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)
  • Patent number: 9862683
    Abstract: 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: Grant
    Filed: December 8, 2016
    Date of Patent: January 9, 2018
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventor: Dongcheng Dai
  • Patent number: 9546137
    Abstract: 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: Grant
    Filed: August 14, 2013
    Date of Patent: January 17, 2017
    Assignee: Siga Technologies Inc.
    Inventor: Dongcheng Dai
  • Patent number: 9045418
    Abstract: 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: Grant
    Filed: July 3, 2014
    Date of Patent: June 2, 2015
    Assignee: SIGA TECHNOLOGIES, INC.
    Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin, Dongcheng Dai
  • Publication number: 20140316145
    Abstract: 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: Application
    Filed: July 3, 2014
    Publication date: October 23, 2014
    Applicant: SIGA TECHNOLOGIES, INC.,
    Inventors: Robert JORDAN, Thomas R. BAILEY, Susan R. RIPPIN, Dongcheng DAI
  • Publication number: 20130319610
    Abstract: 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: Application
    Filed: August 12, 2011
    Publication date: December 5, 2013
    Applicants: FORSCHUNGSZENTRUM JUELICH GMBH, Deutsches Krebsforschungszentrum
    Inventors: Marlen Fleischhacker, Nadja Fleischhacker, Karola Ursula Fleischhacker
  • Publication number: 20130274440
    Abstract: The present invention concerns a new dimedon derivative and a method for the purification of PNA and peptide oligomers.
    Type: Application
    Filed: April 8, 2013
    Publication date: October 17, 2013
    Inventors: Anette JACOB, Jörg HOHEISEL, Marc DAUBER, Manfred WIESSLER, Peter LORENZ, Heinz FLEISCHHACKER, Hans-Christian KLIEM
  • Patent number: 8486989
    Abstract: 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: Grant
    Filed: May 22, 2007
    Date of Patent: July 16, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie, Jr.
  • Patent number: 8124643
    Abstract: 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: Grant
    Filed: December 21, 2009
    Date of Patent: February 28, 2012
    Assignee: Siga Technologies, Inc.
    Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
  • Publication number: 20110236434
    Abstract: 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: Application
    Filed: March 23, 2011
    Publication date: September 29, 2011
    Applicant: 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
  • Patent number: 7956197
    Abstract: 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: Grant
    Filed: April 1, 2010
    Date of Patent: June 7, 2011
    Assignee: Siga Technologies, Inc.
    Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
  • Publication number: 20110009456
    Abstract: 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: Application
    Filed: December 21, 2009
    Publication date: January 13, 2011
    Applicant: Siga Technologies Inc.
    Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
  • Patent number: 7687641
    Abstract: 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: Grant
    Filed: April 23, 2007
    Date of Patent: March 30, 2010
    Assignee: Siga Technologies, Inc.
    Inventors: Robert F Jordan, Thomas R. Bailey, Susan R. Rippin, Dongcheng Dai
  • Patent number: 7446129
    Abstract: 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: Grant
    Filed: March 18, 2003
    Date of Patent: November 4, 2008
    Assignee: Biolipox AB
    Inventors: Ronald W Lauener, David L Burgoyne, Patrick J Rebstein, Lloyd F Mackenzie, Yuanlin Zhou, Yaping Shen
  • Patent number: 7241796
    Abstract: 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: Grant
    Filed: October 24, 2002
    Date of Patent: July 10, 2007
    Assignee: Vertex Pharmaceuticals Inc.
    Inventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie, Jr.
  • Patent number: 6849619
    Abstract: 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: Grant
    Filed: February 20, 2004
    Date of Patent: February 1, 2005
    Assignee: Bristol-Myers Squibb Company
    Inventors: Albert J. Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Publication number: 20040132758
    Abstract: 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 1
    Type: Application
    Filed: July 17, 2003
    Publication date: July 8, 2004
    Inventors: 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
  • Patent number: 6699852
    Abstract: 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: Grant
    Filed: December 19, 2001
    Date of Patent: March 2, 2004
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Albert Robichaud, John M. Fevig, Ian S. Mitchell, Taekyu Lee, Wenting Chen, Joseph Cacciola
  • Publication number: 20030134889
    Abstract: 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: Application
    Filed: October 24, 2002
    Publication date: July 17, 2003
    Inventors: Luc J. Farmer, Robert B. Perni, Janos Pitlik, John H. van Drie
  • Publication number: 20030087948
    Abstract: Compounds of the general formula I 1
    Type: Application
    Filed: October 18, 2002
    Publication date: May 8, 2003
    Inventors: Hakan Wikstrom, Durk Dijkstra, Bastiaan Johan Venhuis
  • Patent number: 6548493
    Abstract: 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: Grant
    Filed: June 15, 2000
    Date of Patent: April 15, 2003
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Albert J. Robichaud, Taekyu Lee, Wei Deng, Ian S. Mitchell, Wenting Chen, Christopher D. McClung, Emilie J. B. Calvello, David M. Zawrotny
  • Publication number: 20020119961
    Abstract: A compound of the formula 1
    Type: Application
    Filed: October 5, 2001
    Publication date: August 29, 2002
    Applicant: Pfizer Inc.
    Inventors: Laura C. Blumberg, Matthew F. Brown, Ronald P. Gladue, Christopher S. Poss
  • Patent number: 5364856
    Abstract: 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: Grant
    Filed: September 30, 1992
    Date of Patent: November 15, 1994
    Assignee: Eli Lilly and Company
    Inventors: Richard N. Booher, David E. Lawhorn, Charles J. Paget, Jr., John M. Schaus
  • Patent number: 5356885
    Abstract: 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: Grant
    Filed: April 24, 1991
    Date of Patent: October 18, 1994
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
  • Patent number: 5212170
    Abstract: 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: Grant
    Filed: May 13, 1992
    Date of Patent: May 18, 1993
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 5126363
    Abstract: 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: Grant
    Filed: January 23, 1991
    Date of Patent: June 30, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Lone Jeppesen, Peter H. Andersen, Louis B. Hansen, Peter Faarup, John B. Hansen
  • Patent number: 4939012
    Abstract: 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: Grant
    Filed: August 21, 1989
    Date of Patent: July 3, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Dust, Peter Neumann, Ernst Schefczik, Heidi Benthack-Thoms, Helmut Barzynski, Klaus-Dieter Schomann, Harald Kupplemaier, Eberhard Koester
  • Patent number: 4927934
    Abstract: 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: Grant
    Filed: May 5, 1989
    Date of Patent: May 22, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Usha R. Patel
  • Patent number: 4910302
    Abstract: 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: Grant
    Filed: December 19, 1988
    Date of Patent: March 20, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Gary P. Stack
  • Patent number: 4876356
    Abstract: 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: Grant
    Filed: March 12, 1987
    Date of Patent: October 24, 1989
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Dust, Peter Neumann, Ernst Schefczik, Heidi Benthack-Thoms, Helmut Barzynski, Klaus-Dieter Schomann, Harald Kuppelmaier, Eberhard Koester
  • Patent number: 4871656
    Abstract: 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: Grant
    Filed: March 10, 1988
    Date of Patent: October 3, 1989
    Assignee: Eastman Kodak Company
    Inventors: Richard L. Parton, ANthony D. Gingello, David J. Collett, David A. Stegman, ANthony Adin
  • Patent number: 4866073
    Abstract: 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: Grant
    Filed: October 22, 1987
    Date of Patent: September 12, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4866070
    Abstract: The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.
    Type: Grant
    Filed: December 11, 1987
    Date of Patent: September 12, 1989
    Assignee: Burroughs Wellcome Co.
    Inventor: Kenneth W. Bair
  • Patent number: 4801603
    Abstract: 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: Grant
    Filed: December 24, 1986
    Date of Patent: January 31, 1989
    Assignee: 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
  • Patent number: 4777254
    Abstract: 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: Grant
    Filed: December 2, 1986
    Date of Patent: October 11, 1988
    Assignee: American Home Products Corp.
    Inventors: Magid A. Abou-Gharbia, Susan T. Nielsen
  • Patent number: 4555563
    Abstract: 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: Grant
    Filed: December 7, 1984
    Date of Patent: November 26, 1985
    Assignee: The Dow Chemical Company
    Inventors: Robert E. Hefner, Jr., Mary N. White