Cyano Or Nitrogen And The Hetero Ring Bonded Directly To The Same Carbon Patents (Class 549/552)
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Patent number: 10974110Abstract: Provided is a golf shaft comprising an element tube made of steel, a plating layer formed on an outer periphery of the element tube, an outer layer covering the plating layer, an adhesive layer interposed between the plating layer and the outer layer to bond between the plating layer and the outer layer. The outer layer is formed of a fiber reinforced plastic having a matrix resin that is an epoxy resin, and the adhesive layer is an epoxy resin composition or a carbon nano tube resin composition, the epoxy resin composition comprising an epoxy resin and a mixed curing agent in which two or more kinds of amine-based curing agents are mixed, and the carbon nano tube resin composition comprising an epoxy resin and at least one kind of curing agents as well as dispersed carbon nano tubes.Type: GrantFiled: May 17, 2018Date of Patent: April 13, 2021Assignee: NHK SPRING CO., LTD.Inventors: Kosuke Fujiwara, Akihisa Inoue
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Publication number: 20140005292Abstract: A compound represented by the following general formula (1). In the formula, A represents a benzene ring, a naphthalene ring and the like, wherein these rings may be substituted with a halogen atom and the like, R1 represents a hydrogen atom and the like, R2 represents a C1-35 hydrocarbon group having or not having at least one group selected from an epoxy group, 4-vinylphenyl group and a (meth)acryloyloxy group, or a hydrogen atom, wherein at least one of R2 with n occurrences is a C3-35 hydrocarbon group having at least one group selected from an epoxy group, a 4-vinylphenyl group and a (meth)acryloyloxy group, n represents an integer of 1 to 6, and X represents a nitrogen atom, an oxygen atom, a sulfur atom, a phosphorus atom, or an n-valent organic group having 35 or less carbon atoms.Type: ApplicationFiled: April 12, 2012Publication date: January 2, 2014Applicant: Adeka CorporationInventors: Yosuke Maeda, Masaaki Shimizu, Koich Shigeno
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Publication number: 20130203998Abstract: The present invention relates to drug derivatives and linkers. The invention specifically relates to compounds and methods of phosphonates and linkers, that are useful as carriers for imaging agents and useful in the treatment of various bone diseases.Type: ApplicationFiled: March 14, 2013Publication date: August 8, 2013Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventor: UNIVERSITY OF SOUTHERN CALIFORNIA
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Publication number: 20130116457Abstract: The present invention provides compounds and methods that can be used to convert the intermediate halomethyl ketones (HMKs), e.g., chloromethyl ketones, to the corresponding S,S- and R,S-diastereomers. More particularly, the present invention provides: (1) reduction methods; (2) inversion methods; and (3) methods involving the epoxidation of alkenes. Using the various methods of the present invention, the R,S-epoxide and the intermediary compounds can be prepared reliably, in high yields and in high purity.Type: ApplicationFiled: June 7, 2012Publication date: May 9, 2013Applicant: Aerojet Fine Chemicals LLCInventors: Aslam A. Malik, Todd E. Clement, Hasan Palandoken, James Robinson, III, Joy A. Stringer
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Patent number: 8415490Abstract: A novel epoxy compound represented by the following formula and a method for producing the same are provided: wherein R1 and R2 are members selected from the group consisting of hydrogen, aliphatic hydrocarbon group having 1 to 4 carbon atoms, alicyclic hydrocarbon group having 3 to 6 carbon atoms, aromatic hydrocarbon group having 6 to 10 carbon atoms, halogen atom, ether group, ester group, acyl group and nitro group, n is an integer of 1 to 4, and m is an integer of 1 to 5.Type: GrantFiled: October 13, 2009Date of Patent: April 9, 2013Assignee: Toray Fine Chemicals Co., Ltd.Inventors: Koutaro Ono, Michiya Ishikawa, Jiro Nakatani
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Publication number: 20130053557Abstract: Processes and intermediates for preparing linezolid, and pharmaceutically acceptable salts thereof, are described herein.Type: ApplicationFiled: April 28, 2011Publication date: February 28, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventor: James R. McCarthy
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Publication number: 20120289706Abstract: The present invention relates to a new process for the preparation of substituted thiotriazolo groups of the general formula (I) wherein the variables have the meanings as given in the claims and the description.Type: ApplicationFiled: December 13, 2010Publication date: November 15, 2012Applicant: BASF SEInventors: Jens Renner, Jochen Dietz, Thomas Grote, Joachim Gebhardt, Markus Nett, Michael Keil
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Patent number: 8168826Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethylamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.Type: GrantFiled: December 3, 2009Date of Patent: May 1, 2012Assignee: Janssen Pharamcuetica N.V.Inventors: Steve J. Coats, Dennis J. Hlasta, Mark J. Schulz
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Patent number: 8076495Abstract: A process for the preparation of aromatic N-glycidylamines is described, wherein an amine which contains at least one aromatic aminehydrogen atom is heated with at least 0.7 equivalent of epichlorohydrin per aminehydrogen equivalent of the aromatic amine, using a divalent or polyvalent metal salt of nitric acid, as a catalyst, dissolved in propylene carbonate, and the product is then dehydrochiorinated.Type: GrantFiled: June 28, 2004Date of Patent: December 13, 2011Assignee: Huntsman Advanced Materials Americas LLCInventors: Roger Malherbe, Jean-Marc Pfefferle
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Publication number: 20100317515Abstract: The present invention relates to triazolylmethyloxiranes of the formula I in which the variables A, B and D have the meanings described in the claims and the description.Type: ApplicationFiled: December 12, 2008Publication date: December 16, 2010Applicant: BASF SEInventors: Jochen Dietz, Thomas Grote, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Alice Glaettli, Marianna Vrettou
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Publication number: 20100099898Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.Type: ApplicationFiled: December 23, 2009Publication date: April 22, 2010Inventor: Michael R. Reeder
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Patent number: 7649055Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethylamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.Type: GrantFiled: July 1, 2008Date of Patent: January 19, 2010Assignee: Janssen Pharmaceutica N.V.Inventors: Steve J. Coats, Dennis J. Hlasta, Mark J. Schulz
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Publication number: 20090270499Abstract: This invention relates to a process for synthesizing Atazanvir, including novel intermediates and novel steps to various intermediates along the synthetic pathway.Type: ApplicationFiled: April 24, 2008Publication date: October 29, 2009Applicant: OXYRANE (UK) LIMITEDInventor: Weiping Chen
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Patent number: 7569699Abstract: This invention provides a process for producing an epoxytriazole derivative represented by formula (2): (wherein R and Ar are defined below), which comprises a step including a reaction of an epoxy derivative represented by formula (1?): (wherein R represents a hydrogen atom or C1-12 alkyl group and Ar represents an aromatic group optionally substituted by a halogen atom(s) or trifluoromethyl group(s), and X? represents a hydroxy group or leaving group), with 1,2,4-triazole in the presence of a base and water.Type: GrantFiled: November 29, 2005Date of Patent: August 4, 2009Assignee: Sumitomo Chemical Company, LimitedInventors: Taro Ishibahsi, Hideo Muraoka, Tadashi Mizuno
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Patent number: 7462728Abstract: The present invention relates to novel diepoxides having the formulas I. and II. R*N(A)SO2RSO2N(A)R*??I R*SO2N(A)RN(A)SO2R*??II where A=2,3-epoxypropyl, R* is a monovalent hydrocarbon alkyl aryl, aryl-alkyl, alkyl-aryl radical of 1-20 carbon atoms or a monovalent inertly substituted hydrocarbon aryl, alkyl, alkyl-aryl or aryl-alkyl radical of 1-20 carbons atoms and R is a divalent hydrocarbon arylene, alkylene, alkylene-aryl, arylene-alkyl radical or combinations thereof of 2-20 carbon atoms or an inertly substituted divalent hydrocarbon alkylene, arylene, arylene-alkyl, or alkylene-aryl radical or combinations thereof of 2-20 carbon atoms. The epoxides are useful in preparing novel epoxide resins.Type: GrantFiled: December 15, 2004Date of Patent: December 9, 2008Inventor: R. Garth Pews
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Patent number: 7408008Abstract: The invention is directed to compounds and methods of synthesizing hydroxyethlamino amides and their use in treatment of aspartyl protease mediated diseases and conditions.Type: GrantFiled: December 7, 2004Date of Patent: August 5, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Steve J. Coats, Dennis J. Hlasta, Mark J. Schulz
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Patent number: 6849750Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.Type: GrantFiled: April 23, 2002Date of Patent: February 1, 2005Assignee: Pharmacia & UpJohn Company LLCInventor: Michael R. Reeder
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Patent number: 6818727Abstract: Provided is an epoxy resin having glycidylamino group, wherein the content of hydrolyzable chlorine is 1000 ppm or less. The epoxy resin is useful for adhesives, paints and electric/electronic materials(e.g. insulation materials, laminated plate, etc.).Type: GrantFiled: May 27, 1999Date of Patent: November 16, 2004Assignee: Sumitomo Chemical Company, LimitedInventors: Akira Yokota, Nobuyuki Nakajima
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Patent number: 6570027Abstract: A synthesis is described for intermediates which are readily amenable to the large scale preparation of hydroxyethylurea-based chiral HIV protease inhibitors. The method includes forming a diastereoselective epoxide from a chiral alpha amino aldehyde.Type: GrantFiled: April 3, 2002Date of Patent: May 27, 2003Assignee: G. D. Searle & Co.Inventors: John S Ng, Claire A. Przybyla, Richard A Mueller, Michael L Vazquez, Daniel P Getman
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Patent number: 6278002Abstract: A process for producing (2R,3S)-3-amino-4-phenylbutane-1,2-epoxide compounds which comprises treating a (2S,3S)-3-amino-1-halo-2-hydroxy-4-phenylbutane compound or a (2S,3S)-3-amino-4-phenylbutane-1,2-epoxide with a carboxylic acid quaternary ammonium salt or a carboxylic acid metal salt a quaternary ammonium salt and a quaternary ammonium salt, to give a (2S,3S)-1-acyloxy-3-amino-2-hydroxy-4-phenylbutane compound, further treating the same with a sulfonic acid halide in the presence of an organic base to give a (2S,3S)-1-acyloxy-3-amino-2-sulfonyloxy-4-phenylbutane compound, furthermore treating said compound with an inorganic base.Type: GrantFiled: September 1, 2000Date of Patent: August 21, 2001Assignee: Kaneka CorporationInventors: Kazumi Okuro, Kenji Inoue
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Patent number: 6153771Abstract: 5-Substituted isophthalic acid bis(allylamides) and bis(allylamide epoxides) in which said 5-substituent is --NO.sub.2, --NH.sub.2, --NHR.sup.1 or --NR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are independently optionally substituted alkyl, alkenyl, acyl, aryl, aralkyl or alkaryl groups.Type: GrantFiled: September 30, 1998Date of Patent: November 28, 2000Assignee: Nycomed Imaging ASInventors: David Redick Lane, Janis Vasilevskis
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Patent number: 6127556Abstract: In a method of preparing an aminoepoxide wherein a protected aminoaldehyde is reacted with a halomethyl organometallic reagent in an appropriate solvent at a temperature above -80.degree. C., wherein said halomethyl organometallic reagent is formed by reaction between an organometallic reagent and a dihalomethane, the improvement comprising flowing said protected aminoaldehyde into a mixing zone maintained at a temperature below 0.degree. C., also flowing said halomethyl organometallic reagent in said mixing zone for contacting in said mixing zone with said protected aminoaldehyde and also withdrawing from said mixing zone reaction products of said protected aminoaldehyde and said halomethyl organometallic reagent.Type: GrantFiled: December 16, 1997Date of Patent: October 3, 2000Assignee: G. D. Searle & Co.Inventors: Chin Liu, John S. Ng, James R. Behling, Arthur L. Campbell
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Patent number: 5998330Abstract: A method of treating vegetation by application of a microbial insecticide in which a quinone has been covalently bonded to the viral occlusion body surface of the microbial insecticide in order to improve the UV stability of the microbial insecticide by forming a protective shield around the pathogen.Type: GrantFiled: February 21, 1997Date of Patent: December 7, 1999Assignee: The Board of Trustees of the University of ArkansasInventor: Gary W. Felton
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Patent number: 5962704Abstract: A method for producing an amide derivative of the formula ?XV! ##STR1## wherein each symbol is as defined in the specification, and an enantiomer thereof, a novel intermediate useful for producing said compound and a production method thereof. The production method of the present invention is extremely easy and simple as compared to the conventional methods, and enables effective production of compound ?XV! at high yields, which includes compound ?XVI! having an HIV protease inhibitory action. In addition, the novel intermediates of the present invention are extremely useful as intermediates for producing not only the aforementioned compound ?XVI! but also compounds useful as X-ray contrast media.Type: GrantFiled: March 25, 1998Date of Patent: October 5, 1999Assignees: Japan Tobacco Inc., Agouron Pharmaceuticals, Inc.Inventors: Takashi Inaba, Yasuki Yamada
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Patent number: 5962683Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.Type: GrantFiled: June 17, 1997Date of Patent: October 5, 1999Assignee: Ciba Specialty Chemicals Corp.Inventors: Alfred Steinmann, Rolf Mulhaupt
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Patent number: 5883264Abstract: Process for preparing optically active trans-3-phenylglycidamide compound, which comprises subjecting racemic trans-3-phenylglycidamide compound of the formula (I) ##STR1## wherein Ring A is substituted or unsubstituted benzene, and R.sup.1 is H or lower alkyl, to optical resolution using a microorganism having ability of preferentially hydrolyzing one of (2S,3R) isomer or (2R,3S) isomer thereof, and process for preparing an optically active 1,5-benzothiazepine derivative from the thus-obtained optically active trans-3-phenylglycidamide compound.Type: GrantFiled: March 6, 1997Date of Patent: March 16, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hiroaki Matsumae, Akiko Idei, Takuo Nishida, Yasuhiko Ozaki, Takeji Shibatani
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Patent number: 5883121Abstract: The invention relates an epoxysuccinamide derivative represented by the general formula (1) ##STR1## wherein R.sup.1 and R.sup.2 are the same or different from each other and independently represent H or an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.1 and R.sup.2 may form a nitrogen-containing heterocyclic ring together with the adjacent nitrogen atoms, R.sup.3 is H or an acyl group, R.sup.4 is H or an aralkyl group, and R.sup.5 is an aromatic hydrocarbon group or aralkyl group which may be substituted, or R.sup.5 may form an amino acid residue, which may be protected, together with the adjacent nitrogen atom, or a salt thereof, and a medicine comprising the derivative as an active ingredient; and this compound has an inhibiting activity against cathepsin, and particularly, specifically inhibits cathepsin L and is hence useful for prevention and treatment of osteopathy such as osteoporosis.Type: GrantFiled: August 12, 1997Date of Patent: March 16, 1999Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Tomohiro Yamashita, Yoshimitsu Suda, Yukio Tada, Nobuhiko Katunuma, Tetsuji Asao
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Patent number: 5854303Abstract: A polymeric material incorporating a polyvalent cation chelating agent in an amount effective to inhibit the growth of an ocular pathogen, particularly a protozoan, can be used to produce eye care products such as contact lens cases and containers for containing eye care solutions and contact lenses.Type: GrantFiled: January 27, 1998Date of Patent: December 29, 1998Assignee: Allergan Sales, Inc.Inventors: Charles Hayes Powell, David C. Rupp
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Patent number: 5773468Abstract: The present invention relates to a novel compound of formula (I) and pharmaceutically acceptable salts, hydrates and solvates thereof which is an irreversible HIV protease inhibitor; a process for the preparation thereof; and a pharmaceutical composition containing the compound as an active ingredient which is useful for treating or preventing diseases caused by HIV infection.Type: GrantFiled: December 14, 1995Date of Patent: June 30, 1998Assignee: LG Chemical LimitedInventors: Sung Chun Kim, Young Chan Son, Ho Il Choi, Heungsik Yoon, Chi Hyo Park, Nakyen Choy, Chang Sun Lee, Jong Sung Koh, Kwang Yul Moon, Won Hee Jung, Chung Ryeol Kim
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Patent number: 5763631Abstract: Cis-epoxide compounds of formula (I-3) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or arly-substituted lower alkyl group;K and J are independently a group having the formula of ##STR2## wherein R.sup.18 is a lower alkyl group optionally substituted with an aryl radical; X is O, NH, or N--CH.sub.3 ; and R.sup.19 is an aromatic hetercyclic sysstem containing a nitrogen atom in its ring, or a lower alkyl group optionally substituted with an aryl radical, or a hydrogen;G is an amino acid which is linked to K-- and ##STR3## by peptide bonds in formula (I-3); Q is an amino acid which is linked toby peptide bonds in formula (I-3), or a group having the formula ofwherein R.sup.20 is a lower alkyl group optionally substituted with an aromatic radical; and Y is CH.sub.2, O or NH; andr is 0 or 1, except that Q is a group having the formula ofr is 0.Type: GrantFiled: June 20, 1996Date of Patent: June 9, 1998Assignee: Lucky LimitedInventors: Sung Chun Kim, Nakyen Choy, Chang Sun Lee, Ho I. Choi, Jong Sung Koh, Heungsik Yoon, Chi Hyo Park, Sang Soo Kim, Young Chan Son
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Patent number: 5739178Abstract: A polymeric material incorporating a polyvalent cation chelating agent in an amount effective to inhibit the growth of an ocular pathogen, particularly a protozoan, can be used to produce eye care products such as contact lens cases and containers for containing eye care solutions and contact lenses.Type: GrantFiled: May 15, 1995Date of Patent: April 14, 1998Assignee: AllerganInventors: Charles Hayes Powell, David C. Rupp
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Patent number: 5717054Abstract: This invention relates to flexible epoxy resins that have a structural composition comprising an oligomeric backbone of alkylene or alkyleneoxy repeat units, terminated with an aromatic moiety bearing one or more epoxy functionalities.Type: GrantFiled: May 31, 1996Date of Patent: February 10, 1998Assignee: National Starch & Chemical Investment Holding Corp.Inventor: Rose Ann Schultz
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Patent number: 5693847Abstract: The present invention relates to functionalized ketones and novel processes for synthesizing those ketones. The processes of this invention are especially well suited for synthesizing .alpha.-methyl leaving group functionalized ketones. This invention also relates to processes for using .alpha.-methyl leaving group functionalized ketones to produce other compounds and intermediates useful in those processes.Type: GrantFiled: April 19, 1995Date of Patent: December 2, 1997Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger D. Tung, Thomas E. D'Ambra
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Patent number: 5679687Abstract: The present invention relates to novel compounds of formula (I) which have inhibitory activity against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group;R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group;R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group;R.sup.4 is hydrogen or a C.sub.1-4 alkyl group;R.sup.5 is an aromatic group, a C.sub.1-10 alkyl group or a C.sub.1-4 alkyl groups optionally substituted with an aromatic group; andn is 1 or 2.Type: GrantFiled: June 6, 1996Date of Patent: October 21, 1997Assignee: LG Chemical LimitedInventors: Nakyen Choy, Hoil Choi, Chi-Hyo Park, Young-Chan Son, Chang-Sun Lee, Heungsik Yoon, Sung-Chun Kim, Jong-Sung Koh, Chung-Ryeol Kim
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Patent number: 5670517Abstract: The present invention relates to novel compounds of formula (I) which has inhibitory activities against human immunodeficiency virus ("HIV") protease, a process for the preparation thereof, and compositions for prevention or treatment of AIDS by HIV infection comprising the above compounds as active ingredients. ##STR1## wherein: R.sup.1 is an aromatic group, a nitrogen-containing aromatic group, C.sub.1-4 alkyl group optionally substituted with an aromatic group or a nitrogen-containing aromatic group, C.sub.1-4 alkoxy group optionally substituted with an aromatic group or a nitrogen-containing aromatic group;R.sup.2 is an amino acid residue or a C.sub.1-8 alkyl group substituted with a C.sub.1-4 alkylsulfonyl group;R.sup.3 is a C.sub.1-4 alkyl group optionally substituted with an aromatic group;R.sup.4 is hydrogen or a C.sub.1-2 alkyl group;R.sup.5 is a C.sub.1-10 alkyl group optionally substituted with an aromatic group; andn is 1 or 2.Type: GrantFiled: June 6, 1996Date of Patent: September 23, 1997Assignee: LG Chemical LimitedInventors: Nakyen Choy, Hoil Choi, Chi-Hyo Park, Young-Chan Son, Chang-Sun Lee, Heungsik Yoon, Sung-Chun Kim, Jong-Sung Koh, Chung-Ryeol Kim
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Patent number: 5670675Abstract: A retroviral protease inhibiting compound of the formulaA-X-Bor a pharmaceutically acceptable salt, prodrug or ester thereof, wherein X is a linking group;A is(1) substituted amino,(2) substituted carbonyl,(3) functionalized imino,(4) functionalized alkyl,(5) functionalized acyl,(6) functionalized heterocyclic or(7) functionalized (heterocyclic)alkyl; andB is(1) substituted carbonyl independently defined as herein,(2) substituted amino independently defined as herein,(3) functionalized imino independently defined as herein,(4) functionalized alkyl independently defined as herein,(5) functionalized acyl independently defined as herein,(6) functionalized heterocyclic independently defined as herein or(7) functionalized (heterocyclic)alkyl independently defined as herein.Type: GrantFiled: March 23, 1995Date of Patent: September 23, 1997Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck
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Patent number: 5668227Abstract: Novel cyclohexyl-group-containing glycidyl ethers of formulae I to IV according to claim 1, which are distinguished especially by a low chlorine content and a low viscosity and which can be used, for example, in epoxy resin formulations as reactive diluents, flexibilisers or adhesion enhancers, or can also be polymerised per se and used as coatings or casting resins, the products having only slight water absorption and having good external weather resistance.Type: GrantFiled: March 11, 1996Date of Patent: September 16, 1997Assignee: Ciba-Geigy CorporationInventors: Heinz Wolleb, Andreas Kramer
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Patent number: 5650412Abstract: Compounds of formula ##STR1## are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.Type: GrantFiled: October 26, 1995Date of Patent: July 22, 1997Assignee: Merck & Co., Inc.Inventors: Byeong Moon Kim, Joseph P. Vacca
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Patent number: 5618939Abstract: A process is disclosed for making a chiral compound of the formula ##STR1## comprising reacting an epoxide compound of the formula ##STR2## and an amide of the formula ##STR3## in the presence of a strong base at a low temperature.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: Merck & Co., Inc.Inventors: David Askin, Paul Reider, Kai Rossen, Richard J. Varsolona, Ralph P. Volante, Kenneth M. Wells
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Patent number: 5612339Abstract: 2-Hydroxy-3-aminopropylsulfonamides are provided along with methods for synthesizing and using such compounds, and chemical intermediates employed in the synthetic methods.Type: GrantFiled: January 17, 1995Date of Patent: March 18, 1997Assignee: Trustees Of The University Of PennsylvaniaInventors: Paul Sprengeler, Amos B. Smith, III, Ralph F. Hirschmann, Akihisa Yokoyama
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5552558Abstract: A retroviral protease inhibiting compound of the formula: ##STR1## is disclosed.Type: GrantFiled: March 27, 1995Date of Patent: September 3, 1996Assignee: Abbott LaboratoriesInventors: Dale J. Kempf, Daniel W. Norbeck
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Patent number: 5508430Abstract: Novel alcohols of the formula ##STR1## wherein R.sup.a is azido or phthalimido, R.sup.4 is alkyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl, R.sup.7 and R.sup.8 together are a trimethylene or tetramethylene group which is optionally substituted by hydroxy, alkoxycarbonylamino or acylamino or in which one --CH.sub.2 -- group is replaced by --NH--, --N(alkoxycarbonyl)--, --N(acyl)-- or --S-- or which carries a fused cycloalkane, aromatic or heteroaromatic ring, and R.sup.9 is alkoxycarbonyl, monoalkylcarbamoyl, monoaralkylcarbamoyl, monoarylcarbamoyl or a group of the formula ##STR2## in which R.sup.10 and R.sup.11 each is alkyl, are described along with a process for their manufacture. These alcohols are useful as intermediates, for example in the manufacture of amino acid derivatives having antiviral activity.Type: GrantFiled: May 12, 1995Date of Patent: April 16, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Kevin E. B. Parkes, Sally Redshaw, Gareth J. Thomas
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Patent number: 5391552Abstract: A diphenylpiperazine derivative represented by general formula (1), salt thereof, and drug for the circulatory organs containing the same as the active ingredient: ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different from each other and each represents hydrogen, halogen, alkyl, alkoxy, nitro, amino, hydroxy, optionally esterified carboxyl or trifluoromethyl; R.sup.3 represents hydrogen, alkyl, aralkyl, acyl, nitro or optionally esterified carboxymethyl; Ar represents phenyl or naphthyl which may have one to three substituents such as halogen, alkyl, alkoxy, aryloxy, aralkyloxy, nitro, amino, cyano, acyl, hydroxy, optionally esterified carboxyl, substituted sulfonyl, aryl or trifluoromethyl; Z represents sulfur or -NR.sup.4 - wherein R.sup.4 represents hydrogen, alkyl, aralkyl, acyl, aryl, substituted sulfonyl or optionally esterified carboxyl; m represents a number of 1 to 5; and n represents a number of 0 to 5.Type: GrantFiled: May 10, 1993Date of Patent: February 21, 1995Assignee: Pola Chemical Industries, Inc.Inventors: Masato Inazu, Yoshiyuki Miyata, Toshihiro Morimoto, Takeshi Yamamoto, Yuji Yoshiko, Kazunori Harada, Yoshiharu Momota, Masayuki Yanagi, Ryoko Yokota, Tetsuo Katoh, Takayuki Namiki, Makoto Kimura, Nobuyuki Kawakatsu
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Patent number: 5362849Abstract: The new compound N,N,N'N'-tetraglycidyl-3,3'-diethyl-4,4'-diaminodiphenylmethane and curable resin compositions containing it.Type: GrantFiled: November 4, 1993Date of Patent: November 8, 1994Assignee: Ciba-Geigy CorporationInventors: Bryan Dobinson, Michael R. Thoseby
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Patent number: 5360884Abstract: Glycidyl amines containing mesogenic moieties result in improved properties when cured. These amines are useful in coatings, adhesives, encapsulants, moldings, laminates, and the like.Type: GrantFiled: May 28, 1992Date of Patent: November 1, 1994Assignee: The Dow Chemical CompanyInventors: Robert E. Hefner, Jr., Jimmy D. Earls
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Patent number: 5310956Abstract: The present invention is optically active epoxides and its production characterized in that the process comprises reacting alkenyl ethylene glycols with 0.5 to 2.0 equivalents of a titanium-tetraalkoxyde, a peroxide and an L-(+)- or D-(-)-dialkyl tartrate at a temperature of -78.degree. to 50.degree. C. to asymmetrically oxidize the alkenyl ethylene glycols. The production of the present invention is an excellent method for producing chiral epoxides in which steric configuration of three asymmetric points can be perfectly controlled, the reaction is performed by mild conditions and the chemical yield and the optical yield are extremely high. The optically active epoxides which can be efficiently produced by the production of the present invention are useful as stating materials of several kinds of compounds.Type: GrantFiled: May 19, 1993Date of Patent: May 10, 1994Assignee: Chisso CorporationInventors: Seiichi Takano, Kunio Ogasawara
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Patent number: 5283270Abstract: Disclosed are glycidyl diamines having the formulas ##STR1## where n is 1 or 2, m is 0, 1, or 2, X is Y or ##STR2## and Y is --, O, S, SO, SO.sub.2, CO, C(CH.sub.3).sub.2, or C(CF.sub.3).sub.2. An epoxy resin can be made by mixing the glycidyl diamine with an epoxy curing agent. The epoxy resins can be used as adhesives or to make composites.Type: GrantFiled: February 5, 1993Date of Patent: February 1, 1994Assignee: Occidental Chemical CorporationInventors: Robert A. Buchanan, Robert L. Ostrozynski
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Patent number: 5280069Abstract: The new compound N,N,N'N'-tetraglycidyl-3,3'-diethyl-4,4'-diaminodiphenylmethane and curable resin compositions containing it.Type: GrantFiled: April 30, 1991Date of Patent: January 18, 1994Assignee: Ciba-Geigy CorporationInventors: Bryan Dobinson, Michael R. Thoseby
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Patent number: 5266365Abstract: The present invention is directed to an epoxy-containing polymeric material having nonlinear optical properties, particularly a glycidyl amine polymer, and a process for making the nonlinear optical (NLO) epoxy-containing polymeric material including poling the polymeric material under high voltage at elevated temperature for a period of time to bring about orientation of the nonlinear optical functionalities in the polymer. The polymers have enhanced thermal stability and good NLO properties.Type: GrantFiled: February 28, 1992Date of Patent: November 30, 1993Assignee: The Dow Chemical CompanyInventors: John J. Kester, H. Craig Silvis