Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/494)
  • Patent number: 6605608
    Abstract: The present invention relates to the compounds of the formula (I) and salts thereof (all the symbols are the same meanings as described in the specification). The compounds of the formula (I) possess inhibitory activity of N-type calcium channel, so they are useful as drug for prevention and/or treatment of cerebral infarct, transient ischemic attack, encephalomyelopathy after cardiac operation, spinal angiopathy, hypertension with stress, neurosis, epilepsy, asthma and pollakiuria etc. or agent for the treatment of pain.
    Type: Grant
    Filed: December 22, 2000
    Date of Patent: August 12, 2003
    Assignee: Ono Pharmaceutical Co., Ltd
    Inventors: Takuya Seko, Masashi Kato
  • Patent number: 6593352
    Abstract: Substituted anthranilic acids of the formula I their use as a medicament or diagnostic, and medicament comprising them, and a pharmaceutical combination preparation containing a sodium/hydrogen exchange (NHE) blocker.
    Type: Grant
    Filed: December 6, 2001
    Date of Patent: July 15, 2003
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Andreas Weichert, Hans-Willi Jansen, Heinz-Werner Kleemann, Hans-Jochen Lang, Hartmut Rütten
  • Patent number: 6579987
    Abstract: Provided, among other things, is a compound of Formula I: wherein: Ar1 and Ar2 are independently selected aryl groups, optionally substituted with up to five substituents independently selected from the group consisting of alkyl, alkoxy, cycloalkyl, cycloalkyloxy, heterocycloalkyl, heterocycloalkyloxy, alkanoyl, thioalkyl, aralkyl, aralkyloxy, aryloxyalkyl, aryloxyalkoxy, cycloalkyl-substituted alkyl, cycloalkyloxy-substituted alkyl, cycloalkyl-substituted alkoxy, cycloalkyloxy-substituted alkoxy, heterocycloalkyl-substituted alkyl, heterocycloalkyloxy-substituted alkyl, heterocycloalkyl-substituted alkoxy, heterocycloalkyloxy-substituted alkoxy, thioaryl, aralkylthio, thioaryl-alkyl, aralkylthioalkyl, halo, NO2, CF3, CN, OH, alkylenedioxy, SO2NRR′, NRR′, CO2R (where R and R′ are independently selected from the group consisting of H and alkyl), and a second aryl group, which may be substituted as above; R1 is selected from the group consisting of H and alkyl; R2 is sele
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: June 17, 2003
    Assignee: NPS Allelix Corporation
    Inventors: Ian Egle, Jennifer Frey, Methvin Isaac
  • Publication number: 20030087945
    Abstract: Compounds of formula (I) 1
    Type: Application
    Filed: June 13, 2002
    Publication date: May 8, 2003
    Applicant: Aventis Pharma Deutschland GmbH
    Inventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
  • Patent number: 6548538
    Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.
    Type: Grant
    Filed: October 9, 2001
    Date of Patent: April 15, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Urbahns, Michael Woltering, Susanne Nikolic, Josef Pernerstorfer, Berthold Hinzen, Elke Dittrich-Wengenroth, Hilmar Bischoff, Claudia Hirth-Dietrich, Klemens Lustig
  • Publication number: 20030065185
    Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds aslo inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
    Type: Application
    Filed: April 8, 2002
    Publication date: April 3, 2003
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Louis John Lombardo, Francine S. Grant, Darren B. Dressen, Michael S. Dappen
  • Publication number: 20030045569
    Abstract: This invention relates to a series of difluoromethylene aromatic ethers of the formula 1
    Type: Application
    Filed: August 15, 2002
    Publication date: March 6, 2003
    Applicant: Pfizer Inc.
    Inventor: John Adams Lowe
  • Publication number: 20030045568
    Abstract: Thiosemicarbazone compounds of formula: 1
    Type: Application
    Filed: April 19, 2002
    Publication date: March 6, 2003
    Inventors: Sergio Altamura, Uwe Koch
  • Publication number: 20020177723
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.
    Type: Application
    Filed: April 11, 2000
    Publication date: November 28, 2002
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T.Y. Shen
  • Patent number: 6444840
    Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: September 3, 2002
    Assignee: The Procter & Gamble Co.
    Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
  • Publication number: 20020115018
    Abstract: Amine compounds having a cyano group are useful in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.
    Type: Application
    Filed: December 6, 2001
    Publication date: August 22, 2002
    Applicant: Shin-Etsu Chemical Co., Ltd.
    Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe
  • Patent number: 6410780
    Abstract: The invention provides novel prostaglandin analogs. In particular, the present invention relates to compounds having a structure according to formula (I) wherein R1, R2, R3, R4, R5, R6, W, X, Z, a, b, p and q are defined below. This invention also includes optical isomers, diastereomers and enantiomers of formula (I), and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.
    Type: Grant
    Filed: September 28, 2000
    Date of Patent: June 25, 2002
    Assignee: The Procter & Gamble Co.
    Inventors: Mitchell Anthony deLong, Jack Snyder Amburgey, Jr., John August Wos, Biswanath De, David Lindsey Soper
  • Patent number: 6391918
    Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-p
    Type: Grant
    Filed: August 25, 2000
    Date of Patent: May 21, 2002
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: André Jeanguenat, Martin Zeller
  • Publication number: 20020049332
    Abstract: The invention includes selected novel optically active &agr;-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.
    Type: Application
    Filed: October 11, 2001
    Publication date: April 25, 2002
    Inventor: John J. Talley
  • Patent number: 6316630
    Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: November 13, 2001
    Assignee: Sloan Kettering Institute for Cancer Research
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin
  • Publication number: 20010029300
    Abstract: A process for the synthesis of a compound of the formula 1
    Type: Application
    Filed: May 15, 2001
    Publication date: October 11, 2001
    Inventors: Ahmed F. Abdel-Magid, Judith H. Cohen, Cynthia A. Maryanoff, Frank John Villani, Hua M. Zhong
  • Patent number: 6204388
    Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.
    Type: Grant
    Filed: February 24, 1999
    Date of Patent: March 20, 2001
    Assignee: Sloan-Kettering Institute For Cancer Research
    Inventors: Samuel J. Danishefsky, Peter Bertinato, Dai-Shi Su, DongFang Meng, Ting-Chao Chou, Ted Kamenecka, Erik J Sorensen, Aaron Balog, Kenneth A. Savin, Scott Kuduk, Christina Harris, Xiu-Guo Zhang, Joseph R. Bertino
  • Patent number: 6174915
    Abstract: The present invention is directed to compound of the formula I: wherein R1, R2, R3, R4, R5, X, Y, and  are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
    Type: Grant
    Filed: May 11, 1999
    Date of Patent: January 16, 2001
    Assignees: Agouron Pharmaceuticals, Inc., Syntex (U.S.A.) Inc.
    Inventors: Steven L. Bender, Arlindo L. Castelhano, Wesley K. M. Chong, Melwyn A. Abreo, Roland J. Billedeau, Jian Jeffrey Chen, Judith G. Deal
  • Patent number: 6153591
    Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.
    Type: Grant
    Filed: March 16, 1999
    Date of Patent: November 28, 2000
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John Drewe, Yan Wang, Eckard Weber
  • Patent number: 6037498
    Abstract: This invention relates to novel compounds of general formula (I) ##STR1## wherein R.sup.1 represents an organic group, R.sup.2 represents a hydrogen atom or an organic group, and the asterisk denotes that the group R.sup.1 is predominantly in the R- or S-configuration such that the compound is in substantially enantiomerically pure form. The compounds are a useful source of chiral nucleophiles, e.g. undergoing stereoselective Michael addition to .alpha.,.beta.-unsaturated carboxylic acid derivatives.
    Type: Grant
    Filed: August 12, 1996
    Date of Patent: March 14, 2000
    Assignee: Oxford Asymmetry International PLC
    Inventors: Stephen Graham Davies, Mario Eugenio Cosamino Polywka, David Roy Fenwick, Frank Reed
  • Patent number: 6017918
    Abstract: The present invention provides compounds having the Formula I ##STR1## The present invention also provides methods of treating atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
    Type: Grant
    Filed: July 26, 1999
    Date of Patent: January 25, 2000
    Assignee: Warner-Lambert Company
    Inventors: Helen Tsenwhei Lee, Mark Alan Massa, William Chester Patt, Bruce David Roth
  • Patent number: 5856323
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i. e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 5, 1999
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5840961
    Abstract: The invention herein is directed to a process for the preparation of ethyl 3S-amino-4-pentynoate which involves treating 3-(trimethylsilyl)-2-propynal with L-phenylglycinol in toluene to produce .alpha.S-??3-(trimethylsilyl)-2-propynylidene amino!benzenethanol; reacting .alpha.S-??3-(trimethylsilyl)-2-propynylidene!amino!benzenethanol with BrZnCH.sub.2 CO.sub.2 t-Bu in THF/NMP to produce 1,1-dimethylethyl 3S-?(2-hydroxy-1S-phenylethyl)amino!-5-(trimethylsilyl)-4-pentynoate; reacting the 1,1-dimethylethyl 3S-?(2-hydroxy-1S-phenylethyl)amino!-5-(trimethylsilyl)-4-pentynoate with sodium periodate to form 1,1-dimethylethyl 3S-?(phenylmethylene)amino!-5-(trimethylsilyl)-4-pentynoate; hydrolyzing 1,1-dimethylethyl 3S-?(phenylmethylene)amino!-5-(trimethylsilyl)-4-pentynoate to produce 1,1-dimethylethyl 3S-amino-5-(trimethylsilyl)-4-pentynoate; transesterifying 1,1-dimethyl 3S-amino-5-(trimethylsilyl)-4-pentynoate and desilylating to produce ethyl 3S-amino-4-pentynoate.
    Type: Grant
    Filed: July 10, 1997
    Date of Patent: November 24, 1998
    Assignee: G. D. Searle & Co.
    Inventors: James Richard Behling, Mark Laurence Boys, Kimberly Jo Cain-Janicki, Pierre-Jean Colson, Wendel William Doubleday, Joseph Edward Duran, Payman N. Farid, Carl Matthew Knable, Frank Walter Muellner, Sean Thomas Nugent, Ravindra S. Topgi
  • Patent number: 5739361
    Abstract: A new process for the preparation of furosemide ?4-chloro-N-(2-furylmethyl)-5-sulfamoyl-anthranilic acid!comprising the photochlorination of 4-chloro-2-fluoro-toluene to give 4-chloro-2-fluoro-benzotrichloride, the aminosulfonylation of the same and the subsequent condensation with furfurylamine.
    Type: Grant
    Filed: April 23, 1997
    Date of Patent: April 14, 1998
    Assignee: Proteos S.r.L.
    Inventors: Angelo Signor, Alfredo Guerrato, Giovanni Signor
  • Patent number: 5648486
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: May 12, 1993
    Date of Patent: July 15, 1997
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5604256
    Abstract: Compounds of formula (I): ##STR1## (in which: R is hydrogen, methyl or hydroxy; X is alkyl, alkenyl, cycloalkyl, aryl, aralkyl, or a heterocyclic group; A is a single bond, or an alkylene, alkenylene, alkynylene or alkadienylene group; Y is hydrogen, aryl, cycloalkyl or a heterocyclic group) have the ability to inhibit the biosynthesis of cholesterol, and can thus be used for the treatment and prophylaxis of diseases relating to high blood cholesterol levels.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: February 18, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroshi Kogen, Masaaki Kurabayashi, Teiichiro Koga, Toru Komai, Haruo Iwabuchi
  • Patent number: 5597839
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## X represents a divalent radical, Z represents O, S or a divalent radical,and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: January 28, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William R. Pilgrim
  • Patent number: 5532267
    Abstract: Amidinonaphthyl furancarboxylate derivatives of the formula I ##STR1## wherein A is a single bond or A denotes (a) a phenyl group, cyclopentyl group, or cyclohexyl group,(b) an alkenylphenyl group, alkylphenyl group, phenylalkenyl group, or phenylalkyl group wherein alkyl is C.sub.1 to C.sub.7 alkyl and alkenyl is C.sub.2 to C.sub.7 alkenyl,(c) a C.sub.1 to C.sub.18 alkyl or C.sub.2 to C.sub.7 alkenyl group which may be substituted by one or two substituents selected from C.sub.1 to C.sub.5 alkyl groups and quanidino groups, wherein an alkyl substituent together with the carbon atom to which it is attached may form a cycloalkyl ring having from 3 to 6 carbon atoms, or said C.sub.1 to C.sub.5 alkyl may itself be substituted by a C.sub.3 to C.sub.6 cycloalkyl ring, or(d) --(CH.sub.2).sub.n --NH--CO--(CH.sub.2).sub.n' wherein n and n' may be the same or different and represent an integer from 1 to 4; andwherein R denotes(e) a hydroxyl group,(f) a C.sub.1 to C.sub.
    Type: Grant
    Filed: March 22, 1994
    Date of Patent: July 2, 1996
    Assignee: Torii & Co., Ltd.
    Inventors: Toyoo Nakayama, Seizo Taira, Hiroyuki Kawamura, Masaoki Shibuya, Masahiro Iwaki
  • Patent number: 5436244
    Abstract: Novel indanes in all possible stereoisomer forms of the formula ##STR1## wherein the substituents are as defined in the specification and their non-toxic, pharmaceutically acceptable acid addition salts and their hydrates having central analgesic properties as well as antiarrhythmic and diuretic activities.
    Type: Grant
    Filed: July 22, 1993
    Date of Patent: July 25, 1995
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Michel Fortin, Gilles Hamon, Odile Le Martret, Anne M. Moura
  • Patent number: 5434151
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: August 24, 1992
    Date of Patent: July 18, 1995
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Sajjat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5434181
    Abstract: The present invention relates to novel (tetrahydro-3-furanyl)methylamino derivatives of the following formula (1): ##STR1## wherein the variables are defined in the specification, which are useful as insecticides.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: July 18, 1995
    Assignee: Mitsui Toatsu Chemicals, Inc.
    Inventors: Kenji Kodaka, Katsutoshi Kinoshita, Takeo Wakita, Shirou Shiraishi, Kazutomi Ohnuma, Eiichi Yamada, Naoko Yasui, Michihiko Nakaya, Hirozumi Matsuno, Nobuyuki Kawahara, Koichi Ebihara
  • Patent number: 5399690
    Abstract: Solid particle dispersions of dyes according to the formula: ##STR1## wherein D is selected from the group consisting of ##STR2## and ketomethylene nuclei are disclosed as filter dyes for photographic elements.In this formula, E.sup.1 and E.sup.2 are each independently electron withdrawing groups. R.sup.1 and R.sup.6 are each independently R or NHR, where R is aryl. R.sup.2 and R.sup.3 are each independently alkyl or aryl, or represent the carbon atoms necessary to form a fused ring with the phenyl ring to which the N atom is attached. R.sup.4 and R.sup.7 are each independently hydrogen, alkyl or aryl. R.sup.5 is alkyl. Z represents the atoms necessary to complete a 5 or 6 memebered heterocyclic nucleus. M.sup.+ is a cation. L.sup.1 through L.sup.7 are each independently methine groups. m is 0, 1, 2, or 3. n is 0 or 1. p is 0, 1, 2, 3, or 4. q is 0, 1, 2, or 3. At least one of R.sup.1 or D includes an aryl ring substituted with a carboxy or sulfonamido substituent.
    Type: Grant
    Filed: February 10, 1993
    Date of Patent: March 21, 1995
    Assignee: Eastman Kodak Company
    Inventors: Donald R. Diehl, Glenn M. Brown, Margaret J. Helber
  • Patent number: 5358938
    Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl terahydrothiophenes, 2,4-diaryl tetrahydrofurans, 2,4-diaryl tetrahydrothiphenes, 1,3-diaryl cyclopentanes, 2,4-diaryl pyrrolidines, and 2,5-diaryl pyrrolidines are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i.e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase.A method to treat disorders mediated by PAF or leukotrienes is also disclosed, that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: July 13, 1992
    Date of Patent: October 25, 1994
    Assignee: CytoMed, Inc.
    Inventors: Xiong Cai, Saijat Hussoin, San-Bao Hwang, David Killian, T. Y. Shen
  • Patent number: 5330965
    Abstract: Cyclohexenone oxime ethers of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; A=substituted or unsubstituted alkylene or alkenylene;Z=a 5-membered or 6-membered heteroaromatic structure;X=substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and phenyl;n=0 to 3, or 1 to 4 where Z is halogen-substituted pyridyl; andR.sup.
    Type: Grant
    Filed: January 15, 1993
    Date of Patent: July 19, 1994
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Norbert Goetz, Albrecht Harreus, Thomas Kuekenhoehner, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
  • Patent number: 5290756
    Abstract: Compounds of the formula: ##STR1## wherein X is hydrogen, halo, trihalomethyl, alkyl, nitroor cyano; X.sup.1 is hydrogen, halo, or trihalomethyl; R.sup.1 and R.sup.2 are hydrogen, alkyl phenyl or benzyl; n is 1 to 5, and Z is halo, cyano, nitro, trihalomethyl, methylthio, methylsulfinyl, methylsulfonyl, acetyl, phenyl, or heterocycle, and compositions containing these compounds exhibit herbicidal activity.
    Type: Grant
    Filed: June 8, 1982
    Date of Patent: March 1, 1994
    Assignee: Rohm and Haas Company
    Inventors: Colin Swithenbank, Ted Fujimoto
  • Patent number: 5254573
    Abstract: Novel substituted heterocyclic derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
    Type: Grant
    Filed: October 6, 1992
    Date of Patent: October 19, 1993
    Assignees: Monsanto Company, G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5234946
    Abstract: The substituted alkylamine derivatives represented by formula (I) ##STR1## wherein R.sup.1 represents (a) substituted or unsubstituted C.sub.2-6 alkenyl group, (b) substituted or unsubstituted C.sub.3-6 cycloalkenyl group, (c) substituted or unsubstituted C.sub.2-6 alkynyl group, (d) substituted or unsubstituted aryl group, (e) substituted or unsubstituted heterocyclic group, (f) fused heterocyclic group which may be substituted, or (g) group represented by the formula Ru.sup.11 -Ar wherein R.sup.11 is a heterocyclic group and Ar is a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and which may be substituted; ##STR2## represents a 5- or 6-membered aromatic ring which may contain a hetero N, O or S atom, and may be substituted by R.sup.7,X and Y are linking groups,R.sup.2 is H or lower alkyl,R.sup.3 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower cycloalkyl,R.sup.4 and R.sup.5 are independently hydrogen or halogen atoms,R.sup.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: August 10, 1993
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Takezawa, Masahiro Hayashi, Yoshikazu Iwasawa, Masaaki Hosoi, Yoshiaki Iida, Yoshimi Tsuchiya, Masahiro Horie, Toshio Kamei
  • Patent number: 5182300
    Abstract: Compounds of the formula ##STR1## wherein AA is a basic amino acid in optically active or racemic form having better bio-availability and a method of treating asthma.
    Type: Grant
    Filed: October 23, 1990
    Date of Patent: January 26, 1993
    Assignee: Roussel Uclaf
    Inventor: Renato L. Pellegata
  • Patent number: 5162364
    Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.
    Type: Grant
    Filed: June 11, 1991
    Date of Patent: November 10, 1992
    Assignee: Adir et Compagnie
    Inventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
  • Patent number: 5134231
    Abstract: An amino acid compound of the formula: ##STR1## wherein R is a lower alkyl group, R.sub.1 is a hydrogen atom or a protecting group for carboxyl, R.sub.2 is a hydrogen atom, a protecting group for amino, an optionally substituted allyl group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each a hydrogen atom, a lower alkyl group or an aryl group), a beta-hydroxyethyl group in which the hydroxyl group is optionally protected, a formylmethyl group in which the formyl group is optionally protected, a carboxymethyl group in which the carboxyl group is protected or a 2-furylmethyl group and X is an optionally protected carboxyl group, a hydroxymethyl group in which the hydroxyl group is optionally protected or a substituted mercaptomethyl group of the formula:--CH.sub.2 SR.sub.5(wherein R.sub.5 is an aryl group or an ar(lower)alkyl group), which is a useful intermediate in the synthesis of 1-alkylcarbapenem compounds.
    Type: Grant
    Filed: January 17, 1991
    Date of Patent: July 28, 1992
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Makoto Sunagawa, Yoshihito Nozaki, Akira Sasaki, Haruki Matsumura
  • Patent number: 5120746
    Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.
    Type: Grant
    Filed: March 30, 1990
    Date of Patent: June 9, 1992
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanag, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
  • Patent number: 5117057
    Abstract: This invention relates to insecticidal compositions containing N'-substituted-N,N'-disubstitutedhydrazines, methods of using such compositions and N'-substituted-N, N'-disubstitutedhydrazines. Specifically, the invention relates to insect growth regulating compositions, and methods of using such compositions, which include compounds having a nucleus of the formula ##STR1## where A', B', D and J are independently any atom or group of atoms; where E is a tertiary carbon containing organic radical, a haloalkyl 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, and is attached to the nitrogen shown in the formula by a carbon-to-nitrogen single bond; where one G.sub.1 is C, N, O and S, and both G.sub.2 's and the other G.sub.1 are carbon; or one G.sub.2 is S or P, and both G.sub.1 's and the other G.sub.
    Type: Grant
    Filed: June 14, 1991
    Date of Patent: May 26, 1992
    Assignee: Rohm and Haas Company
    Inventors: Adam C. Hsu, Harold E. Aller, Raymond A. Murphy, Dat P. Le, Donald W. Hamp, Barry Weinstein
  • Patent number: 5112848
    Abstract: Substituted furan and pyrrole compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.
    Type: Grant
    Filed: April 19, 1990
    Date of Patent: May 12, 1992
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Bruce P. Gunn, James H. Holms, James B. Summers
  • Patent number: 5112977
    Abstract: Substituted naphthacenediones of the formula I ##STR1## in which R.sup.1 to R.sup.8 are H and at least one of R.sup.1 to R.sup.8, for example R.sup.2 and R.sup.3 or R.sup.2 and R.sup.6, are, for example, C.sub.1 -C.sub.20 alkoxy, C.sub.1 -C.sub.20 alkenoxy, C.sub.1 -C.sub.20 -alkylsulfinyl, --CN, --CF.sub.3, --NO.sub.2, --Si(CH.sub.3).sub.3 or --COO(C.sub.1 -C.sub.12 alkyl), are suitable, when incorporated into polymers having hydroxyalkyl groups, for currentless deposition of metals onto the polymer surface. They are in some cases suitable as photoinitiators.
    Type: Grant
    Filed: May 24, 1989
    Date of Patent: May 12, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Fischer, Marcus Baumann, Jurgen Finter, Vratislav Kvita, Carl W. Mayer, Wolfgang Wernet
  • Patent number: 5073641
    Abstract: Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R.sub.1 and R.sub.2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R.sub.1 and R.sub.2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution.
    Type: Grant
    Filed: April 26, 1988
    Date of Patent: December 17, 1991
    Inventors: Hans Bundgaard, Niels M. Nielsen
  • Patent number: 5053430
    Abstract: Novel compounds having the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein. These compounds are useful in the treatment of schizophrenia.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: October 1, 1991
    Assignee: Boehringer Ingelheim KG
    Inventors: Matthias Grauert, Herbert Merz, Joachim Mierau, Gunter Schingnitz, Claus Schneider
  • Patent number: 5030738
    Abstract: To synthesize molecules with antiulcer action, specifically ranitidine, niperotidine and cimetidine, having the formula: ##STR1## wherein R.sub.1 is hydrogen or together with R.sub.2 represents the rest of a cycloaliphatic or heterocyclic optionally substituted ring with 5 or 6 carbon atoms, R.sub.2 represents H, alkyl, alkyl substituted with a simple or substituted aromatic ring or with a single or substituted heterocyclic ring, Ar represents a simple or substituted phenyl group, a simple or substituted heterocyclic aromatic group, N=1, 2, 3, 4, 5 or 6 and X represents CH--NO.sub.2, S, N--C.tbd.N, the compound (II) is prepared through the following process sequence: ##STR2## wherein Z=H, NO.sub.2, halogen and R.sub.3 =--(CH.sub.2).sub.n Ar, --(CH.sub.2).sub.n --SH, --(CH.sub.2).sub.n --S--S--(CH.sub.2).sub.n, --(CH.sub.2).sub.n --S--CH.sub.2 Ar Y being halogen.
    Type: Grant
    Filed: May 22, 1990
    Date of Patent: July 9, 1991
    Assignee: Janus Farmaceutici S.r.l.
    Inventor: Alberto Reiner
  • Patent number: 5028256
    Abstract: A composition for protecting culture plants from the phytotoxic action of herbicidally active chloracetanilides contains as active ingredient an acylamine derivative of the formula I ##STR1## wherein X is oxygen, sulfur, --SO-- or --SO.sub.2 --,Q is an alkyl, alkenyl, alkinyl group, which may be interrupted by oxygen sulfur sulfonyl or sulfonyl, or a test 1,3-dioxolan-2-yl-alkyl, 1,3-dioxolan-4-alkyl, 2,2-dialkyl-1,3-dioxolan-4-ylalkyl, 1,3-dioxan-2-ylalkyl, 2-benzopyranylalkyl, alkoxycarbonyl alkenyloxycarbonyl or tetrahydrofurylalkyl, or the groupQ--X represents also a halogenoalkyl radical,n is 1, 2 or 3,Z is hydrogen, halogen, alkyl or dioxymethylene, alkoxy, alkenyloxy or alkinyloxy, A is a C.sub.1 -C.sub.8 -hydrocarbon radical which may be straight-chained, branched or cyclic and which is unsubstituted or substituted by alkoxy, alkylthio, cyano or halogen,R is halogenoalkyl or halogenoalkenyl,R.sub.1 is hydrogen, a C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.5 alkenyl or C.sub.3 -C.sub.
    Type: Grant
    Filed: December 22, 1988
    Date of Patent: July 2, 1991
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Martin
  • Patent number: 5008290
    Abstract: The invention relates to new sulphonamidoethyl compounds having valuable pharmacological properties, particularly anti-thrombotic properties, and which are also thromboxane antagonists.
    Type: Grant
    Filed: March 3, 1989
    Date of Patent: April 16, 1991
    Assignee: Dr. Karl Thomae GmbH
    Inventors: Armin Heckel, Josef Nickl, Erich Muller, Berthold Narr, Johannes Weisenberger, Wolfgang Eisert, Thomas Muller
  • Patent number: 4929751
    Abstract: A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.
    Type: Grant
    Filed: October 19, 1987
    Date of Patent: May 29, 1990
    Assignee: Yale University
    Inventors: Harry H. Wasserman, Natesan Murugesan, John H. Van Duzer