Ring Sulfur In The Polycyclo Ring System Patents (Class 514/324)
  • Patent number: 5439922
    Abstract: A method for treating anxiety in mammals comprising administering in an effective amount to said mammal an 1-aryl-3-(4-piperidyl)-indole derivative having the general formula: ##STR1## wherein R.sup.1 is H, F, Cl, Br, methyl, methoxy or cyano; and R.sup.3 is H or methyl; or a pharmaceutical acceptable acid addition salt thereof.
    Type: Grant
    Filed: December 17, 1992
    Date of Patent: August 8, 1995
    Assignee: H. Lundbeck A/S
    Inventors: Jens K. Perregaard, Brenda Costall
  • Patent number: 5438056
    Abstract: The compounds of the present invention have the following formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently phenyl, pyridyl, thienyl, naphthyl, substituted phenyl wherein the substituent is selected from the group consisting of halogen, methoxy, and dialkylamino wherein alkyl contains 1 to 3 carbon atoms; or R.sup.1 and R.sup.2 are independently substituted furanone of the structure ##STR2## wherein R.sup.5 and R.sup.6 are independently alkyl containing 1 to 3 carbon atoms, cycloalkyl containing 5 to 7 carbon atoms, phenyl or substituted phenyl wherein the substituent is alkyl containing 1 to 5 carbon atoms or halogen; R.sup.7 is hydrogen or halogen; or R.sup.1 and R.sup.2 are joined to form ##STR3## R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 4 to 20 branched, straight chain, cyclic, saturated or unsaturated carbon atoms; or R.sup.3 and R.sup.4 are joined to form ##STR4## wherein R.sup.
    Type: Grant
    Filed: October 5, 1993
    Date of Patent: August 1, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Kevin A. Memoli, Ivo Jirkovsky
  • Patent number: 5428043
    Abstract: Compounds of the formula ##STR1## wherein ring A, ring B, ring D, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6,R.sup.11, R.sup.12, R.sup.13, E, G, X and P are as defined below. The compounds of formula I are cholinesterase inhibitors and are useful in enhancing memory in patients suffering from dementia and Alzheimer's disease.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: June 27, 1995
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 5420132
    Abstract: A compound of formula (I): ##STR1## wherein: X represents O, S or H.sub.2,R and R' each represents hydrogen or together form a bond,R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.useful in the treatment or prevention of disorders involving oxidative processes.
    Type: Grant
    Filed: May 6, 1994
    Date of Patent: May 30, 1995
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Valerie Thiery, Gerard Adam, Jean-Guy Bizot-Espiard, Bruno Pfeiffer, Pierre Renard
  • Patent number: 5413997
    Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.
    Type: Grant
    Filed: January 21, 1993
    Date of Patent: May 9, 1995
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
  • Patent number: 5399360
    Abstract: A ketotifen pharmaceutical composition adapted for once-a-day oral administration e.g. based on a fat matrix.
    Type: Grant
    Filed: August 11, 1993
    Date of Patent: March 21, 1995
    Assignee: Sandoz Pharmaceuticals Corp.
    Inventors: Hansruedi Surer, Aldo Riva
  • Patent number: 5391557
    Abstract: A method of treating peri-menopasual syndrome comprising administering to a human in need of treatment an effective amount of a compound having the formula ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, --CH.sub.3, ##STR2## wherein Ar is optionally substituted phenyl; R.sup.2 is selected from the group consisting of pyrrolidine and piperidino; or a pharmaceutically acceptable salt of solvate thereof.
    Type: Grant
    Filed: October 15, 1993
    Date of Patent: February 21, 1995
    Assignee: Eli Lilly and Company
    Inventors: George J. Cullinan, John D. Termine
  • Patent number: 5385930
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, and medicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: January 14, 1994
    Date of Patent: January 31, 1995
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5376677
    Abstract: The invention relates to novel compounds of the formula ##STR1## in which R is as defined in the description, to their preparation, to fungicidal compositions which contain such compounds as active substances, and to the use of the active substances or compositions for controlling fungi in agriculture and horticulture.
    Type: Grant
    Filed: March 22, 1993
    Date of Patent: December 27, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: Stephan Trah
  • Patent number: 5371093
    Abstract: Piperidinyl thiacyclic derivatives ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are defined in the specification. useful in the treatment of allergic diseases and diseases responding to antagonism of 5HT.sub.2 receptors, pharmaceutical compositions and a methods of treatment using these compounds.
    Type: Grant
    Filed: February 24, 1994
    Date of Patent: December 6, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, George D. Maynard, John M. Kane, Hsien C. Cheng, Mark W. Dudley
  • Patent number: 5369105
    Abstract: Methods for using substituted phenoxy-, 1-, and 2-naphthalenyloxy-, indenyl-, indolyl-, benzo[b]furanyl-, and benzo[b]thienylcarboxamides of 7,8-(substituted-diamino)-1-oxaspiro[4.5]decanes as agents for alleviating the symptoms of Parkinson's disease, dystonia, and other movement disorders are disclosed. Pharmaceutical compositions employing the compounds are also disclosed.
    Type: Grant
    Filed: December 1, 1993
    Date of Patent: November 29, 1994
    Assignee: Warner-Lambert Company
    Inventors: Alexander McKnight, Geoffrey N. Woodruff
  • Patent number: 5356907
    Abstract: A compound selected from the group consisting of all possible racemic, enantiomeric and diastereoisomeric forms of a compound of the formula ##STR1## wherein E and G together form a group selected from the group: ##STR2## consisting of a) ##STR3## wherein, A is a cycloalkyl of 3-6 carbon optionally substituted, R, R.sub.1, R.sub.2 and Y are defined in the specification.
    Type: Grant
    Filed: October 1, 1992
    Date of Patent: October 18, 1994
    Assignee: Roussel UCLAF
    Inventors: Francois Clemence, Michel Fortin, Odile Le Martret
  • Patent number: 5346908
    Abstract: Certain nitrogen-containing cyclohetero cycloalkylaminoaryl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from hydrido, lower alkyl, benzyl, and haloloweralkyl; wherein each of R.sup.2, R.sup.3 and R.sup.8 through R.sup.11 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein n is an integer of from four to six; wherein m is an integer of from two to four; wherein A is selected from phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 25, 1992
    Date of Patent: September 13, 1994
    Assignees: National Institutes of Health, Brown University
    Inventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
  • Patent number: 5344835
    Abstract: According to the invention there is provided a compound of formula (I): R.sup.1 --O(CH.sub.2).sub.m A(CH.sub.2).sub.n XR or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is a group of formula (a or b) where Z is --(CH.sub.2).sub.2-, --CH.dbd.CH--, --CH.sub.2 --S-- or --CH.sub.2 --O--; R is a group of formula (c, d or Het) and A is a group of formula (e, f or g) in which the N atom is attached to the group (CH.sub.2)n; m is 1 or 2; n is an integer of from 1 to 4; p is 1, 2 or 3; R.sup.2 and R.sup.3 are each independently hydrogen, C.sub.1 -C.sub.4 alkyl, hydroxy-(C.sub.1 -C.sub.4 alkyl), hydroxy, C.sub.1 -C.sub.4 alkoxy, halo, trifluoromethyl, nitro, cyano, sulphamoyl, --CO(C.sub.1 -C.sub.4 alkyl), --OCO(C.sub.1 -C.sub.4 alkyl), carboxy, --CO.sub.2 (C.sub.1 -C.sub.4 alkyl), --CH.sub.2).sub.q CONR.sup.4 R.sup.5, -- (CH.sub.2).sub.q OCONR.sup.4 R.sup.5, --CH.sub.2).sub.q NR.sup.6 R.sup.7 or --NHSO.sub.2 NH.sub.2 in which R.sup.4 and R.sup.5 are each independently H or C.sub.1 -C.sub.
    Type: Grant
    Filed: July 2, 1992
    Date of Patent: September 6, 1994
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross
  • Patent number: 5338735
    Abstract: Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.The compounds are indicated for use in the treatment of disorders of the central nervous system.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: August 16, 1994
    Assignee: Lilly Industries Limited
    Inventors: John Fairhurst, David E. Tupper
  • Patent number: 5332741
    Abstract: The invention relates to compounds of the formula I: ##STR1## in which R.sub.1 is as defined in the description, their optical isomers and their addition salts with a pharmaceutically-acceptable acid or base, andmedicinal products which are useful for treating Central Nervous System disorders.
    Type: Grant
    Filed: May 17, 1993
    Date of Patent: July 26, 1994
    Assignee: Adir et Compagnie
    Inventors: Gerald Guillaumet, Gerard Coudert, Tchao Podona, Beatrice Guardiola-Lemaitre, Pierre Renard, Gerard Adam, Daniel Henri-Caignard
  • Patent number: 5322848
    Abstract: A compound, or solvate or salt thereof, of formula ##STR1## R.sub.1 is hydrogen, halogen, or C.sub.1-6 alkyl; R.sub.2 and R.sub.3 are hydrogen or C.sub.1-6 alkyl;R.sub.5 together with R.sub.4 forms a --(CH).sub.2).sub.2 -- group optionally substituted by one or two C.sub.1-6 alkyl;W is halogen or when A is gem-dimethyl substituted piperidine, is OH;a is 1 or 2,useful in the treatment of pain.
    Type: Grant
    Filed: May 22, 1992
    Date of Patent: June 21, 1994
    Assignee: Dr. Lo Zembeletti S.p.A.
    Inventors: Robert Colle, Giulio Dondio, Giuseppe Giardina, Lorenzo Leurini, Vittorio Vecchietti
  • Patent number: 5317020
    Abstract: Aromatic amine derivatives of the general formula (I) ##STR1## or salts of the derivatives with mineral or organic acids are useful as neurokinin receptor antagonists.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: May 31, 1994
    Assignee: Sanofi
    Inventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5306723
    Abstract: 5-(1-Hydroxy-2-piperidinopropyl)-2(1H,3H)-indolone derivatives and analogs; pharmaceutical compositions thereof; methods of treating CNS disorders therewith; and intermediates useful in the preparation of said compounds.
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: April 26, 1994
    Assignee: Pfizer Inc.
    Inventor: Bertrand L. Chenard
  • Patent number: 5286735
    Abstract: The application discloses pharmacologically-active derivatives of 4-aminomethyl piperidine having the general formula 1 ##STR1## wherein the symbols have the meanings set forth in the Specification, as well as pharmaceutically-acceptable acid addition salts thereof, the use of the compounds as serotoninergic receptor ligands and for the treatment of anxiety, depression, and other related serotoninergic system disorders, pharmaceutical compositions thereof, and a method for their preparation.
    Type: Grant
    Filed: September 14, 1992
    Date of Patent: February 15, 1994
    Assignee: Pierre Fabre Medicament
    Inventors: Bernard Bonnaud, Dennis Bigg
  • Patent number: 5280032
    Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.
    Type: Grant
    Filed: September 8, 1992
    Date of Patent: January 18, 1994
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
  • Patent number: 5278174
    Abstract: Sigma binding site agents having the formula ##STR1## which are useful to inhibit sigma binding site-induced activity, pharmaceutical compositions including these agents, and methods of using these agents to inhibit sigma binding site-induced activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented agents.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 11, 1994
    Assignee: Scios Nova, Inc.
    Inventors: Ronald H. Erickson, Kenneth J. Natalie, Jr., Michael J. Pontecorvo, Waclaw J. Rzeszotarski
  • Patent number: 5276053
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: January 4, 1994
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5264448
    Abstract: The present invention relates to certain novel amide compound represented by the formula of ##STR1## wherein A is an oxazole and, X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y, the ring B, R.sup.5, R.sup.6, l and m are the same as defined in the present specification, its production and an insecticidal and/or acaricidal composition containing it as an active ingredient.
    Type: Grant
    Filed: October 17, 1991
    Date of Patent: November 23, 1993
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Akira Shuto, Hirosi Kisida, Naoto Meki, Tomotoshi Imahase, Hiroaki Fujimoto, Kimitoshi Umeda
  • Patent number: 5256672
    Abstract: This invention relates to 6,7-dihydro-3-phenyl-1,2-benzisoxazol-4(5H)-ones and -ols of the formula ##STR1## wherein X is ##STR2## or loweralkyl; Y is hydrogen, halogen, loweralkyl, loweralkoxy, trifluoromethyl, nitro or amino; R is H when the bond between the oxygen atom and the carbon atom in question is a single bond; otherwise the dotted line signifies part of a double bond to the oxygen atom; R.sub.1 is hydrogen, loweralkyl or arylloweralkyl; R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl or arylloweralkyl, or R.sub.2 and R.sub.3 taken together with the nitrogen atom form an optionally substituted heterocycle selected from the group consisting of piperidinyl, pyrtolidinyl, morpholinyl, imidazol-1-yl, 1-piperazinyl, said substituents being hydrogen or loweralkyl; 4-substituted-1-piperazinyl of the formula where R.sub.
    Type: Grant
    Filed: December 13, 1992
    Date of Patent: October 26, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: David G. Wettlaufer, Gregory M. Shutske, Peter A. Nemoto
  • Patent number: 5248686
    Abstract: The invention relates to substituted arylamines and heteroarylamines, their preparation process and the pharmaceutical composition containing them. Said substituted amine is in accordance with the formula: ##STR1## in which R.sup.1 and R.sup.2 are optionally substituted alkyl radicals or form with N an optionally substituted piperazine or piperidine cycle, R.sup.3 and R.sup.4 represent a hydrogen atom or an organic radical, Y represents CR.sup.6 or N and R.sup.5 is an optionally substituted benzothiophenyl, benzofuranyl or naphthyl radical.These amines can be used in pharmaceutical compositions for the treatment of nervous depression or for stimulating vigilance.
    Type: Grant
    Filed: May 12, 1992
    Date of Patent: September 28, 1993
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Marc Kamenka, Alain Privat, Robert Chicheportiche, Jean Costentin
  • Patent number: 5244893
    Abstract: New compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.6 have the meanings given in the description, their preparation and use in plant protection, the protection of materials and in the field of human and veterinary medicine.Formula (I) gives a definition of the compounds which can be prepared by analogous processes, for example from suitable benzothiophene derivatives by oxidation.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: September 14, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Ludwig Elbe, Dieter Berg, Heinz-Wilhelm Dehne, Stefan Dutzmann, Georg-Wilhelm Ludwig, Manfred Plempel
  • Patent number: 5236921
    Abstract: The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group;or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.
    Type: Grant
    Filed: September 5, 1991
    Date of Patent: August 17, 1993
    Assignee: Sanofi
    Inventors: Xavier Emonds-Ai, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
  • Patent number: 5231104
    Abstract: A series of novel 1-(phenethyl) and 1-(2-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone.
    Type: Grant
    Filed: February 5, 1992
    Date of Patent: July 27, 1993
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross, Robert M. Wallis
  • Patent number: 5227388
    Abstract: Novel naphtho[2,3-b]thiophen-9(4H)-ones of the formula ##STR1## wherein R is loweralkyl or arylloweralkyl; X and Y are independently hydrogen, loweralkyl, halogen, loweralkoxy, or trifluoromethyl; W is CH.sub.2, CHOH, or C.dbd.O; n is 1 or 2; an optical isomer or pharmaceutically acceptable salt thereof, processes for the preparation thereof, and methods of alleviating pain utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: January 30, 1991
    Date of Patent: July 13, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Incorporated
    Inventors: Richard C. Effland, David G. Wettlaufer
  • Patent number: 5194440
    Abstract: A class of substituted cyclic sulphamide derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: February 20, 1992
    Date of Patent: March 16, 1993
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Jose L. C. Pineiro
  • Patent number: 5185335
    Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula ##STR2## wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula ##STR3## the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.
    Type: Grant
    Filed: February 4, 1991
    Date of Patent: February 9, 1993
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
  • Patent number: 5180736
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: May 17, 1991
    Date of Patent: January 19, 1993
    Assignee: Warner-Lambert Company
    Inventor: Graham Johnson
  • Patent number: 5179092
    Abstract: A compound having the formula (I): ##STR1## wherein A is --CH.sub.2 --, --O--, or --S--; R.sup.1 is CH.sub.3 or OCH.sub.3 ; R.sup.2 is hydroxy or carboxy which may be optionally esterized or amidated; R.sup.3 is H or a lower alkyl; and n is 0 or an integer of 1 to 6 or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: July 30, 1991
    Date of Patent: January 12, 1993
    Assignee: Suntory Limited
    Inventors: Toshio Tatsuoka, Kenji Suzuki, Fumio Satoh, Seiji Miyano, Kunihiro Sumoto
  • Patent number: 5169856
    Abstract: 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: Grant
    Filed: February 6, 1989
    Date of Patent: December 8, 1992
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Giichi Goto, Akinobu Nagaoka
  • Patent number: 5164391
    Abstract: The invention relates to a hydantoin derivative, salt thereof, process for the preparation thereof, and medicine containing the derivative. The derivative is represented by the formula ##STR1## wherein M is --CONH--NHR.sup.1 group, --CONH--OR.sup.2 group, ##STR2## in which R.sup.1 is hydrogen atom, an alkyl group, an alkenyl group, a phenyl radical, a substituted phenyl group, a naphthyl radical, a substituted naphthyl group, a pyridyl radical, a furyl radical or a thienyl radical, R.sup.2 is a hydrogen atom, an alkyl group, a phenyl radical or a substituted phenyl group, R.sup.3 and R.sup.4 are the same or different independently, each being a phenyl radical, or an aralkyl group, or R.sup.3 may form a substituted or non-substituted C.sub.5-6 saturated heterocyclic ring together with R.sup.4 and a possible nitrogen or oxygen atom, R.sup.5 forms a substituted or non-substituted saturated heterocyclic ring together with R.sup.6 and a possible nitrogen or oxygen atom, R.sup.
    Type: Grant
    Filed: September 13, 1990
    Date of Patent: November 17, 1992
    Assignee: Sanwa Kagaku Kenkyusho Co., Ltd.
    Inventors: Masayasu Kurono, Ryoichi Unno, Hiromoto Kimura, Noboru Tomiya, Kiichi Sawai, Kenji Miura, Toshinao Usui, Yasuaki Kondo, Yukiya Tanaka, Shigeyoshi Nakamura, Tsunemasa Suzuki, Motohide Hayashi
  • Patent number: 5143923
    Abstract: Novel benzisothiazole- and benzisoxazole-3-carboxamides, processes and intermediates for the preparation thereof, and methods of treating psychoses utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: April 29, 1991
    Date of Patent: September 1, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Nicholas J. Hrib, John G. Jurcak
  • Patent number: 5140034
    Abstract: A class of 5-membered heterocyclic compounds having at least one heteroatom, substituted on the heterocyclic ring by an imidazolyl moiety, are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania); anxiety; alcohol or drug withdrawal or dependence; pain; gastric stasis; gastric dysfunction (such as occurs with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence); migraine, nausea and vomiting; movement disorders; and presenile and senile dementia.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: August 18, 1992
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Christopher Swain, John Saunders
  • Patent number: 5128348
    Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: July 7, 1992
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Gregory S. Basarab
  • Patent number: 5126356
    Abstract: The compounds disclosed are 1-R'-4-RS-piperidines in which R' and R, which are different, may each represent: (1) (alkoxybenzyl)-alkyl or -alkenyl, or (2) (optionally-substituted chromanyl-, thiochromanyl-, chromenyl- or thiochromenyl)-alkyl or -alkenyl. The compounds are useful in the treatment of disorders associated with tissue ischaemia and of peripheral vascular disorders or in the treatment of disorders in which lipid peroxidation plays an initiating and/or aggravating role. A typical disclosed compound is: 4-(2,3,4-tirmethoxybenzylthio)-1-(3,5-di- tert-butyl-4-hydroxybenzyl)piperidine. ,3,4-trimethoxybenzylthio)-1-(3,5-di-tert-butyl-4-hydroxybenzyl)piperidine .
    Type: Grant
    Filed: December 11, 1990
    Date of Patent: June 30, 1992
    Assignee: Adir et Compagnie
    Inventors: Gilbert Regnier, J. F. Benaud De La Faverie, Alain Lombet, Jean-Pierre Iliou, Jean-Paul Vilaine, Jean-Pierre Bidouard, Albert Lenaers
  • Patent number: 5118680
    Abstract: A method of combating endoparasites in humans and animals which comprises administering to such humans and animals an endoparasiticidally effective amount of a 3-hydroxybenzothiophene of the formula ##STR1## in which X represents .dbd.CH-- or .dbd.N--,Y represents .dbd.O or .dbd.NH,R.sup.1 represents one or more identical or different radicals from the group consisting of hydrogen, alkyl, alkoxy, alkylthio, halogenoalkyl, halogenoalkoxy, halogenoalkylthio, alkylenedioxy, halogenoalkylenedioxy, halogen, CN, NO.sub.2, NH.sub.2, alkylamino, dialkylamino, alkylcarbonyl, carbalkoxy, alkylsulphonyl, arylsulphonyl, sulphamoyl, alkylsulphamoyl, dialkylsulphamoyl, aryl, aryloxy and arylthio, which, in turn, may again be substituted,R.sup.2 represents optionally substituted alkoxy, cycloalkoxy or the radical --NR.sup.3 R.sup.4,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents an alkyl or carbocyclic or heterocyclic armoatic radical or the radical --COOR.sup.5,R.sup.3 and R.sup.
    Type: Grant
    Filed: June 20, 1991
    Date of Patent: June 2, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Nikolaus Muller, Werner Hallenbach, Achim Harder, Werner Lindner
  • Patent number: 5114949
    Abstract: Compounds are disclosed of formula:R.sub.1 --(CH.sub.2).sub.n --Hetin which R.sub.1 represents a residue of formula ##STR1## X represents a hydrogen atom or an alkyl radical, Y represents a hydrogen atom or an alkyl or alkoxy radical,Z represents an alkyl radical,n is equal to 2 or 3,Het represents a substituted piperidino (substituted at the 4-position with a 1-indenylidene, 1-indenyl or 1-indanyl radical or with a chain --(CH.sub.2).sub.m --R.sub.2 or .dbd.CH--R.sub.2), substituted 1,2,3,6-tetrahydro-1-pyridyl (substituted at the 4-position with a chain --(CH.sub.2).sub.m --R.sub.2),m is equal to 1 or 2, andR.sub.2 represents an optionally substituted 2- or 3-indolyl radical, a 1- or 2-indanyl, 1- or 2-indenyl, an optionally substituted 1,2,3,4-tetrahydro-5H-pyrido[4,3-b]indol-2-yl radical, a 1,2,3,4-tetrahydro-3-quinolyl radical, an optionally substituted 1,2,3,4-tetrahydro-2-naphthyl radical or a 1-indolyl radical, their preparation and medicinal products containing them.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: May 19, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: Claude Gueremy, Jean-Luc Malleron, Serge Mignani
  • Patent number: 5100903
    Abstract: This invention pertains to novel N-aryl-N-[N-substituted 3-alkoxy-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts thereof, wherein:R is an aryl group selected from the group consisting of phenyl and substituted phenyl, wherein the substituents on the phenyl group are independently selected from the group consisting of halogen, lower-alkyl, lower-alkoxy, and combinations thereof;R.sub.1 is an alkyl group selected from the group consisting of lower-alkyl, lower-alkenyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms;R.sub.
    Type: Grant
    Filed: November 21, 1990
    Date of Patent: March 31, 1992
    Assignee: Anaquest, Inc.
    Inventors: Nhora L. Lalinde, John Moliterni, H. Kenneth Spencer
  • Patent number: 5098915
    Abstract: Substituted N-benzylpiperidine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compunds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.
    Type: Grant
    Filed: September 5, 1989
    Date of Patent: March 24, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Bipinchandra N. Desai, Kerry W. Fowler, Alan E. Moormann
  • Patent number: 5089507
    Abstract: A compound, or a solvate or salt thereof, of formula (I): ##STR1## in which: RCO is an acyl group in which the group R contains a substituted or unsubstituted carbocyclic aromatic or heterocyclic aromatic ring;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl or C.sub.4-12 cycloalkylalkyl groups, or together form a C.sub.2-8 branched or linear polymethylene or C.sub.2-6 alkenylene group, optionally substituted with a hetero-atom,R.sub.3 is hydrogen, C.sub.1-6 alkyl or phenyl, or R.sub.3 together with R.sub.1 form a --(CH.sub.2).sub.3 -- or --(CH.sub.2).sub.4 -- group;R.sub.4 and R.sub.5 are independently hydrogen, hydroxyl, halogen, C.sub.1-6 alkyl or aryl, provided both R.sub.4 and R.sub.5 are not simultaneously hydrogen; and p is an integer from 1 to 4,is useful for the treatment of pain or hyponatraemic disease states.
    Type: Grant
    Filed: September 25, 1989
    Date of Patent: February 18, 1992
    Assignee: Dr. L. Zambeletti SpA
    Inventors: Vittorio Vecchietti, Roberto Colle, Antonio Giordani, Giulio Dondio
  • Patent number: 5089505
    Abstract: A series of novel 1-(phenethyl) and 1-(1-heteroarylethyl)-3-substituted piperidine derivatives have been prepared, including their pharmaceutically acceptable salts and various novel key intermediates therefor. The 3-substituent present in these compounds is an unsubstituted or substituted diphenylmethoxy group or a diphenylmethoxy-derived group, while the 1-substituent is unsubstituted or substituted phenethyl or 1-(2-heteroarylethyl) wherein the heteroaryl moiety is thienyl, pyridyl or pyrazinyl. These compounds in the form of both their racemates and 3R-isomers, are useful in therapy as smooth muscle muscarinic receptor antagonists and therefore, are of value in the treatment diseases associated with altered motility and/or smooth muscle tone. The most preferred compound is (3R)-diphenylmethoxy-1-(3,4-methylenedioxyphenethyl)piperidine. Methods for preparing these compounds from known starting materials are provided.
    Type: Grant
    Filed: July 6, 1989
    Date of Patent: February 18, 1992
    Assignee: Pfizer Inc.
    Inventors: David Alker, Peter E. Cross, Robert M. Wallis
  • Patent number: 5075321
    Abstract: Clearance of antibody-coated cells from the circulation is modulated by administering an effective amount of certain benzothiophene derivatives, or the physiologically acceptable acid addition salts thereof. The compounds are useful in treating mammalian diseases characterized by interactions between IgG containing immune complexes and macrophage Fc receptors.
    Type: Grant
    Filed: February 24, 1988
    Date of Patent: December 24, 1991
    Assignee: University of Pennsylvania
    Inventor: Alan D. Schreiber
  • Patent number: 5071858
    Abstract: Disclosed are 3,4-dihydro-2H-1-benzothiopyran-3-yl-methyl- and ethylamines useful as antipsychotics, processes for the preparation of said compounds, pharmaceutical compositions containing same, and a method of treating psychotic disorders by administering said compounds.
    Type: Grant
    Filed: October 12, 1990
    Date of Patent: December 10, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Alan J. Hutchison
  • Patent number: 5071841
    Abstract: The present invention provides a sulfur-containing heterocyclic compound of the formula (I) ##STR1## wherein ring A is a benzene ring which may be substituted; R is a hydrogen atom or a hydrocarbon group which may be substituted; B is a carboxyl group which may be esterified or amidated; X is --CH(OH)-- or --CO--; k is 0 or 1; and k' is 0, 1 or 2 or a pharmaceutically acceptable salt thereof.Also, it provides a process for producing the compound (I) or a salt thereof and a pharmaceutical preparation for use in the treatment of osteoporosis comprising the compound (I) or salt thereof.The compounds (I) and salts thereof show excellent bone resorption inhibitory activity.
    Type: Grant
    Filed: December 28, 1989
    Date of Patent: December 10, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Takashi Sohda, Masao Tsuda, Iwao Yamazaki
  • Patent number: 5071853
    Abstract: A novel series of polycyclic amines, derivatives, methods of making the compounds, novel intermediates, compositions containing them, and methods for using them in the treatment and prevention of cerebrovascular disorders are disclosed.
    Type: Grant
    Filed: February 27, 1990
    Date of Patent: December 10, 1991
    Inventors: Christopher F. Bigge, Sheryl J. Hays, Graham Johnson, Perry M. Novak, Daniel F. Ortwine