Chalcogen Bonded Directly To The Bicyclo-carbocyclic Ring System Patents (Class 546/206)
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Patent number: 5081246Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.Type: GrantFiled: December 20, 1989Date of Patent: January 14, 1992Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki KaishaInventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
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Patent number: 5077035Abstract: Radioiodinated benzovesamicol analogs which selectively localize in presynaptic cholinergic neurons of the general formula: ##STR1## where X is selected from the group consisting of H, OH, NH.sub.2, NHCO-3-[I]-Ph, and a radioactive isotope of iodine, and Y is selected from the group of H and a radioactive isotope of iodine, Y being H is X contains iodine. Illustrative examples include: (.+-.)-trans-2-hydroxy-5-iodo-3-(4-phenylpiperidino)tetralin; (.+-.)-trans-3-hydroxy-5-iodo-2-(4-phenylpiperidino)tetralin; (.+-.)-trans-5-amino-2-hydroxy-8-iodo-3-(4-phenylpiperidino)tetralin; and (.+-.)-trans-2-hydroxy-5-(3-iodobenzamido)-3-(4-phenylpiperidino)tetralin. The novel radioiodinated benzovesamicol analogs may be used as radiopharmaceuticals to visualize cholinergic neurons with conventional imaging devices which are typically found in most nuclear medicine or radiology clinics.Type: GrantFiled: May 14, 1990Date of Patent: December 31, 1991Assignee: The University of MichiganInventors: Donald M. Wieland, Yong-Woon Jung, Marcian E. Van Dort, David L. Gildersleeve
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Patent number: 5061705Abstract: Compounds of formula I ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo, L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen, methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: February 8, 1990Date of Patent: October 29, 1991Assignee: BASF AktiengesellschaftInventors: Hans H. Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
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Patent number: 5059696Abstract: This invention discloses novel intermediates and novel process for their preparation where said intermediates are useful for the preparation of 5-oxygenated derivatives (T) of lovastatin and analogs thereof at the 8-acyl side chain and 6-position of the polyhydronaphthyl ring. Said derivatives of lovastatin (T) and analogs thereof are useful in treating hypercholesterolemia and are disclosed in the U.S. Pat. No. 4,963,538.Type: GrantFiled: March 15, 1990Date of Patent: October 22, 1991Assignee: Merck & Co., Inc.Inventors: Robert K. Anderson, Ann E. DeCamp, Alan T. Kawaguchi, Anthony O. King, Sander G. Mills, Ralph P. Volante
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Patent number: 5055474Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: November 14, 1989Date of Patent: October 8, 1991Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 5051409Abstract: 2-Aminodecalin derivatives of the formula I ##STR1## where R.sup.1, R.sup.2 and R.sup.3 are H or methyl,A is H, OH, O-alkylcarbonyl, O-benzoyl or O-CH.sub.3,R.sup.4 is H, cyclopropyl, alkyl, alkenyl, or alkynyl,R.sup.5 is alkyl, alkenyl or alkynyl which is substituted or unsubstituted,cycloalkyl or cycloalkenyl whic is substituted or unsubstituted, substituted phenylalkyl, substituted cycloalkyl-alkyl, substituted 5-membered heterocyclic ring, bicycloalkyl-alkyl orR.sup.4 and R.sup.5, together with the nitrogen atom, are a substituted or unsubstituted, saturated or unsaturated piperidine radical,their plant-tolerated salts and N-oxides, and fungicides containing these compounds.Type: GrantFiled: November 1, 1989Date of Patent: September 24, 1991Assignee: BASF AktiengesellschaftInventors: Matthias Zipplies, Bernhard Zipperer, Hubert Sauter, Norbert Goetz, Franz Roehl, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5026857Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine or a group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andx denotes oxygen, sulphur or NR.sup.5,and their salts.Type: GrantFiled: July 12, 1989Date of Patent: June 25, 1991Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 5023363Abstract: An aromatic compound of the formula ##STR1## These compounds are useful in human and veterinary medicines and in cosmetic compositions.Type: GrantFiled: April 1, 1988Date of Patent: June 11, 1991Assignee: L'OrealInventors: Jean Maignan, Gerard Lang, Gerard Malle, Serge Restle, Braham Shroot
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Patent number: 5021480Abstract: Compounds which contain azo linkages as well as a hindered amine light stabilizer moiety of low basicity function as free radical polymerization initiators and provide a polymer containing a hindered amine stabilizer chemically bonded to said polymer. The low basicity of the instant compounds prevents interaction with acid catalysts used in some polymerization systems.Type: GrantFiled: February 14, 1990Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 5019650Abstract: Known and novel 4-aryl-4-piperidinecarbinols and heterocyclic analogs are useful as analgesics. Also provided are novel pyrrolidinecarbinols and hexhydroazepine carbinols which are useful as analgesics, antidepressants and, in some cases, as anorectic agents.Type: GrantFiled: August 28, 1989Date of Patent: May 28, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Engelbert Ciganek, Leonard Cook
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Patent number: 5019582Abstract: Novel piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, aryl or heteroaryl which are optionally substituted with one or more C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, C.sub.3-5 -alkylene or aralkoxy,R.sup.1 is straight or branched C.sub.1-8 -alkyl, C.sub.4-8 -alkoxy-C.sub.4-8 -alkyl, C.sub.4-7 -cycloalkyl, aryloxy-C.sub.3-8 -alkyl, C.sub.4-8 -alkenyl, or C.sub.4-8 -cycloalkylalkyl, or R.sup.1 may also be hydrogen or C.sub.1-3 -alkyl, when R.sup.3 is aryl, which is substituted with two or more of C.sub.1-6 - alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, aralkoxy, or with C.sub.3-5 -alkylene.X is hydrogen or halogen, and whereinY is O or Sor a salt thereof with a pharmaceutically-acceptable acid, pharmaceutical compositions thereof, method-of-treating therewith.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: September 14, 1989Date of Patent: May 28, 1991Assignee: Novo Nordisk A/SInventors: Jorgen Drejer, Palle Jakobsen
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Patent number: 5001148Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.Type: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 5000777Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.Type: GrantFiled: November 21, 1989Date of Patent: March 19, 1991Assignees: Ciba-Geigy Corporation, Janssen PharmaceuticaInventors: Henry Szczepanski, Lourens Wals
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Patent number: 4997848Abstract: Compounds of formula (I): ##STR1## in which: R represents hydrogen, methyl of hydroxy; X represents an alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or heterocyclic group; A represents a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y represents hydrogen, or an aryl, cycloalkyl or heterocyclic group] have valuable antihypercholesteremic activities and may be used in the treatment of disorders arising from a blood cholesterol imbalance in humans and other animals.Type: GrantFiled: October 21, 1988Date of Patent: March 5, 1991Assignee: Sankyo Company, LimitedInventors: Masaaki Kurabayashi, Hiroshi Kogen, Hiroshi Kadokawa, Hideshi Kurihara, Kazuo Hasegawa, Masao Kuroda
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Patent number: 4996215Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.Type: GrantFiled: September 15, 1989Date of Patent: February 26, 1991Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
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Patent number: 4994450Abstract: A compound, or a solvate or salt thereof, of formula (I) ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group optionally substituted with a hetero-atom, provided that R.sub.1 and R.sub.2 are not simultaneously hydrogen;R.sub.3 is hydrogen, C.sub.1-6 alkyl, preferably methyl or ethyl, or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;p is 1, 2, 3 or 4, andR is a group of formula (II) ##STR2## in which the group --(CHR.sub.4).sub.n --X-- is in the meta- or para-position with respect to YR.sub.5 or R.sub.6, R.sub.4 is hydrogen or C.sub.1-6 alkyl, preferably hydrogen;n is 0, 1 or 2, preferably 1;X is a direct bond, or O, S or NR.sub.a in which R.sub.a is hydrogen or C.sub.1-6 alkyl, and is preferably a direct bond;Y is >C.dbd.O, >CHOH, --S.dbd.O or --SO.Type: GrantFiled: February 10, 1989Date of Patent: February 19, 1991Assignee: Dr. Lo. Zambeletti S.p.A.Inventors: Vittorio Vecchietti, Antonio Giordani
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Patent number: 4972009Abstract: Compounds possessing both a hindered amine moiety, such as a derivative of 2,2,6,6-tetramethylpiperidine, and a nitrone moiety are valuable stabilizers for protecting polymer compositions against the deleterious effects of actinic light and from the adverse effects of high temperature polymer processing environments. Additionally, the instant compounds present the opportunity for grafting onto preformed polymer backbones.Type: GrantFiled: August 18, 1989Date of Patent: November 20, 1990Assignee: Ciba-Geigy CorporationInventors: Joseph Suhadolnik, Ramanathan Ravichandran
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Patent number: 4970022Abstract: Mustard oils of the formula IR--(A.sup.1 --Z.sup.1).sub.n --A.sup.2 --Z.sup.2 --A.sup.3 --NCSin which A.sup.1, A.sup.2, A.sup.3, R, Z.sup.1, Z.sup.2 and n have the meaning specified in claim 1 can be used as components of liquid-crystalline phases.Type: GrantFiled: August 19, 1987Date of Patent: November 13, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Bernhard Scheuble, Rudolf Eidenschink, Joachim Krause, Eike Poetsch, Andreas Wachtler
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Patent number: 4970231Abstract: HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed.Type: GrantFiled: June 9, 1989Date of Patent: November 13, 1990Assignee: Merck & Co., Inc.Inventors: Ta J. Lee, Wilbur J. Holtz
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Patent number: 4968679Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: May 22, 1989Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4968677Abstract: 1-Aryl-2-naphthoylamines of formula I are described ##STR1## wherein R.sub.1 is halogen, nitro, cyano, C.sub.1 -C.sub.6 alkyl that is unsubstituted or mono- or poly-substituted by halogen and/or C.sub.1 -C.sub.3 alkoxy, or is C.sub.3 -C.sub.6 cycloalkyl, OR.sub.4, NR.sub.5 R.sub.6, CO2R.sub.5, CONR.sub.5 R.sub.6 or NHCOR.sub.7, or wherein two adjacent positions in the nucleus are bridged by a methylenedioxy or ethylenedioxy group that is unsubstituted or mono- or poly-substituted by fluorine, wherein further R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl that is unsubstituted or substituted by C.sub.1 -C.sub.3 alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.4 alkenyl, 2-propynyl, 3-halo-2-propynyl, ##STR2## or COR.sub.7, each of R.sub.5 and R.sub.6, independently of the other, is H or C.sub.1 -C.sub.4 alkyl, R.sub.7 is C.sub.1 -C.sub.Type: GrantFiled: June 14, 1989Date of Patent: November 6, 1990Assignee: Ciba-Geigy CorporationInventor: Peter Riebli
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N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannonojirimycin and pharmaceutical use
Patent number: 4940705Abstract: N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannojirimycin of the formula ##STR1## in which one of R and R' are hydroxyl and the other is hydrogenn is a number from 1 to 6R.sup.1 is hydrogen, alkyl or benzyl andR.sup.2 is alkyl which is optionally substituted by an optionally substituted aryl or by pyridyl, thienyl, furyl, pyrimidyl, pyrazinyl or quinolyl or R.sub.1 is cycloalkyl or R.sup.2 is optionally substituted by aryl or R.sup.2 is a saturated bridged heterocycle or R.sup.1 and R.sup.2 together can form a heterocyclic ring which is optionally substituted. These compounds are useful in the treatment of and prophylaxis of viral infections.Type: GrantFiled: October 26, 1988Date of Patent: July 10, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Bodo Junge, Arnold Paessens, Matthias Schuller -
Patent number: 4939160Abstract: Hydropyridine derivatives of the formula ##STR1## in which R.sub.1 represents carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl, R.sub.2 represents hydrogen, an optionally etherified or acylated hydroxy group or an optionally acylated amino group, and R.sub.3 represents a radical of the formula R- (Ia), R-alk.sub.1 - (Ib) or R'=alk.sub.2 - (Ic) in which R represents a benzocycloalkenyl radical having a total of from 8 to 12 ring carbon atoms which is bonded via a saturated carbon atom and which is unsubstituted or is mono- or poly-substituted in the benzo moiety by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, lower alkyl and/or by trifluoromethyl, and/or substituted in the .alpha.Type: GrantFiled: December 9, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
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Patent number: 4921863Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.Type: GrantFiled: February 17, 1988Date of Patent: May 1, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizou Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu
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Patent number: 4921974Abstract: This invention relates to novel intermediates and novel processes for their preparation where said intermediates are useful in the preparation of 5'-oxygenated derivatives (I) of lovastation and analogs thereof at the 8'-acyl side chain and 6'-position of the polyhydronaphthyl ring. Derivatives (I) and analogs thereof are useful in treating hypercholesterolemia.Type: GrantFiled: September 29, 1988Date of Patent: May 1, 1990Assignee: Merck & Co., Inc.Inventor: Mark E. Duggan
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Patent number: 4909830Abstract: Herbicidal 3-aminopyrazolin-5-ones of the formula ##STR1## in which R.sup.1 stands for alkyl, alkenyl, halogenoalkyl, halogenoalkenyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, for optionally substituted aralkyl or for optionally substituted aryl,R.sup.2 stands for hydrogen or alkyl,R.sup.3 stands for hydrogen or alkyl,R.sup.4 stands for hydrogen, alkyl, alkenyl, alkinyl, alkoxyalkyl, alkylthioalkyl, alkoxycarbonylalkyl or alkanoyl, orR.sup.3 and R.sup.4 together stand for an alkylene or alkenylene radical, each of which is divalent,X stands for halogen, alkyl, alkoxy, alkylthio, halogenoalkyl. halogenoalkoxy or halogenoalkylthio, andZ stands for hydrogen, halogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy or halogenoalkylthio,and acid addition salts thereof. Intermediates of the formula ##STR2## are also disclosed.Type: GrantFiled: November 10, 1988Date of Patent: March 20, 1990Assignee: Bayer AktiengesellschaftInventors: Uta Jensen-Korte, Hans-Joachim Santel, Robert R. Schmidt, Harry Strang
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Patent number: 4902799Abstract: Novel bicyclic alkoxy- and alkylthio-substituted aminoalcohols of formula (I). The compounds show anti-hypertensive, platelet aggregation inhibiting, hypolipemic, antianoxic, spasmolytic, antithrombotic, calcium antagonizing and neuroleptic activity.Type: GrantFiled: June 4, 1987Date of Patent: February 20, 1990Assignee: Maggioni-Winthrop S.p.A.Inventors: Giampaolo Picciola, Mario Riva, Franco Ravenna, Piergiorgio Gentili
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Patent number: 4898607Abstract: 1,5-substituted imidazole derivatives of formula I ##STR1## the stereochemically isomeric forms thereof, and the salts thereof, have useful herbicidal properties. The substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, X.sup.1, X.sup.2, X.sup.3, A, L and m have the meanings defined herein.Type: GrantFiled: August 18, 1988Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Henry Szczepanski, Lourens Wals
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Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
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Patent number: 4895841Abstract: A cyclic amine compound is defined by the formula: ##STR1## in which J is indanyl, indanonyl, indenyl, indenonyl, indanedionyl, tetralonyl, benzosuberonyl, indanolyl or a divalent group thereof, K is phenyl, an arylalkyl or cynnamyl, B is --(CHR22)r--, R22 being H or methyl, --CO--(CHR22)r--, .dbd.(CH--CH.dbd.CH)b--, .dbd.CH--(CH2)c-- or .dbd.(CH--CH)d.dbd. and the ring including T and Q is piperidine. The compound is useful to treat senile dementia.Type: GrantFiled: June 20, 1988Date of Patent: January 23, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Yutaka Tsuchiya, Kunizou Higurashi, Norio Karibe, Youichi Iimura, Atsushi Sasaki, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Takashi Kosasa, Atsuhiko Kubota, Michiko Kosasa, Kiyomi Yamatsu
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Patent number: 4895847Abstract: Novel 2,3-dihydro-1H-indene derivatives and salts thereof represented by the general formula (1), ##STR1## [wherein R.sup.1 and R.sup.2 are each a hydrogen atom, a lower alkyl group, a phenyl group which may have halogen atoms and/or alkyl groups as the substituents on the phenyl ring; R.sup.3 is a halogen atom or a lower alkyl group; R.sup.4 is a hydrogen atom, a halogen atom, a phenyl-lower alkyl group, a cycloalkyl-lower alkyl group or the like; R.sup.5 is a hydroxyimino group, an alkylamino group or a group of the formula --NHR.sup.8 (wherein R.sup.8 is a hydrogen atom, a halogen-substituted lower alkanoyl group or the like); R.sup.6 is a hydrogen atom or a phenyl group; and R.sup.7 is a hydrogen atom or a lower alkyl group].Type: GrantFiled: September 21, 1988Date of Patent: January 23, 1990Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Hiraki Ueda, Kazuyuki Nakagawa
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Patent number: 4888433Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.Type: GrantFiled: August 5, 1987Date of Patent: December 19, 1989Assignee: Zambon, S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4888355Abstract: 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: GrantFiled: December 22, 1987Date of Patent: December 19, 1989Assignee: Roussel UclafInventors: Francois Clemence, Odile Le Martret, Michel Fortin, Francoise Delevallee
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Patent number: 4882339Abstract: Disclosed are compounds of the formula ##STR1## wherein R.sub.1 represents unsubstituted or lower alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, unsubstituted or lower alkyl substituted C.sub.7 -or C.sub.8 -bicycloalkyl, unsubstituted or lower alkyl-substituted adamantyl, 4-piperidinyl or N-lower alkyl or aryl-lower alkyl-substituted piperidinyl, 1- or 2-indanyl, 1- or 2-tetrahydronaphthyl, 1- or 2-perhydroindanyl, 1- or 2-perhydronaphthyl; R.sub.2 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, lower alkanoyl or aryl-lower alkanoyl; or R.sub.1 and R.sub.2 combined with the nitrogen to which they are attached represent pyrrolidino, piperidino, perhydroazepino, morpholino, thiomorpholino, tetrahydro- or perhydro-(isoquinolinyl or quinolinyl), dihydro- or perhydroindolyl, piperazino or N-lower alkyl-piperazino; R.sub.Type: GrantFiled: July 10, 1987Date of Patent: November 21, 1989Assignee: Ciba-Geigy CorporationInventor: Jan W. F. Wasley
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Patent number: 4879284Abstract: The invention relates to a compound of formula: ##STR1## in which formula: R.sub.1 to R.sub.4 denote, independently, H, OH, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; andA denotes --COR.sub.5, R.sub.5 being H when at least one of the substituents R.sub.1 to R.sub.4 is other than H; C.sub.1 -C.sub.6 alkyl; amino; (C.sub.1 -C.sub.6)alkylamino; di(C.sub.1 -C.sub.6) alkylamino; arylamino; benzylamino; amino drived from a cyclic or heterocyclic amine; (--COR.sub.5 being able, when it is an amide group, to be the amide group of an amino acid or of a glucosamine); or alternatively R.sub.5 denotes --OR.sub.6, R.sub.6 being H or (C.sub.1 -C.sub.6)alkyl; C.sub.1 -C.sub.6 mono- or polyhydroxyalkyl, or aryl or benzyl, both optionally substituted; --OR.sub.6 also being able to be derived from a sugar; and the salts and isomers of this compound. The invention also relates to a process for preparing this compound and medicinal and cosmetic compositions containing them.Type: GrantFiled: December 5, 1986Date of Patent: November 7, 1989Assignee: L'OrealInventors: Gerard Land, Jean Maignan, Serge Restle, Gerard Malle
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Patent number: 4877799Abstract: Novel piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, aryl or heteroaryl which are optionally substituted with one or more C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, C.sub.3-5 -alkylene or aralkoxy,R.sup.1 is straight or branched C.sub.1-8 -alkyl, C.sub.4-8 -alkoxy-C.sub.4-8 -alkyl, C.sub.4-7 -cycloalkyl, aryloxy-C.sub.3-8 -alkyl, C.sub.4-8 -alkenyl, or C.sub.4-8 -cycloalkylalkyl, or R.sup.1 may also be hydrogen or C.sub.1-3 -alkyl, when R.sup.3 is aryl, which is substituted with two or more of C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, C.sub.3-8 -cycloalkyl, aralkoxy, or with C.sub.3-5 -alkylene.X is hydrogen or halogen, and whereinY is O or S or a salt thereof with a pharmaceutically-acceptable acid, pharmaceutical compositions thereof, method-of-treating therewith.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: October 8, 1987Date of Patent: October 31, 1989Assignee: A/S FerrosanInventors: Jorgen Drejer, Palle Jakobsen
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Patent number: 4874870Abstract: A process for converting 6-carboxy to 6-hydroxymethyl mevinolin analogs and novel intermediates formed in this process are disclosed.Type: GrantFiled: August 12, 1988Date of Patent: October 17, 1989Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, Thomas H. Scholz
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Patent number: 4873262Abstract: New 8-substituted 2-aminotetralins can be prepared from the corresponding aminotetralins or tetralones. They can be used in medicaments.Type: GrantFiled: December 15, 1987Date of Patent: October 10, 1989Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Bernd Richter, Thomas Glaser, Jorg Traber, George S. Allen
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Patent number: 4866090Abstract: Novel 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1##Type: GrantFiled: January 7, 1988Date of Patent: September 12, 1989Assignee: Merck & Co., Inc.Inventors: William F. Hoffman, Robert L. Smith, Ta J. Lee
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Patent number: 4857524Abstract: In one embodiment this invention provides novel thiazolidine compounds, such as 3-[R-(-)-3-benzyloxycarbonylthiazolidine-4-carbonyl]thiazolidine corresponding to the formula: ##STR1## An invention thiazolidine compound exhibits prolyl endopeplidase inhibitory activity, and has utility as a therapeutic agent for the treatment of dementia and amnesia disorders.Type: GrantFiled: August 3, 1988Date of Patent: August 15, 1989Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Sunao Furukawa, Tadashi Yoshimoto, Yukiyoshi Ajisawa, Seiichi Ikeguchi, Yukihiko Kinoshita
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Patent number: 4857522Abstract: Derivatives of pravastatin are provided which are useful in inhibiting cholesterol biosynthesis and in preparing radiolabeled compounds useful in the radioimmunoassay (RIA) of pravastatin and derivatives thereof. The pravastatin derivatives have the structure ##STR1## wherein R is hydroxy, lower alkylamine, arylamine, arylalkylamine or heterocyclic alkylamine such as histamine, tyramine, O-benzyltyramine, methyl tyrosinate as well as iodinated derivatives thereof.Type: GrantFiled: March 21, 1988Date of Patent: August 15, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Richard A. DiPietro, Jan-I Tu, Noor Z. Turabi
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Patent number: 4855464Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## group, R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.Type: GrantFiled: December 17, 1987Date of Patent: August 8, 1989Assignee: Zambon S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4845237Abstract: A novel acylation process using an alkali metal bromide and a dialkylaminopyridine to form a sterically hindered ester functionality from an alkanoyl chloride and an alcohol is disclosed.Type: GrantFiled: April 15, 1987Date of Patent: July 4, 1989Assignee: Merck & Co., Inc.Inventors: Ann E. DeCamp, Leonard M. Weinstock, Thomas R. Verhoeven
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Patent number: 4840951Abstract: Naphthalene derivative of the formula: ##STR1## wherein Ring A is a substituted or unsubstituted benzene ring; each of R.sup.1 and R.sup.2 is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR2## or either one of R.sup.1 and R.sup.2 is a lower alkoxy group and the other one is a group of the formula: --OR.sup.5, --NHR.sup.5 or ##STR3## each of R.sup.3 and R.sup.4 is a lower alkoxy group, or one of R.sup.3 and R.sup.4 is a lower alkoxy group and the other is a hydrogen atom; R.sup.5 is a substituted alkyl group, a heterocyclic group, a cycloalkyl group, an alkyl group of at least 5 carbon atoms or alkenyl group; and each of R.sup.6 and R.sup.7 is hydrogen atom or a lower alkyl group and salts thereof are disclosed. Said naphthalene derivative (I) and its salts have excellent hypolipidemic activity and are useful for treatment or prophylaxis of hyperlipidemia and/or arteriosclerosis.Type: GrantFiled: June 17, 1987Date of Patent: June 20, 1989Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tameo Iwasaki, Kohki Takashima
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Patent number: 4838931Abstract: 1,2-Disubstituted piperidines of the general formula I ##STR1## in which X denotes oxygen or sulfur; R denotes alkyl, R.sup.1 and R.sup.2 denote hydrogen, alkyl or benzyl, R.sup.3 denotes hydrogen, (substituted) alkyl, (substituted) benzyl or a radical of the formulae ##STR2## Y and X denote S or O; Z denotes S, O or NR.sup.1 ; R.sup.4 denotes hydrogen, (substituted) alkyl, (substituted) phenyl, (substituted) naphthyl or (substituted) pyridyl, A denotes (substituted) phenyl or (substituted) naphthyl and m denotes 0, 1 or 2, possess advantageous herbicidal properties.Type: GrantFiled: January 14, 1987Date of Patent: June 13, 1989Assignee: Hoechst AktiengesellschaftInventors: Rainer Liebl, Michael Frey, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer
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Patent number: 4833169Abstract: Hydropyridine derivatives of the formula ##STR1## in which R.sub.1 represents carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl, R.sub.2 represents hydrogen, an optionally etherified or acylated hydroxy group or an optionally acylated amino group, and R.sub.3 represents a radical of the formula R-- (Ia), R--alk.sub.1 -- (Ib) or R'.dbd.alk.sub.2 -- (Ic) in which R represents a benzocycloalkenyl radical having a total of from 8 to 12 ring carbon atoms which is bonded via a saturated carbon atom and which is unsubstituted or is mono- or poly-substituted in the benzo moiety by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, lower alkyl and/or by trifluoromethyl, and/or subsituted in the .alpha.Type: GrantFiled: August 3, 1988Date of Patent: May 23, 1989Assignee: Ciba-Geigy CorporationInventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
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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: 4818431Abstract: New tetrahydropyran derivatives of the formula I ##STR1## in which G is H.sub.2 or .dbd.O, R.sup.1 and R.sup.2 are each an alkyl group having 1-10 C atoms, it also being possible for one or two CH.sub.2 groups to be replaced by O atoms, or are F, Cl, Br or CN, R.sup.2 is also H, A.sup.1 and A.sup.2 are each 1,4-phenylene, 1,4-cyclohexylene, 1,3-dioxane-2,5-diyl, piperidine-1,4-diyl, 1,4-bicyclo[2.2.2]octylene or pyrimidine-2,5-diyl groups which are unsubstituted or substituted by 1-4 F atoms, Z.sup.1 and Z.sup.2 are each --CO--O--, --O--CO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.2 --, --CH.sub.2 O--, or a single bond, m and n are each 0, 1, 2 or 3, but (m+n) is at least 1 and at most 3, it being possible, when m is 2 or 3, for the group A.sup.1 and, when n is 2 or 3, for the groups A.sup.2 each to be identical or different from one another, and the acid addition salts of those among these compounds which are basic, are suitable for use as components in liquid-crystal dielectrics.Type: GrantFiled: November 24, 1986Date of Patent: April 4, 1989Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rudolf Eidenschink, Joachim Krause, Peter Fuss
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Patent number: 4810791Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definintion of X may also be useful as analgesics due to their enkephalinase inhibition activity.Type: GrantFiled: December 28, 1987Date of Patent: March 7, 1989Assignee: E. R. Squibb & Sons, Inc.Inventors: Harold N. Weller, III, Eric M. Gordon
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Patent number: 4810819Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represents a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.Type: GrantFiled: August 5, 1987Date of Patent: March 7, 1989Assignee: Zambon SpaInventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli