Oxy Patents (Class 562/451)
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Patent number: 6265604Abstract: The compound of the present invention (R)-3-hydroxy-3-(2-phenylethyl)-hexanoic acid is an intermediate in the preparation of the anti-AIDS compound, [R-(R*,R*)]-N-[3-[1-5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl]propyl]phenyl]-5-(trifluoromethyl)-2-pyridinesulfonamide.Type: GrantFiled: February 28, 2000Date of Patent: July 24, 2001Assignee: Pharmacia & Upjohn CompanyInventors: James R. Gage, Robert Charles Kelly, Bradley D. Hewitt
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Patent number: 6251925Abstract: The present invention relates to therapeutic biaryl derivatives of formula (I), and pharmaceutically acceptable derivatives thereof wherein R1 is a phenyl, naphthyl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1-6alkoxy, C1-6alkyl, nitro, cyano, hydroxymethyl, trifluoromethyl, —NR6R6, and —NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1-6alkyl; X is oxygen, sulfur, —NH, or —NC1-4alkyl; R3 is cyano, tetrazol-5-yl, or —CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, —CO2H, —CO2C1-6alkyl, cyano, tetrazol-5-yl, halogen, trifluoromethyl, or C1-6alkoxy, or, when R4 and R5 are bonded to adjacent carbon atoms, R4 and R5 may, together with the carbon atoms to which they are bonded, form a fused 5 or 6 membered ring optionally containing one or two nitrogen, oxygen,Type: GrantFiled: December 13, 2000Date of Patent: June 26, 2001Assignee: Glaxo Wellcome Inc.Inventors: Kelly Horne Donaldson, Barry George Shearer, David Edward Uehling
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Patent number: 6252104Abstract: A naphthol derivative represented by the general formula (I), [wherein Y and Y′ indicate —(CONH)n—X or —COR; X is a phenyl group, a naphthyl group, an anthraquinonyl group, a benzimidazolonyl group or a carbazolyl group; R is a hydroxyl group, an alkoxy group having 1 to 6 carbon atoms, a halogen atom, a benzyloxy group, a phenyloxy group or a phenacyloxy group; R2 is a hydrogen atom, an alkaline metal, an alkyl group having 1 to 6 carbon atoms, an acyl group having 1 to 6 carbon atoms or a phenylalkyl group; Z is a group selected from the group consisting of a hydrogen atom, a halogen atom, a nitro group, a nitroso group and an amino group (Z may be substituted on any ring of the naphthalene ring); and n is an integer of 1 or 2; provided that R2 and Z do not simultaneously indicate a hydrogen atom when both R simultaneously indicate a hydroxyl group], and a process for producing the same.Type: GrantFiled: December 12, 1996Date of Patent: June 26, 2001Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Shigeru Ito, Kenji Minami, Masaya Kitayama
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Patent number: 6242492Abstract: The use of a novel mono-cationic salt of N,N′-bis(2-hydroxybenzyl)ethylenediamine-N,N′-diacetic acid (HBED) in iron chelating therapy is disclosed. In particular, the invention relates to the subcutaneous use of a mono cationic salt of HBED for treating a human with a disease treatable by an iron chelator such as iron overload, especially transfusional iron overload.Type: GrantFiled: December 21, 1999Date of Patent: June 5, 2001Inventor: Raymond J. Bergeron, Jr.
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Patent number: 6197817Abstract: Disclosed are compounds of the formula: R represents hydrogen or is a C-3 to C-6 cycloalkyl or C-4 to C-10 straight or branched carbon chain alkyl-cycloalkyl or a group —B—D, where B is C-2 to C-10 straight or branched carbon chain alkyl and D is hydroxy or alkyloxy or 2,3-dihydroxypropyl or 2,3-dialkyloxypropyl or 2,2-dialkyl-1,3-dioxolane-5-methyl, where alkyl is C-1 to C-10 straight or branched carbon chain; W represents CH(CH3)CH2—, C(CH3)2CH2—; Z represents hydrogen, —NHCOR2, —NHCONR2R3 or —NHSO2R2 or —NHSO2NR2R3 or —NHCOOR4 wherein R4 is alkyl of from 1 to about 6 carbon atoms, alkoxyalkyl wherein the alkyl groups may be the same or different and contain from 1 to about 6 carbon atoms, alkoxyaryl, cycloalkyl of from 3 to about 8 carbon atoms.Type: GrantFiled: January 22, 1999Date of Patent: March 6, 2001Assignee: Selectus Pharmaceuticals, Inc.Inventors: William L. Matier, Shyam Patil
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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: 6160013Abstract: 14-Aza analogs of PGF.sub.2.alpha., PGD.sub.2, and PGE.sub.2 and methods of their use in treating glaucoma and ocular hypertension are disclosed.Type: GrantFiled: November 30, 1999Date of Patent: December 12, 2000Assignee: Alcon Laboratories, Inc.Inventor: Robert D. Selliah
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Patent number: 6136842Abstract: Products of formula (I), wherein n is 0 or 1, R.sub.1 is particularly phenyl or biphenyl optionally substituted particularly by benzyloxy, dioxol or halogen, R.sub.2 is particularly hydrogen or methyl substituted particularly by indolyl, phenylthio or phenyl, which may in turn be substituted, and A is carboxy, tetrazolyl or substituted alkyl as well as all salts and isomers thereof, are disclosed.Type: GrantFiled: January 12, 1999Date of Patent: October 24, 2000Assignee: Hoechst Marion RousselInventors: Pierre Deprez, Jacques Dumas, Marie-Claude Fournie-Zaluski, Jacques Guillaume, Bernard Pierre Roques
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Patent number: 6114386Abstract: A sialidase inhibitor of the shown formula I: ##STR1## where dashed lines d.sub.1 and d.sub.2, X.sub.1, R.sub.1, R.sub.2, R.sub.6, R.sub.3, R.sub.4 and R.sub.5 are as described in the specification; or an analog, pharmaceutically acceptable salt, or derivative of the inhibitor, with the proviso that the inhibitor is not HANBA GBA or Neu5Ac2en. The inhibitor in a composition with a pharmaceutically acceptable carrier. Methods of making a pharmaceutical composition of an acceptable carrier and the inhibitor. Methods of inhibiting sialidase and methods of treating and preventing bacterial or trypanosomal infection using the inhibitor.Type: GrantFiled: October 14, 1997Date of Patent: September 5, 2000Assignee: University of AlabamaInventors: Ming Luo, Clinton L. White
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Patent number: 6100258Abstract: Compounds antagonistic of the pain enhancing effects of prostaglandins are disclosed. The compounds comprise an optionally-substituted A ring with a --CH(R.sup.3)N(R.sup.2)B--R.sup.1 and --OD groups positioned in a 1,2 relationship to one another on ring carbon atoms. The 3-position ring-atom is not substituted. B is also an optionally-substituted ring and the group R.sup.1 is positioned on B in a 1,3 or 1,4 relationship with the --CH(R.sup.3)N(R.sup.2)-- linking group. R.sup.1, R.sup.2 and R.sup.3 and D can be a number of different organic or halogen moieties. N-oxides of --NR.sup.2 and S-oxides of sulphur containing rings are disclosed as are processes for the preparation of the compounds, intermediates in their preparation, pharmaceutical compositions containing them, and their use as therapeutic agents.Type: GrantFiled: December 16, 1997Date of Patent: August 8, 2000Assignee: Zeneca LimitedInventor: Gloria Anne Breault
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Patent number: 6090850Abstract: A class of novel naphthyl glyoxamide compounds of formula (I) is disclosed together with a process for making the novel naphthyl glyoxamide compounds and 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: June 9, 1998Date of Patent: July 18, 2000Assignee: Eli Lilly and CompanyInventors: Theodore Goodson, Jr., David K. Herron
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Patent number: 6072042Abstract: The present invention provides a bis (aminocarbonylnaphthol) derivative which is useful as a raw material for novel azo pigments by bisamidation of each one carboxyl group of two 2-hydroxynaphthalene-3,6-dicarboxylic acids using an aliphatic or aromatic diamine.Type: GrantFiled: June 5, 1998Date of Patent: June 6, 2000Assignee: Kabushiki Kaisha Ueno Seiyaku Oyo KenkyujoInventors: Ryuzo Ueno, Masaya Kitayama, Kenji Minami, Hiroyuki Wakamori, Katsunori Tanikawa, Mariko Tanigawa
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Patent number: 6043279Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.Type: GrantFiled: February 12, 1997Date of Patent: March 28, 2000Assignee: Ligand Pharmaceuticals, IncorporatedInventors: Marcus F. Boehm, Richard A. Heyman
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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: 6020518Abstract: An object of the present invention is to provide a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative via efficient and industrially utilizable steps.The present invention provides a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative represented by the general formula (2) given below which comprises hydrolyzing an .alpha.-amino-.alpha.', .alpha.'-dihaloketone derivative of the general formula (1) given below in the presence of a base, followed by protecting the amino group or without protecting the same.Type: GrantFiled: May 14, 1999Date of Patent: February 1, 2000Assignee: Kaneka CorporationInventors: Shingo Matsumoto, Kazuhiko Matsuo, Tadashi Sugawa, Tadashi Moroshima, Kenji Inoue
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Patent number: 5998654Abstract: Trienoic compounds having activity as antagonists for retinoic acid receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.Type: GrantFiled: July 25, 1997Date of Patent: December 7, 1999Assignee: Ligand Pharmaceuticals IncorporatedInventors: Marcus F. Boehm, Lin Zhang
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Patent number: 5962688Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.Type: GrantFiled: August 8, 1997Date of Patent: October 5, 1999Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Paul N. Devine, Ulf H. Dolling, Lisa F. Frey, Richard D. Tillyer, David M. Tschaen, Yoshiaki Kato
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Patent number: 5958981Abstract: A .gamma.-diketone compound represented by the following formula (I) and a pharmaceutically acceptable salt and solvate thereof having platelet aggregation inhibitory activity is disclosed: ##STR1## wherein B is --Z--(CH.sub.2).sub.q COOR.sup.Type: GrantFiled: March 27, 1998Date of Patent: September 28, 1999Assignee: Meiji Seika Kabushiki KaishaInventors: Tomoaki Miura, Eiki Shitara, Shokichi Ohuchi, Kiyoaki Katano
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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: 5907043Abstract: The present invention relates to pyrrolidine derivatives, and more particularly to the compound (S)-1-?(S)-2-(4-methoxybenzamido)-3-methylbutyryl!-N-?(S)-2-methyl-1-(trif luoroacetyl)propyl!pyrrolidine-2-carboxamide, shown by formula I, and solvates thereof. The present invention also provides pharmaceutical compositions, intermediates and methods of preparation of the compound. The compound of formula I is an inhibitor of human neutrophil elastase and is useful in the treatment of diseases in which the enzyme is implicated, such as, for example, emphysema and acute respiratory distress syndrome (ARDS).Type: GrantFiled: January 27, 1998Date of Patent: May 25, 1999Assignee: Zeneca LimitedInventors: Stephen John Pegg, George Joseph Sependa, Elwyn Peter Davies, Chris Allan Veale
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Patent number: 5883293Abstract: Novel backbone cyclized peptide analogs are formed by means of bridging groups attached via the alpha nitrogens of amino acid derivatives to provide novel non-peptidic linkages. Novel building units disclosed are N.sup..alpha. (.omega.-functionalized) amino acids constructed to include a spacer and a terminal functional group. One or more of these N.sup..alpha. (.omega.-functionalized) amino acids are incorporated into a peptide sequence, preferably during solid phase peptide synthesis. The reactive terminal functional groups are protected by specific protecting groups that can be selectively removed to effect either backbone-to-backbone or backbone-to-side chain cyclizations. The invention is exemplified by backbone cyclized bradykinin antagonists having biological activity. Further embodiments of the invention are somatostatin analogs having one or two ring structures involving backbone cyclization.Type: GrantFiled: December 5, 1996Date of Patent: March 16, 1999Assignees: Peptor Ltd., Yissum Research Development Co. of the Hebrew UniversityInventors: Chaim Gilon, Doron Eren, Irina Zeltser, Alon Seri-Levy, Gal Bitan, Dan Muller
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Patent number: 5874467Abstract: The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## and their salts. The invention additionally relates to processes and intermediates for preparing these compounds and compositions containing them for controlling animal pests and harmful fungi.Type: GrantFiled: July 31, 1996Date of Patent: February 23, 1999Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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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: 5831115Abstract: The present invention provides a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, which are useful for 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: April 11, 1996Date of Patent: November 3, 1998Assignee: Abbott LaboratoriesInventors: David L Arendsen, William R. Baker, Stephen A Fakhoury, Anthony K. L. Fung, David S. Garvey, William J. McClellan, Stephen J. O'Connor, Rajnandan N. Prasad, Todd W. Rockway, Saul H. Rosenberg, Herman H. Stein, Wang Shen, David M. Stout, Gerard M. Sullivan, David J. Augeri
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Patent number: 5827887Abstract: Novel compounds of the formula ##STR1## wherein the substituents are defined as in the application and their salts with non-toxic, pharmaceutically acceptable acids and bases having 5-.alpha.-reductase inhibiting activity and a process and intermediates for their preparation.Type: GrantFiled: July 31, 1996Date of Patent: October 27, 1998Assignee: Roussel UclafInventors: Jean-Fran.cedilla.ois Gourvest, Dominique Lesuisse, Jean-Georges Teutsch
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Patent number: 5795914Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## wherein the substituents are defined in the specification.Type: GrantFiled: June 5, 1995Date of Patent: August 18, 1998Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5780506Abstract: The present invention relates to phenylacetic acid derivatives of the formula I ##STR1## and their salts. The invention additionally relates to processes and intermediates for preparing these compounds and compositions containing them for controlling animal pests and harmful fungi.Type: GrantFiled: July 31, 1996Date of Patent: July 14, 1998Inventors: Herbert Bayer, Hubert Sauter, Ruth Muller, Wassilios Grammenos, Albrecht Harreus, Reinhard Kirstgen, Franz Rohl, Eberhard Ammermann, Gisela Lorenz
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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: 5739163Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: March 8, 1996Date of Patent: April 14, 1998Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Gary Avonn Cain, Charles Joseph Eyermann, Richard Eric Olson
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Patent number: 5726165Abstract: A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, or solvate thereof, wherein,R.sup.o represents an aryl group, optionally substituted;X represents O or S;R.sup.1 and R.sup.1a each independently represents hydrogen or an alkyl group;R.sup.2 represents OCH.sub.2 CO.sub.2 H, or an ester or amide thereof, or R.sup.2 represents a moiety of formula (b): ##STR2## wherein R.sup.4 represent hydrogen, alkyl, hydroxyalkyl, arylalkyl, aralkyloxyalkyl or cycloalkyl and R.sup.5 represent hydroxy, alkoxy, arylalkyloxy, hydroxyalkyloxy, alkoxyalkyloxy, arylalkoxyalkyloxy, cycloalkyloxy, hydrogen, alkyl, substituted alkyl, cycloalkyl, aryl, arylalkyl, arylalkyloxyalkyl or R.sup.5 together with OR.sup.4 represents O(CH.sub.2).sub.n O wherein n is 2, 3 or 4; andR.sup.3 represents hydrogen, halogen, alkyl or alkoxy or R.sup.3 together with R.sup.Type: GrantFiled: June 5, 1995Date of Patent: March 10, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Lee James Beeley, Mervyn Thompson, David Kenneth Dean, Nikesh Rasiklal Kotecha, John Michael Berge, Robert William Ward
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Patent number: 5723489Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: May 7, 1996Date of Patent: March 3, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
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Patent number: 5719152Abstract: A tricyclic quinoxalinedione derivative represented by the formula 1: ##STR1## wherein X represents hydrogen, alkyl, halogen, cyano, trifluoromethyl, or nitro;R.sup.1 represents hydrogen, alkyl, cycloalkyl, or cycloalkylalkyl;G represents --CONR.sup.2 -- or --NR.sup.2 CO--, wherein R.sup.2 represents hydrogen or alkyl;J represents an acidic group or a group which is convertible thereto in vivo;E represents an basic group or a group which is convertible thereto in vivo;Y represents a single bond, alkylene, alkenylene, substituted alkylene, or Y.sup.1 --Q--Y.sup.2, wherein Y.sup.1 represents a single bond or alkylene, Y.sup.2 represents alkylene, and Q represents a heteroatom selected from oxygen or sulfur;Z represents alkylene,or a pharmaceutically acceptable salt thereof, these compounds are selective antagonists of glycine binding site of the NMDA receptor.Type: GrantFiled: March 6, 1996Date of Patent: February 17, 1998Assignee: Sumitomo Pharmaceuticals Co., Ltd.Inventors: Ryu Nagata, Norihiko Tanno, Toru Kodo, Hiroshi Yamaguchi, Nobuyuki Ae
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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: 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: 5698692Abstract: A compound represented by the general formula (I) and a pharmaceutically acceptable salt and solvate thereof having an effect for inhibiting the agglutination of platelets is disclosed: ##STR1## wherein R.sup.1 represents a group --W--(CH.sub.2).sub.i --COOR.sup.3,R.sup.2 represents a hydrogen atom or a group --W--(CH.sub.2).sub.i --COOR.sup.3 or --OR.sup.4,X represents --CH.dbd. or --N.dbd.,Y represents(i) a group --(CO).sub.k --N(R.sup.5)--Z--, wherein Z represents a bond or a group --(CH.sub.2).sub.m --CO-- or a group --(CH.sub.2).sub.m --CHR.sup.6 --,(ii) a group --(CH.sub.2).sub.m --N(R.sup.5)--(CO).sub.k --, or(iii) a group --(CO).sub.k --Het, wherein Het represents a five- or six-membered heterocyclic ring comprising a nitrogen atom,A represents(i) the following groups (II), (III) or (IV) ##STR2## B represents a bond, C.sub.1-6 alkylene or C.sub.2-6 alkenylen.Type: GrantFiled: October 18, 1996Date of Patent: December 16, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Kiyoaki Katano, Shokichi Ohuchi, Eiki Shitara, Masaro Shimizu, Kazue Yaegashi, Tomoaki Miura, Yasuko Isomura, Hiroyuki Iida, Midori Ishikawa, Kenji Asai, Emiko Hatsushiba, Mami Kawaguchi, Takashi Tsuruoka
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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: 5663413Abstract: The invention relates to novel contrast media particularly useful for X-ray diagnostic investigations of human and animal body.Type: GrantFiled: May 24, 1995Date of Patent: September 2, 1997Assignee: Dibra S.p.A.Inventors: Fulvio Uggeri, Pier Lucio Anelli, Marino Brocchetta, Massimo Visigalli
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Method for lowering oxygen affinity of hemoglobin in redcell suspensions, in whole blood and in vivo
Patent number: 5661182Abstract: Drug compounds are used as allosteric modifiers of hemoglobin present in red blood cells. The compounds bind to only a single pair of symmetry related sites in the central water cavity of hemoglobin at the Lys 99.alpha., Arg 141.alpha., and Asn 108 .beta. residues. When one of the drug compounds is bound to hemoglobin, it will join three separate sub-units of the hemoglobin molecule and stabilize the hemoglobin in a lower oxygen affinity state. Because the compounds used in this method are either not bound by serum albumin or only interact to small degrees with serum albumin, the compounds are active in whole blood and in vivo. The process of allosterically modifying hemoglobin towards a low oxygen affinity state in whole blood and in vivo could be used in a wide variety of applications including in treatments for ischemia, heart disease, wound healing, Alzheimer's, depression, schizophrenia, adult respiratory distress syndrome (ARDS), etc.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Virginia Commonwealth UniversityInventors: Donald J. Abraham, Claude Poyart -
Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents
Patent number: 5631369Abstract: Novel processes for producing compounds of formula I ##STR1## wherein R.sup.1 and R.sup.2 each are independently C.sub.1 -C.sub.4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; andn is 2 or 3;or a pharmaceutically acceptable salt thereof employing alkylacetate solvents are provided.Type: GrantFiled: August 31, 1994Date of Patent: May 20, 1997Assignee: Eli Lilly and CompanyInventors: Douglas P. Kjell, Fred M. Perry -
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: 5606071Abstract: The present invention provides a novel process for the preparation of 5-arylhydantoins as an important intermediate of (D)-arylglycines (e.g., (D)-p-hydroxyphenyl-glycine) useful for the synthesis of semisynthetic penicillines and cephalosporins, the process comprising (i) reacting a 5-unsubstituted hydantoin compound with a halogenating agent and (ii) reacting the resulting product with a p-unsubstituted phenol compound, the hydroxy group of which may be protected, to substitute the 5-position of the hydantoin compound with the phenol compound at the para position.Type: GrantFiled: October 6, 1994Date of Patent: February 25, 1997Assignee: Showa Denko K.K.Inventor: Hiroshi Yasuda
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Patent number: 5606095Abstract: 2-Aminooxymethylenephenylacetic acid ester derivatives of the formula ##STR1## wherein Z.sub.1 and Z.sub.2 are hydrogen, halogen, hydroxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkylcarbonyl, phenoxy, nitro or cyano, or Z.sub.1 and Z.sub.2, together with the linking phenyl radical, are naphthalene or hydrogenated naphthalene, and R.sub.3 is hydrogen or C.sub.1 -C.sub.12 alkyl. The compounds of this invention may be used as the free base or as a protic acid salt and are important intermediates for the manufacture of microbicides for plant protection.Type: GrantFiled: June 5, 1995Date of Patent: February 25, 1997Assignee: Ciba-Geigy CorporationInventors: Albert Pfiffner, Stephan Trah, Hugo Ziegler
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Patent number: 5596009Abstract: A fused benzeneoxyacetic acid derivative of the formula (I): ##STR1## A is --COW, --NR.sup.4 --Y or --Z--NR.sup.4 --CONR.sup.2 R.sup.3 ; and salts thereof possess an agonistic on PGI.sub.2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertention.Type: GrantFiled: May 19, 1994Date of Patent: January 21, 1997Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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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: 5574036Abstract: Novel pharmaceutically/cosmetically-active adamantyl-substituted polycyclic acetylene compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(f): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 26, 1995Date of Patent: November 12, 1996Assignee: Centre International de Recherches Dermatologiques GaldermaInventors: Jean-Michel Bernardon, Bruno Charpenter
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Patent number: 5569677Abstract: This invention relates to a compound of formula I ##STR1## where the several groups are defined herein. These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.Type: GrantFiled: June 5, 1995Date of Patent: October 29, 1996Assignee: SmithKline Beecham CorporationInventor: Robert A. Daines
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Patent number: 5523476Abstract: A process for producing tetrafluorophthalic anhydride, which comprises chlorinating tetrachlorophthalic anhydride to obtain 3,3,4,5,6,7-hexachloro-1-[3H]-isobenzofuranone, then fluorinating it to obtain 3,4,5,6-tetrafluorophthaloyldifluoride and/or 3,3,4,5,6,7-hexafluoro-1-[3H]-isobenzofuranone, and further reacting the tetrafluorophthalolyldifluoride and/or the hexafluoro-1-[3H]-isobenzofuranone with an inorganic base or an organic acid to obtain tetrafluorophthalic anhydride.Type: GrantFiled: February 21, 1995Date of Patent: June 4, 1996Assignee: Asahi Glass Company Ltd.Inventors: Ryuji Seki, Koji Sugimoto, Seisaku Kumai
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Patent number: 5523302Abstract: This invention relates to novel compounds containing basic and acidic termini, pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.Type: GrantFiled: November 24, 1993Date of Patent: June 4, 1996Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Gary A. Cain, Charles J. Eyermann
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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.