The Nitrogen Is Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 549/553)
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Publication number: 20150025257Abstract: The invention describes novel mono or dihydroxy docosahexaenoic acid (DHA) analogues, their preparation, isolation, identification, purification and uses thereof.Type: ApplicationFiled: June 8, 2012Publication date: January 22, 2015Applicant: The Brigham and Women's Hospital, Inc.Inventors: Charles N. Serhan, Rong Yang
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Patent number: 8501937Abstract: 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: March 28, 2012Date of Patent: August 6, 2013Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Dennis J. Hlasta, Mark J. Schulz
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Patent number: 8097741Abstract: The invention relates to solvent-containing two-component polyurethane moisture cured hybrid sol-gel coating formulation comprising 1) an epoxy-functional binder with carbamate functionality and 2) a blended curing component comprising at least one sol gel precursor and an amine crosslinker.Type: GrantFiled: March 31, 2008Date of Patent: January 17, 2012Assignee: NDSU Research FoundationInventors: Dean C. Webster, Dipak Chattopadhyay
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Publication number: 20110130479Abstract: Compounds of formula (I) in the field of heat-curing and two-component epoxy resin compositions, which may be used as adhesion promoters or adhesion promoter ingredients and methods of producing such compounds. Such compounds may be prepared as liquids. A heat-curing epoxy resin composition including at least one epoxy resin with more than one epoxy group per molecule on the average; at least one curing agent for epoxy resins, which is activated by elevated temperature; and at least one compound of formula (I).Type: ApplicationFiled: July 17, 2009Publication date: June 2, 2011Applicant: SIKA TECHNOLOGY AGInventors: Andreas Kramer, Jurgen Finter
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Publication number: 20110118347Abstract: A compound of the formula CH3(CH2)n—RA—(CH2)m-(CH?CH)q—(CH2)p—X wherein RA=(a); q=0 or 1; m and p are independently selected integers of at least 1; n=0 or an integer of at least 1; X is a polar group selected from —CO2RS, where Rs?H, Na, K, —NHRI, —NRIRII or RIII; —CH3OH; —CH3NH2; —CH3NHRI; or —CH3NRIRII; wherein RI, RII and RIII are independently selected from C1-C6 alkyl or an aryl group, preferably a hydrophilically substituted C1-C6 alkyl or aryl group, or RIII is an esterified glycol; and wherein 20>m+n+p+2q?2; is useful for the treatment of ringworm infection caused by Trichophyton tonsurans.Type: ApplicationFiled: May 29, 2009Publication date: May 19, 2011Applicant: Vernolix LimitedInventor: Michael William Fowler
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Publication number: 20110046321Abstract: An adduct and a process for preparing such adduct, wherein the adduct includes at least one reaction product of an epoxy resin material (A) and a compound (B); wherein the epoxy resin material (A) comprises a glycidyl ether or glycidyl ester of an alkanolamide; and compound (B) comprises a compound having two or more reactive hydrogen atoms per molecule, and the reactive hydrogen atoms are reactive with epoxide groups. A curable epoxy resin composition can be prepared from (i) the adduct described above, and (ii) one or more epoxy resins other than the epoxy resin material (A). A cured epoxy resin may be prepared from such curable composition including an article such as a coating, an electrical or structural laminate, an electrical or structural composite, a filament winding, a molding, a casting, and an encapsulation.Type: ApplicationFiled: May 18, 2009Publication date: February 24, 2011Inventors: Jim D. Earls, Robert E. Hefner, JR.
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Publication number: 20100319580Abstract: The invention relates to alcohol-modified glycidyl carbamate resins wherein at least some of the glycidol groups in the resin have been replaced with an alcohol. The invention also relates to coating compositions containing the resins.Type: ApplicationFiled: September 29, 2008Publication date: December 23, 2010Inventors: Dean C. Webster, Umesh Harkal, James Garrett
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Publication number: 20100179302Abstract: Manufacture of dichloropropanol Process for manufacturing dichloropropanol wherein a glycerol-based product comprising at least one diol containing at least 3 carbon atoms other than 1,2-propanediol, is reacted with a chlorinating agent, and of products derived from dichloropropanol such as epichlorohydrin and epoxy resins. No figure.Type: ApplicationFiled: June 20, 2008Publication date: July 15, 2010Applicant: SOLVAY (SOCIETE ANONYME)Inventors: Philippe Krafft, Patrick Gilbeau
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Publication number: 20100144917Abstract: The invention is to provide an epoxy compound or an actinic energy radiation hardenable composition each having high safety and stability, and to provide an actinic energy radiation hardenable composition with excellent photo-hardenability under high humidity, which gives high solvent resistance, high water proof and a hardened layer with high strength. There is provided an actinic energy radiation hardenable composition containing an epoxy compound represented by the following formula (1).Type: ApplicationFiled: July 12, 2006Publication date: June 10, 2010Applicant: KONICA MINOLTA MEDICAL & GRAPHIC, INC.Inventor: Nobumasa Sasa
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Patent number: 7612237Abstract: The present invention is directed to a process for preparing ?-amino-?-hydroxycarboxamides. The process works with epoxycarboxamides of the formula 2 which are reacted with ammonia or other amines.Type: GrantFiled: June 29, 2007Date of Patent: November 3, 2009Assignee: Degussa GmbHInventor: Günter Knaup
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Publication number: 20090247708Abstract: The invention relates to compounds embodying amino group-terminal viscosifiers, the resultant products thereof, and the uses thereof. The inventive viscosifiers are provided with formula (I), wherein R1 represents a divalent radical of a carboxyl group-terminal butadiene/acrylonitrile copolymer after removing the terminal carboxyl groups. The disclosed compounds increase the viscosity of the compositions formulated therewith. Compounds containing glycidyl groups are particularly important as resultant products thereof which can be used in thermosetting single-component epoxy resin adhesives.Type: ApplicationFiled: August 16, 2006Publication date: October 1, 2009Applicant: SIKA Technology AGInventors: Ulrich Gerber, Juergen Finter
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Publication number: 20090105156Abstract: The invention relates to crystalline peptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions. This invention also relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.Type: ApplicationFiled: October 3, 2008Publication date: April 23, 2009Applicant: Proteolix, Inc.Inventors: Pasit Phiasivongsa, Louis C. Sehl, William Dean Fuller, Guy J. Laidig
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Publication number: 20080167332Abstract: Compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, and R10 are as defined in the specification, are described. The present invention also relates to pharmaceutical composition comprising said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. Beside, the invention relates to salts and polymorphic forms of the new compounds as well as the preparation thereof.Type: ApplicationFiled: July 18, 2007Publication date: July 10, 2008Inventors: Scott Gibson, Barry Elkins, Mike Rogers, Ian Hassall, Hong Gu, Zhenyu Wang, Vinod Kumar, Synthana Suresh Kumar, Santosh Kavitake, Sidda Lingesha, Eric Merifield, David Ennis, John Pavey, Austen Pimm, James Reuberson, Bo-Goran Josefsson, Martin Hemmerling, Svetlana Ivanova, Marguerite Mensonides-Harsema, Hakan Schulz, John Mo, Tomas Eriksson, Per Strandberg
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Patent number: 7326799Abstract: The present invention is to provide manufacturing intermediates which can be led to useful ?-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: wherein R1 and R2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R6—O— or R7—N(R8)—; where R6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R7 and R8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R4 and R5 represent the same groups as R7 and R8, respectively, and R4 and R5 optionally form a ring together; and X represents —O— or —N(R9)—, where R9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R4 or R5, andType: GrantFiled: December 30, 2002Date of Patent: February 5, 2008Assignee: Seikagaku Kogyo Kabushiki KaishaInventors: Nobuo Kobayashi, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
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Patent number: 6841536Abstract: Disclosed is a prodrug of the formula: where A is a sulfur or a selenium, and R is derived from a mono- di- or oligo- saccharide. Also disclosed is a prodrug of the formula: where A is sulfur or selenium, R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O, and the R? groups may be the same or different and may be hydrogen, alkyl, alkoxy, carboxy. Also disclosed is a conjugate of an antioxidant vitamin and a thiolamine or selenolamine. Also disclosed is a prodrug of the formula; where A is sulfur or selenium, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH, where n is 1 to 5, or R? is also be an alkyl or aryl group, or R? is ?O, and R‡ is an alkoxy, or an amine group. Also disclosed is a prodrug of the formula: where R is COOH or H, and R? is derived from a sugar and R? has the formula (CHOH)nCH2OH,where n is 1 to 5, or R? is an alkyl or aryl group, or R? is ?O.Type: GrantFiled: January 18, 2002Date of Patent: January 11, 2005Assignee: University of Utah Research FoundationInventors: Jeannette C. Roberts, Britta H. Wilmore, Pamela B. Cassidy, Pamela K. Dominick, Megan D. Short
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Patent number: 6812229Abstract: It is to provide a novel fungicide having high controlling effects on plant diseases particularly on wheat powdery mildew and cucumber gray mold, without ill effects on crops. A carbamate derivative represented by the general formula [I] {wherein X is a halogen atom, a C1-C6 alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a C1-C6 alkyl group, R2 is a hydrogen atom, a C1-C6 alkyl group or the like, R3 is a hydrogen atom or a C1-C6 alkyl group, G is an oxygen atom, a sulfur atom or the like, Y is a hydrogen atom, a C1-C10 alkyl group, C2-C10 alkenyl group or the like, and Q is a hydrogen atom, a C1-C6 haloalkyl group, a phenyl group or the like} and an agricultural/horticultural fungicide containing the same as the active ingredient.Type: GrantFiled: February 5, 2002Date of Patent: November 2, 2004Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Masami Ozaki, Shunichiro Fukumoto, Ryuji Tamai, Kazuhiro Ikegaya, Norihisa Yonekura, Takahiro Kawashima, Junetsu Sakai, Norimichi Muramatsu, Makikazu Takagaki, Kouzou Nagayama
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Patent number: 6743929Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 6, 2000Date of Patent: June 1, 2004Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
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Publication number: 20030153788Abstract: The present invention is to provide manufacturing intermediates which can be led to useful &agr;-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide epoxycarboxamide compounds, azide compounds and amino alcohol compounds represented by the following formulae: 1Type: ApplicationFiled: December 30, 2002Publication date: August 14, 2003Applicant: Seikagaku CorporationInventors: Nobuo Kobayashi, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
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Publication number: 20030065219Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)Type: ApplicationFiled: October 16, 2002Publication date: April 3, 2003Applicant: Pharmacia & Upjohn CompanyInventor: Bruce Allen Pearlman
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Patent number: 6437134Abstract: A method for making phenylthiobutyl-isoquinoline compounds of formula and novel intermediates therefor.Type: GrantFiled: March 29, 2001Date of Patent: August 20, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 6376468Abstract: The invention pertains to novel peptide analogs suitable for inhibiting protein:prenyl transferases. As such they are therapeutically useful in e.g. inhibiting oncogenesis and other unwanted cell proliferation, and in supressing aberrant high signal transduction. The analogs comply with the following formula: in which: R1 is hydrogen or a thiol-protecting group; R2 and R3 are independently hydrogen or C1-C4 alkyl; R4 is hydrogen, C1-C4 alkyl, C1-C4 acyl or peptidyl; R5 is hydrogen or C1-C4 alkyl; R6 is hydrogen or optionally substituted C1-C6 alkyl; A is a direct bond or an optionally substituted C1-C4 alkylene chain; Y represents an oxo group or two hydrogen atoms; Z is oxygen, sulphur, imino or C1-C5 alkyl-, aryl- or acylimino; M is 0, 1 or 2; N is 0 or 1.Type: GrantFiled: February 3, 2000Date of Patent: April 23, 2002Assignees: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO, Rijksuniversiteit LeidenInventors: Herman Steven Overkleeft, Steven Hendrik Leonard Verhelst, Nicolaas Johannes Meeuwenoord, Elsbet Jantine Pieterman, Louis Hartog Cohen, Mark Overhand, Gijsbert Arie Van der Marel, Jacobus Hubertus Van Boom
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Patent number: 6369188Abstract: Polyfunctional polymerizable urethane- or urea-containing oligomers allow the design, adjustment, and regulation of chemical and physical properties of the described oligomers. The invention discloses the formulas and compositions of these oligomers, methods of their synthesis, and methods of converting the described oligomers into useful polymeric products. The described oligomers can be used for many purposes, both directly and in combination with other chemicals in multiple applications such as adhesives, sealants, coatings, composites, etc., as well as in castable and moldable materials.Type: GrantFiled: March 27, 1999Date of Patent: April 9, 2002Assignee: Polymeright, Inc.Inventors: Leonid Rappoport, Alex Vainer, Aleksandr Yam
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Publication number: 20020032348Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)Type: ApplicationFiled: August 9, 2001Publication date: March 14, 2002Inventor: Bruce Allen Pearlman
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Publication number: 20020019538Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: ApplicationFiled: August 10, 2001Publication date: February 14, 2002Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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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: 6268533Abstract: A method is disclosed for the preparation of optically pure isomers of formoterol by the reaction of an optically pure 4-benzyloxy-3-formamidostyrene oxide with an optically pure 4-methoxy-&agr;-methyl-N-(phenylmethyl)benzeneethanamine followed by debenzylation. Useful intermediates in the process are also disclosed, as are the novel L-tartrate salt of R,R-formoterol and pharmaceutical compositions thereof.Type: GrantFiled: January 27, 2000Date of Patent: July 31, 2001Assignee: Sepracor Inc.Inventors: Yun Gao, Robert Hett, Kevin Q. Fang, Stephen A. Wald, Chris Hugh Senanayake
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Patent number: 6239296Abstract: Intermediate compounds useful for making phenylthiobutyl-isoquinoline compounds of formulaType: GrantFiled: February 25, 2000Date of Patent: May 29, 2001Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 6225478Abstract: Novel iridoid derivatives represented by general formula (I): and a vascularization inhibitor having for its active ingredient said derivative are disclosed. This vascularization inhibitor has remarkable vascularization inhibitory effects unaccompanied by serious adverse side effects, which is useful for the treatment and prevention of various diseases accompanied by abnormal acceleration of vascularization.Type: GrantFiled: September 13, 1999Date of Patent: May 1, 2001Assignee: Tsumura & Co.Inventors: Hideaki Morishige, Yukiko Kurita, Yousuke Yamazaki, Chiaki Sakakibara, Masaharu Kigawa
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Patent number: 6207704Abstract: Novel compounds that are anti-angiogenic or immunosuppressive are described. Also described are methods for determining if an animal is at risk for a disease involving abnormal angiogenesis or an immune reaction resulting in pathology comprising evaluating an aspect of MetAP2 metabolism or structure; methods for identifying agents that are anti-angiogenic or immunosuppressive comprising evaluating the effect of the agent on an aspect of MetAP2 metabolism; methods for treating a cell having an abnormality in metabolism or structure of MetAP2; and methods for treating abnormal angiogenesis or an immune reaction which results in pathology in an animal. Pharmaceutical compositions are also provided.Type: GrantFiled: June 8, 1998Date of Patent: March 27, 2001Assignee: Massachusetts Institute of TechnologyInventors: Jun O. Liu, Eric C. Griffith, Zhuang Su
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 6133457Abstract: A compound of formula IV ##STR1## wherein G is C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl or Ar;Ar is an aromatic or heteroaromatic group or a substituted aromatic or heteroaromatic group;R.sup.1 is halo, SR, OR, amino, mono or di-(C.sub.1 -C.sub.6 -alkyl)amino, tri (C.sub.1 -C.sub.6 -alkyl)ammonium, C.sub.1 -C.sub.6 -alkylthio, di(C.sub.1 -C.sub.6 -alkyl)sulfonium, C.sub.1 -C.sub.6 -alkylsulfonyl, or C.sub.1 -C.sub.6 -alkylphosphonyl;R.sup.2 is OH or SH; orR.sup.1 and R.sup.2 taken together form a second bond or together form an epoxide, aziridine, episulfide, or cyclopropyl ring;R is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkanoyl or Ar;R.sup.3 is C.sub.1 -C.sub.6 alkyl;R.sup.4 and R.sup.5 are H; orR.sup.4 and R.sup.5 taken together form a second bond;R.sup.24 is a leaving group; andR.sup.26 is an alcohol protecting group;X is O, NH or (C1-C3 alkyl)N--.Type: GrantFiled: July 2, 1999Date of Patent: October 17, 2000Assignees: Eli Lilly and Company, Wayne State University, University of HawaiiInventor: Vinod F Patel
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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: 6013836Abstract: This invention relates to N'-substituted-N,N'-disubstitutedhydrazines of formula I ##STR1## wherein X and X' are independently O, S, or NR; A' and B' are independently substituted or unsubstituted aryl or aromatic heterocycle; wherein F is alkyl, alkenyl, or aralkyl; and wherein E is a tertiary carbon containing organic radical having a total of at least four carbon and halogen atoms but not more than six halogen atoms, or a non-tertiary carbon containing non-haloalkyl organic or organometallic radical having at least five atoms other than hydrogen, oxygen and halogen which are useful as insecticides, compositions containing those compounds, methods of producing the compounds, and methods of their use. More particularly, the invention relates to insect growth regulating compounds and compositions, and methods of using such compounds and compositions. Compounds of the present invention are particularly suitable for controlling plant-destructive insects in crops of cultivated plants, ornamentals and forestry.Type: GrantFiled: May 22, 1995Date of Patent: January 11, 2000Assignee: Rohm and Haas CompanyInventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
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Patent number: 5994539Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.Type: GrantFiled: December 18, 1997Date of Patent: November 30, 1999Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
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Patent number: 5977387Abstract: This invention provides processes for preparing cryptophycin compounds and novel intermediates which are useful in such processes.Type: GrantFiled: February 25, 1998Date of Patent: November 2, 1999Assignees: Eli Lilly and Company, Wayne State University, University of HawaiiInventor: Vinod F Patel
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Patent number: 5977388Abstract: A process for the manufacture of the .alpha.,.alpha.'-diaminoalcohol of formula ##STR1## is via N-protected L-phenylalanine lower alkyl esters, corresponding N-protected .alpha.-amino-.alpha.'-haloketones, and .alpha.-amino-.alpha.'-haloalcohols.Type: GrantFiled: July 9, 1998Date of Patent: November 2, 1999Assignee: Hoffmann-La Roche Inc.Inventor: Hans Hilpert
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Patent number: 5965609Abstract: The invention concernes borneol esters of general formula (I), in which R.sup.1 means T--C(O)--CH(OR.sup.6)--(NR.sup.7a R.sup.7b)--R.sup.8, C(O)--CH(OR.sup.6a)--CH[NR.sup.7 (C(O)--CH(OR.sup.6b)--CH (NR.sup.7a R.sup.7b)--R.sup.8a)]--R.sup.8b ; R.sup.7a R.sup.7b are identical or different and means R.sup.7 ; R.sup.7 means hydrogen, A, --C(O)R.sup.12, --C(O)OR.sup.12, --C(O)SR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, --SO.sub.2 R.sup.12, C.sub.1 -C.sub.10 alkyl; R.sup.8a, R.sup.8b are identical or different and mean R.sup.8 ; R.sup.8 means (i), heteroaryl substituted by X.sup.3, C.sub.7 -C.sub.16 aralkyl, alkyl; A is B--[O--(CH.sub.2).sub.t --C(O)].sub.0 or 1-, farnesyl--P(O)(OR.sup.9d)--O--(CH.sub.2).sub.t --C(O)--; B means protein kinase-inhibitors or farnesyl protein transferase-inhibitors such as for example farnesyl (ii); and T is a bond, Z.sup.i or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.Type: GrantFiled: March 13, 1998Date of Patent: October 12, 1999Assignee: Schering AGInventors: Ulrich Klar, Hermann Graf, Gunter Neef, Siegfried Blechert
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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: 5792792Abstract: The invention relates to borneol derivatives of general formula I ##STR1## in which R.sup.1 means C(O)--CH(OR.sup.6)--CH(NHR.sup.7)--R.sup.8,R.sup.2 means hydrogen, --OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9a, --OSO.sub.2 R.sup.9a, --OP(O)(OH).sub.2, NHR.sup.9a, NR.sup.9a R.sup.9b,R.sup.3 means hydrogen, --OH, C.sub.1 -C.sub.10 alkoxy, --OC(O)R.sup.9b, --OSO.sub.2 R.sup.9b, --OP(O)(OH).sub.2, orR.sup.2, R.sup.3 together mean an oxygen atom,R.sup.4 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.n --OR.sup.11a,R.sup.5 means hydrogen, C.sub.1 -C.sub.10 alkyl, --(CH.sub.2).sub.p --OR.sup.11b, orR.sup.4, R.sup.5 together mean an oxygen atom, a=CHR.sup.10 group,n means 0 to 8,p means 1 to 8,R.sup.7 means --C(O)R.sup.12, --SO.sub.2 R.sup.12, --C(O)OR.sup.12, --C(O)NHR.sup.9d, --C(O)NR.sup.9d R.sup.9e, ##STR2## R.sup.8 means aryl, R.sup.9a-e, R.sup.12 are the same or different and mean C.sub.1 -C.sub.10 alkyl, C.sub.4 -C.sub.8 cycloalkyl, aryl, C.sub.7 -C.sub.16 aralkyl,R.sup.Type: GrantFiled: January 3, 1997Date of Patent: August 11, 1998Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hermann Graf, Gunter Neef, Siegfried Blechert
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Patent number: 5744621Abstract: Cis-epoxide compounds of formula (I-1) and pharmaceutically acceptable salts, hydrates and solvates thereof: ##STR1## wherein: R.sup.1 is a cycloalkyl, or aryl-substituted lower alkyl group;A is a functionalized acyl group of the formula ##STR2## wherein R.sup.2 is a C.sub.1-4 alkyl, or amide-substituted C.sub.1-2 alkyl group;R.sup.3 is a C.sub.1-4 alkoxy, aryloxyalkyl or arylalkoxy, or a nitrogen-containing aromatic radical, or a lower alkoxy group substituted with a nitrogen-containing aromatic radical, or a radical having the formula of ##STR3## wherein R.sup.4 is a hydrogen or a methyl group and R.sup.5 is an alkyl group substituted with a nitrogen-containing aromatic radical; and m is 0 or 1; and B is a functionalized amino group of the formula ##STR4## wherein R.sup.8 and R.sup.9 are independently a C.sub.1-4 alkyl group optionally substituted with an aromatic radical, or an aromatic group.Type: GrantFiled: June 20, 1996Date of Patent: April 28, 1998Assignee: Lucky Limited.Inventors: Sung Chun Kim, Nakyen Choy, Chang Sun Lee, Young Chan Son, Ho Il Choi, Jong Sung Koh, Heungsik Yoon, Chi Hyo Park, Sang Soo Kim
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Patent number: 5736620Abstract: Epoxy resins containing rodlike mesogenic moieties are prepared from phenolic hydroxyl containing compounds which contain such moieties.Type: GrantFiled: May 25, 1995Date of Patent: April 7, 1998Assignee: The Dow Chemical CompanyInventors: Jimmy D. Earls, Robert E. Hefner, Jr., Paul M. Puckett
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Patent number: 5693859Abstract: There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.Type: GrantFiled: December 26, 1995Date of Patent: December 2, 1997Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Moriyasu Masui
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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: 5578608Abstract: An HIV protease inhibiting compound of formula I ##STR1## wherein: R is C.sub.1 -C.sub.6 alkyl, cycloalkyl, heterocycle, unsaturated heterocycle, aryl, cycloalkyl (C.sub.1 -C.sub.4)alkyl, heterocycle(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, or --A--(CH.sub.2).sub.q --R.sup.0, where A is --O--, --NH-- or --S--; q is 0, 1, 2 or 3; and R.sup.0 is cycloalkyl, aryl, heterocycle or unsaturated heterocycle; ##STR2## where R.sup.1 is aryl, cycloalkyl, heterocycle or unsaturated heterocycle; R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; R.sup.3 is an amino acid side chain, --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH.sub.2 (CH.sub.2).sub.2 CH.sub.3, --C(CH.sub.3).sub.3, cyano(C.sub.1 -C.sub.4)alkyl, unsaturated heterocycle (C.sub.1 -C.sub.4)alkyl, aryl(C.sub.1 -C.sub.4)alkyl, --(CH.sub.2).sub.s --A.sup.0 --(CH.sub.2).sub.r --R.sup.4, or --CH.sub.2 --C(O)--NR.sup.2 --(CH.sub.2).sub.r --R.sup.5, where s is 1, 2, 3 or 4; r is 0, 1, 2 or 3; A.sup.Type: GrantFiled: January 17, 1995Date of Patent: November 26, 1996Assignee: Eli Lilly and CompanyInventors: William J. Hornback, John E. Munroe
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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: 5502252Abstract: There is disclosed a process of producing an .alpha.-ketamide as an intermediate for use in the production of various alkoxyiminoacetamide compounds which are useful as fungicides. Also disclosed is an intermediate to be used in this process.Type: GrantFiled: November 10, 1994Date of Patent: March 26, 1996Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Moriyasu Masui
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Patent number: 5495029Abstract: Novel (meth)acrylates containing urethane groups Novel (meth)acrylates which also contain urethane groups and other polymerizable groups in one and the same molecule and can be polymerized either by means of free radicals and/or cationically are used for the production of coatings, adhesives, photoresists, solder masks or in stereolithography. The mouldings produced therefrom contain a coherent, homogeneous network and have high strength properties, in particular mechanical properties.Type: GrantFiled: August 4, 1994Date of Patent: February 27, 1996Assignee: Ciba-Geigy CorporationInventors: Bettina Steinmann, Jean-Pierre Wolf, Adrian Schulthess, Max Hunziker
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Patent number: 5481012Abstract: Process for the epoxidation of an unsaturated (meth)acrylic compound of formula: ##STR1## in which R.sub.1 is chosen from H and C.sub.1 -C.sub.5 -alkyl; R.sub.2 is chosen from H, alkyl and aryl; R.sub.3 is a straight-chain, branched or cyclic alkylene or oxyalkylene radical having from 1 to 12 carbon atoms, it being possible for one of the carbon atoms of R.sub.2, when the latter is an alkyl radical, to be linked to one of the carbon atoms of R.sub.3 to form a ring; and A is chosen from O, S, NH and NR.sub.4, R.sub.4 being a C.sub.1 -C.sub.12 -alkyl group; by the action of hydrogen peroxide on the said unsaturated (meth)acrylic compound, at a temperature of between 10.degree. C. and 50.degree. C., in the presence of at least one catalyst chosen from the alkali metal molybdates and the alkali metal pertungstates and in the presence of at least one phase transfer agent.Type: GrantFiled: November 3, 1994Date of Patent: January 2, 1996Assignee: AtochemInventors: Paul Caubere, Yves Fort, Agnes Ortar
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Patent number: 5391735Abstract: The present invention relates to a new process for the preparation of 3-substituted derivatives of 1-amino-2-hydroxy-propane in the form of single diastereoisomers, to certain of these diastereoisomers, and to compounds which are intermediates in the new process of the invention.Type: GrantFiled: April 12, 1994Date of Patent: February 21, 1995Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Piero Melloni, Arturo D. Torre, Ettore Lazzari, Giuseppe Mazzini