The Hetero Ring Contains At Least Three Nitrogens Patents (Class 540/554)
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Patent number: 6472525Abstract: 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: GrantFiled: May 16, 1997Date of Patent: October 29, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Tamotsu Kodama, Masahiro Tojo, Masanori Ikeda
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Patent number: 6414143Abstract: Nitramine oxidizers are recovered from propellant, explosive, and pyrotechnic materials with a concentrated mineral acid bath, preferably comprising 70 to 90 wt. % nitric acid, that serves to dissolve the nitramine oxidizers into solution and permit filtration of the binder therefrom. The recovery process is conducted in the absence of organic solvents.Type: GrantFiled: February 17, 2000Date of Patent: July 2, 2002Assignee: Alliant Techsystems Inc.Inventors: Louis Cannizzo, Lew Huntsmann
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Patent number: 6391130Abstract: In this process 2,6,8,12-tetraacetyl-2,4,6,8,10,12-hexaazatetracyclo-[5.5.0.05,903,11]-dodecane (“TADH”) is subjected to nitrolysis in the presence of a mixed acid to form HNIW. The mixed acid comprises at least one nitronium ion source (preferably nitric acid) and at least one strong acid (preferably sulfuric acid) capable of generating a nitronium ion from the source. The ratio of nitronium ion source to strong acid and the amount of TADH used are selected so that, in the event that the nitrolysis reaction is carried out at 85° C., 99% nitramine conversion will occur within ten minutes.Type: GrantFiled: February 15, 2000Date of Patent: May 21, 2002Assignee: Alliant Techsystems Inc.Inventors: Andrew J. Sanderson, Kirstin Warner, Robert B. Wardle
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Patent number: 6358976Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the &agr;v&bgr;3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: February 22, 2000Date of Patent: March 19, 2002Inventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6350871Abstract: CL-20 is crystallized from a solution containing a CL-20 organic solvent and a CL-20 non-solvent miscible with the solvent. The CL-20 non-solvent is a nitrate ester, preferably poly(glycidyl nitrate) and/or triethyleneglycol-dinitrate, although other nitrate ester plasticizers having acceptable volatilities and impact sensitivities can be used. The solution is saturated with CL-20, and CL-20 is then crystallized from the saturated solution by adding &egr;-polymorph CL-20 crystalline seeds to the solution and evaporating off the CL-20 solvent, preferably under vacuum. The nitrate ester non-solvent is then separated from the crystalline CL-20, such as by filtration of the CL-20 crystals or by diluting the slurry of non-solvent and CL-20 with an environmentally acceptable solvent that is miscible with the non-solvent but in which the CL-20 is insoluble.Type: GrantFiled: March 21, 2001Date of Patent: February 26, 2002Assignee: Alliant Techsystems Inc.Inventors: Andrew J. Sanderson, Richard S. Hamilton, Kirstin F. Warner
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Publication number: 20020022619Abstract: The present invention relates to tricyclic fused pyrimidine and pyridine derivatives having the following general formula: 1Type: ApplicationFiled: April 30, 2001Publication date: February 21, 2002Inventor: Rajagopal Bakthavatachalam
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Patent number: 6297373Abstract: A method for acylating a hexakis (arylmethyl) hexaazaisowurtzitane (WB6) by reductively removing the arylmethyl groups in the presence of an acylating agent, characterized by contacting a WB6 (a) with a heterogeneous system reduction catalyst (b) in the presence of an acylating agent (c) and a reducing agent (d) in a solvent (e) for the WB6 (a) to reductively remove the arylmethyl groups from the WB6 (a) and acylate the same, and by preventing the WB6 (a) and the catalyst (b) from being contacted with each other when at least either of the acylating agent (c) and the reducing agent (d) is not present. In this method, the decomposition of the WB6 skeleton, which readily occurs in the beginning of the acylation of the WB6 as a starting material, can be highly effectively inhibited. This method can hence stably produce a tetraacylhexaazaisowurtzitane derivative in a high yield and is industrially advantageous.Type: GrantFiled: March 14, 2000Date of Patent: October 2, 2001Assignee: Asahi Kasei Kabushiki KaishaInventors: Tamotsu Kodama, Naoko Ishihara, Haruyuki Minoura, Nobuhisa Miyake, Setsuo Yamamatsu
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Patent number: 6297372Abstract: A nitro group-containing hexaazaisowurtzitane derivative represented by the following general formula (I): W An N(6−n) (I) wherein n is an integer of 4 or 5, A is an acyl group having 1-10 carbon atoms with each acyl group being the same as or different from one or more of the others, N is a nitro group and W is a hexavalent hexaazaisowurtzitane residue represented by the following formula (II): a nitroso group-containing hexaazaisowurtzitane derivative represented by the following general formula (III): W An NS(6−n) (III) wherein n is an integer of 4 or 5, A is an acyl group having 1-10 carbon atoms with each acyl group being the same as or different from one or more of the others, NS is a nitroso group and W is a hexavalent hexaazaisowurtzitane residue of formula (II) above, and an acyl group-containing hexaazaisowurtzitane derivative represented by the following general formula (IV): W Am H(6−m) (IV) wherein N is an integer of 4-6,Type: GrantFiled: September 30, 1999Date of Patent: October 2, 2001Assignee: Asahi Kasei Kabushiki KaishaInventors: Shuji Kawabe, Hiroshi Miya, Tamotsu Kodama, Nobuhisa Miyake
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Patent number: 6194571Abstract: A process for making alpha-HMX comprises the steps of: (a) combining phosphorus pentoxide and nitric acid at a temperature of about 0-25° C., forming a reaction mixture; and (b) adding a compound having the formula: wherein R is straight chain or branched alkyl having 1-5 carbon atoms, to the reaction mixture, whereby a product comprising alpha-HMX is produced.Type: GrantFiled: January 3, 2000Date of Patent: February 27, 2001Assignee: Schlumberger Technology CorporationInventor: William J. Lukasavage
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Patent number: 6160113Abstract: Processes and compositions for nitration of N-substituted isowurtzitane compounds with concentrated nitric acid at elevated temperatures to form HNIW and recovery thereof with high yields and purities. Polymorphic conversions to the epsilon HNIW crystal form at quanititative yields are also described.Type: GrantFiled: April 28, 1999Date of Patent: December 12, 2000Assignee: The United States of America as represented by the Secretary of the ArmyInventors: Raja Duddu, Paritosh R. Dave
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Patent number: 6156747Abstract: This invention concerns the compounds of formula (I), ##STR1## the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero to 6; p is zero to 3; q is zero to 3; r is zero to 3; R.sup.1 and R.sup.2 each independently are hydrogen; optionally substituted C.sub.1-6 alkyl; C.sub.1-6 alkylcarbonyl; trihalomethylcarbonyl; or R.sup.1 and R.sup.2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; each R.sup.3 and R.sup.4 independently are halo, cyano, hydroxy, trihalomethyl, trihalomethoxy, carboxyl, nitro, amino, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkylcarbonylamino, aminosulfonyl, mono- or di(C.sub.1-6 alkyl)-aminosulfonyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyloxycarbonyl; each R.sup.5 independently is C.sub.1-6 alkyl, cyano or trihalomethyl; X is CR.sup.6 R.sup.7, NR.sup.8, O, S, S(.dbd.O) or S(.dbd.O).sub.Type: GrantFiled: October 6, 1998Date of Patent: December 5, 2000Assignee: Janssen Pharmaceutica N.V.Inventors: Jose Ignacio Andres-Gil, Pedro Martinez-Jimenez, Francisco Javier Fernandez-Gadea, Victor Karel Sipido
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Patent number: 6153749Abstract: Disclosed is a method for producing an acyl group-containing hexaazaisowurtzitane derivative represented by the following formula (1),WA.sub.n H.sub.(6-n) (1)wherein n represents an integer of 4 or 6, each A independently represents an acyl group having 1 to 10 carbon atoms, H represents a hydrogen atom, and W represents a hexavalent hexaazaisowurtzitane residue represented by the following formula (2): ##STR1## which comprises: providing a composition system comprising a mixed solvent of a first solvent and a second solvent respectively having high and low dissolving abilities for the desired compound, wherein the mixed solvent has the desired compound dissolved therein; and removing the first solvent having a high dissolving ability from the composition system to thereby deposit crystals of the desired compound. The desired compound, which is useful as a precursor of high performance explosive additive, i.e.Type: GrantFiled: January 11, 1999Date of Patent: November 28, 2000Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Tamotsu Kodama, Haruyuki Minoura, Nobuhisa Miyake, Setsuo Yamamatsu, Tsutomu Katsumata
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Patent number: 6147209Abstract: 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 8, 1992Date of Patent: November 14, 2000Assignee: Cordant Technologies Inc.Inventors: Robert B. Wardle, Jerald C. Hinshaw
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Patent number: 6080758Abstract: The present invention relates to compounds selected from the group consisting of the compounds of formula (I): ##STR1## X is a halogen atom, A is --CH.sub.2 --, --CH(OH)--, --CH(NH--COCH.sub.3)-- or S, R is H, CO.sub.2 H, CO.sub.2 --B--R.sub.1 or CO--N(R.sub.2)--B--R.sub.1, B is linear, branched or cyclic C.sub.1 -C.sub.10 -alkylene, R.sub.1 is H, CH.sub.2 OH, CH.sub.2 --O--CH.sub.3, CH.sub.2 --NR.sub.3 R.sub.4 or phenyl, R.sub.2 is H or C.sub.1 -C.sub.4 -alkyl, R.sub.3 is H or linear, branched or cyclic C.sub.1 -C.sub.10 -alkyl, R.sub.4 is H or linear or branched C.sub.1 -C.sub.10 -alkyl, it being possible for NR.sub.3 R.sub.4 to be a saturated heterocyclic radical having from 5 to 8 ring members and containing at least one nitrogen atom, and the carbon carrying the substituent R, when Q is saturated, can be of indeterminate (R,S) configuration or of determinate (R) or (S) configuration; and their addition salts.Type: GrantFiled: April 7, 1997Date of Patent: June 27, 2000Assignee: Fournier Industrie et SanteInventors: Pierre Dodey, Michel Bondoux, Patrick Houziaux, Martine Barth, Khan Ou
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Patent number: 6015898Abstract: Processes and compositions for nitration of N-substituted isowurtzitane compounds with concentrated nitric acid at elevated temperatures to form HNIW and recovery of gamma HNIW with high yields and purities. Polymorphic conversion of HNIW crystals to epsilon HNIW crystals is also disclosed.Type: GrantFiled: May 1, 1998Date of Patent: January 18, 2000Assignee: The United States of America, as represented by the Secretary of the ArmyInventors: Raja G. Duddu, Paritosh R. Dave
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Patent number: 5877170Abstract: This invention relates to novel substituted caprolactams, including 4-azacaprolactams, and derivatives thereof which inhibit HIV protease and are useful for treatment of HIV disease. Also included in this invention are pharmaceutical compositions containing such caprolactams, and to methods of using such caprolactams for the treatment of HIV disease.Type: GrantFiled: May 23, 1997Date of Patent: March 2, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Carl Nicholas Hodge, Christina Howard Fernandez, Prabhakar Kondaji Jadhav, Patrick Yuk-Sun Lam
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Patent number: 5846969Abstract: A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents O or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alkyl); and M represents ##STR2## rings A and B represent each an unsaturated 5- or 6-membered ring; Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15).Type: GrantFiled: June 11, 1997Date of Patent: December 8, 1998Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
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Patent number: 5807850Abstract: Therapeutic agents for osteoporosis comprising, as an active ingredient, a triazepine compound of the formula ?I! ##STR1## wherein R.sup.1 is aryl or heteroaryl; R.sup.2 is hydrogen atom, hydroxy, halogen atom or lower alkyl; R.sup.4 is hydrogen atom or halogen atom, or R.sup.2 and R.sup.4 form carbonyl combinedly together with the carbon atom to which they bond; R.sup.3 is hydrogen atom, lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, --X--Y wherein X is --(CH.sub.2).sub.m --, --CO--, --COCH.sub.2 --, --NH--, --NHCH.sub.2 --, --CH.sub.2 NH--, --CH.sub.2 NHCO--, --OCH.sub.2 --, --(CH.sub.2).sub.n O-- or --CH.sub.2 S-- and Y is halogen atom, cycloallyl, aryl or heteroaryl; and A is benzene ring or thiophene ring, or a salt thereof, novel triazepine compounds, and intermediate triazepine compounds for producing these triazepine compounds. The triazepine compounds of the formula ?I! have superior bone resorption-inhibitory action and are useful as therapeutic agents for osteoporosis.Type: GrantFiled: May 5, 1997Date of Patent: September 15, 1998Assignee: Japan Tobacco, Inc.Inventors: Takeshi Nakamura, Yoshihisa Koga, Masanori Shindo
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Patent number: 5786352Abstract: Novel compounds of the following general formula or salts thereof. ##STR1## wherein Ring M is a heterocyclic ring having --N.dbd.C<, --CO--N< or --CS--N< as the partial structure --X . . . Y<; R.sup.a and R.sup.b are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Ring C is optionally substituted homocyclic or heterocyclic ring; Ring Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: March 25, 1996Date of Patent: July 28, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura
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Patent number: 5760028Abstract: This invention relates to novel heterocycles including 3-?1-?3-(imidazolin-2-ylamino)propyl!indazol-5-ylcarbonylamino!-2-(benzylo xycarbonylamino)propionic acid, which are useful as antagonists of the .alpha..sub.v .beta..sub.3 integrin and related cell surface adhesive protein receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: December 20, 1996Date of Patent: June 2, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Prabhakar Kondaji Jadhav, Joseph James Petraitis, Douglas Guy Batt
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Patent number: 5739325Abstract: A process for the hydrogenolysis of 2,4,6,8,10,12-hexabenzyl-2,4,6,8,10,12-hexaazatetracyclo?5.5.0.0.sup.5,9.0 .sup.3,11 !dodecane ("HBIW") is disclosed. In the process, a quantity of HBIW, a cosolvent, and a bromine source are placed into a reaction vessel. Acetic anhydride and a palladium hydrogenolysis catalyst are rapidly added to the reaction vessel. The hydrogenolysis catalyst should be substantially free of water. The reaction vessel is purged of an atmosphere capable of reacting with hydrogen, and hydrogen is quickly introduced into the reaction vessel to convert the HBIW to tetraacetyldibenzylhexaazaisowurtzitane ("TADB"). The acetic anhydride is added immediately prior to hydrogen introduction so that the acetic anhydride does not have time to react with the HBIW to form an acetylated derivative prior to commencement of the desired hydrogenation reaction. The process requires very little palladium catalyst, preferably less than 10% wt/wt based on the HBIW substrate.Type: GrantFiled: December 7, 1995Date of Patent: April 14, 1998Assignee: Thiokol CorporationInventors: Robert B. Wardle, W. Wayne Edwards
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Patent number: 5731432Abstract: Novel diazepine derivatives which selectively inhibit adenosine monophosphate deaminase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.Type: GrantFiled: February 3, 1994Date of Patent: March 24, 1998Assignee: Gensia Sicor Inc.Inventors: Mark D. Erion, Brett C. Bookser, Srinivas Rao Kasibhatla, Harry E. Gruber
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Patent number: 5698691Abstract: Disclosed is a squalene synthetase inhibitor which comprises the compound represented by the formula ##STR1## wherein R.sub.1 is hydrogen or an optionally substituted hydrocarbon group; R.sub.2 is hydrogen, an optionally substituted alkyl group, an optionally substituted phenyl group or an optionally substituted aromatic heterocyclic ring group; X' is a substituent comprising an optionally esterified carboxyl group, an optionally substituted carbamoyl group, an optionally substituted hydroxyl group, an optionally substituted amino group or an optionally substituted heterocyclic radical having a protonizable hydrogen; Ring A is an optionally substituted benzene ring or an optionally substituted aromatic heterocyclic ring; Ring J' is a 7- to 8-membered heterocyclic ring containing at most three ring constituting hetero atoms; D is C or N; the Ring J' optionally having, besides R.sub.1, R.sub.Type: GrantFiled: September 26, 1994Date of Patent: December 16, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Hidefumi Yukimasa, Ryuichi Tozawa, Yasuo Sugiyama, Masakuni Kori
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Patent number: 5693794Abstract: A new compound, 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?5.5.0.0.sup.5,9.0 3,11 !dodecane) is disclosed and a method of preparation thereof. The new compound is useful as a high energy, high density explosive.Type: GrantFiled: September 30, 1988Date of Patent: December 2, 1997Assignee: The United States of America as represented by the Secretary of the NavyInventor: Arnold T. Nielsen
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Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5393752Abstract: Methylpiperazinoazepine derivatives corresponding to formula (I): ##STR1## wherein the symbols X, R.sub.1, R.sub.2, N.sub.1 and N.sub.2 have different meanings and pharmaceutically acceptable salts thereof, preparation and use thereof.Type: GrantFiled: June 14, 1994Date of Patent: February 28, 1995Assignee: Therabel Research S.A./N.V.Inventors: Jean-Francois F. Liegeois, Jacques E. Delarge
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Patent number: 5324834Abstract: The present invention relates to novel co-oligomers containing recurring units of the formulae (Ia) and (Ib) ##STR1## which have a number average molecular weight of e.g. from 1,000 to 5,000 and a (Ia):(Ib) ratio of e.g. 1:1, and in which R.sub.1 and R.sub.5 are e.g. N-(2,2,6,6-tetramethyl-4-piperidyl)-n-butylamino, R.sub.2 is e.g. 2,2,6,6-tetramethyl-4-piperidyl, R.sub.3 is e.g. hexamethylene, R.sub.4 is e.g. hydrogen and X is e.g. a group ##STR2## These compounds are particularly suitable for stabilizing organic materials against light, heat and oxidation.Type: GrantFiled: April 16, 1993Date of Patent: June 28, 1994Assignee: Ciba-Geigy CorporationInventors: Valerio Borzatta, Primo Carrozza
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Patent number: 5210209Abstract: The invention provides a method for the production of a pyrazolo(1,5-a)benzimidazole of the general formula (A): ##STR1## wherein R is a substituted or unsubstituted alkyl or aryl group, andR.sup.1 -R.sup.4 =R, H, halogen, OR, COOR, CONHR, SO.sub.2, NO.sub.2 NHR, NR.sub.2, or CN, andX is hydogen or a reactive group releasable on coupling with an oxidized color developer, wherein the invention provides reacting a 2-amino or 2-mercapto substituted benzimidazole to form a triazepinone or a thiadiazino derivative respectively, ring contracting said triazepinone or thiadiazino derivative to give the corresponding 2-methylpyrazolobenzimidazole product, and subsequently removing the substituents at the -3 or -4 positions to provide a compound of the general formula (1).Type: GrantFiled: June 3, 1991Date of Patent: May 11, 1993Assignee: Eastman Kodak CompanyInventor: Michael W. Crawley
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Patent number: 5047531Abstract: Piperidine-triazine compounds of the general formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 is e.g. C.sub.2 -C.sub.6 alkylene, R.sub.3 is e.g. a group ##STR2## ##STR3## can be used as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials, in particular synthetic polymers.Type: GrantFiled: August 2, 1989Date of Patent: September 10, 1991Assignee: Ciba-Geigy CorporationInventors: Giuseppe Cantatore, Graziano Vignali
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 4997938Abstract: The novel compounds of the formula (I) ##STR1## in which R.sub.1 is di(C.sub.1 -C.sub.4 -alkyl)amino, C.sub.1 -C.sub.4 -alkoxy, a 5-membered to 7-membered nitrogen containing heterocyclic group with the nitrogen atom bonded to the triazine ring, or a group of the formula (II), ##STR2## R.sub.2 and R.sub.4 which are identical or different are C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, benzyl or 1,2,2,6,6-pentamethyl-4-piperidyl, n is 2 or 3 and, if n is 2, R.sub.3 is a group ##STR3## with R.sub.5 and R.sub.7, which are identical or different, being hydrogen, C.sub.1 -C.sub.12 -alkyl, C.sub.5 -C.sub.7 -cycloalkyl, benzyl or 1,2,2,6,6-pentamethyl-4-piperidyl and R.sub.6 being C.sub.2 -C.sub.12 -alkylene, cyclohexylene, cyclohexylenedimethylene or methylenedicyclohexylene, or R.sub.3 is the divalent radical of a 6-membered to 7-membered heterocyclic compound with two nitrogen atoms which are each bonded to a triazine ring, or, if n is 3, R.sub.3 is a group ##STR4## with R.sub.8 and R.sub.Type: GrantFiled: December 8, 1989Date of Patent: March 5, 1991Assignee: Ciba-Geigy CorporationInventors: Giuseppe Cantatore, Valerio Borzatta, Franca Masina
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Patent number: 4970205Abstract: Invented are sulfonic acid substituted analogues of steroidal synthetic compounds, pharmaceutical compositions containing these compounds, and methods of using these compounds to inhibit steroid 5-.alpha.-reductase, including using these compounds to reduce or maintain prostate size. Also invented are intermediates used in preparing these compounds.Type: GrantFiled: December 23, 1988Date of Patent: November 13, 1990Assignee: SmithKline Beecham CorporationInventors: Dennis A. Holt, Mark A. Levy, Brian W. Metcalf
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Patent number: 4935515Abstract: Disclosed herein are novel 1,2,3,4,5,6-hexahydro[1,3,6]triazocino[1,2-a]benzimidazole of Formulas I and II: ##STR1## wherein R.sup.1 may be phenyl, m- or p-nitrophenyl, m- or p-methylsulfonylaminophenyl, napthtyl, naphthyl mono-substituted by nitro or methylsulfonylamino, benzofurazanyl, 2-pyrimidinyl, 2- or 4-pyridinyl, 2- or 4-naphthyridinyl, pyrazinyl, isoquinolinyl, or quinolinyl;R.sup.2 may be hydrogen; C.sub.1 -C.sub.8 alkyl; phenyl(C.sub.1 -C.sub.4)alkyl or substituted-phenyl(C.sub.1 -C.sub.4)alkyl, in which phenyl may have one to three substituents selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluorine, chlorine or bromine; phenyl or substituted-phenyl in which the phenyl substituents are the same as for substituted-phenyl (C.sub.1 -C.sub.4)alkyl; 2- or 4-pyrimidinyl; pyrazinyl; imidazolyl; C.sub.1 -C.sub.4 alkanoyl; halo or dihalo-(C.sub.1 -C.sub.4)alkanoyl, in which halo is fluoro or chloro; benzoyl or benzoyl substituted on the phenyl ring by one or two C.sub.1 -C.sub.Type: GrantFiled: November 6, 1989Date of Patent: June 19, 1990Assignee: American Home Products CorporationInventors: Michael W. Winkley, James L. Diebold
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Patent number: 4879382Abstract: Pyrido[3,4-f]pyrrolo[1,2-b][1,2]triazepines and methods for treating depression, alleviating pain and inflammation, and enhancing memory utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: July 25, 1988Date of Patent: November 7, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Richard C. Effland, Larry Davis, Kevin J. Kapples, Gordon E. Olsen
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Patent number: 4871387Abstract: New pyri(mi)dyl-oxy- or -thio-benzoic acid derivatives of the formula ##STR1## are taught which have herbicidal and plant growth regulating activity. In the formula Z can be Ch or N, X is oxygen or sulphur, A is oxygen, sulphur, a radical R.sup.5 --N.dbd.or a radical R.sup.6 O--N.dbd.and B is oxygen, sulphur, a radical ##STR2## with the proviso that at least one of the radicals R.sup.1, R.sup.2 or R.sup.3 represents alkyl or a part of a 3- to 6-membered fused carbocyclic ring.Type: GrantFiled: December 4, 1986Date of Patent: October 3, 1989Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Reiner Fischer, Hermann Hagemann, Hans-Joachim Santel, Robert R. Schmidt, Kalus Lurssen
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Patent number: 4801706Abstract: Disclosed herein are N-substituted-hexahydro-1,2,5-triazepines of formula I, which is ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.1 is (R.sup.6).sub.2 --CH--(CH.sub.2).sub.n -- in which n is 0, 1, 2 or 3 and R.sup.6 is p-fluoro, chloro or methoxyphenyl; andR.sup.3 is hydrogen and R.sup.2 is benzoyl, 2,6-dimethyl or diethylbenzoyl, 2,6-dichlorobenzoyl, N-methyl, ethyl or propylcarboxamido, N-phenylcarboxamido, N-2,6-dimethyl or diethylphenylcarboxamido, N-2,6-dichlorophenylcarboxamido, N-methyl, ethyl or propylacetamido, N-phenylacetamido, N-2,6-dimethyl or diethylphenylacetamido, or N-2,6-dichlorophenylacetamido orR.sup.2 and R.sup.3 are the same and are N-methyl, ethyl or propylcarboxamido, benzoyl, 2,6-dimethyl or diethlbenzoyl, 2,6-dichlorobenzoyl, benzyl, 2,6-dimethyl or diethlbenzoyl, 2,6-dichlorobenzoyl, or a removable amino protective group.Type: GrantFiled: April 28, 1988Date of Patent: January 31, 1989Assignee: American Home Products CorporationInventors: Michael W. Winkley, James L. Diebold
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Patent number: 4792547Abstract: Novel pyrazine derivatives useful for treatment of bronchial asthma, allergic gastorenteric trouble, hay fever urticaria, allertic rhinitis, and allergic conjunctivitis, and pharmaceutical compositions thereof, are disclosed. The compounds have the formula I as follows: ##STR1## wherein R represents hydrogen or ##STR2## wherein R.sub.1 and R.sub.2 may be the same or different and each independently represents hydrogen, straight or branched-chain lower-alkyl, or cycloalkyl having three to six carbon atoms inclusive, phenyl which may be substituted with halogen, lower-alkyl, or lower-alkoxy, or wherein R.sub.1 and R.sub.2 together represent alkylene of four to six carbon atoms, inclusive, optionally interrupted by one or two nitrogen atoms or one oxygen atom and said ring being optionally substituted by straight or branched-chain lower-alkyl having one to six carbon atoms inclusive, hydroxy, or phenyl,and pharmaceutically-acceptable salts thereof.Type: GrantFiled: December 15, 1986Date of Patent: December 20, 1988Assignee: Hokuriku Pharmaceutical Co., Ltd.Inventors: Yasuo Itoh, Hideo Kato, Eiichi Koshinaka, Nobuo Ogawa, Kazuya Mitani
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Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
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Patent number: 4751316Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is >C.dbd.O or >CH--OR.sub.5 (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.Type: GrantFiled: April 15, 1987Date of Patent: June 14, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4702998Abstract: There are disclosed a processing solution having bleaching ability for use in light-sensitive silver halide photographic material, which comprises at least one selected from metal complexes of large cyclic polyamine derivatives and a method for processing of light-sensitive silver halide photographic material, which comprises carrying out development processing of an exposed light-sensitive silver halide photographic material and then processing the developed material with the processing solution.The processing solution of the present invention has potent bleaching power, and can afford excellent photographic image characteristics by processing therewith.Type: GrantFiled: March 24, 1986Date of Patent: October 27, 1987Assignee: Konishiroku Photo Industry Co., Ltd.Inventors: M. Tanaka, Kazuhiro Kobayashi, Shigeharu Koboshi
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Patent number: 4672064Abstract: Novel 1,5-benzoxathiepin derivatives of the formula: ##STR1## [wherein R.sub.1 and R.sub.2 are independently hydrogen, halogen, hydroxy, lower alkyl or lower alkoxy; R.sub.3 and R.sub.4 are independently hydrogen, optionally substituted lower alkyl or optionally substituted cycloalkyl or optionally substituted aralkyl, or both jointly form an optionally substituted ring together with the adjacent nitrogen atom; X is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or a carboxyl group which may be esterified or amidated; Y is ##STR2## (wherein R.sub.5 is hydrogen, acyl or optionally substituted carbamoyl); m is an integer of 0 to 2; n is an integer of 1 to 6] and salts thereof exhibit serotonin S.sub.Type: GrantFiled: December 10, 1985Date of Patent: June 9, 1987Assignee: Takeda Chemical Industries, Ltd.Inventors: Hirosada Sugihara, Minoru Hirata
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Patent number: 4612309Abstract: A class of bicyclic benzo-oxy heterocyclic ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastro-intestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: October 23, 1984Date of Patent: September 16, 1986Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander