Plural Acyclic Nitrogens Bonded Directly To The Same Carbon Or Single Bonded Directly To Each Other Patents (Class 546/332)
-
Patent number: 6743790Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R3, R4, R5, R6, A, X, m and n have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, for example as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 6, 2001Date of Patent: June 1, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Otmar Klingler, Manfred Schudok, Hans-Peter Nestler, Hans Matter, Herman Schreuder
-
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
-
Patent number: 6730783Abstract: 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: April 22, 2003Date of Patent: May 4, 2004Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan
-
Publication number: 20040067943Abstract: Compounds of the formula (I), in which M is a central building block selected from the group below in which Al, A2, K1 and K2 are as defined in the description, are novel effective tryptase inhibitors.Type: ApplicationFiled: August 18, 2003Publication date: April 8, 2004Inventor: Thomas Martin
-
Patent number: 6716860Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: December 2, 2002Date of Patent: April 6, 2004Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Lauffer, Michael Mullican
-
Patent number: 6706715Abstract: The present invention relates to compounds of the formula I, in which R1, R2, R4, R5, D1, D2, X1, X2, X3, A and B have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of thromboembolic diseases and restenoses. They are reversible inhibitors of the blood clotting enzyme factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 26, 2002Date of Patent: March 16, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Manfred Schudok, Otmar Klingler, Hans-Peter Nestler, Hans Matter, Herman Schreuder, Hauke Szillat
-
Publication number: 20040044049Abstract: Compounds, compositions and methods for altering insulin secretion, particularly in the context of treatment of subjects having, or suspected of being at risk for having, diabetes mellitus.Type: ApplicationFiled: February 10, 2003Publication date: March 4, 2004Applicant: MitoKorInventors: Yazhong Pei, Soumitra S. Ghosh, Ian William James
-
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
-
Publication number: 20040034231Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: August 12, 2003Publication date: February 19, 2004Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
-
Patent number: 6664393Abstract: The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: August 26, 2002Date of Patent: December 16, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Otmar Klingler, Gerhard Zoller, Elisabeth Defossa, Fahad A. Al-Obeidi, Armin Walser, James Ostrem
-
Publication number: 20030225144Abstract: The present invention relates to novel crystalline forms of an inhibitor of Factor Xa, processes for its preparation, compositions comprising it, and its therapeutic use.Type: ApplicationFiled: April 1, 2003Publication date: December 4, 2003Applicant: Aventis Pharmaceuticals Inc.Inventors: Rick G. Woodward, David S. Teager
-
Patent number: 6653312Abstract: Amidine compounds of the formula wherein the substituents are defined as in the application useful as NO-synthase enzyme inhibitors.Type: GrantFiled: March 16, 2001Date of Patent: November 25, 2003Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Serge Auvin, Pierre-Etienne Chabrier de Lassauniere, Jeremiah Harnett, Dominique Pons, Gérard Ulibarri
-
Publication number: 20030208067Abstract: The present invention is directed in part towards methods of modulating the function of protein kinases with phenol- and hydroxynaphthalene-based compounds. The methods incorporate cells that express a protein kinase. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to phenol- and hydroxynaphthalene-based compounds and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: May 28, 2002Publication date: November 6, 2003Inventors: Sheldon Xiaodong Cao, David Paul Dumas, Xiaohua Chen, Jae Young Yang
-
Publication number: 20030203944Abstract: The present invention relates to an antagonist against vanilloid receptor and the pharmaceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain, acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fevescence, stomach-duodenal ulcer, inflammatory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: February 3, 2003Publication date: October 30, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Young Ho Park, Jung Bum Yi
-
Patent number: 6638931Abstract: 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: November 28, 2000Date of Patent: October 28, 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
-
Patent number: 6632840Abstract: Monoacyl-substituted guanidines of formula III, or a salt or acid thereof, and their use as medicine or diagnostic aid: in which X(2) isType: GrantFiled: March 24, 2000Date of Patent: October 14, 2003Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
-
Publication number: 20030191113Abstract: The invention concerns compounds of general formula (1) wherein: n, G, Q1, Q2, X1, X2, Y and Z are as defied in the description, the method for preparing said compounds, fungicide compositions comprising said compounds and methods for treating plants using said compounds or compositions.Type: ApplicationFiled: July 8, 2002Publication date: October 9, 2003Inventors: Francisco Nieto-Roman, Jean-Pierre Vors, Alain Villier, Helene Lachaise, Adeline Mousques, Benoit Hartmann, Pierre Hutin, Jose Lorenzo Molina, Benoit Muller
-
Publication number: 20030181717Abstract: Novel chiral derivitaves of non-nucleoside inhibitors (NNI), particularly R-isomers of halopyridyl and thiazoyl thiourea compounds are provided as potent inhibitors of reverse transcriptase (RT), and particularly of retroviral RT, most particularly HIV RT. The stereospecific compounds and compositions of the invention inhibit replication of retrovirus, particularly human immunodeficiency virus-1 (HIV-1) and drug resistant strains.Type: ApplicationFiled: January 21, 2003Publication date: September 25, 2003Applicant: Parker Hughes Institute located at Roseville, MinnesotaInventors: Fatih M. Uckun, Taracad K. Venkatachalam
-
Publication number: 20030176469Abstract: The invention relates to substituted anthranylalkyl and cycloalkyl amides of general formula (I) and to their use as medicaments for treating diseases caused by persistent angiogenesis.Type: ApplicationFiled: May 9, 2003Publication date: September 18, 2003Inventors: Dieter Seidelmann, Martin Kruger, Eckhard Ottow, Andreas Huth, Karl-heinz Thierauch, Andreas Menrad, Martin Haberey
-
Publication number: 20030176465Abstract: Novel compounds of the formula I 1Type: ApplicationFiled: January 17, 2003Publication date: September 18, 2003Inventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleitz, Christopher Barnes
-
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
-
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
-
Publication number: 20030162814Abstract: The novel compounds of formula (I), wherein R1, R2, R2′, R2″, R3, R4, R5, R5′, R5″, R5′″, R″″, X, Y, U, V and W have the meanings given in patent claim no. 1, are inhibitors of the coagulation factors Xa and VIIa and can be used for treating thromboses, myocardial infarction, arteriosclerosis, inflammations, apoplexy, angina pectoris, restenosis following angioplasty, intermittent claudication, tumours, tumour diseases and/or tumour metastases.Type: ApplicationFiled: January 23, 2003Publication date: August 28, 2003Inventors: Horst Juraszyk, Dieter Dorsch, Werner Mederski, Christos Tsaklakidis, Christopher Barnes, Johannes Gleitz
-
Publication number: 20030153596Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.Type: ApplicationFiled: July 9, 2002Publication date: August 14, 2003Inventors: Young Ger Suh, Uh Taek Oh, Hee Doo Kim, Jee Woo Lee, Hyeung Geun Park, Ok Hui Park, Yong Sil Lee, Young Ho Park, Yung Hyup Joo, Jin Kyu Choi, Kyung Min Lim, Sun Young Kim, Jin Kwan Kim, Hyun Ju Koh, Joo Hyun Moh, Yeon Su Jeong, Jung Bum Yi, Young Im Oh
-
Publication number: 20030144310Abstract: This invention provides a compound having the structure: 1Type: ApplicationFiled: September 24, 2002Publication date: July 31, 2003Inventors: Lakmal W. Boteju, Michael J. Konkel, Joel K. Kawakami, John Wetzel
-
Patent number: 6596863Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formulaType: GrantFiled: April 29, 2002Date of Patent: July 22, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
-
Publication number: 20030108970Abstract: The present invention provides immunogens for generating anti-neonicotinoid antibodies as well as antibodies, methods, reagents and kits for determining the presence of one or more neonicotinoid insecticides in a sample by immunoassay. The present invention has particular application to determination of the concentration of neonicotinoid insecticides applied to a plant propagation materials such as seed.Type: ApplicationFiled: June 7, 2002Publication date: June 12, 2003Inventors: James Francis Brady, Dana Philip Simmons, Timothy Edward Wilson
-
Publication number: 20030083504Abstract: The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: 1Type: ApplicationFiled: October 4, 2002Publication date: May 1, 2003Inventors: Jean Ackermann, Leo Alig, Alexander Chucholowski, Katrin Groebke, Kurt Hilpert, Holger Kuehne, Ulrike Obst, Lutz Weber, Hans Peter Wessel
-
Patent number: 6545029Abstract: The present invention relates to new phenylserine derivatives as integrin antagonists with a broad spectrum of action having, inter alia, antiosteoporotic, antirestenotic, anticarcinogenic and antiatherosclerotic activity. The present invention moreover relates to the preparation of these compounds and their use for the production of medicaments, and also medicaments comprising them.Type: GrantFiled: June 12, 2001Date of Patent: April 8, 2003Assignee: Bayer AktiengesellschaftInventor: Andrea Vaupel
-
Patent number: 6538013Abstract: Novel pesticides of formula (I) wherein the substituents R, R1, R2, R2′, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2′, T, U, X and Y are as defined in claim 1 and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).Type: GrantFiled: May 7, 2001Date of Patent: March 25, 2003Assignee: Novartis Animal Health US, Inc.Inventors: Thomas Goebel, Eliane Humbert-Droz, Maurizio Schwarzenbach
-
Patent number: 6534499Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: March 18, 2003Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
-
Patent number: 6528532Abstract: The present invention provides HIV aspartyl protease inhibitors of the formula: and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein n is 3 or 4, Y is O, S, NH or N—CN, wherein Cx may be, for example COOH, or CH2OH, wherein R1 is selected from the group consisting of a benzenesulfonyl group of formula II as defined herein, wherein R2 may be, for example, iso-butyl, or 3-methylbutyl, and wherein R3 and R4 are as defined herein.Type: GrantFiled: May 13, 2002Date of Patent: March 4, 2003Assignee: Pharmacor Inc.Inventors: Brent Richard Stranix, Abderrahim Bouzide, Gilles Sauvé
-
Patent number: 6528533Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: January 3, 2002Date of Patent: March 4, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: David Lauffer, Michael Mullican
-
Patent number: 6528651Abstract: The present invention relates to a process for the preparation of compounds of the formula (I) by reacting compounds of the formula (II) in which Het, R1, R2 and R4 are as defined in the description, with anhydrous hydrogen chloride or compounds which generate hydrogen chloride.Type: GrantFiled: June 14, 2002Date of Patent: March 4, 2003Assignee: Bayer AktiengesellschaftInventors: Kai van Laak, Wolfram Sirges, Detlef Wollweber
-
Patent number: 6518433Abstract: A process for the production of a compound of formula (I) wherein R1 is hydrogen or C1-C4-alkyl; R2 is hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl, C3-C6-cycloalkyl or a radical —CH2B; A is selected from the group consisiting of 2-chloropyrid-5-yl, tetrahydrofuran-3 -yl, 5-methyl-tetrahydrofuran-3-yl or 2-chlorothiazol-5-yl; and B is phenyl, 3-pyridyl or thiazolyl, which are optionally substituted by one to three substituents selected from the group consisting of C1-C3-alkyl, C1-C3-halogenalkyl, cyclopropyl, halogencyclopropyl, C2-C3-alkenyl, C2-C3-alkinyl, C1-C3-alkoxy, C2-C3-halogenalkenyl, C2-C3-halogenalkinyl, C1-C3-halogenalkoxy, C1-C3-alkylthio, C1-C3-halogenalkylthio, allyloxy, propargyloxy, allylthio, propargylthio, halogenallyloxy, halogenallylthio, halogen, cyano or nitro; and optionally the possible E/Z isomers, E/Z isomeric mixtures and/or tautomers thereof, respectively in free form or in salt form; characterised in that a compound of formula (II)Type: GrantFiled: September 18, 2000Date of Patent: February 11, 2003Assignee: Syngenta Crop Protection, Inc.Inventors: Peter Maienfisch, Thomas Rapold, Henry Szczepanski
-
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
-
Patent number: 6512121Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.Type: GrantFiled: June 11, 2001Date of Patent: January 28, 2003Assignee: G.D. Searle & Co.Inventors: John J Talley, James A Sikorski, Matthew J Graneto, Jeffrey S Carter, Bryan H Norman, Balekudru Devadas, Hwang-Fun Lu
-
Publication number: 20030018056Abstract: A compound represented by the following formula: 1Type: ApplicationFiled: June 17, 2002Publication date: January 23, 2003Inventors: Masahumi Kitano, Masatoshi Yuri, Naohito Ohashi
-
Patent number: 6500823Abstract: The object of the invention consists of novel unsaturated hydroximic acid derivatives, the process for their preparation and as active substance such as compounds containing pharmaceutical compositions. The novel compounds possess valuable pharmaceutical effects, so they can be used in the treatment of states connected with energy deficiency of the cell caused by PARP inhibition, in diabetes complications, in oxygen deficient status of the heart and brain, in neurodegenerative diseases, in the treatment of autoimmune and/or viral diseases. In formula (I).Type: GrantFiled: March 2, 2001Date of Patent: December 31, 2002Assignee: N-Gene Research Laboratories, Inc.Inventors: Péter Literáti Nagy, Kálmán Takács, Balázs Sümegi
-
Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
-
Patent number: 6472562Abstract: The present invention relates to compounds of the formula I, in which A, L, Y, and k have the meanings indicated in the specification and claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa and/or factor VIIa and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of conditions in which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: October 27, 2000Date of Patent: October 29, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Otmar Klingler, Gerhard Zoller, Elisabeth Defossa, Fahad A. Al-Obeidi, Armin Walser, James Ostrem
-
Publication number: 20020151545Abstract: Compounds of formula I and II, 1Type: ApplicationFiled: November 7, 2001Publication date: October 17, 2002Inventors: Gregory S. Bisacchi, James C. Sutton, Shung C. Wu
-
Patent number: 6451792Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.Type: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
-
Patent number: 6444817Abstract: Compounds of the formula where A, B, D, R1 and R2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases. The novel compounds are prepared via compounds of the formula H2N—CH2—G—M.Type: GrantFiled: October 8, 1999Date of Patent: September 3, 2002Assignee: Abbott LaboratoriesInventors: Hans-Joachim Böhm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
-
Patent number: 6436999Abstract: Diacyl-substituted guanidines of the formula I are described where X(1) and X(2) are as defined herein. The compounds are suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventitive manner the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 18, 1997Date of Patent: August 20, 2002Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Peter Crause, Wolfgang Scholz, Udo Albus, Jan-Robert Schwark
-
Patent number: 6414158Abstract: The invention relates to novel carbazate intermediates of formula (II), and to a process for their preparation, and their usefulness in the preparation of (1,3,4) oxadiazine derivatives useful as pesticides, in particular as anthelminthicides, insecticides, acaricides, and nematicides.Type: GrantFiled: July 6, 2000Date of Patent: July 2, 2002Assignee: Bayer AKtiengesellschaftInventors: Hubert Dyker, Andrew Plant, Jürgen Scherkenbeck, Christoph Erdelen, Achim Harder
-
Patent number: 6410573Abstract: Novel 2,5-substituted benzolsulfonyl ureas and thioureas of formula (I) as illustrated in the disclosure. The compounds are useful active ingredients for medicaments. The compounds of formula (I) act as inhibitors on ATP-sensitive potassium canals and are suitable for the treatment of cardiovascular disorders, especially the treatment of arrhythmias, prevention of sudden death from heart disease or affect diminished contractility of the heart. The invention also relates to methods for producing compounds of formula (I), the use thereof and pharmaceutical preparations containing said compounds.Type: GrantFiled: January 16, 2001Date of Patent: June 25, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Holger Heitsch, Heinrich Christian Englert, Heinz Gögelein
-
Publication number: 20020058195Abstract: A high contrast photographic material is disclosed containing a new type of hydrazine compound characterized in that said hydrazine compound comprises a redox moiety capable of developing an exposed silver halide crystal.Type: ApplicationFiled: September 7, 2001Publication date: May 16, 2002Inventors: Johan Loccufier, Stefaan Lingier
-
Patent number: 6365745Abstract: The present invention provides a method for producing a hydrazine derivative of the formula [2]: wherein R1 is alkyl group having 1-12 carbon atoms and the like, R2 is alkyl group having 1-12 carbon atoms and the like, and Ar is phenylene group and the like, from a hydrazone derivative of the formula [1] wherein R1, R2 and Ar are as defined above, in the presence of at least one base selected from the group consisting of an organic base and an inorganic base, and a metal hydrogenating catalyst. By this method, reduction proceeds selectively and a hydrogenolysis reaction (side reaction) can be suppressed.Type: GrantFiled: July 13, 2001Date of Patent: April 2, 2002Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Kozo Matsui, Kiyoshi Sugi, Hiromi Suga, Nobushige Itaya
-
Publication number: 20020022730Abstract: The present invention provides a method for producing a hydrazine derivative of the formula [2]: 1Type: ApplicationFiled: July 13, 2001Publication date: February 21, 2002Inventors: Kozo Matsui, Kiyoshi Sugi, Hiromi Suga, Nobushige Itaya