Nitrogen In Acid Moiety Patents (Class 560/16)
-
Patent number: 7105545Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkyType: GrantFiled: April 2, 2002Date of Patent: September 12, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Walter Kunz, Clemens Lamberth, Fredrik Cederbaum, Martin Zeller
-
Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
-
Patent number: 6946474Abstract: The present invention provides trichloroethyl-sulfonylurea-containing compounds that inhibit glycing transporters, pharmaceutical compositions comprising such compounds, methods for using such compounds for inhibiting glycine transporters and methods for using such compounds for the treatment of disease states in which glycine is involved.Type: GrantFiled: September 13, 2001Date of Patent: September 20, 2005Assignee: Merck & Co., Inc.Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
-
Patent number: 6878845Abstract: Oligomers from multifunctional acrylates and organonitro compounds are provided. Films obtained from crosslinked oligomers of the present invention are useful as protective or decorative coatings as well as components in adhesives and composites.Type: GrantFiled: October 15, 2002Date of Patent: April 12, 2005Assignee: Ashland Inc.Inventors: Matthew S. Sheridan, Laurence G. Dammann, Sridevi Narayan-Sarathy
-
Patent number: 6838472Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: GrantFiled: September 17, 2002Date of Patent: January 4, 2005Assignee: Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
-
Patent number: 6803480Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.Type: GrantFiled: March 11, 2003Date of Patent: October 12, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Gunter Schmidt, Josef Pernerstorfer, Hilmar Bischoff, Carsten Schmeck, Verena Vöhringer, Michael Woltering, Axel Kretschmer, Christiane Faeste
-
Publication number: 20040127739Abstract: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkyType: ApplicationFiled: September 23, 2003Publication date: July 1, 2004Inventors: Walter Kunz, Clemens Lamberth, Fredrik Cederbaum, Martin Zeller
-
Patent number: 6683200Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: January 27, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
-
Publication number: 20030158155Abstract: A compound of the formula (1): 1Type: ApplicationFiled: October 15, 2002Publication date: August 21, 2003Inventors: Yozo Hori, Fumihiko Watanabe, Hiroshige Tsuzuki, Shingo Furue, Yoshinori Tamura
-
Publication number: 20030125383Abstract: The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.Type: ApplicationFiled: September 17, 2002Publication date: July 3, 2003Applicant: Roche Bioscience, a division of Syntex (U.S.A.) LLCInventors: Michael Klaus, Jean-Marc Lapierre
-
Patent number: 6583139Abstract: Disclosed as compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: October 17, 2000Date of Patent: June 24, 2003Inventors: Eugene D. Thorsett, Christopher M. Semko, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Reinhardt Bernhard Baudy, Dimitrios Sarantakis
-
Patent number: 6559334Abstract: The invention relates to novel optically active polymerizable dipeptides, to the process for the preparation thereof, to the polymerization thereof and to the use of the polymers as adsorbents for the chromatographic separation of enantiomers.Type: GrantFiled: August 12, 1994Date of Patent: May 6, 2003Assignee: Bayer AktiengesellschaftInventors: Walter Lange, Michael Grosse-Bley, Bruno Bömer, Rolf Grosser, Franz-Peter Hoever
-
Patent number: 6534546Abstract: Compounds represented by the general formula (1): (where R1 is SR6 or NR7R8, where R6 is typically an alkyl group having 1-6 carbon atoms, R7 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or a nitro group, and R8 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; R2 and R3 are each typically a hydrogen atom or an alkyl group having 1-6 carbon atoms; R4 is a hydrogen atom, an alkyl group having 1-6 carbon atoms or an amidino group of which the amine portion may be substituted by an alkyl or nitro group; R5 is a hydrogen atom or an alkyl group having 1-6 carbon atoms; Y1, Y2, Y3 and Y4 which may be the same or different are each typically a hydrogen atom, a halogen atom or an alkoxy group having 1-6 carbon atoms; n and m are each an integer of 0 or 1), or possible stereoisomers or optically active forms of the compounds or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 6, 1997Date of Patent: March 18, 2003Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Toshio Honda, Toshihiko Makino, Toshiaki Nagafuji, Yasushi Kitoh, Nobuaki Kimura
-
Patent number: 6525093Abstract: Compounds are provided that lower blood glucose concentrations, lower serum triglyceride concentrations, lower systolic blood pressure, and increase glucose uptake by adipose tissue, but do not affect the expression of PPAR-&ggr; by adipose tissue.Type: GrantFiled: November 8, 1999Date of Patent: February 25, 2003Assignee: Calyx Therapeutics Inc.Inventors: Partha Neogi, Bishwajit Nag, Frederick J. Lakner, Debendranath Dey, Satyanarayana Medicherla
-
Publication number: 20030036653Abstract: Compounds of the formula 1Type: ApplicationFiled: March 15, 2002Publication date: February 20, 2003Applicant: American Home Products CorporationInventors: Jonathan Bloom, Martin DiGrandi, Russell Dushin, Stanley Lang, Bryan O'Hara
-
Publication number: 20030032671Abstract: The present application relates to novel potent PPAR-alpha-activating compounds for treating, for example, coronary heart disease, and to their preparation.Type: ApplicationFiled: October 9, 2001Publication date: February 13, 2003Inventors: Klaus Urbahns, Michael Woltering, Susanne Nikolic, Josef Pernerstorfer, Berthold Hinzen, Elke Dittrich-Wengenroth, Hilmar Bischoff, Claudia Hirth-Dietrich, Klemens Lustig
-
Publication number: 20030013847Abstract: Certain known and novel pyruvate derivatives are particularly active in restoring or preserving metabolic integrity in oxidatively competent cells that have been subjected to oxygen deprivation. These pyruvate-derived compounds include, but are not limited to oximes, amides, pyruvate analogues, modified pyruvate analogues, esters of pyruvate (e.g., polyol-pyruvate esters, pyruvate thioesters, glycerol-pyruvate esters and dihydroxyacetone-pyruvate esters). Such pyruvate derivatives (including single tautomers, single stereoisomers and mixtures of tautomers and/or stereoisomers, and the pharmaceutically acceptable salts thereof) are useful in the manufacture of pharmaceutical compositions for treating a number of conditions characterized by oxidative stress.Type: ApplicationFiled: May 3, 2002Publication date: January 16, 2003Inventors: Bing Wang, Guy Miller, Wei Zhang, Satyanarayana Janagani, Jiangao Song
-
Publication number: 20020183260Abstract: Compounds of the formula 1Type: ApplicationFiled: May 9, 2002Publication date: December 5, 2002Inventor: Cynthia Anne Fink
-
Publication number: 20020169337Abstract: A process for producing optically active cysteine derivatives with high optical purity and good quality which is economically advantageous and is high in productivity even on a commercial scale is provided.Type: ApplicationFiled: May 13, 2002Publication date: November 14, 2002Applicant: Kaneka CorporationInventors: Yasuyoshi Ueda, Hiroshi Murao, Takeshi Kondo, Noboru Ueyama, Hajime Manabe, Kenji Yoneda, Akira Nishiyama
-
Patent number: 6472430Abstract: Antiatherosclerotic compounds are provided which have the following structure: wherein R is lower alkyl; R1 is hydroxy, amino, or lower alkoxy, R2 and R3 are each independently hydrogen, alkyl or aryl; Ar is phenyl, indanyl, benzhydryl, or phenyl substituted with one or more member selected from the group consisting of halogen, lower alkyl, perfluoroalkyl, lower alkoxy, perfluoroalkylalkoxy, dialkylamino, and aryloxy; or pharmaceutically acceptable salts thereof.Type: GrantFiled: September 28, 2001Date of Patent: October 29, 2002Inventors: Hassan M. Elokdah, Theodore S. Sulkowski
-
Patent number: 6455581Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: September 24, 2002Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
-
Patent number: 6444850Abstract: A fungicidal compound of formula (I) having a fluorovinyloxyphenyl moiety and stereoisomers thereof are useful for protecting crops from fungal diseases: wherein: X is CH or N; Y is O or S; Z is O or NH; R1 is hydrogen or CF3; and R2 is hydrogen, a C1-10 alkyl, naphthyl, thiophenyl or a phenyl group optionally carrying one or more substituents selected from the group consisting of C1-6 alkyl, halogen-substituted C1-6 alkyl, C1-6 alkoxy, phenoxy, halogen, and methylenedioxy radicals.Type: GrantFiled: February 8, 2000Date of Patent: September 3, 2002Assignee: Korea Research Institute of Chemical TechnologyInventors: Chwang-Siek Pak, Bum-Tae Kim, No-Kyun Park, Gyung-Ja Choi, Heung-Tae Kim
-
Patent number: 6420603Abstract: A novel process for the preparation of N,N′-bis[2,3-dihydroxypropyl]-5-[(hydroxyacetyl) methylamino]-2,4,6-triiodo-1, 3-benzenedi carboxamide of formula (I), commonly known as lomeprol, a novel non-ionic contrast agent which shows very good safety and contrast effectiveness.Type: GrantFiled: July 17, 2001Date of Patent: July 16, 2002Assignee: Bracco International B.V.Inventors: Laura Alessandroni, Patrizia Ambrosetti, Maria Argese, Renato Geremia, Enrico Moretti, Vittorio Valle, Giorgio Ripa, Marcella Murru
-
Patent number: 6407100Abstract: The invention relates to novel compounds of the formula in which R1 is C1-4alkyl and (Y—X) is CH2, C1-2alkylthio-CH═ or C1-2alkyl-ON═ and Z is an aldimino or ketimino group, and to their preparation, as well as fungicidal compositions with such compounds as active substances. The compounds can be employed for controlling fungi in agriculture, in horticulture and in wood preservation.Type: GrantFiled: September 1, 1993Date of Patent: June 18, 2002Assignee: Bayer AktiengesellschaftInventors: Hans Peter Isenring, Bettina Weiss
-
Patent number: 6388122Abstract: A tryptase inhibitor comprising as an active ingredient at least one member selected from among guanidinoaliphatic acid derivatives of the formula (I), guanidinobenzoic acid derivatives of the formula (II), guanidinophenol derivatives of the formula (III), amidinophenol derivatives of the formula (IV), and novel guanidinophenol derivatives of the formula (V) (in the formulae, Gu is guanidino).Type: GrantFiled: October 7, 1998Date of Patent: May 14, 2002Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hiroshi Kido, Hisao Nakai
-
Publication number: 20020055645Abstract: The instant invention relates to a process for preparing a compound of formula (I): 1Type: ApplicationFiled: November 9, 2001Publication date: May 9, 2002Inventors: Thierry Monteil, Denis Danvy, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Serge Piettre
-
Publication number: 20020037857Abstract: Novel compounds having activity as non-covalent inhibitors of urokinase and having activity in reducing or inhibiting blood vessel formation are provided. These compounds have Pi a group having an amidino or guanidino moiety or derivative thereof. These compounds are useful in vitro for monitoring plasminogen activator levels and in vivo in treatment of conditions which are ameliorated by inhibition of or decreased activity of urokinase and in treating pathologic conditions wherein blood vessel formation is related to a pathologic condition.Type: ApplicationFiled: December 7, 2000Publication date: March 28, 2002Applicant: Corvas International, Inc.Inventors: Joseph Edward Semple, Michael I. Weinhouse, Odile Esther Levy, Edwin L. Madison, Amir P. Tamiz
-
Patent number: 6331627Abstract: The present invention relates to novel antiobesity and hypocholesterolemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel &bgr;-aryl-&agr;-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereo-somers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: GrantFiled: July 5, 2000Date of Patent: December 18, 2001Assignee: Reddy's Laboratories Ltd.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
-
Patent number: 6310095Abstract: Compounds having the formula or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2—, and (i) heterocyclic-L2—; R2 is selected from (a) (b) —C(O)NH—CH(R14)—C(O)OR15, (d) —C(O)NH—CH(R14)—C(O)NHSO2R16, (e) —C(O)NH—CH(R14)-tetrazolyl, (f) —C(O)NH-heterocyclic, and (g) —C(O)NH—CH(R14)—C(O)NR17R18; R3 is substituted or unsubstituted heterocyclic or aryl, substituted or unsubstituted cycloalkyl or cycloalkenyl, and —P(W)RR3RR3′; R4 is hydrogen, lower alkyl, haloalkyl, halogen, aryl, arylakyl, heterocyclic, or (heterocyclic)alkyl; L1 is absent or is selected from (a) —L4—N(R5)—L5—, (b) —L4—O—L5—, (c) —L4—S(O)n—L5— (d) —L4—L6—C(W)—N(R5)—L5&Type: GrantFiled: May 7, 1998Date of Patent: October 30, 2001Assignee: University of PittsburghInventors: Said M. Sebti, Andrew D. Hamilton, David J. Augeri, Kenneth J. Barr, Stephen A. Fakhoury, David A. Janowick, Douglas M. Kalvin, Stephen J. O'Connor, Saul H. Rosenberg, Wang Shen, Rolf E. Swenson, Bryan K. Sorenson, Gerard M. Sullivan, Andrew S. Tasker, James T. Wasicak, Lissa T. J. Nelson, Kenneth J. Henry, Le Wang
-
Patent number: 6284914Abstract: New compounds of general formulae (III), (IV) and (V).Type: GrantFiled: January 27, 2000Date of Patent: September 4, 2001Assignee: Fuji Yakuhin Kogyo Kabushiki KaishaInventors: Junko Fujisawa, Eiko Suda, Katsuhiro Igeta, Tadanori Morikawa, Tetsunori Fujisawa, Shinjiro Odake, Yasuo Morita, Tomoko Hongo, Hajime Ito
-
Publication number: 20010014754Abstract: 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: ApplicationFiled: March 20, 2001Publication date: August 16, 2001Applicant: AJINOMOTO CO., INC.Inventors: Takayuki Suzuki, Takayuki Hamada, Kunisuke Izawa
-
Patent number: 6265603Abstract: Peptidomimetic isoprenyl transferase inhibitors R6SCHR1′CHR1WCHR2YC(:X)NR3CHR5COR4 wherein R1=OH, H, alkyl, amino group or R1 and R6 together form a heterocyclic ring; R1′=H, alkyl, aryl; R2=H, alkyl, arylalkyl, heteroarylalkyl; R3=H, alkyl, arylalkyl; R4=OH, alkoxy, amino group; R5=natural amino acid residue or D—E—F, where D is alkyl or alkenyl, E is O, S, N, or null, F is H, alkyl, aryl, carboxy amino, etc.; R6=H, alkyl, acyl, etc.; W=alkyl, alkenyl; X=O, S, Y is M—O—P, where M is C0-6 alkyl, O is oxygen-C0-4 alkyl, P is(un)substituted C6-20 aryl are disclosed.Type: GrantFiled: April 1, 1999Date of Patent: July 24, 2001Assignee: Eisai Co., Ltd.Inventors: Michael D. Lewis, Ana Maria Garcia, James J. Kowalczyk, Hu Yang, Eric Schwartz
-
Patent number: 6265590Abstract: Protected amino acid derivatives of general formula (I) and methods for the prepatation of the derivatives are provided.Type: GrantFiled: July 12, 1999Date of Patent: July 24, 2001Assignee: Hyundai Pharm, Ind. Co., Ltd.Inventors: Vladimir V. Samukov, Aydar N. Sabirov, Pavel I. Pozdnyakov, Hack-Joo Kim, Young-Deug Kim
-
Patent number: 6239308Abstract: 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: October 6, 2000Date of Patent: May 29, 2001Assignee: Ajinomoto Co., Inc.Inventors: Takayuki Suzuki, Yutaka Honda, Kunisuke Izawa
-
Patent number: 6235922Abstract: Compounds having the following formula I, and pharmaceutically acceptable salts thereof, including dual inhibitors of ACE and NEP and selective ACE inhibitors: wherein: Y1 and Y2 are each independently hydrogen, alkyl, aryl, halogen, or alkoxy; X is O or S(O)t; A is t is zero, one or two; m and n are independently zero or one; and wherein R, R5, R5a, R5b, R6, R7, R11, q and r are defined herein.Type: GrantFiled: December 4, 1998Date of Patent: May 22, 2001Assignee: Bristol-Myers Squibb Co.Inventors: Jeffrey A. Robl, Chong-Qing Sun
-
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
-
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
-
Patent number: 6066754Abstract: The present invention provides a process for making N-alkoxy(or aryloxy)carbonyl isothiocyanate derivatives by reacting a chloroformate with a thiocyanate, in the presence of an organic solvent and a catalytic amount of a N,N-dialkylarylamine, to produce a N-alkoxy(or aryloxy)carbonyl isothiocyanate intermediate product, wherein the intermediate product is converted to a N-alkoxy(or aryloxy)carbonyl isothiocyanate derivative in high yield and purity.Type: GrantFiled: June 10, 1999Date of Patent: May 23, 2000Assignee: Bayer CorporationInventor: Shekhar V. Kulkarni
-
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
-
Patent number: 6030803Abstract: Dibenzodihydropyridinecarboxylic esters are provided which comply with formula (1) or (2), wherein: R.sub.1 is substituted alkyl or cyano; R.sub.2 and R.sub.3 are independently hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sub.4 is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl; R.sub.5 and R.sub.6 are independently alkyl, alkoxy or another substituent which is relatively resistant to oxidation; m and n are integers from 0 to 4; wherein, if m or n is at least 2, two groups R.sub.5 or R.sub.6 may be linked together; and Z is oxygen or sulphur. The new compounds are used in a method as chemiluminogenic reagents for detecting the presence of peroxidase activity at extremely low levels (10.sub.-20 moles). A kit containing the dibenzodihydropyridine-carboxylic esters for use in assaying peroxidase activity has also been described.Type: GrantFiled: January 7, 1999Date of Patent: February 29, 2000Assignee: De Staat der Nederlanden, vertegenwoordigd door de Minister van Welzijn, Volksgeszonheid en CultuurInventors: Marjorie Jacquemijns, Gijsbert Zomer
-
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
-
Patent number: 6013829Abstract: Process for the asymmetric synthesis of S-acyl derivatives of 2-mercaptomethyl-3-phenylpropanoic acid of formula (I): characterized in that it comprises the steps consisting in:a) preparing the diol (VI) by reduction of a malonic ester (V) in the presence of a hydride;b) preparing the monoacetates (VII R) or (VII S) respectively;c) subjecting these monoacetates to an oxidation in order to form the acids (IX S) or (IX R);d) saponifying the compounds (IX S) or (IX R) in order to form the hydroxy acids (X S) or (X R);e) thioacylating the hydroxy acids (X S) or (X R) with a mercapto acid R.sub.1 SH (XI), according to a Mitsunobu-type reaction, in order to lead to the desired acids (I R) (I S) respectively and application to the synthesis of N-(mercaptoacyl)amino acid derivatives (II).Type: GrantFiled: November 26, 1997Date of Patent: January 11, 2000Assignee: Societe Civile BioprojetInventors: Denis Danvy, Thierry Monteil, Pierre Duhamel, Lucette Duhamel, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Nadine Noel-Lefebvre, Claude Gros, Jean-Christophe Plaquevent
-
Patent number: 5994539Abstract: Compounds of formula ##STR1## wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, m and n have the meanings reported in the description, processes for their preparation and pharmaceutical compositions which contain them as active ingredients are described.The compounds of formula I are endowed with a mixed ACE-inhibitory and NEP-inhibitory activity and are useful in the treatment of cardiovascular diseases.Type: GrantFiled: December 18, 1997Date of Patent: November 30, 1999Assignee: Zambon Group S.p.A.Inventors: Franco Pellacini, Stefano Romagnano, Gabriele Norcini, Francesco Santangelo, Mario Fantucci, Claudio Semeraro
-
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
-
Patent number: 5962487Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of picornaviral 3C proteases. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses. Several novel methods and intermediates can be used to prepare the novel picornaviral 3C protease inhibitors of the present invention.Type: GrantFiled: December 16, 1997Date of Patent: October 5, 1999Assignee: Agouron Pharmaceuticals, Inc.Inventors: Stephen E. Webber, Peter S. Dragovich, Thomas J. Prins, Ethel S. Littlefield, Joseph T. Marakovits, Robert E. Babine
-
Patent number: 5959120Abstract: The present invention provides an acetate ester compound of formula (III), ##STR1## a process for synthesizing compound (III), and a process for using that compound to prepare a pyrazolone compound, where the substituent definitions are as defined in the Summary of the Invention.Type: GrantFiled: June 12, 1997Date of Patent: September 28, 1999Assignee: Eastman Kodak CompanyInventors: Jared B. Mooberry, Thomas E. Gompf, Brian H. Johnston
-
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
-
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
-
Patent number: 5888972Abstract: A compound of the formula: ##STR1## in which R.sup.4 is acyl,R.sup.5 is lower alkyl,R.sup.6 is optionally substituted ar(lower)alkyl or optionally substituted heterocyclic-(lower)alkyl,R.sup.7 is lower alkyl or lower alkylthio(lower)alkyl,R.sup.8 is carboxy or protected carboxy,A is lower alkylene,Z is a group of the formula: ##STR2## wherein R.sup.1 is hydrogen, lower alkyl, common amino-protective group or optionally substituted ar(lower)alkyl,R.sup.2 is hydrogen, lower alkyl, optionally substituted ar(lower)alkyl, optionally substituted heterocyclic-(lower)alkyl, optionally substituted cyclo(lower)alkyl(lower)alkyl, common amino-protective group, amino(or protected amino)(lower)alkyl, optionally substituted heterocyclic-carbonyl or cyclo(lower)alkyl, andR.sup.3 is optionally substituted heterocyclic(lower)alkyl, andm is an integer of 0 to 2,or pharmaceutically acceptable salts thereof, useful as endothelin antagonist.Type: GrantFiled: June 24, 1997Date of Patent: March 30, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Keiji Hemmi, deceased, Masahiro Neya, Naoki Fukami, Natsuko Kayakiri, Hirokazu Tanaka
-
Patent number: H1950Abstract: Oxadiazines of formula I, wherein R1 is F, Cl or fluoroalkoxy and R2 is alkyl, are prepared by reacting hydrazine derivatives of formula II with a dialkoxymethane in the presence of a protic acid catalyst in an inert solvent under conditions which allow for the prompt removal of the alcohol by-product by distillation. The reaction can be combined with the preparation of the hydrazines derivatives II from the corresponding ketones and hydrazines NH2-NHR3 in the presence of the same protic acid catalyst and an inert solvent. Oxadiazines I are useful as intermediates in the preparation of arthropodicidal agents.Type: GrantFiled: February 3, 1999Date of Patent: March 6, 2001Assignee: E. I. du Pont de Nemours and CompanyInventor: Donald J. Dumas