The Hetero Ring Contains At Least Three Nitrogens Patents (Class 540/554)
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Patent number: 11744247Abstract: Disclosed herein are veterinary compositions including imidacloprid or an analogue thereof; a pyrethroid; a solvent selected from the group consisting of N-methyl pyrrolidone, N-ethyl pyrrolidone and mixtures thereof; and dimethyl sulfoxide. The veterinary compositions of the invention are useful in methods of controlling parasites on or within warm-blooded domesticated animals.Type: GrantFiled: April 22, 2020Date of Patent: September 5, 2023Assignee: NEOGEN CORPORATIONInventor: Martin Donnelly
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Patent number: 9353456Abstract: 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: GrantFiled: April 5, 2012Date of Patent: May 31, 2016Assignees: HERAKLES, EURENCOInventors: Florent Muscatelli, Philippe Lescop
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Patent number: 9227981Abstract: 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: GrantFiled: October 1, 2012Date of Patent: January 5, 2016Assignee: UNIVERSITY OF PARDUBICEInventors: Ahmed Ikhlas Mohamed Elbeih, Adela Husarova, Svatopluk Zeman
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Patent number: 9056868Abstract: 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: GrantFiled: September 10, 2013Date of Patent: June 16, 2015Assignee: The United States of America as Represented by the Secretary of the NavyInventor: Michael E. Wright
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Publication number: 20140341986Abstract: 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: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Alain D. Baron, Mark S. Fineman, Nigel R.A. Beeley
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Publication number: 20140235853Abstract: 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: ApplicationFiled: October 1, 2012Publication date: August 21, 2014Applicant: UNIVERSITY OF PARDUBICEInventors: Ahmed Ikhlas Mohamed Elbeih, Adela Husarova, Svatopluk Zeman
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Patent number: 8785625Abstract: 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: GrantFiled: February 14, 2012Date of Patent: July 22, 2014Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
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Publication number: 20140148339Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides and herbicides.Type: ApplicationFiled: June 22, 2012Publication date: May 29, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Tomas Smejkal, Michel Muehlebach
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Publication number: 20140073781Abstract: 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: ApplicationFiled: April 5, 2012Publication date: March 13, 2014Applicants: EURENCO, HERAKLESInventors: Florent Muscatelli, Philippe Lescop
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Publication number: 20130324536Abstract: 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: ApplicationFiled: December 8, 2011Publication date: December 5, 2013Applicant: Lycera CorporationInventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
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Patent number: 8530646Abstract: 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: GrantFiled: October 1, 2008Date of Patent: September 10, 2013Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
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Publication number: 20130150809Abstract: 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: ApplicationFiled: September 17, 2012Publication date: June 13, 2013Inventors: Jeffery A. Whiteford, William P. Freeman
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Patent number: 8426582Abstract: 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: GrantFiled: December 22, 2010Date of Patent: April 23, 2013Assignee: The United States of America as Represented by the Secretary of the NavyInventors: Robert D. Chapman, Richard A. Hollins
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Patent number: 8426583Abstract: 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: GrantFiled: December 30, 2010Date of Patent: April 23, 2013Inventors: Robert D. Chapman, Richard A. Hollins
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Publication number: 20130095140Abstract: 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: ApplicationFiled: July 11, 2012Publication date: April 18, 2013Applicant: Elcelyx Therapeutics, Inc.Inventors: Alain D. Baron, Mark S. Fineman, Nigel R. A. Beeley
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Publication number: 20120238546Abstract: 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: ApplicationFiled: June 15, 2010Publication date: September 20, 2012Inventors: Zhaoning Zhu, Xianhai Huang, Anandan Palani, William J. Greenlee, Robert G. Aslanian
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Patent number: 8268991Abstract: 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: GrantFiled: January 30, 2008Date of Patent: September 18, 2012Assignee: The United States of America as represented by the Secretary of the NavyInventors: Robert D. Chapman, Richard A. Hollins
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Patent number: 8268993Abstract: 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: GrantFiled: December 22, 2010Date of Patent: September 18, 2012Assignee: The United States of America as represented by the Secretary of the NavyInventor: Robert D. Chapman
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Publication number: 20120208997Abstract: 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: ApplicationFiled: February 14, 2012Publication date: August 16, 2012Inventors: Hideyuki SUZUKI, Shoji HIZATATE, Iwao UTSUNOMIYA, Koichi SHUDO
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Publication number: 20120199256Abstract: 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: ApplicationFiled: September 28, 2010Publication date: August 9, 2012Applicants: EURENCO, SMEInventors: Florent Muscatelli, Philippe Lescop
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Patent number: 8202854Abstract: 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: GrantFiled: July 27, 2011Date of Patent: June 19, 2012Assignee: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Publication number: 20120129846Abstract: 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: ApplicationFiled: November 5, 2009Publication date: May 24, 2012Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
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Patent number: 8148362Abstract: 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: GrantFiled: March 30, 2007Date of Patent: April 3, 2012Assignees: Research Foundation Itsuu Laboratory, Shionogi & Co., Ltd.Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
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Patent number: 8133993Abstract: 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: GrantFiled: November 26, 2008Date of Patent: March 13, 2012Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Raja Duddu, Paritosh Dave, Reddy Damavarapu, Rao Surapaneni
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Publication number: 20120059010Abstract: 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: ApplicationFiled: March 28, 2011Publication date: March 8, 2012Applicant: Institute for Chemical GenomicsInventors: Michael Kahn, Masakatsu Eguchi
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Patent number: 8063032Abstract: 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: GrantFiled: February 11, 2010Date of Patent: November 22, 2011Assignee: Sunovion Pharmaceuticals Inc.Inventors: Milan Chytil, Qun Kevin Fang, Kerry L. Spear
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Publication number: 20110280867Abstract: 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: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Patent number: 8017768Abstract: 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: GrantFiled: April 5, 1994Date of Patent: September 13, 2011Assignee: The United States of America as represented by the Secretary of the NavyInventors: William P. Norris, Arnold T. Nielsen
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Patent number: 7875714Abstract: 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: GrantFiled: April 23, 2007Date of Patent: January 25, 2011Assignee: The United States of America as represented by the Secretary of the NavyInventors: Robert D. Chapman, Richard A. Hollins
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Publication number: 20100256355Abstract: 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 oxazolidType: ApplicationFiled: October 1, 2008Publication date: October 7, 2010Inventors: Hideyuki Suzuki, Iwao Utsunomiya, Koichi Shudo, Tsutomu Iwaki, Tatsuro Yasukata
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Patent number: 7759354Abstract: 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: GrantFiled: June 12, 2006Date of Patent: July 20, 2010Assignee: Schering CorporationInventors: Zhaoning Zhu, Brian McKittrick, Andrew Stamford, Ying Huang, Elizabeth M. Smith
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Patent number: 7737272Abstract: 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: GrantFiled: February 15, 2008Date of Patent: June 15, 2010Assignee: Wisconsin Alumni Research FoundationInventors: Clark R. Landis, Wiechang Jin, Jonathan S. Owen, Thomas P. Clark
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Patent number: 7709467Abstract: 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: GrantFiled: May 15, 2008Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Publication number: 20090299059Abstract: 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: ApplicationFiled: March 30, 2007Publication date: December 3, 2009Inventors: Hideyuki Suzuki, Shoji Hizatate, Iwao Utsunomiya, Koichi Shudo
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Patent number: 7592448Abstract: 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: GrantFiled: March 1, 2004Date of Patent: September 22, 2009Assignee: The Secretary of State for Defence in Her Britannic Majesty's Government of the United Kingdon of Great Britain and Northern IrelandInventors: Peter Golding, Alistair J Maccuish, Anthony John Bellamy
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Patent number: 7465722Abstract: 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 (unsaturatedType: GrantFiled: August 11, 2006Date of Patent: December 16, 2008Assignee: WyethInventors: Amedeo A. Failli, John P. Dusza, Thomas J. Caggiano, Jay S. Shumsky, Kevin A. Memoli, Eugene J. Trybulski
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Publication number: 20080261951Abstract: 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: ApplicationFiled: June 23, 2008Publication date: October 23, 2008Inventors: Doreen Mary Ashworth, Gary Robert William Pitt, Peter Hudson, Christopher Martyn Yea, Richard Jeremy Franklin
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Publication number: 20080262222Abstract: Near infrared (NIR) dyes, image recording substrate including the NIR dye, and methods of making the NIR dyes, are disclosed.Type: ApplicationFiled: April 23, 2007Publication date: October 23, 2008Inventors: Vladek Kasperchik, Vyacheslav Olkhovik, Andreii Pap, Dimitriy Vasilevskii, Cari L. Dorsh, Sterling Chaffins
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Publication number: 20080249080Abstract: 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-C6Type: ApplicationFiled: May 26, 2006Publication date: October 9, 2008Inventors: 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
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Patent number: 7407949Abstract: 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: GrantFiled: February 12, 2004Date of Patent: August 5, 2008Assignee: Ferring B.V.Inventors: Peter Hudson, Andrzej Roman Batt, Celine Marguerite Simone Heeney, Andrew John Baxter, Michael Bryan Roe, Peter Andrew Robson
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Patent number: 7390799Abstract: 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: GrantFiled: May 12, 2006Date of Patent: June 24, 2008Assignee: Abbott LaboratoriesInventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol Min Park, Xiahong Song, Xilu Wang
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Patent number: 7329653Abstract: 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: GrantFiled: April 11, 2006Date of Patent: February 12, 2008Assignee: WyethInventors: Amedeo A. Failli, Jay S. Shumsky, Thomas J. Caggiano, John P. Dusza, Kevin A. Memoli
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Patent number: 7288648Abstract: 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: GrantFiled: August 6, 2003Date of Patent: October 30, 2007Assignee: Alliant Techsystems Inc.Inventors: R. Scott Hamilton, Vincent Mancini, Clint Nelson, Sharon Yeung Dressen
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Patent number: 7279572Abstract: 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: GrantFiled: April 28, 2004Date of Patent: October 9, 2007Assignee: SNPE Materiaux EnergetiquesInventors: Guy Cagnon, Geneviève Eck, Grégoire Herve, Guy Jacob
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Patent number: 7270683Abstract: 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: GrantFiled: April 18, 2002Date of Patent: September 18, 2007Assignee: Kao CorporationInventors: Hideyuki Abe, Akira Kawamata, Akira Kiyomine
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Patent number: 7192953Abstract: 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 optionallType: GrantFiled: December 1, 2003Date of Patent: March 20, 2007Assignee: Vernalis (Oxford) LimitedInventor: Stephen Peter East
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Patent number: 7129348Abstract: 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: GrantFiled: December 21, 1988Date of Patent: October 31, 2006Assignee: Alliant Techsystems Inc.Inventors: Robert B. Wardle, Jerald C. Hinshaw
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Patent number: 7053083Abstract: 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: GrantFiled: April 11, 2002Date of Patent: May 30, 2006Assignee: WyethInventors: Amedeo Arturo Failli, Jay Scott Shumsky, Thomas Joseph Caggiano, John P. Dusza, Kevin A. Memoli
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Crystallization of 2,4,6,8,10,12-hexanitro-2,4,6,8,10,12-hexaazatetracyclo[5.5.0.05,903,11]-dodecane
Patent number: 6992185Abstract: 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: GrantFiled: January 9, 2002Date of Patent: January 31, 2006Assignee: Alliant Techsystems Inc.Inventor: R. Scott Hamilton -
Patent number: 6916925Abstract: 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: GrantFiled: July 22, 2003Date of Patent: July 12, 2005Assignee: 3M Innovative Properties Co.Inventors: Michael J. Rice, Mark A. Tomai, Ai-Ping Wei