Nitrogen Not Bonded Directly To A Ring Patents (Class 562/442)
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Patent number: 6306911Abstract: This invention relates to a series of substituted amino acids of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention are small molecules that bind to neutral sphingomyelinase and inhibit its activity.Type: GrantFiled: February 7, 2000Date of Patent: October 23, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael P. Wachter, Praful Lalan
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Patent number: 6245938Abstract: A method of separating a racemic mixture of amino acid enantiomers, which entails reacting the mixture with a 4-pentenoyl compound, thereby derivatizing the enantiomers to form two diastereomers, and separating the diastereomers.Type: GrantFiled: November 14, 1997Date of Patent: June 12, 2001Assignee: University of Virginia Patent FoundationInventors: Sidney Hecht, Michiel Lodder
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Patent number: 6207709Abstract: An N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of the formula (I): wherein X, Y, W and R are as defined herein.Type: GrantFiled: February 24, 1999Date of Patent: March 27, 2001Assignee: Pharmacia & Upjohn S.p.A.Inventors: Mario Varasi, Antonio Giordani, Massimo Cini, Carmela Speciale, Alberto Bianchetti
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Patent number: 6204391Abstract: A water soluble derivative of buckministerfullerene (C60) having antiviral and virucidal properties is used to inhibit human retroviral replication and infections. The derivatized fullerene is symmetrically substituted with polar organic moieties containing 1 to 20 carbon atoms and optionally further containing oxygen or nitrogen.Type: GrantFiled: September 21, 1998Date of Patent: March 20, 2001Assignee: The Regents of the University of CaliforniaInventors: Simon H. Friedman, Raymond F. Schinazi, Fred Wudl, Craig L. Hill, Diane L. DeCamp, Rintje P. Sijbesma, George L. Kenyon
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Patent number: 6191171Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.Type: GrantFiled: November 13, 1998Date of Patent: February 20, 2001Assignee: Merck & Co., Inc.Inventors: Stephen E. DeLaszlo, William K. Hagmann
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Patent number: 6172058Abstract: A pharmaceutical compound of the formula in which R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-10 alkyl, C3-10 cycloalkyl-C2-10 alkenyl, C3-10 cycloalky-C2-10 alkynyl, optionally substituted phenyl-C1-10 alkyl, optionally substituted phenyl-C2-10 alkenyl, optionally substituted phenyl-C2-10 alkynyl, optionally substituted naphthyl, optionally substituted naphthyl-C1-10 alkyl, C1-10 alkoxy-C1-10 alkyl, C3-10 cycloalkoxy-C1-10 alkyl, optionally substituted heterocyclyl, optionally substituted heterocyclyl-C1-10 alkyl, optionally substituted phenyl fused to C5-10 cycloalkyl, optionally substituted tricyclic, optionally substituted tricyclic-C1-10 alkyl, or [optionally substituted phenyl(CH2)n]2-C1-10 alkyl, where n is 0 or 1 to 4, and R2 is hydrogen or one of the values for R1; or a salt or ester thereof.Type: GrantFiled: April 3, 1998Date of Patent: January 9, 2001Assignee: Lilly, SAInventors: Concepci{acute over (o)}n Pedregal Tercero, Ivan Collado Cano, Angel Maz{acute over (o)}n Ruiz
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Patent number: 6166081Abstract: A pharmaceutical composition for treatment of Parkinson's disease comprising a compound of levodopa dissolved in a non-degradative solvent which allows transdermal administrtion of levodopa. The compound of levodopa is an alkyl-ester of levodopa and the solvent is a formulation comprising a substantially non-aqueous solvent, a transdermal enhancer and a detergent. The alkyl-ester of levodopa is preferably levodopa-ethyl-ester (LDEE).Type: GrantFiled: April 7, 1999Date of Patent: December 26, 2000Inventors: Moshe Kushnir, Eliahu Heldman
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Patent number: 6153591Abstract: The present invention is directed to novel dipeptides represented by the general Formula I: ##STR1## where R.sub.1 -R.sub.2 and AA are defined herein. The present invention relates to the discovery that compounds having Formula I are potent inhibitors of caspases and apoptotic cell death. Therefore, the inhibitors of this invention can retard or block cell death in a variety of clinical conditions in which the loss of cells, tissues or entire organs occurs.Type: GrantFiled: March 16, 1999Date of Patent: November 28, 2000Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John Drewe, Yan Wang, Eckard Weber
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Patent number: 6153650Abstract: Novel gamma aminobutyric acids of formula (I) are disclosed and are useful as agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, inflammation, and gastrointestinal damage. Processes for the preparation and intermediates useful in the preparation are also disclosed.Type: GrantFiled: March 1, 1999Date of Patent: November 28, 2000Assignee: Warner-Lambert CompanyInventors: Justin Stephen Bryans, David Christopher Horwell, Clare Octavia Kneen, Andrew John Thorpe, David Juergen Wustrow
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Patent number: 6136834Abstract: A tetrazole derivative of formula (I) ##STR1## wherein R is H, alkyl, alkoxy, carbocyclic ring, alkyl or alkoxy substituted by carbocyclic ring;AA.sup.1 and AA.sup.2 is a bond or ##STR2## and ##STR3## respectively, or AA.sup.1 and AA.sup.2, together, may have the formula (a); ##STR4## and Y is formula (b) ##STR5## wherein the Tet ring is tetrazole; Z is alkylene, alkenylene, O, S, SO, SO.sub.2, NR.sup.26, methylene in alkylene replaced by O, S, --SO--, --SO.sub.2 -- or --NR.sup.26 --; and E is H, alkyl, or COOR.sup.27.Type: GrantFiled: June 29, 1998Date of Patent: October 24, 2000Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Makoto Tanaka, Tohru Miyazaki, Hiroyuki Ohno
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Patent number: 6127515Abstract: This invention is directed to a functionalized amino resin of formula ##STR1## wherein S is a solid support; R is H or alkyl; A is ##STR2## Y is OH or OCOR.sup.1 ; and R.sup.1 is aliphatic or aromatic which is useful for the solid phase synthesis of amides, peptides and hydroxamic acids.Type: GrantFiled: May 21, 1999Date of Patent: October 3, 2000Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Franco Manfre, Benoit J. Vanasse, Richard F. Labaudiniere, George C. Morton
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Patent number: 6100423Abstract: The present invention is directed to compounds of the formula ##STR1## where R.sup.1 is BOC or H, R is H or lower alkyl; X and Y are the same or different halo atoms selected from the group consisting of Cl, Br or I and pharmaceutically acceptable salts and isomers thereof.Type: GrantFiled: March 3, 1999Date of Patent: August 8, 2000Assignee: G. D. Searle & Co.Inventors: Joe T. Collins, Balekudru Devadas, Hwang-fun Lu, James W. Malecha, Julie Marion Miyashiro, Srinivasan Nagarajan, Joseph Gerace Rico, Thomas E. Rogers
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Patent number: 6075051Abstract: A method for protecting a crop against fungal diseases by inducing local and systemic resistance of the crop comprising applying to the crop or its locus a composition containing an effective amount of at least one .beta.-aminobutyric acid or .beta.-amino valeric acid and salts and derivatives thereof.Type: GrantFiled: October 29, 1998Date of Patent: June 13, 2000Assignee: Agrogene Ltd.Inventor: Yigal Cohen
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Patent number: 6048872Abstract: The present invention relates to phenethanolamine derivatives of formula (I) wherein R.sup.1 represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R.sup.2 represents hydrogen or C.sub.1-6 -alkyl; R.sup.3 represents a group (A) where the ring is substituted by one to four further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; or R.sup.3 represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; R.sup.4 represents hydrogen, or C.sub.1-6 -alkyl; R.sup.5 represents ZCH.sub.2 CO.sub.2 H wherein Z represents a bond, or O; Y represents (CH.sub.2).sub.Type: GrantFiled: June 5, 1998Date of Patent: April 11, 2000Assignee: Glaxo Wellcome Inc.Inventors: Richard Howard Green, Michael Walter Foxton
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Patent number: 6037472Abstract: Compounds of formula (I) ##STR1## and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as stromelysin, gelatinase, matrilysin and collagenase, and are useful in the treatment of mammals having disease-states alleviated by the inhibition of such matrix metalloproteases.Type: GrantFiled: November 22, 1994Date of Patent: March 14, 2000Assignee: Syntex (U.S.A.) Inc.Inventors: Arlindo Lucas Castelhano, Steven Lee Bender, Judith Gail Deal, Stephen Horne, Teng J. Liak, Zhengyu Yuan
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Patent number: 6034067Abstract: The invention relates to a compound having formula (I), wherein A, B, X, N, Z and Q are defined as described in the description. The compounds of the invention have anticoagulant activity and can be used in treating or preventing thrombin-related diseases.Type: GrantFiled: August 12, 1998Date of Patent: March 7, 2000Assignee: Akzo Nobel, N.V.Inventors: Peter Diederik Jan Grootenhuis, Adrianus Petrus Antonius de Man, Anton Egbert Peter Adang
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Patent number: 6011174Abstract: The present invention relates to a compound of the formula (I), or its pharmaceutically acceptable salt or ester: ##STR1## wherein Ar.sup.1 is an aryl group or a heteroaromatic ring group; Ar is a group of the formula ##STR2## each of Ar.sup.2 and Ar.sup.3 is an aryl group or a heteroaromatic ring group; Cy is an aryl group, a heteroaromatic ring group or an aliphatic ring group which may contain one or two oxygen atoms; A.sup.1 is a C.sub.1-4 chain hydrocarbon group; m is an integer of from 1 to 6; each of n and p is an integer of from 0 to 3; Q.sup.1 is a single bond, a group of the formula --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 S-- or --SCH.sub.2 --, or a C.sub.1-6 chain hydrocarbon group; Q.sup.2 is a single bond or a group of the formula --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p --; Q.sup.3 is a single bond, an oxygen atom, a sulfur atom, a methylene group, a vinylene group or a group of the formula --CO--, --NH--, --COO--, --OCO--, --CH.sub.2 CH.sub.2 --, --OCH.sub.Type: GrantFiled: August 4, 1998Date of Patent: January 4, 2000Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 6001877Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: May 20, 1998Date of Patent: December 14, 1999Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5968581Abstract: Novel dipeptide derivatives, such as N-3,3-dimethylbutyl-.alpha.-L-aspartyl-.alpha.-methyl-L-phenylalanine methyl ester and N-3,3-dimethylbutyl-.alpha.-L-aspartyl-.alpha.-methyl-L-tyrosine methyl ester, and sweetening agents comprising, as the active ingredient, anyone of the derivatives and their salts, being low-calorie sweetening agents which are excellent in stability, safety and degree of sweetness, are provided. The products to have been sweetened, comprising such above sweetening agents are also provided.Type: GrantFiled: March 10, 1998Date of Patent: October 19, 1999Assignee: Ajinomoto Co., Inc.Inventors: Ryoichiro Nakamura, Yusuke Amino, Tadashi Takemoto
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Patent number: 5958496Abstract: Novel aspartyldipeptidoamides and salts thereof. The apartyldipeptides are useful as a low-calorie sweetener for food and beverage products and have excellent taste and chemical stability.Type: GrantFiled: July 10, 1997Date of Patent: September 28, 1999Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Ryoichiro Nakamura, Tadashi Takemoto
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Patent number: 5955505Abstract: A method comprising administering a sulfonamide derivative to a patient requiring activation of glutamate receptors, the sulfonamide derivative represented by the formula ##STR1## wherein A is a napthyl group, a pyridyl group, a phenyl group, a phenyl group substituted by 1 to 5 members selected from the group consisting of a halogen atom, an alkyl group having 1 to 40 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a nitro group, and an acetamido group, or an alkyl group having 1 to 20 carbon atoms; B is an alkylene group having 1 to 3 carbon atoms, a group of --OCH.sub.2 -- or a group of --CH.dbd.CH--; X and Y are the same or different, and are each a hydrogen atom or a fluorine atom; R is a carboxy group, an alkoxycarbonyl group having 2 to 5 carbon atoms, a hydroxymethyl group or a group of ##STR2## wherein R.sub.1 is a hydrogen atom or an alkyl group having 1 to 3 carbon atoms; and R.sub.Type: GrantFiled: August 20, 1997Date of Patent: September 21, 1999Assignee: Nippon Suisan Kaisha, Ltd.Inventors: Jiro Takeo, Shinya Yamashita, Keiji Wada, Yoshiyuki Chiba
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Patent number: 5916922Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.Type: GrantFiled: November 24, 1997Date of Patent: June 29, 1999Assignee: Eli Lilly and CompanyInventors: Theodore Goodson, Jr., Richard Waltz Harper, David Kent Herron
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Patent number: 5905127Abstract: Mesogens are provided based on substituted unsaturated carboxylic acids such as acrylic and methacrylic acid. Substitution of a variety of hydrophobic tails onto the carboxylic acid or acid derivative via the vinyl carbon proximal to the carbonyl of the carboxylic acid results in mesogens that are capable of forming thermotropic and single-phase lyotropic mesophases over a broad range of compositions. The mesophases can be polymerized to lock in the ordered phases.Type: GrantFiled: April 8, 1997Date of Patent: May 18, 1999Assignee: The University of Southern MississippiInventors: Robert Y Lochhead, Lon J Mathias
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Patent number: 5891995Abstract: The present invention is directed to a novel "handle" for solid phase peptide synthesis. The handles can be converted from a stable form to a labile form, allowing for cleavage of a peptide amide from the support after synthesis under mild conditions, and after deprotection of the amino acid side chains. The handles are based on a substituted benzhydrylamine skeleton.Type: GrantFiled: October 30, 1997Date of Patent: April 6, 1999Inventors: Michal Lebl, Marcel Patek
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Patent number: 5889058Abstract: Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof.Type: GrantFiled: November 3, 1994Date of Patent: March 30, 1999Assignee: Celltech LimitedInventors: John Robert Porter, Thomas Andrew Millican, John Richard Morphy, Nigel Robert Arnold Beeley
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Patent number: 5872282Abstract: A family of compounds has been found to be useful for right-shifting hemoglobin towards a low oxygen affinity state. The compounds are capable of acting on hemoglobin in whole blood. In addition, the compounds can maintain the oxygen affinity in blood during storage and can restore the oxygen affinity of outdated blood.Type: GrantFiled: March 13, 1998Date of Patent: February 16, 1999Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Gajanan Joshi, Ramnarayan Randad
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Patent number: 5852199Abstract: The present invention provides a novel carbamazepine hydrazide compound suitable for covalent attachment to a polymer particle reagent, having the general formula ##STR1## The present invention provides a novel carbamazepine acid compound suitable for attachment to proteins for the production of carbamazepine immunogens. The carbamazepine antigen of the present invention has the following general structure: ##STR2## where X is C.dbd.O, CH.sub.2 or SO.sub.2 ; Y is C.dbd.O, CH.sub.2, SO.sub.2 ; R is an alkyl and P is a protein or a hapten.Type: GrantFiled: July 25, 1997Date of Patent: December 22, 1998Assignee: Dade Behring Inc.Inventor: Chengrong Wang
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Patent number: 5849951Abstract: A method for the preparation of a compound of formula (I) ##STR1## wherein X is hydrogen; Y is (i) a group --CO.sub.2 R.sub.5 wherein R.sub.5 is a carboxyl protecting group or (ii) a group --CONR.sub.6 OR.sub.7 wherein R.sub.6 is an amino protecting group and R.sub.7 is a hydroxyl protecting group; and S.sub.1, S.sub.2, S.sub.3 and S.sub.4 each represent covalently bound moieties which are substantially non-reactive with the reaction components (II), (III), or (IV) defined below, which method comprises causing the co-condensation in a liquid organic medium of a carboxylic acid reaction component of formula (II); an aldehyde of formula (IIIA); ammonia; and an isonitrile reaction component of formula (IV): ##STR2## wherein Y, S.sub.1, S.sub.2, S.sub.3 and S.sub.4 are as defined with respect to formula (I).Type: GrantFiled: August 29, 1997Date of Patent: December 15, 1998Assignee: British Biotech Pharmaceuticals LimitedInventors: Christopher David Floyd, Mark Whittaker
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Patent number: 5834518Abstract: Human skin is depigmented or bleached by applying thereto a compound of formula (1): ##STR1## wherein X represents COOH or the ring: ##STR2## wherein Z.sub.1, Z.sub.2 and Z.sub.3, independently of each other, are H, OR or R, R representing an optionally substituted saturated or unsaturated, linear or branched C.sub.1 -C.sub.8 -alkyl radical, or a salt, a metal complex or an ester of the compound.Type: GrantFiled: July 24, 1997Date of Patent: November 10, 1998Assignee: L'OrealInventors: Jean-Baptiste Galey, Laurent Marrot, Catherine Causse
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Patent number: 5804581Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formula: ##STR1## wherein T is a substituent and R.sup.24 is a substituted amide moiety. These compounds are useful for inhibiting matrix metalloproteases and, therefore, combating conditions to which MMP's contribute, such as osteoarthritis, rheumatoid arthritis, septic arthritis, periodontal disease, corneal ulceration, proteinuria, aneurysmal aortic disease, dystrophobic epidermolysis, bullosa, conditions leading to inflammatory responses, osteopenias mediated by MMP activity, tempera mandibular joint disease, demyelating diseases of the nervous system, tumor metastasis or degenerative cartilage loss following traumatic joint injury, and coronary thrombosis from athrosclerotic plaque rupture. The present invention also provides pharmaceutical compositions and methods for treating such conditions.Type: GrantFiled: May 15, 1997Date of Patent: September 8, 1998Assignee: Bayer CorporationInventor: Donald J. Wolanin
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Patent number: 5795612Abstract: Novel aspartyldipeptideamide derivatives of formula (I):L--Asp--X--NH--C*HR.sub.1 R.sub.2and salts thereof, wherein X is a D-.alpha.-amino acid residue or a DL-.alpha.-amino acid residue selected from the group consisting of D-alanine, D-.alpha.-aminobutyric acid, D-norvaline, D-valine, D-norleucine, D-leucine, D-isoleucine, D-alloisoleucine, D-t-leucine, D-serine, D-O-methylserine, D-threonine, D-O-methylthreonine, D-allothreonine, D-O-methylallothreonine, D-phenyl glycine and D- or DL furyl glycine, or X is a cyclic or non-cyclic .alpha., .alpha.-dialkyl amino acid residue having 3 to 6 carbon atoms; R.sub.1 is a linear or branched alkyl group having 1 to 6 carbon atoms or an alkoxymethyl group having 2 to 7 carbon atoms in the alkoxy portion; R.sub.Type: GrantFiled: December 28, 1995Date of Patent: August 18, 1998Assignee: Ajinomoto Co., Inc.Inventors: Tadashi Takemoto, Yusuke Amino, Ryoichiro Nakamura
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Patent number: 5783593Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.Type: GrantFiled: April 29, 1996Date of Patent: July 21, 1998Assignee: Abbott LaboratoriesInventors: William R. Baker, Saul H. Rosenberg, Anthony K. L. Fung, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, Stephen J. O'Connor, Rajnandan N. Prasad, Wang Shen, David M. Stout, Gerard M. Sullivan
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Patent number: 5777158Abstract: The novel non-hygroscopic crystals of p-aminomethylbenzoic acid can be obtained by heating hygroscopic crystals of p-aminomethylbenzoic acid with keeping the hygroscopic crystals in contact with moisture to transit the hygroscopic crystals to non-hygroscopic crystals.The non-hygroscopic crystals of p-aminomethylbenzoic acid can be particularly advantageously handled in the atmosphere as compared with the conventional hygroscopic crystals. Especially when the p-aminomethylbenzoic acid is used for the non-aqueous reaction, the crystals of the invention are exceptionally advantageous from the viewpoints of removal of moisture and humidity control.Type: GrantFiled: August 26, 1997Date of Patent: July 7, 1998Assignee: Showa Denko K.K.Inventors: Motoo Miura, Hideo Miyata, Kohei Morikawa
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Patent number: 5776888Abstract: Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.Type: GrantFiled: February 7, 1997Date of Patent: July 7, 1998Assignee: Emisphere Technologies, Inc.Inventors: Andrea Leone-Bay, Eric Wang, Donald J. Sarubbi, Harry Leipold
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Patent number: 5719182Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: May 16, 1995Date of Patent: February 17, 1998Assignee: SmithKline Beecham CorporationInventors: Russell Donovan Cousins, John Duncan Elliott, Maria Amparo Lago, Jack Dale Leber, Catherine Elizabeth Peishoff
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Patent number: 5719306Abstract: The present invention provides compounds of the formula Ar.sup.1 --Q--Ar.sup.2 --Y--R--Z and pharmaceutically acceptable salts thereof wherein Ar.sup.1 and Ar.sup.2 are optionally substituted aryl moieties, Z is an optionally substituted nitrogen-containing moiety which may be an acyclic, cyclic or bicyclic amine or an optionally substituted monocyclic or bicyclic nitrogen-containing heteroaromatic moiety; Q is a linking group capable of linking two aryl groups; R is an alkylene moiety; Y is a linking moiety capable of linking an aryl group to an alkylene moiety and wherein Z is bonded to R through a nitrogen atom. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD and asthma.Type: GrantFiled: June 6, 1995Date of Patent: February 17, 1998Assignee: G.D. Searle & Co.Inventors: Nizal Samuel Chandrakumar, Barbara Baosheng Chen, Michael Clare, Bipinchandra Nanubhai Desai, Stevan Wakefield Djuric, Stephen Hermann Docter, Alan Frank Gasiecki, Richard Arthur Haack, Chi-Dean Liang, Julie Marion Miyashiro, Thomas Dale Penning, Mark Andrew Russell, Stella Siu-tzyy Yu
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Patent number: 5717109Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.Type: GrantFiled: July 10, 1995Date of Patent: February 10, 1998Assignee: Eli Lilly and CompanyInventors: M. Brian Arnold, Thomas J. Bleisch, David R. Helton, Mary Jeanne Kallman, Paul L. Ornstein, Darryle D. Schoepp, Joseph P. Tizzano
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Patent number: 5684131Abstract: The present invention is directed to a novel "handle" for solid phase peptide synthesis. The handles can be converted from a stable form to a labile form, allowing for cleavage of a peptide amide from the support after synthesis under mild conditions, and after deprotection of the amino acid side chains. The handles are based on a substituted benzhydrylamine skeleton.Type: GrantFiled: July 5, 1994Date of Patent: November 4, 1997Inventors: Michal Lebl, Marcel Patek
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Patent number: 5679711Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoalkanoate salts and substituted N,N-substituted-aminoalkanoate salts.Type: GrantFiled: June 7, 1995Date of Patent: October 21, 1997Assignee: FHJ Scientific, Inc.Inventors: Delton R. Carrell, Edward J. Cragoe, Jr.
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Patent number: 5631401Abstract: The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful in inhibiting protein farnesyltransferase and the farnesylation of the oncogene protein Ras or inhibiting de novo squalene production resulting in the inhibition of cholesterol biosynthesis, processes for the preparation of the compounds of the invention in addition to intermediates useful in these processes, a pharmaceutical composition, and to methods of using such compounds.Type: GrantFiled: January 24, 1995Date of Patent: May 20, 1997Assignee: Abbott LaboratoriesInventors: Herman H. Stein, William R. Baker, Anthony K. L. Fung, Saul H. Rosenberg, Todd W. Rockway, Stephen A. Fakhoury, David S. Garvey, B. Gregory Donner, William J. McClellan, Stephen J. O'Connor, Rajnandan Prasad, Wang Shen, Gerard M. Sullivan
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Patent number: 5585391Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoacetate salts and substituted N,N-substituted-aminoacetate salts.Type: GrantFiled: October 8, 1993Date of Patent: December 17, 1996Assignee: FHJ Scientific, Inc.Inventors: Delton R. Carrell, Edward J. Cragoe, Jr.
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Patent number: 5565430Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukinprotease activity. The compounds, .alpha.-substituted acetamides a ##STR1## wherein: R.sub.2 =H or alkyl;R.sup.3 =halo, O(CO).sub.0-1 aryl, OPOR.sup.4 R.sup.5 ; ##STR2## where R.sup.4 and R.sup.5 =aryl;R.sup.6 =H, aryl or aralkyl;R.sup.7 =independently selected from R.sup.6, CF.sub.3 and CF.sub.2 CF.sub.3 ;R.sup.1 =R.sup.6 -CO, heteroaryl-CO, heteroaralkyl-CO and amino acid.Type: GrantFiled: August 2, 1994Date of Patent: October 15, 1996Assignee: Sterling Winthrop Inc.Inventors: Roland E. Dolle, Todd L. Graybill
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Patent number: 5541228Abstract: New melatonergic agents are phenyl alkanyl or phenyl alkyl substituted carboxamides and ureas of Formula I: ##STR1## wherein: R.sub.1 =C.sub.1-3 alkyl, allyl, C.sub.3-6 cycloalkyl substituted C.sub.1-4 alkyl;R.sub.2 =hydrogen, halogen or C.sub.1-4 alkoxy;R.sub.3 =hydrogen or C.sub.1-4 alkyl;R.sub.4 =C.sub.1-4 alkyl, C.sub.1-4 alkyl substituted amino, carboxylic acid substitutedC.sub.1-4 alkyl or C.sub.3-6 cycloalkyl, C.sub.3-6 cycloalkyl, or straight or branched chain C.sub.2-4 alkenyl;A=a linear C.sub.2-4 alkanediyl or alkenediyl chain, provided that A not be --CH.sub.2 CH.sub.2 -- when X is a bond; andX=a covalent bond or oxygen.Type: GrantFiled: March 8, 1995Date of Patent: July 30, 1996Assignee: Bristol-Myers Squibb Co.Inventors: Katherine S, Takaki, George N. Karageorge, Daniel J. Keavy, Michael F. Parker, Brett T. Watson
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Patent number: 5514716Abstract: This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.Type: GrantFiled: February 25, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop, Inc.Inventors: Madhusudhan R. Gowravaram, Jeffrey Johnson, Ewell R. Cook, Robert C. Wahl, Alan M. Mathiowetz, Bruce E. Tomczuk, Ashis K. Saha
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Patent number: 5514808Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoacetate salts and substituted N,N-substituted-aminoacetate salts.Type: GrantFiled: August 25, 1994Date of Patent: May 7, 1996Assignee: FHJ Scientific, IncInventors: Delton R. Carrell, Edward J. Cragoe, Jr.
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Patent number: 5508306Abstract: This invention relates to novel aromatic amine compounds having the structure: ##STR1## where each W, Z.sup.1 and Z.sup.2 is independently H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, OH, F, Cl, Br, I, NO.sub.2, CN, SO.sub.2 NHR.sup.3, NR.sup.4.sub.2, CONR.sup.3.sub.2, COR.sup.5 ; where each R.sup.1 and R.sup.2 is independently H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where each X and Y is independently CH.sub.2, NR.sup.4, S, S.dbd.O, SO.sub.2 ; where n is 0, 1 or 2; where each p and q is independently 1 or 2; where R.sup.3 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl; where R.sup.4 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or COR.sup.3 ; and where R.sup.5 is H, C.sub.1 -C.sub.6 straight or branched chain alkyl or phenyl, C.sub.1 -C.sub.6 straight or branched chain alkoxy or OH.Type: GrantFiled: September 9, 1993Date of Patent: April 16, 1996Assignee: Synaptic Pharmaceutical CorporationInventors: George Chiu, Charles Gluchowski
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Patent number: 5488132Abstract: The invention includes selected novel optically active .alpha.-amino ketones which either are themselves useful or are intermediates for the preparation of known ketomethylene pseudopeptides useful as antibiotics, antibiotic enhancers, or enzyme inhibitors. Further, the present invention provides a method for dehydrogenation/asymmetrical hydrogenation to obtain essentially pure antipodes of ketomethylene pseudopeptides having two chiral centers.Type: GrantFiled: April 22, 1994Date of Patent: January 30, 1996Assignee: Monsanto CompanyInventor: John J. Talley
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Patent number: 5463083Abstract: 2,5-Diaryl tetrahydrofurans, 2,5-diaryl tetrahydrothiophenes, 1,3-diaryl cyclopentanes are disclosed that reduce the chemotaxis and respiratory burst leading to the formation of damaging oxygen radicals of polymorphonuclear leukocytes during an inflammatory or immune response. The compounds exhibit this biological activity by acting as PAF receptor antagonists, by inhibiting the enzyme 5-lipoxygenase, or by exhibiting dual activity, i,e., by acting as both a PAF receptor antagonist and inhibitor of 5-lipoxygenase. Also disclosed is a method to treat disorders mediated by PAF and/or leukotrienes that includes administering an effective amount of one or more of the above-identified compounds or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable carrier, to a patient in need of such therapy.Type: GrantFiled: January 6, 1994Date of Patent: October 31, 1995Assignee: Cytomed, Inc.Inventors: Tesfaye Biftu, Xiong Cai, Sajjet Hussion, Gurmit Grewal, T. Y. Shen
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Patent number: 5439925Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function. Use is in human and veterinary medicine and in cosmetics.Type: GrantFiled: December 16, 1993Date of Patent: August 8, 1995Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)Inventors: Jean-Michel Bernardon, Willliam R. Pilgrim
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Patent number: 5436369Abstract: Certain novel alicyclic compounds are effective phospholipase A.sub.2 (PLA.sub.2) inhibitors.Type: GrantFiled: February 23, 1994Date of Patent: July 25, 1995Assignee: Bristol-Myers Squibb CompanyInventors: Joanne J. Bronson, Katharine M. Greene, Muzammil M. Mansuri, Stanley V. D'Andrea, F. Ivy Carroll, Anita Lewin