Plural Ring Chalcogens In The Polycyclo Ring System Or The Piperazine Ring Bonded Directly To The Polycyclo Ring System Patents (Class 544/378)
  • Patent number: 5798350
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or 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., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: May 3, 1996
    Date of Patent: August 25, 1998
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5759450
    Abstract: A naphthopyran compound represented by the formula: ##STR1## wherein R.sub.5, R.sub.6, R.sub.8, R.sub.9, and R.sub.10 are each selected from hydrogen, a first stable organic radical, an organic heterocyclic group, halogen, a first nitrogen-substituted group, and a first nitrogen-substituted ring compound; A and B are each selected from hydrogen, substituted phenyl, and substituted naphthyl, provided that at least one of A or B is substituted phenyl or substituted naphthyl; and any substituent of any substituted phenyl or substituted naphthyl at A or B is selected from hydrogen, a second stable organic radical, an organic heterocyclic group, halogen, a second nitrogen-substituted group, and a second nitrogen-substituted ring compound, provided that at least one substituent of any substituted phenyl or substituted naphthyl at either A or B is phenyl, naphthyl, or furyl.
    Type: Grant
    Filed: July 31, 1996
    Date of Patent: June 2, 1998
    Assignee: Vision-Ease Lens, Inc.
    Inventors: Frank J. Hughes, Edward A. Travnicek
  • Patent number: 5702645
    Abstract: Described herein are photochromic compounds or a structural isomer of the photochromic compound, the photochromic compounds represented by the formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.4, R.sub.5, R.sub.6, R.sub.8, A, B, C, and D are each selected from the group consisting essentially of hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted radical, and a nitrogen-substituted ring radical.
    Type: Grant
    Filed: October 30, 1995
    Date of Patent: December 30, 1997
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 5646175
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5543427
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: August 24, 1994
    Date of Patent: August 6, 1996
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • 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: 5538965
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or 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., C(O)--, O--, and S--;R.sub.1 represents C.sub.1-4 alkyl;Y is selected from CH and N;n is 0, 1 or 2;q is 1 or 2;R.sub.2 is C.sub.1-6 alkyl optionally incorporating a heteroatom selected from N, O and S;D is cyclohexane or benzene; andE is a saturated or unsaturated 5- or 6-membered heterocycle incorporating 1, 2 or 3 heteroatoms selected from O, N, and S, wherein E is optionally substituted with 1 or 2 substituents selected from halogen, C.sub.1-4 alkyl and halogen-substituted C.sub.1-4 alkyl;and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: July 23, 1996
    Assignee: Allelix Biopharmaceuticals Inc.
    Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5428043
    Abstract: 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: Grant
    Filed: October 29, 1992
    Date of Patent: June 27, 1995
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 5424455
    Abstract: A heterocyclic compound of the formula, ##STR1## wherein A and B are each hydrogen, halogen, alkyl or alkoxy, R.sup.1 is alkylene having upto 6 carbon atoms, X is direct linkage or divalent group such as --O--, --S--and the like, T and U are each hydrogen or alkyl, l is 0 or 1 to 3, Q is 5-, 6- or 7- membered saturated or unsaturated heterocyclic residue, and Y is hydrogen, halogen, alkyl, alkoxy or ##STR2## and B are taken together with each other to form methylene-dioxy, which is useful for dyeing or printing hydrophobic fiber materials with superior dyeability to give a dyed or printed product of a red color excellent in fastness properties, particularly those such as washing fastness.
    Type: Grant
    Filed: July 28, 1993
    Date of Patent: June 13, 1995
    Assignee: Sumitomo Chemical Co., Ltd.
    Inventors: Jun Yamamoto, Yasuyoshi Ueda, Junichi Sekihachi, Yosuke Yamamoto, Takashi Omura
  • Patent number: 5374650
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: March 25, 1993
    Date of Patent: December 20, 1994
    Assignee: Hoechst-Roussel Pharmaceuticals, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
  • Patent number: 5332811
    Abstract: Compounds which are analogs of etoposide and which exhibit anti-tumor activity are disclosed. These compounds having the following structure: ##STR1## wherein R is selected from ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each independently selected from H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, i--C.sub.3 H.sub.7, C.sub.4 H.sub.9, CF.sub.3, OCH.sub.3, OC.sub.2 H.sub.5 , OC.sub.3 H.sub.7, OC.sub.4 H.sub.9, O--i--C.sub.3 H.sub.7, O--i--C.sub.4 H.sub.9, --OCH.sub.2 O--, --OCH.sub.2 CH.sub.2 O--, CH.sub.2 OH, C.sub.2 H.sub.4 OH, CH.sub.2 Cl C.sub.2 H.sub.4 Cl, CH.sub.2 F, C.sub.2 H.sub.4 F, CH.sub.2 OCH.sub.3, COCH.sub.3, COC.sub.2 H.sub.5, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, NO.sub.2, NH.sub.2, NH.sub.2.HCl, NH.sub.2.HAc, NH.sub.2.1/2H.sub.2 SO.sub.4 , NH.sub.2.1/3H.sub.3 PO.sub.4, N(CH.sub.3).sub.2, N(C.sub.2 H.sub.5).sub.2, OH, CN, N.sub.3, SO.sub.2 H, SO.sub.2 NH.sub.2 , SO.sub.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: July 26, 1994
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Xiao-Ming Zhou, Zhe-Qing Wang, Jang-Yang Chang, Hong-Xing Chen, Yung-Chi Cheng, Ya-Ching Shen, Fu-Shen Han, Hong Hu, Yi-Lin Zhang
  • Patent number: 5286881
    Abstract: 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: Grant
    Filed: September 30, 1992
    Date of Patent: February 15, 1994
    Assignee: Sumitomo Chemical Company Limited
    Inventors: Junichi Sekihachi, Jun Yamamoto, Yutaka Kayane
  • Patent number: 5246930
    Abstract: Compounds of formula I ##STR1## in which the substituted R has the given meaning, have an antimalarial and a antiviral activity.
    Type: Grant
    Filed: May 3, 1991
    Date of Patent: September 21, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Bindumadhavan Venugopalan, Chintamani P. Bapat, Pravin J. Karnik, Bansi Lal, Dipak K. Chatterjee, Subramani N. Iyer, Jurgen Blumbach
  • Patent number: 5238939
    Abstract: The invention concerns an isochromane derivative having the general formula I ##STR1## in which R.sub.1 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or as two adjacent substituents together a methylenedioxy group;R.sub.2 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or as two adjacent substituents together a methylenedioxy group;R.sub.3 is one to four substituents independently selected from hydrogen, hydroxy, alkyl (1-4 C), alkoxy (1-4 C), halogen, or CF.sub.3, or as two adjacent substituents together a methylenedioxy group;R.sub.4 is selected from hydrogen or alkyl (1-4 C);A is a bond or an alkylene or alkylidene group with 1-6 carbon atoms;B is an alkylene or alkylidene group with 1-6 carbon atoms when Y is a bond, or B is an alkylene group with 2-6 carbon atoms when Y is a group selected from O, S, or NR.sub.5 ;X is CH or N; andR.sub.
    Type: Grant
    Filed: May 19, 1992
    Date of Patent: August 24, 1993
    Assignee: Akzo N.V.
    Inventors: Michel Combourieu, Jean-Claude Laigle, Nadine Simbille
  • Patent number: 5225436
    Abstract: Certain aryl substituted naphthalene, benzoxepine, benzazepine and henzocycloheptene derivatives are disclosed. The compounds are useful in treating hyperproliferative skin disease, allergic reactions and inflammation.
    Type: Grant
    Filed: October 15, 1991
    Date of Patent: July 6, 1993
    Assignee: Schering Corporation
    Inventors: Neng-Yang Shih, Pietro Mangiaracina, Michael J. Green, Ashit K. Ganguly
  • Patent number: 5225427
    Abstract: 10-substituted ether derivatives of 3.alpha., 12.alpha.-Epoxy-3,4,5 5a.alpha., 6,7,8,8a.alpha.,9,10,12.beta., 12a-dodecahydro-10-hydroxy-3.beta.,6.alpha.,9.beta.-trimethylpyano-(4,3-j) (1,2) benzodioxepin, also known as Dihydroartemisinin or Dihydroquinghaosu (DHQ), pharmaceutically acceptable salts thereof, processes for their preparation and their use as chemotherapeutics against protozoal infections are provided.
    Type: Grant
    Filed: November 27, 1991
    Date of Patent: July 6, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Bindumadhavan Venugopalan, Chintamani P. Bapat, Pravin J. Karnik, Bansi Lal, Dipak K. Chatterjee, Subramani N. Iver, Richard H. Rupp
  • 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: 5180717
    Abstract: 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: Grant
    Filed: May 7, 1991
    Date of Patent: January 19, 1993
    Assignee: The Upjohn Company
    Inventors: Ronald B. Gammill, Frank P. Bell
  • Patent number: 5149714
    Abstract: The present invention provides novel aryloxy indanamines of the formula ##STR1## wherein n, p and q are each independently 0, 1 or 2,Y and X are each independently lower alkyl, lower alkoxy, hydroxy, CF.sub.3, halogeno or when p or q are 2 and each of the Y or each of the X groups are on adjacent aryl carbon atoms, both of the X or both of the Y groups can be taken together to form a methylenedioxy moiety,R.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl, aralkyl, or R.sub.1 and R.sub.2 taken together with the nitrogen to which they are attached are pyrrolidino, morpholino, piperidino, piperazino, or 4-methylpiperazino,or an acid addition salt thereof, which are useful as antidepressants and as inhibitors of synaptic norepinephrine and serotonin uptake.
    Type: Grant
    Filed: August 15, 1990
    Date of Patent: September 22, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Jules Freedman
  • Patent number: 4997836
    Abstract: Novel trisubstituted piperazine compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.
    Type: Grant
    Filed: November 9, 1989
    Date of Patent: March 5, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hirosada Sugihara, Kohei Nishikawa
  • Patent number: 4981962
    Abstract: Substituted tetrathiotetracenes and tetraselenotetracenes of the formula I ##STR1## in which Z is --S-- or --Se-- and (a) R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are H and R.sup.5 to R.sup.8 are each H and at least one of the radicals R.sup.5 to R.sup.8 independently of one another is a substituent belonging to the group comprising C.sub.1 -C.sub.20 alkyl--X--.sub.p which is unsubstituted or substituted by halogen, --CN, --CONR.sup.9 R.sup.10, --OR.sup.9, --SR.sup.9 or --COOR.sup.9, with the exception of C.sub.1 -C.sub.4 alkyl and methoxy, C.sub.2 -C.sub.18 alkenyl--X--.sub.p, C.sub.2 -C.sub.18 -alkynyl--X--.sub.p, C.sub.3 -C.sub.8 cycloalkyl--X--.sub.p, (C.sub.1 -C.sub.12 alkyl)--C.sub.3 -C.sub.8 cycloalkyl--X--.sub.p, C.sub.3 -C.sub.8 cycloalkyl-C.sub.r H.sub.2r --X--.sub.p, (C.sub.1 -C.sub.12 alkyl)-C.sub.3 -C.sub.8 -cyclo alkyl-C.sub.r H.sub.2r --X--.sub.p, phenyl--X--.sub.p, (C.sub.1 -C.sub.12)alkyl)-phenyl--X--, phenyl-C.sub.r H.sub. 2r --X--.sub.p and (C.sub.1 -C.sub.12 alkyl)-phenyl-C.sub.r H.sub.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: January 1, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Marcus Baumann, Walter Fischer, Vratislav Kvita, Carl W. Mayer, Wolfgang Wernet
  • Patent number: 4948796
    Abstract: A piperazine derivative represented by the following formula or a salt thereof: ##STR1## which is useful for curing cerebro-vascular disease and post-cerebro-vascular disease.
    Type: Grant
    Filed: February 27, 1989
    Date of Patent: August 14, 1990
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Toru Hiraiwa, Kenji Takeda, Joji Nakano, Mineichi Sudani, Kunikazu Furuhata, Makoto Takata, Hiroyo Kawafuchi, Isao Watanabe
  • Patent number: 4933344
    Abstract: Ethanone oximes represented by the following general formula: ##STR1## wherein R.sup.1 represents a cycloalkyl group, aryl group, aralkyl group, aryloxy group, aralkyloxy group, arylthio group or aryl sulfonyl group, those groups being optionally substituted with a substituent selected from an alkyl group having 1 to 3 carbon atoms, an alkoxy group having 1 to 3 carbon atoms and a halogen atom, piperidino group, piperazino group, 4-alkyl substituted piparazino group, imidazolyl group, 4-alkyl substituted imidazolyl group or substituted amino group,R.sup.2 represents a hydrogen atom or an alkoxy group having 1 to 3 carbon atoms, andR.sup.3 represents a piperidino group, piperazino group or 4-alkyl substituted piperazino group, orR.sup.1 and R.sup.2 together with a phenyl group to which they are attached may form a phenothiazin-2-yl group, N-acetyl-phenothiazin-2-yl group, thianthren-2-yl group, dibenzothiophen-3-yl group, dibenzofuran-3-yl group or a group of the formula: ##STR2## wherein R.sup.
    Type: Grant
    Filed: August 31, 1988
    Date of Patent: June 12, 1990
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
  • Patent number: 4826840
    Abstract: An indene compound of the general formula (I): ##STR1## in which R.sub.1 represents a lower alkyl group, R.sub.2 represents a hydrogen atom, an aryl group or lower alkyl group, R.sub.3 represents an alkyl group, and n indicates an integer of 2 or 3; or a salt thereof. The compound has very strong ameliorating or improving effects on cerebral circulation and metabolism, and thus is very useful for ameliorating, or suppressing the progress of, disturbances of brain tissues and functions.
    Type: Grant
    Filed: June 19, 1987
    Date of Patent: May 2, 1989
    Assignee: Taiyo Pharmaceutical Industry Co., Ltd.
    Inventors: Shozo Nakaoku, Eiji Imai, Yasuhiro Oshika, Kazuo Ohira
  • Patent number: 4826975
    Abstract: The invention is concerned with fused cycloaliphatic aminoalcohols having pharmacological activity as anti-hypertensive, platelet aggregation inhibiting, hypolipemic, antianoxic and spasmolytic activity. The compounds have the generic formula ##STR1## in which the symbol n is an integer selected from 1 to 2, the compounds pertaining therefore to the indanol and tetralol series.
    Type: Grant
    Filed: December 10, 1986
    Date of Patent: May 2, 1989
    Assignee: Maggioni-Winthrop S.P.A.
    Inventors: Giampaolo Picciola, Mario Riva, Franco Ravenna, Piergiorgio Gentili
  • Patent number: 4762927
    Abstract: The invention provides an indene compound represented by the following general formula (I): ##STR1## wherein R.sub.1 means a lower alkyl group, R.sub.2 and R.sub.3 denote a lower alkyl group individually or an alkylenedioxy group in combination, and R.sub.4 and R.sub.5 mean individually a substituted or unsubstituted lower alkyl or aryl group or in combination a substituted or unsubstituted piperidino, piperazinyl or homopiperazinyl group together with the adjacent nitrogen atom, with a proviso that not both R.sub.4 and R.sub.5 are a methyl group at the same time.
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: August 9, 1988
    Assignee: Taiyo Pharmaceutical Industry Co., Ltd.
    Inventors: Shozo Nakaoku, Kazuhiko Sakuma, Yasuhiro Oshika, Kazuo Ohira
  • Patent number: 4684664
    Abstract: Disclosed herein are derivatives of .beta.-(4-isocyano-1,2,3,4-diepoxycyclopentyl)acrylic acid, the derivatives showing an antibacterial activity, an antifungal activity and an antimycoplasmal activity.
    Type: Grant
    Filed: January 16, 1985
    Date of Patent: August 4, 1987
    Assignee: Kureha Kagaku Kogyo Kabushiki Kaisha
    Inventors: Katsuhisa Osugi, Isao Ichinose, Eisaku Takahashi, Masato Arahira
  • Patent number: 4677103
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: June 30, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4666904
    Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: May 19, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4652651
    Abstract: The manufacture of 1-sulpho-2-oxazetidine derivatives of the formula ##STR1## in which Het is an optionally amino-substituted, 5- or 6-membered, aromatic heterocycle containing 1 or 2 nitrogen atoms and optionally also an oxygen or sulphur atom, R.sup.1 is hydrogen, lower alkyl, phenyl-lower alkyl, lower alkanoyl, lower alkoxycarbonyl, lower alkenyl-lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl-lower-alkoxycarbonyl-lower alkyl, nitrophenyl-lower-alkoxycarbonyl-lower alkyl or carboxy-lower alkyl and R.sup.2 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, lower alkoxycarbonyl, lower alkanoyloxy-lower alkyl, lower alkoxycarbonyl-lower alkenyl, hydroxyiminomethyl, lower alkoxyiminomethyl, carbamoyl, carbamoyl-lower alkenyl or carbamoyloxy-lower alkyl, the group .dbd.NOR.sup.
    Type: Grant
    Filed: April 14, 1986
    Date of Patent: March 24, 1987
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
  • Patent number: 4639443
    Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: April 4, 1986
    Date of Patent: January 27, 1987
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
  • Patent number: 4596804
    Abstract: A dibenz[b,e]oxepin compound having an antiallergic activity is represented by the following general formula: ##STR1## wherein R.sub.1 represents a cyano group, a 5-tetrazolyl group, a carbamoyl group or --CO.sub.2 R.sub.3 wherein R.sub.3 represents a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a 1-(ethoxycarbonyloxy)ethyl group, and R.sub.2 represents a 4-alkylpiperazino group wherein the alkyl group has 1 to 5 carbon atoms, a 3-quinuclidinylamino group or --X--(CH.sub.2).sub.n --NR.sub.4 R.sub.5 wherein X represents --NH--, --S -- or --O--, R.sub.4 and R.sub.5 are same or different and each represents an alkyl group having 1 to 5 carbon atoms and n represents 2 or 3; and the pharmaceutically acceptable acid addition salts or metal salts thereof.
    Type: Grant
    Filed: June 26, 1984
    Date of Patent: June 24, 1986
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Hiroshi Takizawa, Yoshimasa Oiji, Kenji Ohmori, Katsuichi Shuto
  • Patent number: 4590274
    Abstract: Antihypertensive piperazineethylidenebenzocycloalkanes are provided. These compounds have the formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently C.sub.1 -C.sub.6 alkyl, hydrogen, C.sub.1 -C.sub.6 alkoxy, hydroxy, or halo, or R.sub.1 and R.sub.2 or R.sub.2 and R.sub.3 together can form a methylenedioxy bridge;R.sub.4 is H or C.sub.1 -C.sub.6 alkyl;n is 0, 1 or 2;m is 0, 1, 2 or 3; andAr.sub.1 and Ar.sub.2 are independently phenyl optionally substituted with one or two of halogen, hydroxy, or C.sub.1 -C.sub.6 alkoxy groups,or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 3, 1985
    Date of Patent: May 20, 1986
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Anthony J. Cocuzza
  • Patent number: 4556657
    Abstract: New compounds of the formula: ##STR1## wherein X represents hydrogen, halogen, alkyl (1 to 4 C), alkoxy (1 to 4 C), cyano or nitro, R represents alkyl (1 to 4 C) optionally substituted by hydroxy, or alkenyl (2 to 4 C), and n represents 0 or 1, and one of the symbols m and p represents the figure 0 and the other represents the figure 1.The new compounds are therapeutically useful, more particularly as tranquillizers and anticonvulsants.
    Type: Grant
    Filed: April 21, 1983
    Date of Patent: December 3, 1985
    Assignee: Rhone-Poulenc Sante
    Inventors: Daniel Farge, Andre Leger, Gerard Ponsinet
  • Patent number: 4491654
    Abstract: A water-insoluble curing agent for epoxy resins, made by mixing a major amount by weight of a water-insoluble propylene diamine chosen from the group consisting of the C.sub.8 to C.sub.20 fatty propylene diamines and the C.sub.12 to C.sub.15 ether propylene diamines with a minor amount by weight of a water-soluble polyamine suitable for rapid cure of epoxy resins, mixing the resulting mixture with a water-insoluble substituted phenol to give a water-insoluble reaction product, and then reacting said reaction product with formaldehyde. A novel cured epoxy resin is produced by reacting the agent with an uncured epoxy resin, and the reaction can be done in a wet environment or even under water.
    Type: Grant
    Filed: July 11, 1984
    Date of Patent: January 1, 1985
    Inventor: Lowell O. Cummings
  • Patent number: 4487774
    Abstract: Amino derivatives of isochromans are described. These compounds exhibit antipsychotic and hypotensive activity.
    Type: Grant
    Filed: April 21, 1982
    Date of Patent: December 11, 1984
    Assignee: The Upjohn Company
    Inventor: John M. McCall
  • Patent number: 4486428
    Abstract: Bicyclic fused benzenoid compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, where M is O, CH.sub.2 or NR.sub.6 ; R.sub.6 is hydrogen, formyl, carbobenzyloxy or certain carboalkoxyalkyl, alkanoyl, alkyl, aralkyl or aralkylcarbonyl groups;A' is:(1) A where one of A and B is hydrogen such that when A is hydrogen, B is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 1 or 2; when B is hydrogen, A is C(R.sub.2 R.sub.3)(CH.sub.2).sub.f Q and f is 0 or 1, when taken together A and OR.sub.1 form a lactone or certain derivatives thereof;(2) A' is ##STR2## (3) A' is Q.sub.3 ; Q is CO.sub.2 R.sub.7, COR.sub.8, C(OH)R.sub.8 R.sub.9, CN, CONR.sub.12 R.sub.13, CH.sub.2 NR.sub.12 R.sub.13, CH.sub.2 NHCOR.sub.14, CH.sub.2 NHSO.sub.2 R.sub.17 or 5-tetrazoyl;Q.sub.3 is ##STR3## 5-tetrazolyl, CH.sub.2 CONHCOR.sub.7, COOH or certain ester, amide, carboximido or sulfonimido derivatives thereof, CONHOH, CONHCONH.sub.2, or COCH.sub.2 Q.sub.4 where Q.sub.
    Type: Grant
    Filed: January 13, 1983
    Date of Patent: December 4, 1984
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4465848
    Abstract: The present specification provides novel antimicrobial analogs of spectinomycin and intermediates and processes for their preparation. Particularly described are novel 3'-diazo-secospectinomycin derivatives useful in the preparation of a variety of 3'-substituted spectinomycin analogs.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: August 14, 1984
    Assignee: The Upjohn Company
    Inventors: Richard C. Thomas, Edward L. Fritzen
  • Patent number: 4463001
    Abstract: The present invention relates to new 6-substituted 6H-dibenzo [b,d]pyran derivatives, to a process for their preparation and pharmaceutical and veterinary compositions containing them.
    Type: Grant
    Filed: October 1, 1981
    Date of Patent: July 31, 1984
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
  • Patent number: 4459306
    Abstract: This invention relates to novel tricyclic ethers, pharmaceutically acceptable addition salts and optical isomers therefrom. The compounds described herein are useful as psychotropic agents in the treatment of depression and anxiety. Also included herein are methods of preparing said compounds, pharmaceutical compositions including them and methods of treating human or animal beings by administering these pharmaceutical compositions.
    Type: Grant
    Filed: April 6, 1981
    Date of Patent: July 10, 1984
    Assignee: Science Union et Cie
    Inventors: Charles Malen, Jean-Claude Poignant
  • Patent number: 4436921
    Abstract: A 1-(4-aminobenzyl)-2,3-dioxopiperazine derivative represented by the formula: ##STR1## and an acid addition salt thereof have excellent carcinostatic activity but a low toxicity. Therefore, said compounds are useful as medicines and also as intermediates.
    Type: Grant
    Filed: July 16, 1980
    Date of Patent: March 13, 1984
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Takako Hori, Chosaku Yoshida, Yasuo Kiba, Ryuko Takeno, Joji Nakano, Jun Nitta, Sumiko Kishimoto, Shohachi Murakami, Hisatsugu Tsuda, Isamu Saikawa
  • Patent number: 4434295
    Abstract: The present specification provides novel analogs of khellin. These analogs are all useful as antiatherosclerotic agents. Particularly, the present specification provides 4-methoxy, 9-methoxy, or 4,9-dimethoxy-6,7-dihydro-7,7-disubstituted-5H-furo[3,2-g][1]benzopyran-5- ones.
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: February 28, 1984
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4315006
    Abstract: Compounds are disclosed of general formula ##STR1## wherein R.sub.1 represents a hydrogen atom or C.sub.1-4 alkyl or C.sub.2-4 alkenyl group, or the group COANH.sub.2, CSANH.sub.2, or COANHCOCH.sub.2 NH.sub.2 in which A is methylene optionally substituted by a C.sub.1-3 alkyl group; andR.sub.2 represents a hydrogen atom or a C.sub.1-4 alkyl group; or NR.sub.1 R.sub.2 forms a piperidino, piperazino or N-methylpiperazino group;R.sub.3 represents a C.sub.1-4 alkyl group or a benzyl group;R.sub.4 represents a hydrogen or halogen atom; andR.sub.5 represents a hydrogen atom or a C.sub.1-4 alkyl or C.sub.1-4 alkoxy group, with the proviso that one of R.sub.4 and R.sub.5 is a hydrogen atomand physiologically acceptable salts and bioprecursors thereof.The compounds exert effects on the central nervous system and, in particular exhibit anxiolytic and anti-convulsant activity. The compounds may be formulated with pharmaceutically acceptable carriers or diluents for administration in conventional manner.
    Type: Grant
    Filed: August 8, 1980
    Date of Patent: February 9, 1982
    Assignee: Glaxo Group Limited
    Inventor: Richard Storer
  • Patent number: 4284569
    Abstract: The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.
    Type: Grant
    Filed: January 28, 1980
    Date of Patent: August 18, 1981
    Assignee: The Upjohn Company
    Inventor: Ronald B. Gammill
  • Patent number: 4276294
    Abstract: 1-(2-phenyl-3-benzofuryl)-piperazines, e.g. those of the formula ##STR1## R=H, alkyl or halo R', R"=H, alkyl, alkoxy, alkylenedioxy, alkylthio or haloR.degree.=H, alkyl or hydroxyalkyln=2 or 3acyl derivatives, quaternaries and salts thereof are anticonvulsants.
    Type: Grant
    Filed: March 31, 1980
    Date of Patent: June 30, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Robert M. Bowman
  • Patent number: 4252810
    Abstract: 9,10-Dihydro-4H-benzo[4,5]cyclohepta [1,2-b]thiophen-4,9-imines, derivatives and pharmaceutically acceptable salts thereof are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: February 24, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Paul S. Anderson, Ben E. Evans
  • Patent number: 4182889
    Abstract: A process for preparing 10-methyl-2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives is disclosed, wherein a 10-methylen-3-iodomethyl compound of the formula ##STR1## is hydrogenated to obtain a mixture of the corresponding epimeric 10.beta.- and 10.alpha.-methyl-3-iodomethyl compounds, the pure 10.alpha.- and 10.beta.-methyl epimers are separated and recovered from this mixture and are reacted with a secondary amine. Optionally, the substituent in the 4-position of the resulting 10.alpha.- or 10.beta.-methyl-3-aminomethyl compounds are further changed.
    Type: Grant
    Filed: August 22, 1977
    Date of Patent: January 8, 1980
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Akiji Asai, Ivan Ban, Samuel David, Peter W. Thies
  • Patent number: 4166062
    Abstract: 1-Alkoxyethanol-isochromas, -isothiochromas, -2-benzoxepins, and -2-benzothiepins are described. These compounds are useful for preparing the corresponding aminoalkoxyalkyl derivatives that possess antihypertensive and CNS activity.
    Type: Grant
    Filed: July 21, 1978
    Date of Patent: August 28, 1979
    Assignee: The Upjohn Company
    Inventors: John M. McCall, Ruth E. TenBrink
  • Patent number: 4163055
    Abstract: New 2,9-dioxatricyclo[4,3,1,0.sup.3,7 ] decane derivatives are disclosed which are substituted by an amino methyl group in the C.sub.3 position, and which exhibit sedative, especially sleep improving properties, and which have the formula ##STR1## wherein R.sub.1 represents an amino group ONE OF R.sub.2 and R.sub.3 is hydrogen and the other represents hydroxy acyloxy or carbamyloxy or R.sub.2 and R.sub.3 jointly represent oxygenOne of R.sub.4 and R.sub.5 is hydrogen and the other represents alkyloxy or aralkyloxyY and y' each represent hydrogen or jointly form a bond and their pharmacologically acceptable salts, as well as pharmaceutical formulations thereof.
    Type: Grant
    Filed: February 18, 1977
    Date of Patent: July 31, 1979
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Peter W. Thies, Akiji Asai
  • Patent number: 4161589
    Abstract: Spirodipyrans of the formula ##STR1## where A is the radical of a fused benzene ring or 2,1-naphthalene ring, the rings being unsubstituted or substituted by alkyl, alkoxy, nitro, chlorine, bromine or carbalkoxy,R.sup.1 is alkyl, phenyl, substituted alkyl or phenalkyl andR.sup.2 is hydrogen, orR.sup.1 and R.sup.2 together are trimethylene which is unsubstituted or substituted by 1, 2 or 3 alkyl andB is N-morpholinyl, substituted morpholinyl, thiomorpholinyl-S-dioxide, N-(N'-alkyl)-piperazinyl or N-isoindolinyl,And pressure-sensitive recording materials containing these spirodipyrans as dye-forming components.With electron acceptors, the spirodipyrans give reddish violet to blue colorations, while no coloration is produced on paper which has not been coated with an electron acceptor.
    Type: Grant
    Filed: August 8, 1978
    Date of Patent: July 17, 1979
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans Baumann, Andreas Oberlinner