The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/235)
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Patent number: 5317024Abstract: 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: August 3, 1993Date of Patent: May 31, 1994Assignee: DuPont Merck Pharmaceutical Co.Inventors: Gary A. Cain, Thomas E. Christos, Sang W. Tam
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Patent number: 5294623Abstract: Compounds of formula (I): ##STR1## in which: R.sup.1 and R.sup.2 are independently alkyl, alkoxy, trifluoromethyl, nitro or halogen; A is an aliphatic hydrocarbon group having from 2 to 8 carbon atoms whose chain contains at least 2 carbon atoms in a linear chain between the piperidine group and --COOH, said group optionally being unsaturated; and m and n are independently 0, 1, 2 or 3; and pharmaceutically acceptable salts and esters thereof have been found to have valuable anti-histamine properties without the usual side effects of anti-histamines. Methods of preparing the compounds are also provided.Type: GrantFiled: December 22, 1992Date of Patent: March 15, 1994Assignee: Sankyo Company, LimitedInventors: Hiroshi Fukumi, Toshiaki Sakamoto, Mitsuo Sugiyama, Yoshio Iizuka, Takeshi Yamaguchi
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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: 5246946Abstract: A piperidine compound has the generic formula and is useful to treat arrhythmia. ##STR1## in which R1 is a lower alkyl and W is: ##STR2## X is --S--, --SO-- or --SO2--, R2 is hydrogen or --(CH2)n--Y, n is an integer of 1 to 5, Y is an aryl, pyridyl or a substituted pyridyl, X' is --CO-- or --CH(OH)--,p is an integer of 1 to 4, R12 is hydrogen or a lower alkyl, Y' is --(CH2)m--A, m is 1 or 2, A is an aryl, a substituted aryl, pyridyl or a substituted pyridyl, R12 and Y may form a 5- or 6-membered ring or a 5- or 6-membered ring having one or more substituents andR22 is hydrogen, a halogen, a lower alkyl, a lower alkoxy or hydroxy.Type: GrantFiled: August 14, 1992Date of Patent: September 21, 1993Assignee: 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: 5206373Abstract: The invention is a highly efficient synthesis for making compounds of the formula: ##STR1## wherein: R.sup.1 is a six member saturated or unsaturated heterocyclic ring containing one or two heterocyclic atoms wherein the heteroatoms are N; or NR.sup.6, wherein R.sup.6 is H or C.sub.1-10 alkyl;m is an integer from two to six; andR.sup.4 is aryl, C.sub.1-10 alkyl, or C.sub.4-10 aralkyl.Type: GrantFiled: February 28, 1992Date of Patent: April 27, 1993Assignee: Merck & Co., Inc.Inventors: John Y. L. Chung, David L. Hughes, Dalian Zhao
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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: 5159081Abstract: Intermediates of N-carbonyl-3,4,4-substituted piperidines are provided which are useful in the preparation of peripheral opioid antagonists.Type: GrantFiled: March 29, 1991Date of Patent: October 27, 1992Assignee: Eli Lilly and CompanyInventors: Buddy E. Cantrell, Dennis M. Zimmerman
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Patent number: 5128349Abstract: The present invention relates to 1-(4-aminophenyl)-2-piperidinopropanone derivatives which are selected from(a) the compounds corresponding to the general formula ##STR1## where R is H or CH.sub.3 CO, A is H or Cl, B is H or Cl and Z is C.sub.1 -C.sub.4 -alkyl; and(b) their addition salts,These products are used as cardiovascular agents. In particular, the compounds of the formula I where R=H or CH.sub.3 CO, A=B=Cl and Z=CH.sub.3, and their addition salts, are especially very worthwhile as vasodilators.Type: GrantFiled: October 29, 1990Date of Patent: July 7, 1992Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 5104872Abstract: Compound of the general formula (I), which is useful as an agricultural and horticultural fungicide, an agricultural and horticultural fungicidal composition containing said compound, use of said composition for controlling plant disease, and process for the production of said compound: ##STR1## wherein ##STR2## shows a case in which R.sup.3 and R.sup.4 together form a cyclic substituent, and R.sup.1 and R.sup.4 are substituents disclosed in the specification.Type: GrantFiled: August 15, 1990Date of Patent: April 14, 1992Assignee: Nihon Hohyaku Co., Ltd.Inventors: Kenji Tsubata, Nobuyuki Niino, Katsutoshi Endo, Yoshinobu Yamamoto, Hideo Kanno
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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: 5081254Abstract: A novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections.Type: GrantFiled: June 15, 1990Date of Patent: January 14, 1992Assignee: Warner-Lambert CompanyInventors: Townley P. Culbertson, John M. Domagala, Susan E. Hagen, Joseph P. Sanchez
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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: 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: 4980377Abstract: The present invention relates to the preparation of new 1-(aminophenyl)-2-aminopropanone derivatives of the general formula: ##STR1## in which X is NH.sub.2, Y is H or a halogen atom, Z is H or a halogen atom, R.sub.1 is C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.6 cycloalkyl and R.sub.2 is H or C.sub.1 -C.sub.4 alkyl, or R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, a heterocyclic group selected from the group consisting of the pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methyl-piperazino, 4-(.beta.-hydroxyethyl)piperzaino, 4-phenylpiperazino and 4-(p-chlorophenyl)piperazino groups, and addition salts thereof.These new derivatives are useful as pharmaceuticals. They are obtained by deacetylation of the corresponding acetylated products.Type: GrantFiled: November 14, 1988Date of Patent: December 25, 1990Assignee: Laboratoire L. LafonInventor: Louis Lafon
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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: 4933367Abstract: This invention relates to carboxylic acid derivatives and their use thereof. The compounds are useful in treatment of various diseases such as diabetes, prediabetic conditions, adipositas ailments or atherosclerosis.Type: GrantFiled: March 12, 1987Date of Patent: June 12, 1990Assignee: Boehringer Mannheim GmbHInventors: Hans P. Wolff, Ernst-Christian Witte, Hans-Frieder Kuhnle
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Patent number: 4931581Abstract: A method and composition for the immunization of healthy useful plants against plant diseases containing as active ingredients compounds of formula ##STR1## in which: X is hydrogen, halogen, hydroxy, methyl, methoxy, HOOC or MOOC;Y is hydrogen, halogen, SO.sub.3 H, SO.sub.3 M, nitro, hydroxy or amino, M being the molar equivalent of an alkali metal or alkaline earth metal ion that is formed from a corresponding base or basic compound; andZ is cyano or --CO--A;A represents either --OH or --SH, the hydrogen atom of which may also be replaced by the molar equivalent of an inorganic or organic cationic residue,or wherein A represents any other organic residue which has a molecular weight of less than 900 and which may also contain one, or more than one, hetero atom, including the salts of the phytophysiologically tolerable 7-carboxylic acid or 7-thiocarboxylic acid with primary, secondary or tertiary amines or with inorganic bases.Type: GrantFiled: August 18, 1988Date of Patent: June 5, 1990Assignee: Ciba-Geigy CorporationInventors: Rolf Schurter, Walter Kunz, Robert Nyfeler
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Patent number: 4929613Abstract: The novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections.Type: GrantFiled: July 25, 1988Date of Patent: May 29, 1990Assignee: Warner-Lambert CompanyInventors: Townley P. Culbertson, John M. Domagala, Susan E. Hagen, Joseph P. Sanchez
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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: 4906634Abstract: Novel N-[4-(aminosubstituted)phenyl]methanesulfonamides and their use as cardiovascular agents, especially as antiarrhythmic agents are described. Pharmaceutical formulations containing such compounds are also discussed.Type: GrantFiled: March 8, 1988Date of Patent: March 6, 1990Assignee: Schering A.G.Inventors: Stanley S. Greenberg, William C. Lumma, Jr., Klaus Nickisch, Ronald A. Wohl
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Patent number: 4902334Abstract: A plant metabolism regulating agent comprising as an active ingredient an alpha,beta or beta,gamma-un-saturated carboxylic acid or its derivative. It is useful for controlling the metabolism of a plant, facilitating the growth of a beneficial plant such as cereals by inhibiting the growth of undesirable plants or eradicating them, regulating the growth of a plant and dwarfing a plant.Type: GrantFiled: October 31, 1984Date of Patent: February 20, 1990Assignee: Teijin LimitedInventors: Shizuo Azuma, Toshiyuki Hiramatsu, Teizo Yamaji, Yataro Ichikawa
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Patent number: 4898977Abstract: The invention relates to novel processes and intermediates for the preparation of 5-amino-4-hydroxyvaleric acid derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl or the radical of a natural amino acid, R.sup.2 represents hydrogen, optionally substituted alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl, aryl-lower alkyl, amino, hydroxy, mercapto, sulphinyl, sulphonyl or the radical of a natural amino acid, and R.sup.3 represents optionally substituted hydroxy or amino, by sigmatropic rearrangement of a suitable allyl ester, halolactonisation of the resulting .gamma.,.delta.-unsaturated acid or of a suitable derivative thereof, exchange of halogen for a nitrogen-containing nucleophile, opening of the lactone ring and freeing of the amino group. Compounds of the formula I are starting materials for the preparation of renin-inhibitors which have an anti-hypertensive action.Type: GrantFiled: August 13, 1987Date of Patent: February 6, 1990Assignee: Ciba-Geigy CorporationInventors: Peter Herold, Christof Angst
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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: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4877812Abstract: The present invention relates, by way of new industrial products, to 1-(acetylaminophenyl)-2-amino-propanone derivatives selected from the group consisting of(a) the compounds of the formulaAr--CO--CH(CH.sub.3)--NR.sub.1 R.sub.2 (I)in whichR.sub.1 represents a C.sub.1 -C.sub.4 alkyl group or a C.sub.3 -C.sub.6 cycloalkyl group;R.sub.2 represents the hydrogen atom or a C.sub.1 -C.sub.4 alkyl group;R.sub.1 and R.sub.2, taken together, can form, with the nitrogen atom to which they are bonded, an N-heterocyclic group with 5 to 7 ring members, capable (i) of including a second heteroatom selected from N, O and S, and (ii) of being substituted, the said heterocyclic group NR.sub.1 R.sub.2 being selected from the group comprising pyrrolidino, morpholino, thiomorpholino, piperidino, hexamethyleneimino, piperazino, 4-methylpiperazino, 4-(.beta.-hydroxyethyl) piperazino, 4-phenylpiperazino and 4-(p-chlorophenyl)-piperazino groups; andAr represents an acetylaminophenyl group of the formula ##STR1## in which X is CH.Type: GrantFiled: April 16, 1987Date of Patent: October 31, 1989Assignee: Laboratoire L. LafonInventor: Louis Lafon
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Patent number: 4876262Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R1 is a lower alkyl or a tolyl, R2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH2-- 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, --CH2COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## 1 being 1 or 2, --A--B, A being --(CH2)n--, n being an integer of 1 to 5, a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalent group derived from a straight-chain alkane having lower alkyl, phenyl or hydroxyl group(s) bonded directly to one or more carbon atoms constituting said alkane by removing a hydrogen atom bonded to each of the carbon atoms placed at both ends thereof,a straight-chain alkylene group having 1 to 5 carbon atoms which is a divalentType: GrantFiled: February 18, 1987Date of Patent: October 24, 1989Assignee: 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: 4835277Abstract: In one embodiment this invention provides a nonlinear optical medium whcih is a transparent film of a thermoplastic polymer composed of recurring monomeric units corresponding to the formula: ##STR1##Type: GrantFiled: October 5, 1987Date of Patent: May 30, 1989Assignee: Hoechst Celanese CorporationInventor: Eui W. Choe
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Patent number: 4731369Abstract: Amides and esters of 2-[N-(hydroxypiperidinoalkyl) and (hydroxypyrrolidinoalkyl) aminosulfonyl]-6-nitrobenzoic acids are disclosed to have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds, pharmaceutical compositions including such compounds and methods of treating patients in need of therapeutic radiation with effective amounts of such compounds.Type: GrantFiled: June 26, 1987Date of Patent: March 15, 1988Assignee: Merck & Co. Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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Patent number: 4694020Abstract: Derivatives of 2-(substituted sulfamyl) 6-nitrobenzoic acids are disclosed, wherein at least one of the sulfamyl substituents is selected from amino-(lower alkyl), (lower alkyl)-amino-(lower alkyl), or di(lower alkyl)-amino-(lower alkyl), hydrogen, lower alkyl, hydroxy-(lower alkyl), allyl, or when taken together with the nitrogen of the sulfamyl moiety, form a heterocyclic ring. These compounds have activity in increasing the sensitivity of hypoxic tumor cells to therapeutic radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.Type: GrantFiled: October 21, 1986Date of Patent: September 15, 1987Assignee: Merck & Co., Inc.Inventors: Edward L. Engelhardt, Walfred S. Saari
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Patent number: 4680402Abstract: Intermediate products usable in particular for preparing corresponding amino derivatives by converting their nitro function, said products being of formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent an atom of hydrogen, a halogen, a lower alkyl group or a lower alkoxy group;R.sub.5 and R.sub.6, which are identical or different, each represent an atom of hydrogen, a lower alkyl group, an OH group, a phenyl group or a benzyl group.Type: GrantFiled: May 30, 1986Date of Patent: July 14, 1987Assignee: Societe de Recherches Industrielles (S.O.R.I.)Inventors: Bernard Majoie, Francois Bellamy, Pierre Dodey, Jacques Robin
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Patent number: 4673747Abstract: Substituted aminoalkylphenoxy derivatives represented by the general formula of: ##STR1## wherein the substituting group Z is either one of the following groups of: ##STR2## were prepared. These derivatives exert antagonism against Histamine H.sub.2 -receptors and hence are efficacious for the treatments of digestive ulcers.Type: GrantFiled: December 3, 1985Date of Patent: June 16, 1987Assignee: Ikeda Mohando Co., Ltd.Inventors: Fujio Nohara, Tomoaki Fujinawa
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Patent number: 4652679Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.Type: GrantFiled: May 9, 1983Date of Patent: March 24, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4640925Abstract: Novel chemical compounds which are diphenylmethylene piperidine compounds are provided, as well as methods for their production, pharmaceutical compositions comprising the compounds, and methods of treatment using the compounds in dosage form. The compounds have pharmacological properties especially anticholinergic properties, and are useful as antiemetic, antihistamine, pulmonary, antiallergy, and antispasmodic agents.Type: GrantFiled: February 11, 1986Date of Patent: February 3, 1987Assignee: Warner-Lambert CompanyInventors: David A. Downs, Haile Tecle
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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: 4595757Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is ##STR2## wherein B is a moiety having the formula ##STR3## R is H, mono- or dihalo, amino, nitro, cyano, hydroxy, trifuoromethyl, mercapto, lower alkyl, lower alkoxy, alkanoyl, lowercycloalkyl, carboxy, alkoxycarbonyl, mono- or di-lower alkyl substituted amino, alkanoylamino, lower alkyl thio, loweralkylsulfonyl, sulfamoyl, lower alkyl substituted sulfamoyl, phenyl or phenyl substituted with halo, lower alkyl, lower alkoxy, trifluoromethyl, hydroxy, amino, cyano or nitro;X is SO.sub.2, SO, S or C.dbd.O; andR.sup.2 is phenyl or 1,3-benzodioxol-5-yl;and the pharmacologically acceptable salts thereof, which are (H.sup.+ +K.sup.+)ATPase inhibitors exhibiting a cytoprotective action, are useful in the treatment of conditions where there is hypersecretion of gastric acid, such as gastric and peptic ulceration, as well as in conditions such as stress ulceration.Type: GrantFiled: December 13, 1984Date of Patent: June 17, 1986Assignee: American Home Products CorporationInventors: Guy A. Schiehser, Susan T. Nielsen, Donald P. Strike
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Patent number: 4537698Abstract: New piperidine derivatives ##STR1## in which R.sup.1 and R.sup.2 each independently is alkyl or alkoxy each of 1 to 10 C atoms, --Y--Z, F, Cl, Br or CN, and the radical R.sup.1 can also be H,Y is --CO--O--, --O--CO or a single bond,Z is --Q--R.sup.3 or alkyl having 1-10 C atoms,Q is 1,4-phenylene or 1,4-cyclohexylene,R.sup.3 is alkyl having 1-10 C atoms, F or CN, andA is 1,4-cyclohexylene or 1,3-dioxane-2,5-diyl, and their acid addition salts,can be used as components of dielectrics for electro-optical display elements.Type: GrantFiled: May 31, 1983Date of Patent: August 27, 1985Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Wolfgang Sucrow, Wolfgang Schatull, Peter Fuss
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Patent number: 4529732Abstract: 2-[2-Hydroxy-4-(substituted)phenyl]piperidines and derivatives thereof of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sub.1 is H, benzyl or certain acyl groups, R.sub.2 is H, certain alkyl, alkenyl, alkynyl, hydroxyalkyl, acyl or alkylsulfonyl groups; R.sub.3 is H.sub.2, O, ##STR2## and Z is (C.sub.1 -C.sub.13)alkylene or -(alk.sub.1).sub.m -O-(alk.sub.2).sub.n - where each of (alk.sub.1) and (alk.sub.2) is (C.sub.1 -C.sub.13)alkylene, provided that the number of carbon atoms in (alk.sub.1) plus (alk.sub.2) is not greater than 13; each of m and n is 0 or 1; and W is H, pyridyl or optionally substituted phenyl; their use as analgesic agents, intermediates therefor and processes for their preparation.Type: GrantFiled: March 14, 1983Date of Patent: July 16, 1985Assignee: Pfizer Inc.Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4528294Abstract: The present invention relates to new benzoyl-phenyl-piperidine derivatives selected from the group consisting of:(i) 2-piperidinobenzophenones of the general formula: ##STR1## in which: R.sub.1, R.sub.2 and R.sub.3, which are identical or different, each represent an atom of hydrogen, a hydroxy group, CF.sub.3, a halogen, a lower alkyl group or a lower alkoxy group;R.sub.4 represents an atom of hydrogen, a halogen, an NO.sub.2 group, an NR'R" group [where R' and R", which are identical or different, represent an atom of hydrogen, a lower alkyl group or a CO.sub.2 R group (where R represents a lower alkyl group or a benzyl group)];R.sub.5 and R.sub.6, which are identical or different, each represent an atom of hydrogen, a C.sub.1 -C.sub.4 -alkyl group, an OH group, a phenyl group or a benzyl group; and(ii) acid addition salts thereof.The invention also relates to the method for preparing these new derivatives and to their use in therapeutics, particularly as immunostimulant and immunoadjuvant agents.Type: GrantFiled: June 24, 1982Date of Patent: July 9, 1985Assignee: Societe de Recherches Industrielle S.O.R.I.Inventors: Bernard Majoie, Francois Bellamy, Pierre Dodey, Jacques Robin
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Patent number: 4528376Abstract: Novel 3-(4-piperidyl)-1,2-benzisoxazoles, intermediates and processes for the preparation thereof, and methods for alleviating pain utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: May 9, 1983Date of Patent: July 9, 1985Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Beth A. Gardner, Richard C. Allen
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Patent number: 4526973Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones of the general formula ##STR1## are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers. A preferred compound, 1-amino-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dione, is prepared by treating an intermediate, 1-methoxy-2-[3-(3-piperidinomethylphenoxy)propylamino]cyclobutene-3,4-dion e, with ammonia.Type: GrantFiled: June 9, 1982Date of Patent: July 2, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4522943Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: April 21, 1982Date of Patent: June 11, 1985Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4495350Abstract: Herbicidally effective aminoalkyl esters of 2-nitro-5-(o-chloro-p-trifluoromethylphenoxy)-benzoic acid, and acid addition salts and quaternary ammonium salts thereof, are suitable for the selective control of weeds in crops of useful plants, for example soya bean and rice crops.The aminoalkyl esters correspond to the formula ##STR1## wherein A is a C.sub.2 -C.sub.4 -alkylene bridge or the direct bond, and ##STR2## is an open amino group, and ##STR3## is a cyclic amino group.Type: GrantFiled: September 13, 1982Date of Patent: January 22, 1985Assignee: Ciba-Geigy CorporationInventors: Dieter Durr, Otto Rohr, Beat Bohner
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Patent number: 4483986Abstract: A compound of the formula I ##STR1## and other compounds and process for preparing, which compounds are useful as intermediates.Type: GrantFiled: May 3, 1982Date of Patent: November 20, 1984Assignee: Eli Lilly and CompanyInventor: Samuel J. Dominianni
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4481315Abstract: Compounds which contain, in their molecule, at least one 2-(2'-hydroxyphenyl)-benztriazole group or one 2-hydroxybenzophenone group and at least one polyalkylpiperidine group are effective light stabilizers for organic materials, in particular for polymers. The use of the compounds as light stabilizers for lacquers is of particular importance.Type: GrantFiled: February 28, 1983Date of Patent: November 6, 1984Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Mario Slongo
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Patent number: 4474810Abstract: Arylglyoxals which are new compounds, active as hypoglycemic agents.Type: GrantFiled: January 27, 1983Date of Patent: October 2, 1984Assignee: American Cyanamid CompanyInventors: Middleton B. Floyd, Jr., Vern G. DeVries
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Patent number: 4448986Abstract: (1R,cis)-Oxyimino-substituted cyclopropanecarboxylic acids are prepared via a (1R,4R,5S)-2-acetoxy-6,6-dimethyl-4-oxo-3-oxabicyclo[3.1.0]hexane intermediate.Type: GrantFiled: July 14, 1982Date of Patent: May 15, 1984Assignee: Shell Oil CompanyInventor: Steven A. Roman
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Patent number: 4447368Abstract: Aromatic aminosulphonic acids which have a reduced content of discoloring by-products are obtained when aromatic amines are reacted with a sulphonating agent in a reaction medium at least some of which consists of tetramethylene sulphone.Type: GrantFiled: March 31, 1982Date of Patent: May 8, 1984Assignee: Siemens-Allis, Inc.Inventors: Herbert Emde, Heinz U. Blank, Peter Schnegg
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Patent number: 4447428Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH--or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: July 15, 1983Date of Patent: May 8, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton