Nitrogen Attached Indirectly To The Thiocarbonyl By Nonionic Bonding Patents (Class 564/27)
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Patent number: 6350778Abstract: The present invention relates to cinnamoylaminoalkyl-substituted benzenesulfonamide derivatives of formula I in which A(1), A(2), A(3), R(1), R(2), R(3), R(4), X, Y, and Z have the meanings indicated in the claims. Compounds of formula I are valuable pharmaceutical active compounds which exhibit, for example, an inhibitory action on ATP-sensitive potassium channels in the cardiac muscle and/or in the cardiac nerve and are suitable, for example, for the treatment of disorders of the cardiovascular system such as coronary heart disease, arrhythmias, cardiac insufficiency or cardiomyopathies, or for the prevention of sudden cardiac death, or for improving decreased contractility of the heart. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, and pharmaceutical preparations comprising them.Type: GrantFiled: May 19, 2000Date of Patent: February 26, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert, Klaus Wirth, Heinz Gögelein
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Patent number: 6316616Abstract: The present invention provides methods and compositions, i.e. synthetic libraries of candidate compounds, useful in the discovery and optimization of compounds which catalyze at least one chemical transformation. In certain instances, the subject compounds catalyze a chemoselective, regioselective, stereoselective or enantioselective transformation.Type: GrantFiled: April 22, 1998Date of Patent: November 13, 2001Assignee: President and Fellows of Harvard CollegeInventors: Eric N. Jacobsen, Matthew S. Sigman
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Patent number: 6316478Abstract: This invention relates to novel spiro compound derivatives of benzoisothiazolyl-urea and -thiourea and compositions thereof. These compounds are useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: March 3, 2000Date of Patent: November 13, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine L. Widdowson, Hong Nie
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Publication number: 20010039348Abstract: Compounds having the formula: 1Type: ApplicationFiled: April 30, 2001Publication date: November 8, 2001Applicant: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6271261Abstract: Novel IL-8 receptor antagonists and methods of using them are provided.Type: GrantFiled: December 17, 1998Date of Patent: August 7, 2001Assignee: SmithKline Beecham CorporationInventor: Katherine L Widdowson
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Patent number: 6268387Abstract: The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).Type: GrantFiled: April 5, 2000Date of Patent: July 31, 2001Assignee: Warner-Lambert CompanyInventors: David Thomas Connor, William Howard Roark, Karen Elaine Sexton, Roderick Joseph Sorenson
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Patent number: 6265445Abstract: The present invention relates to novel, antiarrhythmically active phenoxyalkylamine derivatives possessing a double point of attack. More particularly, the present invention relates to new phenoxyalkylamine derivatives of the formula (1) wherein R1 and R2, independently from each other, mean hydrogen, halogen or C1-4 alkyl group; R3, R4 and R5, independently from each other, stand for hydrogen or C1-4 alkyl group; R6 represents hydrogen, C1-4 alkyl or benzyl group; R7 means nitro group or amino group optionally monosubstituted by C1-4 alkyl, benzoyl, C1-4 alkylcarbonyl, C1-4 alkylsulfonyl, C1-4 alkylcarbamoyl or C1-4 alkylthiocarbamoyl group; both n and m are 0 or 1, with the proviso that R2 is different from hydrogen, when R1 is hydrogen, as well as stereoisomers or mixtures of stereoisomers thereof, acid addition salts thereof and hydrates, prodrugs and metabolites of all these compounds.Type: GrantFiled: July 28, 2000Date of Patent: July 24, 2001Assignees: Gyogyszerkutato Intezet Kft, Szent-Gyorgyi Albert Orvostudomanyi EgyetemInventors: Gyula Papp, András Varró, Péter Mátyus, Ildikó Varga, Tivadar Rettegi, Alice Druga, Antal Simay, Imre Moravcsik, Pál Berzsenyi, Daniella Barlocco, Giorgio Cignarella, Márta Pátfalusi
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Patent number: 6262113Abstract: The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).Type: GrantFiled: August 14, 1998Date of Patent: July 17, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6255349Abstract: Compounds having the formula: wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 anType: GrantFiled: November 22, 1999Date of Patent: July 3, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6255351Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: September 30, 1999Date of Patent: July 3, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Patent number: 6232498Abstract: There are described processes for the preparation of a compound of formula I and novel intermediates in the preparative process.Type: GrantFiled: October 1, 1999Date of Patent: May 15, 2001Assignee: Astra Zeneca UK LimitedInventor: Christopher Goodwin
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Patent number: 6221913Abstract: Dialkyl urea compounds are described which act as calcitonin mimetics. These compounds are useful in the treatment of diseases which are associated with bone resorption. The calcitonin mimetics of the present invention are also useful in assays for the determination of calcitonin receptor activity.Type: GrantFiled: January 20, 1999Date of Patent: April 24, 2001Assignee: ZymoGenetics, Inc.Inventors: Charles R. Petrie, Patricia A. McKernan, Emma E. Moore, John M. Ostresh, Jean-Philippe Meyer, Richard A. Houghten, Clemencia Pinilla
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Patent number: 6211373Abstract: This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor.Type: GrantFiled: July 8, 1998Date of Patent: April 3, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6207715Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.Type: GrantFiled: November 22, 1999Date of Patent: March 27, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6114578Abstract: There are described processes for the preparation of a compound of formula I ##STR1## and novel intermediates in the preparative process.Type: GrantFiled: October 1, 1999Date of Patent: September 5, 2000Assignee: AstraZeneca UK LimitedInventor: Christopher Goodwin
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Patent number: 6083986Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: July 15, 1997Date of Patent: July 4, 2000Assignees: ICAgen, Inc., Eli Lilly & CompanyInventors: Neil Alexander Castle, Sean Patrick Hollinshead, Philip Floyd Hughes, Jose Serafin Mendoza, Joseph Wendell Wilson, George Salvatore Amato, Serge Beaudoin, Michael Gross, Grant McNaughton-Smith
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Patent number: 6028223Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is ##STR2## pharmaceutical compositions thereof and methods of using such compounds and compositions as .alpha..sub.v .beta..sub.3 antagonists.Type: GrantFiled: August 27, 1996Date of Patent: February 22, 2000Assignee: G. D. Searle & Co.Inventors: Peter Gerrard Ruminski, Michael Clare, Paul Waddell Collins, Bipinchandra Nanubhai Desai, Richard John Lindmark, Joseph Gerace Rico, Thomas Edward Rogers, Mark Andrew Russell
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Patent number: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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Patent number: 5849732Abstract: Disclosed are a phenol compound represented by the formula (1): ##STR1## wherein R.sup.0 represents H, alkyl or alkyloxy; R.sup.1 represents alkyl; R.sup.2 represents alkyl or alkyloxy; OR.sup.3 represents OH; R.sup.4 represents H, lower alkyl or acyl, each of the above substituents may be substituted; W represents O, S or NR.sup.7 ; where R.sup.7 represents H, alkyl, aryl, OH or alkyloxy, a group of the formula (2): ##STR2## represents an amino which may be mono- or di-substituted or heterocyclic group containing N atom,or a pharmaceutically acceptable salt thereof, and a process for preparing the same.Type: GrantFiled: February 14, 1997Date of Patent: December 15, 1998Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Toshikazu Suzuki, Hiroshi Ohmizu, Yoshimasa Hashimura, Hitoshi Kubota, Keiko Tanaka
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Patent number: 5723075Abstract: A near-infrared absorbent is obtained by heating a dimerized thiourea derivative of Formula ?1! or ?2! and a copper compound: ##STR1## The near-infrared absorbent is used to obtain a near-infrared absorbent resin material having a wide absorption in the near-infrared region, and the absorbent does not substantially decompose at a molding temperature of the resin. Typical examples of the dimerized thiourea derivative are 4,4'-di(benzylthiocarbamoyl)-aminodiphenylmethane, 4,4'-di(benzylthiocarbamoyl)-aminodiphenylhexafluoropropane, and 1,4'-di(dibenzoylthiocarbamoylamino)-2,5-dimethylbenzene, and typical examples of the copper compound are copper stearate and copper .beta.-acryloyloxypropylhydrogenphthalate.Type: GrantFiled: April 19, 1996Date of Patent: March 3, 1998Assignee: Nippon Paper Industries Co., Ltd.Inventors: Hideki Hayasaka, Toshiyuki Takano, Toshimi Satake
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Patent number: 5684156Abstract: A novel process for preparing clonidine derivatives has been discovered which is shorter, less expensive and safer than previously known methods. A new thiourea complex has also been discovered which can be directly cyclized to produce the corresponding heterocyclic product.Type: GrantFiled: August 31, 1995Date of Patent: November 4, 1997Inventors: David R. Pierce, William D. Dean, Michael E. Deason
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Patent number: 5624937Abstract: A compound of the formula I in which ##STR1## Z is O or S; R.sup.11 is a halogen atom;R.sup.12 is a halogen atom or a trifluoromethyl group; andX is S, SO, SO.sub.2, O or NH;R.sup.4 is naphthyl, quinolinyl, benzimidazolyl, pyridyl, pyradazinyl, benzoxazolyl or benzothiazolyl, unsubstituted or substituted by one or two substituents selected from a halogen atom, (1-4C)alkyl, (1-4C)alkoxy, nitro, (1-4C)alkoxycarbonyl, halo(1-4C)alkyl, and phenyl;or a pharmaceutically acceptable salt thereof.The compounds are useful as inhibitors of amyloid beta-protein production.Type: GrantFiled: March 2, 1995Date of Patent: April 29, 1997Assignee: Eli Lilly and CompanyInventors: Jon K. Reel, Richard L. Simon, Celia A. Whitesitt
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Patent number: 5620977Abstract: Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: June 7, 1995Date of Patent: April 15, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Daniel P. Getman, John N. Freskos, Ko-Chung Lin, Robert M. Heintz, Donald J. Rogier, Jr., Deborah E. Bertenshaw
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Patent number: 5614522Abstract: Urea-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: July 24, 1995Date of Patent: March 25, 1997Assignee: G.D. Searle & Co.Inventors: John J. Talley, Kathryn L. Reed
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Patent number: 5585373Abstract: A derivative of 3-(7'-oxo-1'-aza-4'-oxabicyclo[3.2.0 ]hept-3'-yl)propionic acid represented by the formula ##STR1## wherein R.sub.1 is a hydrogen atom, a lower alkyl group optionally having one or more cycloalkyl groups, a lower acyl group, a benzoyl group optionally having one or more substituents or a benzyl group optionally having one or more substituents, R.sub.2 is a hydrogen atom or a carboxyl-protecting group, R.sub.3 is a hydroxyl group, an azido group, a benzenesulfonyloxy group optionally having one or more substituents, a lower alkylsulfonyloxy group optionally having one or more substituents, a tri-substituted silyloxy group or an amino group optionally having one or more substituents, provided that when R.sub.1 and R.sub.2 are hydrogen atoms, R.sub.3 is not an amino group, and a salt thereof.Type: GrantFiled: November 18, 1994Date of Patent: December 17, 1996Assignee: Taiho Pharmaceutical Co., LtdInventors: Zhang Z. Ping, Zhen J. Sheng, Zhang Q. Rong, Zhang J. Liang, Singh Rajeshwar, Tomohiro Yamashita, Toshiyuki Toko, Hiroshi Matsumoto
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Patent number: 5574054Abstract: Novel quaternary ammonium salts having utility in the medical field for treating gastrointestinal disorders.Type: GrantFiled: January 12, 1995Date of Patent: November 12, 1996Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Osamu Kitagawa, Katsuyuki Ishii, Seiichi Niwa, Sigeru Ueki, Masao Seiki
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Patent number: 5567411Abstract: Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject.Type: GrantFiled: September 29, 1994Date of Patent: October 22, 1996Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of the University of OregonInventors: John F. W. Keana, Vladimir Martin, William H. Ralston
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Patent number: 5559153Abstract: Urea-substituted benzoylguanidines, process for their preparation, their use as pharmaceutical or diagnostic, and pharmaceutical containing themThere are described benzoylguanidines of the formula I ##STR1## where R(1), R(3) or R(4) is --NR(6) C.dbd.X NR(7)R(8); X is oxygen, sulfur, R(6), R(7) and R(8) are H, (perfluoro)alk(en)yl, where R(7) and R(8) can also together be 4 or 5 methylene groups,the substituents R(1) to R(5) remaining in each case are H, Hal, (fluoro) alk(en)yl, CN, NO.sub.2, NR(16)R(17).Type: GrantFiled: August 11, 1994Date of Patent: September 24, 1996Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Hans-Jochen Lang, Heinz-Werner Kleemann, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5449761Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R' and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer .gtoreq.2, provided that the groups R, R', R', L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer .gtoreq.Type: GrantFiled: September 28, 1993Date of Patent: September 12, 1995Assignee: Cytogen CorporationInventors: Benjamin A. Belinka, Jr., Daniel J. Coughlin, Vernon L. Alvarez, Richard Wood
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Patent number: 5430059Abstract: A butenoic acid compound of the following formula: ##STR1## in which Z is O, S, vinylene or azomethyne, A is an alkylene group and J is phenyl group, is a useful in treating heart disease.Type: GrantFiled: December 20, 1993Date of Patent: July 4, 1995Assignee: Eisai Co., Ltd.Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Toshiaki Ogawa, Hideyuki Adachi, Takanori Kawamura
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Patent number: 5403868Abstract: Novel capsaicin derivatives of general formula I ##STR1## wherein R, R.sub.1 to R.sub.7 and X may be a variety of substituents, processes for the production thereof, pharmaceutical compositions containing them and use thereof as pharmaceuticals.Type: GrantFiled: February 14, 1994Date of Patent: April 4, 1995Assignee: Sandoz Ltd.Inventors: Derek J. Reid, Christopher S. J. Walpole, Roger Wrigglesworth
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Patent number: 5389682Abstract: The invention concerns a series of novel bis-urea derivatives, nonpeptides, which show good binding affinity for the CCK-B receptor. The compounds, compositions containing them, methods of preparation, and utilities including anxiety, gastric acid secretion inhibition, and psychoses are included.Type: GrantFiled: September 13, 1993Date of Patent: February 14, 1995Assignee: Warner-Lambert CompanyInventors: Bradley D. Tait, Michael W. Wilson
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Patent number: 5384425Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## wherein, R.sup.1 and R.sup.2 are the same or different, and each represents C.sup.1 -10 alkyl group, a C.sup.3 -18 cycloalkyl group, or a lower alkyl group substituted by cycloalkyl radical(s);R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are the same or different, and each represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, hydrocarbyl aralkyl group, a pyridyl group, or an unsubstituted or substituted phenyl group, the substituents of the phenyl group being selected from a group consisting of lower alkyl radical, halogen atom-substituted lower alkyl radical, halogen atom, nitro radical, amino radical, mono- or di-lower alkylamino radical, lower acylamino radical, hydroxyl radical, lower alkoxy radical and lower acyloxy radical;X represents an oxygen atom or a sulfur atom, and n.sup.1 and n.sup.2 represent an integer of 1 to 6; and wherein at least one of R.sup.3 -R.sup.Type: GrantFiled: October 7, 1993Date of Patent: January 24, 1995Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5326856Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.Type: GrantFiled: April 9, 1992Date of Patent: July 5, 1994Assignee: Cytogen CorporationInventors: Daniel J. Coughlin, Benjamin A. Belinka, Jr.
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Patent number: 5264441Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.Type: GrantFiled: February 18, 1992Date of Patent: November 23, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
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Patent number: 5252317Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.Type: GrantFiled: May 22, 1992Date of Patent: October 12, 1993Assignee: The State of Oregon Acting by and through the State Board of Higher Education on Behalf of the University of OregonInventor: John F. W. Keana
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Patent number: 5250717Abstract: Isothiocyanates of the formula ##STR1## where R, R.sub.1, and R.sub.2 are the same or different and are hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl and thioureas of the formula ##STR2## where R, R.sub.1, and R.sub.2 are defined above, are disclosed. Processes for their preparation are also disclosed.Type: GrantFiled: June 1, 1992Date of Patent: October 5, 1993Assignee: Ethyl CorporationInventor: Gordon G. Knapp
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Patent number: 5231216Abstract: There are described novel trans-2-acylaminocyclohexyloxyacyldipeptides of formula I ##STR1## wherein R.sub.1 represents --CO--R.sub.6, --SO.sub.2 --R.sub.7 or ##STR2## R.sub.6 is C.sub.1 -C.sub.18 alkyl or C.sub.1 -C.sub.18 alkoxy, R.sub.7 is C.sub.1 -C.sub.18 alkyl or an optionally substituted phenyl group,Y is .dbd.O, .dbd.S or .dbd.NH;R.sub.2 =R.sub.3 and represent --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 represents --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, a straight or branched chain C.sub.1 -C.sub.18 alkyl group or benzyl group;R.sub.5 represents --OR.sub.9 or --NHR.sub.9,and novel (1R,2R)- and (1S,2S)-trans-2-acylaminocyclohexyloxyacetyldipeptides of the formulas Ia and Ib ##STR3## wherein R.sub.1 is --CO--R.sub.6, R.sub.6 is C.sub.1 -C.sub.18 alkyl,R.sub.2 is --H,R.sub.3 is --H or C.sub.1 -C.sub.12 alkyl,R.sub.4 is --OR.sub.8 or --NHR.sub.9,R.sub.8 is --H, C.sub.1 -C.sub.8 alkyl or benzyl,R.sub.9 is --H, C.sub.1 -C.sub.18 alkyl or benzyl,R.sub.5 is --OR.Type: GrantFiled: August 19, 1991Date of Patent: July 27, 1993Assignee: Univerza Edvarda Kardelja v LjubljanaInventors: Slavko Pecar, Danijel Kikelj, Uros Urleb, Marija Sollner, Gasper Marc, Ales Krbavcic, Vlado Kotnik, Branka Wraber-Herzog, Sasa Simcie, Alojz Than, Lidija Klamfer, Lucka Povsic, Zdravko Kopitar, Anton Stalc
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Patent number: 5227492Abstract: Diurea derivatives are provided which can be represented by the following general formula and salts thereof: ##STR1## Illustrative derivatives include 1,3-bis[[1-cycloheptyl-3-(3-pyridyl)ureido]-methyl]benzene, 1,3-bis[[1-cycloheptyl-3-(2-pyridyl)ureido]-methyl]benzene, and 1,3-bis[[1-cycloheptyl-3-(4-pyridyl)ureido]-methyl]benzene.The above compounds inhibit acyl-coenzyme A cholesterol acyltransferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: June 30, 1992Date of Patent: July 13, 1993Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5220022Abstract: Disclosed are novel compounds of the formula ##STR1## wherein: R is ##STR2## where Ph is phenyl, or ##STR3## X is --NR.sub.5 R.sub.6 or --OR.sub.7 ; R.sub.1 and R.sub.2 are independently hydrogen, methyl, ethyl, cyclohexyl, ##STR4## butyl, or heptyl; R.sub.4 is o-phenylene or p-phenylene and R.sub.4 can be alkyl- halo- or alkoxy- substituted;R.sub.3 is hydrogen;R.sub.5, R.sub.6, and R.sub.7 are independently hydrogen, methyl, ethyl, tert-butyl, isobutyl, butyl, alkoxy, acyl, acylamino, aryl, amino, cyclohexyl, aminoalkyl and substituted or unsubstituted phenylamino;Y is sulfur and oxygen atom; and n is zero or 1; provided n=1 when Y is sulfur.Type: GrantFiled: January 28, 1991Date of Patent: June 15, 1993Assignee: International Paper Co.Inventors: Bruce M. Resnick, Allan J. Wexler
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Patent number: 5190961Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.Type: GrantFiled: August 2, 1991Date of Patent: March 2, 1993Assignee: Terumo Kabushiki KaishaInventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
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Patent number: 5166429Abstract: Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.Type: GrantFiled: September 24, 1991Date of Patent: November 24, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5155127Abstract: Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.Type: GrantFiled: January 18, 1990Date of Patent: October 13, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5135737Abstract: Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines.Type: GrantFiled: September 5, 1989Date of Patent: August 4, 1992Assignee: The State of Oregon Acting by and through the State Board of Higher Education on behalf of the University of OregonInventor: John F. W. Keana
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Patent number: 5116848Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.Type: GrantFiled: March 30, 1988Date of Patent: May 26, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5114975Abstract: The invention relates to novel substituted aryloxyphenylthioureas, aryloxyphenylisothioureas and aryloxyphenylcarobodiimides of formula I ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.12 alkyl, unsubstituted or substituted by one or more halogen atoms and/or C.sub.1 -C.sub.6 alkoxy groups; C.sub.3 -C.sub.8 cycloalkyl, unsubstituted or substituted by one or more C.sub.1 -C.sub.3 alkyl groups; or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl,R.sub.2 and R.sub.3 are each C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl,R.sub.4 is hydrogen, methyl or --CHO,R.sub.5 is halogen; C.sub.1 -C.sub.4 alkyl, unsubstituted or substituted by one or more halogen atoms; C.sub.1 -C.sub.4 alkoxy, unsubstituted or substituted by one or more halogen atoms; or is a --CH.dbd.CH).sub.2, --CH.sub.2).sub.3 or --CH.sub.2).sub.4 bridge in 2,3- or 3,4-position,n is 0, 1, 2, 3 or 4,Z is --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N--; andR.sub.6 is C.sub.1 -C.sub.Type: GrantFiled: April 3, 1991Date of Patent: May 19, 1992Assignee: Ciba-Geigy CorporationInventors: Manfred Boger, Jozef Drabek, Josef Ehrenfreund
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Patent number: 5106873Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.Type: GrantFiled: June 26, 1990Date of Patent: April 21, 1992Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
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Patent number: 5107021Abstract: The invention relates to polyfluoroalkyl nitrogen compounds of general formula:R.sub.F --(CH.sub.2).sub.2 --Xin which X denotes an isothiocynate --N.dbd.C.dbd.S, carbodiimide --N.dbd.C.dbd.N(CH.sub.2).sub.2 --R'.sub.F or thiourea --NH--CS--A group, A denoting an optionally substituted amino group, and each of the symbols R.sub.F and R'.sub.F denotes a perfluoroalkyl radical.These compounds, prepared from the corresponding azides R.sub.F (CH.sub.2).sub.2 N.sub.3 or amines R.sub.F (CH.sub.2).sub.2 NH.sub.2, can be used as surface-active agents or precursors of such agents.Type: GrantFiled: April 12, 1991Date of Patent: April 21, 1992Assignee: Societe ATOCHEMInventors: Eric Bollens, Francois Szonyi, Aime Cambon
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Patent number: 5099030Abstract: The present invention relates to beta-aminoethyl-substituted phenyl compounds, especially beta-aminoethoxy-substituted phenyl compounds. The present invention also relates to pharmaceutical compositions comprising a safe and effective amount of a compound of the present invention and a pharmaceutically-acceptable carrier. The present invention further relates to methods for producing analgesia and reducing inflammation, in humans and lower animals, by administering the compounds or compositions of the present invention. In addition, the present invention relates to methods for making compounds of the present invention and intermediates useful in these synthesis methods.Type: GrantFiled: June 27, 1991Date of Patent: March 24, 1992Assignee: The Procter & Gamble CompanyInventors: Joseph H. Gardner, Gerald B. Kasting, Thomas L. Cupps, Richard S. Echler, Thomas W. Gibson, Joel I. Shulman
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Patent number: 5091419Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.Type: GrantFiled: October 2, 1990Date of Patent: February 25, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki