Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/405)
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Patent number: 6191158Abstract: Use of a compound having formula (I) and salts thereof with pharmaceutically acceptable organic or inorganic bases, for preparing a pharmaceutical composition active in the treatment of disorders characterized by production of MCP-1 protein.Type: GrantFiled: April 25, 2000Date of Patent: February 20, 2001Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Angelo Guglielmotti, Claudio Milanese
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Patent number: 6180637Abstract: The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) wherein X is —SO2—, —SO—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Y is —(C═O)—, —(C═O)—NH—, —(C═O)—NH—(CH2)p—, —C═O)—(CH2)p—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—(C═O)—NH—(CH2)p—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Z is —O—, —O—(CH2)p—, —NH—, —NH—(Type: GrantFiled: May 5, 1999Date of Patent: January 30, 2001Assignee: Arzneimittelwerk Dresden GmbHInventors: Rudolf Schindler, Norbert Höfgen, Hildegard Poppe, Kay Brune
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Patent number: 6169104Abstract: The present invention relates, inter alia, to compounds that bind tubulin and exhibit anti-mitotic properties and to methods of using such compounds to inhibit abnormal cell mitosis and, in particular, to inhibit tumor cell growth. In addition, methods are presented of treating mammalian diseases associated with undesired and uncontrolled angiogenesis.Type: GrantFiled: March 25, 1998Date of Patent: January 2, 2001Assignees: Large Scale Biology Corporation, SRI InternationalInventors: Daniel Tus{acute over (e)}, Xiaoying Chen, Charles K. Hiebert, Cris M. Olsen, Keith Laderoute, Nahid Waleh, A. Merrill Knapp
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Patent number: 6166055Abstract: This invention relates to compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: GrantFiled: July 9, 1999Date of Patent: December 26, 2000Assignee: SmithKline Beecham CorporationInventors: Katherine L. Widdowson, Hong Nie, Melvin Clarence Rutledge, Jr.
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Patent number: 6162819Abstract: The present invention relates to pyrazole derivatives of the formula I, their preparation and their use in pharmaceuticals: ##STR1## in which X, R.sup.1, R.sup.1a, R.sup.2, R.sup.3, R.sup.4 and n are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate "cGMP" and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula 1, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for this purpose, and also to pharmaceutical preparations which comprise the compounds of the formula I.Type: GrantFiled: October 5, 1998Date of Patent: December 19, 2000Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schonafinger, Hartmut Strobel
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Patent number: 6124264Type: GrantFiled: March 1, 1999Date of Patent: September 26, 2000Assignee: Pfizer Inc.Inventors: Philip A Carpino, Paul A DaSilva-Jardine, Bruce A Lefker, John A Ragan
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Patent number: 6040329Abstract: The invention relates to compounds of the formula I ##STR1## and pharmaceutically acceptable salts thereof, wherein R, R.sub.1, and R.sub.2, are as defined herein. The invention further relates to pharmaceutical compositions containing, and methods of using, the compounds of formula I, or acceptable salts thereof, for the inhibition of phosphodiesterase (PDE) type IV or the production of tumor necrosis factor (TNF) in a mammal.Type: GrantFiled: June 5, 1997Date of Patent: March 21, 2000Assignee: Pfizer IncInventor: Anthony Marfat
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Patent number: 6020331Abstract: There are disclosed .beta.-sheet mimetics and methods relating to the same for imparting or stabilizing the .beta.-sheet structure of a peptide, protein or molecule. In one aspect, the .beta.-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The .beta.-sheet mimetics have utility as protease inhibitors generally, including activity as serine protease inhibitors such as thrombin, elastase and Factor X.Type: GrantFiled: January 20, 1998Date of Patent: February 1, 2000Assignee: Molecumetics, Ltd.Inventor: Michael Kahn
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Patent number: 6011045Abstract: The present invention relates to compounds of the formula IA--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: January 4, 2000Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5994274Abstract: The present invention relates to new compounds of the formula (I) ##STR1## in which X represents alkyl,Y represents halogen or alkyl andZ represents halogen or alkyl,with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl,Het represents one of the groups ##STR2## in which A, B, D and G have the meanings given in the description,a plurality of processes for their preparation and their use as pesticides and herbicides.Type: GrantFiled: December 23, 1997Date of Patent: November 30, 1999Assignee: Bayer AktiengesellschaftInventors: Reiner Fischer, Thomas Bretschneider, Hermann Hagemann, Folker Lieb, Michael Ruther, Arno Widdig, Peter Dahmen, Markus Dollinger, Christoph Erdelen, Hans-Joachim Santel, Ulrike Wachendorff-Neumann, Alan Graff, Wolfram Andersch
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Patent number: 5990145Abstract: The present invention relates to compounds of the formula I,A--B--D--E--F--G (I)in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: December 22, 1997Date of Patent: November 23, 1999Assignees: Hoechst Aktiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 5981555Abstract: The present invention concerns composition, kits and methods for reducing the flushing effect (cutaneous erythema) of an antilipemic drug, for treating hyperlipemia, for improving the effectiveness of an anti-platelet aggregating drug (e.g., in nonresponders) and for treating thrombosis. The present compositions and kits for reducing the flushing effect and for treating hyperlipemia contain an antilipemic drug (such as niacin) and either a sustained release NSAID (such as aspirin) or an NSAID and a carboxylic acid compound other than the NSAID and antilipemic drug. The kits contain (a) pre-dosages of the NSAID and optional carboxylic acid compound and (b) an antilipemic dosage of the antilipemic drug, which optionally may be combined with NSAID and optional carboxylic acid compound in an amount effective to maintain the reduction of the flushing effect.Type: GrantFiled: September 26, 1997Date of Patent: November 9, 1999Assignees: Lipoprotein Technologies, Inc., Vanderbilt UniversityInventors: Eric H. Kuhrts, L. Jackson Roberts, II, Jason D. Morrow
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Patent number: 5955491Abstract: The present invention provides a cathepsin L inhibitor containing a compound of the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an arylalkyl, heterocyclic-alkyl or lower alkyl group which may be substituted; R.sup.2 and R.sup.3 independently are a hydrogen atom or a hydrocarbon residue which may be substituted; R.sup.4 is an alkanoyl, sulfonyl, carbonyloxy, carbamoyl or thiocarbamoyl group which may be substituted; X is formula: --CHO or --CH.sub.2 OB (wherein B is a hydrogen atom or a protecting group of hydroxyl group); m and n independently are an integer of 0 or 1; provided that R.sup.4 is an alkanoyl group substituted by aryl, a sulfonyl group substituted by aryl having more than 9 carbon atoms or by lower alkyl, or a carbamoyl or thiocarbamoyl group which may be substituted when R.sup.1 is an unsubstituted lower alkyl, arylalkyl on methylthioethyl group, R.sup.2 and R.sup.3 independently are a lower alkyl or arylalkyl, X is --CHO, m is 1 and n is 0 or 1, or a salt thereof.Type: GrantFiled: June 27, 1995Date of Patent: September 21, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Yukio Fujisawa, Tsuneo Yasuma, Junji Mizoguchi, Masakuni Kori, Masayuki Takizawa
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Patent number: 5935908Abstract: Compounds of formula (1), wherein X, Y, Z R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.7, R.sub.9 and n are as defined in claim 1 and, where appropriate, E/Z isomers, mixtures of E/Z isomers and/or tautomers thereof, in each case in free form or in agrochemically suitable salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: February 17, 1998Date of Patent: August 10, 1999Assignee: Novartis Crop Protection, Inc.Inventors: Saleem Farooq, Rene Zurfluh, Henry Szczepanski, Roger Graham Hall
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Patent number: 5891881Abstract: Aminoheterocycle-substituted glycerols of Formula I are disclosed: ##STR1## wherein one of A, B or C is --X--R, wherein X is --O-- or --S--, and R is a substituted or unsubstituted C.sub.12-24 alkyl or alkenyl, the substituent being one or more of halo, C.sub.1-3 alkoxy or cyano, provided that a double bond of the alkenyl does not originate at the carbon atom bound to X; and another of A, B or C is an aminoheterocycle ring substituent --Het--NH.sub.2, wherein Het is a 5 to 11-membered monocyclic, bicyclic or bicyclic fused heterocyclic ring moiety with at least 1 to 4 nitrogens atoms contained within the hetero cyclic moiety, one of which nitrogen atoms is bonded to the glycero carbon; and the remaining A, B, or C substituent is --OH. The compounds of Formula I, isomers, salts, pharmaceutical compositions and appliances incorporating the same, and methods of use thereof are also disclosed.Type: GrantFiled: November 21, 1997Date of Patent: April 6, 1999Assignee: Clarion Pharmaceuticals Inc.Inventors: Haridasan K. Nair, Andrew C. Peterson
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Patent number: 5889035Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 30, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau
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Patent number: 5886016Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A, wherein X, m, n, p, B, R.sup.1, R.sup.2, and R.sup.4 are as described in the specification.Type: GrantFiled: June 9, 1997Date of Patent: March 23, 1999Assignee: G.D. Searle & Co.Inventors: John J Talley, Stephen R Bertenshaw, Donald J Rogier, Jr., Matthew J Graneto
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Patent number: 5883106Abstract: Novel compounds having the ability to inhibit 5-lipoxygenase enzyme and having the following formula I: ##STR1## and the pharmaceutically acceptable salts thereof, wherein Ar.sup.1 is a heterocyclic moiety which is selected from imidazolyl, pyrrolyl, pyrazolyl, 1,2,3-triazolyl, 1,2,4-triazolyl, indolyl, indazolyl and benzimidazolyl, which is bonded to X.sup.1 through a ring nitrogen atom, and which may be optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino, and C.sub.1-4 alkyl; X.sup.1 is a direct bond or C.sub.1-4 alkylene; Ar.sup.2 is phenylene optionally substituted with halo, hydroxy, cyano, and amino X.sup.2 is --A--X-- or --X--A-- wherein A is a direct bond or C.sub.1-4 alkylene and X is oxy, thio, sulfinyl or sulfonyl; Ar.sup.3 is phenylene, pyridylene, thienylene, furylene, oxazolylene or thiazolylene optionally substituted with one or two substituents selected from halo, hydroxy, cyano, amino and C.sub.1-4 alkyl; R.sup.1 and R.sup.2 are each C.sub.Type: GrantFiled: February 6, 1998Date of Patent: March 16, 1999Assignee: Pfizer Inc.Inventors: Rodney W. Stevens, Takashi Mano, Kazunari Nakao, Yoshiyuki Okumura
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Patent number: 5830909Abstract: The invention is a method of using Angiotensin (AII) Antagonists as inhibitors of the growth of adipose tissue, reducing adipocyte growth and body weight gain.Type: GrantFiled: July 19, 1996Date of Patent: November 3, 1998Assignee: American Cyanamid CompanyInventor: David LeRoy Crandall
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Patent number: 5780394Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## in which A and B are identical or different and independently of one another in each case represent hydrogen, alkyl, alkenyl, alkynyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl or optionally substituted aryl orA and B together represent the bivalent radical of a saturated or unsaturated, optionally substituted, mono-, bi-, tri- or polycyclic system,X represents alkyl, halogen or alkoxy,Y represents hydrogen, alkyl, halogen, alkoxy or halogenoalkyl,Z represents alkyl, halogen or alkoxyn represents a number 0, 1, 2 or 3,G represents hydrogen (a) or the groups ##STR2## in which E represents a metal ion equivalent or an ammonium ion,L and M represents oxygen and/or sulphur,and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meaning given in the text of the application.Type: GrantFiled: January 23, 1997Date of Patent: July 14, 1998Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5773453Abstract: The present invention concerns methods for reducing cutaneous flushing in a patient to whom niacin is administered. According to the present method, two or more doses of a nonsteroidal anti-inflammatory drug are administered to a patient prior to administering niacin. Alternatively, the nonstcroidal anti-inflammatory drug can be administered concurrently with niacin administration. The nonstcroidal anti-inflammatory drug can be aspirin, ibuprofen, indomethacin, phenylbutazone, or naproxen. The nonsteroidal anti-inflammatory drug is administered in an amount effective to reduce cutaneous flushing caused by the niacin, and is administered in an amount up to 160 mg for aspirin and ibuprofen, 10 mg for indomethacin, and 100 mg for phenylbutazone and naproxen.Type: GrantFiled: April 19, 1995Date of Patent: June 30, 1998Assignees: Vanderbilt University, Lipoprotein Technologies, Inc.Inventors: L. Jackson Roberts, II, Jason D. Morrow, Eric H. Kuhrts
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Patent number: 5750547Abstract: The present invention is concerned with novel anticancer agents having potent antineoplastic activity without systemic toxicity and mutagenicity. The novel anticancer agents of the present invention are derivatives of formula I: ##STR1## wherein: A is O or NH; andB is an aryl group selected from the group consisting of phenyl, indane, fluorene, indazole, indole, and pyridine, the aryl group being substituted with at least one substituent selected from the group consisting of hydrogen, C.sub.1-16 alkyl optionally substituted with one or more OH or SH, lower alkoxy, C.sub.3-6 cycloallyl, lower alkylthio, nitro, cyano, lower alkene, lower alkyne, OH, SH, carboxy lower alkyl, carboxy lower alkyl esters, amino, N-lower alkyl, N,N-dilower alkyl and halogen; or a prodrug thereof, with the provisos that when A is NH and B is phenyl:a) B is substituted with at least one substituent other than hydrogen;b) B is not:1) mono-substituted in the 4 position with C.sub.1-2 alkyl, tert-butyl or n-butyl halogen, OH, carboxy C.Type: GrantFiled: June 7, 1996Date of Patent: May 12, 1998Assignee: Universite LavalInventors: Rene C. Gaudreault, Patrick Poyet
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Patent number: 5683965Abstract: The aryl-keto-enolic heterocycles according to the invention have the formula (I), in which Het stands for a heterocyclic group from the series (a), (b) or (c), and X, Y, Z, n, A, B, E, L and M have the meanings given in the description. The compounds having the formula (I) are pesticides, in particular acaricides, insecticides, fungicides and herbicides. Also disclosed is their preparation.Type: GrantFiled: May 13, 1996Date of Patent: November 4, 1997Assignee: Bayer AktiengesellschaftInventors: Jurgen Bachmann, Thomas Bretschneider, Reiner Fischer, Bernd-Wieland Kruger, Hans-Joachim Santel, Markus Dollinger, Christoph Erdelen, Ulrike Wachendorff-Neumann
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Patent number: 5665757Abstract: A method of treating anxiety in a warm blooded animal by administering an anti-anxiety effective amount of a nitric oxide synthase inhibitor, and compositions containing the same.Type: GrantFiled: July 13, 1994Date of Patent: September 9, 1997Assignee: Robert W. DunnInventors: Robert W. Dunn, Suzanne La Marca
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Patent number: 5661110Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5633274Abstract: The Applicant has identified a particular class of imidazoles that inhibit nonprostate cancer cell proliferation. These imidazoles can be used to beneficially treat a variety of cancers. The imidazoles can be administered in a variety of formulations, including long-term sustained release implants and anti-cancer cocktails.Type: GrantFiled: February 18, 1993Date of Patent: May 27, 1997Assignee: President and Fellows of Harvard CollegeInventors: Jose Halperin, Carlo Brugnara
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Patent number: 5624921Abstract: The present invention relates to the use of certain aminoacetylmercapto derivatives in treating patients suffering from hypertriglyceridemia, atherosclerosis and hypercholesterolemia.Type: GrantFiled: August 9, 1995Date of Patent: April 29, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, John F. French, Richard C. Dage
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Patent number: 5612360Abstract: This invention provides novel heterocyclic derivatives, their pharmaceutical formulations, and their use for antagonizing angiotensin II receptors in mammals.Type: GrantFiled: April 20, 1993Date of Patent: March 18, 1997Assignee: Eli Lilly and CompanyInventors: Donald B. Boyd, Sherryl L. Lifer, Winston S. Marshall, Alan D. Palkowitz, William Pfeifer, Jon K. Reel, Richard L. Simon, Mitchell I. Steinberg, K. Jeff Thrasher, Venkatraghavan Vasudevan, Celia A. Whitesitt
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Patent number: 5602122Abstract: The present invention relates to the use of certain aminoacetylmercapto derivatives in treating patients suffering from hypercholesterolemia.Type: GrantFiled: October 26, 1995Date of Patent: February 11, 1997Assignee: Merrell Pharmaceuticals Inc.Inventors: Gary A. Flynn, John F. French, Richard C. Dage
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Patent number: 5583152Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: June 5, 1995Date of Patent: December 10, 1996Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5550134Abstract: The present invention provides methods of inhibiting bone loss in mammals via the administration to a mammal in need of such treatment an effective amount of a compound from a series of benzoquinolin-3-ones. Such compounds also are sequentially or concurrently coadministered with a bone antiresorptive agent or a bone anabolic agent.Type: GrantFiled: May 10, 1995Date of Patent: August 27, 1996Assignee: Eli Lilly and CompanyInventors: James E. Audia, Blake L. Neubauer
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Patent number: 5494890Abstract: The present invention relates to herbicidally, acaricidally and insecticidally active pyrazolidine-3,5-diones of the formula I ##STR1## in which R.sub.1 is ##STR2## R.sub.2 and R.sub.3 independently of one another are C.sub.1 -C.sub.6 alkyl; C.sub.3 -C.sub.6 alkenyl; or C.sub.3 -C.sub.6 alkynyl; orR.sub.2 and R.sub.3 together are a --(CH.sub.2).sub.3 --, --(CH.sub.2).sub.4 --, --CH.sub.2 --CH.dbd.CH--CH.sub.2 --, --CH.sub.2 --CH.dbd.CH-- or --(CH.sub.2).sub.2 --CH.dbd.CH-- bridge which is unsubstituted or up to trisubstituted by C.sub.1 -C.sub.4 alkyl;n is 0; 1; 2; 3; or 4;m is 0; or 1; the total of m and n being less than, or equal to, 4; theR.sub.4 radicals independently of one another are halogen; nitro; cyano, C.sub.1 -C.sub.4 alkyl; C.sub.1 -C.sub.4 haloalkyl; C.sub.1 -C.sub.10 alkoxy; C.sub.1 -C.sub.4 haloalkoxy; C.sub.3 -C.sub.6 alkenyloxy; C.sub.1 -C.sub.4 alkoxy-C.sub.2 -C.sub.4 alkoxy; C.sub.3 -C.sub.6 alkynyloxy; C.sub.1 -C.sub.4 alkylcarbonyl; C.sub.1 -C.sub.4 alkoxycarbonyl; C.sub.1 -C.sub.Type: GrantFiled: June 2, 1995Date of Patent: February 27, 1996Assignee: Ciba-Geigy CorporationInventors: Frederik Cederbaum, Hans-Georg Brunner, Manfred Boger
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Patent number: 5474974Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.Type: GrantFiled: April 28, 1994Date of Patent: December 12, 1995Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5374638Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, congestive heart failure, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.Type: GrantFiled: March 19, 1993Date of Patent: December 20, 1994Assignee: Merck & Co., Inc.Inventors: Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
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Patent number: 5366973Abstract: The present invention relates to certain novel mercaptoacetylamido pyridazo[1,2]pyridazine, pyrazolo[1,2]pyridazine, pyridazo[1,2- a] [1,2]diazepine and pyrazolo[1,2- a ][1,2]diazepine derivatives useful as inhibitors of enkephalinase and of ACE.Type: GrantFiled: November 3, 1993Date of Patent: November 22, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gary A. Flynn, Patrick W. Shum
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Patent number: 5352676Abstract: This invention relates to a method of treating rheumatoid arthritis, which method comprises administering to a mammal a therapeutically effective amount of a compound of formula (I): ##STR1## wherein R1 is unsubstituted or substituted phenyl;R.sub.2 is a morpholinomethyl group;R.sub.3 is hydrogen;R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.a is hydrogen; andR.sub.b is a group --(A).sub.m --R.sub.5 wherein m is zero or 1, A is a C.sub.1 -C.sub.6 alkylene chain and R.sub.5 is unsubstituted or substituted phenyl;or a pharmaceutically acceptable salt thereof.Type: GrantFiled: July 1, 1993Date of Patent: October 4, 1994Assignee: Farmitalia Carlo Erba SrlInventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
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Patent number: 5334597Abstract: Compounds having the formula I: ##STR1## are antagonists of the actions of leukotrienes. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.Type: GrantFiled: October 17, 1991Date of Patent: August 2, 1994Assignee: Merck Frosst Canada, Inc.Inventors: Petpiboon Prasit, Marc Blouin
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Patent number: 5332720Abstract: There are provided new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) ##STR1## The new 3-hydroxy-4-aryl-5-oxo-pyrazoline derivatives of the formula (I) have a particularly pronounced activity against animal pests, in particular against insects and arachnids, and against weeds.Type: GrantFiled: December 16, 1992Date of Patent: July 26, 1994Assignee: Bayer AktiengesellschaftInventors: Bernd-Wieland Kruger, Reiner Fischer, Heinz-Jurgen Bertram, Thomas Bretschneider, Stefan Bohm, Andreas Krebs, Thomas Schenke, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5321032Abstract: A tachykinin-antagonistic compound of the following general formula:R.sup.1 --A.sup.1 --D--Trp(R.sup.2)--A.sup.2 --R.sup.3[whereinR.sup.1 is hydrogen or amino-protective groupR.sup.2 is amino-protective groupR.sup.3 is ar(lower)alkoxy or N-(lower)alkyl or N-ar(lower)alkylaminoA.sup.1 is single bond or one amino acid residueA.sup.2 is one amino acid residue other than Phe.]or the salt thereof.Type: GrantFiled: August 12, 1992Date of Patent: June 14, 1994Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masaaki Matsuo, Daijiro Hagiwara, Hiroshi Miyake
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Patent number: 5260327Abstract: This invention provides methods for inhibiting the proliferation of brain or hepatic metastases, in vivo, by contacting the cells with lonidamine and radiation.Type: GrantFiled: August 4, 1992Date of Patent: November 9, 1993Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Jae H. Kim, Sang H. Kim, Alan Alfieri, Charles W. Young
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Patent number: 5229408Abstract: The invention concerns a 1,2-dihydro-3H-indazol-3-one derivative of formula I ##STR1## wherein R.sup.a is hydrogen, halogeno, hydroxy, cyano, trifluoromethyl, (1-6C)alkyl or (1-6C)alkoxy;R.sup.b is hydrogen or (1-6C)alkyl;R.sup.c is hydrogen, (1-8C)alkyl or (3-8C)alkenyl; andY is (1-8C)alkyl, (3-8C)alkenyl or (3-8C)alkynyl, or Y is a group of the formula --A--Q in which A is (1-6C)alkylene or (3-6C)alkenylene, and Q is phenyl or naphthyl, which may optionally bear one or two substituents;or a pharmaceutically-acceptable salt thereof;or a 1-(1-4C)alkoxycarbonyl derivative thereof.The invention also concerns processes for the manufacture of an indazol-3-one of the formula I and pharmaceutical compositions containing said indazol-3-one. Also included in the invention is a method of treating various inflammatory or allergic diseases using an indazol-3-one of the formula I.Type: GrantFiled: May 8, 1991Date of Patent: July 20, 1993Assignees: ICI PHARMA, Imperial Chemical Industries PLCInventor: Pierre A. R. Bruneau
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Patent number: 5196445Abstract: Heteroaryl-3-oxo-propanenitrile derivatives of formula (I) ##STR1## wherein X represents an oxygen atom or a --CH(R.sub.4)--, --O--CH(R.sub.4)--, --S(O).sub.n --CH(R.sub.4)--, --CH(R.sub.4)--O--, --CH(R.sub.4)--S(O).sub.n -- --CH(R.sub.4)--CH.sub.2 -- group wherein n is 0, 1 or 2; R.sub.1 represents C.sub.1 -C.sub.6 alkyl, pyridyl or unsubstituted or substituted phenyl; R.sub.2, R.sub.3, and R.sub.4 are as herein defined; and Q is hydrogen, carboxy, C.sub.2 -C.sub.7 -alkoxycarbonyl or a --CON(R.sub.a)R.sub.b group, R.sub.a and R.sub.b being as defined herein; and their pharmaceutically acceptable salts are useful in the preparation of pharmaceutical compositions active in the treatment of autoimmune diseases.Type: GrantFiled: October 31, 1990Date of Patent: March 23, 1993Assignee: Farmitalia Carlo Erba SrlInventors: Gianfederico Doria, Anna M. Isetta, Rinaldo Ferreccio, Mario Ferrari, Maria C. Fornasiero, Domenico Trizio
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Patent number: 5179093Abstract: Compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein, R is H, halogen, (C.sub.1 -C.sub.6) alkyl, N(C.sub.1 -C.sub.6 alkyl/aryl).sub.2, OH, O--(C.sub.1 -C.sub.6) alkyl/aryl, CH.sub.2 OH, COOH, COO-alkyl/aryl, SO.sub.2 NH.sub.2, or SO.sub.2 NH (C.sub.1 -C.sub.6 alkyl/aryl);R.sub.1 is C.sub.1 -C.sub.6 alkyl, cycloalkyl, C.sub.2 -C.sub.6 alkenyl, heteroaryl, substituted heteroaryl, heterocycloalkyl, --CH.sub.2 -aryl, --CH.sub.2 -substituted aryl, --CH.sub.2 -heteroaryl, or --CH.sub.2 -substituted heteroaryl;R.sub.2 is H, C.sub.1 -C.sub.6 alkyl or aryl; ##STR2## is an aromatic ring or a heteroaromatic ring; and X is O or N-(alkyl/aryl/alkyl-aryl/alkoxylalkoxyaryl)are described. These compounds are useful as agents for treating viruses.Type: GrantFiled: May 10, 1991Date of Patent: January 12, 1993Assignee: Schering CorporationInventors: Adriano Afonso, Stuart W. McCombie, Jay Weinstein
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Patent number: 5179118Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.2-6 alkoxycarbonyl, nitro, cyano, halogeno, C.sub.1-6 alkylsulfonamindo, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.2-6 alkanoylamino, C.sub.2-6 perfluoroalkanoylamino, C.sub.1-12 mono- or di-alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.6-12 arylsulfonyl, carboxyl, or C.sub.2-12 mono- or di-alkylcarbamoyl; R.sub.2 is hydrogen, C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.2-6 alkoxycarbonyl, nitro, cyano, halogeno, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.2-6 alkanoylamino, C.sub.2-6 perfluoroalkanoylamino, C.sub.1-12 mono- or di-alkylamino, C.sub.1-6 alkylsulfonyl, C.sub.1-12 arylsulfonyl, carboxyl, or C.sub.2-12 mono- or di-alkylcarboamoyl; R.sub.3 and R.sub.4, independent from each other, are C.sub.1-6 alkyl; either R.sub.5 is hydrogen, hydroxyl, C.Type: GrantFiled: May 8, 1992Date of Patent: January 12, 1993Assignee: American Home Products CorporationInventors: John A. Butera, Schuyler A. Antane
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Patent number: 5179112Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: June 6, 1991Date of Patent: January 12, 1993Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5173496Abstract: The invention concerns pharmaceutical compositions containing a 1,2-dihydro-3H-indazol-3-one derivative of the formula I ##STR1## wherein Ra is hydrogen, halogeno, nitro, hydroxy, (2-6C)alkanoyloxy, (1-6C)alkyl, (1-6C)alkoxy, fluoro-(1-4C)alkyl, (2-6C)alkanoyl, amino, (1-6C)alkylamino, di-[(1-4C)alkyl]amino, (2-6C)alkanoylamino or hydroxy-(1-6C)alkyl; Rb is hydrogen, halogeno, (1-6C)alkyl or (1-6C)alkoxy; and Y is a group of the formula --A.sup.1 --X--A.sup.2 --Q in which A.sup.1 is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene, or A.sup.1 is phenylene; X is oxy, thio, sulphinyl, sulphonyl, imino, (1-6C)alkylimino, (1-6C)alkanoylimino, iminocarbonyl or phenylene, or X is a direct link to A.sup.2 ; A.sup.2 is (1-6C)alkylene, (3-6C)alkenylene or (3-6C)alkynylene or A.sup.2 is cyclo(3-6C)alkylene or is a direct link to Q, or the group --A.sup.1 --X--A.sup.2 -- is a direct link to Q; or Y is (2-10)alkyl, (3-10C)alkenyl or (3-6C)alkynyl; and Q is aryl or heteroaryl.Type: GrantFiled: April 2, 1992Date of Patent: December 22, 1992Assignees: ICI Pharma, Imperial Chemical Industries PLCInventors: Pierre A. R. Bruneau, Frank Carey, Christian R. E. Delvare, Keith H. Gibson, Rodger M. McMillan
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Patent number: 5036082Abstract: Nitro-substituted heterocyclic compounds of the formula (I) ##STR1## wherein R is hydrogen or alkyl, Z is an optionally substituted aryl or optionally substituted heterocyclic group containing at least one atom selected from N, O and S,A is optionally substituted ethylene or optionally substituted trimethylene, andB stands for 2 or 3 members of a heterocyclic ring which is formed, together with the adjacent C-atom and N-atom and at least one of said members may represent a hetero atom and may be optionally substituted, provided that when B stands for 3 members, two of which are carbon atoms and the other one is a nitrogen atom which is located in the middle of the three members, then at least one of said two carbon atoms must be substituted by a keto group. Such compounds being useful as insecticides.Type: GrantFiled: April 18, 1990Date of Patent: July 30, 1991Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shoko Sasaki, Koichi Moriya, Yumi Hattori, Katsuhiko Shibuya
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Patent number: 5034398Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein X is CO and Y is NH or O, or X is NH and Y is CO;Z is CH.sub.2, O, S or NR.sub.3 wherein R.sub.3 is hydrogen, C.sub.1-6 alkyl, C.sub.3-7 alkenyl-methyl, phenyl or phenyl C.sub.1-4 alkyl either of which phenyl moieties may be substituted by one or two of halogen, CF.sub.3, C.sub.1-6 alkoxy or C.sub.1-6 alkyl; and R.sub.a is not present; orZ is CH or N and R.sub.a is as defined for R.sub.3 above;R.sub.b is present when X--Y--R.sub.2 is attached at the phenyl ring and is selected from hydrogen, halogen, CF.sub.3, hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl;R.sub.1 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.Type: GrantFiled: October 3, 1989Date of Patent: July 23, 1991Assignee: Beecham Group p.l.c.Inventor: Francis D. King
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Patent number: 4977153Abstract: Compounds of formula (I), ##STR1## characterized in that R signifies optionally substituted heteroaryl-, heteroarylakyl or heteroarylalkenyl, R.sub.1 signifies hydrogen or a substituent, R.sub.2 is hydroxy or a group --z--(CH.sub.2).sub.n --Y--R.sub.3 wherein R.sub.3 is hydrogen, alkyl, hydroxyalkyl, alkenyl, cycloalkyl, cycloalkylalkylene, hydroxy substituted cycloalkyl or cycloalkylalkylene, or optionally substituted aryl or aralkyl or aralkenyl moiety, and Y signifies oxygen or sulfur, and either Z is an oxygen atom and n is 2 or 3, or Z is a bond and n is 1, 2 or 3, A signifies alkylene or branched alkylene of 2 to 5 carbon atoms, W signifies a bond or imino, and X signifies a bond or imino, and their physiologically hydrolyzable derivatives, in which at least one hydroxy group is in esterified form. The compounds exhibit beta adrenoceptor blocking activity. Processes for the preparation of the compounds are also disclosed.Type: GrantFiled: January 14, 1987Date of Patent: December 11, 1990Assignee: William J. LouisInventors: William J. Louis, Richard Berthold, Max-Peter Seiler, Andre Stoll
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Patent number: RE35801Abstract: A prophylactic and therapeutic agent for circulatory disorders, comprising a pyrazolone derivative of the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom, an aryl group, an alkyl group having 1 to 5 carbon atoms or an alkoxycarbonylalkyl group having a total carbon number of 3 to 6; R.sub.2 represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group having 1 to 5 carbon atoms or hydroxyalkyl group having 1 to 3 carbon atoms or R.sub.1 and R.sub.2 taken together represent an alkylene group having 3 to 5 carbon atoms; R.sub.Type: GrantFiled: September 20, 1994Date of Patent: May 19, 1998Assignee: Mitsubishi Chemical CorporationInventors: Hiroyoshi Nishi, Toshiaki Watanabe, Satoshi Yuki, Yasuhiro Morinaka, Katsuhiko Iseki, Hiroko Nakajima (nee Sakurai)