N-n Containing (e.g., Aminimine, Hydrazine, Etc.) Patents (Class 514/614)
-
Patent number: 6924312Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: GrantFiled: January 15, 2003Date of Patent: August 2, 2005Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
-
Patent number: 6893659Abstract: The pharmaceutical compositions for oral administration according to the invention contain 0.5% to 20% of N-piperidino-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide in microcrystalline form, and pharmaceutical excipients; they are formulated by wet granulation.Type: GrantFiled: May 1, 2002Date of Patent: May 17, 2005Assignee: Sanoti-SynthelaboInventors: Bernard Abramovici, Christian Condamine, Jean-Claude Gromenil
-
Patent number: 6887863Abstract: Compounds having the formula are methionine aminopeptidase type 2 (MetAP2) inhibitors and are useful for inhibiting angiogenesis. Also disclosed are MetAP2-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.Type: GrantFiled: February 19, 2004Date of Patent: May 3, 2005Assignee: Abbott LaboratoriesInventors: Richard A. Craig, Megumi Kawai, Linda M. Lynch, Jyoti R. Patel, George S. Sheppard, Jieyi Wang, Fan Yang, Nwe Ba-Maung, Xenia Beebe Searle
-
Patent number: 6831196Abstract: 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: GrantFiled: December 9, 2002Date of Patent: December 14, 2004Assignee: Curacyte AGInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz
-
Publication number: 20040242656Abstract: Compounds of formula (I) 1Type: ApplicationFiled: June 28, 2004Publication date: December 2, 2004Inventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
-
Publication number: 20040235911Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.Type: ApplicationFiled: June 25, 2004Publication date: November 25, 2004Applicant: Tularik Inc.Inventors: Leping Li, Xiaoqi Chen, Pingchen Fan, Jeffrey Thomas Mihalic, Serena Cutler
-
Patent number: 6800660Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and R8 are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and R8 is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ═O or ═S.Type: GrantFiled: July 10, 2002Date of Patent: October 5, 2004Assignee: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
-
Patent number: 6774116Abstract: A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site.Type: GrantFiled: January 31, 2002Date of Patent: August 10, 2004Assignee: Cryolife, Inc.Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
-
Publication number: 20040142851Abstract: Compounds of general formula (I), wherein: n represents an integer from 1 to 10; R1 and R6, independently of each other, represent a hydrogen atom, a group useful for protecting nitrogen atoms in peptide synthesis or a group of formula COR or —CH2COR, wherein R represents a hydrogen atom, an alkyl group of 1 to 10 carbon atoms, a —COORa group wherein Ra represents H or an alkyl group, a primary —NH2 amino group or a secondary or tertiary amine, an alkoxy group, a phenyl group or a pyridinium group; R2, R3, R4 and R5, independently of one another, represent a hydrogen atom, an alkyl group of 1 to 10 carbon atoms; Y represents CH2 and Z represents CO, or Y represents CO and Z represents CH2, for preparing a medicine for treating tumoral pathologies or neurodegenerative diseases such as Alzheimer's or Lehn's disease.Type: ApplicationFiled: April 7, 2004Publication date: July 22, 2004Inventors: Yannick Bonnemains, Karine Bouget, Michele Floc'h, Philippe Le Grel, Sandrine Aubin
-
Patent number: 6703426Abstract: Compounds of the class of 4-oxo-butenoic acid derivatives are disclosed along with the surprising use property of these compounds as a anti-tumor agents in humans against breast carcinoma, which include: 2-(N′-Fluoren-9-ylidene-hydrazino)5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester (OF-06), 1-(2,4-Dimethyl-phenyl)-2,4-dihydroxy-3-(4-methyl-benzoyl)-5-oxo-2,5-dihydro-1H-pyrrole-2-carboxylic acid methyl ester (1F-07), 4-(4-Methoxy-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid (3F-10), 4-(4-Chloro-phenyl)-2,4-dioxo-3-(phenyl-hydrazono)-butyric acid ethyl ester (3F-11), 2-Hydroxy-4-oxo-4-(2,3,5,6-tetrafluoro-4-methoxy-phenyl)-but-2-enoic acid (3F-15), and 4,4-Dihydroxy-5-(4-methyl-benzoyl)-2-phenyl-2,4-dihydro-pyrazol-3-one (3F-16) as well as some novel derivatives of these compounds claimed (see Table 2).Type: GrantFiled: December 4, 2002Date of Patent: March 9, 2004Assignee: University of Central FloridaInventors: D. Howard Miles, Solodnikov Sergey Yurjevich, Krasnykh Olga Petrovna, Pimenova Elena Valentinovna, Elena A. Goun
-
Patent number: 6703424Abstract: The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase inhibitor, a filler, a disintegrant, and a lubricant. The present invention also provides a method of preparing the pharmaceutical composition described herein.Type: GrantFiled: February 25, 2002Date of Patent: March 9, 2004Assignee: Teva Pharmaceutical Industries, Ltgd.Inventors: Galit Levin, Omer Tsipori
-
Publication number: 20040039025Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.Type: ApplicationFiled: August 28, 2003Publication date: February 26, 2004Inventors: Syed M. Ali, Kurt R. Brunden, Dario Doller, Brian Herbert, Jack B. Jiang, Amy Jordan
-
Patent number: 6673777Abstract: There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.Type: GrantFiled: November 2, 2000Date of Patent: January 6, 2004Assignee: Cytokine PharmaSciences, Inc.Inventors: Kevin J. Tracey, Pamela Cohen, Michael Bukrinsky, Helena Schmidtmayerova
-
Publication number: 20030229138Abstract: Disclosed are compounds of formula: 1Type: ApplicationFiled: May 22, 2002Publication date: December 11, 2003Inventors: Heinrich Schostarez, Robert Alan Chrusciel, Rebecca S. Centko
-
Publication number: 20030195258Abstract: Disclosed is a compound represented by the Structural Formula (I): 1Type: ApplicationFiled: January 15, 2003Publication date: October 16, 2003Applicant: Synta Pharmaceuticals Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
-
Publication number: 20030170316Abstract: Asthma is ameliorated, and mild or moderate asthma is prevented from progressing to more severe asthma by administering agents which prevent and/or accommodate for S-nitrosothiol breakdown. The method reduces requirements for systemic corticosteroids for the treatment of severe asthma.Type: ApplicationFiled: April 1, 2003Publication date: September 11, 2003Inventors: Benjamin Gaston, Jonathan S. Stamler, Owen W. Griffith
-
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
-
Publication number: 20030134904Abstract: The present invention features compounds useful for inhibiting RNase P activity. These compounds can be used as therapeutics for treating or preventing a variety of bacterial infections. The compounds belong to several classes including mono- and bis-guanylhydrazones, guanylhydrazone mimetics, and benzothiazolium compounds.Type: ApplicationFiled: September 23, 2002Publication date: July 17, 2003Inventors: Tony Giordano, Michael A. Sturgess, Samala J. Rao
-
Publication number: 20030125360Abstract: The present invention is directed to carbocyclic hydrazino compounds that function as inhibitors of copper-containg amine oxidases commonly known as semicarbazide-sensitive amine oxidases (SSAO), including the human SSAO known as Vascular Adhesion Protein-I (VAP-1). These SSAO inhibitors have therapeutic utility as drugs to treat conditions and diseases including, but not limited to, a number of inflammatory conditions and diseases (in particular chronic inflammatory conditions such as chronic arthritis, inflammatory bowel diseases, and chronic skin dermatoses), diseases related to carbohydrate metabolism and to aberrations in adipocyte differentiation or function and smooth muscle cell function, and vascular diseases.Type: ApplicationFiled: July 12, 2001Publication date: July 3, 2003Applicant: Biotie Therapies Corp.Inventors: David John Smith, Ferenc Fulop, Marjo Pihlavisto, Laszlo Lazar, Sakari Alaranta, Petri Vainio, Zsolt Szakonyi
-
Publication number: 20030119914Abstract: Disclosed is a compound represented by the Structural Formula (I): 1Type: ApplicationFiled: July 10, 2002Publication date: June 26, 2003Applicant: Shionogi BioResearch Corp.Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
-
Patent number: 6521663Abstract: Phenyl acetamide compounds are described, including compounds of Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein R3-R6, R11, B, Y and W are set forth in the specification. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as thrombin and factor Xa. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described. Other uses of compounds of the invention are as anticoagulants either embedded in or physically linked to materials used in the manufacture of devices used in blood collection, blood circulation, and blood storage, such as catheters, blood dialysis machines, blood collection syringes and tubes, blood lines and stents. Additionally, the compounds can be detectably labeled and employed for in vivo imaging of thrombi.Type: GrantFiled: October 5, 2001Date of Patent: February 18, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Wenxi Pan, Tianbao Lu, Thomas P. Markotan, Bruce E. Tomczuk
-
Patent number: 6518310Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.Type: GrantFiled: March 16, 2001Date of Patent: February 11, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L Fedde, Carl R Illig, Thomas P. Markotan, Thomas P Stagnaro
-
Publication number: 20020187972Abstract: In accordance with the present invention, there are provided various methods for modulating the expression of an exogenous gene in an isolated cell and in a mammalian subject employing modified ecdysone receptors. Also provided are modified ecdysone receptors, as well as homomeric and heterodimeric receptors containing same, nucleic acids encoding invention modified ecdysone receptors, modified hormone response elements, gene transfer vectors, recombinant cells, and transgenic animals containing nucleic acids encoding invention modified ecdysone receptor.Type: ApplicationFiled: September 7, 2001Publication date: December 12, 2002Applicant: The Salk Institute of Biological StudiesInventors: Ronald M. Evans, Enrique Saez
-
Publication number: 20020173469Abstract: 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: ApplicationFiled: May 30, 2002Publication date: November 21, 2002Applicant: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
-
Publication number: 20020151589Abstract: The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase inhibitor, a filler, a disintegrant, and a lubricant. The present invention also provides a method of preparing the pharmaceutical composition described herein.Type: ApplicationFiled: February 25, 2002Publication date: October 17, 2002Applicant: Teva Pharmaceutical Industries, Ltd.Inventors: Galit Levin, Omer Tsipori
-
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
-
Patent number: 6433017Abstract: In accordance with the present invention, there are provided amphiphilic polyamine compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: February 28, 2001Date of Patent: August 13, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
-
Patent number: 6410574Abstract: The present invention relates to a fungicidal composition obtained by mixing a 1,2,3-thiadiazole derivative of general formula (I) useful as a plant disease controller with at least one fungicide selected from the compounds having a fungicidal activity against plant diseases, and to a method for using the same: wherein R1 is hydrogen, alkyl or cycloalkyl and R2 is CO—Y—R3, wherein Y is O, S, NR4 or the like and R3 is hydrogen, alkyl, phenyl, 5- or 6-membered heterocycle or the like.Type: GrantFiled: July 28, 1999Date of Patent: June 25, 2002Assignee: Nihon Nohyaku Co., Ltd.Inventors: Tsutomu Nishiguchi, Tsuyoshi Takemoto, Sohkichi Tajima, Yoshinobu Yamamoto
-
Patent number: 6399659Abstract: The present invention relates to a hydrazine oxoacetamide derivative or its salt which exhibits an excellent insecticidal effect even at a low concentration. The hydrazine oxoacetamide derivative has the following Formula (I): wherein R1 represents a chlorine atom or a bromine atom, Y represents an oxygen atom or a methylene group, and when Y is an oxygen atom, p is 2 and when Y is a methylene group, p is 0, R2 represents a trifluoromethyl group, R3 represents a hydrogen atom or a methyl group, R4 represents a hydrogen atom or a methyl group, and R5 represents a methyl group, an ethyl group, an n-propyl group, a cyclopropyl group, an allyl group or a propargyl group.Type: GrantFiled: April 19, 2001Date of Patent: June 4, 2002Assignee: Agro-Kanesho Co., Ltd.Inventors: Syuichi Usui, Kiyoshi Takasuka, Yukinori Takekita, Junko Uchida, Norio Osaki
-
Patent number: 6376545Abstract: The present invention relates to a dispersible pharmaceutical composition comprising a therapeutically effective amount of L-DOPA ethyl ester, a therapeutically effective amount of a decarboxylase inhibitor, a filler, a disintegrant, and a lubricant. The present invention also provides a method of preparing the pharmaceutical composition described herein.Type: GrantFiled: November 10, 1999Date of Patent: April 23, 2002Assignee: Teva Pharmaceutical Industries, Ltd.Inventor: Galit Levin
-
Publication number: 20020045655Abstract: The invention relates to compounds having usefulness in the control of Take-AIl disease in plants, particularly cereals, a method for the control of Take-All disease, and fungicidal compositions for carrying out the method. Compounds of the invention are oximes or hydrazones of arylgloxamides or heteroarylglyoxamides or cycloalkenylglyoxamides.Type: ApplicationFiled: August 21, 2001Publication date: April 18, 2002Applicant: MONSANTO TECHNOLOGY LLC.Inventor: Dennis P. Phillion
-
Salicylic acid derivatives, processes for their preparation, compositions comprising them, their use
Publication number: 20020032178Abstract: Salicylic acid derivatives of the formula I, 1Type: ApplicationFiled: July 2, 2001Publication date: March 14, 2002Inventors: Andreas Gypser, Thomas Grote, Joachim Rheimheimer, Ingo Rose, Oliver Cullmann, Markus Gewehr, Wassilios Grammenos, Jordi Tormo i Blasco, Bernd Muller, Hubert Sauter, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl -
Patent number: 6348499Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.Type: GrantFiled: November 24, 1999Date of Patent: February 19, 2002Assignee: Gene Therapy Systems, Inc.Inventors: Philip L. Felgner, Xiang Gao, Jing Ling
-
Patent number: 6346547Abstract: Low-toxicity, highly-bioavailable, pharmaceutical antioxidant compositions for preferred oral administration to mammals are provided which have at least one amino acid-based compound of the general formula (I): A—N(Z)—CH(R1)C(O)—Q (I) wherein A is represented by the formula: XO—[C(R2)2]n— wherein n is an integer of from 1 to about 3, X is selected from the group consisting of a hydrogen atom, an acyl group and a halogenated acyl group and each R2 is independently selected from the group consisting of a hydrogen atom, an alkyl group having from 1 to about 3 carbon atoms, a hydroxyalkyl group having from 1 to about 3 carbon atoms, and CH2OX; Z is selected from the group consisting of a hydrogen atom, an alkyl group of from 1 to about 3 carbon atoms, and A; R1 is an amino acid side chain group or an amino acid side chain group which forms with R2 a single heterocyclic structure having a total of from 5 to 7 atoms in the ring; and wherein Q is a substituent sType: GrantFiled: February 8, 2000Date of Patent: February 12, 2002Assignee: Checkpoint, Genetics, Inc.Inventor: Nathan Tzodikov
-
Publication number: 20020010142Abstract: A parasiticidal formulation is provided. This formulation includes a pyrrolidone solvent, a bridging solvent, and an parasiticidal agent. One or more parasiticidal agents may be included in the formulation. Preferably, the formulation contains both closantel and ivermectin. Another aspect of the present invention is a method of making this parasiticidal formulation. This method includes mixing a pyrrolidone solvent and a bridging solvent to form a solvent solution and adding one or more parasiticidal agents to the solvent solution. A further aspect of the present invention is a method for administering the parasiticidal formulation of the present invention to an animal. This method of administration includes providing the parasiticidal formulation described above and applying this formulation to the skin of an animal, wherein the formulation is absorbed through the animal's skin.Type: ApplicationFiled: September 26, 2001Publication date: January 24, 2002Inventor: Richard Mihalik
-
Publication number: 20020002152Abstract: Compounds having the formula 1Type: ApplicationFiled: April 12, 2001Publication date: January 3, 2002Inventors: Richard A. Craig, Megumi Kawai, Linda M. Lynch, Jyoti R. Patel, George S. Sheppard, Jieyi Wang, Fan Yang, Nwe Ba-Maung
-
Publication number: 20010044464Abstract: The present invention relates to a hydrazine oxoacetamide derivative or its salt which exhibits an excellent insecticidal effect even at a low concentration.Type: ApplicationFiled: April 19, 2001Publication date: November 22, 2001Applicant: AGRO-KANESHO CO., LTD.Inventors: Syuichi Usui, Kiyoshi Takasuka, Yukinori Takekita, Junko Uchida, Norio Osaki
-
Patent number: 6300519Abstract: There are described compounds of formula I*, wherein R1 is lower alkoxycarbonyl, R2 is secondary or tertiary lower alkyl or lower alkylthio-lower alkyl, R3 is phenyl that is unsubstituted or substituted by one or more lower alkoxy radicals, or C4-C8cycloalkyl, R4 is phenyl or cyclohexyl each substituted in the 4-position by unsaturated heterocyclyl that is bonded by way of a ring carbon atom, has from 5 to 8 ring atoms, contains from 1 to 4 hetero atoms selected from nitrogen, oxygen, sulfur, suffinyl (—SO—) and sulfonyl (—SO2—) and is unsubstituted or substituted by lower alkyl or by phenyl-lower alkyl, R5, independently of R2, has one of the meanings mentioned for R2, and R6, independently of R1, is lower alkoxycarbonyl, or salts thereof, provided that at least one salt-forming group is present. The compounds are inhibitors of retroviral aspartate protease and can be used, for example, in the treatment of AIDS.Type: GrantFiled: November 23, 1999Date of Patent: October 9, 2001Assignee: Novartis Finance CorporationInventors: Alexander Fässler, Guido Bold, Hans-Georg Capraro, Marc Lang, Satish Chandra Khanna
-
Patent number: 6297275Abstract: A method for controlling fungi using a phenylhydrazine derivative compound of the formula: wherein: X is phenyl, phenylalkoxy, phenoxy, or benzyl, alone or in combination with one or more halogen, alkyl, or alkylthio; Y is hydrogen, alkanoyl, haloalkanoyl, or alkoxy carbonyl; and R is hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, or phenylalkoxy.Type: GrantFiled: September 7, 1999Date of Patent: October 2, 2001Assignees: Uniroyal Chemical Company, Inc., Crompton Co./CieInventors: Mark Achiel Dekeyser, Kenneth Wesley Seebold, Jr., Gaik-Lean Chee
-
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
-
Patent number: 6265613Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the indexes have the meanings given in the specification, their salts, their preparation and their use.Type: GrantFiled: February 24, 1998Date of Patent: July 24, 2001Assignee: BASF AktiengesellschaftInventors: Bernd Müller, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Klaus Oberdorf, Franz Röhl, Norbert Götz, Michael Rack, Ruth Müller, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
-
Patent number: 6248787Abstract: This invention concerns new methods and compositions that are useful in preventing and ameliorating cachexia, the clinical syndrome of poor nutritional status and bodily wasting associated with cancer and other chronic diseases. More particularly, the invention relates to aromatic guanylhydrazone (more properly termed amidinohydrazone) compositions and their use to inhibit the uptake of arginine by macrophages and/or its conversion to urea. These compositions and methods are also useful in preventing the generation of nitric oxide (NO) by cells, and so to prevent NO-mediated inflammation and other responses in persons in need of same. In another embodiment, the compounds can be used to inhibit arginine uptake in arginine-dependent tumors and infections.Type: GrantFiled: June 6, 1995Date of Patent: June 19, 2001Assignee: The Picower Institute for Medical ResearchInventors: Marina Bianchi, Anthony Cerami, Kevin J. Tracey, Peter Ulrich
-
Patent number: 6235787Abstract: Hydrazine derivatives of the formula wherein Y is CO or SO2; R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y is SO2 and is lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR5R6 when Y is CO; and R3 is hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R2 and R3 together form the residue of a 5-, 6- or 7-membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 is lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula X-aryl, X-heteroarType: GrantFiled: June 16, 1998Date of Patent: May 22, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael John Broadhurst, William Henry Johnson, Daryl Simon Walter
-
Patent number: 6172108Abstract: Compounds of formula (I): R—NH—A—CO—NH—NH—(W)n—Z (I) wherein: n is 0 or 1, W represents —CO— or S(O)r wherein r is 0, 1 or 2, Z represents a group selected from aryl, arylalkyl, heteroaryl and heteroarylalkyl, each optionally substituted, R represents a grouping selected from: Z1—T—CO—, Z1—O—T—CO—, Z1—T—O—CO—, Z1—T—S(O)q— wherein Z1, T and q are as defined in the description, A represents alkylene, alkenylene or alkynylene each having from 3 to 8 carbon atoms, alkylenecycloalkylene, cycloalkylenealkylene, alkylenecycloalkylenealkylene, alkylenearylene, arylenealkylene, alkylenearylenealkylene a grouping wherein B1 is as defined in the description, or A forms with the adjacent nitrogen atom a grouping as defined in the description, and medicinal products containing the same which are useful as Neuropeptide Y receptorType: GrantFiled: December 16, 1999Date of Patent: January 9, 2001Assignee: Adir et CompagnieInventors: Antonio Monge Vega, Ignacio Aldana Moraza, Daniel-Henri Caignard, Jacques Duhault, Jean Boutin, Odile Dellazuana
-
Patent number: 6143728Abstract: There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.Type: GrantFiled: November 14, 1997Date of Patent: November 7, 2000Assignee: The Picower Institute for Medical ResearchInventors: Kevin J. Tracey, Pamela Cohen, Michael Bukrinsky, Helena Schmidtmayerova
-
Patent number: 6140368Abstract: The present invention relates to a novel class of compounds that are potent inhibitors of HIV reverse transcriptase and HIV integrase. In addition to being multienzyme inhibitors, the inventive compounds of the present invention are remarkable in at least two other respects. First, they do not appear to be toxic to cells at typical therapeutic concentrations. Second, they appear to be equally effective against mutant strains of HIV reverse transcriptase commonly found in patients who have developed resistance to current reverse transcriptase inhibitors. Because the inventive compounds show promise in combatting viral resistance and are potent inhibitors of both HIV reverse transcriptase and integrase, they are ideal candidates for use in combination with existing therapies or alone in treating AIDS or HIV infection.Type: GrantFiled: May 4, 1998Date of Patent: October 31, 2000Assignees: The Regents of the University of California, Rutgers, The University of New JerseyInventors: George L. Kenyon, Margaret Stauber, Karl Maurer, Dolan Eargle, Angelika Muscate, Andrew Leavitt, Diana C. Roe, Todd J. A. Ewing, Allan G. Skillman, Jr., Edward Arnold, Irwin D. Kuntz, Malin Young
-
Patent number: 6117910Abstract: This invention relates to compounds of the formula: ##STR1## which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.Type: GrantFiled: June 13, 1997Date of Patent: September 12, 2000Assignee: SmithKline Beecham CorporationInventors: James Francis Callahan, Richard McCulloch Keenan, Chet Kwon, James Martin Samanen
-
Patent number: 6083908Abstract: Compounds of Formula I ##STR1## and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed, wherein R.sup.1, R.sup.2, R.sup.3a, R.sup.4a, R.sup.5a, G, J and D are as defined in the specification.Type: GrantFiled: January 12, 1999Date of Patent: July 4, 2000Assignee: Novo Nordisk A/SInventor: Michael Ankersen
-
Patent number: 6075044Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.Type: GrantFiled: July 17, 1998Date of Patent: June 13, 2000Assignee: The Regents of the University of CaliforniaInventors: Ching C. Wang, John Somoza, Jon P. Page, Ronaldus Marcellus Alphonsus Knegtel, Irwin D. Kuntz, Connie M. Oshiro, A. Geoffrey Skillman
-
Patent number: 6031003Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca.sup.2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.Type: GrantFiled: June 7, 1995Date of Patent: February 29, 2000Assignees: NPS Pharmaceuticals, Inc., The Brigham and Women's HospitalInventors: Edward F. Nemeth, Bradford C. Van Wagenen, Manuel F. Balandrin, Eric G. DelMar, Scott T. Moe