Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/477)
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Patent number: 7057035Abstract: A process for converting an aryl triflate, heteroaryl triflate, aryl halide or heteroaryl halide to an N-hydroxysuccinimido ester is disclosed. The process involves reacting the triflate or halide with carbon monoxide and N-hydroxysuccinimide in a solvent in the presence of a palladium catalyst and a base.Type: GrantFiled: January 14, 2005Date of Patent: June 6, 2006Assignee: Rensselaer Polytechnic InstituteInventors: Mark P. Wentland, Rongliang Lou
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Patent number: 6887868Abstract: The present invention provides compounds of Formula (I): wherein: R1, R2, R3, R4, R5, R6 R7, R8, n, m, and X have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: September 19, 2002Date of Patent: May 3, 2005Assignee: Pharmacia & Upjohn CompanyInventor: Jian-Min Fu
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Patent number: 6849619Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: February 20, 2004Date of Patent: February 1, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Albert J. Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6720316Abstract: The present invention provides compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8 and Z have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.Type: GrantFiled: August 2, 2002Date of Patent: April 13, 2004Assignee: Pharmacia & Upjohn CompanyInventor: William W. McWhorter, Jr.
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Patent number: 6699852Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6, R7, R8, R9, X, b, k, and n, and the dashed lines are described herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are serotonin agonists and antagonists and are useful in the control or prevention of central nervous system disorders including obesity, anxiety, depression, psychosis, schizophrenia, sleep disorders, sexual disorders, migraine, conditions associated with cephalic pain, social phobias, and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: December 19, 2001Date of Patent: March 2, 2004Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
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Patent number: 6482567Abstract: New photoacid generator compounds (“PAGs”) are provided and photoresist compositions that comprise such compounds. In particular, non-ionic PAGs are provided that contain an oxime sulfonate group, and/or an N-oxyimidosulfonate group. PAGs of the invention are particularly useful as photoactive components of photoresists imaged at short wavelengths such as 248 nm, 193 nm and 157 nm.Type: GrantFiled: August 25, 2000Date of Patent: November 19, 2002Assignee: Shipley Company, L.L.C.Inventors: James F. Cameron, Gerhard Pohlers
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Patent number: 6465491Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: April 4, 2001Date of Patent: October 15, 2002Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 6410534Abstract: The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.Type: GrantFiled: June 29, 1999Date of Patent: June 25, 2002Assignee: Merck & Co., Inc.Inventors: Christopher J. Dinsmore, Ian M. Bell, Douglas C. Beshore, Theresa M. Williams
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Patent number: 6387512Abstract: A photochromic grey coloring 2H-naphtho[1,2-b]pyran of formula (1) wherein R1 is selected from mono-, di- or poly-substituted aryl groups, mono-, di- or poly-substituted naphthyl groups and mono-, di- or poly-substituted heteroaryl groups, wherein at least one substituent is a nitrogen containing group, including amino, C1-C20 and C6-C20 alkylamino, C1-C20 and C6-C20 dialkylamino, C2-C20 dialkenylamino, C2-C20 or C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, tetra (C1-C10 linear or branched alkyl) guanidino and cyclic-amino groups and at least one of R7 and R9, which may be the same or different, is selected from C1-C20 N alkylamino C1-C20 N-alkylamido, C1-C20 N,N-dialkylamido, amido, nitro, amino, C1-C20 alkylamino, C1-C20 dialkylamino, C2-C20 dialkenylamino, C4-C20 di(polyalkenyl)amino, arylamino, diarylamino, C1-C20 alkylarylamino, or cyclicamino groups.Type: GrantFiled: March 16, 2001Date of Patent: May 14, 2002Assignee: James Robinson LimitedInventors: David Allan Clarke, Bernard Mark Heron, Christopher David Gabbutt, John David Hepworth, Steven Michael Partington, Stephen Nigel Corns
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Publication number: 20020037560Abstract: Thirteen-membered ring containing terpenoid analog compounds are synthesized from analinogeranylpyrophosphate using 5-epi-aristolochene synthase as a reaction catalyst. The method provides a generalized procedure for making high-ordered ring structures having various substituent groups. The products can be used in assays for 5-epi-aristolochene synthase activity, and as precursors and intermediates for biologically active substances.Type: ApplicationFiled: June 8, 2001Publication date: March 28, 2002Inventors: Joseph Chappell, H.P. Spielmann
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Publication number: 20020010085Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example 1Type: ApplicationFiled: March 6, 2001Publication date: January 24, 2002Inventor: Peter Herold
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Patent number: 6323194Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof useful in the treatment of pain. The compounds of the present invention are azaadamantanes, azanoradamantanes and azahomoadamantanes.Type: GrantFiled: October 17, 2000Date of Patent: November 27, 2001Assignee: UCB, S.A.Inventors: Gurmit Grewal, Anna Toy-Palmer, Xiong Cai, George Mark Latham
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Patent number: 6235747Abstract: The present invention relates to certain 6-phenyl-pyridin-2-ylamine derivatives that exhibit activity as nitric oxide synthase (NOS) inhibitors, to pharmaceutical compositions containing them and to their use in the treatment and prevention of central nervous system disorders.Type: GrantFiled: March 13, 1997Date of Patent: May 22, 2001Assignee: Pfizer Inc.Inventors: John A. Lowe, III, Peter J. Whittle
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Patent number: 6211360Abstract: The present invention is directed to compounds having formula (1), wherein n is from 0 to 8; R1 is CH2OH, CH(OH)R5, CH2OR5, CO2R5, C(O)NH2, C(I)NHR5, C(O)NR5R6, C(O)NHNH2, C(O)NHNHR5, C(O)NHNR5R6, C(O)NR5NH2, C(O)NR5NHR6, C(O)NR5NR6R7, C(O)NHNH(C(O)R5), C(O)NHNR5(C(O)R6) C(O)NR5NH(C(O)R6), C(O)NR5NR6(C(O)R7), CN, or C(O)R5; R2 is H, unsubstituted or substituted alkyl, YH, YR8, YC(O)R8, C(O)YR8, C(O)NH2, C(O)NHR8, C(O)NR8R9, NH2, NHR8, NR8R9, NHC(O)R8, or NR8C(O)R9; R3 and R4 are the same or different and are selected from the group consisting of H, halogens, unsubstituted or substituted alkyl, OH, OR10, NH2, NHR10, NR10R11, NHC(O)R10, or NR10C(O)R11; R5, R6, R7, R8, R9, R10, and R11 are the same or different and are selected from the group consisting of unsubstituted alkyl and substituted alkyl and substituted alkyl; R12 is selected from the group consisting of J, unsubstituted alkyl, and substituted alkyl; and Y is O or S; provided that when n is O, R2 is selected from the group consisting of H, substitutedType: GrantFiled: August 31, 1998Date of Patent: April 3, 2001Assignees: Albany Medical College, University of VermontInventors: Stanley D. Glick, Martin E. Kuehne
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Patent number: 6130330Abstract: What is claimed is a process for preparing macropolycyclic polyamines of the formula ##STR1## where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description. These compounds are prepared by a novel improved process by reacting a cyclic amine of the formula ##STR2## with a compound of the formula X--A.sup.2 --Y or X--A.sup.3 --Y where A.sup.1, A.sup.2, A.sup.3 and A.sup.4 are as defined in the description and X and Y are a leaving group.Type: GrantFiled: March 4, 1999Date of Patent: October 10, 2000Assignee: Clariant GmbHInventors: Bernd Nestler, Michael Seebach
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Patent number: 6048980Abstract: The present invention relates to the novel compound, 1,4,7,10-tetraazabicyclo[8.2.2]tetradecan-2-one of formula (I), its preparation and the use thereof for the preparation of tetraazamacrocycles.Type: GrantFiled: July 28, 1999Date of Patent: April 11, 2000Assignee: Dibra S.p.AInventors: Maria Argese, Giorgio Ripa
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Patent number: 6040442Abstract: The presently claimed process provides a method for preparing compounds of the formula ##STR1## phosphorous (III) compound and a diester of azodicarboxylate.Type: GrantFiled: June 1, 1995Date of Patent: March 21, 2000Assignee: Eli Lilly and CompanyInventors: Leander Merritt, John S. Ward
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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: 5952324Abstract: Phenyloxazolidinone compound of formula (I)or a pharmaceutically acceptable salt thereof characterized by a bicyclic thiazine or oxazine substituent. The compounds are useful antimicrobial agents, effective against a number of human and veterinary pathogens, including gram-positive aerobic bacteria such as multiply-resistant staphylococci, streptococci and enterococci as well as anaerobic organisms such as Bacteroides spp. and Clostridia spp. species, and acid-fast organisms such as Mycobacterium tuberculosis, Mycobacterium avium and Mycobacterium spp.Type: GrantFiled: May 14, 1997Date of Patent: September 14, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Richard C. Thomas, Gary L. Cleek, Lisa M. Thomasco, Robert C. Gadwood
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Patent number: 5912343Abstract: A compound comprising at least one cyclic amine, having an organolithium side-chain, defined according to formula (I) ##STR1## wherein Z is a lithium atom (Li); R.sub.1 is selected from the group consisting of organic groups containing from 1 to about 12 carbon atoms and a bridging bond; each R.sub.2 is independently selected from the group consisting of hydrogen, organic groups containing from 1 to about 12 carbon atoms, and a bridging bond; each R.sub.3 is independently selected from the group consisting of hydrogen and organic groups containing from 1 to about 12 carbon atoms; a is an integer from 4 to about 16; and b is an integer from 0 to about 12; and optionally including a bridge, formed by the selection of two of said bridging bonds, the bridge having 0 to about 6 carbon atoms between the bridging ring members.Type: GrantFiled: December 31, 1996Date of Patent: June 15, 1999Assignee: Bridgestone CorporationInventors: David F. Lawson, William L. Hergenrother, Michael L. Kerns
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Patent number: 5854239Abstract: The present invention relates to diazabicyclic compounds and, specifically, to compounds of the formula ##STR1## wherein A, G, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined in the specification. The compounds of formula I are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: June 20, 1996Date of Patent: December 29, 1998Assignee: Pfizer Inc.Inventors: Harry R. Howard, Kevin D. Shenk
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Patent number: 5852189Abstract: Relatively pure tertiaryaminoalkyllithium initiators suitable for anionic polymerization reactions are prepared at low temperatures in an organic ether by reacting an equivalent excess of lithium metal with a tertiaryaminoalkylhalide. The lithium initiators are very stable at moderate temperatures when the ether is replaced by an aliphatic, a cycloaliphatic, or an aromatic solvent. Yields of the initiator in excess of 98% are readily achieved.Type: GrantFiled: December 31, 1996Date of Patent: December 22, 1998Assignee: Bridgestone CorporationInventors: William L. Hergenrother, Michael L. Kerns, David F. Lawson
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Patent number: 5849731Abstract: The present invention relates to indole derivatives represented by the following compound 1 and the pharmacologically acceptable acid addition salt thereof. ##STR1## The compounds of the present invention were found to exhibit strong antitussive and analgesic actions as a result of pharmacological evaluation, and can be used in the pharmaceutical field as effective antitussives and analgesics.Type: GrantFiled: May 16, 1997Date of Patent: December 15, 1998Assignee: Toray Industries, Inc.Inventors: Hiroshi Nagase, Koji Kawai, Takashi Endo, Shinya Ueno, Masayuki Maeda, Satoshi Sakami
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Patent number: 5834456Abstract: Polyazamacrocyclofluoromonoalkylphosphonic acid compounds are disclosed which form inert complexes with Gd, Mn, Fe or La ions. The complexes are useful as contrast agents for diagnostic purposes.Type: GrantFiled: February 23, 1996Date of Patent: November 10, 1998Assignees: The Dow Chemical Company, The University of TexasInventors: Garry E. Kiefer, A. Dean Sherry
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Patent number: 5834454Abstract: A substituted guanidine derivative represented by the general formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently a hydrogen atom, an unsubstituted alkyl group, a substituted alkyl group, a halogen atom or the like; Y.sub.1, Y.sub.2, Y.sub.3, Y.sub.4, Y.sub.5, Y .sub.6 and Y.sub.7, which may be the same or different, are independently a single bond, --CH.sub.2 --, --O--, --CO--or the like, adjacent members of a group consisting of Y.sub.1 through Y.sub.7 being able to be taken together to represent --CH.dbd.CH--, and at least two of Y.sub.1 through Y.sub.7 being independently a group other than a single bond; Z may be absent, or one or more Zs may be present and are, the same or different, independently a substituent for a hydrogen atom bonded to any of the carbon atoms constituting the ring formed by Y.sub.1 through Y.sub.Type: GrantFiled: January 28, 1997Date of Patent: November 10, 1998Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Masahumi Kitano, Naohito Ohashi
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Patent number: 5744607Abstract: The invention is directed to glutamic acid and aspartic acid derivatives represented by formula (I): ##STR1## wherein R.sub.1 is selected from the group consisting of unsubstituted, mono- or di-substituted phenyl groups, unsubstituted, mono- or di-substituted phenylamino groups, a 2(beta)naphthyl group, and heterocyclic, monocyclic and dicyclic groups; R.sub.2 is selected from heterocyclic spiro groups, aminoalkyladamantyl groups, alkylamino groups, C.sub.4 -C.sub.10 cycloalkylamino groups and dicyclic amino groups (condensed); R.sub.3 is H, CH.sub.3 or C.sub.2 H.sub.5 ; A is a bond or a linear or branched alkylene group having from 1 to 4 carbon atoms; W is a tertiary amino group or a heterocyclic group; and r is 1 or 2. The compounds have a potent antagonistic effect on gastrin and cholecystokinin and can be used to treat diseases which are linked to imbalances in the physiological levels of gastrin, cholecystokinin or other biologically active polypeptides related thereto.Type: GrantFiled: October 18, 1996Date of Patent: April 28, 1998Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Lucio C. Rovati, Luigi A. Rovati
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Patent number: 5741788Abstract: 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: November 17, 1995Date of Patent: April 21, 1998Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5733924Abstract: DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, ?wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.Type: GrantFiled: April 17, 1997Date of Patent: March 31, 1998Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yutaka Kanda, Yutaka Saitoh, Hiromitsu Saito, Tadashi Ashizawa, Kazuyo Sugiyama, Katsushige Gomi, Shingo Kakita, Yuichi Takahashi, Chikara Murakata
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Patent number: 5728843Abstract: The present invention involves a rapid synthesis of .sup.18 F-FMISO and analogs thereof. New precursors such as 1-(2'-nitro-1'-imidazolyl)-2-0-acetyl-3-0-tosylpropanol, glycerol-1,3-ditosylate-2-0-acetylate, 1-(2'-nitro-1'-imidazolyl)-2,3-0-diacetylate, are also important aspects of the invention.A further aspect of the invention is the development of a hydrophilic PET ligand to image tumor hypoxia. Erythrotosyl analogue of 2-nitroimidazone (Ts-ETNIM) was prepared from a mixture of 2-nitromidazole, ditosylthreitol and cesium carbonate at 60.degree. C. for 1 hr. Ts-ETNIM was isolated at 70% yield. ?.sup.18 F!fluoroerythronitroimidazole (FETNIM) when prepared from Ts-ETNIM and K.sup.18 F/kryptofix.RTM.. The yield for ?.sup.18 F!FETNIM was 26-30% (60 min, decay corrected). Results of biodistribution and PET studies indicate that ?.sup.18 F!FETNIM has the potential to detect tumor hypoxia and is indicated to be less neurotoxic.Type: GrantFiled: April 4, 1996Date of Patent: March 17, 1998Assignee: Wallace TechnologiesInventors: Sidney Wallace, David J. Yang, Abdallah Cherif
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Patent number: 5707985Abstract: There are disclosed novel substituted naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives that are useful in a method of treating immuno-inflammatory diseases in a mammalian patient suffering therefrom. Pharmaceutical compositions containing the sulfonamide compounds are also provided.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Tanabe Seiyaku Co. Ltd.Inventors: Thomas Charles McKenzie, Gilbert M. Rishton, Nancy K. Harn, Wolfgang Scholz, James Hu
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Patent number: 5679673Abstract: Certain aralkyl diazabicycloalkyl 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, 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.10 through R.sup.13 is independently selected from hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; wherein each of R.sup.8 and R.sup.Type: GrantFiled: November 21, 1994Date of Patent: October 21, 1997Assignee: The United States of America, represented by the Department of Health and Human ServicesInventors: Wayne Bowen, Brian R. de Costa, Celia Dominguez, Xiao-Shu He, Kenner C. Rice
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Patent number: 5643848Abstract: An acyclic alkane soluble anionic polymerization initiator includes a mixture of from about 90 to about 10 parts by weight of a lithio amine having the general formula A.sub.1 Li and from about 10 to about 90 parts by weight of at least one other lithio amine having the general formula A.sub.2 Li. A.sub.1 and A.sub.2 are selected from the dialkyl, alkyl, cycloalkyl and dicycloalkyl amine radicals and cyclic amine radicals. There is also provided a method of forming a mixture of anionic polymerization initiators, a functionalized polymer and a method of forming a functionalized polymer.Type: GrantFiled: May 3, 1995Date of Patent: July 1, 1997Assignee: Bridgestone CorporationInventors: David F. Lawson, James E. Hall, Yoichi Ozawa
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Patent number: 5578542Abstract: An acyclic alkane soluble anionic polymerization initiator includes a mixture of from about 90 to about 10 parts by weight of a lithio amine having the general formula A.sub.1 Li and from about 10 to about 90 parts by weight of at least one other lithio amine having the general formula A.sub.2 Li. A.sub.1 and A.sub.2 are selected from the dialkyl, alkyl, cycloalkyl and dicycloalkyl amine radicals and cyclic amine radicals. There is also provided a method of forming a mixture of anionic polymerization initiators, a functionalized polymer and a method of forming a functionalized polymer.Type: GrantFiled: March 30, 1994Date of Patent: November 26, 1996Assignee: Bridgestone CorporationInventors: David F. Lawson, James E. Hall, Yoichi Ozawa
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Patent number: 5512579Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## wherein R.sup.1 represents a group represented by the formula: ##STR2## {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl. etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5!.Type: GrantFiled: July 18, 1994Date of Patent: April 30, 1996Assignee: Eisai Co., Ltd.Inventors: Shuhei Miyazawa, Yorohisa Hoshino, Hisashi Shibata, Kazuo Hirota, Takaaki Kameyama, Shinya Abe, Takashi Yamanaka
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Patent number: 5498614Abstract: The invention relates to bridged aza-bicyclic derivatives of formula (I). These compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. Also disclosed are intermediates used in the synthesis of compound of formula (I).Type: GrantFiled: November 7, 1994Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventor: Manoj C. Desai
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Patent number: 5414009Abstract: The present invention relates to compounds ##STR1## where G is ##STR2## 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: January 4, 1993Date of Patent: May 9, 1995Assignee: Novo Nordisk A/SInventors: Preben H. Olesen, Per Sauerberg
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Patent number: 5352685Abstract: The thieno[3.2-b]pyridine derivative of the present invention promote the gastric emptying in male ddy mice and the gastric contraction in dogs sutured with a strain-gauge transducer. It is believed that the derivatives have the action to enhance gastric motor action and gastric emptying. Therefore, the compound of the present invention are effective for the prevention and therapeutical treatment of the symptoms caused by gastric hypanakinesis, such as heartburn, abdominal distension feeling, anorexia, unpleasant feeling on upper abdomen, abdominalgia, nausea, vomiting, etc. caused by the underlying diseases such as acute and chronic gastritis, stomach and duodenum ulcer, gastroneurosis, gastroptosis, etc. The present invention also encompasses a pharmaceutical composition containing as the effective ingredient a compound of the present invention, and a method for producing the same.Type: GrantFiled: March 11, 1993Date of Patent: October 4, 1994Assignee: Mitsubishi Kasei CorporationInventors: Akira Maruyama, Shigeru Ogawa, Satoshi Yamazaki, Akihiro Tobe
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Patent number: 5329005Abstract: The present invention is directed toward anionic polymerization initiators which are soluble in hydrocarbon solvents. The initiators include a lithio amine having the general formula ALi. The component A is a dialkyl or dicycloalkyl amine radical or a cyclic amine. The invention is also directed toward polymers and other products made using the initiator, and methods therefor. Further, the invention contemplates a polymer, a polymer composition and products therefrom, which include a functional group from the reaction product of an amine and an organolithium compound. The resulting polymers may be terminated with a terminating, coupling or linking agent, which may provide the polymer with a multifunctionality.Type: GrantFiled: October 2, 1992Date of Patent: July 12, 1994Assignee: Bridgestone CorporationInventors: David F. Lawson, Koichi Morita, Yoichi Ozawa, Mark L. Stayer, Jr., Ryota Fujio
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Patent number: 5256671Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein Q is the residue of an optionally substituted azabicyclic ring system;the dotted line represents an optional double bond;X represents H, --OH, .dbd.O or halo;R.sup.1 represents H, phenyl or thienyl, which phenyl or thienyl groups may be optionally substituted by halo or trifluoromethyl;R.sup.2 represents phenyl, thienyl or benzyl, any of which groups may be optionally substituted by halo or trifluoromethyl; andR.sup.3, R.sup.4 and R.sup.5 independently represent H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo, cyano, nitro, trifluoromethyl, trimethylsilyl, --OR.sup.a, SR.sup.a, SOR.sup.a, SO.sub.2 R.sup.a, --NR.sup.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent H, C.sub.1-6 alkyl, phenyl or trifluoromethyl, are tachykinin receptor antagonists. They and compositions thereof are useful in therapy.Type: GrantFiled: June 29, 1992Date of Patent: October 26, 1993Assignee: Merck Sharp & Dohme, LimitedInventors: Tamara Ladduwahetty, Christopher J. Swain
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Patent number: 5252570Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## wherein the substituents are defined hereinbelow in the specification, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.Type: GrantFiled: May 30, 1991Date of Patent: October 12, 1993Assignee: B.I. ItaliaInventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
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Patent number: 5110828Abstract: Novel compounds of formula (I), a process for their preparation, and their use as pharmaceutical agents are described: ##STR1## wherein R.sub.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is hydrogen or C.sub.1-4 alkyl, subject to the proviso that when R.sub.2 is a group OCOR.sub.5 or a group NHR.sub.6, R.sub.3 is C.sub.1-4 alkyl.Type: GrantFiled: April 13, 1989Date of Patent: May 5, 1992Assignee: Beecham Group p.l.c.Inventors: Steven M. Bromidge, Michael S. Hadley, Barry S. Orlek
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Patent number: 5100884Abstract: The invention relates to new 8,9-annelated-1,2,3,4-tetrahydro-.beta.-carboline derivatives of the formula ##STR1## wherein the symbols have the following meanings: R.sub.1 is hydrogen, straight or branched alkyl having 1-6 C-atoms, fluorinated or hydroxylated alkyl having 1-6 C-atoms;n has the value of one;R.sub.2 +R.sub.3 together with the carbon atom and the nitrogen atom to which they are bonded and the intermediate carbon atom constitute a heterocyclic group consisting of 8 ring atoms;R.sub.4 is hydrogen, straight or branched alkyl having 1-8 C-atoms, alkoxy- or alkylthioalkyl having 2-6 C-atoms, alkenyl or alkynyl having 2-8 C-atoms, which groups may be substituted with one or more fluorine atoms or hydroxy groups, or with one phenyl group containing 0-3 groups R.sub.10, or cycloalkyl group having 3-7 C-atoms, or R.sub.4 is cycloalkyl having 3-8 C-atoms which may be substituted with one or more fluorine atoms, alkyl groups having 1-4 C-atoms, cycloalkyl groups having 3-5 C-atoms, or R.sub.Type: GrantFiled: October 30, 1989Date of Patent: March 31, 1992Assignee: Duphar International Research B.V.Inventors: Derk Hamminga, Ineke Van Wigngaarden, Johannes W. C. M. Jansen
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Patent number: 5061795Abstract: A novel hexa-cyclic compound, a derivative of camptothecin, of the general formura: ##STR1## The compound is prepared from an aminoketone compound and a pyranoindolizine compound through Friedlaender reaction. It has an excellent antitumour activity and a high degree of safety, and can be applied as an antitumour medicine for curing tumors of various kinds.Type: GrantFiled: December 27, 1989Date of Patent: October 29, 1991Assignees: Daiichi Pharmaceutical Co., Ltd., Kabushiki Kaisha Yakult HonshaInventors: Hiroaki Tagawa, Masamichi Sugimori, Hirofumi Terasawa, Akio Ejima, Satoru Ohsuki
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Patent number: 5049556Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH or O;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.Type: GrantFiled: August 2, 1989Date of Patent: September 17, 1991Assignee: Beecham Group p.l.c.Inventors: Francis D. King, Karen A. Joiner
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Patent number: 5021425Abstract: Use of 2-azabicyclo[2.2.2.]octane-3-carboxylic acid derivatives and their salts for the treatment of arteritis and more especially arteritis of the lower limbs, disorders of the cerebral circulation and more especially disorders of cerebral senescence and migraine, and disorders of vision such as retinal disorders of vascular origin, diabetic retinopathy, chorioretinal atrophy and chorioretinal degeneration.Type: GrantFiled: August 22, 1989Date of Patent: June 4, 1991Assignee: Adir et CompagnieInventor: Bernard Teisseire
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Patent number: 4990617Abstract: N-oxide prodrug derivatives of 3-hydroxy morphinan and partial morphinan analgesics, agonist-antogonists, and narcotic antagonists are useful therapeutic entities which provide enhanced bioavailability of 3-hydroxy morphinans and partial morphinans from orally administered dosage forms.Type: GrantFiled: July 27, 1989Date of Patent: February 5, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: George A. Boswell, Melvyn J. Myers
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Patent number: 4968341Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.Type: GrantFiled: August 16, 1988Date of Patent: November 6, 1990Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
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Patent number: 4939136Abstract: The invention relates to new anellated indole derivatives of general formula 2, ##STR1## wherein p1 R.sub.0 is alkyl or alkoxy having 1-4 C-atoms, phenylalkoxy having 1-3 C-atoms in the alkoxy group, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or a group R.sub.7 S(O).sub.p, wherein R.sub.7 is alkyl having 1-4 C-atoms and p has the value 0, 1 or 2, or R.sub.0 is a group R.sub.8 R.sub.9 N, R.sub.8 R.sub.9 N--CO--CH.sub.2 -- or R.sub.8 R.sub.9 --N--CO wherein R.sub.8 and R.sub.9 are hydrogen or alkyl having 1-4 C-atoms or R.sub.8 R.sub.9 N forms a saturated 5- or 6-membered ring and n has the value 0, 1 or 2, Z together with the carbon atom and nitrogen atom to which Z is bound and the intermediate carbon atom, forms a heterocyclic group consisting of 5-8 ring atoms, in which, in addition to the nitrogen atom already present, a --CO--group or a second hetero atom from the group N, O, S, S-O or SO.sub.Type: GrantFiled: June 24, 1988Date of Patent: July 3, 1990Assignee: Duphar International Research B.V.Inventors: Hans H. Haeck, Derk Hamminga, Ineke Van Wijngaarden, Wouter Wouters
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Patent number: 4937239Abstract: Novel 1-azabicycloalkane- and alkene-oximes (Ia) and 8-azabicyclo[3.2.1]octane- and octene-oximes (Ib) are provided, these compounds being useful as agents for treating pain or for treating the symptoms of senile cognitive decline. Also provided are pharmaceutical compositions containing the compounds and methods of treatment using the compounds in dosage form.Type: GrantFiled: February 13, 1989Date of Patent: June 26, 1990Assignee: Warner-Lambert CompanyInventors: David J. Lauffer, Walter H. Moos, Hasile Tecle
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Patent number: 4925937Abstract: The present invention relates to a process for the photocleavage of nucleic acids which consists in bringing a nucleic acid into contact with a solution of a 2,7-diazapyrene derivative and in subjecting the resulting reaction mixture to irradiation with visible light.Type: GrantFiled: December 15, 1987Date of Patent: May 15, 1990Assignee: Compagnie Oris IndustrieInventors: Jean M. Lehn, Jaroslaw Jazwinski, John Blacker