The Bicyclo Ring System Consists Of The Hetero Ring And A Six-membered Carbocyclic Ring Patents (Class 549/398)
  • Patent number: 6166226
    Abstract: A method for preparing an aryl ether compound is provided in which an alcohol is reacted with an aromatic compound in the presence of a base, and a transition metal catalyst selected from the group consisting of platinum and nickel to form an aryl ether. The aromatic compound comprises an activated substituent, X, said activated substituent being a moiety such that its conjugate acid HX has a pKa of less than 5.0. The catalyst is preferably a soluble palladium complex in the presence of supporting ligands.
    Type: Grant
    Filed: December 8, 1998
    Date of Patent: December 26, 2000
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, John P. Wolfe, Michael Palucki
  • Patent number: 6160134
    Abstract: A process is provided for preparing chiral cyclopropane carboxylic acids, preferably of the structure ##STR1## which are intermediates used in preparing acyl guanidine sodium/proton exchange (NHE) inhibitors.
    Type: Grant
    Filed: June 10, 1999
    Date of Patent: December 12, 2000
    Assignee: Bristol-Myers Squibb co.
    Inventors: Bang-Chi Chen, Joseph E. Sundeen, Jeffrey T. North, Annie J. Pullockaran, Saleem Ahmad, Shung C. Wu, Karnail S. Atwal, Sundeep Dugar
  • Patent number: 6150532
    Abstract: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: November 21, 2000
    Inventors: Adnan Mjalli, Sepehr Sarshar, Xiaodong Cao, Farid Bakir
  • Patent number: 6143770
    Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.
    Type: Grant
    Filed: October 28, 1998
    Date of Patent: November 7, 2000
    Assignee: Lipogenics, Inc.
    Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
  • Patent number: 6136985
    Abstract: The present invention provides CLA esters and uses thereof. More particularly, the present invention provides a composition for topical use comprising CLA esters and a topical carrier. In addition, the present invention specifically provides tocopheryl CLA esters, ascorbyl CLA esters and retinyl CLA esters.
    Type: Grant
    Filed: December 21, 1998
    Date of Patent: October 24, 2000
    Assignee: DCV, Inc.
    Inventor: James R. Millis
  • Patent number: 6130341
    Abstract: A process for producing chromans, comprising reacting a phenol, a formaldehyde and an alcohol in the presence of a secondary amine and an acid, to generate an alkoxymethylphenol compound with the ortho position to the phenolic hydroxyl group substituted with an alkoxymethyl group, and reacting the alkoxymethylphenol compound with an unsaturated compound having a carbon--carbon double bond.
    Type: Grant
    Filed: July 17, 1998
    Date of Patent: October 10, 2000
    Assignee: Kuraray Co., Ltd.
    Inventors: Hiroyuki Monoe, Junko Sato, Koichi Kanehira, Yoshin Tamai
  • Patent number: 6124284
    Abstract: Novel compounds of formula (1) together with their salts and solvates have a number of uses in medicine, in particular as central muscle relaxants.
    Type: Grant
    Filed: July 16, 1998
    Date of Patent: September 26, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: James Leroy Kelley, Gregory Cooksey Rigdon, Barrett Randolph Cooper, Ed Williams McLean, David Lee Musso, Gloria Faye Orr, Jeffrey Leaman Selph, Virgil Lee Styles
  • Patent number: 6060506
    Abstract: Novel derivatives of benzopyran are provided which are useful as melatonergic agents.
    Type: Grant
    Filed: July 13, 1999
    Date of Patent: May 9, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: John D. Catt, Graham Johnson, Daniel J. Keavy, Ronald J. Mattson, Michael F. Parker, Katherine S. Takaki, Joseph P. Yevich
  • Patent number: 6020362
    Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: February 1, 2000
    Assignee: Eli Lilly and Company
    Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Jr., Michael Paal, Gerd Ruhter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
  • Patent number: 6013809
    Abstract: This invention relates to substituted heterocyclic benzocycloalkenes of general formula I or pharmaceutically acceptable salts thereof, to a method of producing them and to their use as analgesics.
    Type: Grant
    Filed: December 11, 1998
    Date of Patent: January 11, 2000
    Assignee: Gruenenthal GmbH
    Inventors: Oswald Zimmer, Wolfgang Strassburger, Claudia Puetz, Werner Englberger, Babette-Yvonne Koegel
  • Patent number: 6008245
    Abstract: Sulfonamide-substituted benzopyran derivatives, processes for their preparation, their use as a medicament, and pharmaceutical preparations comprising them Compounds of the formula I ##STR1## having the meanings of the substituents indicated in the claims are outstandingly active substances for the production of medicaments for the prophylaxis and for the therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal diseases.
    Type: Grant
    Filed: November 2, 1998
    Date of Patent: December 28, 1999
    Assignee: Hoechst Marion Roussel Deutschland GmbH
    Inventors: Joachim Brendel, Uwe Gerlach, Hans Jochen Lang, Klaus Weidmann
  • Patent number: 5977351
    Abstract: Dyes comprising an inner salt of a compound of the formula:Q.sup.1 =Z-Q.sup.2wherein:Q.sup.1 is a 4-(benz[b]-4H-pyrylium)methylidene, 4-(benz[b]-4H-thiopyrylium)methylidene or 4-(benz[b]-4H-selenopyrylium)methylidene grouping;Z is a 1,3-(2-hydroxy-4-oxo-2-cyclobutylidene) hydroxide or 1,3-(2-hydroxy-4,5-dioxo-2-cyclopentylidene) hydroxide ring; andQ.sup.2 is a 4-(benz[b]-4H-pyran-4-ylidene)methyl, 4-(benz[b]-4H-thiopyran-4-ylidene)methyl or 4-(benz[b]-4H-selenopyran-4-ylidene)methyl grouping;wherein at least one of the groupings Q.sup.1 and Q.sup.
    Type: Grant
    Filed: May 20, 1993
    Date of Patent: November 2, 1999
    Assignee: Polaroid Corporation
    Inventors: Peter K. Chu, Serajul Haque, Anthony J. Puttick, Socorro M. Ramos, Robert P. Short, Stephen G. Stroud, Stephen J. Telfer, Michael J. Zuraw
  • Patent number: 5919953
    Abstract: There is provided a 2-stage process for making 2H-1-benzopyrans wherein an alpha,beta-unsaturated aldehyde is reacted with an alkanol or an alkane-diol in the presence of a dehydrating compound which is an orthoformate and an aluminum oxide/silicon oxide catalyst to form an aliphatic acetal, which is then condensed in a second stage with a phenol in the presence of base in an organic solvent.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: July 6, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Pierre Bossard, Michael Gottsponer, Frances Finney
  • Patent number: 5919950
    Abstract: Squarylium compounds of the formula: ##STR1## wherein Q.sup.1 and Q.sup.2 are each independently a pyrylium, thiopyrylium, selenopyrylium, benzpyrylium, benzthiopyrylium or benzselenopyrylium nucleus, and R.sup.1 and R.sup.2 are each independently an aliphatic or cycloaliphatic group, can be prepared by reacting a squaric acid derivative of the formula: ##STR2## with a compound of the formula Q.sup.2 CH.sub.2 R.sup.2 in the presence of a base.
    Type: Grant
    Filed: April 23, 1993
    Date of Patent: July 6, 1999
    Assignee: Polaroid Corporation
    Inventors: Paulina P. Garcia, John W. Lee, John L. Marshall, Donald A. McGowan, Anthony J. Puttick, Thomas K. Spencer, Stephen G. Stroud, Stephen J. Telfer, Michael J. Zuraw
  • Patent number: 5912362
    Abstract: High-purity isochroman compounds can be obtained in high yields according to a simple and economical process for preparing isochroman compounds, comprising the step of adding an aquesous solution of formaldehyde having a concentration of 40 to 70 wt. % to a complex of an arylalkanol represented by the following general formula (II) with a Friedel-Crafts catalyst to cyclize the arylalkanol: ##STR1## wherein R.sub.1 and R.sub.2 each stands for a hydrogen atom, a lower alkyl group or a lower alkoxyl group, or alternatively R.sub.1 and R.sub.2 are respectively bonded to adjacent carbon atoms with mutual bonding of R.sub.1 and R.sub.2 together with the carbon atoms respectively bonded to R.sub.1 and R.sub.2 to form a benzene ring, a naphthalene ring, or a C.sub.5 or C.sub.6 cycloalkane or cycloalkene which may have 1 to 6 lower alkyl groups; and R.sub.3 stands for a hydrogen atom or a lower alkyl group.
    Type: Grant
    Filed: November 10, 1997
    Date of Patent: June 15, 1999
    Assignee: Kao Corporation
    Inventors: Shigeyoshi Tanaka, Masayuki Oku, Junji Koshino
  • Patent number: 5908581
    Abstract: A red fluorescent material includes a compound of the formula: ##STR1## wherein: R.sub.1, and R.sub.2 are individually alkyl of from 1 to 20 carbon atoms, aryl, carbocyclic and other heterocyclic systems; andR.sub.3, and R.sub.4 are individually alkyl of from 1 to 10 carbon atoms, and a branched or unbranched 5 or 6 member substituent ring connecting with R.sub.1, R.sub.2 respectively; andR.sub.5 is alkyl of from 2-20 carbon atoms; sterically hindered aryl and heteroaryl; andR.sub.6 is alkyl of from 1 to 10 carbon atoms, and a 5 or 6-member carbocyclic ring connecting with R.sub.5.
    Type: Grant
    Filed: April 7, 1997
    Date of Patent: June 1, 1999
    Assignee: Eastman Kodak Company
    Inventors: Chin H. Chen, Kevin P. Klubek, Jianmin Shi
  • Patent number: 5888432
    Abstract: The present invention has for subjects, novel benzopyran derivatives, substituted in position 2 with an adamantyl group as well as the compositions and (co)polymer matrices containing such derivatives. Said derivatives possess interesting photochromic properties.
    Type: Grant
    Filed: December 3, 1997
    Date of Patent: March 30, 1999
    Assignee: Corning Incorporated
    Inventor: You-Ping Chan
  • Patent number: 5872118
    Abstract: Novel compounds of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro;R.sup.5 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;R.sup.6 is selected from hydrogen, C.sub.1 -C.sub.4 ally and hydroxy; orR.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;R.sup.7 is selected from hydrogen and hydroxy,R.sup.8 and R.sup.9 are each selected from hydrogen, C.sub.1 -C.sub.4 alkyl and cyclo(C.sub.3 or C.sub.4) alkyl or together with the nitrogen form a morpholino group; andX is selected from a bond, methylene and --O-- and is always a bond or --O-- when any of R.sup.5, R.sup.6 and R.sup.7 is other than hydrogen and is always a bond when R.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;and their salts and solvates have a number of uses as central muscle relaxants. In particular, treatment of conditions associated with abnormally raised skeletal muscle tone.
    Type: Grant
    Filed: December 18, 1995
    Date of Patent: February 16, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventors: James Leroy Kelley, Gregory Cooksey Rigdon, Barrett Randolph Cooper, Ed Williams McLean, David Lee Musso, Gloria Faye Orr, Jeffrey Leaman Selph, Virgil Lee Styles
  • Patent number: 5846956
    Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.
    Type: Grant
    Filed: July 7, 1997
    Date of Patent: December 8, 1998
    Assignee: Societe Civile Bioprojet
    Inventors: Jean-Christophe Plaquevent, Denis Danvy, Thierry Monteil
  • Patent number: 5847166
    Abstract: A method for preparing an aryl ether compound is provided in which an alcohol is reacted with an aromatic compound in the presence of a base, and a transition metal catalyst selected from the group consisting of platinum and nickel to form an aryl ether. The aromatic compound comprises an activated substituent, X, said activated substituent being a moiety such that its conjugate acid HX has a pKa of less than 5.0. The catalyst is preferably a soluble palladium complex in the presence of supporting ligands.
    Type: Grant
    Filed: October 10, 1996
    Date of Patent: December 8, 1998
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, John P. Wolfe, Michael Palucki
  • Patent number: 5837725
    Abstract: Bridged bicyclic aromatic compounds are provided having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined herein. The novel compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical compositions and methods for modulating gene expression are provided as well.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: November 17, 1998
    Assignees: SRI International, La Jolla Cancer Research Foundation
    Inventors: Marcia I. Dawson, James F. Cameron, Peter D. Hobbs, Ling Jong, Magnus Pfahl, Xiao-kun Zhang, Jurgen M. Lehmann
  • Patent number: 5821264
    Abstract: The present invention relates to novel tocotrienols and tocotrienol-like compounds displaying biological activity. The tocotrienols and tocotrienol-like compounds of this invention may be conveniently obtained from biological sources or by chemical synthesis and may be used in pharmaceutical compositions, foodstuffs and dietary supplements. This invention also relates to the use of tocotrienols, tocotrienol-like compounds, and mixtures thereof, as hypocholesterolemic, antithrombotic, antioxidizing, antiatherogenic, antiinflammatory and immunoregulatory agents, or as agents useful to decrease lipoprotein (a) concentration in the blood or to increase feed conversion efficiency.
    Type: Grant
    Filed: September 24, 1996
    Date of Patent: October 13, 1998
    Assignee: LipoGenics, Inc.
    Inventors: Ronald H. Lane, Asaf A. Qureshi, Winston A. Salser
  • Patent number: 5817836
    Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.
    Type: Grant
    Filed: May 12, 1997
    Date of Patent: October 6, 1998
    Assignee: Allergan
    Inventors: Vidyasagar Vuligonda, Roshantha A. Chandraratna
  • Patent number: 5795981
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: December 16, 1996
    Date of Patent: August 18, 1998
    Assignee: Polaroid Corporation
    Inventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
  • Patent number: 5739374
    Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.
    Type: Grant
    Filed: February 14, 1997
    Date of Patent: April 14, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Bernd Janssen, Hans-Heiner Wuest
  • Patent number: 5731324
    Abstract: This invention relates to certain bicyclic compounds having a nucleus formed of two fused six membered rings, for example, benzopyran, isoquinoline, isoquinolone, tetrahydronaphthalene, dihydronaphthalene, or tetralone, substituted with both basic and acidic functionality, which are useful in inhibition of platelet aggregation.
    Type: Grant
    Filed: January 19, 1995
    Date of Patent: March 24, 1998
    Assignee: Eli Lilly and Company
    Inventors: Matthew J. Fisher, Anne Marie Happ, Joseph A. Jakubowski, Michael Dean Kinnick, Allen D. Kline, Michael John Martinelli, John Michael Morin, Jr., Michael Paal, Gerd Ruhter, Kenneth James Ruterbories, Daniel J. Sall, Theo Schotten, Marshall A. Skelton, Wolfgang Stenzel, Robert Theodore Vasileff
  • Patent number: 5719291
    Abstract: Compounds of the formula ##STR1## which have antifungal activity.
    Type: Grant
    Filed: May 3, 1995
    Date of Patent: February 17, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Yuhko Aoki, Hiromichi Kotaki, Kazunao Masubuchi, Toru Okuda, Nobuo Shimma, Takuo Tsukuda, Isao Umeda
  • Patent number: 5719186
    Abstract: Novel carbocyclic amides together with their salts, solvates and physiologically active derivatives which have a number of uses in medicine, in particular as central muscle relaxants, and in the treatment or prophylaxis of anxiety, inflammation, arthritis and pain.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: February 17, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
  • Patent number: 5716624
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (1): ##STR1## in which X is one of the radicals: ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: February 10, 1998
    Assignee: C.I.R.D. Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5709867
    Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--, and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.
    Type: Grant
    Filed: December 15, 1994
    Date of Patent: January 20, 1998
    Assignee: Centre International De Recherches Dermatologiques Galderma
    Inventor: Jean-Michel Bernardon
  • Patent number: 5672723
    Abstract: The present invention can provide a process for the preparation of an 1-acyl-2-substituted hydrazine compound from a mixture containing the 1-acyl-2-substituted hydrazine and an 1-acyl-1-substituted hydrazine by selective hydrolysis or alcoholysis of the 1-acyl-yl-1-substituted hydrazine in the presence of an acid catalyst, and by separation of the resulting carboxylic acid and derivative thereof.The 1-acyl-2-alkyl hydrazine obtained has a high purity.
    Type: Grant
    Filed: February 21, 1996
    Date of Patent: September 30, 1997
    Assignees: Nippon Kayaku Kabushiki Kaisha, Sankyo Company, Limited
    Inventors: Hiroki Hotta, Hiroyasu Sugizaki, Tetsuya Toya, Mikio Yanagi
  • Patent number: 5672722
    Abstract: A silver halide color photographic material comprising a support having thereon at least one layer containing at least one compound represented by formula (A) ##STR1## wherein the definition of R.sub.a1, R.sub.a2, R.sub.a3, Z, Y, m and n is described in the specification.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 30, 1997
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Nobuo Seto, Yasuhiro Yoshioka, Masakazu Morigaki
  • Patent number: 5656750
    Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an aromatic unsaturated system conjugated with the squarylium ring and such that in the compounds of formulae Q.sup.1 CH.sub.2 R.sup.1 and Q.sup.2 CH.sub.2 R.sup.2 the methylene hydrogens are active hydrogens, R.sup.1 and R.sup.2 are each independently a hydrogen atom or an aliphatic or cycloaliphatic group, and R.sup.3 and R.sup.4 are each independently a hydrogen atom, or an acyl, aliphatic, cycloaliphatic, aromatic or heterocyclic group, subject to the proviso that one of R.sup.3 and R.sup.4 may be an amino or substituted amino group, or one of R.sup.3 and R.sup.4 is a hydrogen atom and the other is an organosulfonyl group, or R.sup.3 and R.sup.4 together with the intervening nitrogen atom form a nitrogenous heterocyclic ring) are useful as near infra-red absorbers.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 12, 1997
    Assignee: Polaroid Corporation
    Inventors: Richard M. Allen, Peter K. Chu
  • Patent number: 5629321
    Abstract: The invention relates to a novel compound which is represented by the formula (1) and has an excellent platelet aggregation inhibiting action based on fibrinogen antagonism. The platelet aggregation inhibitor containing the compound of the formula (1) as an effective ingredient are effective for prevention and curing of thrombosis and restenosis or reocclusion after percutaneous transluminal coronary angioplasty or percutaneous transluminal coronary recanalization.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: May 13, 1997
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Kunio Okumura, Isao Yokoyama, Toshiyuki Shimazaki, Michihiko Miyamoto, Hiroyuki Yamashita, Kenji Kibayashi, Takanori Yutaka, Kouhei Yazawa
  • Patent number: 5627283
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 6, 1997
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner St uber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5605896
    Abstract: This invention provides bicyclic heterocyclic derivatives and their pharmaceutically acceptable salts useful for the treatment of hypertension, urethral and lower urinary tract contractions, and other disorders. The compounds are also useful for binding .alpha..sub.1 -adrenergic and 5HT.sub.1A serotonergic receptors, in vitro or in vivo.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: February 25, 1997
    Assignee: Recordati S.A., Chemical and Pharmaceutical Company
    Inventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
  • Patent number: 5565191
    Abstract: Stilbene derivatives of formula (I) ##STR1## wherein A, R.sub.1 and R.sub.2 are as defined in the following, are useful for the protection against UV radiation.
    Type: Grant
    Filed: December 13, 1994
    Date of Patent: October 15, 1996
    Assignee: 3V Inc.
    Inventor: Giuseppe Raspanti
  • Patent number: 5519150
    Abstract: A process of preparing intermediates useful in making compounds with retinoic acid-like activity is disclosed. The intermediates are halogenated chromans and thiochromans of the formula shown below and are prepared by the alkylation of a phenol or thiophenol with an alkene compound (the starting materials shown in the formula below), cyclization and halogenation. ##STR1## In the formula the symbols have the following meanings: R.sub.1 and R.sub.2 are C.sub.1 to C.sub.4 alkyl, R.sub.3 is H or C.sub.1 to C.sub.4 alkyl, X is oxygen or sulfur, Y is a leaving group, and Z is chlorine, bromine or iodine.
    Type: Grant
    Filed: March 1, 1995
    Date of Patent: May 21, 1996
    Assignee: Allergan
    Inventors: Michael E. Garst, Lloyd J. Dolby, Nestor A. Fedoruk
  • Patent number: 5510538
    Abstract: A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.
    Type: Grant
    Filed: December 16, 1994
    Date of Patent: April 23, 1996
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Marco Frigerio, Simona Sputore, Marco Santagostino
  • Patent number: 5491238
    Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: February 13, 1996
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Ralph P. Volante, Kan K. Eng
  • Patent number: 5482942
    Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.
    Type: Grant
    Filed: June 28, 1994
    Date of Patent: January 9, 1996
    Assignee: American Home Products Corporation
    Inventors: Richard M. Soll, Paul J. Dollings
  • Patent number: 5480645
    Abstract: Hydroxyamines N-acyl derivatives with benzochroman or 2,3-dihydrobenzofuran carboxy acids and relative pharmaceutical composition for the therapeutic treatment of those CNS, vascular, cardiovascular, dermatologic and ophthalmic pathologies wherein it is important to associate an inflammatory modulation effect to an antioxidant activity.
    Type: Grant
    Filed: December 29, 1993
    Date of Patent: January 2, 1996
    Assignee: LifeGroup S.p.A.
    Inventors: Francesco Della Valle, Silvana Lorenzi, Gabriele Marcolongo
  • Patent number: 5476644
    Abstract: The present invention provides compounds of the formula ##STR1## chelated with a paramagnetic metal ion wherein Z1 and Z2 each represent the atoms necessary to complete a monocyclic or polycyclic carbocyclic or heterocyclic ring system, said Z1 and Z2 independently optionally substituted with R.sup.6 and R.sup.7, respectively;R.sup.l, R.sup.2, R.sup.3 and R.sup.4 are independently carboxyalkyl (C.sub.1 -C.sub.2), --(CH.sub.2).sub.n --C(.dbd.O)--NH--R.sup.8, or --(CH.sub.2).sub.n --C(.dbd.O)--O--R.sup.8R.sup.5 is carboxyalkyl (C.sub.1 -C.sub.2);R.sup.6 and R.sup.7 are independently hydrogen, benzyl, or benzyloxy, said benzyl or benzyloxy optionally substituted with one, two or three substituents selected from the group consisting of amino, isocyanato (--N.dbd.C.dbd.O), isothiocyanato (--N.dbd.C.dbd.S), --NH--C(.dbd.O)--X or --NH--C(.dbd.S)--X;R.sup.8 is alkyl (C.sub.1 -C.sub.20), --(CH.sub.2).sub.m --Ar, or polyhydroxyalkyl (C.sub.1 -C.sub.
    Type: Grant
    Filed: April 13, 1994
    Date of Patent: December 19, 1995
    Assignee: Sterling Winthrop Inc.
    Inventors: Carl R. Illig, Thomas J. Caulfield, John L. Toner, Peng Guo, David L. Ladd
  • Patent number: 5476860
    Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: December 19, 1995
    Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)
    Inventor: Jean-Michel Bernardon
  • Patent number: 5468879
    Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2, independently are alkyl groups having 2 to 8 carbons; R.sub.3 is hydrogen or lower alkyl; X is S, O or N--R.sub.4 where R.sub.4 is hydrogen or lower alkyl; Y is phenyl or pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl, and pyrazinyl; A is (CH.sub.2).sub.n where n is 0-5, or lower branched chain alkyl, alkenyl having 2 to 6 carbons and 1 or 2 double bonds, alkynyl having 2 to 6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a salt thereof, COOR.sub.5, CONR.sub.6 R.sub.7, --CH.sub.2 OH, CH.sub.2 OR.sub.8, CH.sub.2 OCOR.sub.8, CHO, CH(OR.sub.9).sub.2, CHOR.sub.10 O, --COR.sub.11, CR.sub.11 (OR.sub.9).sub.2, or CR.sub.11 OR.sub.10 O, where R.sub.5 is alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or R.sub.5 is phenyl or lower alkylphenyl, R.sub.6 and R.sub.7 independently are hydrogen, alkyl of 1 to 10 carbons, or cycloalkyl of 5 to 10 carbons, or phenyl or lower alkylphenyl, R.sub.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: November 21, 1995
    Assignee: Allergan, Inc.
    Inventor: Roshantha A. S. Chandraratna
  • Patent number: 5457114
    Abstract: Amidinophenylalanine derivatives of the formula I ##STR1## the synthesis of these compounds, the use thereof and pharmaceutical agents which contain these compounds are described.
    Type: Grant
    Filed: January 25, 1994
    Date of Patent: October 10, 1995
    Assignee: Behringwerke Aktiengesellschaft
    Inventors: Werner Stuber, Gerhard Dickneite, Rainer Koschinsky, Cenek Kolar
  • Patent number: 5438074
    Abstract: Certain 3-(phenyl, chroman-2-yl, benzofuran-5-yl or benzoxazol-5-yl)-2-(hydroxy or mercapto)propionic acid derivatives and analogs are useful as hypoglycemic and hypocholesterolemic agents.
    Type: Grant
    Filed: December 6, 1993
    Date of Patent: August 1, 1995
    Assignee: Pfizer Inc.
    Inventor: Bernard Hulin
  • Patent number: 5430060
    Abstract: The invention concerns novel N-phenylacetyl and related acyl derivatives of (4-amino-2,6-dimethylphenylsulphonyl)nitromethane and pharmaceutically acceptable salts thereof which are inhibitors of the enzyme aldose reductase and are of value, for example, in the treatment of certain peripheral effects of diabetes and galactosemia. Also disclosed are pharmaceutical compositions containing one of the derivatives and processes for the manufacture and use of the derivatives.
    Type: Grant
    Filed: September 15, 1993
    Date of Patent: July 4, 1995
    Assignee: Zeneca Limited
    Inventors: David R. Brittain, Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston, Linda Slater
  • Patent number: 5428052
    Abstract: Aromatic heterocyclic derivatives have the formula ##STR1## wherein R.sub.1 represents (i)--CH.sub.3, (ii)--CH.sub.2 OH or (iii) ##STR2## wherein R.sub.3 represents hydrogen, --OR.sub.4 wherein R.sub.4 represents hydrogen, alkyl having 1-20 carbon atoms or mono- or polyhydroxyalkyl or R.sub.3 represents ##STR3## wherein r' and r" represent hydrogen, lower alkyl or together form a heterocycle, R.sub.2 represents hydrogen or --CH.sub.3 and Ar represents ##STR4## wherein R.sub.6 is hydrogen or alkyl having 1-10 carbon atoms and R.sub.7 represents alkyl having 4-12 carbon atoms or cycoalkyl, Y is CH or a nitrogen atom and X represents oxygen, sulfur or --N--R.sub.8 when R.sub.8 represents hydrogen, lower alkyl or lower alkoxycarbonyl, with the proviso that (i) when Y is CH and X is oxygen or sulfur Ar is other than C and (ii) when Y is nitrogen and X is oxygen, Ar is other than (C) or (D) in which R.sub.6 is alkyl having 1-4 carbon atoms and R.sub.7 is branched alkyl having 4-12 atoms.
    Type: Grant
    Filed: December 2, 1993
    Date of Patent: June 27, 1995
    Assignee: Centre Internationale de Recherches Dermatologiques (C.I.R.D.)
    Inventors: Braham Shroot, Jacques Eustache, Jean-Michel Bernardon
  • Patent number: 5420295
    Abstract: A process of preparing intermediates useful in making compounds with retinoic acid-like activity is disclosed. The intermediates are halogenated chromans and thiochromans of the formula shown below and are prepared by the alkylation of a phenol or thiophenol with an alkene compound (the starting materials shown in the formula below), cyclization and halogenation. ##STR1## In the formula the symbols have the following meanings: R.sub.1 and R.sub.2 are C.sub.1 to C.sub.4 alkyl, R.sub.3 is H or C.sub.1 to C.sub.4 alkyl, X is oxygen or sulfur, Y is a leaving group, and Z is chlorine, bromine or iodine.
    Type: Grant
    Filed: January 19, 1994
    Date of Patent: May 30, 1995
    Assignee: Allergan, Inc.
    Inventors: Michael E. Garst, Lloyd J. Dolby, Nestor A. Fedoruk