Tricyclo Ring System Having The 1,2-diazine Ring As One Of The Cyclos Patents (Class 544/234)
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Patent number: 6528649Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein n, R1, R2, R3, W, Q, and X are defined herein, which compounds bind with high selectivity and high affinity to the benzodiazepine site of the GABAA receptors and are therefore useful in the treatment of certain central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples.Type: GrantFiled: May 29, 2001Date of Patent: March 4, 2003Assignee: Neurogen CorporationInventors: Guolin Cai, Kenneth Shaw
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Patent number: 6525055Abstract: Tricyclic phthalazine compounds of formula (I) wherein A is a 5-7 membered heterocycle containing from 1 to 4 nitrogen atoms, optionally partially or totally unsaturated, and optionally substituted by a (C1-4)alkyl group in turn optionally substituted; Z is NH, methylene, a C2-6 alkylene chain optionally branched and/or unsaturated and/or interrupted by a C5-7 cycloalkyl residue; Cy is phenyl or heterocycle optionally substituted by one or more substituents, or a COR4 group wherein R4 is hydroxy, alkoxy, amino optionally substituted by one or two (C1-6)alkyl groups or by hydroxy; R is a (C1-6)alkyl or polyfluoro(C1-6)alkyl group; R1 is hydrogen; a (C1-8)-alkyl, (C2-8)-alkenyl or (C2-8)-alkynyl group optionally substituted by hydroxy, oxo, aryl or heterocycle, and optionally interrupted by one or more heteroatoms or heterogroups; a (C1-4)alkoxy group or a (C4-7)cycloalkoxy group optionally containing an oxygen atom and optionally substituted by a polar substituent in the cyclic moiety, aryloxType: GrantFiled: April 30, 2001Date of Patent: February 25, 2003Assignee: Zambon Group S.p.A.Inventors: Mauro Napoletano, Gabriele Norcini, Franco Pellacini, Gabriele Morazzoni
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Publication number: 20020187983Abstract: Methods of preparing compounds of Formula I 1Type: ApplicationFiled: May 14, 2002Publication date: December 12, 2002Applicant: WyethInventors: Anita W. Chan, Timothy T. Curran, Silvio Iera, Warren Chew, John H. Sellstedt, Galina Vid, Gregg Feigelson, Zhixian Ding
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Publication number: 20020183326Abstract: Heterocyclic compounds of formula (I), 1Type: ApplicationFiled: January 8, 2002Publication date: December 5, 2002Applicant: ALMIRALL PRODESFARMA, S.A.Inventors: Jordi Gracia Ferrer, M. Isabel Crespo Crespo, Armando Vega Noverola, Andres Fernandez Garcia
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Publication number: 20020165203Abstract: N-Heterocyclic derivatives of the formula (I): 1Type: ApplicationFiled: April 12, 2002Publication date: November 7, 2002Applicant: Berlex Laboratories, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Publication number: 20020164287Abstract: Novel azo compounds and their bioconjugates for phototherapy and/or photodiagnosis of tumors and other lesions. The azo derivatives of the present invention are designed to absorb at the low-energy ultraviolet, visible, or near-infrared (NIR) region of the electromagnetic spectrum. The phototherapeutic effect is caused by direct interaction of free radicals, the reactive intermediate produced upon photoexcitation of the azo compound, with the tissue of interest.Type: ApplicationFiled: May 4, 2001Publication date: November 7, 2002Applicant: MALLINCKRODT INC.Inventors: Raghavan Rajagopalan, Gary L. Cantrell, Joseph E. Bugaj, Samuel I. Achilefu, Richard B. Dorshow
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Patent number: 6465462Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof are useful in enhancing cognition.Type: GrantFiled: January 14, 1999Date of Patent: October 15, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Angus Murray MacLeod, Ruth McKernan, Austin John Reeve, Francine Sternfeld, Leslie Joseph Street
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Patent number: 6458802Abstract: Compounds of the formula: are useful for the treatment of depression (including but not limited to major depressive disorder, childhood depression and dysthymia), anxiety, panic disorder, post-traumatic stress disorder, premenstrual dysphoric disorder (also known as pre-menstrual syndrome), attention deficit disorder (with and without hyperactivity), obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, obesity, eating disorders such as anorexia nervosa, bulimia nervosa, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction and related illnesses.Type: GrantFiled: March 12, 2002Date of Patent: October 1, 2002Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Patent number: 6451795Abstract: 4-Oxo-3,5-dihydro-4H-pyridazino[4,5-b]indole-1-carboxamide derivatives having affinity for the peripheral benzodiazepine receptors are useful for the prevention or treatment of peripheral neuropathies and for the treatment of central neurogenerative diseases.Type: GrantFiled: July 25, 2001Date of Patent: September 17, 2002Assignee: Sanofi-SynthelaboInventors: Frank Marguet, Jacques Froissant, Régine Bartsch-Li, Benoît Marabout, Mireille Sevrin
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Patent number: 6448249Abstract: A substituted triazolopyridazine derivative, its use in cognition enhancement therapy, compositions containing it and processes for its manufacture.Type: GrantFiled: July 24, 2000Date of Patent: September 10, 2002Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
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Publication number: 20020119975Abstract: Disclosed are novel compounds of formula (I): 1Type: ApplicationFiled: August 2, 2001Publication date: August 29, 2002Inventors: Roger John Snow, Donghong A. Gao, Daniel R. Goldberg, Abdelhakim Hammach, Daniel Kuzmich, Tina Marie Morwick, Neil Moss, Anthony S. Prokopowicz, Robert D. Selliah, Hidenori Takahashi
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Patent number: 6441167Abstract: This invention relates to novel compounds that can complex with lanthanide cations, processes for their preparation and the use of the resulting lanthanide chelates as biomolecular probes.Type: GrantFiled: February 16, 2001Date of Patent: August 27, 2002Assignee: SmithKline Beecham plcInventors: Colin Andrew Leach, Keith James Millan Moore, Steven James Stanway
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Patent number: 6429311Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4 (1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: February 1, 2001Date of Patent: August 6, 2002Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6423716Abstract: The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc. ), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N—R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C—RA; and D1, D2, D3 and D4 each independently represent C—RB, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N—R2A, an oxygen atom, a sulfur atom, etc.Type: GrantFiled: September 29, 2000Date of Patent: July 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Kenji Matsuno, Yuji Nomoto, Michio Ichimura, Shin-ichi Ide, Shoji Oda
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Patent number: 6407108Abstract: Heterocyclic compounds of formula(I), wherein R1 represents a hydrogen atom or a —(CH2)m—Y group, wherein m is an integer from 0 to 4 and Y represents an alkyl, haloalkyl, alkoxy, alkoxycarbonyl, C3-C7 cycloalkyl, norbornyl or phenylalkenyl group, or an aromatic group which aromatic group {circumflex over ( )} may optionally be substituted by one or more halogen atoms; R2 represents an aromatic group which aromatic group may optionally be substituted by one or more halogen atoms or alkyl, alkoxy, C3-C6 cycloalkoxy, methylenedioxy, nitro, dialkylamino or trifluoromethyl groups, and R3 represents a hydrogen or halogen atom or an alkyl group, and pharmaceutically acceptable salts thereof, processes for preparing the same are disclosed herein. The compounds are phosphodiesterase 4 inhibitors.Type: GrantFiled: January 28, 2000Date of Patent: June 18, 2002Assignee: Almirall Prodesfarma, S.A.Inventors: Jordi Gracia Ferrer, Ma Isabel Crespo Crespo, Armando Vega Noverola, Andres Fernandez Garcia
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Patent number: 6380193Abstract: A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.Type: GrantFiled: September 1, 1998Date of Patent: April 30, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Jia-He Li, Jie Zhang
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Publication number: 20020045623Abstract: This invention provides novel caspase inhibitors of formula I: 1Type: ApplicationFiled: June 7, 2001Publication date: April 18, 2002Inventors: Jean-Damien Charrier, Guy Brenchley
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Patent number: 6365598Abstract: A chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 is selected from hydrogen, alkyl, alkoxy, formyl and cyano; X1 is selected from N and C—R7; X2 is selected from N and C—R8; X3 is selected from N and C—R9; X4 is selected from N and C—R10; wherein at least one of X1, X2, X3 and X4 is N; and R5 to R10 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardType: GrantFiled: March 1, 2001Date of Patent: April 2, 2002Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Jonathan Richard Anthony Roffey, Corinna Dagmar Bodkin, Howard Langham Mansell, Ashley Roger George, Ian Anthony Cliffe
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Publication number: 20020028815Abstract: The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.Type: ApplicationFiled: May 8, 2001Publication date: March 7, 2002Inventors: Mark A. Ator, Ron Bihovsky, Sankar Chatterjee, Derek Dunn, Robert L. Hudkins
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Publication number: 20020025959Abstract: The present invention provides a compound of formula I 1Type: ApplicationFiled: June 22, 2001Publication date: February 28, 2002Inventors: David John Anderson, Thomas J. Beauchamp, Gordon L. Bundy, Fred L. Ciske, John R. Farrell, David R. Graber, Michael J. Genin, Thomas M. Judge, Malcolm Wilson Moon, Mark E. Schnute, Joseph Walter Strohbach, Suvit Thaisrivongs, Atli Thorarensen, Steven Robert Turner, Valerie A. Vaillancourt, Allison J. Wolf
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Patent number: 6348463Abstract: Phenylalanine derivatives of formula (1) are described: in which: Ar1 is an aromatic or heteroaromatic group; L1 is a linker atom or group; R is a carboxylic acid or a derivative thereof; Ar2 is an optionally substituted aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: September 27, 1999Date of Patent: February 19, 2002Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, John Robert Porter, Graham John Warrellow, Sarah Catherine Archibald, Brian Woodside Hutchinson
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Patent number: 6331640Abstract: A compound of formula 1a which is useful for treating reperfusion injury, and salts, prodrugs, and related compounds.Type: GrantFiled: September 29, 1999Date of Patent: December 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Paul Gillespie, Robert William Guthrie, Sherrie Lynn Pietranico-Cole, Weiya Yun
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Patent number: 6329372Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: January 26, 1999Date of Patent: December 11, 2001Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
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Publication number: 20010049439Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.Type: ApplicationFiled: November 30, 2000Publication date: December 6, 2001Applicant: Merck & Co., Inc.Inventors: Michael J. Kaufman, James A. McCauley, Daniel J. Rush, David M. Tschaen, Richard J. Varsolona, Guo-Jie Ho
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Patent number: 6316438Abstract: Compounds of the formula are useful as inhibitors of cGMP PDE especially Type 5.Type: GrantFiled: March 15, 2000Date of Patent: November 13, 2001Assignee: Bristol-Myers Squibb Co.Inventors: Guixue Yu, John Macor, Soojin Kim, Hyei-Jha Chung, Michael Humora, Kishta Katipally, Yizhe Wang
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Patent number: 6313125Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives are ligands for GABAA receptors useful in the treatment of disorders of dementing illnesses.Type: GrantFiled: January 14, 2000Date of Patent: November 6, 2001Assignee: Merck Sharp & Dohme Ltd.Inventors: William Robert Carling, Kevin William Moore, Austin John Reeve
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Precursor compounds to substituted 1,2,4-triazolo[3,4,-a]phathalazine GABA alpha 5 ligands
Patent number: 6310203Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives that are GABA Alpha 5 ligands are prepared from compounds represented by the formula: in which R1 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; R2 is hydrogen, halogen, CF3, OCF3, CN or an optionally substituted C1-4alkyl, C2-4alkenyl, C2-4alkynyl, C1-4alkoxy, C2-4alkenyloxy or C2-4alkynyloxy group; Z is an optionally substituted 5-membered or 6-membered heteroaromatic ring; and G is a leaving group.Type: GrantFiled: April 11, 2000Date of Patent: October 30, 2001Assignee: Merck Sharpe & Dohme LimitedInventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street -
Patent number: 6297252Abstract: Disclosed are compounds of compounds of the formula: or the pharmaceutically acceptable nontoxic salts thereof wherein: X is oxygen, H2 or sulfur Y is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups; W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; or W is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; and Z1, Z2, Z3, and Z4 independently represent nitrogen or C—R1 where R1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.Type: GrantFiled: July 19, 2000Date of Patent: October 2, 2001Assignee: Neurogen CorporationInventors: Paul Chen, Alan Hutchison, Guolin Cai
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Patent number: 6288185Abstract: Initiators for free-radical addition polymerization comprising as structural feature the Diels-Alder adduct of an azo group (—N═N—) with a conjugated double bond (diene).Type: GrantFiled: October 3, 2000Date of Patent: September 11, 2001Assignee: BASF AktiengesellschaftInventors: Rainer Königer, Reinhold Schwalm, Roman Benedikt Raether
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Patent number: 6262045Abstract: Compounds of general formula (I) in which X represents a hydrogen or halogen atom or a methyl, methoxy or phenylmethoxy group, Y represents a hydrogen atom, 1 or 2 halogen atoms or a hydroxyl, methoxy, nitro or methyl group, R1 represents a hydrogen atom or a (C1-C4)alkyl group, R2 and R3 each represent a hydrogen atom, a (C1-C4)alkyl group or a phenylmethyl group or else R2 and R3 form, with the nitrogen atom which carries them, an azetidinyl, pyrrolidinyl, 3-ethoxypyrrolidinyl, piperidinyl, morpholinyl, 4-methylpiperazinyl or 1,3-thiazolidinyl group. Application in therapeutics.Type: GrantFiled: April 13, 2000Date of Patent: July 17, 2001Assignee: Sanofi-SynthelaboInventors: Yannick Evanno, Laurent Dubois, Mireille Sevrin, Frank Marguet, Jacques Froissant, Régine Bartsch, Catherine Gille
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Publication number: 20010007869Abstract: The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: 1Type: ApplicationFiled: November 16, 1998Publication date: July 12, 2001Inventors: THOMAS MICHAEL BARE, JAMES ROY EMPFIELD, JANET MARIE FORST, KEITH JOHN HERZOG, RICHARD BRUCE SPARKS
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Patent number: 6255305Abstract: Substituted triazolo-pyridazine derivative compounds represented by wherein the variables are disclosed herein are selective ligands for GABA-A receptors, particularly for the &agr;2 and/or &agr;3 subunits.Type: GrantFiled: November 10, 1998Date of Patent: July 3, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, William Robert Carling, Jose Luis Castro Pineiro, Alexander Richard Guiblin, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Leslie Joseph Street
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Patent number: 6232313Abstract: The present invention relates to compounds, pharmaceutical compositions and methods of using compounds having the formula below in the treatment and prevention of certain diseases or conditions. Where the ring designated A is chosen from ortho substituted aryl or heteroaryl species, R1 and R2 are chosen independently from —(CH2)nL where L is selected from a variety of substituents including hydrogen, and aryl, heteroaryl or heterocyclic groups and R4 is chosen from a variety of substituents including halogen and alkyl groups. The compounds are useful in treating and preventing neurological disorders associated with excitatory amino acids.Type: GrantFiled: March 19, 1998Date of Patent: May 15, 2001Assignee: Zeneca LimitedInventors: Thomas Michael Bare, Timothy Wayne Davenport, James Roy Empfield, Jeffrey Alan McKinney, Richard Bruce Sparks
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Patent number: 6214826Abstract: The invention relates to pyridazinoquinoline compounds of the formulas B and B′ wherein Ring A is selected from an ortho fused aromatic or heteroaromatic five- or six-membered ring and R1, R3 and R4 are substituents selected from halo, OH, OCF3, NO2, CN, NR′R″, SO2NR′R″, SOmR′alkyl, and a variety of alkyl, aryl, heterocyclic and heteroaryl groups, to pharmaceutical compositions containing them and to methods utilizing them for the treatment of neurological disorders.Type: GrantFiled: August 2, 1999Date of Patent: April 10, 2001Assignee: Zeneca LimitedInventors: Thomas Michael Bare, Marc Jerome Chapdelaine, Timothy Wayne Davenport, James Roy Empfield, Laura Enid Garcia-Davenport, Paul Francis Jackson, Jeffrey Alan McKinney, Charles David McLaren, Richard Bruce Sparks
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Patent number: 6200975Abstract: Substituted 1,2,4-Triazolo[3,4-A]phthalazine derivatives are GABA Alpha 5 ligands and are represented by the formulaType: GrantFiled: November 12, 1998Date of Patent: March 13, 2001Assignee: Merck Sharp & Dohme LimitedInventors: William Robert Carling, Tamara Ladduwahetty, Angus Murray MacLeod, Kevin John Merchant, Kevin William Moore, Francine Sternfeld, Leslie Joseph Street
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Patent number: 6184377Abstract: The present invention is directed to certain N-amino- and N-hydroxy-quinazolinone compounds and synthetic methods for synthesis thereof, which compounds may find use in combinatorial libraries. More specifically, the invention is directed to the synthesis of 3-hydroxy- and 3-amino-4(1H)-quinazolinones via the reaction of an appropriate 2-aminobenzamide compound with a carboxylic acid or acyl halide at ambient temperature performed on a solid support or in solution.Type: GrantFiled: December 15, 1997Date of Patent: February 6, 2001Assignee: Sepracor Inc.Inventor: Yun Gao
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Patent number: 6180630Abstract: Pyrazolo[4,3-c]pyridazin-3-one analogues, represented by are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.Type: GrantFiled: December 8, 1999Date of Patent: January 30, 2001Assignee: Merck Sharp & Dohme LimitedInventors: Peter Blurton, Stephen Robert Fletcher
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Patent number: 6177379Abstract: A method of initiating free-radical addition polymerization, which entails effecting a free-radical addition polymerization in the presence of an initiator, which contains, as a structural feature, a Diels-Alder adduct of an azo group (—N═N—) with a conjugated double bond (diene).Type: GrantFiled: May 18, 1998Date of Patent: January 23, 2001Assignee: BASF AktiengesellschaftInventors: Rainer Königer, Reinhold Schwalm, Roman Benedikt Raether
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Patent number: 6172170Abstract: Initiators for free-radical addition polymerization comprising as structural feature the Diels-Alder adduct of an azo group (—N═N—) with a conjugated double bond (diene).Type: GrantFiled: December 27, 1999Date of Patent: January 9, 2001Assignee: BASF AktiengesellschaftInventors: Rainer Königer, Reinhold Schwalm, Roman Benedikt Raether
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Patent number: 6147080Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The compounds are of the class of pyrido [1,2-c] pyrimidin-3-one or 1,2-dihydro-pyrido [1,2-c] pyrimidin-3-one derivatives, useful as inhibitors of p38. 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 10, 1997Date of Patent: November 14, 2000Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, Edmund Martin Harrington
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Patent number: 6143890Abstract: Hydrazam imides of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are each independently of the other (a) hydrogen or nitro, at least one of which radicals being nitro, or R.sup.1 and R.sup.2 together are (b) one of the following radicals ##STR2## wherein B is ##STR3## and R.sup.5 is C.sub.1 -C.sub.18 alkyl or R.sup.3 or R.sup.4, in which case R.sup.1 and R.sup.2 are bound to the compound of formula I in the positions a and b,R.sup.3 and R.sup.4 are each independently of the other unbranched C.sub.1 -C.sub.10 alkyl, and processes for their preparation and their use.Type: GrantFiled: December 16, 1999Date of Patent: November 7, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Heinz Langhals, Rami Ismael
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Patent number: 6136827Abstract: The present invention is directed to cyclic amines of the formula I: ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, m and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-1, CCR-2, CCR-2A, CCR-2B, CCR-3, CCR-4, CCR-5, CXCR-3, and/or CXCR-4.Type: GrantFiled: July 21, 1998Date of Patent: October 24, 2000Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Paul E. Finke, Malcolm Maccoss, Laura C. Meurer, Sander G. Mills, Bryan Oates
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Patent number: 6121278Abstract: A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein:Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, heterocyclic ring containing at least one nitrogen heteroatom in a 1,3-relationship with the nitrogen atom depicted in formula I, wherein Y may be unsubstituted or substituted with at least one alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, or --COOR.sup.5 group, or a moiety selected from the group consisting of: ##STR2## wherein R.sup.5 and R.sup.7 are independently hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl.Type: GrantFiled: September 1, 1998Date of Patent: September 19, 2000Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Keith M. Maclin, Jie Zhang
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Patent number: 6103731Abstract: Disclosed are compounds of compounds of the formula: or the pharmaceutically acceptable nontoxic salts thereof wherein:X is oxygen, H.sub.2 or sulfurY is hydrogen, or optionally substituted alkyl, alkenyl, (substituted)arylalkyl, aryl or heteroaryl, or a carbonyl group substituted with alkyl, cycloalkyl, aryl, or amino groups;W is alkyl, arylalkyl or heteroarylalkyl, where each aryl group is optionally substituted with up to two groups; orW is aryl, thienyl, pyridyl or heteroaryl, each of which is optionally substituted; andZ.sub.1, Z.sub.2, Z.sub.3, and Z.sub.4 independently represent nitrogen or C-R.sub.1 where R.sub.1 is hydrogen, halogen, hydroxy, amino, or phenyl or pyridyl optionally mono- or independently disubstituted with halogen, hydroxy, lower alkyl, or lower alkoxy,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists or inverse agonists for GABAa brain receptors.Type: GrantFiled: August 11, 1998Date of Patent: August 15, 2000Assignee: Neurogen CorporationInventors: Paul Chen, Alan Hutchison, Guolin Cai
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Patent number: 6103721Abstract: The present invention concerns compounds according to the following formula, ##STR1## wherein: R.sup.1 is (CH.sub.2).sub.n,L where n is an integer in the range 0 to 6, and L is a carbon-linked five-membered heteroaryl ring having an oxygen or sulfur heteroatom, R.sup.4 is hydrogen, halo or NO.sub.2, and pharmaceutical compositions and methods of using thereof in the treatment and/or prevention of neurological diseases or conditions.Type: GrantFiled: December 6, 1999Date of Patent: August 15, 2000Assignee: Zeneca LimitedInventors: Thomas Michael Bare, Timothy Wayne Davenport, James Roy Empfield, Jeffrey Alan McKinney, Richard Bruce Sparks
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Patent number: 6093821Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: July 25, 2000Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L. F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 6057329Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): ##STR1## wherein Ar is an optionally substituted aromatic or heteroaromatic group;X is a carbon or nitrogen atom;Y is a carbon or nitrogen atom;Z is a linker group;A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group;and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56.sup.lck and p59.sup.fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56.sup.lck and/or p59.sup.fyn activity is believed to have a role.Type: GrantFiled: December 22, 1997Date of Patent: May 2, 2000Assignee: Celltech Therapeutics LimitedInventors: Jeremy Martin Davis, Peter David Davis, David Festus Charles Moffat, Mark James Batchelor
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Patent number: 6048853Abstract: Substituted 1-arylphthalazine compositions with the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independentlya) H,b) HO,c) R.sup.11 O--,d) halogen,e) C1-C3-alkyl,f) CF.sub.3,g) R.sup.12 CO.sub.2 --, orh) R.sup.12 CONH--;R.sup.1 and R.sup.2, or R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 can be taken together to bea) --OCH.sub.2 O--, orb) --OCH.sub.2 CH.sub.2 O--;R.sup.5 isa) H,b) C1-C6-alkyl,c) C3-C6-alkenyl,d) C3-C6-alkynyl,e) C3-C6-cycloalkyl,f) phenyl or substituted phenyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alky, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and CO.sub.2 R.sup.12, org) phenyl-C1-C3-alkyl or substituted phenyl-C1-C3-alkyl, wherein the phenyl is substituted with one or two substituents selected from the group consisting of C1-C3-alkyl, halogen, R.sup.12 HN--, R.sup.12 O--, CF.sub.3 --, R.sup.13 SO.sub.2 -- and --CO.sub.2 R.sup.12 ;R.sup.6 isa) R.sup.10 R.sup.11 N--,b) R.Type: GrantFiled: January 18, 1996Date of Patent: April 11, 2000Assignee: Bearsden Bio, Inc.Inventors: Mark A. Collins, Jeffrey C. Pelletier
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Patent number: 6048869Abstract: The novel compounds of the present invention are those of structural formula I: ##STR1## or a pharmaceutically acceptable salt, ester, or stereoisomer thereof, which are inhibitors of 5.alpha.-reductase. The compounds of formula I are useful in the oral, systemic, parenteral or topical treatment of hyperandrogenic conditions. Methods of using the compounds of formula I for the treatment of hyperandrogenic conditions such as acne vulgaris, seborrhea, androgenic alopecia, male pattern baldness, female hirsutism, benign prostatic hyperplasia, and the prevention and treatment of prostatic carcinoma, as well as the treatment of prostatitis the treatment of sweat-related conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa, the treatment of polycystic ovary syndrome, the prevention and treatment of bone loss and related diseases, and the prevention and treatment of premature labor are provided, as well as pharmaceutical compositions for the compounds of formula I.Type: GrantFiled: July 26, 1999Date of Patent: April 11, 2000Assignee: Merck & Co., Inc.Inventors: Derek Von Langen, Susan D. Aster, Donald W. Graham
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Patent number: 5994544Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors and the method of preparing these compounds are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.Type: GrantFiled: October 8, 1997Date of Patent: November 30, 1999Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards