Polycyclo Ring System Having The Six-membered Hetero Ring As One Of The Cyclos Patents (Class 546/18)
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Patent number: 5212186Abstract: Compounds for the treatment of cardiac insufficiency, an arterial thrombo embolism, an arterial occlusive disease, psoriasis, neurodermatitis, asthma, platelet aggregation and hypertension, of the formula ##STR1## in which R.sub.1 is hydrogen, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.3-7 -cycloalkyl,R.sub.2 is hydrogen, C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.1-6 -hydroxyalkyl,R.sub.1 and R.sub.2 together with the carbon atom which carries them can be C.sub.3-7 -spiroalkyl,R.sub.3 is hydrogen or C.sub.1-6 -alkyl, andR.sub.4 is a cyanamido group, a 4-difluoromethoxy-3-pyridyl group or a C.sub.1-2 -nitroalkyl group, andZ is oxygen or sulphur,or a salt, acid addition salt, tautomer or optical isomer thereof.Type: GrantFiled: August 27, 1991Date of Patent: May 18, 1993Assignee: Beiersdorf AktiengesellschaftInventors: Michael Paal, Wolfgang Stenzel, Reinhard Bruckner, Ben Armah
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Patent number: 5208326Abstract: Disclosed are 8-Hydroxy-2H-dibenz[b,f]azepin-2-one dyes, chromogenic enzyme substrates made from them and methods for preparing the same.Type: GrantFiled: November 8, 1991Date of Patent: May 4, 1993Assignee: Miles Inc.Inventor: Paul F. Corey
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Patent number: 5189168Abstract: This invention relates to 1'-amino-2-[(benzothiazolyl)methyl]spiro[isoquinoline-4(1H),3'-pyrrolidine ]-1,2',3,5'(2H)-tetrones represented by formula (I): ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl or nitro;R.sup.4 and R.sup.5 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, aryl, aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms, alkanoyl of 2 to 5 carbon atoms, carboalkoxy, alkylsulfoxy, arylsulfoxy, alkylsulfonyl, arylsulfonyl wherein aryl contains 6 to 10 carbon atoms and alkoxy and alkyl contain 1 to 6 carbon atoms, or R.sup.4 and R.sup.5 together with the nitrogen atoms to which they are bonded represent a heterocyclic ring of 5 to 7 ring atoms and the pharmaceutically acceptable salts thereof when R.sup.4 and R.sup.5 are hydrogen, alkyl or aryl.Type: GrantFiled: November 25, 1991Date of Patent: February 23, 1993Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5189167Abstract: This invention relates to alkylidene analogs of 1'-amino-2-[(benzothiazolyl)-methyl]spiro[isoquinoline-4(1H),3'-pyrrolidon e]-1,2',3,5'(2H)-tetrones represented by formula (I): ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl or nitro;R.sup.4 and R.sup.5 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, aryl, aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms, or R.sup.4 and R.sup.5 are joined to form alicyclic or heterocyclic rings selected from the group consisting of ##STR2## wherein n=1-10; ##STR3## wherein X=O, S, SO, SO.sub.2 ; ##STR4## wherein X=O, S; and ##STR5## wherein R.sup.Type: GrantFiled: November 25, 1991Date of Patent: February 23, 1993Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5185343Abstract: 2-(8-Azabicyclo[3.2.1]oct-8-yl)alkanols of the formula ##STR1## wherein Q is S or CH=CH; X is H, OH or another aromatic substituent; R is hydrogen, alkyl, alkenyl or alkynyl; Y and Y.sup.1 are taken together and are arylmethylene or aralkylmethylene (or a corresponding epoxy derivative) or Y and Y.sup.1 are taken separately and Y is hydrogen or OH, and Y.sup.1 is aryl, aralkyl, arylthio, or aryloxy; and structurally related 2-(piperidino)alkanols; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.Type: GrantFiled: October 23, 1991Date of Patent: February 9, 1993Assignee: Pfizer Inc.Inventor: Bertrand L. Chenard
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Patent number: 5169925Abstract: Novel polymeric polyalkyl-1-oxa-diazaspirodecanes of the formula I ##STR1## are very effective stabilizers for natural any synthetic polymers. They have very low volatility, high migration resistance and high thermal stability.Type: GrantFiled: June 14, 1990Date of Patent: December 8, 1992Assignee: Hoechst AktiengesellschaftInventors: Georg Schmailzl, Gerhard Pfahler, Gunther Nowy
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Patent number: 5149823Abstract: A novel class of sulfonamoyl-substituted 1,6-diaza[4.4]spirodilactams, having a sulfonamoyl substituent on the hydrocarbyl group attached to each spiro ring nitrogen atom, is useful for the preparation of polymers, including polyamides and as latent curing agents for epoxy resins.Type: GrantFiled: August 9, 1990Date of Patent: September 22, 1992Assignee: Shell Oil CompanyInventor: Pen-Chung Wang
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Patent number: 5130442Abstract: Compounds of the formula ##STR1## in which R.sup.1 /R.sup.2 are alkyl, cycloalkyl, aralkyl or alkylene,R.sup.3 is alkyl, cycloalkyl or aralkyl,Z is alkylene,X is O orare highly suitable as color formers in recording materials based on acid developers. They give yellow or orange hues which have excellent sublimation and light fastness.Type: GrantFiled: October 31, 1990Date of Patent: July 14, 1992Assignee: Bayer AktiengesellschaftInventors: Karlheinrich Meisel, Hubertus Psaar
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Patent number: 5109006Abstract: This invention relates to novel derivatives of 1,7'-[imidazo-[1,2-a]pyridine]5'-(6'H)ones, to the method for their preparation and to their use as anti-hypertensive, anxiety, anti-depressant and anti-migraine agents, and to their use as appetite regulators useful for the treatment of anorexia and obesity.Type: GrantFiled: August 22, 1991Date of Patent: April 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Marcel Hibert
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Patent number: 5106978Abstract: The invention relates to a process for producing spiro-isoquinoline pyrrolidines. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: May 22, 1991Date of Patent: April 21, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5102886Abstract: This invention relates to 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones of structural formula (I) ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, alkyl containing 1 to 6 carbon atoms, halogen, lower alkoxy containing 1 to 6 carbon atoms, trifluoromethyl, nitro, aryl or aryl(lower alkyl)oxy wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms;R.sup.3 is lower alkyl containing 1 to 6 carbon atoms, aryl, aryl(lower alkyl) or dihalogen substituted aryl (lower alkyl) wherein aryl contains 6 to 10 carbon atoms and lower alkyl contains 1 to 6 carbon atoms;R.sup.4 and R.sup.Type: GrantFiled: October 12, 1990Date of Patent: April 7, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5093496Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneificial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: April 4, 1991Date of Patent: March 3, 1992Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5084572Abstract: Salts of 3-azabicyclo[3.3.1]nonanes are used in controlling antiarrhythmic processes and precursors thereof are disclosed.Type: GrantFiled: November 13, 1989Date of Patent: January 28, 1992Assignee: Board of Regents of Oklahoma State UniversityInventors: Kenneth D. Berlin, Benjamin J. Scherlag, Cyril R. Clarke, Surendra R. Otiv, Stan A. Zisman, Subbiah Sangiah, Satish V. Mulekar
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Patent number: 5068332Abstract: This invention relates to alkylidene analogs of 1'-aminospiro[isoquinoline-4(1H),3'-pyrrolidine]-1,2',3,5'(2H)-tetrones, represented by formula (I): ##STR1## to processes for the preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: October 11, 1990Date of Patent: November 26, 1991Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5053412Abstract: The invention relates to novel compounds (I) for treating diseases of the central and peripheral nervous system: ##STR1## including enantiomers, racemates and acid addition and quaternary salts thereof, wherein one of X and Y is O and the other of X and Y is N; Q is (CH.sub.2).sub.n or C(CH.sub.3).sub.2 where n is 1, 2 or 3 and the bridge --Q-- is attached at one end to position 1 and at the other end to position 4 or 5, and R.degree. is hydrogen, methyl or hydroxyl; in the moiety ##STR2## the line connecting Z and Y signifies a double bond when X--Z is O--C--R and Y is N, and a single bond when X--Z is N.dbd.C--R and Y is O; Z is C--R wherein R is selected from hydrogen, NH.sub.2, NH-R" (R"=C.sub.1-6 -alkyl), N(R").sub.2, R", C.sub.2-6 -alkenyl, C.sub.2-6 -alkynyl, C.sub.3-7 -cycloalkyl, R" substituted by hydroxy or by 1-6 halogen atoms, R"O-C.sub.1-6 -alkyl, carboxy-C.sub.1-6 -alkyl, R"OCO-C.sub.1-6 -alkyl, amino-C.sub.1-6 -alkyl, R""NH-C.sub.1-6 -alkyl, (R").sub.2 N-C.sub.Type: GrantFiled: April 10, 1990Date of Patent: October 1, 1991Assignee: Israel Institute for Biological ResearchInventors: Abraham Fisher, Ishai Karton
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Patent number: 5045544Abstract: This invention relates to N'-alkyl-spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical perparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes melitus associated complications.Type: GrantFiled: May 21, 1990Date of Patent: September 3, 1991Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5037831Abstract: This invention relates to spiro-isoquinoline-pyrrolidines and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention or treatment of diabetes mellitus associated complications.Type: GrantFiled: May 21, 1990Date of Patent: August 6, 1991Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 5034401Abstract: A compound, in the form of a pure optical isomer or a mixture thereof, of formula (I): ##STR1## in which: Z represents a group of formula --CH.sub.2 --, --C(CH.sub.3).sub.2 --, --CH.dbd.CH--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --NH-- or --N(CH.sub.3)CH.sub.2 --, in which the nitrogen is bonded to the carbonyl group;R1 represents hydrogen or a C.sub.1 -C.sub.4 alkyl group;R2 represents hydrogen or a methyl group; andR3 represents:a phenoxy group which is unsubstituted or substituted by a halogen or a methyl group,a naphthyloxy group,a phenylmethyl group substituted by a halogen or a methyl group,an unsubstituted phenylmethyl group when Z does not representa group of formula --CH.dbd.CH-- or --(CH.sub.2).sub.Type: GrantFiled: July 11, 1989Date of Patent: July 23, 1991Assignee: SynthelaboInventors: Jonathan Frost, Patrick Lardenois, Jean Bertin, Alfred Saarmets, Corinne Rousselle
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Patent number: 5021577Abstract: Polysubstituted N-hydrocarbyloxy hindered amines are effective light stabilizers in protecting organic substrates against the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: June 4, 1991Assignee: Ciba-Geigy CorporationInventor: James P. Galbo
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Patent number: 5006657Abstract: A novel three-step process for resolving a racemic spiro-hydantoin compound into its optical antipodes is disclosed, which involves (1) reacting said racemic compound with an optically-active asymmetric isocyanate of the formula RNCO, wherein R is (S)- or (R)-1-phenylethyl or (S)-or (R)-1-(1-naphthyl)ethyl, to form the corresponding diastereomeric ureido compound; (2) separating the resulting diastereomeric mixture into its component parts, and (3) thereafter converting the separated ureido diasteromers obtained in step (b) to the corresponding asymmetric hydantoin compounds by treatment with an alkali metal lower alkoxide (C.sub.1 -C.sub.4), followed by acidification, whereupon the desired optical isomer is obtained.Type: GrantFiled: June 25, 1990Date of Patent: April 9, 1991Assignee: Pfizer Inc.Inventors: Marcus Brackeen, Harry R. Howard, Jr.
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Patent number: 4996210Abstract: Heterocyclic spiro compounds represented by the following general formula and salts thereof ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.Type: GrantFiled: January 25, 1990Date of Patent: February 26, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Shin-ichi Tsukamoto, Hitoshi Nagaoka, Shinji Usuda, Masatomi Harada, Toshinari Tamura
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Patent number: 4992436Abstract: The present invention provides a spiro-azabicyclic compound or a salt or prodrug thereof, said compound comprising a saturated or unsaturated 5-membered heterocyclic ring containing two heteroatoms selected from oxygen, nitrogen and sulphur, no more than one of said heteroatoms being nitrogen; said heterocyclic ring having a spiro attachment to an optionally substituted azabicyclo[2.2.1]heptane or azabicyclo[3.2.1]octane ring system; which compounds are useful for the treatment of neurological and mental disorders.Type: GrantFiled: June 29, 1989Date of Patent: February 12, 1991Assignee: Merck Sharp & Dohme, Ltd.Inventors: Raymond Baker, Leslie J. Street, John Saunders
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Patent number: 4981858Abstract: The (+)-cis-, (-)-cis-, (+)-trans- and (-)-trans- forms of 2-methylspiro(1,3-oxathiolan-5,3')quinuclidine are prepared by optical resolution of each of the (.+-.)-cis- and (.+-.)-trans-isomers. These compounds find application in treating diseases of the central nervous system in mammals, especially diseases due to a deficiency in the central cholinergic system. Biological tests indicate that the (-)-cis-form, as well as the (.+-.)-cis-isomer, shows particular promise for treating senile dementia of Alzheimer's type.Type: GrantFiled: April 18, 1989Date of Patent: January 1, 1991Assignee: State of Israel, represented by the Prime Minister's Office, Israel Institute for Biological ResearchInventors: Abraham Fisher, Ishal Karton, Eliahu Heidman, Yona Grunfeld, Aharon Levy
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Patent number: 4970309Abstract: This invention relates to a novel method of synthesizing di- and triarylmethane dye precursor compounds possessing a thiolactone ring-closing moiety, from the corresponding lactones.Type: GrantFiled: December 7, 1989Date of Patent: November 13, 1990Assignee: Polaroid CorporationInventor: Patrick F. King
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Patent number: 4943311Abstract: A compound having the structural formula ##STR1## where R is C.sub.2 -C.sub.8 alkylene having 2 to 4 carbon atoms linking X and Y;R.sup.1 is C.sub.1 -C.sub.8 linear or branched alkylene, C.sub.1 -C.sub.6 oxyalkylene, C.sub.1 -C.sub.6 thioalkylene or C.sub.1 -C.sub.6 aminoalkylene;R.sup.2 and R.sup.3 are the same or different and are hydrogen, halogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfonyl, phenyl, substituted phenyl, phenoxy, substituted phenoxy, cyano, nitro, --OCOR.sup.4, --COOR.sup.5, --CH.sub.m Q.sub.3-m or --OCH.sub.m Q.sub.3-m ;R.sup.4 is C.sub.1 -C.sub.4 alkyl;R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl;Q is halogen;X and Y are the same or different and are oxygen, sulfur, sulfinyl, sulfonyl or if one is NH, the other is sulfur;Z is nitrogen or CH; andm is 1, 2 or 3;and physiologically acceptable salts thereof,is disclosed. A process for synthesizing the compound of this invention is also set forth.Type: GrantFiled: May 9, 1988Date of Patent: July 24, 1990Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd/LteeInventors: Hoi K. Lai, Robert A. Davis, Allen R. Blem
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Patent number: 4942235Abstract: A unique process for preparing certain (2R-trans)hexahydroaroquinolizines, especially (2R-trans)-N-[2-(1,3,4,6,7,12b-hexahydro-2'-oxospiro[aro-[2,3-a]-quinolizi ne-2,4'-imidazolidin]-3'-yl)ethyl)-methanesulfonamide from (2R-trans)-N-[2-[(2-cyano-(1,3,4,6,7,12b-hexahydro-aro-[2,3-a]quinolizin-2 -yl)amino]ethyl]methanesulfonamide is described.Type: GrantFiled: March 16, 1989Date of Patent: July 17, 1990Assignee: Merck & Co., Inc.Inventors: Ann E. DeCamp, Ralph P. Volante, Anthony O. King, Ichiro Shinkai
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Patent number: 4940703Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted line represents an optional chemical bond in one of the two possible positions;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, benzyloxy, hydroxy (C.sub.1-6)alkyl, halogen, amino, cyano, nitro, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, halogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, --CH or --C--; andW represents oxygen, sulphur or --NR.sup.8, in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.Type: GrantFiled: April 4, 1989Date of Patent: July 10, 1990Assignee: Merck Sharp & Dohme LimitedInventors: Raymond Baker, Clare O. Kneen, John Saunders, Christopher Swain
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Patent number: 4933336Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.Type: GrantFiled: August 9, 1988Date of Patent: June 12, 1990Assignee: Laboratoires Sobio S.A.Inventors: Michel Martin, Guy Nadler, Richard Zimmermann
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Patent number: 4927831Abstract: This invention relates to spiro-isoquinoline-pyrrolidine tetrones and their pharmaceutically acceptable salts thereof, to processes for their preparation, to methods for using the compounds, and to pharmaceutical preparations thereof. The compounds have pharmaceutical properties which render them beneficial for the prevention of diabetes mellitus associated complications.Type: GrantFiled: May 26, 1989Date of Patent: May 22, 1990Assignee: American Home ProductsInventor: Michael S. Malamas
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Patent number: 4921893Abstract: both R.sub.1 's are CH.sub.3 or together form --CH.sub.2).sub.5 ;both R.sub.2 's are CH.sub.3 or together form --CH.sub.2).sub.5 ;R.sub.3 has a significance of R, independently of R, except for oxygen;X is --O--, --NH-- or ##STR2## m is an integer from 1 to 4 inclusive; R.sub.4 is a saturated or unsaturated aliphatic group unsubstituted or substituted by one or two groups selected from --OH and C.sub.1-4 alkoxy and which can be interrupted by an oxygen or sulphur atom; or an aromatic group unsubstituted or substituted by one or two groups selected from --OH, C.sub.1-4 alkyl and C.sub.1-4 alkoxy are useful as U.V. light stabilizers in polymeric organic compounds.Type: GrantFiled: December 3, 1987Date of Patent: May 1, 1990Assignee: Sandoz Ltd.Inventor: Lajos Avar
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Patent number: 4921982Abstract: This invention provides bicyclic carboxylic esters and amides, their pharmaceutical formulations, and a method for their use in treating migraine, emesis, gastrointestinal disorders, schizophrenia, or anxiety in mammals.Type: GrantFiled: June 14, 1989Date of Patent: May 1, 1990Assignee: Eli Lilly and CompanyInventors: Marlene L. Cohen, William B. Lacefield, David W. Robertson
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Patent number: 4921955Abstract: The invention relates to a process for the preparation of 1,5-disubstituted imidazoles of the formula ##STR1## by alkylation of an N-cyanoformamidine of the formula IIX--NH--CH.dbd.N--CH (II)to form an N,N-disubstituted N'-cyanoformamidine of the formula ##STR2## which is cyclised under the action of bases to form a 4-aminoimidazole of the formula ##STR3## and then reduced to form the product of the formula I. The invention relates also to a special process for the reduction of the aminoimidazole V to I, and to intermediate compounds for carrying out this process and to processes for the preparation of the intermediate compounds.The meaning of the substituents X and L is explained in detail in the text.Type: GrantFiled: December 18, 1987Date of Patent: May 1, 1990Assignee: Ciba-Geigy CorporationInventor: Werner Topfl
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Patent number: 4916175Abstract: Compounds are provided which are useful as light stabilizers for polymeric materials and which have the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are organic radicals, R.sub.3 and R.sub.15 are hydrogen or organic radicals and R is hydrogen, oxygen or an organic radical.Type: GrantFiled: November 5, 1987Date of Patent: April 10, 1990Assignee: Sandoz Ltd.Inventor: Lajos Avar
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Patent number: 4912113Abstract: 3,7-Diazabicyclo[3,3,1]nonane compounds having valuable heart rate-affecting pharmacological properties corresponding to the Formula I: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is lower alkyl,R.sup.3 is lower alkyl, orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents a benzhydryl group, optionally substituted by halogen, lower alkoxy, lower alkyl, hydroxy or trifluoromethyl, or a cinnamyl group optionally substituted by halogen, lower alkyl, lower alkoxy, hydroxy, nitro or trifluoromethyl.Type: GrantFiled: September 2, 1988Date of Patent: March 27, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schon, Wolfgang Kehrbach, Gerd Buschmann, Ulrich Kuhl, Dieter Ziegler
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Patent number: 4906640Abstract: 3-sulfonyl-3,7-diazabicyclo[3,3,1]nonane compounds corresponding to the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkylalkyl or benzyl,R.sup.2 is hydrogen or lower alkyl,R.sup.3 is hydrogen or lower alkyl orR.sup.2 and R.sup.3 together form an alkylene chain, andR.sup.4 represents lower alkyl, thienyl, halogen substituted thienyl or a --(CH.sub.2).sub.n --R.sup.5 group, wherein n=0-3 andR.sup.5 is an optionally substituted phenyl group.The compounds are pharmacologically active, particularly in influencing the motility of the stomach.Type: GrantFiled: June 30, 1988Date of Patent: March 6, 1990Assignee: Kali-Chemie Pharma GmbHInventors: Uwe Schoen, Wolfgang Kehrbach, Klaus-Ullrich Wolf
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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: 4900830Abstract: The invention thus provides a process for obtaining the preferential replacement by isotopes, of at least one of the hydrogen atoms selected from the group consisting of those attached to the .alpha.- or .alpha.'-carbon atoms in a compound containing the structural moiety (I) ##STR1## which comprises the steps of oxidizing the compound to the corresponding sulfoxide or sulfone which contains the corresponding structural moiety (II) ##STR2## wherein in the sulfoxide n is 1 and in the sulfone n is 2, effecting the isotopic replacement by a known method of said at least one hydrogen atom, and reducing the resultant isotope-labelled sulfoxide or sulfone to the correspondingly labelled compound containing the structural moiety (I).Type: GrantFiled: October 28, 1987Date of Patent: February 13, 1990Assignee: Israel Institute for Biological ResearchInventors: Abraham Fisher, Ishai Karton
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Patent number: 4876260Abstract: The present invention accordingly provides in one aspect, novel spiro-oxathiolane/quinuclidine compounds corresponding with the schematic structural formula (I) ##STR1## and geometrical isomers, enantiomers, diastereoisomers, racemates and acid addition salts thereof, wherein one of Y and Z is 0 and the other is S(.dbd.O).sub.n ; n is 0, 1 or 2; R' and R" are each selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, aminoalkyl, C.sub.3-7 cycloalkyl, aryl, diarylmethylol, and alkyl substituted by at least one aryl group, provided that at least R' and R" is other than hydrogen; and each X is hydrogen, or when Y is 0 and Z is S(.dbd.O).sub.n simultaneously, then each X may also be selected from the group consisting of deuterium and tritium, and provided further that when each X is hydrogen, Y is 0 and Z is S simultaneously, then at least one of R' and R" is selected from the group consisting of alkenyl, alkynyl, cyclopropyl, cyclobutyl, cycloheptyl, hydroxyalkyl and aminoalkyl.Type: GrantFiled: May 2, 1988Date of Patent: October 24, 1989Assignee: State of Israel, Israel Institute of Biological ResearchInventors: Abraham Fisher, Ishai Karton
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Patent number: 4874767Abstract: A new biologically active compound discorhabdin D, pharmaceutical compositions containing same, methods of producing the compound and compositions and methods of using them are disclosed.Type: GrantFiled: January 9, 1989Date of Patent: October 17, 1989Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Murray H. G. Munro, Nigel B. Perry, John W. Blunt
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Patent number: 4863932Abstract: Azadecalins and C-7 substituted decalins with squalene oxide cyclase inhibitory activity are useful as inhibitors of cholesterol synthesis and hence may be used in pharmaceuticals for regulating cholesterol levels in a mammal.Type: GrantFiled: March 11, 1988Date of Patent: September 5, 1989Assignees: Somatogenetics International, Inc., Dartmouth CollegeInventors: Michael Sinensky, Thomas A. Spencer
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Patent number: 4855290Abstract: Quinuclidine derivatives having the general formula (I) ##STR1## and geometrical isomers, enantiomers, diastereoisomers, racemates and/or acid addition salts thereof, wherein Z represents the group >CR.sup.1 R.sup.2 or two hydrogen atoms; and R.sup.1 and R.sup.2, which may be identical or different, are each alkyl, cyclopentyl, cyclohexyl, aryl, or diarylmethylol, or alkyl which is substituted by one or more aryl groups, or one of R.sup.1 and R.sup.2 may be hydrogen.Type: GrantFiled: April 18, 1986Date of Patent: August 8, 1989Assignee: State of Israel, represented by Prime Minister's Office, Israel Institute for Biological ResearchInventors: Abraham Fisher, Ishai Karton, Eliahu Heldman, Aharon Levy, Yona Grunfeld
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Patent number: 4855422Abstract: A method for preparing azoniaspironotropanol esters, esters thus produced, and methods of use for these is disclosed. The esters are effective as broncholytics and as agents in therapy of asthmatic conditions.Type: GrantFiled: December 23, 1986Date of Patent: August 8, 1989Assignee: Madaus GmbH & Co.Inventors: Wolf Grimminger, Klaus Gorler, Karl P. Odenthal
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Patent number: 4831035Abstract: Certain substituted hexahydroarylquinolizines and pharmaceutically acceptable salts thereof are peripherally selective .alpha..sub.2 -adrenoceptor antagonists. The compounds are adapted to be employed for the treatment of certain pathological disorders such as hypertension, diabetes, disorders involving platelet aggregation and the like without side effects attributable to effect on the central nervous system.Type: GrantFiled: July 27, 1987Date of Patent: May 16, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Joel R. Huff, Susan J. deSolms, Joseph P. Vacca, Jonathan M. Wiggins, Steven D. Young
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Patent number: 4824849Abstract: Substituted hexahydro arylquinolizines and pharmaceutically acceptable salts thereof are selective .alpha..sub.2 -adrenergic receptor antagonists and thereby useful as antidepressants, antihypertensives, ocular antihypertensives, antidiabetics, platelet aggregation inhibitors, antiobesity agents, and modifiers of gastrointestinal motility.Type: GrantFiled: August 28, 1987Date of Patent: April 25, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Joel R. Huff, Joseph P. Vacca, Steven D. Young, Jane deSolms, James P. Guare, Jr.
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Patent number: 4824835Abstract: The present invention provides isoquinolinedione derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical which is optionally interrupted by a heteroatom or by a heteroatom substituted with an alkyl radical, R.sub.2 is a hydrogen atom or an alkyl or alkenyl radical, or together with R.sub.1, represents a cycloalkylene, alkylidene or cycloalkylidene radical which is optionally interrupted by a heteroatom or by a heteroatom substituted by an alkyl radical and R.sub.3 is a radical of the general formula: ##STR2## which can be in the 5- 6-, 7- or 8-position of the isoquinoline-1,3-dione and in which R.sub.4 and R.sub.5, which can be the same or different, are hydrogen atoms or alkyl, trihaloalkyl, cycloalkyl, cycloalkenyl, dealkylaminoalkyl, alkoxycarbonylalkyl, alkylcarbonyl, aryl or heterayl radicals and X is an oxygen or sulphur atom or a radical of the general formula .dbd.N--R.sub.6, in which R.sub.Type: GrantFiled: April 24, 1987Date of Patent: April 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Bernd Muller-Beckmann
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Patent number: 4813998Abstract: Novel herbicidal 1-heterocyclyl-1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.Type: GrantFiled: August 24, 1987Date of Patent: March 21, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Guy R. E. Van Lommen, William R. Lutz, Jozef F. E. Van Gestel
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Patent number: 4810636Abstract: Chromogenic acridinone enzyme substrate compounds comprising 7-hydroxy-9H-acridin-2-one chromogens derivatized at the 7-hydroxy-position with an enzymatically-cleavable group and disubstituted at the 9-position with alkyl or aryl groups, which can be the same or different, preferably lower alkyl or phenyl, respectively, or together form a cyclohexa-2,5-diene-4-one residue or a 4-hydroxycycloxhexyl residue, and 7-hydroxy-1,3-dihalo-9,9-dimethyl-acridin-2-one intermediates useful for the preparation of the novel chromogenic acridinone enzyme substrate compounds and methods therefor.Type: GrantFiled: November 20, 1987Date of Patent: March 7, 1989Assignee: Miles Inc.Inventor: Paul F. Corey
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Patent number: 4808619Abstract: Compounds of the formula ##STR1## as defined in the specification, and processes for their preparation and methods of using the compounds for the treatment of hypertension in mammals, such as humans and for the treatment and/or prophylaxis of cerebrovascular disorders and/or disorders associated with cerebral senility in mammals, such as humans.Type: GrantFiled: July 30, 1986Date of Patent: February 28, 1989Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp, Charles D. Nicholson, Dieter Angersbach
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Patent number: 4792606Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.Type: GrantFiled: July 16, 1987Date of Patent: December 20, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Hermann-Dieter Krall
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Patent number: 4778891Abstract: A pyranoindolizine derivative represented by the following general formula (I): ##STR1## wherein R means a hydrogen atom or hydroxyl group and Q denotes >C.dbd.O or ##STR2## with a proviso that Q is other than >C.dbd.O when R is a hydrogen atom. Its preparation process is also described.Type: GrantFiled: October 16, 1986Date of Patent: October 18, 1988Assignees: Daiichi Seiyaku Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hiroaki Tagawa, Hirofumi Terasawa, Akio Ejima