Carboxyl, Or Salt Thereof, In Side Chain Having Sulfur Bonded Directly To A Ring Patents (Class 562/431)
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Patent number: 7345191Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.Type: GrantFiled: February 26, 2005Date of Patent: March 18, 2008Assignee: Cambrex Charles City, Inc.Inventors: Paul Alan Jass, Jason Scott Douglas
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Patent number: 7301050Abstract: The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.Type: GrantFiled: September 16, 2004Date of Patent: November 27, 2007Assignee: Janssen Pharmaceutical N.V.Inventors: Gee-Hong Kuo, Rui Zhang, Aihua Wang, Alan R. DeAngelis
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Patent number: 7294737Abstract: Provided are methods for manufacturing compounds of Formula I wherein all substituents are described herein.Type: GrantFiled: April 20, 2005Date of Patent: November 13, 2007Assignee: AtheroGenics, Inc.Inventor: M. David Weingarten
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Patent number: 7138543Abstract: The present invention relates to new thiolalkyl benzoic acids, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, neuropathy, pain, compulsive disorders, prostate diseases, cancers, glaucoma, retinal disorders, and cancer.Type: GrantFiled: April 7, 2004Date of Patent: November 21, 2006Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Doris Stoermer, Dilrukshi Vitharana
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Patent number: 7064146Abstract: A pharmaceutical composition, comprising: a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.Type: GrantFiled: June 24, 2003Date of Patent: June 20, 2006Assignee: MediciNova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Patent number: 7060854Abstract: Process for making a pharmaceutical composition, comprising: a compound of formula (1) in crystalline form: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic crystal form A substantially free of other polymorphs, and methods for making this polymorph.Type: GrantFiled: June 24, 2003Date of Patent: June 13, 2006Assignee: MediciNova, Inc.Inventors: Kenneth Walter Locke, David Gregory Roe
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Patent number: 7053222Abstract: A process for the preparation of N-debenzoylpaclitaxel (I) through esterification of 7-protected baccatin III with a carboxylic acid reactive derivative of general formula (II), and elimination of the ester-protecting groups in acid conditions and in a single step. In formula (II) R1 is aryl or heteroaryl.Type: GrantFiled: October 12, 2004Date of Patent: May 30, 2006Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Gabriele Fontana
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Patent number: 6992215Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: October 7, 2004Date of Patent: January 31, 2006Assignee: Guildford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
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Patent number: 6984661Abstract: The present invention is directed to compounds of the structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof: Formula I (a) R1, R2 and R6 are each independently selected from the group consisting of hydrogen, C1-C8 alkyl substituted C1-C8 alkyl, aryl-C0-4-alkyl, substituted aryl-C0-4-alkyl, heteroaryl-C0-4-alkyl, substituted heteroaryl-C0-4-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl, and substituted C3-C6 cycloalkylaryl-C0-2-alkyl; (b) X is an optionally substituted C1-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S; (c) Y is C, O, S, NH or a single bond; and (d) E is selected from the group consisting of hydrogen, C(R3)(R4)A, A, (CH2)n COOR19 and substituted (CH2)n COOR19.Type: GrantFiled: January 21, 2003Date of Patent: January 10, 2006Assignee: Eli Lilly and CompanyInventors: James Robert Henry, YiHong Li
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Patent number: 6930106Abstract: The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated diseases.Type: GrantFiled: June 30, 2003Date of Patent: August 16, 2005Assignee: Pharmacia & UpJohn CompanyInventors: Barry Craig Finzel, Lee A. Funk, Robert Charles Kelly, Matthew T. Reding, Nancy Anne Wicnienski
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Patent number: 6777442Abstract: The present invention relates to compounds of the general formula (I) in which X represents O, S, SO, SO2, CH2, CHF, CF2 or NR8, and Z represents a group of the formula in which A represents O or S, the subscript “a” is 0 or 1, group D represents a straight-chain (C1-C4)-alkylene group, and R36 represents OR37 or NR38R39. It also relates to processes for preparation of such compounds and to their use in medicaments for the treatment of depression, goiter, cancer of the thyroid gland, arteriosclerosis, hypercholesterolaemia, dyslipidaemia, obesity, cardiac insufficiency, pulmonary emphysema, pain, migraine, Alzheimer's disease, osteoporosis, cardiac arrhythmias, hypothyroidism, skin disorders or diabetes.Type: GrantFiled: February 26, 2002Date of Patent: August 17, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Peter Ellinghaus
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Publication number: 20040127570Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: September 5, 2003Publication date: July 1, 2004Applicant: WyethInventors: Scott Christian Mayer, Alan Howard Katz
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Patent number: 6713514Abstract: N-(substituted)carbamoylaryl- and heteroaryl substituted aminopropanoic and butanoic acid compounds which are highly selective agonists for the PPAR-&ggr; receptor or prodrugs of agonists for the PPAR-&ggr; receptor, and are useful in the treatment of Type II diabetes (NIDDM).Type: GrantFiled: April 18, 2000Date of Patent: March 30, 2004Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Hartmuth C. Kolb, Gerard McGeehan, Zhi-Cai Shi, Laxma Reddy Kolla, Cullen Cavallaro
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Publication number: 20030236253Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.Type: ApplicationFiled: March 14, 2003Publication date: December 25, 2003Applicant: Gruenenthal GmbHInventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
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Patent number: 6586623Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.Type: GrantFiled: January 17, 2002Date of Patent: July 1, 2003Assignee: Guilford Pharmaceuticals Inc.Inventors: Takashi Tsukamoto, Pavel Majer, Doris Stoermer, Barbara S. Slusher
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Patent number: 6548699Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.Type: GrantFiled: August 6, 1999Date of Patent: April 15, 2003Assignee: Atherogenics, Inc.Inventor: Patricia K. Somers
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Patent number: 6521619Abstract: The present invention relates to novel cyclopropane-containing diaryl sulfide compounds that are useful for treating inflammatory and immune diseases, to pharmaceutical compositions comprising these compounds, and to methods of inhibiting inflammation or suppressing immune response in a mammal.Type: GrantFiled: June 25, 2001Date of Patent: February 18, 2003Assignees: Icos Corporation, Abbott LaboratoriesInventors: James T. Link, Bryan K. Sorensen
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Patent number: 6492550Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, X1, R1, R2, Ra and Rb are as defined in the specification.Type: GrantFiled: February 8, 2001Date of Patent: December 10, 2002Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Serge Plamondon, Yonghua Gai, Neelakantan Balasubramanian
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Patent number: 6369261Abstract: Compounds having Formula 2 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Alan T. Johnson, Jayasree Vasudevan, Liming Wang, Roshantha A. Chandraratna
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Patent number: 6320072Abstract: This invention provides a method of isolating N-protected-S-phenylcysteine (1) of high purity, expediently, efficiently and in good yield, which comprises causing said N-protected-S-phenylcysteine to be salted out in the form of a base salt in the presence of water. wherein R1 represents an amino-protecting group; R2 represents a hydrogen atom or, either independently of R1 or taken together with R1, represents an amino-protecting group.Type: GrantFiled: December 14, 2000Date of Patent: November 20, 2001Assignee: Kaneka CorporationInventors: Yasuyoshi Ueda, Hiroshi Murao, Koki Yamashita, Koichi Kinoshita
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Patent number: 6306873Abstract: This invention relates to compounds of general formula (I): in which Ar is a group selected from: A1, A2, B, C, D, E, Q1-Q3, R1-R9, Z1 and Z2 are as defined in the disclosure, and Y represents carboxy or an acid bioisostere. These compounds inhibit the production or physiological effects of TNF and inhibit cyclic AMP phosphodiesterase. The invention is also directed to pharmaceutical compositions comprising compounds of formula (I), their pharmaceutical use and methods for their preparation.Type: GrantFiled: July 20, 1999Date of Patent: October 23, 2001Assignee: Aventis Pharmaceuticals Products Inc.Inventors: Christopher J. Burns, Richard Labaudiniere, Stephen Condon, Robert D. Groneberg, Rose M. Mathew, Joseph M. Salvino
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Patent number: 6306854Abstract: Novel compounds of Formula (1) and esters, salts, and physiologically functional derivatives thereof are disclosed. Methods for preparing and using the compounds are also disclosed. Many of these compounds are selective activators of PPAR alpha. The compounds are particularly useful for treating obesity.Type: GrantFiled: April 16, 2001Date of Patent: October 23, 2001Assignee: GlaxosmithklineInventors: Peter Jonathan Brown, James Mood Chapman, Jr., Jeffrey Alan Oplinger, Ludwig William Stuart, Timothy Mark Willson, Zhengdong Wu
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Patent number: 6303612Abstract: Processes for the preparation of derivatives of hydroxyphenylsulfanylbenzoic and hydroxyphenylsulfanylarylacetic acids of Formula (I) and pharmaceutical compositions including these compounds are provided: wherein X is H, halogen or NO2 group, n is 0 or 1, and m is 2 to 4 if Z is either 4-acetyl-3 -hydroxy-2-propylphenoxy of Formula (II): or a piperazinyl residue, or m is 1 if Z is quinolin-2-yl or 6-chloroquinoli-2-yl.Type: GrantFiled: December 19, 2000Date of Patent: October 16, 2001Assignee: Leciva, A.S.Inventors: Miroslav Kucha{haeck over (r)}, Vojt{haeck over (e)}ch KmonĂ{haeck over (c)}ek, VladimĂra Panajotová, Bohumila Br{haeck over (u)}nová, AntonĂn Jandera, Hana Ji{haeck over (r)}Ă{haeck over (c)}ková, V{haeck over (e)}ra Bucharová
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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: 6262084Abstract: A method for the inhibition of the binding of &agr;4&bgr;1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions thereof; and the use of the compounds either as above, or in formulations for the control or prevention of diseases states in which &agr;4&bgr;1 is involved.Type: GrantFiled: October 14, 1999Date of Patent: July 17, 2001Assignee: Texas Biotechnology CorporationInventors: Ronald J. Biediger, Vanessa O. Grabbe, George W. Holland, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, Shuqun Lin, Robert V. Market, Bore G. Raju, Ian L. Scott, Chengde Wu
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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: 6221898Abstract: There is provided compounds of formula I, wherein R1, R2, R3, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.Type: GrantFiled: August 29, 1997Date of Patent: April 24, 2001Assignee: Astra AktiebolagInventor: Thomas Antonsson
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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: 6130352Abstract: A process for the preparation of (+) (2S, 3S)-3-(2-aminophenylthio)-2-hydroxy-3-(4'-methoxyphenyl)-propionic acid which comprises treating the (.+-.) compound of (2RS, 3RS) 3-(2-aminophenylthio)-2-hydroxy-3-(4'-methoxyphenyl)-propionic acid (formula (II)) with the (+) compound of the 2-methylbenzylamine (formula (III)) and an alkali in the presence of a polar solvent, the amount of the compound of the formula (III) and the alkali being in half equivalent amount of compound of the formula (II) employed, separating the precipitate (+) amine salt form of (2-aminophenylthio)-2-hydroxy-3-(4'-methoxyphenyl)-propionic acid from the 1(-) salt form remaining in solution, by known methods treating the (+) amine salt from with an organic solvent and then decomposing the (+) amine salt form to produce (+)(2s, 3s)-3-(2-aminophenylthio)-2-hydroxy-3-(4'-methoxyphenyl)-propionic acid.Type: GrantFiled: March 27, 1997Date of Patent: October 10, 2000Assignee: Council of Scientific & Industrial ResearchInventors: Yennu Sangiah Sadanandam, Meera Manjaya Shetty, Imtiaz Ahm Ansari, Jhillu Singh Yadav, Alla Venkata Rama Rao
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Patent number: 6127392Abstract: Compounds of the formula: wherein:R.sub.1, R.sub.2, R.sub.3, R.sub.4,R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are, independently, hydrogen, COOR.sub.15, halogen, nitro, cyano, C.sub.1-10 alkoxy, C.sub.1-10 haloalkoxy, sulfonic acid, C.sub.1-10 alkylsulfonyl, C.sub.6-12 arylsulfonyl, C.sub.6-12 aralkylsulfonyl, C.sub.1-10 alkylsulfinyl, C.sub.6-12 arylsufinyl, C.sub.6-12 aralkylsulfinyl, sulfamoyl, C.sub.1-10 alkylsulfamido, C.sub.6-12 arylsulfamido, C.sub.1-10 alkanoyl, C.sub.6-12 aryloyl, C.sub.6-12 aralkanoyl, amino, C.sub.1-10 alkylamino, C.sub.2-10 dialkylamino, C.sub.6-12 aralkylamino, C.sub.6-12 arylamino, carboxamido, C.sub.1-10 alkylcarboxamido, C.sub.6-12 arylcarboxamido, C.sub.1-10 haloalkyl, C.sub.1-10 alkyl, C.sub.2-12 alkenyl, C.sub.6-12 aryl, C.sub.6-12 aralkyl; with the proviso that at least one of R.sub.4 and R.sub.5 is COOR.sub.15 ;R.sub.9 is hydrogen, C.sub.1-10 alkyl and C.sub.1-10 haloalkyl;R.sub.10 is hydrogen, C.sub.1-10 alkyl, C.sub.1-10 haloalkyl, or C.sub.2-12 alkylidene;R.sub.Type: GrantFiled: August 3, 1998Date of Patent: October 3, 2000Assignee: American Home Products CorporationInventors: Joseph Richard Lennox, Schuyler Adam Antane, John Anthony Butera
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Patent number: 6114523Abstract: A process which allows the re-use of compounds of formula ##STR1## in diltiazem synthesis through a process of conversion to a mixture of enantiomers III-(2R,3R) and III-(2S,3S) is described.Type: GrantFiled: October 21, 1998Date of Patent: September 5, 2000Assignee: Zamon Group S.p.A.Inventors: Pietro Allegrini, Gaetano Marchioro, Giuseppe Barreca, Marco Villa, Laura Russo
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Patent number: 6096773Abstract: A method for the inhibition of the binding of .alpha..sub.4 .beta..sub.1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which .alpha..sub.4 .beta..sub.1 is involved.Type: GrantFiled: April 15, 1999Date of Patent: August 1, 2000Assignee: Texas Biotechnology Corporation, Inc.Inventors: Ian L. Scott, Bore G. Raju, Ronald J. Biediger, Vanessa O. Grabbe, Jamal Kassir, Karin M. Keller, Timothy P. Kogan, deceased, Shuqun Lin, Robert V. Market
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Patent number: 6093799Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.Type: GrantFiled: October 20, 1999Date of Patent: July 25, 2000Assignee: Pharmacopeia, Inc.Inventors: Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
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Patent number: 6017889Abstract: Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.Type: GrantFiled: December 23, 1998Date of Patent: January 25, 2000Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller
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Patent number: 6008321Abstract: A substrate for solid phase synthesis of the formula: ##STR1## is disclosed. Also disclosed are processes for preparing the substrate and intermediates useful therein. Among the novel intermediates are compounds of the formula: ##STR2## wherein t is 0 or 1; n is 3-20; R is OH, an activated ester or the residue of a solid support having a plurality of amino functionalities; A is --O-- or --NH-- and Q is hydrogen or a protecting group for an amine or alcohol.Type: GrantFiled: March 16, 1998Date of Patent: December 28, 1999Assignee: Pharmacopeia, Inc.Inventors: Ge Li, Sian Louise Griffiths, Edward McDonald, Libo Xu
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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: 5945548Abstract: Process for the synthesis of .alpha.-substituted acrylic acids of general formula (I) and their application to the synthesis of N-(mercaptoacyl)aminoacid derivatives of formula (II).Type: GrantFiled: May 21, 1998Date of Patent: August 31, 1999Assignee: Societe Civile BioprojectInventors: Pierre Duhamel, Lucette Duhamel, Denis Danvy, Thierry Monteil, Jeanne-Marie Lecomte, Jean-Charles Schwartz
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Patent number: 5936092Abstract: Fatty acid derivatives of sulfhydryl-containing compounds (for example, sulfhydryl-containing peptides or proteins) comprising fatty acid-conjugated products with a disulfide linkage are employed for delivery of the compounds to mammalian cells. This modification markedly increases the absorption of the compounds by mammalian cells relative to the rate of absorption of the unconjugated compounds, as well as prolonging blood and tissue retention of the compounds. Moreover, the disulfide linkage in the conjugate is quite labile in the cells and thus facilitates intracellular release of the intact compounds from the fatty acid moieties.Type: GrantFiled: November 1, 1996Date of Patent: August 10, 1999Assignee: The University of Southern CaliforniaInventors: Wei-Chiang Shen, Hossein M. Ekrami
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Patent number: 5932595Abstract: The present invention relates to compounds of Formula I: ##STR1## that are matrix metalloprotease inhibitors, pharmaceutical compositions containing them, methods for their use and methods of preparing these compounds.Type: GrantFiled: December 18, 1996Date of Patent: August 3, 1999Assignees: Syntex (U.S.A.) Inc., Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Chris Allen Broka, Jeffrey Allen Campbell, Arlindo Lucas Castelhano, Lawrence Emerson Fisher, Robert Than Hendricks, Keshab Sarma
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Patent number: 5919824Abstract: Aminophenol derivatives represented by the following formula (1): ##STR1## wherein X is O or S; A is alkylene, R.sup.1 is phenyl, etc., R.sup.2 and R.sup.3 are H or alkyl; R.sup.4 is substituted carbamoylalkyl, etc.; R.sup.5 is substituted amino, etc.; their salts, and optical isomers of the derivatives and salts. Also disclosed are gastrin receptor antagonists, cholecystokinin receptor antagonists, and medicines for digestive diseases. The compounds have strong binding inhibition against gastrin receptor or CCK-A receptor and also they have higher selectivity to either group of CCK-A receptor or gastrin receptor, and therefore, the compounds are useful for preventing and treating gastrointestinal diseases including peptic ulcers as well as central nervous system diseases.Type: GrantFiled: September 12, 1997Date of Patent: July 6, 1999Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shuichi Yokohama, Keiichi Kawagoe, Yasuyuki Takeda, Yoshihiro Yokomizo, Aki Yokomizo
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Patent number: 5902791Abstract: Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.Type: GrantFiled: July 22, 1996Date of Patent: May 11, 1999Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Mark Whittaker, Andrew Miller
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Patent number: 5891909Abstract: Amidino and benzamidino compounds, including compounds of the formula: ##STR1## wherein R.sup.1 -R.sup.4, R.sup.6 -R.sup.9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: March 27, 1997Date of Patent: April 6, 1999Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Bruce E. Tomczuk, Carl Illig
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Patent number: 5874473Abstract: Inhibitors for matrix metalloproteases, pharmaceutical compositions containing them, and a process for using them to treat a variety of physiological conditions. The compounds of the invention have the generalized formula ##STR1## wherein each T is a substituent group; x is 0, 1, or 2; the group D represents ##STR2## the subscript "e" is 2 or 3; the group R.sup.14 represents a variety of possible substituent groups on the cycloalkyl ring between D and G, and the group G represents M, ##STR3## in which M represents --CO.sub.2 H, --CON(R.sup.11).sub.2, or --CO.sub.2 R.sup.12 ; and R.sup.13 represents any of the side chains of the 19 noncyclic naturally occurring amino acids.Type: GrantFiled: May 28, 1997Date of Patent: February 23, 1999Assignee: Bayer CorporationInventors: Harold Clinton Eugene Kluender, Guenter Hans Herbert Heinz Benz, Kerry Jeanne Combs, Brian Richard Dixon, Michael Christopher VanZandt, Scott McClelland Wilhelm, Donald John Wolanin, Jill Elizabeth Wood, Stephan Schneider
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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: 5739385Abstract: This invention relates to a process for preparing optically active carboxylic acids by oxidizing an optically active aldehyde with a peracid in the presence of an amine and/or amine N-oxide catalyst selected from the group consisting of a substituted or unsubstituted alkyl amine, alkyl amine N-oxide, aromatic amine, aromatic amine N-oxide, heterocyclic amine, heterocyclic amine N-oxide and mixtures thereof, to produce the optically active carboxylic acid. Such optically active carboxylic acids have utility for example as pharmaceuticals.Type: GrantFiled: October 19, 1995Date of Patent: April 14, 1998Assignee: Union Carbide Chemicals & Plastics Technology CorporationInventors: Bruce Armin Barner, Jonathan Joshua Kurland
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Patent number: 5734077Abstract: New substituted 2,2-dimethyl-.omega.-phenoxyalkanoic acids and esters of formula: ##STR1## wherein: X, A, B, R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and Z are as defined in the specification,The corresponding enantiomers and diastereoisomers, and the physiologically tolerable salts thereof with appropriate bases.The products of the invention may be used therapeutically.Type: GrantFiled: September 13, 1996Date of Patent: March 31, 1998Assignee: Adir ET CompagnieInventors: Gilbert Regnier, Claude Guillonneau, Jean-Paul Vilaine, Florence Mahlberg, Christine Breugnot
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Patent number: 5731452Abstract: 7-thiaprostaglandins having the formula (I) which inhibit cell migration induced by monocyte chemoattractant protein MCP-1/MCAF and other chemokines and can serve as drugs for the treatment of atherosclerosis, diabetic angiopathy, and other disorders, their enantiomers, mixtures of the same, and methods of production thereof.Type: GrantFiled: September 18, 1995Date of Patent: March 24, 1998Assignee: Teijin LimitedInventors: Toru Minoshima, Kenichiro Kataoka, Hiroko Tanaka, Koji Ishii, Noriaki Endo
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Patent number: 5710321Abstract: The present invention relates to a process for preparing the cyclohexylamine salt of (+)-threo-2-hydroxy-3-(2'-aminophenylthio)-3-(4"-methoxyphenyl)-propionic acid and of its optical (-)-antipode, by starting from the racemate acid by means of a first crystallization from a suitable chiral base and a second crystallization from a cyclohexylamine-containing solvent. Said salt is an intermediate in the synthesis of diltiazem, a well-known calcium-antagonist drug.Type: GrantFiled: April 15, 1996Date of Patent: January 20, 1998Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.Inventors: Roberto Bortolaso, Siro Serafini
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Patent number: 5710256Abstract: The present invention is directed to novel methadone derivatives which are synthesized for the covalent attachment to antigens (proteins or polypeptides) for the preparation of antibodies or receptors to methadone and methadone metabolites. The resulting novel antigens may be used for the production of antibodies or receptors using standard methods. Once generated, the antibodies or receptors and the novel derivatives which are covalently attached to proteins, polypeptides or labels may be used in the immunoassay process.Type: GrantFiled: April 3, 1995Date of Patent: January 20, 1998Assignee: Biosite Diagnostics IncorporatedInventor: Kenneth F. Buechler
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Patent number: 5705533Abstract: 10-thio-substituted 1,8-dihydroxy-9(10H) anthracenones, therapeutic compositions containing at least one of the 10-thio-substituted 1,8-dihydroxy-9(10H) anthracenones of the invention and methods of treating inflammatory conditions are provided.Type: GrantFiled: June 7, 1995Date of Patent: January 6, 1998Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Klaus Muller, Hsu-Shan Huang, Wolfgang Wiegrebe