Pteridines (including Hydrogenated) Patents (Class 544/257)
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Publication number: 20040019049Abstract: A variety of low molecular weight, guanidino-containing molecules capable of acting as MC4-R agonists are provided. The compounds are useful in treating MC4-R mediated diseases. The compounds have the structure IA, IB, or IC where the values of the variable are defined herein.Type: ApplicationFiled: May 23, 2003Publication date: January 29, 2004Applicant: CHIRON CORPORATIONInventors: Rustum S. Boyce, Natalia Aurrecoechea, Daniel Chu, Aaron Smith
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Publication number: 20030236255Abstract: Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.Type: ApplicationFiled: May 23, 2003Publication date: December 25, 2003Inventors: Mark Jozef Albert Waer, Piet Andre Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer
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Patent number: 6664043Abstract: The present invention is generally directed to detectable chemiluminescent acridinium ester labels having hydrophilic modifiers; to compositions, complexes and/or conjugates which include such labels; and to processes for performing bioanalytical assays for target analytes which use such labels. Assays for folate, theophylline, and tobramycin (using such labels with hydrophilic modifiers such as nonionic polyethylene glycol and polyionic spermine disulfonate and polyionic spermine dicarboxylate) are described in detail.Type: GrantFiled: July 3, 2001Date of Patent: December 16, 2003Assignee: Bayer CorporationInventors: Anand Natrajan, David Sharpe, Qingping Jiang
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Publication number: 20030225274Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.Type: ApplicationFiled: February 27, 2003Publication date: December 4, 2003Inventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
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Publication number: 20030216402Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: March 7, 2003Publication date: November 20, 2003Inventors: Bernard Gaudilliere, Henry Jacobelli, Catherine Kostlan, Jack Jie Li, Wen-Song Yue
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Publication number: 20030199689Abstract: The present invention relates to compounds of formula I, 1Type: ApplicationFiled: November 21, 2002Publication date: October 23, 2003Inventors: Marc Nazare, Melanie Essrich, David William Will, Hans Matter, Kurt Ritter, Volkmar Wehner
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Patent number: 6617330Abstract: Novel pyrimidine derivatives of formula I as well as possible isomers and mixtures of isomers thereof. The novel compounds have plant-protective properties and are suitable for protecting plants against infestations by phytopathogenic microorganisms and insecticidal attack.Type: GrantFiled: May 4, 2001Date of Patent: September 9, 2003Assignee: Syngenta Participations AGInventor: Harald Walter
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Patent number: 6613772Abstract: Compounds of the formula I in which R1, R2, R3 and Ar have the meanings indicated in the claims, are suitable for the production of pharmaceuticals, for example for the prophylaxis and therapy of cardiovascular diseases such as high blood pressure, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I have the ability to modulate the endogenous production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of disease states which are associated with a disturbed cGMP balance.Type: GrantFiled: June 16, 2000Date of Patent: September 2, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schönafinger, Hartmut Strobel, Peter Schindler
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Publication number: 20030158197Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor.Type: ApplicationFiled: November 8, 2002Publication date: August 21, 2003Applicant: NEUROGEN CORPORATIONInventors: Raymond F. Horvath, Jennifer N. Tran, Stephane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 6593332Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.Type: GrantFiled: July 3, 2002Date of Patent: July 15, 2003Assignee: Pfizer Inc.Inventors: Graham Nigel Maw, David James Rawson
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Publication number: 20030130286Abstract: Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3-7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases.Type: ApplicationFiled: March 6, 2002Publication date: July 10, 2003Inventors: William Alexander Denny, Gordon William Rewcastle, Ellen Dobrusin, James Bernard Kramer, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Peter Laurence Toogood
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Publication number: 20030130278Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: October 11, 2002Publication date: July 10, 2003Inventors: Bernard Gaudilliere, Henri Jacobelli, Joseph Armand Picard, Michael William Wilson
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Patent number: 6586439Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, Het1 and X have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.Type: GrantFiled: July 3, 2002Date of Patent: July 1, 2003Assignee: Pfizer Inc.Inventors: Graham Nigel Maw, David James Rawson
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Publication number: 20030055250Abstract: The invention provides pteridine compounds of formula (I), processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. Formula (I) in which A is a group of formula (a) or (b).Type: ApplicationFiled: August 22, 2002Publication date: March 20, 2003Inventors: Roger Bonnert, Stewart Gardiner, Fraser Hunt, Iain Walters
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Publication number: 20030045716Abstract: The present invention is generally directed to detectable chemiluminescent acridinium ester labels having hydrophilic modifiers; to compositions, complexes and/or conjugates which include such labels; and to processes for performing bioanalytical assays for target analytes which use such labels. Assays for folate, theophylline, and tobramycin (using such labels with hydrophilic modifiers such as nonionic polyethylene glycol and polyionic spermine disulfonate and polyionic spermine dicarboxylate) are described in detail.Type: ApplicationFiled: July 3, 2001Publication date: March 6, 2003Inventors: Anand Natrajan, David Sharpe, Qingping Jiang
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Publication number: 20030040625Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstitutedpropanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: ApplicationFiled: August 29, 2002Publication date: February 27, 2003Inventor: Ibert Clifton Wells
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6514988Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, pplycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.Type: GrantFiled: September 29, 2000Date of Patent: February 4, 2003Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuo Choh, Koichi Kato, Shuji Hinuma
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Patent number: 6506762Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV.Type: GrantFiled: September 29, 2000Date of Patent: January 14, 2003Assignees: Neurogen Corporation, Pfizer Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Publication number: 20030007961Abstract: Orthomolecular Vitamin E derivative compounds, compositions, and their uses for effecting aging and longevity, nerve activity, hematopoiesis and maintenance of blood cells, hepatic activity, nephritic activity, heart and cardiovascular function, pulmonary function, muscular function, cartilage, bone, and joint health, gastrointestinal function, reproductive system function, vision, immune function, cell membrane integrity, and pain and inflammation; preventing or treating diseases or conditions; treating cancers or obesity; and reducing the risk of Sudden Infant Death Syndrome in an animal.Type: ApplicationFiled: June 22, 2001Publication date: January 9, 2003Inventor: Michael D. Wilburn
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Publication number: 20030004165Abstract: The present invention relates to an inhibitor of matrix metalloprotease (MMP) production and tumor necrosis factor (TNF) production, and medicines for the treatment of diseases such as chronic rheumatoid arthritis, osteoarthritis, allergic diseases, psoriasis, transplant rejection, arterial sclerosis, ischemic re-perfusion disorder, diabetic nephritic and ocular diseases, cancer, autoimmune glomerulonephritis, infectious diseases, Crohn's disease, inflammatory intestinal diseases and autoimmune hepatitis, each comprising certain polyazanaphthalene compounds or pharmaceutically acceptable salts thereof as active ingredients.Type: ApplicationFiled: May 2, 2002Publication date: January 2, 2003Applicant: AJINOMOTO CO. INCInventors: Yukio Iino, Toshihiro Hatanaka, Yuko Satake, Kenji Takehana, Akiko Oonuki, Tsuyoshi Kobayashi
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Publication number: 20020193377Abstract: A compound selected from those of formula (I): 1Type: ApplicationFiled: February 13, 2002Publication date: December 19, 2002Inventors: Charles Andrianjara, Nicole Chantel Barvian, Bernard Gaudilliere, Henri Jacobelli, Daniel Fred Ortwine, William Chester Patt, Ly Pham, Catherine Rose Kostlan, Michael William Wilson
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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
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Patent number: 6458950Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):Type: GrantFiled: August 3, 2000Date of Patent: October 1, 2002Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Publication number: 20020115855Abstract: The instant invention discloses a process for the preparation of compounds of formula I 1Type: ApplicationFiled: July 5, 2001Publication date: August 22, 2002Inventors: Michele Gerster, Paul Dubs
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Publication number: 20020111355Abstract: This invention provides compounds of the formula: 1Type: ApplicationFiled: January 16, 2002Publication date: August 15, 2002Applicant: American Home Products CorporationInventors: Puwen Zhang, Arthur A. Santilli, Andrew Fensome, Eugene A. Terefenko, Andrew Q. Viet, Jay E. Wrobel, James P. Edwards, Todd K. Jones, Christopher M. Tegley, Lin Zhi
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Patent number: 6423716Abstract: The present invention relates to nitrogen-containing heterocyclic compounds represented by formula (I): wherein W represents 1,4-piperazinediyl, etc.; U represents NR1R2 (wherein R1 represents a hydrogen atom, a substituted or unsubstituted alkyl group, etc.; and R2 represents a hydrogen atom, etc. ), OR4, or SR5; V represents an oxygen atom, a sulfur atom, N—R6, or CR7R8, at least one of X, Y and Z represents a nitrogen atom, and the others are the same or different, and each represents a nitrogen atom or C—RA; and D1, D2, D3 and D4 each independently represent C—RB, a nitrogen atom, an oxygen atom, a sulfur atom, etc., optional adjoining two among D1 to D4 are combined to represent a nitrogen atom, N—R2A, an oxygen atom, a sulfur atom, etc.Type: GrantFiled: September 29, 2000Date of Patent: July 23, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Kenji Matsuno, Yuji Nomoto, Michio Ichimura, Shin-ichi Ide, Shoji Oda
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Patent number: 6423718Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.Type: GrantFiled: August 2, 2000Date of Patent: July 23, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Jeffrey W. Corbett, Soo S. Ko
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Patent number: 6417358Abstract: Process for the preparation of compounds of formula (I), wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula (V), wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.Type: GrantFiled: December 22, 2000Date of Patent: July 9, 2002Assignee: Ciba Specialty Chemicals CorporationInventors: Michael Tinkl, Samuel Evans, Peter Nesvadba
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Publication number: 20020086866Abstract: This invention discloses quinoxalinones which display inhibitory effects on serine proteases such as factor Xa, thrombin, and/or factor VIIa. The invention also discloses pharmaceutically acceptable salts and prodrugs of the compounds, pharmaceutically acceptable compositions comprising the compounds, their salts or prodrugs, and methods of using them as therapeutic agents for treating or preventing disease states in mammals characterized by abnormal thrombosis.Type: ApplicationFiled: January 4, 2002Publication date: July 4, 2002Inventors: Danette Andrea Dudley, Jeremy John Edmunds
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Patent number: 6399609Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: May 11, 2000Date of Patent: June 4, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventor: Richard Gerald Wilde
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Publication number: 20020052368Abstract: Novel compounds of formula I: 1Type: ApplicationFiled: March 26, 2001Publication date: May 2, 2002Inventors: Charles K. Marlowe, Kim A. Kane-Maguire, Bing-Yan Zhu, Robert M. Scarborough
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Publication number: 20020032202Abstract: Described is a heterocycle-containing carboxylic acid derivative represented by the following formula (I): 1Type: ApplicationFiled: July 23, 2001Publication date: March 14, 2002Applicant: Eisai Co. Ltd.Inventors: Kouichi Kikuchi, Katsuya Tagami, Hiroyuki Yoshimura, Shigeki Hibi, Mitsuo Nagai, Shinya Abe, Makoto Okita, Takayuki Hida, Seiko Higashi, Naoki Tokuhara, Seiichi Kobayashi
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Publication number: 20020019395Abstract: Novel compounds of general formula I: 1Type: ApplicationFiled: February 1, 2001Publication date: February 14, 2002Inventors: Bing-Yan Zhu, Robert M. Scarborough
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Patent number: 6323201Abstract: Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-&agr; and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses in stimuli in vivo (particularly TN-&agr;) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression. Compounds having enhanced water solubility are also described.Type: GrantFiled: May 19, 1997Date of Patent: November 27, 2001Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Howard Cottam
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Patent number: 6277849Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and isomeric mixtures 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-C8acycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C8alkenyloxycarbonyl, C1-C5alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl: C2-C12alknyl; C1-C12haloalkyl or a group NR11R12; wherein R11, and R12 are each independently of the other hydrogen, C1-C6alkyl 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 C1C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8acycloalkyl-C1-C4alkyl or wherein 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 eacType: GrantFiled: August 24, 1999Date of Patent: August 21, 2001Assignee: Syngenta Crop Protection, Inc.Inventor: Martin Zeller
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Patent number: 6271231Abstract: The present invention provides optionally substituted and/or annulated compounds of formula (I) wherein X, Y, Z and A is each independently carbon or nitrogen, and at least two of X, Y, Z and A are carbon; and pharmaceutically acceptable salts thereof with the proviso that: 3-(1H-Indol-3-yl)-1H-quinoxalin-2-one, 3-(2-Methyl-1H-indol-3-yl)-1H-quinoxalin-2-one, and 3-(1,2-Diphenyl-1H-indol-3-yl)-1H-quinoxalin-2-one are excluded from compounds of formula (I). The invention includes the use of compounds of formula (I) in medical therapy, particularly in the therapy of conditions requiring inhibition of protein kinase C.Type: GrantFiled: December 18, 1997Date of Patent: August 7, 2001Assignee: Astra AktiebolagInventors: Håkan Bergstrand, Kostas Karabelas, Peter Sjö
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Patent number: 6187788Abstract: A gonadotropin-releasing hormone antagonistic composition, which comprises an optionally substituted condensed-bicyclic compound consisting of a homo or hetero 5 to 7 membered ring and a homo or hetero 5 to 7 membered ring is effective as a propylactic or therapeutic agent for the prevention or treatment of several hormone dependent diseases, for example, a sex hormone dependent cancer (e.g. prostatic cancer, cancer of uterine cervix, breast cancer, pituitary adenoma), benign prostatic hypertrophy, myoma of the uterus, endometriosis, precocious puberty, amenorrhea, premenstrual syndrome, polycystic ovary syndrome and acne vulgaris; is effective as a fertility controlling agent in both sexes (e.g.Type: GrantFiled: October 1, 1998Date of Patent: February 13, 2001Assignee: Takeda Chemical Industries, Ltd.Inventors: Shuichi Furuya, Nobuo Choh, Koichi Kato, Shuji Hinuma
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Patent number: 6166019Abstract: Compounds of Formula I and II and their pharmaceutically acceptable, salts, esters and prodrugs thereof are selective alpha-1D adrenoceptor anatagonists and may be useful for treating disease states.Type: GrantFiled: July 9, 1999Date of Patent: December 26, 2000Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, William A. Caroll
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Patent number: 6124302Abstract: The present invention relates to 4,4-disubstituted-3,4-dihydro-2(1H)-quinazolinones of formula I: ##STR1## or steroisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent, wherein:R.sup.1 is C.sub.1-3 alkyl substituted with 1-7 halogen;R.sup.2 is optionally substituted C.sub.1-5 alkyl, optionally substituted C.sub.2-5 alkenyl, or optionally substituted C.sub.2-5 alkynyl;R.sup.3, at each occurrence, is independently selected from C.sub.1-4 alkyl, OH, C.sub.1-4 alkoxy, F, Cl, Br, I, NR.sup.5 R.sup.5a, NO.sub.2, CN, C(O)R.sup.6, NHC(O)R.sup.7, and NHC(O)NR.sup.5 R.sup.5a ;R.sup.5 and R.sup.5a are independently selected from H and C.sub.1-3 alkyl;R.sup.6 is selected from H, OH, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, and NR.sup.5 R.sup.5a ;R.sup.Type: GrantFiled: April 8, 1998Date of Patent: September 26, 2000Assignee: DuPont PharmaceuticalsInventors: Jeffrey W. Corbett, Soo S. Ko
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Patent number: 6083948Abstract: Corticotropin releasing factor (CRF) antagonists of formula I: and their use in treating anxiety, depression, and other psychiatric and neurological disorders are disclosed.Type: GrantFiled: May 16, 1997Date of Patent: July 4, 2000Assignee: Dupont Pharmaceuticals CompanyInventor: Richard Gerald Wilde
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Patent number: 6066638Abstract: Compounds of Formula I, and their N-oxides and agriculturally suitable salts, are disclosed which are useful as fungicides ##STR1## wherein W is O, S(O).sub.n or NR.sup.5 ;n is 0, 1 or 2;Q is O or S;G is a fused phenyl, naphthalene, thiophene, furan, pyrrole, pyridine, thiazole, oxazole, imidazole, pyrazine, pyridazine or pyrimidine ring; andR.sup.1 -R.sup.5 are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula I and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula I.Type: GrantFiled: January 2, 1998Date of Patent: May 23, 2000Assignee: E. I. du Pont de Nemours and CompanyInventors: James Francis Bereznak, Zen-Yu Chang, Charlene Gross Sternberg
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Patent number: 6046207Abstract: The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 adrenoreceptors and treating BPH.Type: GrantFiled: November 26, 1997Date of Patent: April 4, 2000Inventors: Michael D. Meyer, Robert J. Altenbach, Fatima Z. Basha, William A. Carroll, Irene Drizin, James F. Kerwin, Jr., Michael D. Wendt, Anthony R. Haight, Weijiang Zhang
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Patent number: 6004966Abstract: The use of a compound of formula I ##STR1## in which R.sub.1 and R.sub.2 are N, X.sub.1 and X.sub.2 which may be the same or different are hydrogen, hydroxy, or an optionally substituted alkyl, and Z.sub.1 and Z.sub.2 which may be the same or different are hydrogen, hydroxy, keto (.dbd.O), or one of Z.sub.1 and X.sub.1 and Z.sub.2 and X.sub.2 form a second bond of a double bond at the 1,6 or 2,3 positions with the proviso that at least one of the groupings R.sub.1 Z.sub.1 X.sub.1 R.sub.2 Z.sub.2 X.sub.2 and R.sub.1 X.sub.1 Z.sub.2 form a hydroxamate moiety (--N(OH)C(.dbd.O)-- in which R.sub.1 and R.sub.2 is N, Z.sub.1 and/or Z.sub.2 is .dbd.O and X.sub.1 and/or X.sub.2 is OH or R.sub.1 is N, Z.sub.2 is .dbd.O and X.sub.1 is OH and B is a 5 or 6 membered ring of formula II or III ##STR2## in which R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.Type: GrantFiled: June 9, 1997Date of Patent: December 21, 1999Assignee: BTG International LimitedInventors: Surinder Singh, Anthony Edward Lewis
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Patent number: 5998616Abstract: The present invention provides a general biocatalyst for transforming saturated carbonyl compounds to their .alpha.,.beta.-unsaturated analogs. The transformation is regio- as well as stereoselective. These catalysts are useful in the chiral resolution of carbonyl compounds as well as in the development of libraries of small molecules to screen as potential drug candidates.Type: GrantFiled: August 25, 1997Date of Patent: December 7, 1999Assignee: The University of MichiganInventors: Yerramilli V. S. N. Murthy, Vincent Massey
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Patent number: 5889012Abstract: Substituted cycloalkylamino and cycloalkoxy heterocycles, processes for preparing them and their use as pesticides The invention relates to (I) ##STR1## in which R.sup.1 to R.sup.5, A, X, E, U, p and n are as defined in claim 1, to processes for their preparation and their use as pesticides, such as insecticides, acaricides and fungicides.Type: GrantFiled: October 16, 1995Date of Patent: March 30, 1999Assignee: Hoechst-Schering AgrEvo GmbHInventors: Martin Markl, Wolfgang Schaper, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin, Adolf Linkies, Dieter Bernd Reuschling
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Patent number: 5874433Abstract: Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock).Type: GrantFiled: December 19, 1995Date of Patent: February 23, 1999Assignee: Cornell Research Foundation, Inc.Inventor: Steven S. Gross
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Patent number: 5869665Abstract: Novel quinazolinone derivatives with good binding affinity for the CCK-A and CCK-B receptors, pharmaceutical compositions containing them, methods of using them and a novel process for their preparation are taught. The compounds are useful agents to suppress appetite, reduce gastric acid secretion, and the like.Type: GrantFiled: April 8, 1997Date of Patent: February 9, 1999Assignee: Warner-Lambert CompanyInventor: Janak Khimchand Padia
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Patent number: 5843943Abstract: Novel, heterocyclic compounds having at least one ring nitrogen, disclosed side chains and, in some embodiments, an oxygen ortho to the ring nitrogen inhibit inflammatory responses associated with TNF-.alpha. and fibroblast proliferation in vivo and in vitro. The compounds of the invention neither appreciably inhibit the activity of cAMP phosphodiesterase nor the hydrolysis of phosphatidic acid, and are neither cytotoxic nor cytostatic. Preferred compounds of the invention are esters. Methods for the use of the novel compounds to inhibit ceramide-mediated intracellular responses to stimuli in vivo (particularly TNF-.alpha.) are also described. The methods are expected to be of use in reducing inflammatory responses (for example, after angioplasty), in limiting fibrosis (for example, of the liver in cirrhosis), in inhibiting cell senescence, cell apoptosis and UV induced cutaneous immune suppression.Type: GrantFiled: June 7, 1995Date of Patent: December 1, 1998Assignee: The Regents of the University of CaliforniaInventors: Dennis A. Carson, Howard B. Cottam, D. Bruce Wasson
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Patent number: 5837703Abstract: Therapeutic compounds have the formula:(X)j-(core moiety),j being an integer from one to three, the core moiety comprising a core moiety, the core moiety being a heterocycle having one ring or two-fused rings, each ring having five or six ring atoms, A being a carbon atom of the core moiety and attached to a terminal carbon atom of (CH.sub.2).sub.m, and X has a structure and X being a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkyl or alkenyl of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.Type: GrantFiled: November 12, 1993Date of Patent: November 17, 1998Assignee: Cell Therapeutics, Inc.Inventors: Anil M. Kumar, John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice