Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Hetero Ring Patents (Class 549/468)
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Publication number: 20040024190Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: 1Type: ApplicationFiled: July 18, 2002Publication date: February 5, 2004Applicant: Boehringer Ingelheim (Canada) Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-Andre Poupart, Jean Rancourt
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Patent number: 6683195Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.Type: GrantFiled: April 15, 2002Date of Patent: January 27, 2004Assignee: ARYx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6673784Abstract: A class of compounds is described which can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula II wherein each of R1, R2, and R3 is independently selected from hydrido, halo, and nitro; wherein R8 is selected from haloalkyl, optionally substituted aryl, optionally substituted aralkyl, optionally substituted heteroaryl, optionally substituted arylalkoxy and optionally substituted aryloxyalkyl; where Y is selected from fluoroalkyl, and wherein R9 alkylamino; or a pharmaceutically-acceptable salt or tautomer thereof.Type: GrantFiled: November 14, 2000Date of Patent: January 6, 2004Assignee: G. D. Searle & Co.Inventors: Daniel L. Flynn, Jeffery Zablocki, Kenneth Williams, Susan L. Hockerman
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Patent number: 6653346Abstract: Cytoprotective compounds, many of which are benzofuran derivatives are useful in the treatment of certain ischemic or inflammatory conditions, including but not limited to stroke, myocardial infarction, congestive heart failure, and skin disorders characterized by inflammation or oxidative damage. They are also useful in the manufacture of pharmaceutical and cosmetic formulations for the treatment of such conditions.Type: GrantFiled: February 6, 2003Date of Patent: November 25, 2003Assignee: Galileo Pharmaceuticals, Inc.Inventors: Bing Wang, Jian Chen
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Publication number: 20030195247Abstract: The present invention relates to a new and improved method for treating diabetes and.or its associated complications by modulating the activity of protein tryosin phosphatase 1B (“PTP-1B”). The inventive compounds modulate the activity PTP-1B by binding to a novel binding site referred herein as the PTP-1B exosite that is distal to the active site of PTP-1B. The present invention also relates to a new and improved method of treating immune system disorders by modulating the activity of T-cell protein tyrosine phosphatase (“TC-PTP”). The inventive compound modulate the activity of TC-PTP by binding to a novel binding site referred herein as the TC-PTP exosite that is distal to the active site of PTP-1B.Type: ApplicationFiled: February 25, 2003Publication date: October 16, 2003Inventors: Kenneth Barr, Bruce Fahr, Stig Hansen, Christian Wiesmann
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Patent number: 6620841Abstract: A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORA wherein RA is hydrogen or ester residue, —CONRBRC wherein RB and RC each is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1 is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1 is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.Type: GrantFiled: June 7, 2001Date of Patent: September 16, 2003Assignee: Shionogi & Co., Ltd.Inventors: Toshio Fujishita, Tomokazu Yoshinaga, Akihiko Sato
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Patent number: 6566373Abstract: The invention relates to 3-hydroxy-and 3-keto-cyclohetero-substituted leucine compounds that are inhibitors of cysteine proteases, particularly cathepsin K, and are useful in the treatment of diseases in which inhibition of bone loss is a factor. The 3-hydroxy-or 3-keto-moiety is bonded to a tetrahydrothiophene, tetrahydrothiopyran, tetrahydrofuran or tetrahydropyran ring.Type: GrantFiled: July 30, 2001Date of Patent: May 20, 2003Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: Andrew D Gribble, Ashley Edward Fenwick, Robert W Marquis, Daniel F Veber, Jason Witherington
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Patent number: 6506780Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.Type: GrantFiled: July 2, 2001Date of Patent: January 14, 2003Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Publication number: 20020193428Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.Type: ApplicationFiled: April 15, 2002Publication date: December 19, 2002Inventors: Pascal Druzgala, Peter G. Milner
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Publication number: 20020151728Abstract: The present invention provides a production method of a 5-phthalancarbonitrile compound, which comprises the use of a novel compound of the formula [I] 1Type: ApplicationFiled: June 21, 2002Publication date: October 17, 2002Applicant: Sumika Fine Chemicals Co., Ltd.Inventors: Tetsuya Ikemoto, Masami Igi
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Publication number: 20020151584Abstract: Purified antiviral compounds, pharmaceutical formulations containing the compounds, and methods of use of the compounds are provided. The compositions of the invention are isolated antiviral components from plant extracts derived from, for example, Salvia miltiorrhiza, that find use in the treatment of viral infections, such as by inhibiting the activity of viral integrase. Methods for isolation and purification of the antiviral compounds are additionally provided.Type: ApplicationFiled: September 25, 2001Publication date: October 17, 2002Applicant: Johns Hopkins UniversityInventors: Ru Chih C. Huang, Ibrahim Shawky Abd Elazem, Hong Shan Chen
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Patent number: 6465508Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.Type: GrantFiled: February 23, 2001Date of Patent: October 15, 2002Assignee: WyethInventors: Frances Christy Nelson, Arie Zask, James Ming Chen, Dominick Mobilio, Ramaswamy Nilakantan
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Patent number: 6462055Abstract: Compounds having the formula: wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen; or R1 and R2 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 memberedType: GrantFiled: April 30, 2001Date of Patent: October 8, 2002Assignee: WyethInventors: Jonathan Bloom, Kevin Curran, Martin DiGrandi, Russell Dushin, Stanley Lang, Emily Norton, Adma Ross, Bryan O'Hara
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Patent number: 6441201Abstract: A method for the preparation of 5-cyanophthalide in which 5-carboxyphthalide is reacted with a dehydrating agent, such as thionylchloride, and a sulphonamide, in particular sulfamide. Cyanophthalide is prepared in high yields by a convenient procedure. 5-cyanophthalide is an intermediate used in the preparation of the antidepressant drug citalopram.Type: GrantFiled: July 27, 2001Date of Patent: August 27, 2002Assignee: H. Lundbeck A/SInventor: Beat Weber
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Patent number: 6407102Abstract: The invention relates to tyrosine kinase inhibitors of the bis-indolyl compound type of the general formula I: pharmaceuticals containing them and their use for the treatment of malignant and other diseases based on pathological cell proliferation.Type: GrantFiled: May 4, 1999Date of Patent: June 18, 2002Assignee: Zentaris AGInventors: Siavosh Mahboobi, Sabine Kuhr, Herwig Pongratz, Alfred Popp, Harald Hufsky, Frank-D Bohmer, Steffen Teller, Andrea Uecker, Thomas Beckers
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Patent number: 6395738Abstract: The present invention relates to benzofuran derivatives represented by following general formula (I): wherein R1 represents lower alkyl, R2 represents hydrogen or substituted or unsubstituted lower alkyl, R3, R4, R5 and R6 independently represent hydrogen or lower alkyl, X represents CH2 or C═O, and Y represents CH2 or NH, or pharmaceutically acceptable salts thereof.Type: GrantFiled: March 29, 2000Date of Patent: May 28, 2002Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Ohshima, Tohru Matsuzaki, Haruhiko Manabe
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Patent number: 6372783Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The isolated enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.Type: GrantFiled: October 6, 2000Date of Patent: April 16, 2002Assignee: Aryx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6362223Abstract: The subject invention pertains to novel enantiomerically pure compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making and purifying the compounds. The enantiomerically purified compounds, and compositions of these compounds, exhibit unexpectedly distinct and advantageous characteristics, such as a markedly superior ability to reduce or inhibit ventricular premature beats, as compared to racemic mixtures of the compounds.Type: GrantFiled: October 6, 2000Date of Patent: March 26, 2002Assignee: Aryx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Patent number: 6350777Abstract: Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds' use for treating tumor cells is also described. Additional aspects described here are certain diaryl ether benzo[b]thiophene derivatives. Also described are particular analogs derived from dihydronaphthalene which have proven particularly effective. Certain new benzofuran analogs are described, as well as certain sulfur oxide benzo[b]thiophene analogs. Important compounds described herein include the first nitrogen-containing derivatives of combretastatin. These include nitro, amino and azide combrdtastatin derivatives.Type: GrantFiled: December 15, 2000Date of Patent: February 26, 2002Assignees: Baylor University, Arizona Disease Control Research CommissionInventors: Kevin G. Pinney, George R. Pettit, Vani P. Mocharla, Maria del Pilar Mejia, Anupama Shirali
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Patent number: 6316487Abstract: The subject invention pertains to novel compounds, and compositions comprising the compounds, for the treatment of cardiac arrhythmias. The subject invention further concerns a method of making the novel compounds. The novel compounds are rapidly metabolized analogs of amiodarone, having the distinct and advantageous characteristic of being metabolized to a less lipophilic compound. The new compounds can have particular utility for treating life-threatening ventricular tachyarrhythmias, especially in patients with congestive heart failure (CHF). The product can also provide effective management for ventricular arrhythmias and supraventricular arrhythmias, including atrial fibrillation and re-entrant tachyarrhythmias involving accessory pathways.Type: GrantFiled: October 6, 2000Date of Patent: November 13, 2001Assignee: Aryx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Publication number: 20010034454Abstract: Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds' use for treating tumor cells is also described.Type: ApplicationFiled: December 15, 2000Publication date: October 25, 2001Applicant: BYLOR UNIVERSITY AND ARIZONA DESEASE CONTROL RESEARCH COMMISSIONInventors: Kevin G. Pinney, George R. Pettit, Vani P. Mocharla, Maria del Pilar Mejia, Anupama Shirali
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Publication number: 20010008736Abstract: Novel sulfonylimide and sulfonylmethide compounds are described which are useful as conductive salts. Also described is the use of the above compounds in salt form in battery electrolytes, particular salts having mixed perfluorocarbon and hydrocarbon groups or having all hydrocarbon groups. The above salts are less expensive to produce and still exhibit excellent conductivity and low corrosivity.Type: ApplicationFiled: August 25, 1998Publication date: July 19, 2001Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventors: ALAN DAVID FANTA, PHAT TAN PHAM, STEVEN JOSEPH HAMROCK
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Patent number: 6221902Abstract: This invention provides compounds of Formula I having the structure wherein A, Q, R3, and R4 are as defined hereinbefore in the specification, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: April 24, 2001Assignee: American Home Products CorporationInventors: Michael S. Malamas, Folake O. Adebayo, Paul J. Dollings
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Patent number: 6211203Abstract: Compounds of formula I wherein R1 is 1-2C-alkoxy optionally substituted by flourine, R2 is methyl, 1-methylethyl, 3-7C-cycloalkyl or 3-7Ccycloalkylmethyl and Ar is a pyridyl which is optionally di-halo substituted.Type: GrantFiled: February 5, 1999Date of Patent: April 3, 2001Assignee: Byk Gulden Lomberg Chemische Fabrik GmbHInventor: Hermann Amschler
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Patent number: 6194458Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.Type: GrantFiled: October 21, 1999Date of Patent: February 27, 2001Assignee: Merck & Co., Inc.Inventors: Robert K. Baker, Jianming Bao, Frank Kayser, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
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Patent number: 6180411Abstract: A new class of optical indicators which are capable of memorizing and preserving the spatial localization of intracellular analytes in a time resolved manner is described. The compounds comprise a chromophore carrying a photolabile group capable of undergoing an irreversible and detectable chemical transformation upon irradiation by light. The chromophore is linked to a binding site capable of binding an analyte, wherein binding of the analyte to the binding site alters an optical property of the chromophore, thus altering the ability of the photolabile group to undergo the chemical transformation. Methods and kits for memorizing the spatial localization of the analytes are also described.Type: GrantFiled: July 30, 1998Date of Patent: January 30, 2001Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Stephen R. Adams
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Patent number: 6110963Abstract: This invention provides compounds of Formula I having the structure ##STR1## wherein A is C or N;B is O, S, N, or CH.dbd.CH;E is ##STR2## or --X--D; D is ##STR3## or alkyl of 1-12 carbon atoms; X is CO, CH(OH), CH.sub.2, or --CH--S-2-benzothiazole;Y is hydrogen, alkyl of 1-6 carbon atoms, or halogen;Z is O, S, or N;R is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, halogen, or trifluoromethyl;R.sup.1 is alkyl of 1-12 carbon atoms, aryl of 6-10 carbon atoms, aralkyl of 7-15 carbon atoms, halogen, Het-alkyl wherein the alkyl moiety contains 1-6 carbon atoms, or aryl mono-, di- or tri-substituted with a substituent selected from the group consisting of halogen, alkyl of 1-6 carbon atoms, trifluoromethyl, and alkoxy of 1-6 carbon atoms;Het is ##STR4## G is O, S, or N; and the remaining variables are as defined in claim 1, or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: August 29, 2000Assignee: American Home Products CorporationInventor: Michael S. Malamas
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Patent number: 6046190Abstract: The invention relates to sulfonamide-containing hydroxyethylamine protease inhibitor compounds, their process of making, composition and method of use for inhibiting retroviral proteases such as human immunodeficiency virus.Type: GrantFiled: January 24, 1996Date of Patent: April 4, 2000Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, John N. Freskos, Deborah E. Bertenshaw, Robert M. Heintz
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Patent number: 6040339Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl or various other organic groups; R.sup.3 is alkyl; R.sup.4 is a group of formula (II), (III), (IV), (V), (VI), (VII), (VIII) or (IX): ##STR2## wherein: A.sup.1 is a single bond, alkylene or alkenylene; A.sup.2 is or alkenylene; A.sup.3 is a single bond, alkyleneor alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or various other groups; R.sup.6 is alkyl or phenyl; R.sup.7 is hydrogen or alkyl; R.sup.8 is alkyl or various other groups; and n is 0 and pharmaceutically acceptable salts thereof have valuable inhibitory activity against acyl-CoA: cholesterol acyl transferase.Type: GrantFiled: May 28, 1998Date of Patent: March 21, 2000Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 6028101Abstract: A method of controlling Take-all disease of plants by applying, preferably to the seed prior to planting, a fungicide of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are C and are part of an aromatic ring that is furan;A is selected from --C(X)-amine, --C(O)--SR.sub.3, --NH--C(X)R.sub.4, and --C(.dbd.NR.sub.3)--XR.sub.7 ;B is --W.sub.m --Q(R.sub.2).sub.3 or selected from o-tolyl, 1-naphthyl, 2-naphthyl, and 9-phenanthryl, each optionally substituted with halogen or R.sub.4 ;Q is C, Si, Ge, or Sn;W is --C(R.sub.3).sub.p H.sub.(2-p) --; or when Q is C, W is selected from --C(R.sub.3).sub.p H.sub.(2-p) --, --N(R.sub.3).sub.m H.sub.(1-m) --, --S(O).sub.p --, and --O--;X is O or S;n is 2;m is 0 or 1;p is 0, 1, or 2;R, R.sub.2, R.sub.3, R.sub.4 and R.sub.7 are herein defined;or an agronomic salt thereof.Type: GrantFiled: August 7, 1997Date of Patent: February 22, 2000Assignee: Monsanto CompanyInventors: 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: 5986139Abstract: A process for the preparation of primary or secondary amines by hydrogenation of imines with hydrogen at elevated pressure and in the presence of a dinuclear Ir(III) complex having ditertiary diphosphine ligands, halide bridges, halide and hydride ligands, or an Ir(III) halide complex salt containing ditertiary diphosphine ligands, as catalyst, wherein the catalyst corresponds to formula I or Ia or to mixtures of at least two compounds of formula I, at least two compounds of formulae I and Ia, or at least two compounds of formula Ia[(DIP)IrX.sub.q Y.sub.r ].sub.2 (I),[(DIP)X.sub.4 ].sup..crclbar. Me.sup..sym. (Ia),whereinDIP is the ditertiary diphosphine ligand of a ferrocenyldiphosphine the phosphine groups of which are either bonded directly or via a bridge group --CR.sub.v R.sub.w -- to the ortho positions of a cyclopentadienyl ring or are each bonded to a cyclopentadienyl ring of a ferrocenyl, so that a 5-, 6- or 7-membered ring is formed together with the Ir atom;R.sub.v and R.sub.Type: GrantFiled: January 26, 1998Date of Patent: November 16, 1999Assignee: Novartis Crop Protection, Inc.Inventors: Rafael Sablong, John Anthony Osborn, Felix Spindler
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Patent number: 5981514Abstract: Disclosed herein are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein R.sub.1 is alkyl of 1-6 carbon atoms;A is alkylene having from 2-5 carbon atoms, each of which carbon atoms is substituted with R.sub.2, where each R.sub.2 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is C.sub.1 -C.sub.6 alkyl;Y and Y.sub.1 are hydrogen or halogen; andR.sub.4 is hydrogen or --PO.sub.3 H,which compounds are water soluble and can be used for the treatment of arrhythmias.Type: GrantFiled: February 12, 1999Date of Patent: November 9, 1999Inventor: John C. Somberg
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Patent number: 5972936Abstract: Compounds having the formula (i), ##STR1## wherein the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined herein. The compounds of the present invention can be utilized to treat disease states capable of being modulated by inhibition of proteins which mediate cellular activity, such as tumor necrosis factor (TNF) and/or phosphodiesterase IV (PDE IV).Type: GrantFiled: May 20, 1997Date of Patent: October 26, 1999Assignee: Darwin Discover LimitedInventors: Hazel Joan Dyke, John Gary Montana
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Patent number: 5948817Abstract: Novel polycyclic ethyl alkylamides of formula I are active as melatonergic agents. ##STR1## wherein Z=CH (when a double bond is present) or (CH.sub.2).sub.n, wherein n is 1-4;X=O, CH.sub.2, or CH (when a double bond is present);R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-3 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkoxyalkyl, C.sub.1-4 trifluoromethylalkyl, C.sub.1-6 aminoalkyl; andY=H, C.sub.1-6 alkoxy or halogen.Type: GrantFiled: March 4, 1998Date of Patent: September 7, 1999Assignee: Bristol-Myers Squibb CompanyInventors: James Epperson, Graham Johnson, Daniel J. Keavy, Katherine S. Takaki
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Patent number: 5925636Abstract: Compounds having the formula (i), ##STR1## wherein the groups R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are defined herein. The compounds of the present invention can be utilized to treat disease states capable of being modulated by inhibition of proteins which mediate cellular activity, such as tumor necrosis factor (TNF) and/or phosphodiesterase IV (PDE IV).Type: GrantFiled: May 20, 1997Date of Patent: July 20, 1999Assignee: Darwin Discovery LimitedInventors: Hazel Joan Dyke, Christopher Lowe, John Gary Montana
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Patent number: 5886191Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.Type: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
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Patent number: 5880147Abstract: Compounds of formula (I): ##STR1## wherein: R.sup.1 is alkyl; R.sup.2a, R.sup.2b, R.sup.2c and R.sup.2d are the same or different and each is hydrogen, optionally substituted alkyl, --(C.dbd.O)--B.sup.1 (wherein B.sup.1 is hydrogen or alkyl), nitro, --NR.sup.c R.sup.d (wherein R.sup.c is hydrogen or alkyl and Rd is alkyl), hydroxy, protected hydroxy group, alkoxy, cyano, alkylthio, alkylsulfinyl, alkylsulfonyl or halogen;R.sup.3 is alkyl; R.sup.4 is a group of the formula (II) ##STR2## wherein A.sup.1 is a single bond, alkylene or alkenylene; R.sup.5a and R.sup.5b are the same or different and each is hydrogen, alkyl or --A.sup.4 R.sup.5.sub.c wherein A is a single bond, alkylene or alkenylene and R.sup.5.sub.c is alkoxy; and n is 0, and pharmaceutically acceptable salts thereof. Such compounds have valuable inhibitory activity against acyl-CoA (cholesterol acyl transferase).Type: GrantFiled: September 18, 1996Date of Patent: March 9, 1999Assignee: Sankyo Company, LimitedInventors: Akira Yoshida, Kozo Oda, Takashi Kasai, Kousei Shimada, Hiroshi Kogen, Ichiro Hayakawa, Sadao Ishihara, Teiichiro Koga, Eiichi Kitazawa, Taro Tokui
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Patent number: 5880296Abstract: A method for preparing an optically pure 2-ethyl-2,3-dihydrobenzofurancarboxylic acid of formula II wherein R is a hydrogen atom, halogen, lower alkyl, lower alkoxy or hydroxy is described. ##STR1## The method comprises separating the racemic mixture by selective crystallization with the suitable optically pure enantiomer of 2-phenylglycinol, in a suitable solvent, whereafter the optically pure, crystallized acid of formula II is isolated and recovered. The invention also provides the optically pure 2-ethyl-2,3-dihydro-benzofurancarboxylic acid derivative thus obtained and the use thereof for the preparation of an optically pure derivative of efaroxan.Type: GrantFiled: November 10, 1997Date of Patent: March 9, 1999Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Patrice Mayer
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Patent number: 5858995Abstract: This invention relates to a novel heterocyclic compound represented by formula (I), wherein each symbol is as defined in the specification and a pharmaceutically acceptable salt thereof which are the inhibitors of bone resorption and bone metabolism, to processes for preparation thereof, to a pharmaceutical composition comprising the same and to a method for the treatment of diseases caused by abnormal bone metabolism in human being or an animal.Type: GrantFiled: October 25, 1996Date of Patent: January 12, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Yoshio Kawai, Hitoshi Yamazaki, Natsuko Kayakiri, Kousei Yoshihara, Takumi Yatabe, Teruo Oku
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Patent number: 5854282Abstract: The invention provides compounds according to the formula ##STR1## in which: Ha=I or BrX=CH.sub.2 or C=OR.sup.1 =C.sub.1-4 alkylR.sup.2 =--NHSO.sub.2 R.sup.3 ;--NHCOR.sup.3 ; or--NHCONHR.sup.3where R.sup.3 =--CF.sub.3,C.sub.1-3 alkyl, 4-R.sup.4 C.sub.6 H.sub.4 --;where R.sup.4 =C.sub.1-4 alkoxy-; hydroxy-; fluoro-; or nitro-;or a pharmaceutically acceptable salt thereof.The compounds may particularly be used in the treatment of T3 regulated gene disorders and diseases.Type: GrantFiled: April 7, 1997Date of Patent: December 29, 1998Assignee: Karo Bio ABInventor: Charlotta Mellin
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Patent number: 5849788Abstract: Described is a novel compound and method, useful for treatment of cardiac arrhythmias, especially useful in patients with congestive heart failure (CHF). A process for synthesizing the novel compound is also described.Type: GrantFiled: June 6, 1995Date of Patent: December 15, 1998Assignee: ARYX TherapeuticsInventor: Pascal Druzgala
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Patent number: 5773467Abstract: Benzofuran carboxides and sulphonamides have therapeutic utility, e.g. in the treatment of inflammation and asthma, by virtue of their ability to inhibit phosphodiesterases and tumor necrosis factor.Type: GrantFiled: December 5, 1996Date of Patent: June 30, 1998Assignee: Chiroscience, Ltd.Inventors: Hazel Joan Dyke, Hannah Jayne Kendall, Christopher Lowe, John Gary Montana
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Patent number: 5739396Abstract: Ligands useful for transition metal catalyzed bond forming reactions are provided with a metal binding portion having at least one metal binding moiety ##STR1## wherein Ar and Ar' each is an aryl or a heteroaryl. These ligands may be prepared by providing an aromatic carboxylic acid having a diarylphosphino or diheteroarylphosphino substituent on the aromatic ring, and forming an ester or an amide derivative of the carboxylic acid by coupling with a chiral diol or a chiral diamine. The ligands facilitate, for example, flexible strategies for enantiocontrolled construction of five membered carbocyclic rings with varying substitution patterns and high enantioselectivity.Type: GrantFiled: June 7, 1995Date of Patent: April 14, 1998Assignee: Stanford UniversityInventors: Barry M. Trost, David L. Van Vranken, Richard C. Bunt
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Patent number: 5733476Abstract: A mesomorphic compound of the formula (I) having a coumaran skeleton is suitable as a component for a liquid crystal composition providing improved response characteristics. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of electrode plates. The liquid crystal device is used as a display panel constituting a display apparatus providing good display characteristics.Type: GrantFiled: February 29, 1996Date of Patent: March 31, 1998Assignee: Canon Kabushiki KaishaInventors: Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Yoko Yamada, Shinichi Nakamura
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Patent number: 5708004Abstract: Hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: January 13, 1998Assignee: Monsanto CompanyInventors: John J. Talley, Kathryn L. Reed
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Patent number: 5698696Abstract: This invention relates to a novel process for preparing 2,3-dihydro-benzofuranol derivatives and to the novel intermediates produced thereby.Type: GrantFiled: March 7, 1996Date of Patent: December 16, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Gilbert Marciniak, Richard A. Schnettler, Timothy A. Ayers, Damian J. Krysan
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Patent number: 5635107Abstract: Fluorine-containing five-membered ring compounds of the formula IR.sup.1 -(A.sup.1 -Z.sup.1).sub.m -A.sup.2 -Z.sup.2 -W Iin whichW is ##STR1## is a cyclohexane, cyclohexene or phenyl,Y.sup.1 is O or S,Y.sup.2 is (a) O, S, C.dbd.O or fluoroalkyl,Y.sup.3 is (a) N, CH or CF,Q is C.dbd.O, CHF, CF.sub.2, CHR.sup.2 or CFR.sup.2Q' is CF or CR.sup.2,R.sup.2 is C.sub.1-15 -alkyl, optionally at least mono-substituted by F,X is H, F or Cl,R.sup.1 H or hydrocarbyl,A.sup.1 and A.sup.2 are a carbocyclic, aromatic or heterocyclic radicalZ.sup.1 and Z.sup.2 are --CO--O, --O--CO--, --CH.sub.2 O--, --O--CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.ident.C-- or a single bond, andm is 0, 1 or 2, and liquid-crystalline media containing same.Type: GrantFiled: January 8, 1993Date of Patent: June 3, 1997Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Ekkehard Bartmann, Georg Weber
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Patent number: 5635527Abstract: A novel carboxylic acid compound having a condensed ring, which is represented by the formula (I) ##STR1## wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, a pharmaceutical composition thereof and pharmaceutical use thereof. The novel carboxylic acid compound having a condensed ring and pharmacologically acceptable salt thereof of the present invention have superior GPIIb/IIIa antagonism in mammals inclusive of human; can be administered orally; have long life in blood and low toxicity; and show less side-effects. Accordingly, they are extremely useful for the prophylaxis and treatment of thrombotic diseases and other diseases.Type: GrantFiled: February 6, 1996Date of Patent: June 3, 1997Assignee: The Green Cross CorporationInventors: Shinichiro Ono, Tomohiro Yoshida, Atsuyuki Ashimori, Keigo Kosaka, Takehiro Okada, Kazuhiro Maeda, Masahiro Eda, Fumio Mori, Yoshihisa Inoue, Hajime Ebisu, Teruaki Imada, Ruriko Ikegawa, Feng Wang, Norifumi Nakamura
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Patent number: 5622989Abstract: 6-Amino-benzofuryl- and thienyl-derivatives can be prepared by reacting appropriate amino-substituted benzoyl phenols with appropriate substituted acetophenones and subsequent modification of the substituents. The compounds are useful for the treatment of actual and chronic inflammatory diseases, particularly of the airways and the gastro-intestinal tract.Type: GrantFiled: May 23, 1995Date of Patent: April 22, 1997Assignee: Bayer AktiengesellschaftInventors: Gabriele Br aunlich, R udiger Fischer, Mazen Es-Sayed, Rudolf Hanko, Stephen Tudhope, Graham Sturton, Trevor Abram, Wendy J. McDonald-Gibson, Mary F. Fitzgerald
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Patent number: 5596106Abstract: This invention discloses methods of using certain aryl-benzo[b]thiophene and benzo[b]furan compounds to block or inhibit cannabinoid receptors in mammals. It also discloses novel compounds which are antagonists of the cannabinoid receptors and also discloses pharmaceutical formulations which contain the compounds as an active ingredient.Type: GrantFiled: June 7, 1995Date of Patent: January 21, 1997Assignee: Eli Lilly and CompanyInventors: George J. Cullinan, Kennan J. Fahey, Gary A. Koppel