Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 544/375)
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Patent number: 6025385Abstract: This invention relates to a taxane derivative represented by the following formula (1): wherein at least one of X and Y represents a group --CO--A--B in which A represents a single bond, an alkylenecarbonyl group or the like and B represents a substituted or unsubstituted piperidino group or the like, the other represents a tert-butoxycarbonyl group or the like, and Z represents a hydrogen atom or a triethylenesilyl group, and also to a drug containing the same.This compound has high solubility in water and also has excellent antitumor activities.Type: GrantFiled: January 14, 1999Date of Patent: February 15, 2000Assignee: Kabushiki Kaisha Yakult HonshaInventors: Hideaki Shimizu, Atsuhiro Abe, Takashi Yaegashi, Seigo Sawada, Hiroshi Nagata
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Patent number: 6022497Abstract: Described are novel photochromic six-membered heterocyclic-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted six-membered heterocyclic group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline) type compounds.Type: GrantFiled: March 19, 1999Date of Patent: February 8, 2000Assignee: PPG Industries Ohio, Inc.Inventor: Anil Kumar
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Patent number: 6017915Abstract: The present invention relates to novel N-substituted amino alcohols, amino acids and acid derivatives thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 15, 1998Date of Patent: January 25, 2000Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Uffe Bang Olsen, Peter Madsen, Zdenek Polivka, Otylie Konigova, Frantisek Miksik, Martina Kovandova, Alexandra Silhankova, Karel Sindelar
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Patent number: 5998464Abstract: The compounds of the present invention are those of structural formula (I) ##STR1## wherein X is oxygen or sulfur. Pharmaceutical compositions and methods of use of the compounds in the treatment of hyperandrogenic conditions are disclosed. In addition, the combination of the compounds with other active agents such as finasteride, minoxidil and retinoic acid or a derivative thereof is disclosed.Type: GrantFiled: April 23, 1998Date of Patent: December 7, 1999Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Gool F. Patel, Gary H. Rasmusson, Richard L. Tolman
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Patent number: 5932725Abstract: The present invention relates to a novel chromene compound having favorable photochromic properties, developing a color of a high density, exhibiting a small degree of initial color and permitting the color to quickly fade.Type: GrantFiled: April 30, 1998Date of Patent: August 3, 1999Assignee: Tokuyama CorporationInventors: Yuichiro Kawabata, Tsuneyoshi Tanizawa, Tadashi Hara
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Patent number: 5916889Abstract: The present invention relates to 1,4-disubstituted piperazines of the general formula ##STR1## wherein X, Y, Z, R.sup.1, R.sup.2 and r are as defined in the detailed part of the present description or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation as well as their use for the treatment of indications caused by or related to the secretion and circulation of insulin antagonizing peptides, e.g. non-insulin-dependent diabetes mellitus (NIDDM) and ageing-associated obesity.Type: GrantFiled: October 3, 1997Date of Patent: June 29, 1999Assignee: Novo Nordisk A/SInventors: Rolf Hohlweg, Peter Madsen, Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Brett Watson, Zdenek Polivka, Otylie Konigova, Martina Kovandova, Alexandra Silhankova, Vladimir Valenta
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Patent number: 5877317Abstract: Novel aromatic bicyclic amines of formula (I) ##STR1## are useful in treating central nervous system disorders and cardiac arrhythmias and cardiac fibrillation.Type: GrantFiled: June 24, 1996Date of Patent: March 2, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Ruth E. TenBrink, Michael D. Ennis, Robert A. Lahti
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Patent number: 5834459Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd. and C(O);Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which D4 receptor stimulation is implicated, such as schizophrenia, is also described.Type: GrantFiled: April 1, 1996Date of Patent: November 10, 1998Assignee: Allelix Biopharmaceuticals Inc.Inventor: Jian-Min Fu
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Patent number: 5801175Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: September 13, 1996Date of Patent: September 1, 1998Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Adriano Afonso, John J. Baldwin, Ronald J. Doll, Ge Li, Alan K. Mallams, F. George Njoroge, Dinanath F. Rane, John C. Reader, Randall R. Rossman
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Patent number: 5783116Abstract: Described are novel pentahydrophenanthro?9,10-b!pyrans and tetrahydrocyclopenta?c!-naphtho?1,2-b!pyrans. Also described are polymeric organic host materials that contain or that are coated with such compounds.Type: GrantFiled: October 16, 1997Date of Patent: July 21, 1998Assignee: PPG Industries, Inc.Inventor: Jibing Lin
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Patent number: 5763609Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1 or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'R", or --NR'R" where R' and R" independently represent hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders.Type: GrantFiled: March 21, 1996Date of Patent: June 9, 1998Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5710274Abstract: Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof, wherein: R.sub.1, R.sub.2, R.sub.3, R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C.sub.1 -C.sub.6 alkoxy, --O.sub.2 CR', --NHCOR', --COR', --SO.sub.m R', where R' is C.sub.1 -C.sub.6 alkyl and wherein m is 0, 1, or 2; orR.sub.1, R.sub.2, R.sub.3, R.sub.4 independently represent --CONR'.sub.m, or --NR'.sub.m where m is 0, 1 or 2 and R' is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; andR represents an aminoalkyl group,which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockage such as substance abuse and obsessive compulsive disorders.Type: GrantFiled: February 28, 1996Date of Patent: January 20, 1998Assignee: Neurogen CorporationInventors: Jun Yuan, Xi Chen
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Patent number: 5705102Abstract: A naphthopyran compound represented by the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are each selected from the group consisting essentially of hydrogen, a stable organic radical, a heterocyclic group, a halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound and wherein A is a substituted divalent aromatic radical that includes substituents selected from the group consisting essentially of hydrogen and the stable organic radical.Type: GrantFiled: May 31, 1995Date of Patent: January 6, 1998Assignee: Vision-Ease Lens, Inc.Inventors: Frank J. Hughes, Edward A. Travnicek
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Patent number: 5658501Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b] pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: June 14, 1995Date of Patent: August 19, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5658500Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho-portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: June 14, 1995Date of Patent: August 19, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5656206Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the number 5 carbon atom of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 6, 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: June 14, 1995Date of Patent: August 12, 1997Assignee: Transitions Optical, Inc.Inventors: David B. Knowles, Barry Van Gemert, Anil Kumar
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Patent number: 5651923Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds fused on the naphtho-portion of the naphthopyran ring with an indeno group or certain heterocyclic substituents. Certain substituents are also present at the 2 and 5 positions and sometimes at the 6 position of the naphthopyran ring. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 12, 1995Date of Patent: July 29, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5650098Abstract: Described are novel reversible photochromic 2H-naphtho[1,2-b]pyran compounds, examples of which are compounds having certain substituents at the 5 and 6-positions of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring, e.g., 2,2-bis(4-methoxy phenyl)-5-methoxycarbonyl-6-morpholino-2H-naphtho[1,2-b]pyran. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: October 13, 1995Date of Patent: July 22, 1997Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, David B. Knowles, Barry Van Gemert
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Patent number: 5628935Abstract: A naphthopyran compound represented by the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are each selected from the group consisting essentially of hydrogen, a stable organic radical, a heterocyclic group, a halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound and wherein A is a substituted divalent aromatic radical that includes substituents selected from the group consisting essentially of hydrogen and the stable organic radical.Type: GrantFiled: October 28, 1994Date of Patent: May 13, 1997Assignee: Vision-Ease Lens, Inc.Inventors: Frank J. Hughes, Edward A. Travnicek
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Patent number: 5571914Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.Type: GrantFiled: June 6, 1995Date of Patent: November 5, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
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Patent number: 5543533Abstract: Photochromic products belonging to the group of chromenes having general formula (I): ##STR1##Type: GrantFiled: June 2, 1994Date of Patent: August 6, 1996Assignee: Great Lakes Chemical Italia S.r.l.Inventors: Pietro Allegrini, Nereo Nodari, Luciana Crisci, Vincenzo Malatesta
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Patent number: 5536847Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.Type: GrantFiled: June 6, 1995Date of Patent: July 16, 1996Assignee: Taiho Pharmaceutical Co. Ltd.Inventors: Tadafumi Terada, Katsuhiko Fujimoto, Makoto Nomura, Junichi Yamashita, Setsuo Takeda, Takashi Kobunai, Hideo Yamaguchi, Konstanty Wierzba
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Patent number: 5512567Abstract: Analgesic compounds of the formula (I); ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents oxygen or an imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is an aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen; provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.4 together represent a group of the formula (IV).Type: GrantFiled: January 17, 1995Date of Patent: April 30, 1996Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
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Patent number: 5508450Abstract: Benzopyran derivatives which have an inhibitory effect on the Maillard reaction as well as an antioxidizing effect are described herein. These derivatives may be utilized in the treatment and/or prevention of diabetic complications such as, for example, coronary heart disease, peripheral circulatory insufficiency or failure, cerebrovascular hindrance, neurogenous diabetes, nephropathy, arteriosclerosis, arthrosclerosis, cataracts and retinopathy. Further, the derivatives may also be used in the treatment and/or prevention of diseases induced by aging and in the treatment and/or prevention of diseases caused by the formation of peroxidized fat.Type: GrantFiled: September 30, 1994Date of Patent: April 16, 1996Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Masaaki Toda, Tsumoru Miyamoto
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Patent number: 5495022Abstract: Piperidine and piperazine derivatives of formula I ##STR1## wherein R.sup.1 and R.sup.2 are H or A,R.sup.3, R.sup.4 and R.sup.5 are each independently H, Hal, OH, OA, OAc, NO.sub.2, NH.sub.2, NHAc, NHSO.sub.2 A or CN, orR.sup.3 and R.sup.4 together are --O--(CH.sub.2).sub.m --O--,n is 0, 1 or 2X is O or CH.sub.2, if n=0 or 2, or CH.sub.2, NH, NA or NAc, if n=1,Y is CH or N,m is 1 or 2,Hal is F, Cl, Br or I,A is C.sub.1-6 -alkyl,Ac is C.sub.1-8 -alkanoyl C.sub.1-10 -aralkanoyl or C.sub.7-11 -aroyl,and their physiologically acceptable salts show antiarrhythmic effects.Type: GrantFiled: June 24, 1994Date of Patent: February 27, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Manfred Baumgarth, Inge Lues, Klaus-Otto Minck, Norbert Beier
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Patent number: 5489589Abstract: The present invention concerns water-soluble amino acid derivatives of paclitaxel, their use as antitumor agents, and pharmaceutical compositions containg the compounds.Type: GrantFiled: December 7, 1994Date of Patent: February 6, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Mark D. Wittman, John F. Kadow
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Patent number: 5484954Abstract: This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.Type: GrantFiled: January 19, 1994Date of Patent: January 16, 1996Assignee: Nippon Kayaku Kabushiki KaishaInventors: Tochiro Tatee, Akira Shiozawa, Hirotaka Yamamoto, Yuh-ichiro Ichikawa, Aya Narita
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Patent number: 5466398Abstract: Described are novel reversible photochromic 3H-naphtho[2,1-b]pyran compounds, of the following graphic formula: ##STR1## wherein R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen or preferably a carboalkoxy group and R.sub.3 is hydrogen or preferably an alkyl group, provided that either R.sub.1 or R.sub.2 is hydrogen, and B and B' are the aryl groups phenyl or naphthyl, a heterocyclic aromatic group or together form a spiro adamantylene group. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(oxazine) type compounds, are also described.Type: GrantFiled: June 21, 1993Date of Patent: November 14, 1995Assignee: Transitions Optical, Inc.Inventors: Barry Van Gemert, Anil Kumar
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Patent number: 5458814Abstract: Described are novel reversible photochromic naphthopyran compounds, examples of which are compounds having certain substituents at the number 5 and 6 carbon atoms of the naphtho portion of the naphthopyran and at the 2-position of the pyran ring. Certain substituents may also be present at the number 7, 8, 9 or 10 carbon atoms of the naphtho portion of the naphthopyran. Also described are organic host materials that contain or that are coated with such compounds. Articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., spiro(indoline) type compounds, are also described.Type: GrantFiled: December 9, 1993Date of Patent: October 17, 1995Assignee: Transitions Optical, Inc.Inventors: Anil Kumar, Barry Van Gemert, David B. Knowles
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Patent number: 5428043Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.Type: GrantFiled: October 29, 1992Date of Patent: June 27, 1995Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 5369103Type: GrantFiled: June 19, 1992Date of Patent: November 29, 1994Assignee: John Wyeth & Brother, LimitedInventors: Ian A. Cliffe, Alan C. White, Anderson D. Ifill
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Patent number: 5314889Abstract: A 2-Acylaminothiazole of formula: ##STR1## in which R.sub.1 is H, an alkyl or a substituted alkyl; R.sub.IV is a cycloalkyl, an aromatic group such as phenyl or a heterocyclic group which are unsubstituted or substituted; R.sub.V is a substituted alkyl, a substituted carboxy such as an ester or an amide; or R.sub.IV and R.sub.V together represent a phenoxyalkylene group which may be substituted on the phenyl; and Z is a heterocyclic e.g. indolyl group; or a salt of compound (I).Type: GrantFiled: May 29, 1992Date of Patent: May 24, 1994Assignee: Elf SanofiInventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
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Patent number: 5286881Abstract: A benzodifuranone compounds of the formula, ##STR1## wherein R.sup.1 and R.sup.2 are each independently a naphthyl group or an unsubstituted or substituted phenyl group, which is useful for dyeing or printing hydrophobic fiber materials, is prepared in high purity and high yield by allowing benzofuran compounds of the formula, ##STR2## wherein R.sup.1 is as defined above, to react with acetonitrile compounds of the formula, ##STR3## wherein R.sup.2 is as defined above, and then carrying out an oxidation reaction to give the benzodifuranone compound.Type: GrantFiled: September 30, 1992Date of Patent: February 15, 1994Assignee: Sumitomo Chemical Company LimitedInventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
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Patent number: 5284864Abstract: Taxane derivatives of the formula ##STR1## wherein R.sub.1 is butenyl,R.sub.3 is phenyl,T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or monocylic aryl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: November 13, 1992Date of Patent: February 8, 1994Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh
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Patent number: 5284865Abstract: Taxane derivatives of the formula ##STR1## wherein R.sub.1 is cyclohexyl,R.sub.3 is phenyl,T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or monocylic aryl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: November 13, 1992Date of Patent: February 8, 1994Inventors: Robert A. Holton, Hossain Nadizadeh
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Patent number: 5283253Abstract: Taxane derivatives of the formula ##STR1## wherein R.sub.1 is phenyl or p-nitrophenyl,R.sub.3 is furyl or thienyl,T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl or monocylic aryl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: November 13, 1992Date of Patent: February 1, 1994Assignee: Florida State UniversityInventors: Robert A. Holton, Kasthuri Rengan, Hossain Nadizadeh
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Patent number: 5268471Abstract: Process for the preparation of 6-acyl-, 7-acyl- or 6,7-diacyl analogues of forskolin of the general formula ##STR1##Type: GrantFiled: January 15, 1993Date of Patent: December 7, 1993Assignee: Hoechst AktiengesellschaftInventors: Noel J. de Souza, Premanand D. Desai, Shrikant V. Savanur, Jurgen Blumbach
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Patent number: 5252598Abstract: The present invention relates to labdane-derivatives of the formula ##STR1## a process for their preparation and the use of these substances as medicaments, preferably as medicaments having a positive ionotropic effect, an effect of lowering intraocular pressure and lowing blood pressure.Type: GrantFiled: May 4, 1992Date of Patent: October 12, 1993Assignee: Hoechst AktiengesellschaftInventors: Yatendra Khandelwal, Greta Moraes, Bansi Lal, Vijay A. Aroskar, Alihussein N. Dohadwalla, Richard H. Rupp
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Patent number: 5250682Abstract: Process for the manufacture of 6.beta.Type: GrantFiled: July 22, 1991Date of Patent: October 5, 1993Assignee: Hoechst AktiengesellschaftInventors: Yatendra Khandelwal, Bansi Lal, Jurgen Blumbach
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Patent number: 5216178Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.Type: GrantFiled: August 15, 1991Date of Patent: June 1, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 5206241Abstract: Labdanes of the formula ##STR1## a process for their manufacture, pharmaceutical preparations containing an effective amount of these compounds and their use for the manufacture of a pharmaceutical preparation for treatment of cardiovascular diseases and high intraocular pressure.Type: GrantFiled: March 14, 1991Date of Patent: April 27, 1993Assignee: Hoechst AktiengesellschaftInventors: Yatendra Khandelwal, Rajeshwari Kannan, Bansi Lal, Ramanujam Rajagopalan, Vijay A. Aroskar, deceased AliHussein N. Dohadwalla, Rashida A. Dohadwalla, Anis S. Dohadwalla, Samina A. Dohadwalla, Richard H. Rupp
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Patent number: 5192766Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 is each --R.sup.5, --CH.dbd.CH--R.sup.5 or --C.tbd.C--R.sup.5, wherein R.sup.5 is optionally substituted aryl or aromatic heterocyclic; R.sup.3 is hydrogen, alkyl, cyano or --R.sup.5 ; X is oxygen or sulfur; A is 1,4-piperazin-1,4-diyl or a 1,4-homopiperazin-1,4-diyl; B' is alkylene, carbonyl, thiocarbonyl, sulfinyl or sulfonyl; and R.sup.4 is optionally substituted phenyl and pharmaceutically acceptable salts thereof have valuable PAF antagonist activity, and may be prepared by reacting a compound containing the piperazine or homopiperazine part of the molecular with a compound containing the other part of the molecule.Type: GrantFiled: August 28, 1991Date of Patent: March 9, 1993Assignee: Sankyo Company, LimitedInventors: Norio Nakamura, Nobuyuki Ohkawa, Takeshi Oshima, Masaaki Miyamoto, Yasuteru Iijima
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Patent number: 5180717Abstract: Bivalent ligand compounds synthesized from a tether composition joining two heterocyclic groups comprising furochromones, furobenzoxazinones, and benzobisdifurans. These compounds show pharmacological activity in blocking ACAT enzymes which are major regulators of cholesterol metabolism. The compounds also show activity in lowering plasma triglycerides and elevating HDL cholesterol. They are useful in the prevention or treatment of the constriction or obstruction of arterial vessels, atherosclerosis, hyperlipidemia, hypertriglyceridemia, chylomicronemia, and pancreatitis.Type: GrantFiled: May 7, 1991Date of Patent: January 19, 1993Assignee: The Upjohn CompanyInventors: Ronald B. Gammill, Frank P. Bell
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Patent number: 5175286Abstract: A dibenz[b,e]oxepin derivative represented by the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, halogen, lower alkyl or alkoxy; one of R.sup.3 and R.sup.4 is lower alkoxy, and other is a group represented by the formula (II) ##STR2## wherein R.sup.5 is hydrogen or lower alkyl, A is hydroxyl, --O(CH.sub.2).sub.m --R.sup.6 (wherein m is an integer of 1-6, R.sup.6 is hydrogen, lower alkyl or alkoxy, cycloamino, or lower alkoxycarbonyl), cycloamino, di-lower alkylamino or --NH(CH.sub.2).sub.n --R.sup.7 (wherein n is an integer of 0-3, R.sup.7 is hydrogen, hydroxyl, phenyl, thiazole or cycloamino).Type: GrantFiled: March 8, 1991Date of Patent: December 29, 1992Assignee: Hisamitsu Pharmaceutical Co., Inc.Inventors: Masaru Saita, Hisataka Inoue, Terumi Hachiya, Mikio Nakashima, Shigenori Yahiro, Yasuaki Taniguchi, Yoshiki Deguchi, Shoji Hamanaka, Masayoshi Tsuji, Kanji Noda
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Patent number: 5164388Abstract: A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: April 18, 1991Date of Patent: November 17, 1992Assignee: Abbott LaboratoriesInventors: Biswanath De, Thomas N. Zydowsky, William R. Baker, Joseph F. Dellaria, Saul H. Rosenberg, Hwan S. Jae
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Patent number: 5143922Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic acitvity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: November 20, 1990Date of Patent: September 1, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 5140027Abstract: Novel aminoalkylthiodibenzoxepins, physiologically tolerable acid addition salts thereof, a method of preparing same, pharmaceutical and veterinary preparations including same and methods of treating by administering same are disclosed. These compounds are useful as analgesic, antidepressant and anticonvulsant agents. A process for selectively reducing olefins by alkaline earth metals in loweralkanols is also disclosed.Type: GrantFiled: May 14, 1990Date of Patent: August 18, 1992Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Helen H. Ong, Vernon B. Anderson, James A. Profitt
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Patent number: 5124457Abstract: The present invention is directed to a fluorescence polarization assay for phencyclidine and phencyclidine derivatives, to the various components needed for preparing and carrying out such an assay, and to methods of making these components. Specifically, tracers, immunogens and antibodies are disclosed, as well as methods for making them. The tracers and the immunogens are made from substituted phencyclidine compounds. A fluorescein moiety is included in the tracer, while a poly(amino acid) forms a part of the immunogen. The assay is conducted by measuring the degree of polarization retention of plane polarized light that has been passed through a sample containing antiserum and tracer.Type: GrantFiled: August 6, 1990Date of Patent: June 23, 1992Assignee: Abbott LaboratoriesInventors: Frank S. Ungemach, Daniel S. Nam
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Patent number: 5116863Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma and also employed in the treatment of inflammation.Type: GrantFiled: March 2, 1987Date of Patent: May 26, 1992Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Toshiaki Kumazawa, Shizuo Otaki, Hiroyuki Obase, Kenji Ohmori, Hidee Ishii, Haruhiko Manabe, Tadafumi Tamura, Katsuichi Shuto
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Patent number: H1487Abstract: This invention relates to a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, in which R.sup.2 is a radical of the formula ##STR2## in which R.sup.a and R.sup.b are independently hydrogen or C.sub.1-6 alkyl, said C.sub.1-6 alkyl being optionally substituted with hydroxy, phosphono, phosphonooxy, carboxy or di(C.sub.1-6 alkyl) amino; or NR.sup.a R.sup.b together represents a radical of the formula ##STR3## in which y is one to three, and R.sup.a is as defined above; R.sup.p and R.sup.r are independently same or different C.sub.1-6 alkyl;R.sup.1 is hydrogen or a radical Z of the formula ##STR4## in which Q is --(CH.sub.2).sub.f --, optionally substituted with one to six same or different C.sub.1-6 alkyl or C.sub.3-6 cycloalkyl, or a carbon atom of said --(CH.sub.2).sub.f -- radical may also be a part of C.sub.3-6 cycloalkylidene;R.sup.3 and R.sup.4 are independently hydrogen or C.sub.1-6 alkyl, or R.sup.3 and R.sup.Type: GrantFiled: September 29, 1993Date of Patent: September 5, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Henry Wong, Terrence Doyle