The Nitrogen Is Bonded Directly To A -c(=x)- Group, Wherein X Is Chalcogen Patents (Class 549/553)
  • Publication number: 20150025257
    Abstract: The invention describes novel mono or dihydroxy docosahexaenoic acid (DHA) analogues, their preparation, isolation, identification, purification and uses thereof.
    Type: Application
    Filed: June 8, 2012
    Publication date: January 22, 2015
    Applicant: The Brigham and Women's Hospital, Inc.
    Inventors: Charles N. Serhan, Rong Yang
  • Patent number: 8501937
    Abstract: 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: Grant
    Filed: March 28, 2012
    Date of Patent: August 6, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Steven J. Coats, Dennis J. Hlasta, Mark J. Schulz
  • Patent number: 8097741
    Abstract: 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: Grant
    Filed: March 31, 2008
    Date of Patent: January 17, 2012
    Assignee: NDSU Research Foundation
    Inventors: Dean C. Webster, Dipak Chattopadhyay
  • Publication number: 20110130479
    Abstract: 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: Application
    Filed: July 17, 2009
    Publication date: June 2, 2011
    Applicant: SIKA TECHNOLOGY AG
    Inventors: Andreas Kramer, Jurgen Finter
  • Publication number: 20110118347
    Abstract: 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: Application
    Filed: May 29, 2009
    Publication date: May 19, 2011
    Applicant: Vernolix Limited
    Inventor: Michael William Fowler
  • Publication number: 20110046321
    Abstract: 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: Application
    Filed: May 18, 2009
    Publication date: February 24, 2011
    Inventors: Jim D. Earls, Robert E. Hefner, JR.
  • Publication number: 20100319580
    Abstract: 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: Application
    Filed: September 29, 2008
    Publication date: December 23, 2010
    Inventors: Dean C. Webster, Umesh Harkal, James Garrett
  • Publication number: 20100179302
    Abstract: 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: Application
    Filed: June 20, 2008
    Publication date: July 15, 2010
    Applicant: SOLVAY (SOCIETE ANONYME)
    Inventors: Philippe Krafft, Patrick Gilbeau
  • Publication number: 20100144917
    Abstract: 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: Application
    Filed: July 12, 2006
    Publication date: June 10, 2010
    Applicant: KONICA MINOLTA MEDICAL & GRAPHIC, INC.
    Inventor: Nobumasa Sasa
  • Patent number: 7612237
    Abstract: 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: Grant
    Filed: June 29, 2007
    Date of Patent: November 3, 2009
    Assignee: Degussa GmbH
    Inventor: Günter Knaup
  • Publication number: 20090247708
    Abstract: 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: Application
    Filed: August 16, 2006
    Publication date: October 1, 2009
    Applicant: SIKA Technology AG
    Inventors: Ulrich Gerber, Juergen Finter
  • Publication number: 20090105156
    Abstract: 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: Application
    Filed: October 3, 2008
    Publication date: April 23, 2009
    Applicant: Proteolix, Inc.
    Inventors: Pasit Phiasivongsa, Louis C. Sehl, William Dean Fuller, Guy J. Laidig
  • Publication number: 20080167332
    Abstract: 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: Application
    Filed: July 18, 2007
    Publication date: July 10, 2008
    Inventors: 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
  • Patent number: 7326799
    Abstract: 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, and
    Type: Grant
    Filed: December 30, 2002
    Date of Patent: February 5, 2008
    Assignee: Seikagaku Kogyo Kabushiki Kaisha
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
  • Patent number: 6841536
    Abstract: 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: Grant
    Filed: January 18, 2002
    Date of Patent: January 11, 2005
    Assignee: University of Utah Research Foundation
    Inventors: Jeannette C. Roberts, Britta H. Wilmore, Pamela B. Cassidy, Pamela K. Dominick, Megan D. Short
  • Patent number: 6812229
    Abstract: 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: Grant
    Filed: February 5, 2002
    Date of Patent: November 2, 2004
    Assignees: 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
  • Patent number: 6743929
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: June 1, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Publication number: 20030153788
    Abstract: 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: 1
    Type: Application
    Filed: December 30, 2002
    Publication date: August 14, 2003
    Applicant: Seikagaku Corporation
    Inventors: Nobuo Kobayashi, Tsuneo Koji, Takashi Fujita, Tomofumi Nishimura, Akihiko Hosoda
  • Publication number: 20030065219
    Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
    Type: Application
    Filed: October 16, 2002
    Publication date: April 3, 2003
    Applicant: Pharmacia & Upjohn Company
    Inventor: Bruce Allen Pearlman
  • Patent number: 6437134
    Abstract: A method for making phenylthiobutyl-isoquinoline compounds of formula and novel intermediates therefor.
    Type: Grant
    Filed: March 29, 2001
    Date of Patent: August 20, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 6376468
    Abstract: 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: Grant
    Filed: February 3, 2000
    Date of Patent: April 23, 2002
    Assignees: Nederlandse Organisatie Voor Toegepast-Natuurwetenschappelijk Onderzoek TNO, Rijksuniversiteit Leiden
    Inventors: 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
  • Patent number: 6369188
    Abstract: 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: Grant
    Filed: March 27, 1999
    Date of Patent: April 9, 2002
    Assignee: Polymeright, Inc.
    Inventors: Leonid Rappoport, Alex Vainer, Aleksandr Yam
  • Publication number: 20020032348
    Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA)
    Type: Application
    Filed: August 9, 2001
    Publication date: March 14, 2002
    Inventor: Bruce Allen Pearlman
  • Publication number: 20020019538
    Abstract: 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: Application
    Filed: August 10, 2001
    Publication date: February 14, 2002
    Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
  • Patent number: 6278002
    Abstract: 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: Grant
    Filed: September 1, 2000
    Date of Patent: August 21, 2001
    Assignee: Kaneka Corporation
    Inventors: Kazumi Okuro, Kenji Inoue
  • Patent number: 6268533
    Abstract: 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: Grant
    Filed: January 27, 2000
    Date of Patent: July 31, 2001
    Assignee: Sepracor Inc.
    Inventors: Yun Gao, Robert Hett, Kevin Q. Fang, Stephen A. Wald, Chris Hugh Senanayake
  • Patent number: 6239296
    Abstract: Intermediate compounds useful for making phenylthiobutyl-isoquinoline compounds of formula
    Type: Grant
    Filed: February 25, 2000
    Date of Patent: May 29, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 6225478
    Abstract: 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: Grant
    Filed: September 13, 1999
    Date of Patent: May 1, 2001
    Assignee: Tsumura & Co.
    Inventors: Hideaki Morishige, Yukiko Kurita, Yousuke Yamazaki, Chiaki Sakakibara, Masaharu Kigawa
  • Patent number: 6207704
    Abstract: 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: Grant
    Filed: June 8, 1998
    Date of Patent: March 27, 2001
    Assignee: Massachusetts Institute of Technology
    Inventors: Jun O. Liu, Eric C. Griffith, Zhuang Su
  • Patent number: 6147224
    Abstract: 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: Grant
    Filed: October 1, 1998
    Date of Patent: November 14, 2000
    Assignee: Allergan Sales, Inc.
    Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
  • Patent number: 6133457
    Abstract: 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: Grant
    Filed: July 2, 1999
    Date of Patent: October 17, 2000
    Assignees: Eli Lilly and Company, Wayne State University, University of Hawaii
    Inventor: Vinod F Patel
  • Patent number: 6127556
    Abstract: 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: Grant
    Filed: December 16, 1997
    Date of Patent: October 3, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Chin Liu, John S. Ng, James R. Behling, Arthur L. Campbell
  • Patent number: 6013836
    Abstract: 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: Grant
    Filed: May 22, 1995
    Date of Patent: January 11, 2000
    Assignee: Rohm and Haas Company
    Inventors: Adam Chi-Tung Hsu, Harold Ernest Aller, Dat Phat Le, Donald Wesley Hamp, Barry Weinstein, Raymond August Murphy
  • Patent number: 5994539
    Abstract: 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: Grant
    Filed: December 18, 1997
    Date of Patent: November 30, 1999
    Assignee: Zambon Group S.p.A.
    Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
  • Patent number: 5977388
    Abstract: 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: Grant
    Filed: July 9, 1998
    Date of Patent: November 2, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Patent number: 5977387
    Abstract: This invention provides processes for preparing cryptophycin compounds and novel intermediates which are useful in such processes.
    Type: Grant
    Filed: February 25, 1998
    Date of Patent: November 2, 1999
    Assignees: Eli Lilly and Company, Wayne State University, University of Hawaii
    Inventor: Vinod F Patel
  • Patent number: 5965609
    Abstract: 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: Grant
    Filed: March 13, 1998
    Date of Patent: October 12, 1999
    Assignee: Schering AG
    Inventors: Ulrich Klar, Hermann Graf, Gunter Neef, Siegfried Blechert
  • Patent number: 5883264
    Abstract: 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: Grant
    Filed: March 6, 1997
    Date of Patent: March 16, 1999
    Assignee: Tanabe Seiyaku Co., Ltd.
    Inventors: Hiroaki Matsumae, Akiko Idei, Takuo Nishida, Yasuhiko Ozaki, Takeji Shibatani
  • Patent number: 5883121
    Abstract: 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: Grant
    Filed: August 12, 1997
    Date of Patent: March 16, 1999
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Tomohiro Yamashita, Yoshimitsu Suda, Yukio Tada, Nobuhiko Katunuma, Tetsuji Asao
  • Patent number: 5792792
    Abstract: 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: Grant
    Filed: January 3, 1997
    Date of Patent: August 11, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Ulrich Klar, Hermann Graf, Gunter Neef, Siegfried Blechert
  • Patent number: 5744621
    Abstract: 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: Grant
    Filed: June 20, 1996
    Date of Patent: April 28, 1998
    Assignee: 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
  • Patent number: 5736620
    Abstract: Epoxy resins containing rodlike mesogenic moieties are prepared from phenolic hydroxyl containing compounds which contain such moieties.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: April 7, 1998
    Assignee: The Dow Chemical Company
    Inventors: Jimmy D. Earls, Robert E. Hefner, Jr., Paul M. Puckett
  • Patent number: 5693859
    Abstract: 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: Grant
    Filed: December 26, 1995
    Date of Patent: December 2, 1997
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Moriyasu Masui
  • Patent number: 5670675
    Abstract: 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: Grant
    Filed: March 23, 1995
    Date of Patent: September 23, 1997
    Assignee: Abbott Laboratories
    Inventors: Dale J. Kempf, Daniel W. Norbeck
  • Patent number: 5578608
    Abstract: 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: Grant
    Filed: January 17, 1995
    Date of Patent: November 26, 1996
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, John E. Munroe
  • Patent number: 5563168
    Abstract: 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: Grant
    Filed: June 16, 1995
    Date of Patent: October 8, 1996
    Assignee: BASF Aktiengesellschaft
    Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
  • Patent number: 5502252
    Abstract: 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: Grant
    Filed: November 10, 1994
    Date of Patent: March 26, 1996
    Assignee: Shionogi & Co., Ltd.
    Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Moriyasu Masui
  • Patent number: 5495029
    Abstract: 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: Grant
    Filed: August 4, 1994
    Date of Patent: February 27, 1996
    Assignee: Ciba-Geigy Corporation
    Inventors: Bettina Steinmann, Jean-Pierre Wolf, Adrian Schulthess, Max Hunziker
  • Patent number: 5481012
    Abstract: 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: Grant
    Filed: November 3, 1994
    Date of Patent: January 2, 1996
    Assignee: Atochem
    Inventors: Paul Caubere, Yves Fort, Agnes Ortar
  • Patent number: 5391735
    Abstract: 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: Grant
    Filed: April 12, 1994
    Date of Patent: February 21, 1995
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Piero Melloni, Arturo D. Torre, Ettore Lazzari, Giuseppe Mazzini