The Five-membered Hetero Ring Is One Of The Cyclos In A Polycyclo Ring System Patents (Class 544/153)
  • Patent number: 5637583
    Abstract: Aminocyclohexylester compounds, including thioesters, are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the blockade of ion channels and the treatment of arrhythmias.
    Type: Grant
    Filed: September 27, 1994
    Date of Patent: June 10, 1997
    Assignee: University of British Columbia
    Inventors: Bernard A. MacLeod, Michael J. A. Walker, Richard A. Wall
  • Patent number: 5633279
    Abstract: The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: May 27, 1997
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Morgans, Jr., David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, John C. Rohloff, Eric B. Sjogren, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Patent number: 5622974
    Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzofurans which are .alpha.-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: April 22, 1997
    Assignee: Eli Lilly and Company
    Inventor: Brian S. Muehl
  • 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: 5574039
    Abstract: The invention relates to TS-inhibiting compounds of the formula ##STR1## where W is an alkylene group; D is a structure having two rings that are unsubstituted or substituted, where (i) one ring is a phenyl ring and (ii) the other ring is a phenyl ring or a 6-membered heterocyclic ring; R is a hydrogen atom or an alkyl group; and X and Y together form ##STR2## and to salts of these compounds. The moiety W can be CH.sub.2, and D can be a phenyl ring bridged through a sulfonyl group to another ring.
    Type: Grant
    Filed: September 22, 1994
    Date of Patent: November 12, 1996
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Michael D. Varney, Gifford P. Marzoni, Cynthia L. Palmer, Judith P. Deal, Terence R. Jones
  • Patent number: 5554612
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: September 10, 1996
    Inventors: John W. Patterson, David Morgans, Jr., Eric B. Sjogren, David B Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Patent number: 5547478
    Abstract: The invention is to provide a composition made by blending a benzodifuranone compound of the formula (I): ##STR1## wherein R.sub.1 represents a methylene or straight or branched C.sub.2 -C.sub.6 alkylene group optionally substituted with a hydroxy, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylcarbonyloxy group; and Q represents 5- or 6-membered saturated or unsaturated heterocyclic ring residue, with an anthraquinone compound of the formula (II): ##STR2## wherein R.sub.2 represents an optionally substituted C.sub.1 -C.sub.6 alkyl, optionally substituted phenyl or C.sub.1 -C.sub.4 alkoxyphenylsulfonyl group, and a method for dyeing hydrophobic materials using the composition to obtain red dyed products with excellent pH dependency and fastnesses to light and washing.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: August 20, 1996
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Toshinori Fukui, Nobuyuki Katsuda, Shinichi Yabushita, Shuhei Hashizume
  • Patent number: 5543408
    Abstract: The crystalline anhydrous salt formed by complexing mycophenolate mofetil with an anion selected from the group chloride, sulfate, phosphate and acetate (in particular the hydrochloride salt), and pharmaceutical compositions, intravenous formulations and a kit thereof, and associated methods of treatment.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: August 6, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Roger C. Fu, De-Mei Leung, Jeffrey S. Fleitman, Michele C. Rizzolio, Andrew R. Miksztal
  • Patent number: 5541183
    Abstract: The present invention is directed to new ginkgolide derivatives, which may be used for the prevention or treatment of various PAF-induced diseases, and the pharmaceutical uses of these derivatives. The present invention is also directed to a process for preparing these ginkgolide derivatives.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: July 30, 1996
    Assignee: Sunkyong Industries Co., Ltd.
    Inventors: Pyeong-Uk Park, Sungsoo Pyo, Suk-Kwan Lee, Jin H. Sung, Wie J. Kwak, Hwa-Kun Park, Yong-Baik Cho, Geun Ho Ryu, Taek S. Kim
  • Patent number: 5538969
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: July 23, 1996
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: David Morgans, Jr., Eric B. Sjogren, David B. Smith, Francisco X. Talam as, Dean R. Artis, Alicia Cervantes, Todd R. Elworthy, Mario Fern andez, Fidencio Franco, Ronald C. Hawley, Teresa Lara, David G. Loughhead, Peter H. Nelson, John W. Patterson, Alejandra Trejo, Ann M. Waltos, Robert J. Weikert
  • Patent number: 5527922
    Abstract: The invention relates to pyrrolo[3,4-c]pyrroles of formula ##STR1## wherein D and E are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.7 -C.sub.10 aralkyl, unsubstituted phenyl or phenyl which is substituted by chloro, bromo, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl or nitro, or --COO--C.sub.1 -C.sub.5 alkyl or a group --COOR.sub.8,wherein R.sub.8 is benzyl, piperidyl or a group ##STR2## and X and Y are N--CN or O, with the proviso that at least one of X or Y N--CN must be N--CN.These pyrrolo[3,4-c]pyrroles are preeminently suitable for use as colorants, i.e. as pigments or as polymer-soluble dyes, for colouring high molecular weight organic material. They are distinguished by unexpectedly high solid-state fluorescence.The substituents A and B are as defined in claim 1.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: June 18, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: John S. Zambounis, Zhimin Hao, Abul Iqbal
  • Patent number: 5523309
    Abstract: The present invention provides a compound of formula I ##STR1## wherein R.sub.1 is H, OH, halo, OCO(C.sub.1 -C.sub.6 alkyl), OCO(aryl), OSO.sub.2 (C.sub.4 -C.sub.6 alkyl), OCOO(C.sub.1 -C.sub.6 alkyl), OCOO(aryl), OCONH(C.sub.1 -C.sub.6 alkyl), or OCON(C.sub.1 -C.sub.6 alkyl).sub.2 ;R.sub.2 is aryl, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, or 4-cyclohexanol;R.sub.3 is O(CH.sub.2).sub.2 or O(CH.sub.2).sub.3 ;R.sub.4 and R.sub.5 are optionally CO(CH.sub.2).sub.2 CH.sub.3, CO(CH.sub.2).sub.3 CH.sub.3 C.sub.1 -C.sub.6 alkyl, or R.sub.4 and R.sub.5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline;R.sub.6 is >CH(C.sub.1 -C.sub.5 alkyl), >CH(C.sub.2 -C.sub.5 alkenyl), >C.dbd.CH(C.sub.1 -C.sub.5 alkyl) >CH(aryl), >C(OH)(C.sub.1 -C.sub.5 alkyl), >C(OH)(C.sub.2 -C.sub.5 alkenyl), >C(OH)aryl;and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: June 4, 1996
    Assignee: Eli Lilly and Company
    Inventors: Henry U. Bryant, Jeffrey A. Dodge
  • Patent number: 5510358
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for treating endometriosis.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 23, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5510357
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO (C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof for, inter alia, alleviating the symptoms of post menopausal syndrome and hormonally-dependent cancer, particularly breast cancer.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: April 23, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5492922
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for inhibiting aortal smooth muscle proliferation.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 20, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5488058
    Abstract: The present invention provides pharmaceutically active compounds of formula I ##STR1## wherein R.sup.1 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), or --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl);R.sup.2 is --H, --OH, --O(C.sub.1 -C.sub.4 alkyl), --OCOC.sub.6 H.sub.5, --OCO(C.sub.1 -C.sub.6 alkyl), --OSO.sub.2 (C.sub.2 -C.sub.6 alkyl), or halo, providing when Z is --S--, R.sup.2 is not halo;R.sup.3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino;n is 2 or 3; andz is --O-- or --S--;or a pharmaceutically acceptable salt thereof, for inhibiting restenosis.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 30, 1996
    Assignee: Eli Lilly and Company
    Inventor: Alan D. Palkowitz
  • Patent number: 5472707
    Abstract: Mycophenolate mofetil, mycophenolic acid, and ranolazine can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil, mycophenolic acid, or ranolazine liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.
    Type: Grant
    Filed: May 9, 1994
    Date of Patent: December 5, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Glenn J. Samuels, Jung-Chung Lee, Charles Lee, Stephen Berry, Paul J. Jarosz
  • Patent number: 5441953
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: August 15, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Eric B. Sjogren
  • Patent number: 5380879
    Abstract: The disclosed derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil and other immunosuppressant agents.
    Type: Grant
    Filed: February 18, 1994
    Date of Patent: January 10, 1995
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Eric B. Sjogren
  • Patent number: 5354861
    Abstract: The synthesis and the biological evaluation of a series of basic ethers of 2-benzyl-3-arylbenzofurans as antitumor agents is described. These compounds bind significantly to the antiestrogen-binding sites but only poorly to the estrogen receptor sites and are cytotoxic to tumor cells. Some of these compounds also significantly inhibited de novo cholesterol biosynthesis in an estrogen receptor negative lymphoma cell line rich in antiestrogen-binding sites.
    Type: Grant
    Filed: November 4, 1992
    Date of Patent: October 11, 1994
    Assignee: National University of Singapore
    Inventors: Keng-Yeow Sim, Oi-Lian Kon, Chin-Chin Teo, Siu-Choon Ng, Srikanth Natarajan
  • Patent number: 5326759
    Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.
    Type: Grant
    Filed: November 1, 1993
    Date of Patent: July 5, 1994
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee
  • Patent number: 5314889
    Abstract: 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: Grant
    Filed: May 29, 1992
    Date of Patent: May 24, 1994
    Assignee: Elf Sanofi
    Inventors: Robert Boigegrain, Roger Brodin, Danielle Gully, Jean-Charles Molimard, Dominique Olliero
  • Patent number: 5300522
    Abstract: 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: Grant
    Filed: August 18, 1992
    Date of Patent: April 5, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr, Ekkehard Weiss
  • Patent number: 5266707
    Abstract: 4-hydroxytetrahydropyran-2-one and 3,5-Dihydroxyheptanoic acid derivatives of formula (I) and formula (II) have an inhibition effect on HMG-CoA reductase, a cholesterol value reduction effect, and an antioxidation function, thus serving as cholesterol reducing agent or lipid reducing agents: ##STR1## wherein R.sup.1 represents hydrogen, a nitro group, or -N(R.sup.4)R.sup.5 in which R.sup.4 and R.sup.5 each represent an alkyl group, an alkenyl group, an aryl group, an aralkyl group; an acyl group, an aroyl group, a carbamoyl group, or a thiocarbamoyl group, and R.sup.4 and R.sup.5 may be combined to form a cyclic amino group; and R.sup.2 and R.sup.3 each represent hydrogen or an alkyl group; and R.sup.6 represents hydrogen, an alkyl group, an alkali metal, or an alkaline earth metal.
    Type: Grant
    Filed: September 17, 1992
    Date of Patent: November 30, 1993
    Assignee: Fujirebio Inc.
    Inventors: Masakatsu Matsumoto, Nobuko Watanabe, Eiko Mori, Tetsuaki Yamaura, Misao Aoyama
  • Patent number: 5247083
    Abstract: Mycophenolate mofetil is made non-catalytically by refluxing mycophenolic acid with 2-morpholinoethanol in an inert organic solvent capable of azeotropic removal of water.
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: September 21, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Martin Knox, Gregory Donegan, Dennis A. Smith
  • Patent number: 5223616
    Abstract: A heterocyclic compound which is useful for dyeing or printing hydrophobic fiber materials and which has the following formula (I), ##STR1##wherein A.sub.1, A.sub.2, A.sub.3 and A.sub.4 are each hydrogen, halogen, alkyl, alkoxy or alkenyl, X.sub.1 is --O-- or the like, R.sub.1 is a methylene or the like, X.sub.2 is a direct linkage or a divalent group of --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## in which R.sub.3 is a hydrogen atom or a C.sub.1-4 alkyl group, ##STR3## in which R.sub.3 is as defined above, T and u are each independently hydrogen or a C.sub.1-4 alkyl, l is O or an integer of 1 to 3, Q is an unsubstituted or substituted 5-, 6- or 7-membered saturated or unsaturated heterocyclic residue, Y is hydrogen, C.sub.1-4 alkyl, a C.sub.1-4 alkoxy group or the like.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Sumitomo Chemical Company, Ltd.
    Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
  • Patent number: 5192799
    Abstract: Amine represented by the following formula (1), or their acid addition salts or their quaternary ammonium salts. ##STR1## The amines of formula (1) or their pharmaceutically acceptable acid addition salts or quaternary ammonium salts are useful for the treatment and prevention of heart diseases of animals, particularly arrhythima, myocardial infarction, angina pectoris and heart failure and psychoneurological diseases.
    Type: Grant
    Filed: June 5, 1992
    Date of Patent: March 9, 1993
    Assignee: Mitsui Petrochemical Industries, Ltd.
    Inventors: Ikuo Tomino, Masaharu Ishiguro, Takumi Kitahara, Keiichi Yokoyama, Noriaki Kihara, Joji Kamiya, Kanji Yoshihara, Masaaki Ishii, Akira Mizuchi, Kazutoshi Horikomi, Akira Awaya, Takuo Nakano
  • Patent number: 5183888
    Abstract: The present invention relates to a process for the preparation of certain polycyclic dyes and in particularly the preparation of a polycyclic dye of Formula I: ##STR1## By reacting a phenyltartronic acid of Formula II: ##STR2## With either a compound of Formula III: ##STR3## or a compound of Formula IV: ##STR4##
    Type: Grant
    Filed: November 9, 1990
    Date of Patent: February 2, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Ronald W. Kenyon, David F. Newton, Derek Thorp
  • Patent number: 5128348
    Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: July 7, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Gregory S. Basarab
  • Patent number: 5104869
    Abstract: Renin inhibiting compounds containing a single .alpha.-amino acid of the formula: ##STR1## and analogs thereof which inhibit the substrate-cleaving acting or renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.
    Type: Grant
    Filed: October 25, 1990
    Date of Patent: April 14, 1992
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Charles Frederick, Jeremy I. Levin, Fuk-Wah Sum, Marvin F. Reich
  • Patent number: 5091526
    Abstract: Biologically active, enantiomerically substantially pure intermediates of trans-hexahydro-benzo[d]naphtho[2,1-b]azepines are prepared.The present invention involves a process for preparing compounds of the general formula 3: ##STR1## wherein: R* is ##STR2## Each R.sup.1 is independently H or alkyl; Q is methylene, --O-- or --S--;m and n are independently variable and may each have a value of 0, 1 or 2, with the provisos that the sum of m and n is not greater than 3, that m may not equal zero when Q is --O-- or --S--, and that when Q is --CH.sub.2 --, m and n cannot both be zero;X is hydrogen, halo, alkyl, alkylthio, alkylsulfinyl, alkylsufonyl, hydroxy, alkoxy or trifluoromethyl;Y is hydrogen, hydroxy, alkoxy, --OC(O)NR.sup.2 R.sup.3, --OC(O)--R.sup.9, --N(R.sup.1).sub.2, --NHC(O)R.sup.1 or --OP(O)(OH)OR.sup.1,R.sup.2 and R.sup.3 are the same or different and each is hydrogen (provided that both are not hydrogen), alkyl, aralkyl, cycloalkyl, aryl, hydroxyalkyl, or alkoxyalkyl;in addition, when one of R.sup.
    Type: Grant
    Filed: January 8, 1991
    Date of Patent: February 25, 1992
    Assignee: Schering Corporation
    Inventors: Joel G. Berger, John W. Clader
  • Patent number: 5082840
    Abstract: A method for increasing the weight gain and/or improving the feed utilization efficiency and/or increasing the lean body mass and/or decreasing birth mortality rate and increasing post-natal survival rate of livestock comprises the administration to livestock of an effective, non-toxic amount of a compound of formula (I), or a veterinarily acceptable acid addition salt thereof: ##STR1## wherein R.sup.1 is phenyl (C.sub.1-6) alkyl or optionally substituted C.sub.1-6 alkyl, andW is optionally substituted phenyl, a heterocyclyl group, or phenoxymethyl optionally substituted on the phenyl group. Certain compounds of formula (I) are novel.
    Type: Grant
    Filed: August 29, 1989
    Date of Patent: January 21, 1992
    Assignee: Beecham Group p.l.c.
    Inventors: Jonathan R. Arch, Norman H. Rogers
  • Patent number: 5019573
    Abstract: Novel substituted dibenzofuran compounds are disclosed. The compounds exhibit activity in antagonizing the effects of leukotriene B.sub.4 (LTB.sub.4). Pharmaceutical compositions containing the novel compounds and methods of treatment employing the same are also described.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: May 28, 1991
    Assignee: Euroceltique, S.A.
    Inventors: T. Scott Shoupe, David C. Baker, Stephen M. Coutts, Elli S. Hand
  • Patent number: 5004813
    Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: April 2, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Rox Phaff, Davor Bedekovic
  • Patent number: 4999350
    Abstract: The present invention relates to (RS)-2-(2,3-dihydro-5-hydroxy-4,6,7-trimethylbenzofuranyl) acetic acids and 2-(2,3-dihydro-5-acyloxy-4,6,7-trimethylbenzofuranyl) acetic acids and esters thereof, the process for producing them and their relevant therapeutical use as mucoregulators and antiischemic agents.
    Type: Grant
    Filed: April 13, 1989
    Date of Patent: March 12, 1991
    Assignee: Biomedica Foscama Industria Chimico-Farmaceutica S.p.A.
    Inventors: Mario Brufani, Stefano Ceccarelli, Patrizia Giannetti, Agnese Paesano, Romolo Scuri, Sergio Zanarella
  • Patent number: 4988727
    Abstract: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.
    Type: Grant
    Filed: September 19, 1989
    Date of Patent: January 29, 1991
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Michel Fortin
  • Patent number: 4978761
    Abstract: The present invention relates to a compound of the formula: ##STR1## wherein R.sup.1 is hydrogen or a lower alkyl; R.sup.2 is methyl which is substituted by a carboxy, alkoxycarbonyl, cyano, halogen, aryl or heterocyclic group of C.sub.2-15 chain hydrocarbon residue having no lower alkyl at the .alpha.-position which may be substituted by a carboxy, alkoxycarbonyl, cyano, halogen, aryl or heterocyclic group; R.sup.3 is a lower alkyl; R.sup.4 is hydrogen or acyl; and R.sup.5 and R.sup.6 each is a lower alkyl or lower alkoxy, or R.sup.5 and R.sup.6 combinedly are butadienylene or a salt thereof.The compound (I) of the present invention has a strong 5- and 12-lipoxygenase inhibiting action, is of high safety and is useful as, among others, an agent for ameliorating dysfunction circulatory system, an anti-allergic agent and a pharmaceutical agent for central nervous system.
    Type: Grant
    Filed: June 9, 1989
    Date of Patent: December 18, 1990
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Shigenori Ohkawa, Naohisa Fukuda
  • Patent number: 4952571
    Abstract: The invention relates to pyridazinone compounds of the general formula I: ##STR1## wherein R.sup.1 represents one to four substituents, which may be the same or different and are selected from H, OH, halogen, NO.sub.2, unsubstituted or C1-C4 alkyl substituted amino, C1-C4 alkyl, C1-C4 halogen substituted alkyl, O--ALK--NR.sup.4 R.sup.5, C1-C4 alkoxy, whereby two substituents taken together may also represent a methylenedioxy group;R.sup.2 and R.sup.3 represent independently H or C1-C4 alkyl;R.sup.4 and R.sup.5 represent independently H or C1-C4 alkyl, or form together with the nitrogen a 5- or 6- membered ring;X represents S or O;the dotted line represents an optional bond;and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: July 11, 1989
    Date of Patent: August 28, 1990
    Assignee: Akzo, N.V.
    Inventors: James Redpath, Robert T. Logan, Robert G. Roy, George McGarry
  • Patent number: 4952579
    Abstract: The compounds and pharmaceutical compositions of Formula A, wherein Z is hydrogen or --C(O)R, where R is lower alkyl or aryl, and the pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
    Type: Grant
    Filed: November 14, 1988
    Date of Patent: August 28, 1990
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
  • Patent number: 4923641
    Abstract: Highly concentrated stable solutions of color-forming agents of the general formula ##STR1## wherein x denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused onto the rings A, B, C and D and the cyclic and acyclic radicals and the rings A, B, C and D can carry further non-ionic substituents which are customary in dyestuff chemistry, or mixtures thereof, in water-insoluble organic solvents from the group comprising optionally chlorinated hydrocarbons, vegetable oils and phthalic acid esters are used for the preparation of pressure-sensitive recording materials.
    Type: Grant
    Filed: September 20, 1988
    Date of Patent: May 8, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Udo Eckstein, Hubertus Psaar
  • Patent number: 4918206
    Abstract: Highly effective diuretic antihypertensives, i.e., sulfamoyl-2-benzofurancarboxylic acid derivatives which are classified as loop diuretics with less adverse side-effects and can be administered orally at a daily dosage of 0.5 mg to 200 mg or parenterally at 0.01 mg to 50 mg.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: April 17, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Hiroshi Harada, Yoshihiro Matsushita, Masuhisa Nakamura, Yukio Yonetani
  • Patent number: 4891373
    Abstract: Novel aminopropanol derivatives of 1,4:3,6-dianhydro-hexitol nitrates of the general formula I ##STR1## in which X has the meaning given in the specification, processes for their preparation and their use in preventing and treating angina pectoris, systemic hypertension and pulmonary hypertension in mammals.
    Type: Grant
    Filed: November 23, 1988
    Date of Patent: January 2, 1990
    Assignee: Pfizer Inc.
    Inventors: Peter Stoss, Matyas Leitold, Rodney Yeates
  • Patent number: 4886799
    Abstract: The invention relates to new acetamides derived from 2,3-dihydro-3-phenyl-2-benzofuranone, of general formula I ##STR1## in which: R.sub.1 denotes a hydrogen or halogen atom,R.sub.2 and R.sub.3, which may be identical or different, each denote a hydrogen atom or a linear or branched alkyl radical containing 1 to 4 carbon atoms, a benzyl radical optionally substituted with a halogen atom, with an alkoxy radical containing 1 to 4 carbon atoms or with an alkyl radical having 1 to 4 carbon atoms, or a 3,4-methylene-dioxybenzyl radical, or form, together with the nitrogen to which they are attached, a 4-morpholinyl radical or a 1-piperazinyl radical.
    Type: Grant
    Filed: September 14, 1988
    Date of Patent: December 12, 1989
    Assignee: Adir Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4885299
    Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: December 5, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4882340
    Abstract: A novel benzofuran derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, a lower alkoxy group or a halogen atom, one of R.sup.2 and R.sup.3 is a lower alkyl group and the other is a lower alkyl group or a phenyl-lower alkyl group, or R.sup.2 and R.sup.3 combine together with adjacent nitrogen atom to form a heteromonocyclic group, Ring A is a substituted or unsubstituted phenyl group, Y is oxygen atom or sulfur atom and n is an integer of 2 or 3, or a pharmaceutically acceptable salt thereof is disclosed.The compound (I) or a pharmaceutically acceptable salt thereof has a potent inhibitory activity against reflective contractions of urinary bladder.
    Type: Grant
    Filed: September 2, 1988
    Date of Patent: November 21, 1989
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Ikuo Iijima, Masakatsu Ozeki, Yutaka Saiga, Tohru Ishizuka, Kunio Nosaka
  • Patent number: 4876357
    Abstract: Chromogenic phthalides and azaphthalides of the formula ##STR1## in which V.sub.1 and V.sub.2 are each, independently of the other, hydrogen, halogen, lower alkyl, lower alkoxy, (lower alkoxy)carbonyl or --NR.sub.1 R.sub.2, at least one of the radicals V.sub.1 and V.sub.2 being lower alkoxy or --NR.sub.1 R.sub.2, A is an unsubstituted or halogen-, cyano-, nitro-, (lower alkyl)-, (lower alkoxy)-, (lower alkyl)thio-, (lower alkyl)amino- or di(lower alkyl)amino-substituted benzene, naphthalene, pyridine, quinoline, pyrazine or quinoxaline ring, B is a substituted phenyl radical of the formula ##STR2## or a 3-indolyl of the formula ##STR3## Q is ##STR4## --S-- or --O--, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, unsubstituted or halogen-, hydroxy-, cyano- or (lower alkoxy)-substituted alkyl, cycloalkyl or unsubstituted or ringsubstituted phenalkyl or phenyl, or the substituent pairs (R.sub.1 and R.sub.2) and (R.sub.3 and R.sub.
    Type: Grant
    Filed: October 26, 1987
    Date of Patent: October 24, 1989
    Assignee: Ciba-Geigy Corporation
    Inventors: Rox Phaff, Davor Bedekovic
  • Patent number: 4861776
    Abstract: Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
    Type: Grant
    Filed: February 25, 1988
    Date of Patent: August 29, 1989
    Assignee: Syntex (U.S.A) Inc.
    Inventors: Peter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
  • Patent number: 4859700
    Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.
    Type: Grant
    Filed: February 12, 1988
    Date of Patent: August 22, 1989
    Assignee: ADIR Et Cie
    Inventors: Gilbert Lavielle, Jean Lepagnol
  • Patent number: 4851554
    Abstract: The disclosure relates to compounds of the formula ##STR1## and pharmaceutically acceptable addition salts thereof wherein X represents a single, direct bond or a substituted or unsubstituted alkylene chain containing 1 to 4 carbon atoms, wherein R.sub.5 is a lower alkyl group, wherein R.sub.6 is either hydrogen or methyl, wherein Am is selected from the class consisting of amino, lower mono and dialkylamino, piperidino, piperazino, N-lower alkyl piperazino, pyrrolidino, and morpholino groups, wherein Y.sub.1 and Y.sub.2 are identical and are hydrogen, a halogen, methyl or ethyl048505325 and n is an integer in the range of 1-5.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: July 25, 1989
    Assignee: University of Tennessee Research Corporation
    Inventors: Thomas P. Kennedy, George W. Kabalka
  • Patent number: 4845096
    Abstract: Benzofuran derivatives of the general formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen, alkyl or phenylalkyl, where alkyl in each case is of 1 to 4 carbon atoms, R.sup.3 and R.sup.4 are identical or different and are each hydrogen or C.sub.1 -C.sub.4 -alkyl or together form a 3-membered to 5-membered chain which may be interrupted by an oxygen atom or an NR.sup.1 group, X is --CO--CH.dbd.CH--, --CO--CH.sub.2 --CH.sub.2 --or --CHOH--CH.sub.2 --CH.sub.2 --, n is 2 or 3 and Het is an aromatic 5-membered or 6-membered ring which contains a hetero atom from the group consisting of N, O and S and may additionally contain a (further) N atom, in which the ring may be substituted by C.sub.1 -C.sub.4 -alkyl, fluorine, chlorine, bromine, NH.sub.2 or NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 have the abovementioned meanings, the use of these benzofuran derivatives for the preparation of pharmaceutical, in particular antiulcerogenic, agents, and these agents themselves are described.
    Type: Grant
    Filed: March 18, 1988
    Date of Patent: July 4, 1989
    Assignee: BASF Aktiengsellschaft
    Inventors: Rainer Schlecker, Klaus Ruebsamen