Plural Ring Chalcogens In The Polycyclo Ring System Or The Piperazine Ring Bonded Directly To The Polycyclo Ring System Patents (Class 544/378)
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Patent number: 5798350Abstract: 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: GrantFiled: May 3, 1996Date of Patent: August 25, 1998Assignee: Allelix Biopharmaceuticals, Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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Patent number: 5759450Abstract: 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: GrantFiled: July 31, 1996Date of Patent: June 2, 1998Assignee: Vision-Ease Lens, Inc.Inventors: Frank J. Hughes, Edward A. Travnicek
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Patent number: 5702645Abstract: 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: GrantFiled: October 30, 1995Date of Patent: December 30, 1997Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5646175Abstract: 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: GrantFiled: June 1, 1995Date of Patent: July 8, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5543427Abstract: 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: GrantFiled: August 24, 1994Date of Patent: August 6, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
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Patent number: 5541183Abstract: 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: GrantFiled: December 29, 1994Date of Patent: July 30, 1996Assignee: 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
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Patent number: 5538965Abstract: 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: GrantFiled: December 12, 1994Date of Patent: July 23, 1996Assignee: Allelix Biopharmaceuticals Inc.Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
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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: 5424455Abstract: 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: GrantFiled: July 28, 1993Date of Patent: June 13, 1995Assignee: Sumitomo Chemical Co., Ltd.Inventors: Jun Yamamoto, Yasuyoshi Ueda, Junichi Sekihachi, Yosuke Yamamoto, Takashi Omura
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Patent number: 5374650Abstract: 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: GrantFiled: March 25, 1993Date of Patent: December 20, 1994Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill, Gerard O'Malley
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Patent number: 5332811Abstract: 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: GrantFiled: May 1, 1991Date of Patent: July 26, 1994Assignee: The University of North Carolina at Chapel HillInventors: 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
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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: 5246930Abstract: Compounds of formula I ##STR1## in which the substituted R has the given meaning, have an antimalarial and a antiviral activity.Type: GrantFiled: May 3, 1991Date of Patent: September 21, 1993Assignee: Hoechst AktiengesellschaftInventors: Bindumadhavan Venugopalan, Chintamani P. Bapat, Pravin J. Karnik, Bansi Lal, Dipak K. Chatterjee, Subramani N. Iyer, Jurgen Blumbach
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Patent number: 5238939Abstract: 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: GrantFiled: May 19, 1992Date of Patent: August 24, 1993Assignee: Akzo N.V.Inventors: Michel Combourieu, Jean-Claude Laigle, Nadine Simbille
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Patent number: 5225436Abstract: 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: GrantFiled: October 15, 1991Date of Patent: July 6, 1993Assignee: Schering CorporationInventors: Neng-Yang Shih, Pietro Mangiaracina, Michael J. Green, Ashit K. Ganguly
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Patent number: 5225427Abstract: 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: GrantFiled: November 27, 1991Date of Patent: July 6, 1993Assignee: Hoechst AktiengesellschaftInventors: Bindumadhavan Venugopalan, Chintamani P. Bapat, Pravin J. Karnik, Bansi Lal, Dipak K. Chatterjee, Subramani N. Iver, Richard H. Rupp
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Patent number: 5223616Abstract: 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: GrantFiled: November 4, 1991Date of Patent: June 29, 1993Assignee: Sumitomo Chemical Company, Ltd.Inventors: Jun Yamamoto, Junichi Sekihachi, Yosuke Yamamoto, Kazuhiro Machiguchi, Yutaka Kayane
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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: 5149714Abstract: 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: GrantFiled: August 15, 1990Date of Patent: September 22, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Jules Freedman
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Patent number: 4997836Abstract: 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: GrantFiled: November 9, 1989Date of Patent: March 5, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Kohei Nishikawa
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Patent number: 4981962Abstract: 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: GrantFiled: May 24, 1989Date of Patent: January 1, 1991Assignee: Ciba-Geigy CorporationInventors: Marcus Baumann, Walter Fischer, Vratislav Kvita, Carl W. Mayer, Wolfgang Wernet
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Patent number: 4948796Abstract: 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: GrantFiled: February 27, 1989Date of Patent: August 14, 1990Assignee: Toyama Chemical Co., Ltd.Inventors: Toru Hiraiwa, Kenji Takeda, Joji Nakano, Mineichi Sudani, Kunikazu Furuhata, Makoto Takata, Hiroyo Kawafuchi, Isao Watanabe
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Patent number: 4933344Abstract: 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: GrantFiled: August 31, 1988Date of Patent: June 12, 1990Assignee: Mitsubishi Kasei CorporationInventors: Shinichiro Fujimori, Satoshi Yamazaki, Mamoru Sugano, Makoto Kawamura, Kunihiro Ninomiya, Akihiro Tobe, Issei Nitta
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Patent number: 4826840Abstract: 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: GrantFiled: June 19, 1987Date of Patent: May 2, 1989Assignee: Taiyo Pharmaceutical Industry Co., Ltd.Inventors: Shozo Nakaoku, Eiji Imai, Yasuhiro Oshika, Kazuo Ohira
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Patent number: 4826975Abstract: 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: GrantFiled: December 10, 1986Date of Patent: May 2, 1989Assignee: Maggioni-Winthrop S.P.A.Inventors: Giampaolo Picciola, Mario Riva, Franco Ravenna, Piergiorgio Gentili
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Patent number: 4762927Abstract: 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: GrantFiled: July 11, 1986Date of Patent: August 9, 1988Assignee: Taiyo Pharmaceutical Industry Co., Ltd.Inventors: Shozo Nakaoku, Kazuhiko Sakuma, Yasuhiro Oshika, Kazuo Ohira
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Patent number: 4684664Abstract: 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: GrantFiled: January 16, 1985Date of Patent: August 4, 1987Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Katsuhisa Osugi, Isao Ichinose, Eisaku Takahashi, Masato Arahira
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Patent number: 4677103Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: October 20, 1986Date of Patent: June 30, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4666904Abstract: Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: October 20, 1986Date of Patent: May 19, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4652651Abstract: 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: GrantFiled: April 14, 1986Date of Patent: March 24, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Andre Furlenmeier, Werner Hofheinz, Christian N. Hubschwerlen, Hans P. Isenring
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Patent number: 4639443Abstract: Novel labdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: April 4, 1986Date of Patent: January 27, 1987Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Raymond W. Kosley, Jr., Robert J. Cherill
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Patent number: 4596804Abstract: 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: GrantFiled: June 26, 1984Date of Patent: June 24, 1986Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Hiroshi Takizawa, Yoshimasa Oiji, Kenji Ohmori, Katsuichi Shuto
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Patent number: 4590274Abstract: 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: GrantFiled: January 3, 1985Date of Patent: May 20, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Anthony J. Cocuzza
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Patent number: 4556657Abstract: 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: GrantFiled: April 21, 1983Date of Patent: December 3, 1985Assignee: Rhone-Poulenc SanteInventors: Daniel Farge, Andre Leger, Gerard Ponsinet
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Patent number: 4491654Abstract: 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: GrantFiled: July 11, 1984Date of Patent: January 1, 1985Inventor: Lowell O. Cummings
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Patent number: 4487774Abstract: Amino derivatives of isochromans are described. These compounds exhibit antipsychotic and hypotensive activity.Type: GrantFiled: April 21, 1982Date of Patent: December 11, 1984Assignee: The Upjohn CompanyInventor: John M. McCall
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Patent number: 4486428Abstract: 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: GrantFiled: January 13, 1983Date of Patent: December 4, 1984Assignee: Pfizer Inc.Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4465848Abstract: 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: GrantFiled: September 13, 1982Date of Patent: August 14, 1984Assignee: The Upjohn CompanyInventors: Richard C. Thomas, Edward L. Fritzen
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Patent number: 4463001Abstract: 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: GrantFiled: October 1, 1981Date of Patent: July 31, 1984Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Piero Melloni, Paolo Salvadori, Pier P. Lovisolo
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Patent number: 4459306Abstract: 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: GrantFiled: April 6, 1981Date of Patent: July 10, 1984Assignee: Science Union et CieInventors: Charles Malen, Jean-Claude Poignant
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Patent number: 4436921Abstract: 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: GrantFiled: July 16, 1980Date of Patent: March 13, 1984Assignee: 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
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Patent number: 4434295Abstract: 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: GrantFiled: May 17, 1982Date of Patent: February 28, 1984Assignee: The Upjohn CompanyInventor: Ronald B. Gammill
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Patent number: 4315006Abstract: 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: GrantFiled: August 8, 1980Date of Patent: February 9, 1982Assignee: Glaxo Group LimitedInventor: Richard Storer
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Patent number: 4284569Abstract: The present specification relates to the antiatherosclerotic use of khellin and related furochromones, and further provides novel antiatherogenic furochromones.Type: GrantFiled: January 28, 1980Date of Patent: August 18, 1981Assignee: The Upjohn CompanyInventor: Ronald B. Gammill
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Patent number: 4276294Abstract: 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: GrantFiled: March 31, 1980Date of Patent: June 30, 1981Assignee: Ciba-Geigy CorporationInventor: Robert M. Bowman
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Patent number: 4252810Abstract: 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: GrantFiled: November 15, 1978Date of Patent: February 24, 1981Assignee: Merck & Co., Inc.Inventors: Paul S. Anderson, Ben E. Evans
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Patent number: 4182889Abstract: 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: GrantFiled: August 22, 1977Date of Patent: January 8, 1980Assignee: Kali-Chemie Pharma GmbHInventors: Akiji Asai, Ivan Ban, Samuel David, Peter W. Thies
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Patent number: 4166062Abstract: 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: GrantFiled: July 21, 1978Date of Patent: August 28, 1979Assignee: The Upjohn CompanyInventors: John M. McCall, Ruth E. TenBrink
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Patent number: 4163055Abstract: 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: GrantFiled: February 18, 1977Date of Patent: July 31, 1979Assignee: Kali-Chemie Pharma GmbHInventors: Peter W. Thies, Akiji Asai
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Patent number: 4161589Abstract: 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: GrantFiled: August 8, 1978Date of Patent: July 17, 1979Assignee: BASF AktiengesellschaftInventors: Hans Baumann, Andreas Oberlinner