The Additional Six-membered Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/151)
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Patent number: 5837702Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is alkyl, Y is a single bond, --CH.sub.2 --, --C(O)--, --O--, --S-- or --N(R.sup.8)-- where R.sup.8 is hydrogen, alkyl, haloalkyl, aryl, arylalkyl, cycloalkyl or (cycloalkyl)alkyl, and R.sup.1 to R.sup.7 are as defined herein. These compounds have potassium channel activating activity and are useful, therefore for example, as cardiovascular agents.Type: GrantFiled: August 30, 1994Date of Patent: November 17, 1998Assignee: Bristol-Myers Squibb Co.Inventors: George C. Rovnyak, Karnail S. Atwal, Dinos P. Santafianos, Charles Z. Ding
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Patent number: 5795981Abstract: 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: GrantFiled: December 16, 1996Date of Patent: August 18, 1998Assignee: Polaroid CorporationInventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5747528Abstract: Chroman derivatives of Formula I or a pharmaceutically acceptable salt thereof are inhibitors of VCAM-1 and ICAM-1 and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection ##STR1## wherein: R=Hydrogen or phenyl;R.sub.2 =Hydrogen or lower alkyl of from 1-4 carbon atoms;X=Oxygen or Sulfur;Y=(CH.sub.2).sub.n, --NR' where R' is hydrogen, alkyl of from 1 to 12 carbon atoms or aryl of from 6 to 10 carbon atoms, or Z; and Z is an alkyl or aryl containing moiety.Type: GrantFiled: January 24, 1997Date of Patent: May 5, 1998Assignee: Warner-Lambert CompanyInventor: Bharat Kakidas Trivedi
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Patent number: 5731293Abstract: A compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are, independently, --CON(R.sup.4)R.sup.5, or a monosaccharide, or acylated monosaccharide group, with the proviso that at least one of R.sup.1 and R.sup.2 is --CON(R.sup.4)R.sup.5, and R.sup.4 and R.sup.5 are, independently, a hydrogen atom, or a hydroxyl, alkyl, aryl, or aralkyl group, or R.sup.4 and R.sup.5 together with the nitrogen atom attached thereto form a 3- to 7-membered saturated cycloaliphatic amino group, and R.sup.3 is a hydrogen atom, or a hydroxyl, alkyl, aryl, aralkyl, or --COOR.sup.8 group, and R.sup.3 is at 3- or 4-position, and R.sup.8 is a hydrogen atom or an alkyl group, or a salt thereof is disclosed. The compound has a function to inhibit a matrix metalloproteinase.Type: GrantFiled: December 28, 1995Date of Patent: March 24, 1998Assignee: Kureha Chemical Industry Co., Ltd.Inventors: Koju Watanabe, Koichi Niimura, Toru Yamazaki, Hiroshi Maruoka
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Patent number: 5719145Abstract: The invention relates to a substituted amidine derivative which has an excellent platelet aggregation inhibiting action on the basis of fibrinogen antagonism and is particularly excellent in effectiveness on oral administration, and the platelet aggregation inhibitor containing the substituted amidine derivative of the invention as an effective ingredient is effective for prevention and treatment of thrombosis, and restenosis or reocclusion after percutaneous transluminal coronary angioplasty or percutaneous transluminal coronary recanalization.Type: GrantFiled: August 19, 1996Date of Patent: February 17, 1998Assignee: Mitsui Toatsu Chemicals, Inc.Inventors: Hiroyuki Yamashita, Kunio Okumura, Toshiyuki Shimazaki, Akihito Kanematsu, Yoji Aoki, Yuki Nakajima, Kouhei Yazawa, Kenji Kibayashi
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Patent number: 5703075Abstract: This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: December 30, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Ronald B. Gammill, Thomas M. Judge, Joel Morris
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Patent number: 5686486Abstract: The present invention relates to compounds of formula I which are 4-hydroxy-benzopyran-2-ones and 4-hydroxy-cycloalkyl?b!pyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus. ##STR1## Wherein R.sub.10 and R.sub.Type: GrantFiled: August 4, 1995Date of Patent: November 11, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Paul Kosta Tomich, Michael John Bohanon, Steven Ronald Turner, Joseph Walter Strohbach, Suvit Thaisrivongs, Richard C. Thomas, Karen Rene Romines, Chih-Ping Yang, Paul Adrian Aristoff, Harvey Irving Skulnick, Paul D. Johnson, Ronald B. Gammill, Qingwei Zhang, Gordon L. Bundy, David John Anderson, Lee S. Banitt
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Patent number: 5656750Abstract: 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: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu
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Patent number: 5650456Abstract: This invention relates to coumarin derivatives of formula (I) ##STR1## where Z represents OR.sup.3 or NR.sup.4 R.sup.5,to their preparation, and to their use for the production of polymers with luminophors on their side chains.Type: GrantFiled: February 9, 1996Date of Patent: July 22, 1997Assignee: Bayer AktiengesellschaftInventors: Chen Yun, Rolf Wehrmann, Burkhard Kohler
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Patent number: 5607939Abstract: The compound ##STR1## wherein ring A represents a benzene ring; Ar represents an aromatic group; R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group; m represents an integer of 1 to 6; n represents an integer of 2 to 3; ----- represents a single bond or a double bond; X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where ----- is a single bond or .dbd.N-- where ----- is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.Type: GrantFiled: April 25, 1995Date of Patent: March 4, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
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Patent number: 5605896Abstract: 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: GrantFiled: August 31, 1994Date of Patent: February 25, 1997Assignee: Recordati S.A., Chemical and Pharmaceutical CompanyInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Rodolfo Testa
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Patent number: 5580863Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.Type: GrantFiled: May 13, 1994Date of Patent: December 3, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Shigehisa Taketomi, Tsuneo Oda
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Patent number: 5543517Abstract: This invention relates to substituted bicyclic phosphoramides and derivatives thereof, useful as retroviral protease inhibitors and as standards and reagents in determining the ability of a potential pharmaceutical to inhibit viral replication or HIV protease, to pharmaceutical compositions comprising such compounds, and to methods of using these compounds for treating viral infection.Type: GrantFiled: January 13, 1994Date of Patent: August 6, 1996Assignee: The DuPont Merck Pharmaceutical CompanyInventor: Joanne M. Smallheer
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Patent number: 5539112Abstract: 5-Aminoflavone derivatives represented by the formula (I): ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and represent hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, halogen-substituted or unsubstituted lower alkanoyl or lower alkoxycarbonyl, X.sup.1, X.sup.2, Y.sup.1 and Y.sup.2 are the same or different and represent hydrogen, halogen or lower alkyl, at least one of X.sup.1 and X.sup.2 represents halogen or lower alkyl, X.sup.3 represents hydrogen, substituted or unsubstituted lower alkyl, lower alkenyl, lower alkynyl, halogen, hydroxy, substituted or unsubstituted lower alkoxy, NR.sup.5 R.sup.6 (wherein R.sup.5 and R.sup.6 are the same or different and represent hydrogen, or substituted or unsubstituted lower alkyl, or R.sup.5 and R.sup.Type: GrantFiled: June 5, 1995Date of Patent: July 23, 1996Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Akama, Shun-ichi Ikeda, Yasushi Shida, Masaji Kasai, Hiroyuki Ishida, Uichiro Kimura, Katsushige Gomi, Hiromitsu Saito, Kimihisa Ueno
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Patent number: 5536833Abstract: A process for preparing compounds of the formula ##STR1## where a, b, c, R.sub.1, R.sub.2, and R.sub.3 are as defined herein including the step of alkylating a phenol of formula ##STR2## with an acetylene of formula ##STR3## where X is chlorine; bromine; --OC(O)--R.sub.5, where R.sub.5 is alkyl, aryl or substituted aryl; or --OCO.sub.2 R.sub.6, where R.sub.6 is alkyl or ##STR4## in the presence of a catalytic amount of a cuprous or cupric salt. The compounds of formula I are intermediates useful in the preparation of pyranyl cyanoguanidine derivatives.Type: GrantFiled: May 26, 1995Date of Patent: July 16, 1996Assignee: E. R. Squibb & Sons, Inc.Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas C. Sedergran, Nachimuthu Soundararajan
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Patent number: 5506262Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: November 10, 1993Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
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Patent number: 5500425Abstract: Compounds of the formula I ##STR1## processes for their preparation, pharmaceutical preparations, use of and method of treatment of disorders in CNS by using compounds of formula I.Type: GrantFiled: September 9, 1994Date of Patent: March 19, 1996Assignee: Aktiebolaget AstraInventors: Lars-Gunnar Larsson, Lucy A. Renyl, Svante B. Ross, Daniel D. Sohn, Seth-Olov Thorberg
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Patent number: 5457103Abstract: Compounds of the general formula (I): ##STR1## in which R represents: a hydrogen atom, ora radical --OR'in which R' is as defined in the description.Type: GrantFiled: August 18, 1993Date of Patent: October 10, 1995Assignee: Adir et CompagnieInventors: Yves Rolland, Guy Lewin, Jean-Paul Vilaine, Albert Lenaers, Catherine Thollon
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Patent number: 5428027Abstract: Certain substituted semicarbazones, including all geometric and stereoisomers thereof, agricultural compositions containing them and their use as arthropodicides.Type: GrantFiled: October 28, 1993Date of Patent: June 27, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventors: John P. Daub, George P. Lahm, Bradford S. Marlin
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Patent number: 5412117Abstract: Benzopyran derivatives represented by formula (I): ##STR1## wherein X represents =O, =S, =N-Z (Z represents a lower alkyl group, etc.), or =CHNO.sub.2 ; Y represents a substituted amino group, an alkoxy group, an alkylthio group, etc., and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 each represent a hydrogen atom, a lower alkyl group, etc., are disclosed. The benzopyran derivatives exhibit K.sup.+ channel activating activities and are widely applicable as antiasthmatics, antiepileptics, and the like.Type: GrantFiled: January 26, 1993Date of Patent: May 2, 1995Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroshi Koga, Hiroyuki Nabata
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Patent number: 5405976Abstract: 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: GrantFiled: September 24, 1993Date of Patent: April 11, 1995Assignee: Polaroid CorporationInventors: Stephen J. Telfer, Robert P. Short, Stephen G. Stroud, Anthony J. Puttick, Socorro Ramos, Michael J. Zuraw
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Patent number: 5354873Abstract: 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: GrantFiled: November 20, 1992Date of Patent: October 11, 1994Assignee: Polaroid CorporationInventors: Richard M. Allen, Peter K. Chu, John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5326783Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.Type: GrantFiled: January 19, 1993Date of Patent: July 5, 1994Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Chan-Hwa Kuo, Conrad Santini
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Patent number: 5300522Abstract: The invention relates to compounds of the formula ##STR1## wherein R.sup.1 is hydrogen. acyl, lower-alkyl or --CHO, --CH.sub.2 OR.sup.10, --COR.sup.7 or OR.sup.13 ; R.sup.2, R.sup.3 and R.sup.4 are, independently, hydrogen, lower-alkyl, lower-alkoxy or halogen; R.sup.5 and R.sup.5 are, independently, hydrogen or lower-alkyl; R.sup.7 is hydroxy, lower-alkoxy or NR.sup.8 R.sup.9 ; R.sup.8 and R.sup.9 are, independently, hydrogen or lower-alkyl; X and Y are, independently, >CR.sup.14 R.sup.15, --O--, --S--, >SO, >SO.sub.2 or >NR.sup.18 ; R.sup.10 and R.sup.18 are, independently, hydrogen, lower-alkyl or acyl; M is --C(R.sup.11).dbd.C(R.sup.12)--, --CONH-- or --NH--CO--; R.sup.11, R.sup.12, R.sup.14 and R.sup.15 are, independently, hydrogen or lower-alkyl, R.sup.Type: GrantFiled: August 18, 1992Date of Patent: April 5, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
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Patent number: 5300656Abstract: Coumarin deviatives of the formula ##STR1## in which R.sup.1 denotes cyano,R.sup.2 represents phenyl or thiazolyl bonded in the 2-, 4-, or 5-position,R.sup.3 denotes hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxycarbonyl-C.sub.1 -C.sub.4 -alkyl andR.sup.4 represents hydrogen, C.sub.1 -C.sub.4 -alkyl or phenylsulphonyl, where C.sub.1 -C.sub.4 -alkyl can be substituted by hydroxyl, amino, carboxyl or C.sub.1 -C.sub.4 -alkoxy-carbonyl and phenyl can be monosubstituted or disubstituted by chlorine, bromine or C.sub.1 -C.sub.4 -alkyl, where furthermore R.sup.3 and R.sup.4, together with the N atom which they substitute, can denote a morpholine ring, a piperazine ring or a triazole ring which can carry one or two substituents from the group comprising methyl, ethyl and phenyl, andwhere furthermore one of the radicals R.sup.2, R.sup.3 and R.sup.4 denotes or carries a primary or secondary amino group, the hydroxyl group, the carboxyl group or the C.sub.1 -C.sub.Type: GrantFiled: July 16, 1992Date of Patent: April 5, 1994Assignee: Bayer AktiengesellschaftInventors: Eberhard Kuckert, Gunther Beck, Florin Seng, Antonius Lobberding
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Patent number: 5280024Abstract: Compounds of the general formula (I): ##STR1## in which R represents: a hydrogen atom, ora radical --OR'in which R' is as defined in the description.Type: GrantFiled: March 25, 1993Date of Patent: January 18, 1994Assignee: Adir et CompagnieInventors: Yves Bolland, Guy Lewin, Jean-Paul Vilaine, Lenaers Albert, Catherine Thollon
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Patent number: 5278174Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.Type: GrantFiled: May 17, 1991Date of Patent: January 11, 1994Assignee: Scios Nova, Inc.Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
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Patent number: 5276168Abstract: A new method for the treatment of ischemic conditions and arrhythmia is disclosed. The method uses compounds of the formula ##STR1## wherein A can be --CH.sub.2 --, --O--, --NR.sub.9 --, --S--, --SO--, --SO.sub.2 --; X can be oxygen or sulfur; Y can be --NR.sub.8, --O--, --S--, --CH.sub.2 -- and the R groups are as defined herein. Novel compounds within the definition of formula I are also disclosed.Type: GrantFiled: June 19, 1992Date of Patent: January 4, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5262549Abstract: 4-[3-(benz[b]pyran-4-ylidene)prop-1-enyl]benz[b]pyrylium, 4-[5-(4H-benz[b]pyran-4-ylidene)penta-1,3-dienyl]benz[b]pyrylium and 4-[7-(4H-benz[b]pyran-4-ylidene)hepta-1,3,5-trienyl]benz[b]pyrylium dyes, wherein at least one of the benzpyrylium nuclei carries at its 2-position a substituent in which a non-aromatic carbon atom is bonded directly to the benzpyrylium nucleus, subject to the proviso that if the or each 2-substituent contains an aromatic nucleus, this aromatic nucleus is not conjugated with the benzpyrylium nucleus, are useful as visible and near infra-red absorbers, having high extinction coefficients and a reduced tendency to develop absorptions at shorter wavelengths when dispersed in polymeric media.Type: GrantFiled: March 29, 1993Date of Patent: November 16, 1993Assignee: Polaroid CorporationInventors: Stephen J. Telfer, Socorro M. Ramos, Michael J. Zuraw
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Patent number: 5238954Abstract: A fluorinated flavone acetic acid suitable for use as an antitumor agent. Pharmaceutical compositions comprising the fluorinated flavone acetic acid and a pharmaceutically acceptable carrier. An antitumor composition comprising an antitumor effective amount of a fluorinated flavone acetic acid in a pharmaceutically acceptable carrier.Type: GrantFiled: July 18, 1991Date of Patent: August 24, 1993Assignee: The Upjohn CompanyInventor: Paul A. Aristoff
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Patent number: 5236935Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.Type: GrantFiled: May 21, 1992Date of Patent: August 17, 1993Assignee: Korea Research Institute of Chemical TechnologyInventors: Sung-Eun Yoo, Kyu Y. Yi, Nak C. Jeong, Jee H. Suh, Seon-Ju Kim, Hwa-Sup Shin, Byung H. Lee, Kyu S. Jung
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Patent number: 5227499Abstract: Squarylium compounds of the formula: ##STR1## in which: Q.sup.1 and Q.sup.2 are each a Chromophoric group having an 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; andR.sup.3, R.sup.4 and R.sup.5 are each independently a hydrogen atom, or an aliphatic, cycloaliphatic, aromatic or heterocyclic group, or an electron-withdrawing group able to lower the electron density at the carbon atom to which it is attached, subject to the provisoes that:two of R.sup.3, R.sup.4 and R.sup.5 may form a divalent group of which a single atom is double bonded to the carbon atom to which the two groups are attached, or all three of R.sup.3, R.sup.4 and R.sup.Type: GrantFiled: November 20, 1991Date of Patent: July 13, 1993Assignee: Polaroid CorporationInventors: Donald A. McGowan, Mark R. Mischke, Stephen J. Telfer
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Patent number: 5227498Abstract: Squarylium compounds of the formula: ##STR1## (in which Q.sup.1 and Q.sup.2 are each a chromophoric group having an 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 aliphatic, cycloaliphatic, aromatic or heterocyclic 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 cycloaliphatic or aromatic ring) are useful as near infra-red absorbers.Type: GrantFiled: November 20, 1991Date of Patent: July 13, 1993Assignee: Polaroid CorporationInventors: John W. Lee, Donald A. McGowan, Mark R. Mischke, Socorro M. Ramos, Stephen J. Telfer
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Patent number: 5179092Abstract: A compound having the formula (I): ##STR1## wherein A is --CH.sub.2 --, --O--, or --S--; R.sup.1 is CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydroxy or carboxy which may be optionally esterized or amidated; R.sup.3 is H or a lower alkyl; and n is 0 or an integer of 1 to 6 or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 30, 1991Date of Patent: January 12, 1993Assignee: Suntory LimitedInventors: Toshio Tatsuoka, Kenji Suzuki, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
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Patent number: 5177216Abstract: The present invention provides a new diastereomer ester compound which is useful as an intermediate in the making of an optically active 3,4-dihydro-3,4-epoxy-2H-1-benzopyran compound.Type: GrantFiled: May 13, 1991Date of Patent: January 5, 1993Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventor: Tsutomu Yamanaka
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Patent number: 5140031Abstract: Novel compounds having the formula ##STR1## wherein ##STR2## are disclosed. These compounds have potassium channel activating activity and are useful, for example, as cardiovascular agents, especially as antiischemic agents.Type: GrantFiled: February 27, 1991Date of Patent: August 18, 1992Assignee: E. R. Squibb & Sons, Inc.Inventors: Karnail Atwal, Gary J. Grover, Kyoung S. Kim
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Patent number: 5130310Abstract: Benzo[b]pyran derivatives of the formula I ##STR1## with E--D equal to CH--CHOH or C.dbd.CH;X equal to oxygen or sulfur;Y equal to oxygen, sulfur, SO, SO.sub.2 or NR.sup.9 ;R.sup.1 equal to CN, NO.sub.2, Hal, alkoxycarbonyl, SO.sub.1-2 -alkyl or SO.sub.1-2 -aryl;R.sup.2 equal to H, OH, alkoxy, alkyl, Hal, NR.sup.10 R.sup.11 ;R.sup.3 /R.sup.4 equal to alkyl;R.sup.5 /R.sup.6 equal to alkyl, (CH.sub.2).sub.1-6 COO-alkyl, (CH.sub.2).sub.1-6 CONR.sup.10 R.sup.11, (CH.sub.2).sub.0-6 COOH, (CH.sub.2).sub.1-6 CO-alkyl, CO.sub.2 -alkyl, alkylmercaptoalkyl, alkylsulfi(i)(o)nyl, hydroxyalkyl, mercaptoalkyl, aminoalkyl, N-(di)-alkylaminoalkyl or (CH.sub.2).sub.f Ar with f equal to zero-3;R.sup.7 /R.sup.8 equal to hydrogen, alkyl or phenyl, and m equal to zero-2are outstanding antihypertensives and spasmolytics. Preparation processes and use are described.Type: GrantFiled: January 19, 1990Date of Patent: July 14, 1992Assignee: Hoechst AktiengesellschaftInventors: Klaus Weidman, Heinrich C. Englert, Bernward Scholkens, Martin Bickel
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Patent number: 5128348Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.Type: GrantFiled: September 12, 1990Date of Patent: July 7, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Gregory S. Basarab
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Patent number: 5116954Abstract: Substituted six-membered benzo-fused heterocycles of the formula (I) ##STR1## in which: X=0, NH, S.fwdarw.(O).sub.n (n=0 or 2);R.sub.1 is phenyl, phenyl substituted by methoxy, hydroxy, chlorine, fluorine, diethylaminoethoxy, phenoxy, 2-methyl-4-thiazolyl, 2-amino-4-thiazolyl, phenyl, amino, nitro, terbutyl, carboxymethyl, acetamido, dimethyltriazenyl, benzoyl, hexyl, undecyl, trifluoromethyl, carbamoyl; or R.sub.1 is trifluoromethyl, pyridyl-2,pyridyl-4;R.sub.2 is H, methoxy, hydroxy; orR.sub.1 and R.sub.2 are --CH.dbd.CH--CH.dbd.CH--;R.sub.3 and R.sub.4 are methoxy, hydroxy, fluorine or form a fused benzene ring;CR.sub.5 R.sub.6 R.sub.7 is carboxymethyl, --CH.sub.2 --PO.sub.3 H,--CH.sub.2 --PO(oET).sub.2, 4-methylpiperazinyl, aminomethyl,3-4-5-trimethoxyphenylaminomethyl, acetyl, bromoacetyl, hydroxyethyl, acetoxyethyl, mercaptomethyl, acetylthiomethyl, methoxy-carbopnylthiomethyl, --CH--CONH.sub.2, ##STR2## substituted thiazolyl, subsituted furanone, imidazo(1,2-a)pyridinyl, indolizinyl, or R.sub.4 and R.Type: GrantFiled: August 2, 1989Date of Patent: May 26, 1992Assignee: Lipha, Lyonnaise Industrielle PharmaceutiqueInventors: Philippe Briet, Jean-Jacques Berthelon, Francois Collonges
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Patent number: 5095016Abstract: A compound of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is a hydrogen atom, a substituted or unsubstituted C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group or a R.sup.7 --CO-- group (wherein R.sup.7 is a C.sub.1-6 alkyl group, a phenyl group, a C.sub.2-6 alkenyl group which may be substituted by a phenyl group, or a C.sub.1-6 alkoxy group);R.sup.2 is a hydrogen atom, a substituted or unsubstituted C.sub.1-8 alkyl group, or a phenyl group;R.sup.3 is a hydrogen atom, and R.sup.4 is a hydroxyl group, or R.sup.3 and R.sup.4 together form a bond;each of R.sup.5 and R.sup.6 is a C.sub.1-4 alkyl group; andY is a cyano group, a halogen atom, a nitro group, a C.sub.1-6 alkyl group, a C.sub.2-6 alkynyl group, a C.sub.1-6 alkylcarbonyl group, a C.sub.1-6 alkoxy group, a di-C.sub.1-6 alkylaminocarbonyl group, an aryl group, a C.sub.1-6 alkoxycarbonyl group, a carboxyl group or a morpholinocarbonyl group.Type: GrantFiled: August 3, 1990Date of Patent: March 10, 1992Assignee: Kaken Pharmaceutical Co., Ltd.Inventors: Katuyuki Ohtuka, Nobuo Ishiyama, Yasuhito Iida, Kenji Seri, Takeshi Murai, Kazuko Sanai, Yoshihiro Ishizaka
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Patent number: 5061813Abstract: Novel compounds are disclosed having the formula ##STR1## and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are as defined herein. These compounds are useful, for example, as cardiovascular agents and especially as anti-ischemic agents.Type: GrantFiled: April 2, 1990Date of Patent: October 29, 1991Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 5013734Abstract: The esters of phenylalkanoic acid of the formula: ##STR1## wherein R.sup.1 is 4-10 membered, saturated or unsaturated, mono- or bi-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen,(ii) two or three of nitrogen and sulfur in total, or(iii) one or two sulfur;R.sup.2 is hydrogen; orR.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, form 4-7 membered, saturated or unsaturated, mono-cyclic hetero ring containing as hetero atoms:(i) one or two nitrogen, or(ii) two or three of nitrogen and oxygen in total,the aforementioned hetero rings, represented by R.sup.1 or formed by R.sup.1 and R.sup.2, taken together with a nitrogen to which they are attached, may be substituted by one substituent selected from C1-4 alkyl and C2-5 acyl;R.sup.3 each, independently, is hydrogen or C1-4 alkyl;R.sup.4 is hydrogen, halogen, trihalomethyl, C1-4 alkyl, C1-4 alkoxy, C2-5 acyl, cyano, nitro or nitroxy;R.sup.5 each, independently, is hydrogen, C1-4 alkyl or phenyl; or the two R.sup.Type: GrantFiled: May 11, 1990Date of Patent: May 7, 1991Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Sadahiko Iguchi, Masanori Kawamura, Tsumoru Miyamoto
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Patent number: 4975455Abstract: Compounds of general formula (I): ##STR1## in which: R denotes a hydrogen atom, a halogen atom or a hydroxy, lower alkyl, lower alkyloxy, carboxyl, (lower alkyloxy)carbonyl, (lower arylalkyloxy)carbonyl, aminocarbonyl, (lower mono- or dialkyl)aminocarbonyl or (lower arylalkyl)aminocarbonyl group, an aminocarbonyl group N-substituted with a heterocyclic radical, or a thio, (lower alkyl)thio, sulfonyl or (lower alkyl)sulfonyl group,R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be identical or different, denote a hydrogen atom, a halogen atom or a lower alkyl, lower alkenyl, lower alkyloxy or lower alkenyloxy group, optionally substituted with one or more halogen atoms,their isomers, enantiomers, diastereoisomers and also, when R denotes a carboxyl, their addition salts with a pharmaceutically acceptable base and, when R contains a basic group, their addition salts with a pharmaceutically acceptable acid.Type: GrantFiled: April 11, 1989Date of Patent: December 4, 1990Assignee: Adir et CieInventors: Jean-Daniel Brion, Guillaume Le Baut, Patrick Ducrey, Sylvie Piessard-Robert, Claude Cudennec, Genevieve Seurre
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Patent number: 4973694Abstract: A 6-tertiary amino-2-(Z.dbd.CH--)benzofuran dye is disclosed, where Z represents the atoms providing an electron withdrawing group and a conjugated methine linkage completing a resonant dye chromophore including the 6-tertiary amino group as an electron donor and the electron withdrawing group as an electron acceptor. The dyes are formed by condensing a 6-tertiary amino-2-formylbenzofuran with an electron withdrawing dye nucleus precursor containing an active methyl or methylene site. The dyes exhibit bathocromically shifted absorption peaks.Type: GrantFiled: August 17, 1989Date of Patent: November 27, 1990Assignee: Eastman Kodak CompanyInventors: Chin H. Chen, John L. Fox
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Patent number: 4963568Abstract: Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.Type: GrantFiled: May 31, 1989Date of Patent: October 16, 1990Assignee: Abbott LaboratoriesInventors: Robert W. Schoenleber, John W. Kebabian, Yvonne C. Martin, Michael P. DeNinno, Richard J. Perner, David M. Stout, Chi-Nung W. Hsiao, Stanley DiDomenico, Jr., John F. DeBernardis, Fatima Z. Basha, Michael D. Meyer, Biswanath De
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Patent number: 4960908Abstract: Novel isoflavone derivatives are provided which have the formula ##STR1## and which exhibit cancerocidal and immunosuppressive activity. The invention also provides pharmaceutical compositions containing the derivatives, methods of use and processes for their preparation.Type: GrantFiled: October 21, 1988Date of Patent: October 2, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Hiroshi Ogawara, Shunichi Watanabe
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Patent number: 4958021Abstract: Benzopyran derivatives of the formula ##STR1## where X is the radical ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4 and also the ring A have defined meanings are used in pressure- or heat-sensitive layers.Type: GrantFiled: July 19, 1988Date of Patent: September 18, 1990Assignee: BASF AktiengesellschaftInventors: Andreas Guentner, Udo Mayer, Andreas Oberlinner
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Patent number: 4954518Abstract: This invention relates to a 4H-1-benzopyran-4-one derivative represented by the formula: ##STR1## or a salt thereof, a process for producing the same and a pharmaceutical composition comprising the same as active ingredient.Type: GrantFiled: October 7, 1988Date of Patent: September 4, 1990Assignee: Toyama Chemical Company, Ltd.Inventors: Shuntaro Takano, Chosaku Yoshida, Takihiro Inaba, Keiichi Tanaka, Ryuko Takeno, Hideyoshi Nagaki, Tomoya Shimotori, Shinji Makino
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Patent number: 4929627Abstract: Benzo-fused cycloalkane and oxa- and thia-cycloalkane trans-1,2-diamine compounds of the formula: ##STR1## wherein A, B, C, D, n, X, Y, R, R.sup.1, R.sup.2 and R.sup.3 are as defined in the specification, e.g., trans-3,4-dichloro-N-methyl-N-[2-(pyrrolidin-1-yl)-5-methoxy-1,2,3,4-tetra hydronaphth-1-yl]benezeneacetamide, and the pharmaceutically acceptable salts or N-oxides thereof, are useful as analgesics and/or diuretics.Type: GrantFiled: June 7, 1989Date of Patent: May 29, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventors: Penio Pennev, Parthasarathi Rajagopalan, Richard M. Scribner