Plural Carbocyclic Rings Containing Patents (Class 546/234)
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Patent number: 5306720Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.Type: GrantFiled: December 20, 1991Date of Patent: April 26, 1994Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5290796Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.Type: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5273983Abstract: Novel N-cyclohexylbenzamide derivatives of formula: ##STR1## where R.sub.1 represents an alkoxy radical capable of cyclizing with the aromatic ring;R.sub.2, R.sub.3 and R.sub.4 each independently represent hydrogen, a halogen or an alkoxy, amino, alkylamino or alkyl-carbonylamino group, andZ represents a differently substituted piperidinyl group; and their addition salts with pharmaceutically acceptable acids.The compounds of formula I are powerful gastrointestinal motility stimulants.Type: GrantFiled: March 25, 1992Date of Patent: December 28, 1993Assignee: Laboratories Jacques LogeaisInventors: Helene Christinaki, Thierry Bouyssou, Michel Pairet, Alain Renaud
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Patent number: 5270328Abstract: N-alkylamino-3,4,4-substituted piperidines are provided which are useful as peripheral opioid antagonists.Type: GrantFiled: June 29, 1992Date of Patent: December 14, 1993Assignee: Eli Lilly and CompanyInventors: Buddy E. Cantrell, Dennis M. Zimmerman
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Patent number: 5254569Abstract: This invention relates to (amidomethyl)nitrogen heterocyclic and pyrrolidine compounds, pharmaceutical compositions containing them, methods of using such compounds and processes for making such compounds.Type: GrantFiled: January 14, 1991Date of Patent: October 19, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Robert S. Cheeseman, Hollis S. Kezar, III, Richard M. Scribner
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Patent number: 5252586Abstract: Novel unsaturated ether derivatives of alkyl piperidine and pyrrolidine compounds, pharmaceutical compositions containing them, methods of preparation and methods of using these compounds as antipsychotic agents are disclosed.Type: GrantFiled: September 28, 1990Date of Patent: October 12, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
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Patent number: 5250542Abstract: 3,4,4-trisubstitutedpiperidinyl-N-alkylcarboxylates and intermediates for their preparation are provided. These piperidine-N-alkylcarboxylates are useful as peripheral opioid antagonists.Type: GrantFiled: July 17, 1992Date of Patent: October 5, 1993Assignee: Eli Lilly and CompanyInventors: Buddy E. Cantrell, Dennis M. Zimmerman
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Patent number: 5236956Abstract: The invention concerns compounds having the formula I ##STR1## wherein Ar is a phenyl or benzyl group which is optionally substituted with hydroxy or alkoxy;R.sup.1 is hydrogen, lower alkyl, lower alkoxy, hydroxy;R.sup.2 is hydrogen, lower alkyl;R.sup.3 is NR.sup.4 R.sup.5, whereinR.sup.4 and R.sup.5 which can be the same or different, are lower alkyl, or wherein R.sup.4 and R.sup.5, when taken together, form a ring with the nitrogen atom, whereby said ring optionally is substituted with lower alkyl;n is 0 or 1;m is 2 or 3 andtheir salts with physiologically acceptable acids and when the compounds can be in form of optical isomers, the racemic mixture and the individual isomers, for the treatment of disorders of the urinary bladder.Type: GrantFiled: October 7, 1991Date of Patent: August 17, 1993Assignee: Kabi Pharmacia AktiebolagInventors: Christer Sjogren, Rene Mollberg, Sten Kelfve
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Patent number: 5221692Abstract: The present invention provides a series of ether linked analogues of N-nonanoyl vanillylamide. They are found pharmaceutically effective in antinociceptive treatment and relatively nonpungent.Type: GrantFiled: August 22, 1991Date of Patent: June 22, 1993Assignee: National Science CouncilInventor: Ing-Jun Chen
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Patent number: 5216167Abstract: Phenylacetic acid benzylamides having the following general structure ##STR1## wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: June 21, 1990Date of Patent: June 1, 1993Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, deceased, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht
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Patent number: 5214141Abstract: The present invention relates to an azomethine compound represented by formula (I): ##STR1## wherein X represents a 5- or 6-membered cyclic amino group, R represents an aromatic group, and Ar represents an aromatic group having an aliphatic amino group in the para-position. The azomethine compounds disclosed are useful yellow dyes for photography, for various optical filters, for ink jet, for heat transfer printing, and for printing.Type: GrantFiled: December 31, 1991Date of Patent: May 25, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Masuji Motoki, Naoki Saito, Takayoshi Kamio, Mitsugu Tanaka, Seiji Ichijima
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Piperidinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension
Patent number: 5212185Abstract: Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO.sub.2 ; wherein X is selected from oxygen atom and methylene; wherein B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R.sub.1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R.sub.2 is phenylmethyl; wherein each of R.sub.3 and R.sub.5 is hydrido; wherein R.sub.4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R.sub.6 is cyclohexylmethyl; wherein R.sub.7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: August 14, 1992Date of Patent: May 18, 1993Assignee: G. D. Searle & Co.Inventor: Gunnar J. Hanson -
Patent number: 5204474Abstract: 2,6-Diarylpiperidin-1-yl substituted 2-butene stabilizers of the formula I or IIT--CH.sub.2 --CH.dbd.CH--CH.sub.2 --T (I)T--CH.sub.2 --CH.dbd.CH--CH.sub.2 --N(E.sub.1)(E.sub.2) (II)where T is a 2,6-diarylpiperidin-1-yl moiety and E.sub.1 and E.sub.2 are independently alkyl, cycloalkyl, aralkyl or aryl, are effective in stabilizing organic materials against the deleterious effects of oxygen, heat and actinic radiation.Type: GrantFiled: June 3, 1991Date of Patent: April 20, 1993Assignee: Ciba-Geigy CorporationInventors: Glen T. Cunkle, Joseph E. Babiarz
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Patent number: 5169856Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.Type: GrantFiled: February 6, 1989Date of Patent: December 8, 1992Assignee: Takeda Chemical Industries, Inc.Inventors: Giichi Goto, Akinobu Nagaoka
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Patent number: 5118684Abstract: A novel piperidine derivative is defined by the formula (I), including a slt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: April 3, 1991Date of Patent: June 2, 1992Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5112867Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits born absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: April 27, 1990Date of Patent: May 12, 1992Assignee: Kyowa Hakko Gogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kasaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5093341Abstract: The present invention is directed to a new class of compounds useful as antiarrhythmics, analgesics and serotonin 5HT.sub.2 antagonists, which compounds have the following formula: ##STR1## wherein; Y is represented by H, CO(CH.sub.2).sub.n CH.sub.3 in which n is an integer from 0-3, or SO.sub.2 (CH.sub.2).sub.n CH.sub.3 in which n is an integer from 0--3; X is represented CO, CHOH, or C.dbd.N--O--A, wherein A is represented by hydrogen or a C.sub.1-4 alkyl; R is either selected from the group consisting of halogens, lower alkyl groups, lower alkoxy groups, and hydrogen or R is a divalent substituent and is represented by a 3,4-methylenedioxy or a 3,4-ethylenedioxy substituent; m is an integer from 1-5; and the pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: August 26, 1988Date of Patent: March 3, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Albert A. Carr, John E. Koerner, Richard C. Dage, Tung Li, Francis P. Miller
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Patent number: 5091393Abstract: The invention relates to a group of tertiary 2,5-dialkyl-3-phenylpiperidine derivatives, having opiate-antagonistic activity represented by general formula 4, ##STR1## wherein A.sub.1 is hydrogen, an optionally esterified hydroxyl group or mercapto group, a group NHA.sub.8 or --CONHA.sub.8, wherein A.sub.8 is hydrogen, alkyl having 1-6 C-atoms or alkylcarbonyl having 2-7 C-atoms;A.sub.2 is hydrogen or, when A.sub.1 is hydrogen, one of the other meanings of A.sub.1, orA.sub.1 and A.sub.2 together with the 2 carbon atoms of the benzene ring,constitute a heterocyclic group which consists of five or six ring atoms and which comprises a group --NH-- and optionally as a second hetero atom may comprise an oxygen atom, sulphur atom or nitrogen atom;A.sub.3 and A.sub.4 independently of each other are straight or branched alkyl or alkenyl having 1-6 C-atoms;A.sub.Type: GrantFiled: May 29, 1990Date of Patent: February 25, 1992Assignee: Duphar International Research B.V.Inventors: Jacobus A. Den Hartog, Ineke Van Wijngaarden, Martinus T. Tulp
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Patent number: 5066680Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is aryl which may have one or more suitable substituent(s),R.sup.2 is aryl which may have one or more suitable substituent(s), lower alkyl or cyclo(lower)alkyl,R.sup.3 is hydrogen, hydroxy, halogen, lower alkenyl, amino or protected amino,R.sup.4 is a group of the formula: ##STR2## wherein R.sup.5 is lower alkyl which may have one or more suitable substituent(s), cyclo(lower)alkyl, aryl, ar(lower)alkyl which may have one or more suitable substituent(s), andR.sup.6 is hydrogen or lower alkyl; or N-containing heterocyclic group which may have one or more suitable substituent(s), andA is lower alkylene or lower alkynylene, in which R.sup.1 and R.sup.2 may be linked through oxygen atom, their preparation and use in treatment of dysuria, and starting materials for their preparation.Type: GrantFiled: February 5, 1990Date of Patent: November 19, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Kazuo Okumura, Kazuhiko Take, Kazunori Tsubaki
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Patent number: 5063235Abstract: Novel compounds of the formula: ##STR1## are disclosed wherein Ar and Ar.sup.1 are phenyl, sustituted phenyl or pyridinyl, "alk" is a C.sub.1 -C.sub.12 straight or branched hydrocarbon chain, and R is H, loweralkylcarbonyl, arylcarbonyl, or aminocarbonyl where the amino is unsubstituted or substituted by one or two groups selected from loweralkyl or aryl. The compounds of this invention are useful in the treatment of allergic disorders.Type: GrantFiled: April 30, 1990Date of Patent: November 5, 1991Assignee: A. H. Robins Company, Inc.Inventor: David A. Walsh
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Patent number: 5057524Abstract: Novel compounds useful in the treatment of allergic disorders and having the formula: ##STR1## where Ar and Ar.sup.1 are pyridinyl, phenyl, or substituted phenyl and where Y is --OH,--O.sup..crclbar. M.sup..sym. m,--O--loweralkyl, --O--Aryl, or NR.sup.1 R.sup.2 (R.sup.1, R.sup.2 .dbd.H, loweralkyl, aryl) are herein disclosed.Type: GrantFiled: February 8, 1990Date of Patent: October 15, 1991Assignee: A. H. Robins Company IncorporatedInventor: David A. Walsh
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Patent number: 5053504Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.Type: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 5039681Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: February 14, 1990Date of Patent: August 13, 1991Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5039673Abstract: Compounds are described of the formula (1) ##STR1## where: R.sup.1 is a hydrogen atom or a methyl group;X is cis or trans --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --, m is 2, 3 or 4 and n is 1; or X is trans --CH.dbd.CH--, m is zero and n is 3;Y is a saturated heterocyclic amino group;Alk is a C.sub.1-5 alkyl chain;l is zero or 1;p is zero, 1, 2, 3 or 4;R.sup.2 is a hydroxyl group or a group selected from --OCOR.sup.3, --CO.sub.2 R.sup.3, CONR.sup.3 R.sup.4, --SO.sub.2 NR.sup.3 R.sup.4, --NHCOR.sup.3, --NHSO.sub.2 R.sup.5, --SO.sub.2 R.sup.5, --SR.sup.5, --NR.sup.3 R.sup.4, --COR.sup.5, --NHCONR.sup.3 R.sup.4 and --NHCSNH.sub.2 ; and their physiologically acceptable salts, solvates and cyclodextrin complexes.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formulated for use as antithrombotic agents.Type: GrantFiled: August 22, 1989Date of Patent: August 13, 1991Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger Hayes, Keith Mills, David F. Woodings
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Patent number: 5039805Abstract: The compound of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the significance given in the description, can be used as medicaments for the therapy and prophylaxis of disorders such as thromboses, stroke, cardiac infarct, inflammations and arteriosclerosis as well as for the treatment of tumours.Type: GrantFiled: November 24, 1989Date of Patent: August 13, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Marcel Muller, Arnold Trzeciak, Thomas Weller
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Patent number: 5037837Abstract: Novel phenoxypropylamine derivative having the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom, a hydroxy group, a lower alkyl group or a lower alkoxy group, and R.sub.3 and R.sub.4 represent a lower alkyl group, or R.sub.3 and R.sub.4 taken together represent a group having the formula (CH.sub.2).sub.m wherein m represents 4 or 5, and n represents an integer of from 2 to 6 or a pharmaceutically acceptable salt thereof.The compounds are useful as a 5-lipoxygenase inhibitor and an antiulcer agent.Type: GrantFiled: November 1, 1990Date of Patent: August 6, 1991Assignee: Terumo Kabushiki KaishaInventors: Yoshiyuki Shikata, Ryoichi Nanba, Isamu Endo, Masashi Isozaki, Tadashi Okumura, Masazumi Miyakoshi, Shingo Koyama
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Patent number: 5036098Abstract: Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.Type: GrantFiled: September 14, 1989Date of Patent: July 30, 1991Assignee: Nippon Shinyaku Co., Ltd.Inventors: Kiyoshi Kimura, Masahiro Kise, Iwao Morita
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Patent number: 4983633Abstract: Amide-compounds represented by the formula (I): ##STR1## wherein R.sub.1 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino which can be substituted by lower alkyl, nitro, cyano, sulfamoyl which can be substituted by lower alkyl, R.sub.2 represents hydrogen, lower alkoxy, hydroxy, lower alkyl, halogen, amino, nitro, wherein R.sub.1 and R.sub.2 can be combined to form methylenedioxy, R.sub.3 means hydrogen, lower alkyl, halogen, or amino, R.sub.4 and R.sub.5 may be the same or different and each represents lower alkyl or wherein R.sub.4 and R.sub.Type: GrantFiled: September 2, 1988Date of Patent: January 8, 1991Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Itoh, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Hiroyuki Nishino, Jun Sakaguchi
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Patent number: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
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Patent number: 4952574Abstract: Certain 2,5-disubstituted N-(2-piperidylmethyl)benzamides, wherein one substituent is 2,2,2-trifluoroethyoxy, and pharmaceutically acceptable acid-addition salts thereof, are active as antiarrhythmic agents.Type: GrantFiled: September 26, 1988Date of Patent: August 28, 1990Assignee: Riker Laboratories, Inc.Inventor: Elden H. Banitt
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Patent number: 4948812Abstract: Compounds of formula ##STR1## (the substituents R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are explained in the specification) may be prepared by conventional methods.Owing to their favorable activity profile the compounds may advantageously be used to treat certain heart and circulatory disorders.Type: GrantFiled: November 25, 1987Date of Patent: August 14, 1990Assignee: Boehringer Ingelheim KGInventors: Herbert Koppe, Franz Esser, Walter Kobinge, Christian Lillie
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Patent number: 4942169Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2.] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: March 10, 1989Date of Patent: July 17, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 4908386Abstract: The present invention provides compounds of general formula (I) ##STR1## wherein Ar represents an unsubstituted or substituted phenyl gorup;R.sup.1 and R.sup.2 each represents a hydrogen atom or a C.sub.1-3 alkyl group;X represents a bond or a C.sub.1-7 alkylene, C.sub.2-7 alkenylene or C.sub.2-7 alkynylene chain;Y represents a bond or a C.sub.1-6 alkylene, C.sub.2-6 alkenylene or C.sub.2-6 alkynylene chain;Q represents a substituted phenyl or pyridyl ring;and physiologically acceptable salts and solvates thereof useful as stimulants of .sub.2 -adrenoreceptors and particularly in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: December 20, 1988Date of Patent: March 13, 1990Assignee: Glaxo Group LimitedInventors: Harry Finch, Lawrence H. C. Lunts, Alan Naylor, Ian F. Skidmore, Ian B. Campbell, David Middlemiss, Charles Willbe
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Patent number: 4897223Abstract: Color-forming agents of the general formula ##STR1## wherein X denotes hydroxyl, alkoxy, alkenyloxy, aralkoxy, cycloalkoxy, aryloxy, acyloxy, alkoxycarbonyloxy, alkylamino, dialkylamino, acylamino, aralkylamino or arylamino,Q denotes cyano, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, N-alkylcarbamoyl, N,N-dialkylcarbamoyl, N-alkyl-N-aryl-carbamoyl, acyl, alkoxysulphonyl, aralkoxysulphonyl, sulphamoyl, N-alkylsulphamoyl, N,N-dialkylsulphamoyl, alkylsulphonyl, arylsulphonyl or aralkylsulphonyl andR denotes alkyl, alkenyl or aralkyl,further isocyclic or heterocyclic rings can be fused on to the rings A, B, C and D, and the cyclic and acyclic radicals and the rings A, B, C and D can carry further substituents, are used for the preparation of pressure-sensitive recording materials.Type: GrantFiled: March 1, 1988Date of Patent: January 30, 1990Assignee: Bayer AktiengesellschaftInventors: Udo Eckstein, Hubertus Psaar, Roderich Raue
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Patent number: 4883815Abstract: Hydrocinnamic acid derivatives of the formula ##STR1## wherein one or two of the symbols R.sup.1 to R.sup.4 are halogen or methoxy and the others are hydrogen;R.sup.5 is hydrogen or phenyl;R.sup.6 is a residue of the formula ##STR2## R.sup.7 is (C.sub.1 -C.sub.4)-alkyl, (C.sub.2 -C.sub.5)-alkanoylamino-(C.sub.2 -C.sub.5)-alkyl, amino or (C.sub.1 -C.sub.4)-alkoxyphenyl;R.sup.8 and R.sup.9 each, independently, are hydrogen or (C.sub.1 -C.sub.4)-alkyl;R.sup.10 is hydrogen and R.sup.11 is hydroxy or R.sup.10 and R.sup.11 taken together are oxo;R.sup.12 is hydrogen, (C.sub.1 -C.sub.10)-alkyl, pyridylmethyl or carbamoylmethyl;R.sup.13 is hydrogen, (C.sub.1 -C.sub.4)-alkyl and R.sup.14 is hydrogen, (C.sub.1 -C.sub.4)-alkyl, pyridyl, phenyl-(C.sub.1 -C.sub.4)-alkyl, carboxy-(C.sub.1 -C.sub.4)-alkyl, carbamoyl-(C.sub.1 -C.sub.4)-alkyl, (C.sub.1 -C.sub.4)-alkoxy carbonyl-(C.sub.1 -C.sub.4)-alkyl, di-(C.sub.1 -C.sub.4)-alkoxy carbonyl-C.sub.2 -C.sub.5)-alky, piperidino-C.sub.2 -C.sub.Type: GrantFiled: July 5, 1988Date of Patent: November 28, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Werner Aschwenden, Rene Imhof, Roland Jakob-Roetne, Emilio Kyburz
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Patent number: 4849431Abstract: A novel piperidine derivative or a pharmacologically acceptable salt thereof is used in the treatment and prevention of dementias and sequelae of cerebrovascular diseases. These compounds also exhibit strong, highly selective anticholinesterase activity and may be orally or parenterally administered.Type: GrantFiled: December 24, 1986Date of Patent: July 18, 1989Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 4783537Abstract: Novel .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.-[hydroxy(aralkyl and cycloalkyl)]acetic acid derivatives and .alpha.-aryl-.alpha.-(.omega.-aminoalkyl)-.alpha.[alkanoyloxy(aralkyl and cycloalkyl)]acetic acid derivatives, such as N,N-dimethyl-2-(hydroxyphenylmethyl)-4-dimethylamino-2-phenylbutanamide, 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanenitrile, ethyl 2-(hydroxyphenylmethyl)-5-dimethylamino-2-phenylpentanoate, and N,N-dimethyl-2[(acetyloxy)phenylmethyl]-4-dimethylamino-2-phenylbutanamide , useful in the treatment of cardiovascular disease.Type: GrantFiled: November 13, 1985Date of Patent: November 8, 1988Assignee: Pennwalt CorporationInventor: Robert J. Murray
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Patent number: 4783535Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.Type: GrantFiled: March 18, 1986Date of Patent: November 8, 1988Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Albert D. Cale, Jr.
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Patent number: 4760146Abstract: Novel compounds and processes for making and using them. The compounds include ethyl 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxylate, 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxyamide, and N,N-dimethyl-1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxam ide.Type: GrantFiled: February 18, 1986Date of Patent: July 26, 1988Assignee: Pennwalt CorporationInventor: Bruce H. Toder
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Patent number: 4739106Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 19, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Nobuo Harada
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Patent number: 4735959Abstract: There are described novel carboxylic acid derivatives of the formula ##STR1## and derivatives of the formula ##STR2## and the addition salts thereof, which exhibit an effect on the intermediary metabolism. Furthermore, the compounds of Formula Ia as well as the compounds of Formula I possess blood-sugar lowering properties.Type: GrantFiled: May 14, 1985Date of Patent: April 5, 1988Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Gerhart Griss, Robert Sauter, Rudolf Hurnaus, Eckhard Rupprecht, Nikolaus Kaubisch, Joachim Kahling, Bernhard Eisele
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Patent number: 4686309Abstract: The invention provides compounds of formula: ##STR1## in which R=H, halogen, alkyl, alkyloxy, alkythio, NH.sub.2, alkylamino, dialkylamino or CF.sub.3, R.sub.3 =H or alkyl, either R.sub.4 and R.sub.5 =H and R.sub.1 and R.sub.2 =H or alkyl, optionally substituted by alkenyl (2 to 4 C) or alternatively R.sub.1 and R.sub.2 form together a saturated heterocyclic ring containing 4 to 7 ring members and optionally containing another heteroatom such as O, S or N optionally substituted by alkyl, or R.sub.4 =H, R.sub.1 =H or alkyl and R.sub.2 and R.sub.5 together form an alkylene (3 to 4 C) radical and (i) either A=alkyl or phenyl which is unsubstituted or substituted by one or two substituents chosen from halogen, alkyl, alkyloxy, alkylthio, NH.sub.2, alkylamino, dialkylamino, NO.sub.2 or CF.sub.3 or alternatively A=pyridyl, benzyl or cycloalkyl (3 to 6C), Y=S, SO or SO.sub.2 or a radical: ##STR2## in which R.sub.6 =H or alkyl and R.sub.Type: GrantFiled: February 15, 1985Date of Patent: August 11, 1987Assignee: Rhone-Poulenc SanteInventors: Jean-Claude Barriere, Jean-Pierre Corbet, Claude Cotrel, Daniel Farge, Jean-Marc Paris
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Patent number: 4675409Abstract: A new and novel process for the preparation of encainide (4-methoxy-2'-[2-(1-methyl-2-piperidyl)ethyl]-benzanilide) has been developed. The process utilizes .alpha.-picoline, O-nitrobenzaldehyde, and anisoyl chloride as starting materials.Type: GrantFiled: February 25, 1986Date of Patent: June 23, 1987Assignee: Bristol-Myers CompanyInventors: John L. Dillon, Richard H. Spector
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Patent number: 4673683Abstract: R.sup.2 and R.sup.3 are hydrogen or alkyl,R.sup.4 is hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, unsubstituted or substituted aralkyl, COR.sup.5, CO.sub.2 R.sup.6 or CONR.sup.7 R.sup.8,R.sup.5 and R.sup.6 are alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl,R.sup.7 and R.sup.8 are hydrogen, alkyl, unsubstituted or substituted aryl or unsubstituted or substituted aralkyl andn is 0, 1, 2 or 3,and its plant-tolerated acid addition salts, excluding the compounds where, simultaneously, R.sup.4 is hydrogen, acetyl or propionyl, n is 0 or 1 and R.sup.1, R.sup.2 and R.sup.3 are hydrogen, and fungicides containing the novel piperidines and salts.Type: GrantFiled: September 5, 1985Date of Patent: June 16, 1987Assignee: BASF AktiengesellschaftInventors: Ernst Buschmann, Ludwig Schuster, Norbert Goetz, Ernst-Heinrich Pommer, Eberhard Ammermann
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Patent number: 4663343Abstract: Substituted naphthalenyloxy- or naphthalenylthiooxyamides of trans-1,2-diaminocyclohexanes possess selective kappa opioid receptor site binding activity and are thus useful as analgesic or diuretic agents. Methods of preparing the compounds, pharmaceutical compositions, and a method for their use as analgesic agents are also disclosed.Type: GrantFiled: July 19, 1985Date of Patent: May 5, 1987Assignee: Warner-Lambert CompanyInventors: David C. Horwell, David Schofield
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Patent number: 4642379Abstract: This invention provides certain 4-acylamino benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.Type: GrantFiled: August 30, 1985Date of Patent: February 10, 1987Assignee: Eli Lilly and CompanyInventors: Edward E. Beedle, David W. Robertson
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Patent number: 4634713Abstract: Certain 3-(ureidocyclohexyleneamino)propane-1,2-diol derivatives, such as the compounds of formula III below, represent novel and useful pharmaceutical agents, e.g. potent antihypertensive and cardioactive agents demonstrating both .alpha.- and .beta.-adrenergic blocking activity. ##STR1## R.sub.3 is hydrogen or lower alkyl; R.sub.7 is cyano, lower alkoxycarbonyl, pyrrolyl, morpholino, alkenyloxy of 3 to 6 carbon atoms, alkynyloxy of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms substituted by cyclopropyl.Type: GrantFiled: August 19, 1985Date of Patent: January 6, 1987Assignee: Ciba-Geigy CorporationInventors: Lincoln H. Werner, Neville Ford
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Patent number: 4632935Abstract: OMEGA-(Hydroxy, ether and ester) alkyl-2-Amino-Cycloalkenyl and -cycloalkyl amide compounds of the formula: ##STR1## where the wavy line bonds, m, n, p, A, R, R.sub.1, R.sub.2, X, Y and Z are as defined in the specification, e.g., 3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)-3-(3-acetyloxypropyl)cyclohexe nyl]benzamide, and pharmacologically acceptable salts thereof, are useful as analgesic drug compounds having low physical dependence liability, compared to morphine and methadone. Pharmaceutical compositions and methods for using these compounds and compositions as analgesics are disclosed. Processes for preparing this class of compounds are also disclosed.Type: GrantFiled: May 30, 1984Date of Patent: December 30, 1986Assignee: The Upjohn CompanyInventor: Lester J. Kaplan
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Patent number: 4628095Abstract: The invention relates to compounds of the formula: ##STR1## which are useful cardiovascular agents.Type: GrantFiled: June 5, 1985Date of Patent: December 9, 1986Assignee: G. D. Searle & Co.Inventors: Kurt J. Rorig, Stevan W. Djuric, Kerry W. Fowler, Chi-Dean Liang
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Patent number: 4618680Abstract: 4-Hydroxy-3-methoxy-N-[2-[2-(1-methyl-2-piperidinyl)ethyl]-phenyl]benzamide is an antiarrhythmic agent having relatively low toxicity and increased duration of action.Type: GrantFiled: November 27, 1981Date of Patent: October 21, 1986Assignee: Mead Johnson & CompanyInventors: Robert F. Mayol, Richard E. Gammans