Quinuclidines (including Unsaturation) Patents (Class 514/305)
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Patent number: 6174896Abstract: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. The compound has an antagonistic effect on muscarinic M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.Type: GrantFiled: May 14, 1999Date of Patent: January 16, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Makoto Takeuchi, Ryo Naito, Masahiko Hayakawa, Yoshinori Okamoto, Yasuhiro Yonetoku, Ken Ikeda, Yasuo Isomura
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Patent number: 6156752Abstract: This invention provides a compound of the formula (I): ##STR1## and its pharmaceutically acceptable salts, wherein A.sup.1 and A.sup.2 are each halo; R.sup.1 and R.sup.2 are independently C.sub.1-4 alkyl; R.sup.3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group selected from C.sub.5-10 azacycloalkyl, C.sub.6-10 diazacycloalkyl, C.sub.7-10 azabicycloalkyl and the like; and R.sup.4 is selected from (a) substituted or unsubstituted C.sub.1-8 alkyll; (b) substituted or unsubstituted amino; (c) substituted or unsubstituted C.sub.2-6 alkanoyl; (d) substituted or unsubstituted C.sub.3-8 cycloalkyl or C.sub.7-14 bicycloalkyl; (e) substituted or unsubstituted C.sub.5-10 azacycloalkyl or C.sub.6-10 diazacycloalkyl, and (f) substituted or unsubstituted C.sub.7-14 mono- or di-azabicycloalkyl. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc.Type: GrantFiled: August 13, 1998Date of Patent: December 5, 2000Assignee: Pfizer IncInventors: Takafumi Ikeda, Mitsuhiro Kawamura, Yu-Ting Ge
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Patent number: 6150352Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.Type: GrantFiled: November 12, 1998Date of Patent: November 21, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Richard B. Toupence, Thomas F Walsh, Feroze Ujjainwalla, Jonathan R Young, Robert J. Devita
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Patent number: 6147088Abstract: There are disclosed compounds of formula (I) and pharmaceutical acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions.Type: GrantFiled: November 12, 1998Date of Patent: November 14, 2000Assignee: Merck & Co., Inc.Inventors: Mark Goulet, Eric E Allen, Matthew J. Wyvratt, Jr., Jinlong Jiang, Roy G. Smith, Thomas F Walsh, Yi Tien Yang, Jonathan R Young, Robert J. Devita
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Patent number: 6140324Abstract: The present invention relates to the use of a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine for the treatment or prevention of motion sickness. There is also provided pharmaceutical compositions and products comprising a tachykinin antagonist and a muscarinic antagonist and/or an antihistamine.Type: GrantFiled: December 18, 1997Date of Patent: October 31, 2000Assignee: Merck Sharp & Dohme Ltd.Inventor: Frederick David Tattersall
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Patent number: 6136864Abstract: A pharmaceutical composition has an acid salt of a sympathomimetic amine; and a denaturant of (i) at least one gum or viscosity modifier, and (ii) at least one surfactant, wherein the gum or viscosity modifier and the surfactant are present in amounts sufficient to have a denaturing effect on the sympathomimetic amine without significantly compromising the release of the sympathomimetic amine from the composition.Type: GrantFiled: September 25, 1997Date of Patent: October 24, 2000Assignee: Warner-Lambert CompanyInventors: W. Michael Nichols, William Bess, Stanley Lech
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Patent number: 6121285Abstract: An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone-derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof: ##STR1## wherein Q is represented by formula (II) or (IV). ##STR2## Also disclosed is a quinolone derivative where R.sup.Type: GrantFiled: May 21, 1998Date of Patent: September 19, 2000Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Youichi Kimura, Hisashi Takahashi, Kenichi Kimura, Satoru Miyauchi, Hitoshi Ohki, Kazuyuki Sugita, Rie Miyauchi
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Patent number: 6121281Abstract: Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is vinyl or ethyl; and R.sup.2 is a group R.sup.3, R.sup.4 CH.sub.2 --, or R.sup.5 R.sup.6 C.dbd.CH--; wherein each of R.sup.3 and R.sup.4 is an azabicyclic ring system or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.Type: GrantFiled: January 29, 1999Date of Patent: September 19, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Andrew Kenneth Takle, Eric Hunt, Antoinette Naylor
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Patent number: 6117883Abstract: The present invention provides heterocyclic compounds which are useful for modulating a muscarinic receptor.Type: GrantFiled: August 30, 1999Date of Patent: September 12, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, Jon K Reel, Celia A Whitesitt, Richard L Simon
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Patent number: 6103744Abstract: Disclosed are compounds of the formula ##STR1## wherein: R.sup.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.2 is selected from hydrogen, straight-chain and branched C.sub.1 -C.sub.10 alkyl, cyclohexylmethyl or --(CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl, thienyl, furanyl or pyridinyl, each optionally substituted by one or two substituents selected independently from C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxide and trifluoromethyl;or NR.sup.1 R.sup.2 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinolin-2-yl;m is 1-5;n is 1 or 2;R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;Y is halogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or a pharmaceutically acceptable salt thereof, which are dopamine autoreceptor agonists and as such are useful in the treatment of schizophrenia, Parkinson's disease, Tourette's syndrome, alcohol addiction and drug addiction.Type: GrantFiled: September 10, 1999Date of Patent: August 15, 2000Assignee: American Home Products CorporationInventors: Richard Eric Mewshaw, James Albert Nelson, Uresh Shantilal Shah
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Patent number: 6083957Abstract: The present invention relates to therapeutically active quaternary azacyclic or azabicyclic compounds with formula I: ##STR1## wherein X is oxygen or sulfur and wherein G is selected from the group of azacyclic or azabicyclic ring systems consisting of: ##STR2## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a cholinergic deficit in the peripheral system.Type: GrantFiled: April 17, 1997Date of Patent: July 4, 2000Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 6069148Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The, cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hyperlipoproteinaemia and arteriosclerosis.Type: GrantFiled: July 8, 1997Date of Patent: May 30, 2000Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Logers, Matthias Muller-Gliemann, Carsten Schmeck, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher, Henry Giera, Holger Paulsen, Paul Naab, Michael Conrad, Jurgen Stoltefuss
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Patent number: 6060454Abstract: Methods are provided for conducting surgical procedures in a patient wherein, during the surgical procedure, autonomous ventricular electrical conductivity and escape beats are reversibly and transiently suppressed to facilitate the surgical procedure. Also provided are compositions which are capable of inducing ventricular asystole in a patient. The compositions may include an AV node blocker. In one embodiment, compositions including an atrioventricular (AV) node blocker and a .beta.-blocker are provided, wherein the .beta.-blocker is present in an amount sufficient to substantially reduce the amount of AV node blocker required to induce ventricular asystole in the patient. The compositions and methods may be used for inducing temporary ventricular asystole in a beating heart, and to facilitate the performance of a variety of surgical techniques, including minimally invasive microsurgical techniques.Type: GrantFiled: August 7, 1998Date of Patent: May 9, 2000Assignee: Duke UniversityInventor: Francis G. Duhaylongsod
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Patent number: 6030966Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: July 28, 1999Date of Patent: February 29, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 6020368Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.Type: GrantFiled: December 4, 1998Date of Patent: February 1, 2000Inventors: Jeremy David Hinks, Andrew Kenneth Takle, Eric Hunt
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Patent number: 6017927Abstract: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. ##STR1## The compound has an antagonistic effect on muscarinic M.sub.3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.Type: GrantFiled: August 28, 1997Date of Patent: January 25, 2000Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Makoto Takeuchi, Ryo Naito, Masahiko Hayakawa, Yoshinori Okamoto, Yasuhiro Yonetoku, Ken Ikeda, Yasuo Isomura
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Patent number: 6015813Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: April 8, 1998Date of Patent: January 18, 2000Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Per Sauerberg
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Patent number: 5998404Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds of formula I ##STR1## and to pharmaceutical formulations comprising these compounds and methods of treatment comprising administering these compounds to a subject in need of treatment. The novel oxadiazole compounds, such as (.+-.)-3-butyloxy-4-(1-azabicyclo[2.2.2]octyl-3-oxy)-1,2,5-oxadiazole, are useful in treating central nervous system disorders caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: June 1, 1995Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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Patent number: 5998434Abstract: The present invention provides a composition and method for treating pain using Selected Muscarinic Compounds and one or more compounds selected from the group consisting of Nonsteroidal Anti-inflammatory drugs, acetaminophen, opioids, and alpha-adrenergic compounds.Type: GrantFiled: June 4, 1998Date of Patent: December 7, 1999Assignee: Eli Lilly and CompanyInventors: Charles H. Mitch, Harlan E. Shannon
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Patent number: 5994323Abstract: A pharmaceutical composition is disclosed that comprises clioquinol, vitamin B.sub.12, and, optionally, pharmaceutical acceptable carriers and/or excipients. The use of the pharmaceutical composition removes or alleviates the side effects of clioquinol.Type: GrantFiled: February 13, 1998Date of Patent: November 30, 1999Assignee: P.N. Gerolymatos S.A.Inventor: Panayotis N. Gerolymatos
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Patent number: 5990124Abstract: Alkoxy and/or acyloxy disubstituted and polysubstituted aralkyl and aralkenyl bis-quaternary ammonium derivatives of cyclic alkanol diesters have neuromuscular relaxant properties.Type: GrantFiled: October 24, 1997Date of Patent: November 23, 1999Inventors: Laszlo Gyermek, Chingmuh Lee, Young-Moon Cho
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Patent number: 5990125Abstract: The present invention relates to the use of certain NK-1 receptor antagonists (e.g., substance P receptor antagonists) to treat cancer patients, particularly cancer patients afflicted with a small cell lung carcinoma, APUDoma, astrocytoma, neuroendocrine tumor or extrapulmonary small cell carcinoma.Type: GrantFiled: January 17, 1997Date of Patent: November 23, 1999Assignee: Pfizer Inc.Inventor: Harry Ralph Howard
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Patent number: 5981545Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## in which one of X and Y represents hydrogen and the other represents Z, where Z is a group ##STR2## in which Q represents a 3-membered divalent residue completing a 5-membered aromatic ring and comprises zero, one or two nitrogen atoms, Q being optionally C-substituted by a group R.sub.1 selected from halogen, CN, OR.sub.2, SR.sub.2, N(R.sub.2).sub.2, NHCOR.sub.2, NHCOOCH.sub.3, NHCOOC.sub.2 H.sub.5, NHOR.sub.2, N.sub.3, NHNH.sub.2, NO.sub.2, COR.sub.2, COR.sub.3, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, cyclopropyl or C.sub.1-2 alkyl optionally substituted with OR.sub.2, N(R.sub.2).sub.2, SR.sub.2, CO.sub.2 R.sub.2, CON(R.sub.2).sub.2 or one, two or three halogen atoms, in which each R.sub.2 is independently hydrogen or C.sub.1-2 alkyl and R.sub.3 is OR.sub.2, NH.sub.2 or NHR.sub.2 ; r represents an integer of 2 or 3, s represents an integer of 1 or 2 and t represents 0 or 1; R.sub.a and R.sub.Type: GrantFiled: October 4, 1990Date of Patent: November 9, 1999Assignee: Beecham Group p.l.c.Inventors: Sarah Margaret Jenkins, Harry John Wadsworth, Barry Sidney Orlek, Steven Mark Bromidge
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Patent number: 5977129Abstract: The present invention relates to compounds of formula I: whereinone or both G is an azacyclic ring of formula II: ##STR1## and Z is oxygen or sulfur and the remaining variables are as defined in the specification. The compounds are useful as stimulants of the cognitive function of the forebrain and hippocampus of mammals and especially in the treatment of Alzheimer's disease, severe painful conditions and glaucoma.Type: GrantFiled: May 3, 1995Date of Patent: November 2, 1999Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5972892Abstract: The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating the irritant effect of this product.It also relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition for topical application containing at least one product with an irritant side effect for reducing or even eliminating the irritant effect of this product.The substance P antagonist may be a peptide compound or a nitrogen-containing compound or a nitrogen-, sulphur- or oxygen-containing heterocyclic compound.Type: GrantFiled: June 15, 1998Date of Patent: October 26, 1999Assignee: L'orealInventors: Olivier De Lacharriere, Lionel Breton
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Patent number: 5968926Abstract: The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases.Type: GrantFiled: June 5, 1995Date of Patent: October 19, 1999Assignee: Novo Nordisk A/SInventors: Franklin Porter Bymaster, Harlan E. Shannon, Per Sauerberg, Preben Olesen, John Stanley Ward, Charles H. Mitch
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Patent number: 5965579Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.Type: GrantFiled: November 21, 1997Date of Patent: October 12, 1999Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5939434Abstract: This invention provides a compound of the formula: ##STR1## and its pharmaceutically acceptable salts, wherein R.sup.1 is halo, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halo C.sub.1 -C.sub.6 alkoxy; R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halo C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyl-S-, C.sub.1 -C.sub.6 alkyl-SO--, C.sub.1 -C.sub.6 alkyl-SO.sub.2 --, cyclopropyl, phenyl, --NH.sub.2, --NH(CH.sub.3), --NHC(.dbd.O)CH.sub.3, --N(CH.sub.3).sub.2, --N(C.sub.2 H.sub.5).sub.2 or --CH.sub.2 C(.dbd.O)CF.sub.3 ; Ar.sup.1 and Ar.sup.2 are independently phenyl, halophenyl or thienyl; X is NH, O or S; and Y is hydrogen, --COOR.sup.3 or --CONR.sup.4 R.sup.5, wherein R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.6 alkyl.Type: GrantFiled: September 5, 1997Date of Patent: August 17, 1999Inventor: Kunio Satake
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Patent number: 5939433Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is methoxy and R.sup.2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.Type: GrantFiled: April 30, 1997Date of Patent: August 17, 1999Assignee: Pfizer IncInventors: Fumitaka Ito, Hiroshi Kondo, Masami Nakane, Kaoru Shimada, John Adams Lowe, III, Terry Jay Rosen
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Patent number: 5936088Abstract: The present invention relates to therapeutically active azacyclic and azabicyclic compounds, to methods for their preparation and to pharmaceutical compositions comprising the compounds. These compounds are useful in treating diseases in the central nervous system related to malfunctioning of the nicotinic cholinergic system.Type: GrantFiled: March 20, 1998Date of Patent: August 10, 1999Assignee: Novo Nordisk A/SInventor: Preben Houlberg Olesen
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Patent number: 5925661Abstract: The invention relates to compounds of the formula: ##STR1## Compounds of the above formula have a great affinity for the neurotensin receptors.Type: GrantFiled: November 24, 1997Date of Patent: July 20, 1999Assignee: SANOFIInventors: Bernard Labeeuw, Danielle Gully, Francis Jeanjean, Jean-Charles Molimard, Robert Boigegrain
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Patent number: 5922721Abstract: A 1,2-ethanediol derivative represented by the general formula ?I! or its salt: ##STR1## has a NGF activity-potentiating effect and is useful as a remedy for various diseases caused by degeneration of central nervous system or peripheral nervous system such as senile dementia of Alzheimer type, Huntington's chorea, various neuropathies, Riley-Day syndrome, traumatic nerve injury, amyotrophic lateral sclerosis (ALS) and the like.Type: GrantFiled: December 31, 1997Date of Patent: July 13, 1999Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Mutsuko Maekawa, Kazunari Hirata, Hirokazu Narita
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Patent number: 5919793Abstract: Compounds of formula (I) wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 14 CR.sup.2 is a double bond; X is selected from --Ch.sub.2 CH.sub.2 --, --C.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2, CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S(O).sub.n -- and --S(O).sub.n CH.sub.Type: GrantFiled: October 26, 1995Date of Patent: July 6, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Paul Robert Owen Whittamore, David Robert Brittain
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Patent number: 5900418Abstract: A method is provided for the control of obesity comprising administering to a mammal including humans suffering from obesity an acetylcholine esterase reactivator or prodrug derivative thereof optionally in association with an acetylcholine receptor antagonist.Type: GrantFiled: February 10, 1997Date of Patent: May 4, 1999Assignee: Synapse Pharmaceuticals International, Inc.Inventor: Norman Viner
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Patent number: 5892047Abstract: Compounds of structure (I) in which R is C.sub.1-8 alkyl(phenyl)p, C.sub.2-8 alkenyl(phenyl)p, C.sub.2-8 alkenyl(phenyl)p, C.sub.3-8 cycloalkyl or C.sub.1-8 alkylC.sub.3-8 cycloalkyl; p is 0 to 2; n is 0 to 6; A is a bond, oxygen, sulphur or NR.sup.1 ; R.sup.1 is hydrogen, C.sub.1-8 alkylphenylC.sub.1-4 alkyl; m is 0 to 3; and Ar is aryl or heteroaryl, each of which may be optionally substituted, and salts thereof processes for preparing said compounds, pharmaceutical compositions containing them and their use in therapy, in particular as calcium blocking agents.Type: GrantFiled: August 4, 1997Date of Patent: April 6, 1999Assignee: NeuroSearch A/SInventors: Dan Peters, Oskar Axelsson
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Patent number: 5891888Abstract: A composition to prevent dehydration, supply energy and prevent cramps contains electrolytes, carbohydrates and quinine and/or quinine salts and a method of preventing cramping caused by strenuous bodily activity. Palatability of the composition is improved by the effective use of carbohydrate, pH adjustment, flavoring and carbonation.Type: GrantFiled: January 14, 1998Date of Patent: April 6, 1999Inventor: Robert Charles Strahl
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Patent number: 5889019Abstract: The present invention relates to therapeutically active heterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.Type: GrantFiled: October 31, 1996Date of Patent: March 30, 1999Assignee: Eli Lilly and CompanyInventor: Charles Howard Mitch
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Patent number: 5886009Abstract: This invention relates to the quinuclidine derivative (2S, 3S)-N-(5-n-propyl-2-methoxyphenyl)methyl-2-diphenylmethyl-1-azabicyclo?2.2 .2!octan-3-amine and its pharmaceutically acceptable salts. These compounds are substance P antagonists and are useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.Type: GrantFiled: June 19, 1995Date of Patent: March 23, 1999Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo, Masami Nakane, Kaoru Shimada
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Patent number: 5885974Abstract: Methods are disclosed for correcting biological information transfer in a patient in need of such therapy which comprise administration to a patient of a composition comprising a therapeutically effective amount of a biocomplex comprising at least one bioactive agent from each of the three informational blocks of biological information transfer, each agent being present in an amount sufficient to correct the biological information transfer of the patient under treatment and resulting in the resumption of normal cell metabolism, said amount being less than the buffering amount of said agent; together with a carrier therefor.Type: GrantFiled: December 6, 1994Date of Patent: March 23, 1999Assignee: Michael M. DanielovInventor: Michael M. Danielov
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Patent number: 5883107Abstract: The present invention provides peptide aldehydes having an azetidinyl, prolyl or pipecolyl group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibitors of thrombin. Their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis are also described.Type: GrantFiled: June 7, 1995Date of Patent: March 16, 1999Assignee: Corvas International, Inc.Inventors: Odile Esther Levy, Susan Yoshiko Tamura, Ruth Foelsche Nutt, William Charles Ripka
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Patent number: 5880121Abstract: 4,5-Dihydronaphth?1,2-c!isoxazole derivatives of the general formula: ##STR1## where A, X and n are defined herein are disclosed. Such compounds are useful as serotonin 5-HT.sub.3 antagonists. These compounds art useful for the treatment of anxiety, psychiatric disorders, nausea, vomiting and drug dependency.Type: GrantFiled: December 19, 1996Date of Patent: March 9, 1999Assignee: Hoechst Marion Roussel Inc.Inventor: Nicholas J. Hrib
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Patent number: 5874427Abstract: This invention provides novel 5-HT.sub.1F agonists of the Formula ##STR1## in which X, Y, E, R, A, B, and n are as defined in the specification, which are useful for the treatment of migraine and associated disorders.Type: GrantFiled: April 14, 1998Date of Patent: February 23, 1999Assignee: Eli Lilly and CompanyInventors: Sandra A. Filla, Joseph H. Krushinski, Jr., John Mehnert Schaus
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Patent number: 5874444Abstract: Inhibition of the enzyme poly (ADP-ribose) polymerase can delay the onset of senescence and inhibitors of the enzyme can be used to treat diseases caused or exacerbated by cellular senescence.Type: GrantFiled: August 27, 1996Date of Patent: February 23, 1999Assignee: Geron CorporationInventor: Michael David West
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Patent number: 5872117Abstract: 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: GrantFiled: November 4, 1997Date of Patent: February 16, 1999Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita
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Patent number: 5869499Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.Type: GrantFiled: March 3, 1996Date of Patent: February 9, 1999Assignee: Pfizer IncInventors: Kunio Satake, Hiroaki Wakabayashi
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Patent number: 5863927Abstract: Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.Type: GrantFiled: September 19, 1996Date of Patent: January 26, 1999Assignee: Center for Neurologic StudyInventors: Richard Alan Smith, Jonathan M. Licht
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Patent number: 5859004Abstract: This invention relates to the use of azabicyclic compounds for the treatment of diseases caused by malfunctioning of the nicotinic cholinergic system. These diseases treated include obesity, Parkinson's disease, anxiety, and ulcerative colitis.Type: GrantFiled: August 6, 1997Date of Patent: January 12, 1999Assignee: Novo Nordisk A/SInventor: Preben Houlberg Olesen
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Patent number: 5852038Type: GrantFiled: November 18, 1996Date of Patent: December 22, 1998Assignee: Pfizer IncInventors: Fumitaka Ito, Toshihide Kokura, Masami Nakane, Kunio Satake, Hiroaki Wakabayashi
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Patent number: 5852037Abstract: The present invention provides a method for treating anxiety in humans using azacyclic or azabicyclic compounds.Type: GrantFiled: October 22, 1996Date of Patent: December 22, 1998Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5852036Abstract: The present invention provides a method for treating anxiety in humans using compounds which modulate a muscarinic receptor.Type: GrantFiled: May 23, 1995Date of Patent: December 22, 1998Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon