Acyclic Nitrogen Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 546/336)
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Patent number: 6313345Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: October 18, 1999Date of Patent: November 6, 2001Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 6313153Abstract: The present invention relates to an agent for treating nephritis and a TGF-&bgr; inhibiting agent comprising as an effective ingredient a pyridylacrylamide derivative represented by the following formula (I): wherein Ar1 is a substituted or unsubstituted pyridyl group, Ar2 is a substituted or unsubstituted phenyl group, R1 is a hydrogen atom, an alkyl group or an aryl group, R2 is a hydrogen atom, an alkyl group, a cyano group or an alkoxycarbonyl group, R3 is a hydrogen atom or an optionally substituted alkyl group, X is an oxygen or sulfur atom, A and B are same or different and each represent a hydrogen atom, a hydroxyl group, an alkoxy group or an alkylthio group, or A and B together form an oxo or thioxo group, or a group represented by the formula: ═N—Y in which Y is a dialkylamino, hydroxyl, aralkyloxy or alkoxy group, or a group represented by the formula: —Z1—M—Z2— which Z1 and Z2 are same or different and each represent an oxygen or sulfur atom orType: GrantFiled: January 21, 2000Date of Patent: November 6, 2001Assignee: Tsumura & Co.Inventors: Yoshihiro Hasegawa, Shouichirou Shindou, Tomohisa Hattori, Yousuke Yamazaki, Tatsuhiro Obata, Fumiko Horiuchi, Hiroyuki Hayakawa, Hiroaki Kumazawa
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Patent number: 6300352Abstract: The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations containing them and methods for their preparation.Type: GrantFiled: May 11, 1998Date of Patent: October 9, 2001Assignee: AstraZeneca ABInventors: David Cheshire, David Cladingboel, Simon Hirst, Carol Manners, Michael Stocks
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Patent number: 6291491Abstract: Amide derivatives are selective &bgr;3 adrenergic receptor agonists with very little &bgr;1 and &bgr;2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility are also disclosed.Type: GrantFiled: October 12, 2000Date of Patent: September 18, 2001Assignee: Merck & Co., Inc.Inventors: Ann E. Weber, Emma R. Parmee, Robert Mathvink, Wallace T. Ashton, Elizabeth M. Naylor
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Patent number: 6258851Abstract: Compounds of formula (I), wherein A, B, X, R1, R2, R3, R4, R5, R6 are as defined in the specification, are matrix metalloproteinase inhibitors.Type: GrantFiled: October 8, 1999Date of Patent: July 10, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Christopher David Floyd, Sanjay Ratilal Patel, Mark Whittaker
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Patent number: 6221888Abstract: Compounds of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 29, 1999Date of Patent: April 24, 2001Assignee: Merck & Co., Inc.Inventors: Philippe L. Durette, William K. Hagmann, Malcolm Maccoss, Sander G. Mills, Richard A. Mumford
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Patent number: 6194437Abstract: The compounds of the instant invention are novel compounds of Formula I or a pharmaceutically acceptable salt thereof wherein Ar is phenyl or pyridyl unsubstituted or substituted. Ar1 can be independently selected from Ar and can also include pyridyl-N-oxide, indolyl, imidazole, and pyridyl; R3 can be independently selected from Ar or is hydrogen, hydroxy, NMe2, N-methyl-pyrrole, imidazole, tetrazole, thiazole (a), (b), (c), or (d), wherein Ar2 is phenyl or pyridyl. The instant compounds antagonize the bombesin receptors in mammals and are therefore effective in treating and/or preventing depression, psychoses, seasonal affective disorders, cancer, feeding disorders, gastrointestinal disorders, inflammatory bowel disease, sleep disorders, and memory impairment.Type: GrantFiled: February 3, 1999Date of Patent: February 27, 2001Assignee: Warner-Lambert CompanyInventors: David Christopher Horwell, Martyn Clive Pritchard
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Patent number: 6194418Abstract: The invention relates to novel substituted aminosalicylamides, to a plurality of processes for their preparation and to their use as fungicides, and also to novel intermediates and to a plurality of processes for their preparation.Type: GrantFiled: September 13, 1999Date of Patent: February 27, 2001Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Uwe Stelzer, Peter Wolfrum, Klaus Stenzel
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Patent number: 6153630Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram as well as with improved selectivity with regard to PDE III inhibition. In certain aspects of the invention, the compounds also demonstrate PDE V inhibition. Pharmaceutical compositions containing the same and methods of treatment are also disclosed.Type: GrantFiled: November 13, 1997Date of Patent: November 28, 2000Assignee: Euro-Celtique, S.A.Inventors: David J. Cavalla, Mark Chasin, Lloyd Dolby
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Patent number: 6096768Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: April 29, 1999Date of Patent: August 1, 2000Assignee: Rhone-Poulenc Rorer LimitedInventors: Michael John Ashton, David Charles Cook, Garry Fenton, Susan Jacqueline Hills, Ian Michael McFarlane, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Nigel Vicker
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Patent number: 6093816Abstract: The present invention is directed to new cationic lipids and intermediates in their synthesis that are useful for transfecting nucleic acids or peptides into prokaryotic or eukaryotic cells. The lipids comprise one or two substituted histidine residues, or similar compounds, linked to a lipophilic moiety. The lipids form a complex when mixed with polyanions such as nucleic acids or peptides. The complexes permit efficient transfer of polyanions into cells, usually without significant toxicity to the cells.Type: GrantFiled: June 27, 1996Date of Patent: July 25, 2000Assignee: Isis Pharmaceuticals, Inc.Inventors: Kuei-Ying Lin, Mark D. Mattuecci
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Patent number: 6080839Abstract: The invention relates to a novel labeling reactant, suitable for labeling of a biospecific binding reactant using solid-phase synthesis. The invention further concerns new labeling methods. The novel labeling reactant has the formula (I) ##STR1## wherein -A- is a bivalent aromatic structure capable of absorbing light or energy and transferring the excitation energy to a lanthanide ion after the product made by the said solid-phase synthesis has been released from the used solid support, deprotected and converted to a lanthanide chelate;-G- is a bridge replacing a hydrogen atom in A;R is a protected amino acid residue --CH(NHX)COOH, where X is a transient protecting group, or its active ester, where said ester is e.g. an N-hydroxysuccinimido, p-nitrophenol or pentafluorophenol ester; andR' is --COOR'" where R'" is an alkyl of 1 to 4 carbon atoms, phenyl or benzyl, which phenyl or benzyl can be substituted or unsubstituted.Type: GrantFiled: June 25, 1998Date of Patent: June 27, 2000Assignee: Wallac OyInventors: Harri Takalo, Jari Hovinen, Veli-Matti Mukkala, Paivi Liitti, Heikki Mikola
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Patent number: 6066641Abstract: The present invention relates to novel compounds of the formula (I): ##STR1## wherein Q.sub.3 R.sub.3 and Q.sub.8 R.sub.8 are described herein. The compounds possess PDE-IV inhibitory activity and improved selectivity with regard to PDE-III inhibition. Also disclosed are pharmaceutical compositions and methods of treatment utilizing the disclosed compounds.Type: GrantFiled: June 11, 1997Date of Patent: May 23, 2000Assignee: Euro-Celtique S.A.Inventors: David Cavalla, Peter Hofer, Mark Chasin
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Patent number: 6057345Abstract: Compounds of the formula, ##STR1## and pharmaceutically-acceptable salts thereof, which are useful as antagonists of the pain-enhancing effects of E-type prostaglandins, processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds, and methods for treating pain comprising the administration of such compounds.Type: GrantFiled: October 30, 1998Date of Patent: May 2, 2000Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6028087Abstract: Compounds of the formula (I):W--Z--(CR'R.sup.10).sub.r --U--(CR'.sub.2).sub.s --V--A (I)wherein:A is ##STR1## W is .sup.N ; Z is (CH.sub.2).sub.1-2 ;U and V independently are present as CO, CR'.sub.2, C(.dbd.CR'.sub.2), S(O).sub.r, O, NR', CR'OR', CR'(OR")CR'.sub.2, CR'.sub.2 CR'(OR"), C(O)CR'.sub.2, CR'.sub.2 C(O), CONR', NR'CO, OC(O), C(O)O, C(S)O, OC(S), C(S)NR', NR'C(S), S(O).sub.r NR', NR'S(O).sub.r, N.dbd.N, NR'NR', NR'CR'.sub.2, NR'CR'.sub.2, CR'.sub.2 O, OCR'.sub.2, C.tbd.C, CR'.dbd.CR', or CR'(NR'R")C(O);each r independently is 0 to 3;s is 0 to 2;each R' independently is H, C.sub.1-4 alkyl, C.sub.3-7 cycloalky-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;each R" independently is R', --C(O)R', or --C(O)OR.sup.15 ;R.sup.10 is H, C.sub.1-4 alkyl, or --NR'R';each R.sup.15 independently is C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, or Ar-C.sub.0-4 alkyl;R.sup.2 is present once or twice as C.sub.1-4 alkyl, J--CO.sub.2 R', CONR', SR', NR'R", C .sub.1-4 alkoxy, hydroxy, CN, CF.sub.Type: GrantFiled: January 21, 1998Date of Patent: February 22, 2000Assignee: SmithKline Beecham CorporationInventors: William Edward Bondinell, James Francis Callahan, William Francis Huffman, Richard McCulloch Keenan, Brian Walter Metcalf, James Samanen, Tobias Oregon Yellin
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Patent number: 6022994Abstract: Succinoylamino hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 12, 1998Date of Patent: February 8, 2000Assignee: G. D. Searle &. CO.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 6011174Abstract: The present invention relates to a compound of the formula (I), or its pharmaceutically acceptable salt or ester: ##STR1## wherein Ar.sup.1 is an aryl group or a heteroaromatic ring group; Ar is a group of the formula ##STR2## each of Ar.sup.2 and Ar.sup.3 is an aryl group or a heteroaromatic ring group; Cy is an aryl group, a heteroaromatic ring group or an aliphatic ring group which may contain one or two oxygen atoms; A.sup.1 is a C.sub.1-4 chain hydrocarbon group; m is an integer of from 1 to 6; each of n and p is an integer of from 0 to 3; Q.sup.1 is a single bond, a group of the formula --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --, or a C.sub.1-6 chain hydrocarbon group; Q.sup.2 is a single bond or a group of the formula --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p --; Q.sup.3 is a single bond, an oxygen atom, a sulfur atom, a methylene group, a vinylene group or a group of the formula --CO--, --NH--, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.Type: GrantFiled: August 4, 1998Date of Patent: January 4, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5994507Abstract: A method for binding albumin by contacting an aqueous liquid containing an albumin with an albumin-binding compound is selected from albumin-binding compounds containing the scaffold --CO--NH--C(.dbd.C--)--CO--, and conjugates that are capable of binding albumin and exhibiting the scaffold --CO--NH--C(.dbd.C--)--CO--.Type: GrantFiled: December 31, 1997Date of Patent: November 30, 1999Assignee: Amersham Pharmacia Biotech ABInventors: .ANG.ke Pilotti, Tor Regberg, Christel Ellstrom, Charlotta Lindqvist, Ann Eckersten, Lars Fagerstam
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Patent number: 5990314Abstract: This invention relates to a compound of formula I ##STR1## These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.Type: GrantFiled: June 7, 1996Date of Patent: November 23, 1999Assignee: SmithKline Beecham CorporationInventor: Robert A. Daines
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Patent number: 5968942Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: August 23, 1994Date of Patent: October 19, 1999Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 5965741Abstract: The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.Type: GrantFiled: February 21, 1997Date of Patent: October 12, 1999Assignee: Zeneca LimitedInventors: Gloria Anne Breault, Howard Tucker, John Oldfield, Peter Warner
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Patent number: 5955491Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5948778Abstract: This invention relates to novel statone antiviral analogs, to the processes and intermediates useful for their preparation and to their use as antiviral agents.Type: GrantFiled: May 19, 1998Date of Patent: September 7, 1999Assignee: Merrel Pharmaceuticals Inc.Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
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Patent number: 5942544Abstract: The present application describes m-amidino phenyl analogs of formula I: ##STR1## wherein D can be amidino and E can be phenyl, which are useful as inhibitors of factor Xa.Type: GrantFiled: February 19, 1997Date of Patent: August 24, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Thomas Peter Maduskuie, Jr., Joseph Cacciola, John Matthew Fevig, Mimi Lifen Quan, Petrus Fredericus Wilhelmus Stouten
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Patent number: 5935978Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.Type: GrantFiled: July 28, 1993Date of Patent: August 10, 1999Assignee: Rhone-Poulenc Rorer LimitedInventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher, Michael John Ashton, David Charles Cook, Susan Jacqueline Hills, Ian Michael McFarlane, Nigel Vicker
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Patent number: 5932736Abstract: Described are preferred processes for preparing heterocycles having one or more nitrogen and/or oxygen heteroatoms, utilizing a 1,3-dihalopropene as an effective 3-carbon fragment. Preferred processes yield pyridines, quinolines, oxazoles, pyrimidines and pyrazoles, depending upon the other reactant or reactants utilized with the 1,3-dihalopropene.Type: GrantFiled: April 7, 1998Date of Patent: August 3, 1999Assignee: Reilly Industries, Inc.Inventors: Ramiah Murugan, Eric F. V. Scriven
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Patent number: 5889058Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.Type: GrantFiled: November 3, 1994Date of Patent: March 30, 1999Assignee: Celltech LimitedInventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
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Patent number: 5872257Abstract: The present invention provides a chelating agent suitable for forming coordinated complexes with a metal in liquid and supercritical carbon dioxide of covalently bonded (i) a chelating group selected from the group consisting of a dithio carbamate, a thiol group, and a picolyl amine group, (ii) a non-electron withdrawing spacer group selected from (CH.sub.2).sub.x ; and (iii) a CO.sub.2 -soluble functional group selected from (CF.sub.2 CF.sub.2 O).sub.X, (CF.sub.2 O).sub.X, (CF.sub.2).sub.X, and ?CF.sub.2 (CF.sub.3 FO)!.sub.x. X is selected to be greater or equal to 3 and to minimize the electron withdrawing effect of the CO.sub.2 -soluble functional group and to achieve a chelating agent solubility of at least a 10.sup.-3 gm/gm CO.sub.2. A solubility of at least 10.sup.-2 gm/gm CO.sub.2 is attained at a temperature in the range of approximately 0.degree. to 100.degree. C. and a pressure of approximately 500 to 5000 psi.Type: GrantFiled: April 1, 1997Date of Patent: February 16, 1999Assignee: University of PittsburghInventors: Eric J. Beckman, Alan J. Russell
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Patent number: 5863950Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-viral agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.Type: GrantFiled: October 27, 1994Date of Patent: January 26, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Siegfried H. Reich, Kathleen Lewis, Michael Melnick, Mary Ann M. Fuhry, Stephen Warren Kaldor
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Patent number: 5854232Abstract: This invention relates to compounds of formula (IA), (IB), (IC) or (ID), wherein m, X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.14 and the dotted lines are as defined below, their pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of using them to treat Alzheimer's disease, age-associated memory impairment, Parkinson's disease and other central nervous system disorders. The claimed compounds have the ability to enhance the release of neurotransmitters such as acetylcholine, dopamine and serotonin.Type: GrantFiled: February 19, 1997Date of Patent: December 29, 1998Assignee: Pfizer Inc.Inventors: Robert A. Volkmann, Vytautas J Jasys, Gene M Bright, Anabella Villalobos, Patricia A Seymour
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Patent number: 5849770Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR; R.sup.a is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R.sup.3 is preferably hydrogen; hydrogen, R.sup.4 is preferably --(CH.sub.2).sub.t Ar, --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar' or --(CH.sub.2).sub.t ArN(R.sup.b)CX.sup.1 N(R.sup.b)L.sup.2 (Alk).sub.m Ar; R.sup.5 is preferably --(CH.sub.2).sub.t Ar, --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar' or --(CH.sub.2).sub.t ArN(R.sup.b)CX.sup.1 N(R.sup.b)L.sup.2 (Alk).sub.m Ar; R.sup.6 and R.sup.7 are preferably hydrogen, L.sup.1 and L.sup.2 are preferably divalent linking groups; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing group.Type: GrantFiled: December 20, 1996Date of Patent: December 15, 1998Assignee: Celltech Therapeutics Ltd.Inventors: John Clifford Head, James Thomas Reuberson
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Patent number: 5849771Abstract: Compounds of formula (I), wherein Ar, R.sub.1, R.sub.2, Y and R are as defined in claim 1, are effective as traps for free radicals.Type: GrantFiled: January 26, 1998Date of Patent: December 15, 1998Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Abdelhamid Zeghdaoui, Jean-Pierre Finet, Beatrice Tuccio, Viviane Cerri, Paul Tordo
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Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
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Patent number: 5837717Abstract: A compound of the following formula: ##STR1## and its pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl, C.sub.2-4 alkenyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, phenyl or phenyl-C.sub.1-4 alkyl; or R.sup.1 and R.sup.2 are taken together with the nitrogen to which they are attached and form optionally substituted, saturated or unsaturated 3-, 4-, 5-, 6- or 7-membered heterocyclic cantaining one to two heteroatoms, provided that the heterocyclic is not pyrrolidinyl;R.sup.3 is hydrogen, C.sub.1-4 alkyl or a hydroxy protecting group;Ar is phenyl optionally substituted with one or more substituents selected from halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-C.sub.1-4 alkyloxy, CF.sub.3 and carboxy-C.sub.1-4 alkyloxy; andX is phenyl, naphthyl, biphenyl, indanyl, benzofuranyl, benzothiophenyl, 1-tetralone-6-yl, C.sub.Type: GrantFiled: January 28, 1997Date of Patent: November 17, 1998Assignee: Pfizer Inc.Inventor: Fumitaka Ito
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Patent number: 5830915Abstract: The invention provides compounds which are useful as inhibitors of matrix metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I) ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are described in the claims, a stereoisomer or enantiomer thereof, or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, ester acyloxyamide, imide or derivative thereof.Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by matrix metalloprotease activity using these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: August 26, 1997Date of Patent: November 3, 1998Assignee: The Procter & Gamble CompanyInventors: Stanislaw Pikul, Kelly Lynn McDow-Dunham, Biswanath De, Yetunde Olabisi Taiwo
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Patent number: 5830897Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: November 3, 1998Assignees: G. D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Patent number: 5814633Abstract: Iminooxymephyleneanilides of the formula I ##STR1## where the index and the substituents have the following meanings: n is 0, 1, 2, 3 or 4;R is nitro, cyano, halogen, unsubst. or subst. alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy or an unsubst. or subst. bridge bonded to two adjacent ring atoms;X is a direct bond or CH.sub.2, O or NR.sup.a ;R.sup.a is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl;R.sup.1 is hydrogen,unsubst. or subst. alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcarbonyl or alkoxycarbonyl;R.sup.2 is alkyl, alkenyl, alkynyl, cycloalkyl or cycloalkenyl, or in the case where X is NR.sup.a, additionally hydrogen;R.sup.3 is hydrogen, cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio or cycloalkyl;R.sup.4 is a 6- to 10-membered mono- or bicyclic, substituted heteroaromatic ring system,and process and intermediates for their preparation and their use.Type: GrantFiled: May 20, 1997Date of Patent: September 29, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Muller, Hubert Sauter, Franz Rohl, Eberhard Ammermann, Gisela Lorenz, Norbert Gotz
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Patent number: 5798373Abstract: Tri-substituted phenyl derivatives and pharmaceutical compositions containing them. In a preferred embodiment, the compounds have the general formula (2): ##STR1## wherein L is preferably --OR; R.sup.a is preferably an optionally substituted alkyl group; R is preferably an optionally substituted cycloalkyl group; R.sup.3 is preferably hydrogen; R.sup.4 is preferably hydrogen, --(CH.sub.2).sub.t --Ar or --(CH.sub.2).sub.t --Ar--(L.sup.1).sub.n --Ar'; R.sup.5 is preferably --(CH.sub.2).sub.t --Ar or --(CH.sub.2).sub.t ---Ar--(L.sup.1).sub.n --Ar'; R.sup.6 and R.sup.7 are preferably hydrogen, L.sup.1 is preferably a divalent linking group; Ar is preferably a monocyclic or bicyclic aryl or heteroaryl group; and Ar' is preferably Ar or an Ar containing group. Compounds of the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of various diseases, such as asthma, which are associated with an unwanted inflammatory response or muscular spasm.Type: GrantFiled: December 20, 1996Date of Patent: August 25, 1998Assignee: Celltech Therapeutics, LimitedInventor: Graham John Warrellow
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Patent number: 5792871Abstract: Compound 9 is prepared by a 9-step ##STR1## process in an overall yield of about 35% from 3-acetylpyridine. Compound 10 is prepared by a seven-step ##STR2## process in an overall yield of about 30% from 3-acetyl pyridine. These compounds are key intermediates in the synthesis of Compound 11, an important .beta.-3 agonist useful in the treatment of obesity and diabetes.Type: GrantFiled: June 26, 1997Date of Patent: August 11, 1998Assignee: Merck & Co., Inc.Inventors: Michel M. Chartrain, Christopher Roberge, John Y. L. Chung, Dalian Zhao
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Patent number: 5760236Abstract: Substituted pyridines of the general formula: ##STR1## wherein R.sup.1 is hydroxyl or chlorine, and a) X is hydrogen or chlorine, R.sup.2 and R.sup.3 together are .dbd.O, R.sup.4 is a group of the formula --OR.sup.5 and R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl, orb) X is hydrogen and R.sup.2, R.sup.3 and R.sup.4 together are .dbd.N--NH--, orc) X and R.sup.2 each is hydrogen and R.sup.3 and R.sup.4 together are --O--, ord) X and R.sup.2 each is hydrogen, R.sup.3 is hydroxyl and R.sup.4 is amino or hydroxyl.The compounds are obtained by subjecting nicotine to microbiological oxidation to give 5-succinoyl-2-pyridone, followed by chemical reactions. The compounds are suitable as intermediates for the preparation of pharmaceutically active compounds.Type: GrantFiled: November 21, 1995Date of Patent: June 2, 1998Assignee: Lonza, Ltd.Inventors: Andreas Kiener, Jean-Paul Roduit, Alain Wellig
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Patent number: 5753652Abstract: The invention relates to compounds of formula ##STR1## and salts, pharmaceutical compositions, intermediates and processes of preparation thereof.Type: GrantFiled: April 4, 1995Date of Patent: May 19, 1998Assignee: Novartis CorporationInventors: Alexander Fassler, Guido Bold, Marc Lang, Shripad Bhagwat, Peter Schneider
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Patent number: 5723665Abstract: A process for producing an ethenyl amide compound, which comprises reacting a Schiff base compound having a carbon atom adjacent to a carbon atom constituting an imino group and at least one hydrogen atom on the carbon atom with an acylhalide at a reduced pressure while removing by-produced hydrogen halide by distillation to produce an ethenyl amide compound having an amide bond in the molecule and a double bond between carbons at .alpha.-position and .beta.-position with respect to the nitrogen atom of the amide bond.Type: GrantFiled: November 15, 1996Date of Patent: March 3, 1998Assignee: Tokuyama CorporationInventors: Shozo Kato, Shigeo Tamura, Toshio Kitajima, Noriyuki Fukada
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Patent number: 5714518Abstract: HIV protease inhibitors, obtainable by chemical synthesis, block the biological activity of the HIV protease enzyme, causing the replication of the HIV virus to terminate. These compounds, as well as pharmaceutical compositions that contain these compounds and possibly other anti-vital agents as ingredients, are thus suitable for the treatment of the HIV virus known to cause AIDS.Type: GrantFiled: October 27, 1994Date of Patent: February 3, 1998Assignee: Agouron PharmaceuticalsInventors: Siegfried H. Reich, Mark J. Pino, Dzuy T. Nguyen, Anthony J. Trippe
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Patent number: 5691366Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)-alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4 wherein Y is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5686472Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: October 27, 1993Date of Patent: November 11, 1997Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, S. Jane deSolms, Ta Jyh Lee, deceased
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Patent number: 5681965Abstract: Compositions containing as the active ingredient a spin-trapping reagent, preferably .alpha.-phenyl butyl nitrone (PBN) or spin-trapping derivatives thereof, in a suitable pharmaceutical carrier for administration to a patient are disclosed for treating or preventing symptoms associated with aging or other conditions associated with oxidative tissue damage. Other spin-trapping agents can also be used, such as 5,5-dimethyl pyrroline N-oxide (DMPO) or .alpha.-(4-pyridyl 1-oxide)-N-tert-butylnitrone (POBN), and other spin-trapping derivatives thereof. These compositions and methods are useful in the treatment of age-related disorders, pre-surgical and/or pre-anesthetic preparation or administration of chemotherapeutic agents, and in the treatment of disorders or trauma of the brain, cardiovascular system, and lymphatic system.Type: GrantFiled: June 6, 1995Date of Patent: October 28, 1997Assignees: Oklahoma Medical Research Foundation, University of Kentucky Research FoundationInventors: John M. Carney, Robert A. Floyd
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Patent number: 5656253Abstract: The present invention relates particularly to novel pyridine based nitrogen-sulfur ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, novel aminothiol ligands that are suitable for complexing with a radionuclide, and are useful as general imaging agents for diagnostic purposes, and amide-thiolate ligands having improved metal chelate formation kinetics. The amide-thiolate ligands include an amine which converts to a vinylogous amide upon complexation, thereby providing rapid complexation and thermodynamic stability. The ligands may be used for post formed labeling of biological substances for use in the fields of diagnosis and therapy.Type: GrantFiled: June 7, 1994Date of Patent: August 12, 1997Assignee: Mallinckrodt Medical, Inc.Inventors: Raghavan Rajagopalan, Ananthachari Srinivasan, Jean-Luc Vanderheyden
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Patent number: 5646167Abstract: Disclosed are compounds of formula I ##STR1## wherein R, R.sub.1, R.sub.2 and Ar have meanings as defined; pharmaceutically acceptable prodrug derivatives and pharmaceutically acceptable salts thereof; methods for preparation thereof; pharmaceutical compositions comprising said compounds; and methods of inhibiting matrix-degrading metalloproteinase and of treating matrix-degrading metalloproteinase dependent conditions in mammals using such compounds.Type: GrantFiled: June 7, 1995Date of Patent: July 8, 1997Assignee: Ciba-Geigy CorporationInventors: Lawrence J. MacPherson, David T. Parker
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Patent number: 5646121Abstract: The present invention relates to novel pseudopeptides with antiviral activity of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to a process for their preparation, and to their use as antiviral agents, especially against cytomegaloviruses.Type: GrantFiled: September 7, 1994Date of Patent: July 8, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas-J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens