Nitrogen In Acid Moiety Patents (Class 560/12)
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Patent number: 6310078Abstract: 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 which bind to the erythropoietin receptor and compete with the natural ligand for binding to this receptor.Type: GrantFiled: March 3, 2000Date of Patent: October 30, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Peter J. Connolly, Victor T. Bandurco, Steven K. Wetter, Sigmond Johnson, Jacqueline Bussolari, William V. Murray
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Patent number: 6300514Abstract: Pharmaceutical composition containing aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (1) and the salts thereof as active ingredient (wherein R1 is H, alkyl; R2 is COOR7, CONHOR8; E is —CONR9—, —NR9CO—, —OCO—,—COO—, —CH2—O—, —(CH2)2—, vinylene, ethynylene; J is bond, alkylene; A is H, alkyl, Ar, alkyl-OH ; R3, R4 is H, alkyl, COOR19, hydroxy, —NR20R21, Ar1 etc.); R5, R6 is H, methyl) and the novel aryl (sulfide, sulfoxide, sulfone) derivatives of the formula (I).Type: GrantFiled: January 15, 1999Date of Patent: October 9, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kanji Takahashi, Tsuneyuki Sugiura
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Patent number: 6297398Abstract: The invention concerns a method of sulphonation characterised in that it consists in contacting a nucleophile whose nucleophilic atom is a nitrogen atom with a reagent comprising by successive or simultaneous addition: a heavy sulphonyl halide (i.e. whose atomic number is not less than that of chlorine), advantageously suphonyl chloride; and an organic base both not capable of alkylation and lipid soluble; and the organic part of said sulphonyl is perfluorinated on the carbon carried by the sulphur. The invention is applicable to organic synthesis.Type: GrantFiled: November 9, 1999Date of Patent: October 2, 2001Assignee: Rhodia ChimieInventors: Virginie Pevere, Emmanuel Marx, Laurent Gilbert
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Patent number: 6291522Abstract: The invention relates to the use of cyclopentane heptan(ene)oic acid, 2-thiocarbamoyloxy and carbamoyloxy as therapeutic agents e.g. as ocular hypotensives.Type: GrantFiled: September 27, 2000Date of Patent: September 18, 2001Assignee: Allergan Sales, Inc.Inventor: Robert M. Burk
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Patent number: 6271419Abstract: The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.Type: GrantFiled: November 4, 1999Date of Patent: August 7, 2001Assignee: Rhodia ChimieInventors: Jean-Roger Desmurs, André Millet, Virginie Pevere
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Patent number: 6248781Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: October 19, 1999Date of Patent: June 19, 2001Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6239306Abstract: Compounds of the formula (I) and their salts as defined in claim 1, in which R1 is CO—Q—R8, where R8=H or R R2 and R3 are H or (C1-C4)alkyl, R4 is H, R, RO, OH, RCO, RSO2, PhSO2 R5 is RSO2, PhSO2, PhCO, RNHSO2, R2NSO2, RCO, CHO, COCOR′, CW—T—R9, CW—NR10R11, CW—N(R12)2 or R4 and R5 together are the chain (CH2)mB or —B1—(CH2)m1B— where B=SO2, m=3, 4; m1=2, 3; T and W=O, S; Q=O, S, NR13 where R13=H, R; R6=H, R, RO, RCO, ROCO, Hal, NO2, CN; R7=H, CH3; R9=R; R10, R11=H, R; N(R12)2=heterocycle A=pyrimidinyl and triazinyl radical or an analog thereof, where R=(substituted) aliphatic hydrocarbon radical, are suitable as selective herbicides. They are prepared by analogous processes via sulfonamides, some of which are new, of the formula (II) (see claim 4).Type: GrantFiled: February 1, 1999Date of Patent: May 29, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Lothar Willms, Klaus Bauer, Hermann Bieringer
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Patent number: 6235777Abstract: A benzenesulfonamide compound of the formula (I) (R1 is hydroxy, C1˜4 alkoxy, NR6R7 (each R6 and R7 is, independently, H or C1˜4 alkyl.); R2 is H, C1˜4 alkyl; R3, R4 are C1˜4 alkyl, halogen trifluoromethyl; R5 is H, C1˜4 alkyl, halogen, trifluoromethyl; Y is cis-vinylene, trans-vinylene; and the symbol (i) is single bond, double bond.), non-toxic salt thereof or cyclodextrin clathrate thereof and an antagonist of EP1 receptor which is a prostaglandin E2 receptor subtype comprising it as an active ingredient. The present invention compounds of the of the formula (I) can bind strongly to EP1 receptor which is a prostaglandin E2 receptor subtype and scarcely bind to the other receptor subtypes. Therefore, they are considered to be useful as antipyretic agents, as analgesics or as treating agent for pollakiuria having little side effect.Type: GrantFiled: May 14, 1998Date of Patent: May 22, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Shuichi Ohuchida, Yuuki Nagao, Takayuki Maruyama
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Patent number: 6229041Abstract: The present invention provides a method for preparing S-aryl cysteine. Specifically, the present invention provides enantioselective method for preparing S-aryl cysteine starting from cystine, cysteine or serine amino acid. The methods of the present invention provides S-aryl cysteine in enantiomeric excess of greater than about 96%.Type: GrantFiled: June 24, 1999Date of Patent: May 8, 2001Assignee: F. Hoffmann-La Roche AGInventors: Jack D. Brown, Hiralal N. Khatri, Peter J. Harrington, Dave A. Johnston, Robert J. Topping, Richard R. Dauer, Gary K. Rowe
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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: 6191165Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: May 30, 1997Date of Patent: February 20, 2001Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6187924Abstract: Compounds of formula (I) are useful as therapeutic agents, by virtue of having MMP and TNF inhibitory activity.Type: GrantFiled: November 12, 1998Date of Patent: February 13, 2001Assignee: Darwin Discovery, Ltd.Inventors: Andrew Douglas Baxter, David Alan Owen, John Gary Montana, Robert John Watson
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Patent number: 6177466Abstract: The present invention is related to: (i) matrix metalloproteinase inhibitors containing sulfonylamino acid derivatives of the formula (Ia): wherein R1 is hydrogen, C1-4 alkyl; R is hydrogen, C1-8 alkyl etc.; E is —CONR3—, in which R3 is hydrogen, C1-4 alkyl etc., —NR3CO—, —CO—O—, —O—CO— etc.; A is hydrogen, C1-8 alkyl, C3-7 cycloalkyl, or Ar; J is bond, C2-4 alkylene etc.; G is —(CH2)m— in which m is 2, 3 or 4, or in which R6 and R7 is hydrogen, C1-8 alkyl etc.; and non-toxic salts thereof, (ii) novel sulfonylamino acid derivatives of the formula (Ib): wherein all the symbols are the same meaning as (i); and non-toxic salts thereof, and (iii) process for the preparation of the compound of the formula (Ib). The compounds of the formula (Ia) are useful for prevention and/or treatment of diseases induced by overexpression and excess activity of MMP.Type: GrantFiled: July 29, 1996Date of Patent: January 23, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhito Sakaki, Hidekazu Kanazawa, Tsuneyuki Sugiura, Tohru Miyazaki, Hiroyukii Ohno
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Patent number: 6177462Abstract: Compounds with fungicidal and insecticidal properties having formula wherein X is N or CH; Y is O, S or NR6; A is independently hydrogen, halo, cyano, (C1-C12)alkyl, or (C1-C12)alkoxy; R1 and R6 is independently hydrogen or (C1-C4)alkyl; R2 is independently hydrogen, (C1-C12)alkyl, halo(C1-C12)alkyl, (C3-C7)cycloalkyl, (C2-C8)alkenyl, halo(C2-C8)alkenyl, (C2-C8)alkynyl, halo(C2-C8)alkynyl, aryl, aralkyl, heterocyclic, or heterocyclic(C1-C4)alkyl; R3 is independently hydrogen or (C1-C4)alkyl; R4 and R5 is independently hydrogen, (C1-C4)alkyl, aryl, aralkyl, aryl(C2-C8)alkenyl, aryl(C2-C8)alkynyl, heterocyclic, or heterocyclic(C1-C4)alkyl wherein if one of R4 and R5 is hydrogen or (C1-C4)alkyl than the other of R4 and R5 is other than hydrogen or (C1-C4)alkyl, and its enantiomers and stereoisomers and agronomically acceptable salts.Type: GrantFiled: January 26, 1999Date of Patent: January 23, 2001Assignee: Rohm and Haas CompanyInventors: Zhang Lixin, Li Zongcheng, Li Zhinian, Zhang Hong, Liu Changling, Li Bin, Steven Howard Shaber
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Patent number: 6174922Abstract: The present invention provides novel sulphonamide derivatives which are useful for potentiating glutamate receptor function in a mammal requiring treatment, processes for their preparation, and pharmaceutical compositions containing them.Type: GrantFiled: February 23, 1999Date of Patent: January 16, 2001Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Dennis Michael Zimmerman, Ana Maria Escribano
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Patent number: 6169200Abstract: The present invention provides a simple and inexpensive method for producing &agr;-hydroxy-&bgr;-aminocarboxylic acids and their esters. An ester of an N-protected &agr;-amino acid ester is converted into a &bgr;-ketosulfoxide, which is then processed with an acid to give an &agr;-ketohemimercaptal. Next, this is acylated and then processed with a base to obtain an N-protected &agr;-acyloxy-&bgr;-amino-thioester, which is then saponified to obtain an intended compound. According to the method of the present invention, it is possible to produce &agr;-hydroxy-&bgr;-aminocarboxylic acid derivatives, which are intermediates in producing various HIV protease inhibitors, renin inhibitors and carcinostatics, from a-amino acids. The method comprises reduced reaction steps, the selectivity in the method to give the intended product is high, and the yield of the product obtained is high.Type: GrantFiled: November 5, 1998Date of Patent: January 2, 2001Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Yutaka Honda, Kunisuke Izawa
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Patent number: 6166072Abstract: Described herein are compounds having the general formula: ##STR1## wherein: Ar.sup.1 and Ar.sup.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sup.1 or Ar.sup.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sup.1 and Ar.sup.Type: GrantFiled: June 29, 1999Date of Patent: December 26, 2000Assignee: Allelix Neuroscience, Inc.Inventors: Stanley Charles Bell, Michael De Vivo, Allen Hopper, Methvin Isaac, Anne O'Brien, Vassil Ilya Ognyanov, Richard Schumacher
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Patent number: 6147248Abstract: The invention relates to compounds of the formula (I) ##STR1## in which R=(subst.) alkyl or (subst.) cycloalkyl, which are suitable as intermediates for preparing herbicidal sulfonylureas. According to the invention, the compounds (I) are prepared by(a) diazotizing a compound of the formula (II) ##STR2## in the presence of an acid H.sup.+ X.sup.-, where X.sup.- is an equivalent of an anion, to give the novel compounds (diazonium salts) of the formula (III) ##STR3## (b) reacting the compound of the formula (III) in the presence of iodide ions to give the compound (IV) and ##STR4## (c) reacting the compound of the formula (IV) with an isocyanate of the formula (V)R--N.dbd.C.dbd.O (V)in which R is as defined in formula (I), to give the compound of the formula (I).Type: GrantFiled: December 23, 1998Date of Patent: November 14, 2000Assignee: Hoechst Schering AgrEvo GmbHInventors: Lothar Willms, Harald Knorr
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Patent number: 6114568Abstract: The present invention relates to a process for alkylating hindered sulfonamides useful as intermediates in the preparation of matrix metalloproteinase inhibitors.Type: GrantFiled: April 9, 1999Date of Patent: September 5, 2000Assignee: Pfizer Inc.Inventors: Brian Michael Andresen, Phillip Dietrich Hammen, Joel Michael Hawkins
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Patent number: 6093744Abstract: The instant invention is new compounds of Formula I ##STR1## their use as cerebrovascular agents in diseases such as stroke, peripheral vascular disease, restenosis, and as agents for regulating plasma cholesterol concentrations, for treating hypercholesterolemia and atherosclerosis, and for lowering the serum or plasma level of Lp(a). A pharmaceutical composition is also claimed.Type: GrantFiled: August 10, 1998Date of Patent: July 25, 2000Assignee: Warner-Lambert CompanyInventors: Helen Tsenwhei Lee, Joseph Armand Picard, William Howard Roark, Bruce David Roth, Drago Robert Sliskovic
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Patent number: 6083981Abstract: The present invention relates to compounds that are inhibitors of interleukin-1.beta. converting enzyme that have the Formula I, II, or III. ##STR1## This invention also relates to a method of treatment of stroke, inflammatory diseases, septic shock reperfusion injury, Alzheimer's disease, and shigellosis, and to a pharmaceutically acceptable composition that contains a compound that is an inhibitor of interleukin-1.beta. converting enzyme.Type: GrantFiled: April 9, 1999Date of Patent: July 4, 2000Assignee: Warner-Lambert CompanyInventors: Hamish John Allen, Kenneth Dale Brady, William Glen Harter, Elizabeth Ann Lunney, Mark Stephen Plummer, Tomi Sawyer, Aurash Shahripour, Nigel Walker
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Patent number: 6072073Abstract: The invention is directed to a process for preparing an alpha-arylated or vinylated carbonyl-containing compounds, comprising reacting a compound having a carbonyl group with an arylating or vinylating compound in the presence of a base and a transition metal catalyst. The transition metal catalyst has the formula X.sub.n M(ER.sub.1-4).sub.m, wherein X is an optional ligand, M is a group 8 transition metal, E is an element bearing a nonbonding electron pair when E is not bonded to the metal, and R is a substituent bonded to E through a carbon, nitrogen, oxygen, or sulfur atom, with the proviso that R.sub.3 cannot contain 3 aryl groups, n is an integer from 0 to 4, and m is an integer from 1-4. The process of the invention is useful for preparation of alpha-arylated or vinylated carbonyl-containing compounds which are significant in the development of pharmacologically active compounds and polymers and oligomers.Type: GrantFiled: August 18, 1999Date of Patent: June 6, 2000Assignee: Yale UniversityInventors: Motoi Kawatsura, John F. Hartwig
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Patent number: 6054457Abstract: This invention relates to new benzamide derivatives having a vasopressin antagonistic activity, etc, and represented by general formula (I): ##STR1## wherein R.sup.1 is aryl optionally substituted with lower alkoxy, etc., R.sup.2 is lower alkyl, etc.,R.sup.3 is hydrogen, etc.,R.sup.4 is lower alkoxy, etc.,R.sup.5 is hydrogen, etc.,A is NH, etc.,E is ##STR2## etc., X is --CH.dbd.CH--, --CH.dbd.N--, or S, andY is CH or N,and pharmaceutically acceptable salts thereof, to processes for preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: December 9, 1997Date of Patent: April 25, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Takehiko Ohkawa, Tatsuya Zenkoh, Hitoshi Sawada, Kentaro Sato, Hirokazu Tanaka
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Patent number: 6048896Abstract: 4-Phenyl-4-oxo-butenoic acid derivatives for use in the treatment of the human or animal body by therapy; particularly as kynurenine-3-hydroxylase inhibitors, in the prevention and/or treatment of a neurodegenerative disease wherein the inhibition of such an enzyme is needed. The present invention further comprises a selected class of the above mentioned 4-phenyl-4-oxo-butenoic acid derivatives, their pharmaceutically acceptable salts, a process for their preparation and pharmaceutical compositions containing them.Type: GrantFiled: May 4, 1998Date of Patent: April 11, 2000Assignee: Pharmacia & Upjohn S.p.A.Inventors: Antonio Giordani, Paolo Pevarello, Carmela Speciale, Mario Varasi
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Patent number: 6046355Abstract: This invention pertains to improved antiviral activity of 6,6-disubstituted-5,6-dihydropyran-2-ones caused by judicious placement of certain polar substituents at the 3 and/or 6 positions.The same substituents which enhance the cellular activity also diminish cytotoxicity further enhancing the desirable properties of these agents as antivirals.Type: GrantFiled: July 28, 1998Date of Patent: April 4, 2000Assignee: Warner-Lambert CompanyInventors: Frederick Earl Boyer, Jr., John Michael Domagala, Edmund Lee Ellsworth, Christopher Andrew Gajda, Susan Elizabeth Hagen, Harriet Wall Hamilton, Elizabeth Ann Lunney, Larry James Markoski, Josyula Venkata Nagendra Vara Prasad, Bradley Dean Tait
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Patent number: 6043247Abstract: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention also relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings.Type: GrantFiled: April 16, 1997Date of Patent: March 28, 2000Assignee: Novo Nordisk A/SInventors: Henrik Sune Andersen, Niels Peter Hundahl M.o slashed.ller, Peter Madsen
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Patent number: 6043284Abstract: The present invention is concerned with diaryl compounds of formula (I) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.Type: GrantFiled: February 5, 1998Date of Patent: March 28, 2000Assignee: Glaxo Wellcome Inc.Inventors: Richard James Arrowsmith, John Gordon Dann, Karl Witold Franzmann, Simon Teanby Hodgson, Peter John Wates
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Patent number: 6031121Abstract: Optically active N-(S-2-acetylthiomethyl-1-oxo-3-phenylpropyl)-glycine benzyl ester useful as an enkephalin inhibitory agent or ACE inhibitory agent can be produced at low cost in an industrial manner, by a method comprising subjecting optically active 2-hydroxymethyl-3-phenylpropionic acid and glycine benzyl ester to condensation to subsequently convert the hydroxyl group into an elimination group, and substituting the elimination group with an acetylthio group.Type: GrantFiled: February 16, 1999Date of Patent: February 29, 2000Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
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Patent number: 6028131Abstract: The invention relates to compounds of the formula I ##STR1## in which R is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl, --CH.sub.2 --A--R.sub.2 or a group of the formula II, ##STR2## R.sub.1 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl or a group of the formula (II),R.sub.2 is C.sub.4 -C.sub.18 alkyl, --(CH.sub.2).sub.m --COOR.sub.5 or a group of the formula III, ##STR3## R.sub.3 is hydrogen, C.sub.5 -C.sub.8 cycloalkyl or C.sub.1 -C.sub.12 alkyl,R.sub.4 is C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.8 cycloalkyl, C.sub.7 -C.sub.9 phenylalkyl or a group of the formula II or IV, ##STR4## A is S or SO, E is a direct bond, --CH.sub.2 --, --CH.sub.2 --O-- or --CH.sub.2 --NH--,G is --O-- or --NR.sub.3 --,Y is C.sub.1 -C.sub.18 alkyl, cyclohexyl, phenyl or alpha- or beta-naphthyl,R.sub.5 is C.sub.1 -C.sub.18 alkyl, andm is 1 or 2,with the provisos thateither at least one of the radicals R and R.sub.Type: GrantFiled: April 27, 1998Date of Patent: February 22, 2000Assignee: Ciba Specialty Chemicals CorporationInventors: Hans-Rudolf Meier, Gerrit Knobloch
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Patent number: 6013649Abstract: This invention is directed to proteinase (protease) inhibitors, and more particularly to thiol sulfone inhibitors for matrix metalloproteinase 13(MMP-13), compositions of proteinase inhibitors, intermediates for the syntheses of proteinase inhibitors, processes for the preparation of proteinase inhibitors and processes for treating pathological conditions associated with pathological matrix metalloproteinase activity related to MMP-13.Type: GrantFiled: July 22, 1997Date of Patent: January 11, 2000Assignee: Monsanto CompanyInventors: John N. Freskos, S. Zaheer Abbas, Gary A. DeCrescenzo, Daniel P. Getman, Robert M. Heintz, Brent V. Mischke, Joseph J. McDonald
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Patent number: 5994398Abstract: Arylsulfonamides which have the general structure: with the symbols R.sup.1, R.sup.2, R.sup.3, R.sup.4, A and n representing the groups and integers provided in the detailed description are provided herein. These compounds have activity as inhibitors of phospholipase A2, inhibitors of cytokine release and as inhibitors of neurodegeneration.Type: GrantFiled: December 11, 1996Date of Patent: November 30, 1999Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Russell E. Rydel, Eugene D. Thorsett
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Patent number: 5985900Abstract: Compounds of the formula I: ##STR1## wherein Y is O or S, Ar is an aryl group or a heteroaryl group, R is H, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, or --C(O)R.sub.1, wherein R.sub.1 is hydrogen, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, a heteroaryl group, or NR.sub.2 R.sub.3, wherein R.sub.2 and R.sub.3 independently are hydrogen, an alkyl group, a cycloalkyl group, a heterocycloalkyl group, an aryl group, or a heteroaryl group, and X is --NH--OH or --OH. Pharmaceutically acceptable prodrugs, salts and solvates of these compounds. Methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt of solvate thereof. Pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates.Type: GrantFiled: March 30, 1998Date of Patent: November 16, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven L. Bender, Melwyn A. Abreo
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Patent number: 5977173Abstract: The invention provides novel PGF analogs. In particular, the present invention relates to compounds having a structure according to the following formula: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X, Y, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof.The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using theses compounds or the compositions containing them.Type: GrantFiled: September 4, 1998Date of Patent: November 2, 1999Inventors: John August Wos, Mitchell Anthony deLong, Jack S. Amburgey, Jr., Biswanath De, Haiyan George Dai, Yili Wang
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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: 5952386Abstract: The present invention provides dihalopropene compounds of the general formula: ##STR1## wherein R.sub.1 is C.sub.1 -C.sub.10 alkyl or the like; L is C(.dbd.O)NH or the like; R.sub.2, R.sub.3 and R.sub.4 are independently halogen or the like; R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen or the like; m is an integer of 0 to 4; n is an integer of 0 to 2; X is chlorine or the like; Y is oxygen or the like; and Z is oxygen or the like, which have excellent insecticidal activity so that they are satisfactorily effective for the control of noxious insects.Type: GrantFiled: September 24, 1997Date of Patent: September 14, 1999Assignee: Sumitomo Chemical Company, LimitedInventors: Sanshiro Matsuo, Taro Hirose, Keiichi Izumi, Masaya Suzuki, Noriyasu Sakamoto, Kazunori Tsushima, Shigeru Saito, Hirotaka Takano
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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: 5859281Abstract: .beta.-Hydroxyamines and .beta.-hydroxysulfonamides are synthesized from olefin substrates by means on a catalyzed asymmetric addition reaction. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. Sulfonamides are employed as an oxidant nitrogen source for the production of .beta.-hydroxysulfonamides. Excellent yields and enantiomeric efficiencies are achieved with co-solvents containing a 50/50 (v/v) mixtures of water and organic solvent. .beta.-Hydroxyamines are obtained by deprotecting the corresponding .beta.-hydroxysulfonamides.Type: GrantFiled: May 21, 1996Date of Patent: January 12, 1999Assignee: The Scripps Research InstituteInventors: K. Barry Sharpless, Guigen Li, Han-Ting Chang
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Patent number: 5814110Abstract: Distillate fuel is treated with additives whose structure match the crystal planes of the wax which crystallizes from the fuel to produce crystals below 4000 nanometres in size, suitable additive include novel sulpho-carboxylic materials particularly their esters and amine derivatives such as the amine salts and/or amides of ortho-sulpho benzoic acid.Type: GrantFiled: November 23, 1994Date of Patent: September 29, 1998Assignee: Exxon Chemical Patents Inc.Inventors: Kenneth William Bartz, Jacqueline Dawn Bland, David Paul Gillingham, Richard Dix Kerwood, Edwin William Lehmann, Kenneth Lewtas, John Edward Maddox, Albert Rossi, Robert Dryden Tack
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Patent number: 5801271Abstract: Disclosed is a 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative, 7-(N-substituted amino)-3-hydroxy-2-phenylheptanoate derivative, and 7-(N-substituted amino)-3-benzenesulfonyloxy-2-phenylheptanoate derivative, which are quite important major intermediates for an antidepressant. The 7-(N-substituted amino)-3-oxo-2-phenylheptanoate derivative can be manufactured by condensing an enolate of phenylacetates with a 5-(N-substituted amino) pentanoate derivative.Type: GrantFiled: July 16, 1997Date of Patent: September 1, 1998Assignee: Takasago International CorporationInventors: Nobuo Seido, Takenobu Nishikawa, Tsukasa Sotoguchi, Yoshifumi Yuasa, Takashi Miura, Hidenori Kumobayashi
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Patent number: 5756545Abstract: Compounds of the formula ##STR1## wherein R.sup.1 includes alkyl, halo, nitro, amino, cyano, alkoxy, and alkoxycarbonyl; R.sup.2 is alkyl and substituted alkyl; and R.sup.3 is OH or NHOH are useful for inhibiting matrix metalloproteinase enzymes in animals, and as such, prevent and treat diseases resulting from the breakdown of connective tissues.Type: GrantFiled: April 21, 1997Date of Patent: May 26, 1998Assignee: Warner-Lambert CompanyInventors: Patrick Michael O'Brien, Drago Robert Sliskovic
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Patent number: 5736559Abstract: The invention relates to biphenyl derivatives of general formula ##STR1## wherein A to E and X are defined as in claim 1, the stereoisomers thereof, including their mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing these compounds and processes for preparing them.Type: GrantFiled: August 1, 1996Date of Patent: April 7, 1998Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Gunter Linz, Thomas Muller, Wolfgang Eisert, Johannes Weisenberger
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Patent number: 5733909Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: January 21, 1997Date of Patent: March 31, 1998Assignee: Merck Frosst Canada, Inc.Inventors: Cameron Black, Mario Girard, Daniel Guay, Zhaoyin Wang
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Patent number: 5716989Abstract: The invention relates to bicyclo?3.3.0!octane compounds of formula I, ##STR1## wherein the variable are defined in this specification, as well as their enantiomers, and their salts with physiologically compatible bases. .alpha.-, .beta.-, or .tau.-Cyclodextrin clathrates of the compounds and the compounds encapsulated with liposomes are also included. The invention is further directed to processes for production of the compounds and their pharmaceutical use.Type: GrantFiled: November 27, 1991Date of Patent: February 10, 1998Assignee: Schering AktiengesellschaftInventors: Ulrich Klar, Hartmut Rehwinkel, Helmut Vorbruggen, Karl Heinz Thierauch, Peter Verhallen
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Patent number: 5698591Abstract: A trifluoromethanesulfinanilide compound having a structure represented by the following formula: ##STR1## wherein R.sup.1 represents a halogen and R.sup.2 represents a lower alkyl group is provided. In addition, a process is provided for oxidizing the trifluoromethanesulfinanilide compound with a magnesium monoperoxydicarboxylate to prepare a trifluoromethanesulfonanilide having a structure represented by the following formula: ##STR2## The trifluoromethanesulfinanilide compound (I) also serves as an excellent active ingredient of a controlling agent for regulating the population of house dust mites.Type: GrantFiled: December 5, 1996Date of Patent: December 16, 1997Assignee: Sumitomo Chemical Company, LimitedInventors: Tatsuya Mori, Yoji Takada
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Patent number: 5686633Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.Type: GrantFiled: December 31, 1991Date of Patent: November 11, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Eric Vieira, Hugh Stephen Laver
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Patent number: 5670684Abstract: The present invention provides novel intermediates which are useful for the preparation of excitatory amino acid receptor antagonists. Further provided is a process to enatioselectively prepare hydroisoquinoline compounds with central nervous system activity.Type: GrantFiled: May 19, 1995Date of Patent: September 23, 1997Assignee: Eli Lilly and CompanyInventors: Anita Melikian-Badalian, Paul L. Ornstein
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Patent number: 5637753Abstract: A process for the preparation of N-carbonylarylimine of the general formula I: ##STR1## in which Ar represent an aryl radical and R represent a phenyl or t-butoxy radical, by desulphonating the compound of the general formula II. ##STR2## The compounds of formula II are novel when R is t-butoxy.Type: GrantFiled: January 16, 1996Date of Patent: June 10, 1997Assignee: Rhone-Poulenc Rorer S.A.Inventors: Didier Bernard, Patrick Leon
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Patent number: 5633400Abstract: The invention relates to a process for the preparation of a compound of the formula (I) ##STR1## in which X is an optionally protected formyl group andR is a group which is itself inert to the reaction conditions of the synthesis,which comprises reacting a compound of the formula (II) ##STR2## where X is as defined above, with a substituted phenyl-halogen compound of the formula (III) ##STR3## where the substituent Hal is a halogen group and R is as defined above.Type: GrantFiled: May 24, 1995Date of Patent: May 27, 1997Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Neerja Bhatnagar, Jean Buendia, Christine Griffoul
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Patent number: 5633287Abstract: The present invention is directed to compounds useful for the regulation of cholesterol of Formula I, methods for using them and pharmaceutical compositions thereof, ##STR1## wherein X and Y are oxygen, sulfur, or (CR'R").sub.n wherein n is 1 to 4; R is hydrogen, alkyl, or benzyl; R.sub.1 and R.sub.2 are phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, an alkyl chain, adamantyl, or a cycloalkyl group.Type: GrantFiled: October 23, 1995Date of Patent: May 27, 1997Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic, Wendell Wierenga
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Patent number: H1696Abstract: This invention relates to an improved method of making sulfonyl isocyanates from the corresponding sulfonamides and phosgene.Type: GrantFiled: February 21, 1997Date of Patent: November 4, 1997Assignee: E. I. Du Pont de Nemours and CompanyInventors: David Akueteh Adjei, Charles T. Blaisdell