slivka
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Patent number: 6593322Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially ER-&bgr;. Methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natureal hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: September 21, 2000Date of Patent: July 15, 2003Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah Marie Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Publication number: 20030119870Abstract: The invention relates to compounds of formulae 1Type: ApplicationFiled: October 29, 2002Publication date: June 26, 2003Inventors: Alexander Alanine, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Emmanuel Pinard, Rene Wyler
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Patent number: 6566372Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.Type: GrantFiled: August 24, 2000Date of Patent: May 20, 2003Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Christopher Tegley, Barbara Pio, Cornelis Arjan Van Oeveren, Mehrnouch Motamedi, Esther Martinborough, Sarah West
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Publication number: 20030087901Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: ApplicationFiled: February 27, 2002Publication date: May 8, 2003Applicant: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Qi Chao
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Patent number: 6559146Abstract: There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R1, R2, R3 and R4 are, independent from each other, alkoxy group, alkyl group or aryl group, etc.; E1 and E2 are oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is phenyl group which may be substituted or benzoyl group, etc, or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca2+-binding proteins.Type: GrantFiled: November 1, 2000Date of Patent: May 6, 2003Assignee: Suntory LimitedInventors: Hirokazu Annoura, Naohiro Takemoto, Hiroshi Uramoto
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Patent number: 6555539Abstract: Indazole compounds that modulate and/or inhibit cell proliferation, such as the activity of protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating, e.g., kinases-dependent diseases to modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer as well as other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.Type: GrantFiled: January 18, 2001Date of Patent: April 29, 2003Assignee: Agouron PharmaceuticalsInventors: Siegfried Heinz Reich, Ted Michael Bleckman, Susan Elizabeth Kephart, William Henry Romines, Michael B. Wallace
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Patent number: 6552019Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 11, 2002Date of Patent: April 22, 2003Inventors: John Cochran, Roger Tung
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Publication number: 20030069424Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.Type: ApplicationFiled: November 5, 2001Publication date: April 10, 2003Inventors: Rainer Albert, Nigel Graham Cooke, Sylvain Cottens, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jurgen Wagner, Gerhard Zenke
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Publication number: 20030069243Abstract: Novel 1,4,5 substituted imidazole compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: July 19, 2002Publication date: April 10, 2003Applicant: SmithKline Beecham CorporationInventors: Jerry L. Adams, Ralph F. Hall
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Patent number: 6518266Abstract: The present invention is directed to novel pyrazole derivatives and their use as pesticidal agents. The pyrazole derivatives have Formula I: or a salt thereof, where R1 represents R5O, R5SO2, R5SO or R5S in which R5 is as defined herein; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen, amino, chloro, bromo, iodo, cyano, C1-6 alkoxy, C1-6 alkyl or C6-10 aryl; and R3-R7 each represent hydrogen, halogen, straight- or branched-chain C1-4 alkyl or C1-4 alkoxy, either of which is unsubstituted or substituted by one or more halogen atoms, straight- or branched-chain C1-4 alkylthio or C1-4 alkylsulphinyl, either of which is substituted by one or more halogen atoms, nitro, cyano, or straight- or branched-chain C1-4 alkylsulphonyl group which is unsubstituted or substituted by one or more halogen atoms.Type: GrantFiled: July 21, 2000Date of Patent: February 11, 2003Assignees: 3-Dimensional Pharmaceuticals, Heska CorporationInventors: Daljit S. Dhanoa, Dario Doller, Sanath Meegalla, Richard M. Soll, Nancy Wisnewski, Gary Silver, Dan T. Stinchcomb, R. Lee Seward, Dimitris Agrafiotis, Deyou Sha
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Patent number: 6509467Abstract: A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal neutral hydrocarbyl complex which is coordinated to defined bidentate ligands. Preferred metals include rhodium, ruthenium and iridium. Preferred bidentate ligands are diamines and aminoalcohols, particularly those comprising chiral centers. The hydrogen donor is advantageously a mixture of triethylamine and formic acid. The process can be employed to transfer hydrogenate iminium salts, which are preferably prochiral.Type: GrantFiled: March 21, 2001Date of Patent: January 21, 2003Assignee: Avecia LimitedInventors: Andrew John Blacker, Lynne Alison Campbell
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Patent number: 6482832Abstract: Amides of the general formula I and their tautomeric and isomeric forms, possible enantiomeric and diastereomeric forms, and also possible physiologically tolerated salts, in which the variables have the meanings indicated in the description.Type: GrantFiled: November 15, 2000Date of Patent: November 19, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Publication number: 20020161004Abstract: Compounds, compositions and methods that are useful in the treatment of inflammatory, immunoregulatory, metabolic and cell proliferative conditions or diseases are provided herein. In particular, the invention provides compounds which modulate the expression and/or function of proteins involved in inflammation, metabolism and cell proliferation. The subject compounds contain fused carbocyclic or heterocyclic rings.Type: ApplicationFiled: October 23, 2001Publication date: October 31, 2002Applicant: Syntex (U.S.A.) LLCInventors: Michelle F. Browner, David L. Clark, Timothy D. Cushing, Xiaolin Hao, Ronald C. Hawley, Xiao He, Juan C. Jaen, Sharada S. Labadie, Marie-Louise Smith, Francisco X. Talamas, Nigel P.C. Walker, Marc Labelle
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Patent number: 6452009Abstract: The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R1 to R7, X, Y, Z, b, c and d have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing DHQ derivative compounds.Type: GrantFiled: August 19, 1999Date of Patent: September 17, 2002Assignee: Lion Bioscience AGInventors: Kianoush Motesharei, Michal Lebl, Viktor Krchnak, Yidong Ni
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Patent number: 6436923Abstract: Compounds that modulate the estrogen receptor (ER) are disclosed, as well as pharmaceutical compositions containing the same. In a specific embodiment, the compounds are selective modulators for ER-&bgr; over ER-&agr;. Methods are disclosed for modulating ER-&bgr; in cell and/or tissues expressing the same, including cells and/or tissue that preferentially express ER-&bgr;. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.Type: GrantFiled: March 17, 2000Date of Patent: August 20, 2002Assignee: Signal Pharmaceuticals, Inc.Inventors: Shripad S. Bhagwat, Leah M. Gayo-Fung, Bernd M. Stein, Qi Chao, Anthony R. Gangloff, Jeffrey A. McKie, Kenneth D. Rice
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Patent number: 6407238Abstract: Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.Type: GrantFiled: October 27, 2000Date of Patent: June 18, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: James A. Baron, Vittorio Farina, Nizar Haddad
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Patent number: 6395749Abstract: The present invention provides carboxamine compounds, methods and compositions for inhibiting PARP activity.Type: GrantFiled: September 1, 1998Date of Patent: May 28, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Patent number: 6369053Abstract: 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: April 28, 2000Date of Patent: April 9, 2002Assignee: Neurogen CorporationInventors: Jun Yuan, George D. Maynard, Alan Hutchison
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Publication number: 20020025963Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: 1Type: ApplicationFiled: August 8, 2001Publication date: February 28, 2002Inventors: Patrick Y. Lam, Charles G. Clark, Celia Dominguez, John M. Fevig, Qi Han, Renhua Li, Donald Jp Pinto, James R. Pruitt, Mimi L. Quan
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Patent number: 6339093Abstract: The present invention relates to compounds of the formula wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, amino, nitro, cyano, lower alkyl-amino, di-lower alkyl-amino or halogen; R2 is hydrogen, lower alkyl, amino, pyrrolidin-3-ol, pyrrolidin-2-yl-methanol or —NHCH2CHROH; R3 is hydrogen or halogen; R is hydrogen, lower alkyl or —CH2OH; n is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof which are are NMDA(N-methyl-D-aspartate)-receptor subtype selective blockers.Type: GrantFiled: September 26, 2000Date of Patent: January 15, 2002Assignee: Hoffmann-la Roche Inc.Inventors: Alexander Alanine, Serge Burner, Bernd Buettelmann, Marie-Paule Heitz Neidhart, Georg Jaeschke, Emmanuel Pinard, René Wyler
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Patent number: 6319931Abstract: The present invention relates in particular to a combination product comprising at least one compound with affinity for the mitochondrial benzodiazepine receptor, and to at least one apoptosis-inducing agent for simultaneous or separate use or for use spread out over time, which is intended for the treatment of cancer. Another aspect of the present invention relates to the use of the said compound and/or of the said combination product for the manufacture of a medicinal product intended to facilitate the induction of apoptosis.Type: GrantFiled: June 14, 1999Date of Patent: November 20, 2001Assignee: Centre National de al Recherche Scientifique (CNRS)Inventors: Guido Kroemer, Tamara Hirsch, Didier Decaudin
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Patent number: 6303785Abstract: Compounds having Formula 3 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: October 16, 2001Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Roshantha A. Chandraratna
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Patent number: 6303782Abstract: A process is described for preparing an aromatic compound substituted by a tertiary nitrile of Formula (1.0.0): comprising treating a substituted aromatic compound of Formula (2.0.0): with a secondary nitrile of Formula (3.0.0): in the presence of a base having a pKa numerical value in the range of from about 17 to about 30, provided that the difference in pKa numerical values between said base and the corresponding tertiary nitrile of Formula (3.0.0) is no more than about 6; in an aprotic solvent having a dielectric constant (∈) of less than about 20; and at a reaction temperature in the range of from about 0° C. to about 120° C.; whereby there is formed said tertiary-nitrile-substituted aromatic compound final product of Formula (1.0.0); wherein the constituent parts W1, W2, W3, W4, and W5; and the substituent moieties R1, R2, R3, R4, R5, R6, and R7 in the compounds of Formulas (1.0.0), (2.0.0) and (3.0.Type: GrantFiled: March 1, 2000Date of Patent: October 16, 2001Assignee: Pfizer IncInventor: Stéphane Caron
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Patent number: 6297257Abstract: Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by certain substituents and necessarily substituted by a —B—Cy group where the variables are as defined in the specification and the N→O derivatives and pharmaceutically acceptable salts thereof are phosphodiesterase-4 inhibitors.Type: GrantFiled: July 13, 2000Date of Patent: October 2, 2001Assignee: Zambon Group S.p.A.Inventors: Mauro Napoletano, Gabriele Norcini, Daniela Botta, Giancarlo Grancini, Gabriele Morazzoni
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Patent number: 6242450Abstract: This invention provides 5-HT1f antagonists of Formula I: where AR1, AR2, R, and R′ are as defined in the specification.Type: GrantFiled: June 17, 1999Date of Patent: June 5, 2001Assignee: Eli Lilly and CompanyInventors: Daniel James Koch, Lee Alan Phebus, Vincent Patrick Rocco, Tammy Joy Sajdyk
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Patent number: 6221604Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.Type: GrantFiled: February 7, 2000Date of Patent: April 24, 2001Assignee: PE CorporationInventors: Krishna G. Upadhya, Steven M. Menchen, Weiguo Zhen
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Patent number: 6218537Abstract: 1,4,5,-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: May 13, 1998Date of Patent: April 17, 2001Assignee: SmithKline Beecham CorporationInventors: Jerry Leroy Adams, Timothy Francis Gallagher, Joseph Sisko, Irennegbe Kelly Osifo, Jeffrey Charles Boehm
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Patent number: 6214996Abstract: Naphthalene derivatives of the formula [I]: wherein R1 and R2 are the same or different and are each H, protected or unprotected OH, one of R3 and R4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R5 and R6 are, the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.Type: GrantFiled: December 1, 1998Date of Patent: April 10, 2001Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
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Patent number: 6207715Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.Type: GrantFiled: November 22, 1999Date of Patent: March 27, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6187789Abstract: Ultrashort acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein: X is a halogen; h is from 1 to 2; Y is hydrogen or methoxy; Z1 and Z2 are methyl; W1 and W2 are carbon; and A is a pharmaceutically acceptable anion.Type: GrantFiled: January 19, 2000Date of Patent: February 13, 2001Assignees: Glaxo Wellcome Inc., Cornell Research Foundation Inc.Inventors: Eric Cleveland Bigham, Grady Evan Boswell, John Joseph Savarese, Roy Archibald Swaringen, Jr., Sanjay Shashikant Patel, Eric Eugene Boros, Robert Anthony Mook, Jr., Vincente Samano
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Patent number: 6177443Abstract: The present invention relates to pharmaceutical compositions comprising a pharmaceutically acceptable carrier or diluent and a compound of formula I wherein A together with the double bond of formula I is benzene or thiophene; R1 is optionally substituted C1-6 alkyl or optionally substituted aryl; R2 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or —COR3, wherein R3 is optionally substituted C1-6-alkyl, optionally substituted aralkyl, or optionally substituted aryl; R4 and R5 independently are hydrogen, halogen, perhalomethyl, optionally substituted C1-6-alkyl, hydroxy, optionally substituted C1-6-alkoxy, nitro, cyano, amino, optionally substituted mono- or optionally substituted di-C1-6-alkylamino, acylamino, C1-6-alkoxycarbonyl, carboxy or carbamoyl; n is 0, and m is 1, and methods of treating or preventing a disease of the endocrinologic system.Type: GrantFiled: March 5, 1998Date of Patent: January 23, 2001Assignee: Novo Nordisk A/SInventors: Peter Madsen, Jane Marie Lundbeck, Niels Westergarrd, Lars Naerum, Annemarie Reinhardt Varming, Helle Demuth, Morten Heide
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Patent number: 6177445Abstract: Ultra short acting neuromuscular blocking agents of Formula (I) which are useful as skeletal muscle relaxants during emergency intubation procedures, routine surgery and post-operative settings are disclosed, wherein q and t are independently from 0 to 4; X1 and X2 are independently halogen; ha and hb are independenity from 0 to 2; Z1 and Z2 are indepentdently hydrogen, C1-6 alkyl, C2-6 alkenyl or C2-6 alkynyl with the proviso that Z1 and Z2 are not both hydrogen; Y1, Y2, and Y3 and Y4 are independently hydrogen, halogen or C1-3 alkoxy; m and p are independently 1 to 6; n and r are independently 0 to 4; with the proviso the if ha and hb are both 0, then r is 0 and n is 0 to 2; R1 to R14 are independently hydrogen, halogen, C1-3 alkoxy, or R2 and R3 together with the carbon atoms to which they are bonded, R5 and R6 together with the carbon atoms to which they are bonded, R9 and R10 together with the carbon atoms to which they are bonded, R12 and R13 together with the carbon atoms to which they are bonded, mayType: GrantFiled: December 22, 1999Date of Patent: January 23, 2001Assignees: Glaxo Wellcome Inc., Cornell Research Foundation Inc.Inventors: Eric Cleveland Bigham, Grady Evan Boswell, John Joseph Savarese, Roy Archibald Swaringen, Jr., Sanjay Shashikant Patel, Eric Eugene Boros, Robert Anthony Mook, Jr., Vincente Samano
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Patent number: 6174901Abstract: Selected novel substituted pyridine and pyridazine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as cancer, pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, cancer, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 18, 1998Date of Patent: January 16, 2001Assignee: Amgen Inc.Inventors: Nathan B. Mantlo, Chan-Kou Hwang, Ulrike D. Spohr
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Patent number: 6166041Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The present invention is directed to compounds having the general formula I ##STR1## wherein: X is a halogen;Q is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, a single or a double bond, or --NR.sub.1 --;R.sub.1 is a C.sub.Type: GrantFiled: November 3, 1997Date of Patent: December 26, 2000Assignee: Euro-Celtique, S.A.Inventors: David J. Cavalla, Mark Chasin, John W F Whitehead, Lesley Walton, Andrew C. Mansfield
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Patent number: 6159985Abstract: The subject invention involves compounds having the structure: wherein the C.sub..alpha. --N.sub..beta. and C.sub.5 -C.sub.6 bonds are independently single or double bonds, R1 is selected from alkyl, aryl, and heterocycle; R2-R13 are independently selected from hydrogen and other substituents; and pharmaceutically-acceptable salts thereof. The subject invention also involves pharmaceutical compositions containing such compounds, and methods for treating or preventing diseases and disorders using such compounds.Type: GrantFiled: September 21, 1999Date of Patent: December 12, 2000Assignee: The Procter & Gamble CompanyInventors: Song Liu, David Edward Portlock, Schwe Fang Pong
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Patent number: 6153622Abstract: Compounds of this formula ##STR1## are useful for treating or preventing, obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease and prostatic disease.Type: GrantFiled: August 28, 1998Date of Patent: November 28, 2000Assignee: Pfizer, Inc.Inventors: Kimberly O. Cameron, Paul A. Dasilva-Jardine, Hua Zhu Ke, Robert L. Rosati
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Patent number: 6127381Abstract: The invention relates to melanocortin receptor ligands and methods of using the ligands to alter or regulate the activity of a melanocortin receptor. The invention further relates to tetrahydroisoquinoline aromatic amines that function as melanocortin receptor ligands and as agents for controlling cytokine-regulated physiologic processes and pathologies, and combinatorial libraries thereof.Type: GrantFiled: April 28, 1999Date of Patent: October 3, 2000Inventors: Amaresh Basu, Timothy C. Gahman, Beverly E. Girten, Michael C. Griffith, Curtis C. Hecht, John S. Kiely, Sandra R. Slivka
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Patent number: 6100276Abstract: This application relates to compounds of the formula ##STR1## wherein R, X and Y are defined within, which compounds are useful for the treatment of memory dysfunction characterized by decreased cholinergic function, and for analgesia, pharmaceutical compositions containing the compounds and methods for making and using the compounds.Type: GrantFiled: February 24, 1997Date of Patent: August 8, 2000Assignee: Aventis Pharmaceuticals Inc.Inventors: Stephen J. Shimshock, Susan M. Chesson, Abdul E. Mutlib
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Patent number: 6034240Abstract: Novel aminomethylphosphine ligands have particular substituents on the central carbon atom. Such ligands form coordination complexes that may be catalysts for the polymerization of monomers or other catalytic induced reactions.Type: GrantFiled: March 9, 1998Date of Patent: March 7, 2000Assignee: Symyx Technologies, Inc.Inventor: Anne Marie La Pointe
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Patent number: 6031106Abstract: A process for preparing pyridyl-substituted N-phenylhydroxylamines by catalytic hydrogenation of the corresponding nitro compounds in the presence of an N-substituted morpholine compound and rearrangement of the hydroxylamine compounds obtained to pyridyl-4-fluoraniline compounds is described.Type: GrantFiled: September 14, 1998Date of Patent: February 29, 2000Assignee: BASF AktiengesellschaftInventors: Albrecht Harreus, Norbert Gotz, Michael Rack, Heinz Isak, Peter Schafer
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Patent number: 6028080Abstract: The invention relates to quinoline-2-(1H)-one derivatives of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are in each case independently of one another H, Hal, A or OA; R.sup.4 is H, --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 ; R.sup.5 is H, --(CH.sub.2).sub.n --NR.sup.6 R.sup.7 ; R.sup.6 is H, A or, together with R.sup.7, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sup.7 is H, A or --(CH.sub.2).sub.m -- with a bond to the same ring or adjacent ring B or D or, together with R.sup.6, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; X is --CHR.sup.5 --, --NR.sup.5 --, --O--, --S--; A is alkyl having 1-6 C atoms; Hal is F, Cl, Br or I; m is 1-3 and n is 0-3, where at least one of the two radicals R.sup.4 or R.sup.5 has the meaning --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 or --(CH.sub.2).sub.n --NR.sup.6 R.sup.7, their enantiomers, stereoisomers, salts and solvates. Such compounds are useful for the treatment of neurodegenerative diseases.Type: GrantFiled: July 17, 1998Date of Patent: February 22, 2000Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Karl-August Ackermann, Rudlof Gottschlich, Gunter Holzemann, Joachim Leibrock, Wilfried Rautenberg, Christoph Seyfried
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Patent number: 6015900Abstract: Disclosed are compounds of formula (I) or the pharmaceutically acceptable salts thereof wherein: ##STR1## G represents a group of the formula (a), (b) or (c) where R.sub.a and R.sub.b represent hydrogen, or organic or inorganic substituents; A is an optionally substituted alkylene; R.sub.1, R.sub.2, R.sub.3, R.sub.4 represent organic or inorganic substituents; R.sub.5 is hydrogen or lower alkyl; R.sub.6 and R.sub.7 independently represent hydrogen, lower alkyl; or together form a ring of 5-8 members; Z is nitrogen or carbon; and W is optionally susbtituted aryl or heteroaryl. Compounds of the present invention demonstrate high affinity and selectivity in binding to the D.sub.3 receptor subtype.Type: GrantFiled: November 23, 1998Date of Patent: January 18, 2000Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 6011037Abstract: Compounds having the formula (I): ##STR1## wherein R1, R2, R3, R4, R5 and n have the meanings given in the description. The compounds of formula (I) are selective inhibitors of phosphodiesterase IV.Type: GrantFiled: February 26, 1999Date of Patent: January 4, 2000Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventors: Thomas Bar, Wolf-Rudiger Ulrich
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Patent number: 5998087Abstract: A silver halide photographic material is disclosed containing a new type of hydrazide compounds represented by following general formula I, the different symbols of which are defined in the description. ##STR1## In a preferred embodiment Q is chosen from pyridinium, quinolinium or isoquinolinium. In a most preferred embodiment Q is a pyridinium substituted on the N.sup.+ with a C.sub.5 to C.sub.8 alkyl group.The photographic material is preferably a graphic arts recording material. High gradation and excellent hard dot quality are obtained.Type: GrantFiled: January 22, 1999Date of Patent: December 7, 1999Assignee: Agfa-Gevaert, N.V.Inventors: Johan Loccufier, Stefaan Lingier, Sabine Emmers, Jean-Marie Dewanckele, Pierre De Clercq, Noel Hosten, Dirk Van Haver
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Patent number: 5990305Abstract: Disclosed is a photochromic compound having a diaryl-3H-napthopyran structure, which has at the 8-position a nitrogen atom-linked hetercyclus, in which the heterocylcus can also have a HALS compound as a substituent or the heterocyclus itself can be formed as a HALS compound.Furthermore a photochromic compound is described having a diaryl-3H-naphtopyran structure which has at the 8-position an N-atom linked and an alkyl-bridge linked HALS compound.Type: GrantFiled: February 5, 1998Date of Patent: November 23, 1999Assignee: Optische Werke G. RodenstockInventors: Herbert Zinner, Manfred Melzig
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Patent number: 5972972Abstract: A class of novel pyrazoles is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: December 3, 1997Date of Patent: October 26, 1999Assignee: Eli Lilly and CompanyInventors: Edward D. Mihelich, Tulio Suarez, Gary A. Hite, Peter J. Doman, Stuart E. Willetts
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Patent number: 5968949Abstract: According to the present invention, there is provided a compound, or a solvate or salt thereof of formula (I): ##STR1## Substituted hydroisoquinoline derivatives are potent and selective delta opioid agonists and antagonists and are of potential therapeutic utility as inter alia analgesics.Type: GrantFiled: May 29, 1998Date of Patent: October 19, 1999Assignee: SmithKline Beecham S.p.A.Inventors: Giulio Dondio, Silvano Ronzoni
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler
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Patent number: RE37729Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler