Two Of The Cyclos Share At Least Three Ring Carbons (i.e., Bridged) (e.g., Benzomorphans, Etc.) Patents (Class 514/295)
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Patent number: 5547960Abstract: The present invention provides C.sup.10 -mono- and disubstituted analogs of huperzine A which are active as acetylcholinesterase inhibitors, as well as intermediates for the preparation thereof.Type: GrantFiled: September 7, 1994Date of Patent: August 20, 1996Assignee: Mayo Foundation for Medical Education and ResearchInventors: Alan P. Kozikowski, Werner T uckmantel
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Patent number: 5446049Abstract: This invention relates to methods of treating conditions responsive to 5-HT.sub.4 agonists and/or antagonists and 5-HT.sub.3 antagonists by administering compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;n is 0, 1 or 2;m is 0 or 1;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.Type: GrantFiled: June 22, 1994Date of Patent: August 29, 1995Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Alan E. Moormann
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Patent number: 5354758Abstract: Compounds of the formula I ##STR1## are disclosed. In this formula, R is a member selected from the group consisting of --CR.sub.1 R.sub.2 R.sub.3, hydroxy, an alkoxy group having 1 to 4 carbon atoms and --NR.sub.4 R.sub.5, in which at most one of R.sub.1, R.sub.2 and R.sub.3 is hydrogen and the remainder are each independently selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, a cycloalkylalkyl having 4 to 9 carbon atoms and a 3 to 6 membered cyclic ether; R.sub.4 and R.sub.5 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; R.sub.6 and R.sub.7 are each independently hydrogen or an alkyl group having 1 to 4 carbon atoms; and R.sub.8 is hydrogen, an alkyl group having 1 to 4 carbon atoms, hydroxy, an alkoxy group having 1 to 4 carbon atoms or halogen. Salts of these compounds are also disclosed.Type: GrantFiled: December 16, 1992Date of Patent: October 11, 1994Assignee: Japan Tobacco Inc.Inventors: John A. Lawson, Itsuo Uchida
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Patent number: 5350756Abstract: This invention discloses a method for increasing the effectiveness of dextromethorphan (DM) as an antitussive agent (i.e., as a cough suppressant). This method involves the concurrent administration of DM and a second agent which inhibits the oxidative activity of debrisoquin hydroxylase, a cytochrome P450 oxidase enzyme. Effective anti-oxidant compounds include quinidine, yohimbine, and fluoxetine.Type: GrantFiled: May 28, 1992Date of Patent: September 27, 1994Inventor: Richard A. Smith
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Patent number: 5284854Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.Type: GrantFiled: June 24, 1993Date of Patent: February 8, 1994Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk, Jozef M. Boey
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Patent number: 5246940Abstract: This invention relates to novel N-biphenylyl lactam compounds having a substituted methylidene or methyl moiety adjacent to the lactam nitrogen, and pharmaceutically acceptable salts thereof.The compounds are angiotensin II receptor antagonists, and are useful in treating hypertension (lowering high blood pressure), congestive heart failure, elevated ocular pressure, cerebral stroke, angina, cardiac insufficiency, myocardial infarction or diabetic nephropathy.The invention also relates to a pharmaceutical composition comprising a compound of the invention, a method of treating a physiological condition in a mammal that is mediated by angiotensin II which comprises administering to the mammal an effective amount of a compound of the invention, and novel processes for preparing the compounds of the invention.Type: GrantFiled: January 21, 1993Date of Patent: September 21, 1993Assignee: Ortho Pharmaceutical CorporationInventors: William V. Murray, Michael P. Wachter
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Patent number: 5240935Abstract: Novel substituted 2-azabicyclo[2.2.2]octane derivatives, pharmaceutical compositions containing them, methods for treating central nervous system disorders utilizing them, and processes for synthesizing them.Type: GrantFiled: November 20, 1992Date of Patent: August 31, 1993Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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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: 5179093Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.Type: GrantFiled: May 10, 1991Date of Patent: January 12, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Stuart W. McCombie, Jay Weinstein
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Patent number: 5177082Abstract: The invention relates to compounds of the formulas ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 independently are hydrogen or lower alkyl, and the dotted ( . . . ) line is an optional double bond, and their pharmaceutically acceptable acid addition salts. The compounds of formulas I, II and III possess marked anticholinesterase activity and are useful as analeptic agents and as agents for the treatment of senile dementia and myasthenia gravis.Type: GrantFiled: October 18, 1990Date of Patent: January 5, 1993Inventors: Chao-mei Yu, Xi-can Tang, Jia-sen Liu, Yan-yi Han
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Patent number: 5164398Abstract: This invention relates to pharmaceutical compositions for use in the treatment of pain and inflammation and the relief of cough and cold symptoms in a mammalian organism, said composition comprising:(i) an analgesically and anti-inflammatory effective amount of (S)-ibuprofen, or a salt thereof, substantially free of (R)-ibuprofen; and(ii) an antitussively effective amount of at least one antitussive agent selected from codeine, hydrocodone, caramiphen, carbetapentane, or dextromethorphan, or a therapeutically active stereoisomer thereof substantially free of its other stereoisomers and optionallyiii) a therapeutically effective amount of at least one expectorant selected from guaicolsulfonate, guaifenesin, guaiacol, or terpin;or a pharamceutically acceptable salt thereof.Type: GrantFiled: April 1, 1991Date of Patent: November 17, 1992Assignees: Merck & Co., Inc., McNeil-PPC, Inc.Inventors: Robert T. Sims, William Slivka
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Patent number: 5122528Abstract: Pyrrolidinyl derivatives of Benzofuran-7-carboximides with analgesic activity".Type: GrantFiled: April 5, 1991Date of Patent: June 16, 1992Assignee: Erbamont, Inc.Inventor: Anthony R. Imondi
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Patent number: 5104880Abstract: An acetylcholinesterase inhibitor is provided of the general formula (I): ##STR1## wherein R.sub.1 is H, (C.sub.1 -C.sub.8)alkyl or halo; R.sub.2 is H or (C.sub.1 -C.sub.8)alkyl; R.sub.3 and R.sub.4 are individually H, (C.sub.1 -C.sub.8)alkyl, NO.sub.2, hydroxy or halo; R.sub.5 and R.sub.6 are individually H, (C.sub.1 -C.sub.8)akyl, aryl or aralkyl; R.sub.7 is H, halo or (C.sub.1 -C.sub.8)alkyl, R.sub.8 is halo or (C.sub.1 -C.sub.8)alkyl; R.sub.9 is absent or is H; and the bonds represented by--are individually absent or, together with the adjacent bond, form the unit C.dbd.C, with the proviso that if both of the bonds represented by--are present, R.sub.3 and R.sub.4 cannot both be H unless R.sub.7 or R.sub.8 is halo; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: May 1, 1991Date of Patent: April 14, 1992Assignee: Mayo Foundation for Medical Education and ResearchInventor: Alan P. Kozikowski
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Patent number: 4910193Abstract: Use of a mono or dicyclic carboxylic or heterocyclic carboxylic acid ester or amide of an alcohol or amine nitrogen as a ring atom in free base form or in acid addition or quaternary ammonium salt form as a 5-HT.sub.3 antagonist in the manufacture of a medicament suitable for the treatment of serotonin induced gastrointestinal disturbances.Type: GrantFiled: August 28, 1987Date of Patent: March 20, 1990Assignee: Sandoz Ltd.Inventor: Karl-Heinz Buchheit
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Patent number: 4879274Abstract: Novel external medications comprise, as essential components, the following three components (A) to (C):(A) an .alpha.-monoglyceryl ether represented by the following formula (I): ##STR1## wherein R means an alkyl or alkenyl group having 10 - 24 carbon atoms; (B) a physiologically active material; and(C) an oily material.The external medications have extremely high skin occlusive properties and significantly-improved absorptivity of phosiologically active materials. Therefore, a smaller amount of the medications compared with the conventional ones can give sufficient pharmacological effects and thus side effects can be reduced. The external medications may contain physiologically active materials such as drugs, growth hormones and the like, which are expected to show pharmacological effects upon their percutaneous absorption.Type: GrantFiled: September 12, 1986Date of Patent: November 7, 1989Assignee: Kao CorporationInventors: Tetsuro Kamiya, Shuichi Tsuchiya, Kenji Hara
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Patent number: 4552881Abstract: Novel substituted and bridged pyridines useful as calcium channel blockers, pharmaceutical compositions thereof and methods of treatment are disclosed.Type: GrantFiled: August 1, 1984Date of Patent: November 12, 1985Assignee: Merck & Co., Inc.Inventor: David A. Claremon
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Patent number: 4548941Abstract: There are disclosed novel substituted and bridged pyridines which are useful as calcium channel blockers.Type: GrantFiled: July 30, 1984Date of Patent: October 22, 1985Assignee: Merck & Co., Inc.Inventors: Wasyl Halczenko, George D. Hartman
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Patent number: 4535085Abstract: A perfluorotricyclic amine compound which is usable as an oxygen carrier in an artificial blood, represented by the general formula ##STR1## wherein R denotes a perfluoroalkyl group having 1-4 carbon atoms; the ring A denotes a five- or six-membered ring, the ring B denotes a five-, six- or seven-membered ring, the ring C denotes a five- or six-membered ring any one of the rings A, B and C optionary being substituted by one or more lower perfluoroalkyl group in addition to the above-mentioned substituent R; and further f, g, h, i, j and k denote integers appropriately selected to construct the above-mentioned size of rings A, B, and C; is prepared by reacting the corresponding perhydrotricyclic amine with fluorine.Type: GrantFiled: March 29, 1983Date of Patent: August 13, 1985Assignee: The Green Cross CorporationInventors: Kazumasa Yokoyama, Chikara Fukaya, Yoshio Tsuda, Taizo Ono, Yoshio Arakawa, Yoshihisa Inoue, Youichiro Naito, Tadakazu Suyama
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Patent number: 4530929Abstract: A class of novel fused-ring, benzotricyclic, nitrogen-containing diones useful as agents in reversing electroconvulsive shock-induced amnesia. A method of preparing the compounds, pharmaceutical compositions including the compounds, and a method of reversing electroconvulsive shock-induced amnesia are disclosed.Type: GrantFiled: February 2, 1984Date of Patent: July 23, 1985Assignee: Warner-Lambert CompanyInventors: Donald E. Butler, Michael R. Pavia, Fred M. Hershenson
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Patent number: H734Abstract: A method is provided for inhibiting onset of or treating migraine headache by administering an ACE inhibitor, such as captopril, alone or in combination with a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.Type: GrantFiled: March 7, 1988Date of Patent: February 6, 1990Assignee: E. R. Squibb & Sons, Inc.Inventor: Abraham Sudilovsky