Carbazides Or Semicarbazides (i.e., N-n-c(=o)-n Containing) Patents (Class 514/590)
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Patent number: 6943179Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumorsType: GrantFiled: February 27, 2002Date of Patent: September 13, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Patent number: 6903237Abstract: Ectoparasitic insect pest controllers for animals, containing hydrazine derivatives of the general formula (I) as the active ingredient, and methods for application of the same: (I) [wherein A is (II), (III), (IV), (V) (wherein R4 and R5 are each H, C1-6 alkyl, or the like; and X is H, or one to five substituents selected from among halogeno and optionally halogenated C1-6 alkyl groups); R1 is H or C1-6 alkyl; R2 and R3 are each H, OH, C1-6 alkyl, phenylcarbonyl, or the like; Y is H, or one to five substituents selected from among halogeno, nitro, and cyano; Z is halogeno, cyano, C1-6 alkyl, or the like; and W is O or S]. The insect pest controllers exert remarkable controlling effects on parasitic insect pests harmful to domestic or pet animals, e.g. fleas, lice, ticks.Type: GrantFiled: October 16, 2001Date of Patent: June 7, 2005Assignee: Nihon Nohyaku Co., Ltd.Inventors: Rikio Yamaguchi, Tetsuyoshi Nishimatsu, Kazuhiro Takagi
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Patent number: 6897240Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.Type: GrantFiled: May 8, 2003Date of Patent: May 24, 2005Assignee: The Regents of the University of CaliforniaInventors: Fred E. Cohen, Xiaohui Du, Chun Guo, James H. McKerrow
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Patent number: 6849626Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.Type: GrantFiled: August 21, 2001Date of Patent: February 1, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
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Patent number: 6841701Abstract: The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.Type: GrantFiled: June 15, 2001Date of Patent: January 11, 2005Assignee: Curacyte AGInventors: Jörg Stürzebecher, Torsten Steinmetzer, Sebastian Künzel, Andrea Schweinitz
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Publication number: 20040254103Abstract: The present invention relates to compounds according to the structure (I): 1Type: ApplicationFiled: June 13, 2003Publication date: December 16, 2004Inventors: Xu Lin, Terrence W. Doyle, Ivan King
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Patent number: 6831061Abstract: A substituted apicidin derivative, a method of synthesis therefore, and an anti-tumor composition comprising the same are disclosed. The substituent of the derivative is preferably semicarbazone, thiosemicarbazone, hydrazone, tert-butylhydrazone, phenylhydrazone, 2,4-dinitrophenylhydrazone, 4-methoxyphenylhydrazone, 3-methoxyphenylhydrazone, 4-nitrophenylhydrazone, benzylhydrazone, methanesulfonylhydrazone, benzenesulfonylhydrazone, 4-methylbenzenesulfonylhydrazone, benzoylhydrazone, 4-nitrobenzoylhydrazone, carbohydrazone, benzyloxime or acetoxime. The compound has strong inhibition effect against histone deacetylase and detransforming activities and specifically inhibit growth of cancer cells. Therefore, it is useful in preparation of an anti-tumor composition.Type: GrantFiled: June 20, 2003Date of Patent: December 14, 2004Inventors: Hyang Woo Lee, Young Hoon Jung, Jeung Whan Han, Seok Yong Lee, Yin Won Lee, Hoi Young Lee
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Publication number: 20040116419Abstract: The present invention provides an effective method and composition for the prevention, amelioration or control of external parasites on a human or animal via the administration of a prophylactically, therapeutically or pharmaceutically effective amount of a neuronal sodium channel antagonist to a human or animal in need thereof.Type: ApplicationFiled: October 14, 2003Publication date: June 17, 2004Applicant: WyethInventors: Kathleen Heaney, Susan J. Dunney, Douglas Rugg
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Publication number: 20040110730Abstract: Reagents and methods are provided for crosslinking and immobilizing biomolecules, drugs and synthetic polymers. The reagents possess (i) a thiol or amino reactive group; and (ii) a hydrazino or oxyamino moiety. Conjugates and immobilized biomolecules are also provided.Type: ApplicationFiled: November 24, 2003Publication date: June 10, 2004Inventor: David A. Schwartz
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Publication number: 20040097550Abstract: Novel compounds of the formula I in which X, Y, Z, R, R1, R2 and R3 are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of tromboembolic diseases and for the treatment of tumours 1Type: ApplicationFiled: September 17, 2003Publication date: May 20, 2004Inventors: Werner Mederski, Bertram Cezanne, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
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Publication number: 20040058990Abstract: Invented are non-peptide TPO mimetics. also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected substituted thiosemicarbazone derivative.Type: ApplicationFiled: June 19, 2003Publication date: March 25, 2004Inventors: Kevin J. Duffy, Juan I Luengo, Stephen G. Miller, Julian Jenkins, Alan T. Price, Antony N. Shaw
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Publication number: 20040054005Abstract: Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.Type: ApplicationFiled: August 21, 2003Publication date: March 18, 2004Inventor: Nancy C. Lan
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Publication number: 20040048851Abstract: The compounds of the formula (formula 1) and pharmaceutically acceptable salts thereof and a process for preparing the same and pharmaceutical compositions containing the same are described wherein the substituents have the meaning as specified in the description. The compounds are used as thrombon inhibitors.Type: ApplicationFiled: June 3, 2003Publication date: March 11, 2004Inventors: Uros Urleb, Anamarija Zega, Mojca Stegnar, Bakija Alenka Trampus, Tomas Solmajer, Gregor Mlinsek
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Patent number: 6696442Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl-82-; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: June 25, 2002Date of Patent: February 24, 2004Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin
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Publication number: 20040014801Abstract: The present invention relates to thio semicarbazone and semicarbazone inhibitors of cysteine proteases and methods of using such compounds to prevent and treat protozoan infections such as trypanosomiasis, malaria and leishmaniasis. The compounds also find use in inhibiting cysteine proteases associated with carcinogenesis, including cathepsins B and L.Type: ApplicationFiled: May 8, 2003Publication date: January 22, 2004Applicant: The Regents of the University of CaliforniaInventors: Fred E. Cohen, Xiaohui Du, Chun Guo, James H. McKerrow
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Publication number: 20030211162Abstract: Nanometer particles of poorly water-soluble or substantially water-insoluble compound are produced by finely-spraying a non-aqueous solution of said compound into a heated and fluidized bed of carrier excipient. The resulting product consists of a free flowing mixture of relatively large particles of carrier excipient and nanometer sized particles (less than 3 &mgr;m)) of compound.Type: ApplicationFiled: October 18, 2002Publication date: November 13, 2003Inventor: Nicholas J. Kerkhof
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Patent number: 6638947Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: December 6, 2001Date of Patent: October 28, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, John F. W. Keana
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Publication number: 20030199579Abstract: 1Type: ApplicationFiled: May 21, 2003Publication date: October 23, 2003Inventors: Rikio Yamaguchi, Tetsuyoshi Nishimatsu, Kazuhiro Takagi
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Publication number: 20030166577Abstract: The invention relates to derivatives of amidino-benzylamine, especially derivatives of 4-amidino-benzylamine, with two bonded amino acids. These derivatives represent a novel group of highly active and very selective F Xa-inhibitors for treating cardiovascular diseases and thrombotic events.Type: ApplicationFiled: March 21, 2003Publication date: September 4, 2003Inventors: Jorg Sturzebecher, Torsten Steinmetzer, Sebastian Kunzel, Andreas Schweinitz
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Publication number: 20030166576Abstract: The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-benzylamine, with two bonded amino acids represent a new group of highly active and very selective uPA inhibitors. The urokinase inhibitors can be used in medical applications, e.g. in the treatment of malign tumors such as in cases of metastatic spread.Type: ApplicationFiled: December 9, 2002Publication date: September 4, 2003Inventors: Jorg Strzebecher, Torsten Steinmetzer, Andrea Schweinitz
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Patent number: 6613803Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: October 21, 1999Date of Patent: September 2, 2003Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin, Eckard Weber
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Patent number: 6610715Abstract: The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or —CH2CH2C(═O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, —C(═X)—R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, —NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.Type: GrantFiled: November 13, 2001Date of Patent: August 26, 2003Assignee: Cheil Jedang CorporationInventors: Yong Sik Youn, Myung Xik Xiang, Byoung Chol Suh, Jong Hoon Kim, Kwang Hyuk Lee, Eui Kyung Kim, Jae Kyu Shin, Chung Keun Rhee
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Patent number: 6593362Abstract: This invention relates to pharmaceutical compositions and methods of using non-peptidic cyclophilin-binding compounds in medical conditions involving breakdown of mitochondrial energy metabolism induced by calcium overload, in treating alopecia and promoting hair growth, in treating infections with filarial and helmintic parasites, and in treating and preventing infections with the human immunodeficiency virus.Type: GrantFiled: May 21, 2001Date of Patent: July 15, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Joseph P. Steiner, Gregory S. Hamilton
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Patent number: 6566304Abstract: The invention relates to use of (a) compounds of phosphorus containing at least partly lipophilic organic radicals together with (b) urea and/or urea derivatives in selected quantity ratios of (a) to (b) as a soil additive for biologically controlling plant-parasitic soil nematodes by strengthening the correspondingly antagonistic soil potential, more particularly by strengthening the growth of antagonistic and/or nematicidal rhizosphere bacteria and/or corresponding mycorrhiza strains—and at the same time strengthening the growth of cultivated plants in soil. The multicomponent mixtures which strengthen bacterial growth are preferably introduced into the region of the plant roots in the form of an aqueous preparation using plant-compatible emulsifiers before and/or during plant growth. Components (a) and (b) are used in such quantity ratios that the ratio by weight of C to N is no higher than 6:1 and preferably no higher than 5:1.Type: GrantFiled: February 6, 2001Date of Patent: May 20, 2003Assignee: Cognis Deutschland GmbHInventors: Doris Bell, Bettina Kopp-Holtwiesche, Stephan Von Tapavicza
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Publication number: 20030045581Abstract: The present invention is directed to optionally substituted 4-substituted-1-(arylmethylidene)thiosemicarbazide, 4-substituted-1-(arylcarbonyl)thiosemicarbazide and analogs thereof, represented by the Formulae I and II: 1Type: ApplicationFiled: June 3, 2002Publication date: March 6, 2003Inventors: Sui Xiong Cai, Bao Ngoc Nguyen, John Drewe, P. Sanjeeva Reddy, Shailaja Kasibhatla, Azra Pervin
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Publication number: 20020183321Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: 1Type: ApplicationFiled: June 25, 2002Publication date: December 5, 2002Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F.W. Keana, Victor I. Ilyin
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Publication number: 20020177597Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands.Type: ApplicationFiled: May 16, 2002Publication date: November 28, 2002Inventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Publication number: 20020173548Abstract: Halogenated derivatives of two synthetic anti-tuberculosis agents, thioacetazone and p-aminosalicylic acid, have been synthesized.Type: ApplicationFiled: March 9, 2001Publication date: November 21, 2002Inventors: Farzad Kobarfard, Joel M. Kauffman
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Patent number: 6479543Abstract: The present invention provides a synergistic insecticidal composition comprising as essential active ingredients a neuronal sodium channel antagonist in combination with one or more compounds selected from the group consisting of pyrethroids, pyrethroid-type compounds, recombinant nucleopolyhedroviruses capable of expressing an insect toxin, organophosphates, carbamates, formamidines, macrocyclic lactones, amidinohydrazones, GABA antagonists and acetylcholine receptor ligands. Also provided are methods for synergistic insect control and crop protection.Type: GrantFiled: March 9, 2000Date of Patent: November 12, 2002Assignee: BASF AktiengesellschaftInventors: Michael Frank Treacy, Raymond Frank Borysewicz, Kurt Allen Schwinghammer, Paul E. Rensner, Hassan Oloumi-Sadeghi
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Patent number: 6458843Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Y is oxygen or sulfur; R1, R21, R22 and R23 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; or R22 and R23, together with the N, form a heterocycle; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one or O, S, NR24, CR25R26, C(O), NR24C(O), C(O)NR24, SO, SO2 or a covalent bond; where R24, R25 and R26 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl.Type: GrantFiled: October 21, 1999Date of Patent: October 1, 2002Assignee: Euro-Celtique S.A.Inventors: Yan Wang, Sui Xiong Cai, Nancy C. Lan, John F. W. Keana, Victor I. Ilyin, Eckard Weber
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Publication number: 20020115617Abstract: The present invention relates to the use of beta-naphthoquinone derivatives, and salts thereof, for the prevention and/or the treatment of glutamate cytotoxicity. It further relates to the use of beta-naphthoquinone derivatives, and salts thereof, for preventing and/or treating glutamate induced neurological disorders. Additionally, it concerns the use of beta-naphthoguinone derivatives, and salts thereof, for making drugs exerting an inhibitory effect on the release of glutamate.Type: ApplicationFiled: January 22, 2002Publication date: August 22, 2002Inventors: Maurice Israel, Jordi Molgo, Christian Bloy, Cesar Mattei
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Publication number: 20020061886Abstract: This invention is related to carbocyclic and heterocyclic substituted semicarbazones and thiosemicarbazones represented by Formula I: 1Type: ApplicationFiled: December 6, 2001Publication date: May 23, 2002Applicant: CoCensys, Inc.Inventors: Yan Wang, Sui Xiong Cai, John FW Keana
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Publication number: 20020016299Abstract: An apoptosis inducing agent or an anticancer agent which is characterized in containing glycerolipid and/or glyceroglycolipid as effective component(s).Type: ApplicationFiled: April 5, 1999Publication date: February 7, 2002Inventors: TAKESHI SAKAI, NOBUTO KOYAMA, YOKO TATSUMI, HIROAKI SAGAWA, FU-GONG YU, KATSUSHIGE IKAI, IKUNOSHIN KATO
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Patent number: 6331542Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: April 19, 2000Date of Patent: December 18, 2001Assignee: SmithKline Beecham CorporationInventors: Thomas Joseph Carr, Renee Louise Desjarlais, Timothy Francis Gallagher, Stacie Marie Halbert, Hye-Ja Oh, Scott Kevin Thompson, Daniel Frank Veber, Dennis Shinji Yamashita, Jack Hwekwo Yen
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Patent number: 6291464Abstract: This invention relates to new aminopiperazine derivatives having the potentiation of the cholinergic activity, etc., and represented by general formula [I]. wherein R1 is lower alkyl, etc., R2 is aryl, etc., A is or —SO2—, Q is —N═CH—, etc., X is lower alkylene, etc., and R3 and R4 are taken together to form lower alkylene, etc., and pharmaceutically acceptable salts thereof, to processes for preparation thereof and a pharmaceutical composition comprising the same.Type: GrantFiled: August 17, 1999Date of Patent: September 18, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Ichiro Shima, Kazuhiko Ohne
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Patent number: 6284777Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, inducing osteoporosis; gingival disease including gingivitis and periodontists; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: April 19, 2000Date of Patent: September 4, 2001Assignee: SmithKline Beecham CorporationInventors: Stacie Marie Halbert, Scott Kevin Thompson
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Patent number: 6281211Abstract: This invention is related to substituted semicarbazides represented by Formula (I) or a pharmaceutically acceptable salt or prodrug thereof, wherein: R1 and R2 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; R3, R4, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl, or R3 and R4 is defined as above, and R5 and R6 together with the nitrogen atom to which they are attached form a heterocycle, including piperidine, piperazine, morpholine; A1 and A2 are independently aryl, heteroaryl, saturated or partially unsaturated carbocycle or saturated or partially unsaturated heterocycle, any of which is optionally substituted; X is one of O, S, NR7, CH2, C(O), NR7C(O), C(O)NR7, SO, SO2 or a covalent bond; where R7 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, haloalkyl, aryl, aminoalkyl, hydroxyalkyl, alkoxyalkyl or carboxyalkyl; n isType: GrantFiled: September 21, 2000Date of Patent: August 28, 2001Assignee: Euro-Celtique S.A.Inventors: Sui Xiong Cai, Nancy C. Lan, Soo Hong-Bae
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Publication number: 20010012854Abstract: The present invention relates to methods for the use of specified inhibitors of multicatalytic protease (MCP) for use as inducers of programmed cell death (i.e., apoptosis) in tumor cells, and more particularly as anti-tumor agents. The present invention provides methods for inducing apoptosis in transformed cells, inhibiting proliferation of transformed cells, and inhibiting the growth of tumors using the MCP inhibitors.Type: ApplicationFiled: December 15, 1998Publication date: August 9, 2001Inventors: ROBERT SIMAN, JITESH P. JANI, RONALD H. GOLDFARB, QING PING DOU
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Patent number: 6204384Abstract: The present invention provides peptide aldehydes having an 3-amino-2-hydro yenyl acetamide group as part of the peptide backbone d an arginine group or analog at P1. These compounds e potent and specific or inhibitors of thrombin. Ther pharmaceutically acceptable salts, pharmaceutic ly acceptable compositions thereof, and methods of using t as therapeutic agents for disease states in mammals charachterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having in history activity towards proteases of the trypsin/chymotrypsin class.Type: GrantFiled: November 26, 1997Date of Patent: March 20, 2001Assignee: Corvas International, Inc.Inventors: Joseph Edward Semple, Marguerita S. Lim-Wilby, Terence K. Brunck
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Patent number: 6077866Abstract: Novel benzophenonehydrazone derivatives represented by the formula (I): ##STR1## wherein, R.sup.1 is halogen; R.sup.2 is hydrogen or C.sub.1-4 alkyl; R.sup.3 is cyano, optically substituted C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-4 alkynyl, C.sub.1-4 alkyl-carbonyl or C.sub.1-4 alkoxy-thiocarbonyl; R.sup.4 is hydrogen, phenyl, optionally substituted C.sub.1-6 alkyl, optionally substituted C.sub.2-8 alkenyl, --CO--R.sup.8, --CO--O--R.sup.9 or ##STR2## R.sup.5 is hydrogen, formyl, phenyl, optionally substituted C.sub.1-8 alkyl, optionally substituted C.sub.2-8 alkenyl, optionally substituted C.sub.3-8 alkynyl, optionally substituted C.sub.1-8 alkyl-arbonyl, optionally substituted C.sub.1-6 alkyl-oxalyl, optionally substituted C.sub.1-8 alkoxy-carbonyl, optionally substituted C.sub.1-8 alkoxy-oxalyl, optionally substituted C.sub.3-8 cycloalkyl-carbonyl, optionally substituted C.sub.2-8 alkenyl-carbonyl or optionally substituted benzoyl; R.sup.6 is hydrogen or halogen; R.sup.7 is hydrogen, halogen or C.sub.Type: GrantFiled: May 10, 1996Date of Patent: June 20, 2000Assignee: Nihon Bayer Agrochem K.K.Inventors: Yoshinori Kitagawa, Katsuaki Wada, Yoshiko Kyo, Yuichi Otsu, Yumi Hattori, Toru Obinata, Takahisa Abe, Katsuhiko Shibuya, Wolfram Andersch
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Patent number: 6034137Abstract: This invention provides novel cationic lipids, particularly guanidino lipids, and methods for their preparation. Also provided are polyanionic-lipid complexes comprising the lipids of the invention, their preparation and use to deliver biologically active substances, particularly nucleic acids to cells.Type: GrantFiled: October 20, 1997Date of Patent: March 7, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: Paula N. Belloni, Donald R. Hirschfeld, John O. Link, John J. Nestor, Jr., Gary A. Peltz
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Patent number: 6011047Abstract: The present invention provides peptide aldehydes having a 3-amino-2-hydroxyphyenyl-acetamide group as part of the peptide backbone and an arginine mimic group such as an amidinopiperidine or amidinophenyl tail. These compounds are potent and specific inhibitors of thrombin. Their pharmaceutically salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis are also described. Also described are 3-amino-2-hydroxyphenyl-acetamide derivatives having inhibitory activity toward proteases of the trypsin/chymotrypsin class.Type: GrantFiled: November 26, 1997Date of Patent: January 4, 2000Assignee: Corvas International Inc.Inventors: Joseph Edward Semple, Marguerita S. Lim-Wilby, Terence K. Brunck
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Patent number: 5919816Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.Type: GrantFiled: October 17, 1997Date of Patent: July 6, 1999Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Thomas J. Dodd
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Patent number: 5811456Abstract: Novel monoamine oxidase B inhibitors of formula (I), wherein R.sub.1 .dbd.H, an optionally substituted benzyloxy or phenylethoxy group; p=0-3; R.sub.3 .dbd.H, a CN, OH, CCH group, a C.sub.1 -C.sub.3 alkoxy-carbonyl group, or a C.sub.1 -C.sub.3 alkylated cyanomethyl group; R.sub.2 .dbd.H or a C.sub.1 -C.sub.3 alkyl group; n=0 or 1; if n=0, R.sub.4 is a C.sub.1 -C.sub.3 alkyl group or a C.sub.1 -C.sub.3 alkoxy group, while if n=1, y=1 and R.sub.4 is a C.sub.1 -C.sub.3 alkyl group, a C.sub.1 -C.sub.3 alkoxy group or a phenyl group. The invention also concerns processes for the preparation of said novel inhibitors and the therapeutic use thereof.Type: GrantFiled: August 6, 1996Date of Patent: September 22, 1998Assignees: Laboratoires Mayoly Spindler, Michel SemanInventors: Michel Seman, Suzanne Bernard, Rene Milcent, Catherine Paillat
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Patent number: 5776925Abstract: Methods for cancer chemosensitization are provided. Texaphyrins are new chemosensitizers for enhancing the cytotoxicity of chemotherapeutic agents. The enhancement appears to be P-glycoprotein-independent since texaphyrins are effective in both a P-glycoprotein-expressing and a P-glycoprotein -nonexpressing cell line. Methods are provided for the treatment of cancers such as leukemia, lymphoma, carcinoma, and sarcoma using a texaphyrin as a chemosensitizer.Type: GrantFiled: January 25, 1996Date of Patent: July 7, 1998Assignee: Pharmacyclics, Inc.Inventors: Stuart W. Young, Richard A. Miller
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Patent number: 5741818Abstract: A compound of general formula I below useful as an anticonvulsant for disorders of the central nervous system: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen or halogen atom, or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl, cyano, C.sub.1-9 alkoxy or C.sub.6-10 aryloxy group; R.sup.5 represents a hydrogen atom or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl or C.sub.6-10 aryl group; and X is oxygen or sulfur; or a pharmaceutically-acceptable salt thereof. The compound may be adimistered orally for treating convulsions in humans or animals.Type: GrantFiled: June 7, 1995Date of Patent: April 21, 1998Assignee: University of SaskatchewanInventor: Jonathan Richard Dimmock
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Patent number: 5637619Abstract: The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhy drazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.Type: GrantFiled: July 5, 1995Date of Patent: June 10, 1997Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh
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Patent number: 5589510Abstract: A method for inhibiting retroviral infection in a subject comprising administering to said subject a therapeutically effective amount of a naphthalenesulfonic acid compound or a pharmaceutically acceptable salt thereof, as herein defined.Type: GrantFiled: May 15, 1995Date of Patent: December 31, 1996Assignee: Fuji Immunopharmaceuticals Corp.Inventors: Mitsunori Ono, Yumiko Wada, Yaming Wu, Hiroshi Kitaguchi, Yumiko Jimbo, Ryoichi Nemori, Stephen Gillies, Kin-Ming Lo
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Patent number: 5571843Abstract: Therapeutic compounds having the formula: ##STR1## in which R.sub.2 and R.sub.3 independently denote H, C.sub.1 -C.sub.4 alkoxy or OH and (A, B)=(oxygen, oxygen) in which case one out of R and R.sub.1 denotes OH, halogen, secondary amino or tertiary amine and the other denotes NHNHCONHR.sub.4 or R and R.sub.1 together denote .dbd.N--NH--CX--NHR.sub.5, .dbd.N--NH--CX--N(phenyl).sub.2, .dbd.N--NH--CX--NH--NH--R.sub.5, .dbd.N--NH--C(SCH.sub.3).dbd.N--R.sub.6 or .dbd.N--N.dbd.C(SCH.sub.3)--NH--R.sub.6 ; or (A, B)=(N--OH, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2 ; or (A, B)=(N--NH--CX--NHR.sub.5, oxygen) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 ; or (A, B)=(N--OH, N--OH) in which case R and R.sub.1 together form .dbd.N--NH--CX--NHR.sub.5 or .dbd.N--NH--CX--N(phenyl).sub.2.Type: GrantFiled: March 24, 1994Date of Patent: November 5, 1996Assignee: InnotheraInventors: Michel P. Cugnon de Sevricourt, Catherine G. Dacquet, Michel A. Finet, Florence J. Le Marquer, Max F. Robba, Norbert O. Tembo, Sylvie J. Yannic-Arnoult, Jean-Luc Torregrosa
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Patent number: 5543573Abstract: The present invention relates to a hydrazinecarboxamide derivative of the general formula (I) shown below: ##STR1## wherein the substituents are as defined in the specification, which has a wide insecticidal spectrum at a low dosage, a process for producing said derivative, and utilization of said derivative as an insecticide.Type: GrantFiled: April 14, 1994Date of Patent: August 6, 1996Assignee: Nihon Nohyaku Co., Ltd.Inventors: Kazuhiro Takagi, Takashi Ohtani, Tateki Nishida, Hiroshi Hamaguchi, Tetsuyoshi Nishimatsu, Atsushi Kanaoka