Two Of The Cyclos Share At Least Three Ring Members, Or A Ring Carbon Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 548/424)
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Patent number: 9862683Abstract: Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: GrantFiled: December 8, 2016Date of Patent: January 9, 2018Assignee: SIGA TECHNOLOGIES, INC.Inventor: Dongcheng Dai
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Patent number: 9546137Abstract: Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: GrantFiled: August 14, 2013Date of Patent: January 17, 2017Assignee: Siga Technologies Inc.Inventor: Dongcheng Dai
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Patent number: 9045418Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: GrantFiled: July 3, 2014Date of Patent: June 2, 2015Assignee: SIGA TECHNOLOGIES, INC.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin, Dongcheng Dai
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Publication number: 20140316145Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: July 3, 2014Publication date: October 23, 2014Applicant: SIGA TECHNOLOGIES, INC.,Inventors: Robert JORDAN, Thomas R. BAILEY, Susan R. RIPPIN, Dongcheng DAI
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Publication number: 20130319610Abstract: The present invention concerns a method for applying a first metal onto a second metal, an isolator or semiconductor substrate by a Diels-Alder reaction, in particular a Diels-Alder reaction with inverse electron demand. The present invention further concerns the binding units L 1960 and F 160.Type: ApplicationFiled: August 12, 2011Publication date: December 5, 2013Applicants: FORSCHUNGSZENTRUM JUELICH GMBH, Deutsches KrebsforschungszentrumInventors: Marlen Fleischhacker, Nadja Fleischhacker, Karola Ursula Fleischhacker
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Publication number: 20130274440Abstract: The present invention concerns a new dimedon derivative and a method for the purification of PNA and peptide oligomers.Type: ApplicationFiled: April 8, 2013Publication date: October 17, 2013Inventors: Anette JACOB, Jörg HOHEISEL, Marc DAUBER, Manfred WIESSLER, Peter LORENZ, Heinz FLEISCHHACKER, Hans-Christian KLIEM
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Patent number: 8486989Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: GrantFiled: May 22, 2007Date of Patent: July 16, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie, Jr.
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Patent number: 8124643Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: GrantFiled: December 21, 2009Date of Patent: February 28, 2012Assignee: Siga Technologies, Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Publication number: 20110236434Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.Type: ApplicationFiled: March 23, 2011Publication date: September 29, 2011Applicant: Siga Technologies, Inc.Inventors: Shanthakumar R. Tyavanagimatt, Melialani A.C.L. Stone, William C. Weimers, Dylan Nelson, Tove' C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
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Patent number: 7956197Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: GrantFiled: April 1, 2010Date of Patent: June 7, 2011Assignee: Siga Technologies, Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Publication number: 20110009456Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: December 21, 2009Publication date: January 13, 2011Applicant: Siga Technologies Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Patent number: 7687641Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases cased by the orthopoxvirus.Type: GrantFiled: April 23, 2007Date of Patent: March 30, 2010Assignee: Siga Technologies, Inc.Inventors: Robert F Jordan, Thomas R. Bailey, Susan R. Rippin, Dongcheng Dai
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Patent number: 7446129Abstract: The present invention is directed to a method for reducing the emetogenic effects of PDE inhibitors, and more particularly is directed to compounds having PDE4 inhibition activity with little or no emetogenic side-effects, and chemical methods including benzylation for preparing such compounds. A benzyl group may be attached to either a carbon or nitrogen atom of a PDE4 inhibitor. Suitable benzylation chemistry is to extract a hydrogen from a PDE4 inhibitor, preferably with a base, and then react the resulting nucleophilic PDE4 inhibitor with a benzylating agent, e.g., benzyl bromide or a derivative thereof.Type: GrantFiled: March 18, 2003Date of Patent: November 4, 2008Assignee: Biolipox ABInventors: Ronald W Lauener, David L Burgoyne, Patrick J Rebstein, Lloyd F Mackenzie, Yuanlin Zhou, Yaping Shen
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Patent number: 7241796Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3–NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: GrantFiled: October 24, 2002Date of Patent: July 10, 2007Assignee: Vertex Pharmaceuticals Inc.Inventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie, Jr.
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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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Publication number: 20040132758Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure 1Type: ApplicationFiled: July 17, 2003Publication date: July 8, 2004Inventors: Wayne Vaccaro, Bingwei Vera Yang, Soong-Hoon Kim, Tram Huynh, David R. Tortolani, Kenneth J. Leavitt, Wenying Li, Arthur M. Doweyko, Xiao-Tao Chen, Lidia Doweyko
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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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Publication number: 20030134889Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: ApplicationFiled: October 24, 2002Publication date: July 17, 2003Inventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie
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Publication number: 20030087948Abstract: Compounds of the general formula I 1Type: ApplicationFiled: October 18, 2002Publication date: May 8, 2003Inventors: Hakan Wikstrom, Durk Dijkstra, Bastiaan Johan Venhuis
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Patent number: 6548493Abstract: The present invention is directed to certain novel compounds represented by structural Formula (I) or pharmaceutically acceptable salt forms thereof, wherein R1, R5, R6a, R6b, R7, R8, R9, X, b, k, m, 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: June 15, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrotny
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Publication number: 20020119961Abstract: A compound of the formula 1Type: ApplicationFiled: October 5, 2001Publication date: August 29, 2002Applicant: Pfizer Inc.Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Christopher S. Poss
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Patent number: 5364856Abstract: 6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[cd]indoles are provided which are useful in modifying the function of serotonin in mammals.Type: GrantFiled: September 30, 1992Date of Patent: November 15, 1994Assignee: Eli Lilly and CompanyInventors: Richard N. Booher, David E. Lawhorn, Charles J. Paget, Jr., John M. Schaus
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Patent number: 5356885Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.Type: GrantFiled: April 24, 1991Date of Patent: October 18, 1994Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
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Patent number: 5212170Abstract: The compounds ##STR1## in which Z is ##STR2## where R.sup.4 is --H or alkyl; q is one of the integers 0, 1 or 2; Y is H.sub.2 or O; or Z, taken with R.sup.1 forms ##STR3## R.sup.1 is hydrogen or alkyl or combined with Z as described above; R.sup.2 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, carbamoyl or sulfonamido or R.sup.2 and R.sup.3, taken together are methylenedioxy, ethylenedioxy or propylenedioxy; m is one of the integers 1, 2 or 3; n is one of the integers 0 or 1; or a pharmaceutically acceptable salt thereof are antipsychotic, antidepressant and anxiolytic agents useful in relieving the symptoms of these disease states.Type: GrantFiled: May 13, 1992Date of Patent: May 18, 1993Assignee: American Home Products CorporationInventor: Gary P. Stack
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Patent number: 5126363Abstract: Indole derivatives of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be hydrogen or lower alkyl optionally substituted by halogen; A.sup.1 represents a straight or branched alkylene chain containing from 2 to 4 carbon atoms; R.sup.5 is hydrogen or a straight or branched alkyl group; A.sup.2 is a straight or branched, saturated or unsaturated hydrocarbon chain containing from 2 to 6 carbon atoms; and R.sup.6 is selected from a group consisting of various structures, have been found to exhibit central nervous system activities.Type: GrantFiled: January 23, 1991Date of Patent: June 30, 1992Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen
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Patent number: 4939012Abstract: Naphtholactam dyes of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, n, p, Z.sup.1, Z.sup.2 and the rings A, B, C and D each have the meanings stated in the description, and an optical recording medium which contains one or more naphtholactam dyes and may contain a base.Type: GrantFiled: August 21, 1989Date of Patent: July 3, 1990Assignee: BASF AktiengesellschaftInventors: Matthias Dust, Peter Neumann, Ernst Schefczik, Heidi Benthack-Thoms, Helmut Barzynski, Klaus-Dieter Schomann, Harald Kupplemaier, Eberhard Koester
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Patent number: 4927934Abstract: There are disclosed compounds of the formula ##STR1## wherein R represents ##STR2## where X is lower alkylene, vinylene or O;Y is lower alkylene or vinylene;the dotted line represents an optional double bond;m is 1-3;n is 2-4;A is phenyl, benzoyl, pyridinyl, quinolinyl or quinoxalinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl; or when m is>1, A represents the grouping ##STR3## where B is phenyl, pyrimidinyl, pyridinyl or pyrazinyl, or any of the foregoing substituted with lower alkyl, lower alkoxy, halo, cyano, nitro or trifluoromethyl, with the proviso that were R is ##STR4## A is other than unsubstituted or substituted benzoyl or pyridinyl; and the pharmacologically acceptable salts thereof and their use as antipsychotic/anxiolytic and antidepressant agents and in the treatment of sexual dysfunction and having a low liability for extrapyramidal side effects.Type: GrantFiled: May 5, 1989Date of Patent: May 22, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Usha R. Patel
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Patent number: 4910302Abstract: Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring or a substituted benzene ring, in which said substituents are --OH, --OCH.sub.3, alkyl, halo, --CF.sub.3, --NH.sub.2, monoalkylamino, dialkylamino or alkanoylamino; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl or taken together with the carbon atoms to which they are attached, they form a cycloalkane or cycloalkene ring; m is one of the integers 2-5; R.sup.4 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, amino, alkylamino, phenylamino, tolylamino, xylylamino, mesitylamino, methoxyphenylamino, or halophenylamino; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 19, 1988Date of Patent: March 20, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Gary P. Stack
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Patent number: 4876356Abstract: Naphtholactam dyes of the formula ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, n, p, Z.sup.1, Z.sup.2 and the rings A, B, C and D each have the meanings stated in the description, and an optical recording medium which contains one or more naphtholactam dyes and may contain a base.Type: GrantFiled: March 12, 1987Date of Patent: October 24, 1989Assignee: BASF AktiengesellschaftInventors: Matthias Dust, Peter Neumann, Ernst Schefczik, Heidi Benthack-Thoms, Helmut Barzynski, Klaus-Dieter Schomann, Harald Kuppelmaier, Eberhard Koester
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Patent number: 4871656Abstract: A dye useful for absorbing infrared radiation in photographic elements, having the structure: ##STR1## is disclosed. In this formula, R.sub.1 and R.sub.2 each independently represents sulfoalkyl, carboxyalkyl, or sulfatoalkyl, from 2 to 4 carbon atoms, having 2 carbon atoms in the alkyl chain linking the nitrogen atom of each Z ring and the sulfo or sulfato group, and 1 carbon atom in the alkyl chain linking the nitrogen atom of each Z ring and the carboxy group.R.sub.3 and R.sub.5 are each hydrogen or together represent the atoms necessary to complete a 5- or 6-membered carbocyclic ring, and R.sub.4 represents hydrogen, alkyl of 1 to 4 carbon atoms, halogen, cyano, or ##STR2## where R.sub.6 and R.sub.7 each independently represents alkyl of from 1 to 6 carbon atoms or aryl or together represent the non-metallic atoms necessary to form a 5- or 6-membered heterocyclic ring.X.sup..sym. represents a cation.Z.sub.1 and Z.sub.Type: GrantFiled: March 10, 1988Date of Patent: October 3, 1989Assignee: Eastman Kodak CompanyInventors: Richard L. Parton, ANthony D. Gingello, David J. Collett, David A. Stegman, ANthony Adin
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Patent number: 4866073Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a C.sub.8-13 fused heterotricyclic ring system containing at least two aromatic rings and no more than 3 heteroatoms (in separate rings), or a C.sub.10-17 fused heterotetracyclic ring system containing at least two aromatic rings and no more than 4 heteroatoms (in separate rings) or a C.sub.Type: GrantFiled: October 22, 1987Date of Patent: September 12, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4866070Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.Type: GrantFiled: December 11, 1987Date of Patent: September 12, 1989Assignee: Burroughs Wellcome Co.Inventor: Kenneth W. Bair
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Patent number: 4801603Abstract: A guanidinobenzoic ester derivative having the formula is novel and effective to inhibit enzymes such as trypsin, plasmin and thrombin, being useful for treatment of the pancreatitis and hemorrhagic disease and thrombosis. ##STR1## wherein X represents a group of the formula: ##STR2## in which Y is a group of the formula: --(CH.sub.2).sub.m --, m being an integer of 2 or 3, ##STR3## or a group of the formula:--ORin which R is a hydrogen atom or a lower alkyl group, and n represents an integer of 1 to 5.Type: GrantFiled: December 24, 1986Date of Patent: January 31, 1989Assignee: Eisai Co., Ltd.Inventors: Shigeru Souda, Naoyuki Shimomura, Norihiro Ueda, Shuhei Miyazawa, Takashi Yamanaka, Kaname Miyamoto, Ieharu Hishinuma, Junichi Nagakawa, Naoko Nagaoka, Hidetoshi Kawashima, Tsutomu Kawata, Junsaku Nagaoka, Tsuneo Wakabayashi
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Patent number: 4777254Abstract: Polycyclic 1,3-dione imides N-alkylated with variously N-substituted alkyl- or cycloalkyl amines afford histamine H.sub.1 -receptor antagonists of the formula ##STR1## wherein R is polycyclic alkyl moiety;R.sup.1 is hydrogen or alkyl;R.sup.4 is an aromatic amine or a cycloalkyl amine containing N-substitution;R.sup.7 and R.sup.8 are hydrogen, alkyl or form a spiro cycloalkyl group.Type: GrantFiled: December 2, 1986Date of Patent: October 11, 1988Assignee: American Home Products Corp.Inventors: Magid A. Abou-Gharbia, Susan T. Nielsen
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Patent number: 4555563Abstract: Imide functional polyphenols are prepared by reacting an excess of a phenol with an unsaturated diimide which is prepared by reacting an unsaturated polycycloaliphatic dicarboxylic acid anhydride with a diamine.These materials are useful in the preparation of castings, coatings, laminates and the like.Type: GrantFiled: December 7, 1984Date of Patent: November 26, 1985Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Mary N. White