The Hetero Ring Contains At Least Three Nitrogens Patents (Class 540/554)
  • Patent number: 9353456
    Abstract: The present invention provides a process for obtaining a charge of hexanitrohexaazaisowurtzitane crystals having rounded morphology. It also provides said charge, the energetic material comprising it, and a process for manufacturing said material. Said process for obtaining said charge comprises: preparing a saturated solution of any polymorphic form of hexanitrohexaazaisowurtzitane in a mixture comprising both an organic solvent for said hexanitrohexaazaisowurtzitane and an organic nonsolvent for said hexanitrohexaazaisowurtzitane, said solvent being more volatile than said nonsolvent; seeding this saturated solution with a few hexanitrohexaazaisowurtzitane crystals; and then concentrating the seeded, saturated solution by at least partial evaporation of the solvent, said evaporation of the solvent being performed at a temperature of between 35° C. and 15° C.
    Type: Grant
    Filed: April 5, 2012
    Date of Patent: May 31, 2016
    Assignees: HERAKLES, EURENCO
    Inventors: Florent Muscatelli, Philippe Lescop
  • Patent number: 9227981
    Abstract: The present invention relates to a method of preparation of ?-2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane with reduced impact sensitivity by precipitation of a solution of 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane in a solvent by an antisolvent, wherein phosphorus(V) oxide is added as a recrystallization promoter to the solution of 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane in the solvent, the obtained mixture is stirred and filtered, and the filtrate is subsequently precipitated by the addition of the antisolvent.
    Type: Grant
    Filed: October 1, 2012
    Date of Patent: January 5, 2016
    Assignee: UNIVERSITY OF PARDUBICE
    Inventors: Ahmed Ikhlas Mohamed Elbeih, Adela Husarova, Svatopluk Zeman
  • Patent number: 9056868
    Abstract: Embodiments of the invention relate to the synthesis of CL-20 using only a three step synthesis and because of increased catalyst activity and lifetimes, a continuous flow process can be used with a tremendous reduction in total cost of producing CL-20.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: June 16, 2015
    Assignee: The United States of America as Represented by the Secretary of the Navy
    Inventor: Michael E. Wright
  • Publication number: 20140341986
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: August 4, 2014
    Publication date: November 20, 2014
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
  • Publication number: 20140235853
    Abstract: The present invention relates to a method of preparation of ?-2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane with reduced impact sensitivity by precipitation of a solution of 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane in a solvent by an antisolvent, wherein phosphorus(V) oxide is added as a recrystallization promoter to the solution of 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane in the solvent, the obtained mixture is stirred and filtered, and the filtrate is subsequently precipitated by the addition of the antisolvent.
    Type: Application
    Filed: October 1, 2012
    Publication date: August 21, 2014
    Applicant: UNIVERSITY OF PARDUBICE
    Inventors: Ahmed Ikhlas Mohamed Elbeih, Adela Husarova, Svatopluk Zeman
  • Patent number: 8785625
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A, X1, Ring B and R1 are as described in the description, and an antibacterial agent containing the same.
    Type: Grant
    Filed: February 14, 2012
    Date of Patent: July 22, 2014
    Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.
    Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
  • Publication number: 20140148339
    Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides and herbicides.
    Type: Application
    Filed: June 22, 2012
    Publication date: May 29, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Tomas Smejkal, Michel Muehlebach
  • Publication number: 20140073781
    Abstract: The present invention provides a process for obtaining a charge of hexanitrohexaazaisowurtzitane crystals having rounded morphology. It also provides said charge, the energetic material comprising it, and a process for manufacturing said material. Said process for obtaining said charge comprises: preparing a saturated solution of any polymorphic form of hexanitrohexaazaisowurtzitane in a mixture comprising both an organic solvent for said hexanitrohexaazaisowurtzitane and an organic nonsolvent for said hexanitrohexaazaisowurtzitane, said solvent being more volatile than said nonsolvent; seeding this saturated solution with a few hexanitrohexaazaisowurtzitane crystals; and then concentrating the seeded, saturated solution by at least partial evaporation of the solvent, said evaporation of the solvent being performed at a temperature of between 35° C. and 15° C.
    Type: Application
    Filed: April 5, 2012
    Publication date: March 13, 2014
    Applicants: EURENCO, HERAKLES
    Inventors: Florent Muscatelli, Philippe Lescop
  • Publication number: 20130324536
    Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: December 8, 2011
    Publication date: December 5, 2013
    Applicant: Lycera Corporation
    Inventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
  • Patent number: 8530646
    Abstract: The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Rings A and B are defined as in the specification; X1is a single bond, or a heteroatom-containing group selected from the group consisting of —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SONR5—, and NR6SO2—, wherein R2, R3, R4, R5, and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom containing group; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolidinone antimicrobial agents, pharmaceutically acceptable salts and solvates thereof which are useful as an antibacterial agent.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: September 10, 2013
    Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.
    Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
  • Publication number: 20130150809
    Abstract: An antimicrobial coating system and method are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two of the cyclic groups may include quaternary ammonium moieties. In some embodiments, a method may include applying an antimicrobial coating to an oral surface, a surface of a construction substrate, a surface of a marine substrate, a surface of a medical device, or a surface of a personal care device. The protective coating may be antimicrobial. A protective coating may include antimicrobial bridged polycyclic compounds. Bridged polycyclic compounds may include quaternary ammonium compounds. Bridged polycyclic compounds based coating systems may impart self-cleaning properties to a surface (e.g., a tooth surface).
    Type: Application
    Filed: September 17, 2012
    Publication date: June 13, 2013
    Inventors: Jeffery A. Whiteford, William P. Freeman
  • Patent number: 8426583
    Abstract: A heavy-metal-free sequence leading to a superior, more economical, and scalable process for the high efficiency conversion of hexaallylhexaazaisowurtzitane (HAllylIW) to hexanitohexaazaisowurtzitane (CL-20).
    Type: Grant
    Filed: December 30, 2010
    Date of Patent: April 23, 2013
    Inventors: Robert D. Chapman, Richard A. Hollins
  • Patent number: 8426582
    Abstract: A heavy-metal-free sequence leading to a superior, more economical, and scalable process for the high efficiency conversion of hexaallylhexaazaisowurtzitane (HAllylIW) to hexanitrohexaazaisowurtzitane (CL-20).
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: April 23, 2013
    Assignee: The United States of America as Represented by the Secretary of the Navy
    Inventors: Robert D. Chapman, Richard A. Hollins
  • Publication number: 20130095140
    Abstract: Provided herein are methods for treating certain conditions, including diabetes, obesity, and other metabolic diseases, disorders or conditions by administrating a composition comprising a biguanide or related heterocyclic compound, e.g., metformin. Also provided herein are biguanide or related heterocyclic compound compositions, and methods for the preparation thereof for use in the methods of the present invention. Also provided herein are compositions comprising metformin and salts thereof and methods of use.
    Type: Application
    Filed: July 11, 2012
    Publication date: April 18, 2013
    Applicant: Elcelyx Therapeutics, Inc.
    Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
  • Publication number: 20120238546
    Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the Formula (I): Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of Formula (I).
    Type: Application
    Filed: June 15, 2010
    Publication date: September 20, 2012
    Inventors: Zhaoning Zhu, Xianhai Huang, Anandan Palani, William J. Greenlee, Robert G. Aslanian
  • Patent number: 8268991
    Abstract: The present invention describes a novel heavy-metal-free sequence leading to a superior, more economical, and scalable process for the high efficiency conversion of hexaallylhexaazaisowurtzitane (HAllylIW) to hexa(1-propenyl)hexaazaisowurtzitane (HPIW) and hence via reaction with singlet oxygen and subsequent nitrolysis to hexanitrohexaazaisowurtzitane (CL-20).
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: September 18, 2012
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Robert D. Chapman, Richard A. Hollins
  • Patent number: 8268993
    Abstract: A heavy-metal-free sequence leading to a superior, more economical, and scalable process for the high efficiency conversion of hexaallylhexaazaisowurtzitane (HAllylIW) to hexanitrohexaazaisowurtzitane (CL-20).
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: September 18, 2012
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventor: Robert D. Chapman
  • Publication number: 20120208997
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A, X1, Ring B and R1 are as described in the description, and an antibacterial agent containing the same.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 16, 2012
    Inventors: Hideyuki SUZUKI, Shoji HIZATATE, Iwao UTSUNOMIYA, Koichi SHUDO
  • Publication number: 20120199256
    Abstract: The present invention relates to suspensions of hexanitrohexaazaisowurtzitane crystals in a liquid phase (said liquid phase is composed, to at least 85% by weight, of a nonsolvent for hexanitrohexaazaisowurtzitane, said nonsolvent consisting of at least one nonflammable hydrofluoroether, and includes from 0 to less than 15% by weight of an organic solvent for hexanitrohexaazaisowurtzitane, more volatile than said nonsolvent, chosen from the group consisting of esters, nitriles, ketones and their mixtures), the production of said suspensions and their use to manufacture pyrotechnic objects. The use of said at least one hydrofluoroether as nonsolvent is particularly appropriate.
    Type: Application
    Filed: September 28, 2010
    Publication date: August 9, 2012
    Applicants: EURENCO, SME
    Inventors: Florent Muscatelli, Philippe Lescop
  • Patent number: 8202854
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: June 19, 2012
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
  • Publication number: 20120129846
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: November 5, 2009
    Publication date: May 24, 2012
    Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
  • Patent number: 8148362
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: April 3, 2012
    Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.
    Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
  • Patent number: 8133993
    Abstract: A method for synthesizing pentanitrohexaazaisowurtzintane under neutral reaction conditions. Which synthesis involves treating a solution of hexanitrohexaazaisowurtzitane in ethyl acetate in the presence of a catalytic quantity of palladium on a carbon substrate, until a heterogeneous mixture is formed. This heterogeneous mixture is hydrogenated under a balloon atmosphere until the starting hexanitrohexaazaisowurtzitane is substantially reacted. The resulting pentanitrohexaazaisowurzitane mixture is filtered, dried and recovered from the dried residue through a Si-gel column.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: March 13, 2012
    Assignee: The United States of America as represented by the Secretary of the Army
    Inventors: Raja Duddu, Paritosh Dave, Reddy Damavarapu, Rao Surapaneni
  • Publication number: 20120059010
    Abstract: The invention provides ?-helix mimetic structures and a chemical library relating thereto. The compounds, pharmaceutical compositions comprising the compounds, and methods of the invention using the compounds, relate to the treatment of diseases including fibrosis, such as pulmonary fibrosis.
    Type: Application
    Filed: March 28, 2011
    Publication date: March 8, 2012
    Applicant: Institute for Chemical Genomics
    Inventors: Michael Kahn, Masakatsu Eguchi
  • Patent number: 8063032
    Abstract: Provided herein are fused imidazolyl compounds, methods of synthesis, and methods of use thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders and metabolic disorders. Compounds provided herein inhibit the activity of histamine H3 receptors and modulate the release of various neurotransmitters, such as histamine, acetylcholine, norepinephrine, and dopamine (e.g. at the synapse). Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: November 22, 2011
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Milan Chytil, Qun Kevin Fang, Kerry L. Spear
  • Publication number: 20110280867
    Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.
    Type: Application
    Filed: July 27, 2011
    Publication date: November 17, 2011
    Applicant: Schering Corporation
    Inventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
  • Patent number: 8017768
    Abstract: An improved method of preparing 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazaisowurtzitane (2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.05,9.03,11]dodecane) (HNIW) is disclosed. The compound is useful as a high energy, high density explosive or propellant oxidizer.
    Type: Grant
    Filed: April 5, 1994
    Date of Patent: September 13, 2011
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: William P. Norris, Arnold T. Nielsen
  • Patent number: 7875714
    Abstract: The present invention describes a novel heavy-metal-free sequence leading to a superior, more economical, and scalable process for the high efficiency conversion of hexaallylhexaazaisowurtzitane (HAllylIW) to hexanitrohexaazaisowurtzitane (CL-20). The process of the present invention avoids both the preparation of benzyl chloride, which uses elemental chlorine, and catalytic hydrogenolysis steps that require palladium metal/compounds. It is emphasized that this abstract is provided to comply with the rules requiring an abstract that will allow a searcher or other reader to quickly ascertain the subject matter of the technical disclosure. It is submitted with the understanding that it will not be used to interpret or limit the scope of the claims.
    Type: Grant
    Filed: April 23, 2007
    Date of Patent: January 25, 2011
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Robert D. Chapman, Richard A. Hollins
  • Publication number: 20100256355
    Abstract: The present invention provides a novel oxazolidinone derivative of the formula (I): wherein Ring A is (A-1) a 7-membered monocyclic heterocycle containing three N atoms; (A-2) a 7-membered monocyclic heterocycle containing two N atoms and one O atom; or (A-3) a 7-membered monocyclic heterocycle containing two N atoms and one S atom, SO or SO2, wherein said monocyclic heterocycle is optionally substituted, optionally unsaturated and optionally fused with another ring; X1 is a single bond, or a heteroatom-containing group selected from the group consisting of —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2—, wherein R2, R3, R4, R5 and R6 are independently hydrogen or lower alkyl, or lower alkylene or lower alkenylene each optionally interrupted by said heteroatom-containing group; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; and R1 is hydrogen, or an organic residue which is able to bind to the 5-position of the oxazolidinone ring in oxazolid
    Type: Application
    Filed: October 1, 2008
    Publication date: October 7, 2010
    Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
  • Patent number: 7759354
    Abstract: The present application provides compounds of the Formula: and stereoisomers, tautomers, or pharmaceutically acceptable salts and solvates thereof, wherein U, W, R, R1, R2, R3 and R4 in each formula (when present) are as defined in the specification, and pharmaceutical compositions comprising such compounds. Also disclosed are methods of using such compounds and compositions to inhibit aspartyl protease, and to treat a variety of disease and indications including (but not limited) to cardiovascular disease and cognitive and neurodegenerative disease. The compounds of the present invention are disclosed for use alone or in combination with one or more additional active ingredients such as cholinesterase inhibitors and a muscarinic m1 agonist and/or m2 antagonists.
    Type: Grant
    Filed: June 12, 2006
    Date of Patent: July 20, 2010
    Assignee: Schering Corporation
    Inventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
  • Patent number: 7737272
    Abstract: Transition metal complexes include a diazaphosphacycle of formula III and a transition metal. The phosphorus atom of the diazaphosphacycle is bonded to the transition metal and the diazaphosphacycle of formula III has the following structure where the variables have the values set forth herein.
    Type: Grant
    Filed: February 15, 2008
    Date of Patent: June 15, 2010
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
  • Patent number: 7709467
    Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
    Type: Grant
    Filed: May 15, 2008
    Date of Patent: May 4, 2010
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
  • Publication number: 20090299059
    Abstract: The invention provides a novel oxazolidinone derivative represented by the formula (I): wherein Ring A is optionally substituted or fused and represents (A-1) at least 7-membered monocyclic hetero ring containing at least three N atoms; (A-2) at least 6-membered monocyclic hetero ring containing at least two N atoms and at least one O atom; or (A-3) at least 7-membered monocyclic hetero ring containing at least two N atoms and at least one S atom; X1 is a single bond, —O—, —S—, —NR2—, —CO—, —CS—, —CONR3—, —NR4CO—, —SO2NR5—, and —NR6SO2— (wherein R2-R6 are independently hydrogen or lower alkyl), or lower alkylene or lower alkenylene in which one of the preceding groups may intervene; Ring B is optionally substituted carbocycle or optionally substituted heterocycle; R1 is hydrogen, or an organic residue which is able to bind to the 5-position of oxazolidinone ring in oxazolidinone antimicrobial agent, and an antibacterial agent containing the same.
    Type: Application
    Filed: March 30, 2007
    Publication date: December 3, 2009
    Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
  • Patent number: 7592448
    Abstract: The invention describes the synthesis of novel mono-amine and di-amine derivatives of hexa-nitro-hexaazaisohexawurtzitane (CL-20). The synthesis is affected by the novel use of fluoroacylating compounds to protect the secondary amine groups of acylated precursors to CL-20 against nitrolysis. In so doing the mono-amine and di-amine derivatives of CL-20 are rendered and which in turn may be subsequently utilized as intermediates to generate further novel derivatives with differing physical and chemical properties to the parent compound. Formula (I), wherein: —X?H, and Y?H or NO2.
    Type: Grant
    Filed: March 1, 2004
    Date of Patent: September 22, 2009
    Assignee: The Secretary of State for Defence in Her Britannic Majesty's Government of the United Kingdon of Great Britain and Northern Ireland
    Inventors: Peter Golding, Alistair J Maccuish, Anthony John Bellamy
  • Patent number: 7465722
    Abstract: A compound of the formulae (I) or (II): wherein: Y is a moiety selected from NR or —(CH2)n; wherein R is hydrogen or (C1-C6) lower alkyl, and n is 1; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 6-membered aromatic (unsaturated) heterocyclic ring having one nitrogen atom, optionally substituted by (C1-C6) lower alkyl, halogen or (C1-C6) lower alkoxy; represents: (1) a phenyl ring optionally substituted with one or two substituents selected, independently, from the group comprising hydrogen, (C1-C6) lower alkyl, halogen, cyano, CF3, hydroxy, (C1-C6) lower alkoxy, or (C1-C6) lower alkoxy carbonyl, carboxy, —CONH2, —CONH[(C1-C6) lower alkyl], —CON[(C1-C6) lower alkyl]2; or (2) a 5-membered aromatic (unsaturated
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: December 16, 2008
    Assignee: Wyeth
    Inventors: Amedeo A. Failli, John P. Dusza, Thomas J. Caggiano, Jay S. Shumsky, Kevin A. Memoli, Eugene J. Trybulski
  • Publication number: 20080262222
    Abstract: Near infrared (NIR) dyes, image recording substrate including the NIR dye, and methods of making the NIR dyes, are disclosed.
    Type: Application
    Filed: April 23, 2007
    Publication date: October 23, 2008
    Inventors: Vladek Kasperchik, Vyacheslav Olkhovik, Andreii Pap, Dimitriy Vasilevskii, Cari L. Dorsh, Sterling Chaffins
  • Publication number: 20080261951
    Abstract: This invention provides novel compounds according to general formula (1) wherein A is a bicyclic or tricyclic azepine derivative, V1 and V2 are both H, OMe or F, or one of V1 and V2 is Br, Cl, F, OH, OMe, OBn, OPh, O-acyl, N3, NH2, NHBn or NH-acyl and the other is H, or V1 and V2 together are ?O, —O(CH2)pO— or —S(CH2)S—; W1 is either O or S; X1 and X2 are both H, or together are ?O or ?S; Y is OR5 or NR6R7; R1, R2, R3 and R4 are independently selected from H, lower alkyl, lower alkyloxy, F, Cl and Br; R5 is selected from H and lower alkyl; R6 and R7 are independently selected from H and lower alkyl, or together are —(CH2)n—; n=3, 4, 5, 6; and p is 2 or 3. The compounds are agonists at the vasopressin V2 receptor and are useful as antidiuretics and procoagulants. The invention further comprises pharmaceutical compositions incorporating these vasopressin agonists, which compositions are particularly useful in the treatment of central diabetes insipidus, nocturnal enuresis and nocturia.
    Type: Application
    Filed: June 23, 2008
    Publication date: October 23, 2008
    Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
  • Publication number: 20080249080
    Abstract: The invention concerns benzodiazepine derivatives of formula wherein Y it is SO2 or NR, wherein R is H or C1-C6 alkyl; X is H, C1-C12 alkyl, —CO, —SO, —SO2, or —CO—R2, SO—R2, SO2—R2, wherein R2 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, phenyl, benzyl, naphtyl, biphenyl, or heterocycle, each para-, meta- or ortho-substituted independently of each other with 0 to 3 substituents selected from halogen, —CN, —NH2, —OH, —NO2, COOR3, wherein R3 is selected from H, C1-C12 alkyl, (C3-C8 cycloalkyl) C0-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, or C2-C6 alkoxy carbonyl; phenyl, benzyl, naphtyl, biphenyl, or heterocycle n is 0-6; R4 is selected from H, OH, COOH, CN, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, C2-C6 alkoxycarbonyl, —CO, —SO, —SO2, or —CO—R5, SO—R5, SO2—R2, —OCO—R5, OSO—R5, SO2—R5, COOR5, SOOR5, SO2OR5, NHR5, NHCOR5, NHSO2R5, SR5, SCOR5, wherein R5 is selected from H, C1-C6 alkyl, C1-C6 alkoxy, C2-C6
    Type: Application
    Filed: May 26, 2006
    Publication date: October 9, 2008
    Inventors: Romano Silvestri, Gabriella Marfe', Elisabetta Abruzzese, Gianfranco Catalano, Carla Di Stefano, Ettore Novellino, Paola Sinibaldi Salimei, Maria Gabriella De Martino, Giuseppe La Regina, Antonio La-Vecchia
  • Patent number: 7407949
    Abstract: Novel compounds according to general formula 1, wherein G1 is NR5R6 or a fused polycyclic group that are specific OT receptor agonists and/or V1a receptor antagonists. Pharmaceutical compositions comprising such compounds are useful in the treatment of, inter alia, primary dysmenorrhoea.
    Type: Grant
    Filed: February 12, 2004
    Date of Patent: August 5, 2008
    Assignee: Ferring B.V.
    Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
  • Patent number: 7390799
    Abstract: Compounds which inhibit the activity of anti-apoptotic family protein members, compositions containing the compounds and methods of treating diseases during which occur expression one or more than one of an anti-apoptotic family protein member are disclosed.
    Type: Grant
    Filed: May 12, 2006
    Date of Patent: June 24, 2008
    Assignee: Abbott Laboratories
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
  • Patent number: 7329653
    Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl; “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.
    Type: Grant
    Filed: April 11, 2006
    Date of Patent: February 12, 2008
    Assignee: Wyeth
    Inventors: Amedeo A. Failli, Jay S. Shumsky, Thomas J. Caggiano, John P. Dusza, Kevin A. Memoli
  • Patent number: 7288648
    Abstract: A method of crystallizing an epsilon-polymorph of 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.05,903,11]-dodecane (CL-20). The method comprises combining the CL-20, at least one organic solvent, and at least one nonsolvent to form a crystallization solution. The crystallization solution is saturated and heated to a temperature greater than about 60° C., such as from about 71° C. to about 94° C. The organic solvent is removed from the crystallization solution while retaining a sufficient amount of the nonsolvent to crystallize the CL-20 as the epsilon-polymorph. The nonsolvent is separated from the epsilon-polymorph of CL-20. A composition of CL-20 comprising the epsilon-polymorph having a particle density of 2.035 g/ml is also disclosed.
    Type: Grant
    Filed: August 6, 2003
    Date of Patent: October 30, 2007
    Assignee: Alliant Techsystems Inc.
    Inventors: R. Scott Hamilton, Vincent Mancini, Clint Nelson, Sharon Yeung Dressen
  • Patent number: 7279572
    Abstract: A subject-matter of the present invention is a novel process for the synthesis of hexanitrohexaazaisowurtzitane (HNIW), a compound of use as energetic filler in powders, propellants and explosives. This process comprises a first stage of reaction of an ?,?-dicarbonyl derivative with a primary amine which makes it possible to form a hexasubstituted hexaazaisowurtzitane derivative. The HNIW is subsequently obtained directly, in a single reaction stage, by nitration of the hexasubstituted hexaazaisowurtzitane derivative. This process, in only 2 stages starting from a primary amine, is particularly simple and inexpensive.
    Type: Grant
    Filed: April 28, 2004
    Date of Patent: October 9, 2007
    Assignee: SNPE Materiaux Energetiques
    Inventors: Guy Cagnon, Geneviève Eck, Grégoire Herve, Guy Jacob
  • Patent number: 7270683
    Abstract: Provided is a hair dye composition to be used as a mixture of a first part containing an alkali agent and a second part containing an oxidizing agent, wherein the composition comprises (a) a triazacyclononane compound (1) or salt thereof, (b) 0.1 to 12 wt. %, in terms of hydrogen peroxide, of an oxidizing agent, and (c) 0.05 to 10 wt. % of an alkali agent, and the mixture has a pH of from 7.5 to 12. (R1 to R4: H or C1-6 alkyl which may be substituted by OH, R5 to R7: H, (substituted) C1-6 alkyl, (substituted) aralkyl, (substituted) heteroarylalkyl, (substituted) aryl, (substituted) heteroaryl, (substituted) C1-6 acyl, or a group (2) (in which R8 to R12 represents H, C1-6 alkyl, aralkyl or aryl and n stands for 2 to 30). The hair dye composition of the present invention has excellent hair bleaching power, can dye the hair into a bright favorable color tone, and moreover has less hair damage and less scalp irritation.
    Type: Grant
    Filed: April 18, 2002
    Date of Patent: September 18, 2007
    Assignee: Kao Corporation
    Inventors: Hideyuki Abe, Akira Kawamata, Akira Kiyomine
  • Patent number: 7192953
    Abstract: Compounds of formula (I) have antibacterial activity; wherein Q represents a radical of formula —N(OH)CH(?O) or formula —C(?O)NH(OH); Y represents —C(?O)—, —C(?S)—, —S(?O)—, or —SO2—; R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of formula —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, halogen, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, C1–C3 alkyl-O—C1–C3 alkyl, C1–C3 alkyl-S—C1–C3 alkyl, cycloalkyl(C1–C3 alkyl)-, aryl(C1–C3alkyl)-, heterocyclyl(C1–C3 alkyl)-, or R1R2N—C1–C3 alkyl group wherein R1 represents hydrogen or C1–C3 alkyl and R2 represents C1–C3 alkyl, or R1R2N-represents a cyclic amino group; R3 and R4 taken together with the nitrogen atoms to which they are respectively attached form a saturated heterocyclic ring of from 4 to 7 ring atoms, which may be fused to a second carbocyclic or heterocyclic ring, either of which rings may optionall
    Type: Grant
    Filed: December 1, 2003
    Date of Patent: March 20, 2007
    Assignee: Vernalis (Oxford) Limited
    Inventor: Stephen Peter East
  • Patent number: 7129348
    Abstract: Hexabenzylhexaazaisowurtzitane is converted to tetracetyl, dibenzyl azaisowurtzitane. The benzyl groups are removed by catalytic transfer hydrogenolysis leaving a pair of available nitrogens. The available nitrogens are acetylated, and the resulting intermediate is converted to CL-20 with a strong nitrating agent.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: October 31, 2006
    Assignee: Alliant Techsystems Inc.
    Inventors: Robert B. Wardle, Jerald C. Hinshaw
  • Patent number: 7053083
    Abstract: The present invention provides compounds of the general formulas: wherein Y is NR or —(CH2)n; R is H or alkyl “Z” represents optionally substituted phenyl or a 6-membered aromatic ring having one nitrogen atom; “W” represents a optionally substituted phenyl or 5-membered aromatic ring having one nitrogen atom; “X” represents an optionally substituted 5-membered aromatic ring having one sulfur atom; as well as methods and pharmaceutical compositions utilizing these compounds for the inducing temporary delay of urination or treatment of disorders remedied by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, or bleeding and coagulation disorders.
    Type: Grant
    Filed: April 11, 2002
    Date of Patent: May 30, 2006
    Assignee: Wyeth
    Inventors: Amedeo Arturo Failli, Jay Scott Shumsky, Thomas Joseph Caggiano, John P. Dusza, Kevin A. Memoli
  • Patent number: 6992185
    Abstract: A method is provided in which 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.05,903,11]-dodecane (CL-20 or HNIW) is crystallized to its ?-polymorph by an inverse precipitation technique. A dry CL-20 solvent solution containing an amount of CL-20 dissolved in a CL-20 solvent is prepared. The dry solvent solution is added to a crystallizer containing a CL-20 non-solvent to cause precipitation of epsilon polymorph CL-20 crystals by the inverse precipitation technique. The precipitated epsilon polymorph CL-20 crystals are separated from the non-solvent and the solvent.
    Type: Grant
    Filed: January 9, 2002
    Date of Patent: January 31, 2006
    Assignee: Alliant Techsystems Inc.
    Inventor: R. Scott Hamilton
  • Patent number: 6916925
    Abstract: Dye labeled imidazonaphthyridine, imidazopyridine and imidazoquinoline compounds having immune response modulating activity are disclosed. The compounds arc useful, inter alia, for determining the binding and/or receptor sites of the molecules.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: July 12, 2005
    Assignee: 3M Innovative Properties Co.
    Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei
  • Patent number: 6472525
    Abstract: Disclosed is an acyl group-containing hexaazaisowurtzitane derivative represented by the following formula (I): W At Q(6−t), wherein t represents an integer of from 4 to 6, A independently represents an acyl group having 1 to 10 carbon atoms, each Q independently represents a hydrogen atom or an alkyl group having 1 to 10 carbon atoms, and W represents a hexavalent hexaazaisowurtzitane residue represented by the following formula (II): Also disclosed is a method for producing the above-mentioned acyl group-containing hexaazaisowurtzitane derivative. The acyl group-containing hexaazaisowurtzitane derivative of the present invention is useful as a precursor of a polynitrohexaazaisowurtzitane derivative which can be used not only as a material for explosives but also as an additive for propellants and explosives.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: October 29, 2002
    Assignee: Asahi Kasei Kabushiki Kaisha
    Inventors: Tamotsu Kodama, Masahiro Tojo, Masanori Ikeda