Nitrogen Attached Directly To The Five-membered Hetero Ring By Nonionic Bonding (e.g., 2-amino Indoles, Etc.) Patents (Class 548/483)
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Patent number: 6586459Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: July 1, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20030119793Abstract: The present invention relates to compounds useful as inhibitors of CAK, compositions thereof. The present invention also relates to methods using the compositions for treating CAK-mediated diseases, such as fungal infections.Type: ApplicationFiled: June 6, 2002Publication date: June 26, 2003Inventors: Brian Ledford, Cameron Stuver Moody, Michael Mullican, Mark Namchuk
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Patent number: 6583145Abstract: This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: wherein: R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.Type: GrantFiled: September 24, 2002Date of Patent: June 24, 2003Assignees: Wyeth, Ligand PharmaceuticalsInventors: Andrew Fensome, Puwen Zhang, Marci C. Koko, Lin Zhi, Todd K. Jones, Jay E. Wrobel, Christopher M. Tegley, James P. Edwards, Edward G. Melenski
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Patent number: 6583173Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: June 24, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffrey Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20030083333Abstract: Disclosed are novel 1,4-disubstituted benzo-fused compounds wherein G, X, L, Q, n and Y are defined herein. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are processes of making such compounds.Type: ApplicationFiled: April 10, 2002Publication date: May 1, 2003Inventors: Pier Francesco Cirillo, Daniel R. Goldberg, Abdelhakim Hammach, Neil Moss, Kristen Mueller, John Robinson Regan
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Publication number: 20030078422Abstract: Process for the preparation of benzo-fused heterocycles of general formula I: 1Type: ApplicationFiled: October 9, 2002Publication date: April 24, 2003Inventors: Frank-Hardi Wartenberg, Thomas Koppe, Walter Wetzel, Markus Wydra, Achim Benz
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Patent number: 6545152Abstract: 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: GrantFiled: July 18, 2000Date of Patent: April 8, 2003Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Taracad K. Venkatachalam
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Patent number: 6541503Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by caType: GrantFiled: August 8, 2001Date of Patent: April 1, 2003Assignee: SmithKline Beecham CorporationInventors: Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Patent number: 6534535Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds of formula (I) below: are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: GrantFiled: August 10, 2000Date of Patent: March 18, 2003Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Robert M. Scarborough, Lane Clizbe, Brandon Doughan, Zhaozhong Jon Jia, Kim Kane-Maguire, Charles Marlowe, Yonghong Song, Ting Su, Willy Teng, Penglie Zhang
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Patent number: 6518291Abstract: The present invention relates to a novel class of compounds which are IMPDH inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting IMPDH enzyme activity and consequently, may be advantageously used as therapeutic agents for IMPDH mediated processes. This invention also relates to methods for inhibiting the activity of IMPDH using the compounds of this invention and related compounds.Type: GrantFiled: September 14, 1999Date of Patent: February 11, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Jeffrey O. Saunders, David M. Armistead, Michael C. Badia, Randy S. Bethiel, Catherine A. Frank, Doug Naegele, Perry M. Novak, David A. Pearlman, Steven M. Ronkin
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Patent number: 6512125Abstract: The synthesis of memory enhancing, analgetic, and antidepressant N-alkyl-N-pyridinyl-1H-indol-1-armines is described.Type: GrantFiled: May 31, 1995Date of Patent: January 28, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: Thomas B. Lee, Keith E. Goehring
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Publication number: 20030018053Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: ApplicationFiled: June 28, 2002Publication date: January 23, 2003Applicant: The Institute for Pharmaceutical Discovery LLC.Inventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
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Patent number: 6509369Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: January 8, 2002Date of Patent: January 21, 2003Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Publication number: 20030004308Abstract: Compounds of the formula 1Type: ApplicationFiled: April 29, 2002Publication date: January 2, 2003Inventors: Hans-Joachim Bohm, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Hans Wolfgang Hoffken, Wilfried Hornberger
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Patent number: 6500854Abstract: A chondrogenesis promoter comprising as an active ingredient a compound represented by general formula (I) or a salt thereof: wherein R1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, etc.; R2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group, an acyl group, an aryl group, a heterocyclic group, etc.; R1 represents a lower alkyl group, a cycloalkyl group, an aryl group, a heterocyclic group, etc.; R4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, etc.; X and Y represent —CH2—, —NH—or —O—; and n represents an integer of 0-4.Type: GrantFiled: September 21, 2001Date of Patent: December 31, 2002Assignee: Chugai Sei Yaku Kabushiki KaishaInventors: Hidetomo Kitamura, Atsuhiko Kato, Toru Esaki
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Patent number: 6500855Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.Type: GrantFiled: January 2, 2002Date of Patent: December 31, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. S. Lam, Charles G. Clark, Renhau Li, Donald J. P. Pinto
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Publication number: 20020198253Abstract: The invention concerns melatonin derivatives of formula (I) wherein: R1 represents H, a C1-C4 alkyl group or a C1-C4 alkoxy group; R2 represents H or a C1-C4 alkyl group; R3 represents H, methyl or a halogen atom; R4, R5 represent individually H or a halogen atom; R6 represents H or a C1-C4 alkyl group, or a pharmaceutically acceptable salt thereof. The invention also concerns a medicine comprising said derivatives.Type: ApplicationFiled: July 3, 2002Publication date: December 26, 2002Applicant: Centre National de la Recherche Scientifique (CNRS)Inventors: Claire Ducrocq, Beatric Blanchard
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Patent number: 6498176Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, D, X, Y and Z have the meaning as defined in the claims exhibit protein tyrosine kinase and protein serin/threonine kinase inhibitory activity.Type: GrantFiled: August 22, 2001Date of Patent: December 24, 2002Assignee: SmithKlineBeecham CorporationInventors: Karen Elizabeth Lackey, Robert Walton McNutt, Jr.
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Publication number: 20020193415Abstract: The invention as disclosed herein is a method and composition for the treatment of HIV in humans and other host animals, that includes the administration of an effective HIV treatment amount of a phenylindole as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier. The compounds of this invention either possess antiviral (i.e., anti-HIV) activity, or are metabolized to a compound that exhibits such activity.Type: ApplicationFiled: April 11, 2002Publication date: December 19, 2002Inventors: Paulo LaColla, Marino Artico, Jean-Pierre Sommadossi
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6451839Abstract: A class of novel indole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock.Type: GrantFiled: January 30, 2001Date of Patent: September 17, 2002Assignee: Eli Lilly and CompanyInventors: Nicholas James Bach, Robert Delane Dillard, Susan Elizabeth Draheim, Edward David Mihelich, Tulio Suarez
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Publication number: 20020128490Abstract: The present invention provides methodology for carbon-nitrogen bond formation via vinyl or aryl amination. In the process of the invention, an sp2 hybridized radical is reacted with an azomethine moiety to form pyrrolidine and indole compounds. The methodology provides a facile process for the synthesis of compounds having the pyrrolidine or indole subunit and is especially advantageous for compounds having acid or base labile functional groups andor is comprised of chiral centers susceptible to acidbase epimerization.Type: ApplicationFiled: March 7, 2001Publication date: September 12, 2002Inventors: Jeffrey N. Johnston, Rajesh Viswanathan
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Publication number: 20020128481Abstract: This invention involves compounds having the following structure: 1Type: ApplicationFiled: February 8, 2002Publication date: September 12, 2002Inventors: Thomas Lee Cupps, Sophie Eva Bogdan, Raymond Todd Henry, Russell James Sheldon, William Lee Seibel, Jeffrey Joseph Ares
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Patent number: 6436984Abstract: The invention concerns melatonin derivatives of formula (I) wherein: R1 represents H, a C1-C4 alkyl group or a C1-C4 alkoxy group; R2 represents H or a C1-C4 alkyl group; R3 represents H, methyl or a halogen atom; R4, R5 represent individually H or a halogen atom; R6 represents H or a C1-C4 alkyl group, or a pharmaceutically acceptable salt thereof. The invention also concerns a medicine comprising said derivatives.Type: GrantFiled: August 29, 2001Date of Patent: August 20, 2002Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Claire Ducrocq, Béatrice Blanchard
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Patent number: 6414008Abstract: New disubstituted bicyclic heterocycles of general formula Ra—A—Het—B—Ar—E (I) Compounds of general formula I, wherein E is an RbNH—C(═NH)— group, have valuable pharmacological properties, particularly a thrombin-inhibiting effect and the effect of prolonging thrombin time, and those wherein E is a cyano group, are valuable intermediates for preparing the other compounds of general formula I.Type: GrantFiled: October 13, 2000Date of Patent: July 2, 2002Assignee: Boehringer Ingelheim Pharma KGInventors: Norbert Hauel, Henning Priepke, Uwe Ries, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6410558Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula wherein Z1 and Z2 are C or N and are part of an aromatic ring selected from benzene, pyridine, thiophene, furan, pyrrole, pyrazole, thiazole, and isothiazole; A is selected from —C(X)-amine, —C(O)—SR3, —NH—C(X)R4, and —C(═NR3)—XR7; B is —Wm—Q(R2)3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R4; Q is C, Si, Ge, or Sn; W is —C(R3)pH(2−p)—; or when Q is C, W is selected from —C(R3)pH(2−p)—, —N(R3)mH(1−m)—, —S(O)p—, and —O—; X is O or S; n is 0, 1, 2, or 3; m is 0 or 1; p is 0, 1, or 2; each R is independently selected from a) halo, formyl, cyano, amino, nitro, thiocyanato, isothiocyanato, trimethylsilyl, and hydroxy; b) C1-C4 alkyl, alkenyl, alkynyl,Type: GrantFiled: November 27, 2000Date of Patent: June 25, 2002Assignee: Monsanto Technology LLCInventors: Dennis Paul Phillion, Diane Susan Braccolino, Matthew James Graneto, Wendell Gary Phillips, Karey Alan Van Sant, Daniel Mark Walker, Sai Chi Wong
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Patent number: 6407247Abstract: A method of using compounds of formula I in which the C═C double bond is present in E and/or Z configuration and the variables have the following meanings: R1 denotes COOR5, COR5, CONR5R6, CN, O═S(—R5)═O, O═S(═OR5)═O, R7O—P(—OR8)═O; R2 denotes COOR6, COR6, CONR5R6, CN, O═S(—R6)═O, O═S(═OR6)═O, R7O—P(—OR8)═O; R3 denotes hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms; R4 denotes an optionally substituted aromatic or heteroaromatic radical containing from 5 to 12 ring atoms; R5 to R8 independently denote hydrogen, an open-chain or branched-chain aliphatic, araliphatic, cycloaliphatic or optionally substituted aromatic radical containing in each case up to 18 carbon atoms, where the variables R3 to R8 may also form, together with the carbon atoms to which they are attached, a 5-membered or 6-memberedType: GrantFiled: January 31, 2000Date of Patent: June 18, 2002Assignee: BASF AktiengesellschaftInventors: Thorsten Habeck, Alexander Aumüller, Volker Schehlmann, Horst Westenfelder, Thomas Wünsch
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Publication number: 20020068756Abstract: Compounds represented by formula I: 1Type: ApplicationFiled: March 1, 2001Publication date: June 6, 2002Inventors: Marc Labelle, Claudio Sturino, Nicolas Lachance, Dwight Macdonald
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Patent number: 6380238Abstract: For use in therapy a chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, heterocyclyl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, wherein at least one of R4 to R7 is a substituent group other than hydrogen, and pharmaceutically acceptable salts and prodrugs thereof, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and especially for the treatment of obesitType: GrantFiled: March 1, 2001Date of Patent: April 30, 2002Assignee: Vernalis Research LimitedInventors: David Reginald Adams, Jonathan Mark Bentley, Jonathan Richard Anthony Roffey, Richard John Hamlyn, Suneel Gaur, Matthew Alexander James Duncton, David Bebbington, Nathaniel Julius Monck, Claire Elizabeth Dawson, Robert Mark Pratt, Ashley Roger George
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Patent number: 6372779Abstract: This invention relates to anti-inflammatory compounds, methods of making such compounds and methods of using such compounds having the following structure:Type: GrantFiled: December 28, 1998Date of Patent: April 16, 2002Assignee: Ortho Pharmaceutical CorporationInventors: Malcolm K. Scott, Pauline J. Sanfilippo, Louis J. Fitzpatrick, III, Richard Cordova, Kevin Pan, Joseph Meschino
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Patent number: 6350754Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: January 12, 2000Date of Patent: February 26, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Publication number: 20020006936Abstract: The present invention provides compounds of Formula I 1Type: ApplicationFiled: July 23, 2001Publication date: January 17, 2002Inventors: Jack Bikker, Ellen Myra Dobrusin, Annette Marian Doherty, Matthew Drowns, James Stanley Kaltenbronn, Juergen Kleinschroth, Dennis Joseph McNamara, John Quin, Joseph Thomas Repine, Marcin Stasiak
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Patent number: 6337344Abstract: The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.Type: GrantFiled: August 14, 2000Date of Patent: January 8, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose, Hans Matter
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Patent number: 6326501Abstract: A process for manufacturing a methylated indole compounds of the formula: where R1 is selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkenyl, —OCH3, —NO2, —CHO, —CO2CH3, and —CN, and R2 is selected from the group consisting of C1-C6 alkyl, —CO2CH3, —CN, —CHO, —NH2, —N(C1-C6 alkyl)2, —(CH2)nCOOH, and —(CH2)nCN, where n is an integer from 1 to 4, inclusive, involves reacting a compound of the formula: with dimethyl carbonate in the presence of a base or a catalyst at ambient pressure.Type: GrantFiled: April 5, 2001Date of Patent: December 4, 2001Assignee: Hoffmann-La Roche Inc.Inventor: Xinglong Jiang
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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: 20010044459Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.Type: ApplicationFiled: June 15, 2001Publication date: November 22, 2001Inventors: Paul F. Jackson, Kevin L. Tays, Keith M. Maclin, Barbara S. Slusher
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Patent number: 6313151Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 31, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6302837Abstract: A compound selected from those of formula (I): wherein: X represents oxygen, sulphur, or NR3 wherein R3 is as defined in the description, Y represents oxygen, sulphur, NR3, or may represent single bond in certain cases, T represents nitrogen, carbon, or CH, A represents single bond, alkylene, arylene, cycloalkylene, heterocycloalkylene, heteroarylene, or —SO2—R4— wherein R4 is as defined in the description, W represents hydroxy, alkoxy, aryloxy, arylalkoxy, cycloalkyloxy, heterocycloalkyloxy or heteroaryloxy, or hydroxyamino, U1 represents hetero, or alkylene wherein one or more of carbon may optionally be replaced by one or more hetero atoms, V1 represents arylene, heteroarylene,or heterocycloalkylene, U2 represents single bond, hetero or alkylene wherein one or more carbon may optionally be replaced by one or more hetero atoms, V2 represents aryl, heteroaryl, or heterocycloalkyl, Ra, Rb, Rc, which may be identical or different, each independently of the others rType: GrantFiled: October 13, 2000Date of Patent: October 16, 2001Assignee: Adir et CompagnieInventors: Guillaume De Nanteuil, Christine Lila, Tony Verbeuren, Alain Rupin
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Patent number: 6300363Abstract: This invention provides a compound of the following formula: and the pharmaceutically acceptable salts thereof, wherein L is oxygen or sulfur; Y is a direct bond or C1-4 alkylidene; Q is C1-6 alkyl, C3-7 cycloalkyl, phenyl, naphthyl, heteroaryl or the like; R1 is hydrogen, C1-6 alkyl or the like; R2 is hydrogen, C1-4 alkyl, C(O)R5 wherein R5 is C1-22 alkyl or C2-22 alkenyl, halosubstituted C1-8 alkyl, halosubstituted C2-8alkenyl, —Y—C3-7 cycloalkyl, —Y—C3-7 cycloalkenyl, phenyl, naphthyl, heteroaryl or the like; X is halo, C1-4 alkyl, hydroxy, C1-4 alkoxy or the like; and n is 0, 1, 2 or 3, with the proviso that a group of formula —Y—Q is not methyl or ethyl when X is hydrogen; L is oxygen; R1 is hydrogen; and R2 is acetyl. This invention also provides a pharmaceutical composition useful for the treatment of a medical condition in which prostaglandins are implicated as pathogens.Type: GrantFiled: December 3, 1999Date of Patent: October 9, 2001Assignee: Pfizer Inc.Inventors: Rodney William Stevens, Kasumari Nakao, Kiyoshi Kawamura, Chikara Uchida, Shinya Fujiwara
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Publication number: 20010021719Abstract: The present invention relates to new 2-Phenyl-1-[(2-Aminoethoxy)-Benzyl]-Indole compounds which are usefuil as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utiig these compounds, which have the general structures below: 1Type: ApplicationFiled: February 8, 2001Publication date: September 13, 2001Inventors: Chris P. Miller, Michael D. Collini, Bach D. Tran, Arthur A. Santilli
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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: 6271245Abstract: The present invention relates to hydroxamic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.Type: GrantFiled: June 1, 1999Date of Patent: August 7, 2001Assignee: Guilford Pharmaceuticals, Inc.Inventors: Paul F. Jackson, Kevin L. Tays, Keith M. MacLin, Barbara S. Slusher
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Patent number: 6262090Abstract: Compounds of the formula wherein A is heteroaryl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; W is O, NR6, or is absent; G is aryl or heteroaryl; and X is a bond X is a bond, —NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; and J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6; or a pharmaceutical acceptable salt thereof, useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpesvirus.Type: GrantFiled: November 22, 1999Date of Patent: July 17, 2001Assignee: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
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Patent number: 6252084Abstract: A class of novel 1H-indole-3-acetamides is disclosed together with the use of such indole compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: October 31, 1997Date of Patent: June 26, 2001Assignee: Eli Lilly and CompanyInventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim, Robert B. Hermann, Richard W. Schevitz
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Patent number: 6245761Abstract: This invention provides a series of substituted indoles which are useful in treating or preventing a condition associated with an excess of neuropeptide Y. This invention also provides the novel substituted indoles as well as pharmaceutical formulations with comprise as an active ingredient one or more of these substituted indoles.Type: GrantFiled: August 29, 1996Date of Patent: June 12, 2001Assignee: Eli Lilly and CompanyInventors: Thomas C. Britton, Robert F. Bruns, Jr., Donald R. Gehlert, Philip A. Hipskind, Karen L. Lobb, James A. Nixon, Paul L. Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis M. Zimmerman
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Patent number: 6179883Abstract: Novel 2-imino-2,3-dihydro-1H-indole derivatives of formula (I) or (II) below: in which: R1, R2 and R3 denote hydrogen, alkyl, carboxyl, alkoxycarbonyl, monohydroxyalkyl, polyhydroxyalkyl, alkoxyalkyl, monoalkylaminoalkyl or dialkylaminoalkyl; R′3 and R4 denote alkyl, carboxyl, alkoxycarbonyl, monohydroxyalkyl, polyhydroxyalkyl, alkoxyalkyl, monoalkylaminoalkyl or dialkylaminoalkyl; R5 denotes hydrogen, alkyl, monohydroxyalkyl, polyhydroxyalkyl, alkoxyalkyl, monoalkylaminoalkyl or dialkylaminoalkyl; and the addition salts thereof with an acid, as well as their uses for dyeing keratin fibres.Type: GrantFiled: August 22, 1997Date of Patent: January 30, 2001Assignee: L'OrealInventors: Eric Terranova, Aziz Fadli, Alain Lagrange
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Patent number: 6150394Abstract: Compounds having a metalloproteinase inhibitory activity, represented by the formula (I), its optically active isomers, their pharmaceutically acceptable salts, or hydrates thereof.Type: GrantFiled: July 22, 1998Date of Patent: November 21, 2000Assignee: Shionogi & Co., Ltd.Inventors: Fumihiko Watanabe, Hiroshige Tsuzuki, Mitsuaki Ohtani
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Patent number: 6063806Abstract: A heterocyclic derivative of the formula (I) ##STR1## wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof exhibit superior ACAT inhibitory activity and lipoperoxidation inhibitory activity in mammals, and are useful as ACAT inhibitors and lipoperoxidation inhibitors. Specifically, they are useful for the prophylaxis and treatment of arteriosclerosis, hyperlipemia, arteriosclerosis in diabetes, and cerebrovascular and cardiovascular ischemic diseases.Type: GrantFiled: April 3, 1998Date of Patent: May 16, 2000Assignee: Kyoto Pharmaceutical Industries, Ltd.Inventors: Shoji Kamiya, Hiroaki Shirahase, Hiroshi Matsui, Shohei Nakamura, Katsuo Wada
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Patent number: 6031111Abstract: A compound represented by formula (I): ##STR1## wherein R.sub.1 represents a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a nitro group, a trifluoromethyl group, a lower alkylthio group, an acyl group, a carboxyl group, a mercapto group or an amino group; R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, an alkoxy group, an acyl group, an aryl group or a heterocyclic group; R.sub.3 represents a lower alkyl group, a cycloalkyl group, an aryl group, or a heterocyclic group; R.sub.4 represents a hydrogen atom, a lower alkyl group, an aryl group, a heterocyclic group, --OR.sub.5, --SR.sub.5 or --NR.sub.6 R.sub.7 (wherein R.sub.5, R.sub.6, and R.sub.7 each represent a lower alkyl group, etc.); X and Y each represent --CH.sub.2 --, --NH-- or --O--; and n represents an integer of from 0 to 4, and an intermediate for synthesis thereof are disclosed.Type: GrantFiled: October 30, 1998Date of Patent: February 29, 2000Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toru Esaki, Takashi Emura, Eiichi Hoshino
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Patent number: 5981580Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.Type: GrantFiled: October 20, 1998Date of Patent: November 9, 1999Assignee: G. D. Searle & Co.Inventors: Sean T. Nugent, Richard A. Mueller