Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Five- Membered Hetero Ring Patents (Class 546/278.1)
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Publication number: 20020161025Abstract: The invention relates to novel N-substituted indole-3-glyoxylamides, to processes for their preparation and to their pharmaceutical use. The compounds have antiasthmatic, antiallergic and immunosuppressant/immunomodulating actions.Type: ApplicationFiled: January 30, 2002Publication date: October 31, 2002Inventors: Guillaume Lebaut, Cecilia Menciu, Bernhard Kutscher, Peter Emig, Stefan Szelenyi, Kay Brune
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Publication number: 20020151718Abstract: A method for preparing particular pyrrole-carboxamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloalkanediones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.Type: ApplicationFiled: December 3, 2001Publication date: October 17, 2002Applicant: Pfizer Inc.Inventor: John A. Ragan
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Patent number: 6417214Abstract: This invention provides compounds of the formula 1: wherein: R1 and R2 are chosen independently from each other from H, OH; OAc; alkylaryl; alkylheteroaryl; 1-propynyl; 3-propynyl; and optionally substituted alkyl, O(alkyl); aryl; or heteroaryl groups; or R1 and R2 are joined to form a ring comprising —CH2(CH2)nCH2— where n=0-5; —CH2CH2CMe2CH2CH2—; —O(CH2)mCH2— where m=1-4; O(CH2)pO— where p=1-4; —CH2CH2OCH2CH2—; —CH2CH2N(H or alkyl)CH2CH2—; or R1 and R2 together comprise a double bond to CMe2; C(cycloalkyl), O, or C(cycloether); R3 is H, OH, NH2, CORA, or optionally substituted alkenyl or alkynyl groups; RA=H or optionally substituted alkyl, alkoxy, or aminoalkyl groups; R4=H, halo, CN, NH2, or optionally substituted alkyl, alkoxy, or aminoalkyl; R5 is selected from optionally substituted benzene ring; a five or six membered heterocyclic ring; a 4 or 7-substituted indole or a substitutType: GrantFiled: April 19, 2000Date of Patent: July 9, 2002Assignees: Wyeth, Ligand Pharmaceuticals, Inc.Inventors: John W. Ullrich, Andrew Fensome, Jay E. Wrobel, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley
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Patent number: 6353109Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R3 and R4 represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 1, 1998Date of Patent: March 5, 2002Assignee: Neurogen CorporationInventors: Pamela Albaugh, Gang Liu, Alan Hutchison
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Patent number: 6329523Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: March 10, 1999Date of Patent: December 11, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An
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Patent number: 6323228Abstract: 3-Substituted indole carbohydrazides having the formula are useful for inhibiting angiogenesis. Also disclosed are angiogenesis-inhibiting compositions and methods of inhibiting angiogenesis in a mammal.Type: GrantFiled: September 15, 2000Date of Patent: November 27, 2001Assignee: Abbott LaboratoriesInventors: Nwe Y. BaMaung, Richard A. Craig, Megumi Kawai, Jieyi Wang
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Publication number: 20010039286Abstract: The present invention relates compounds of the formula (I): 1Type: ApplicationFiled: February 13, 2001Publication date: November 8, 2001Inventors: Kevin Dinnell, Jason Matthew Elliott, Gregory John Hollingworth, Mark Peter Ridgill, Duncan Edward Shaw
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Patent number: 6306852Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 oType: GrantFiled: April 24, 2000Date of Patent: October 23, 2001Assignee: Pfizer Inc.Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
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Patent number: 6303600Abstract: This invention is directed to certain physiologically active compounds of formula (I) wherein represents a bicyclic ring system, of about 10 to about 13 ring members, in which the ring is an azaheterocycle, and the ring represents an azaheteroaryl ring, or an optionally halo substituted benzene ring; and N-oxides thereof, and their prodrugs, and pharmaceutically acceptable salts and solvates of the compounds of formula (I) and N-oxides thereof, and their prodrugs. Such compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: December 18, 1998Date of Patent: October 16, 2001Assignee: Rhone-Poulenc Rorer LimitedInventors: Paul Joseph Cox, David John Aldous, Daniel Gerard McGarry, Christopher Hulme, John Robinson Regan, Fu-Chih Huang, Stevan Wakefield Djuric, Kevin Joseph Moriarty, Rose Mappilakunnel Mathew, Gregory Bernard Poli
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Publication number: 20010029299Abstract: Disclosed are compounds of the formula: 1Type: ApplicationFiled: March 8, 2001Publication date: October 11, 2001Applicant: NeurogenInventors: Pamela Albaugh, Gang Liu, Kenneth Shaw, Alan Hutchison
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Publication number: 20010020035Abstract: Disclosed are compounds of the formula 1Type: ApplicationFiled: June 1, 1998Publication date: September 6, 2001Inventors: PAMELA ALBAUGH, GANG LIU, ALAN HUTCHISON
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Patent number: 6277878Abstract: This invention provides a compound of the following formula: or the pharmaceutically acceptable salts thereof wherein R1 is H or C1-4 alkyl; R2 is C(═L′)R3 or So2R4; Y is a direct bond or C1-4 alkylene; L and L′ are independently oxygen or sulfur; Q is selected from the following: C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted C3-7 cycloalkyl, optionally substituted phenyl or naphthyl, optionally substituted 5 or 6-membered monocyclic aromatic group; R3 is —OR6, —NR7R8, N(OR1)R7 or a group of formula: Z is a direct bond, O, S or NR5; R4 is C1-6 alkyl, halo-substituted C1-4 alkyl, optionally substituted phenyl or naphthyl; R5 is C1-4 alkyl or halo-substituted C1-4 alkyl; R6 is C1-4 alkyl C3-7 cycloalkyl, C1-4 alkyl-C3-7 cycloalkyl, halo-substituted C1-4 alkyl, optionally substituted C1-4 alkyl-phenyl or phenyl; R7 and R8 are each selected from the following: H, optionally substituted C1-6 alkyl, optionally substituted C3-7 cycloType: GrantFiled: August 26, 1999Date of Patent: August 21, 2001Assignee: Pfizer IncInventors: Kazunari Nakao, Rodney W. Stevens, Kiyoshi Kawamura, Chikara Uchida
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Patent number: 6262272Abstract: A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakane-diones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.Type: GrantFiled: January 19, 1999Date of Patent: July 17, 2001Assignee: Pfizer IncInventors: John Anthony Ragan, Teresa Woodall Makowski, David Jon Am Ende, Pamela Jane Clifford, Gregory Randall Young, Alyson Kay Conrad, Shane Allen Eisenbeis, George Joseph Quallich, Douglas John Meldrum Allen
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Patent number: 6251923Abstract: The invention relates to new hydroxyindoles of the Formula, their use as inhibitors of phosphodiesterase 4 and processes for their preparation.Type: GrantFiled: April 28, 1999Date of Patent: June 26, 2001Assignee: Arzneimittelwerk Dresden GmbHInventors: Norbert Höfgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelényi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Patent number: 6248743Abstract: A novel butadiene derivative of the formula: wherein Ring A is heterocycle, or benzene being optionally substituted by lower alkyl, alkoxy, nitro, hydroxy, substituted or unsubstituted amino or halogen, Ring B is heterocycle, or benzene being optionally substituted by lower alkoxy, lower alkylenedioxy or di-lower alkylamino, R1 and R2 are each H or lower alkyl, one of —COR32 and —COR42 is carboxyl, and the other is carboxyl being optionally esterified, or the corresponding amide or pyrrolidine derivatives, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 28, 1998Date of Patent: June 19, 2001Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Hiroshi Ohmizu, Akio Ohtani, Tsuyoshi Ohgiku, Hiroshi Sai, Jun Murakami
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Patent number: 6232327Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents and to a pharmaceutical composition having antitumor action, characterized in that it contains at least one of the compounds of the general formula 1, if appropriate also in the form of the physiologically tolerable acid addition salts or N-oxides. Furthermore, the invention also includes antitumor agents comprising as active compound one or more N-substituted indole-3-glyoxylamides according to the general formula 1 and, if appropriate, their physiologically tolerable acid addition salts and, if possible, N-oxides and a pharmaceutically utilizable carrier and/or diluent or auxiliary substance in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments.Type: GrantFiled: April 2, 1999Date of Patent: May 15, 2001Assignee: Asta Medica AktiengesellschaftInventors: Bernd Nickel, Istvan Szelenyi, Jürgen Schmidt, Peter Emig, Dietmar Reichert, Eckhard Günther, Kay Brune
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Patent number: 6197965Abstract: Novel compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: May 17, 1999Date of Patent: March 6, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: P. Dan Cook, Haoyun An