The Nitrogen Is Bonded Directly To A Ring And Is In Same Side Chain As Ester Function Patents (Class 560/43)
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Patent number: 6743940Abstract: There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula wherein R1 and R2 are each independently of the other hydrogen, C1-C20alkyl; C3-C12cycloalkyl; unsubstituted or C1-C5alkyl-, C3-C12cycloalkyl-, C1-C5alkoxy-, C3-C12cycloalkoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C12cycloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl, phenyl-C1-C5alkyl, naphthyl and naphthyl-C1-C5alkyl; and R3 is C1-C20alkyl; C3-C12cycloalkyl. The compounds exhibit a pronounced activity against gram-positive and gram-negative bacteria, and also against yeasts and moulds.Type: GrantFiled: December 13, 2001Date of Patent: June 1, 2004Assignee: Ciba Specialty Chemicals CorporationInventors: Werner Hölzl, Wolfgang Haap, Jürgen Koppold, Dietmar Ochs, Karin Petzold, Marcel Schnyder
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Patent number: 6696489Abstract: The present invention provides novel 2-methylpropionic acid derivatives represented by the general formula: (wherein R1 represents a hydrogen atom, a lower alkyl group or an aralkyl group; R2 represents a hydrogen atom a lower alkyl group or a halogen atom; A represents an oxygen atom or an imino group; the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have excellent &bgr;3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of the biliary tract.Type: GrantFiled: October 13, 2000Date of Patent: February 24, 2004Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Tetsuro Tamai, Nobuyuki Tanaka, Harunobu Mukaiyama, Akihito Hirabayashi, Hideyuki Muranaka, Masaaki Sato, Masuo Akahane
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Patent number: 6689897Abstract: This invention relates to intermediates useful in the preparation of CETP inhibitors and methods of preparation thereof.Type: GrantFiled: April 30, 2002Date of Patent: February 10, 2004Assignee: Pfizer Inc.Inventors: David B. Damon, Robert W. Dugger, Robert W. Scott
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Publication number: 20040024224Abstract: Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.Type: ApplicationFiled: May 15, 2003Publication date: February 5, 2004Applicant: Genzyme CorporationInventors: Mukund S. Chorghade, Mukund K. Gurjar, Debendra K. Mohapatra
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Patent number: 6683201Abstract: The present invention relates to compounds of formula (I) wherein U, Y, V, W, L, X, A1, A2, A3, A4, A5 and A6 are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and/or treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: July 16, 2001Date of Patent: January 27, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Jean Ackermann, Johannes Aebi, Alexander Chucholowski, Henrietta Dehmlow, Olivier Morand, Sabine Wallbaum, Thomas Weller
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Patent number: 6683213Abstract: The present invention relates to substituted aniline compounds of the formula 1 in which R21, R22 and R23 have the meanings indicated in the description. The compounds according to the invention are intermediates for the preparation of herbicidally active pyridinedicarboxamide compounds.Type: GrantFiled: September 11, 2001Date of Patent: January 27, 2004Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Olaf Menke, Michael Puhl, Robert Reinhard, Ingo Sagasser, Cyrill Zagar
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Patent number: 6683110Abstract: A novel class of methyl esters of substituted 4-oxo-2-butenoic acids and their derivatives are disclosed along with the surprising use property of these compounds as a bacteriostatic agents for humans or non-humans against mycobacteria. These compounds include: 4-(4-Ethoxy-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-4-oxo-but-2-enoic acid methyl ester; 4-(4-Ethoxy-phenyl)-2-(N′-fluoren-9-ylidene-hydrazino)-2-hydroxy-4-oxo-butyric acid methyl ester; 2-(4-Bromo-phenylamino)-5,5-dimethyl-4-oxo-hex-2-enoic acid methyl ester; A pharmaceutical composition is disclosed as well as the method of treating human and non-humans infected with M. tuberculosis and related mycobacteria.Type: GrantFiled: May 22, 2002Date of Patent: January 27, 2004Assignee: University of Central FloridaInventors: D. Howard Miles, Krasnykh Olga Petrovna, Saleh Naser, Solodnikov Sergey Yurjevich, Elena A. Goun, Suslonov Vladimir Michailovich
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Patent number: 6680340Abstract: This invention provides a drug combination comprised of a thyroid hormone receptor beta agonist with a fibrate in therapeutically effective amounts, which is useful for reducing cholesterol synthesis, lowering plasma cholesterol levels and lowering plasma triglyceride levels.Type: GrantFiled: February 13, 2003Date of Patent: January 20, 2004Assignee: Merck & Co., Inc.Inventors: Kang Cheng, Samuel D. Wright, Tsuei-Ju Wu
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Patent number: 6667413Abstract: The present invention relates to an uracil compound of the formula [I]: wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl; R2 represents C1 to C3 alkyl; R4 represents hydrogen or methyl; R5 represents C1 to C6 alkyl, C1 to C6 haloalkyl, or the like; X1 represents halogen, cyano or nitro; X2 represents hydrogen or halogen; and each of X3 and X4 independently represents hydrogen, halogen, C1 to C6 alkyl, or the like. The present compound has an excellent herbicidal activity.Type: GrantFiled: July 12, 2002Date of Patent: December 23, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitomo Tohyama, Yuzuru Sanemitsu, Tomohiko Gotou
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Patent number: 6653258Abstract: Fungicidal compounds of the formula (I): and stereoisomers thereof, wherein R1 is optionally substituted aryl or optionally substituted heteroaryl; Y is oxygen, sulphur or NR4; R2, R3 and R4, which may be the same or different, are hydrogen, C1-4 alkyl or C2-4 alkenyl; X is halogen, C1-4 alkyl, C2-4 alkenyl, C1-4 alkoxy, nitro or cyano, and n is 0 or an integer of 1 to 4; provided that when Y is oxygen, n is 0 and R1 is unsubstituted phenyl at least one of R2 and R3 is other than hydrogen or methyl.Type: GrantFiled: March 27, 1995Date of Patent: November 25, 2003Assignee: Syngenta LimitedInventors: John M Clough, Christopher R A Godfrey, Paul J de Fraine, Michael G Hutchings, Vivienne M Anthony
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Patent number: 6653483Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.Type: GrantFiled: April 17, 2000Date of Patent: November 25, 2003Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6624184Abstract: The present invention discloses the identification of the inhibitors of IMPDH (inosine-5′-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.Type: GrantFiled: October 27, 1999Date of Patent: September 23, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Henry H. Gu, T. G. Murali Dhar, Edwin J. Iwanowicz
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Patent number: 6613308Abstract: A method for treating a disorder of the central nervous system includes administering to the respiratory tract of a patient a drug which is delivered to the pulmonary system, for instance to the alveoli or the deep lung. The drug is administered at a dose which is at least about two-fold less than the dose required by oral administration. Particles that include the drug can be employed. Preferred particles have a tap density of less than about 0.4 g/cm3. In addition to the medicament, the particles can include other materials such as, for example, phospholipids, amino acids, combinations thereof and others.Type: GrantFiled: June 8, 2001Date of Patent: September 2, 2003Assignee: Advanced Inhalation Research, Inc.Inventors: Raymond T. Bartus, Dwaine F. Emerich
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Patent number: 6610700Abstract: Enamine derivatives of formula (1) are described: wherein R1 is a group Ar1 L2Ar2Alk- in which Ar1 is an aromatic or heteroaromatic group, L2 is a covalent bond or a linker atom or group, Ar2 is an arylene or heteroarylene group and Alk is a chain —CH2—CH(R)—, —CH═C(R)— or in which R is a carboxylic acid or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6alkyl group; Cy is a cycloaliphatic or heterocycloaliphatic ring in which X is a N atom or a C(Rw) group; Rx is a oxo, thioxo, or imino group; Rw and Rz is each a hydrogen atom or optional substituent; provided that Cy is not a cyclobutenedione group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders, or disorders involving the inappropriate growth or migration of cells.Type: GrantFiled: April 16, 2001Date of Patent: August 26, 2003Assignee: Celltech R & D LimitedInventors: Timothy John Norman, John Robert Porter, Brian Woodside Hutchinson, Andrew James Ratcliffe, John Clifford Head, Rikki Peter Alexander, Barry John Langham, Graham John Warrellow, Sarah Catherine Archibald, Janeen Marsha Linsley
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Patent number: 6602869Abstract: This invention relates to novel compounds of formula (I) wherein R1 represents a polymer, aryl or alkyl group, R2 represents a hydrogen atom, a halogen atom, a radical CN, CF3, OH, OCF3, COOH, R7, OR7 or OCOR7, R3 represents an aryl or alkyl halogen, R4 represents an alkyl radical. The invention also relates to a cosmetic composition comprising said compounds and to the use thereof to reduce and/or curb hair loss i.e. to increase and/or stimulate the growth of said hair.Type: GrantFiled: November 21, 2001Date of Patent: August 5, 2003Assignee: L'Oreal S.A.Inventors: Jean-Baptiste Galey, Maria Dalko, Lionel Breton
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Patent number: 6583180Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof are novel glucocorticoid receptor modulators and are useful for treating type II diabetes in a mammal.Type: GrantFiled: February 8, 2002Date of Patent: June 24, 2003Assignee: Abbott LaboratoriesInventors: James T. Link, Bryan K. Sorensen, Jyoti R. Patel, David L. Arendsen, Gaoquan Li
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Patent number: 6576791Abstract: Novel compounds, pharmaceutical compositions and methods are disclosed for producing local anesthesia of long-duration. The compounds of this invention are multibinding compounds that comprise from 2 to 10 ligands covalently attached to a linker or linkers, each ligand being capable of binding to a ligand binding site in a voltage-gated Na+ channel to modulate the biological processes/functions thereof.Type: GrantFiled: October 3, 2000Date of Patent: June 10, 2003Assignee: Theravance, Inc.Inventors: Sabine M. Axt, Timothy J. Church, Witold N. Hruzewicz, John R. Jacobsen, Thomas E. Jenkins, Yu-Hua Ji, J. Kevin Judice
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Patent number: 6566554Abstract: The present invention relates to a compound of general formula (I) wherein R1, R2, and R3 represents one or more, same or different substituents selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)akylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, or nitro; further R2 can be hydrogen, and R3 can be carboxy and carbamoyl; R4 represents hydrogen, (C1-C3)alkyl, or allyl; X represents oxygen or sulphur; Q represents —(CO)—, —(CS)—, or a bond; Y represents (C5-C15)alkyl; (C2-C15)olefinic group; (C3-C10)monocyclic hydrocarbon group; or phenyl; any of which may be optionally substituted by one or more, same or different substituents selected from the group consisting of the formula R5 defined below; (C1-C4)alkyl substituted by one or more substituents selected for the group R5; or a group of the formula —(Z—O)n—Z, wherein Z is a (C1-C3)alkyl, n is anType: GrantFiled: February 22, 2002Date of Patent: May 20, 2003Assignee: Leo Pharmaceutical Products Ltd. a/s (Lovens Kemiske Fabrik Produktionsaktieselskab)Inventor: Erik Rytter Ottosen
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Patent number: 6548534Abstract: This invention describes the new, nonsteroidal gestagens of general formula I in which A, B, Ar1, R1, R2 and R3 have the meanings that are indicated in more detail in the description. The new compounds show a very great affinity to the gestagen receptor. They can be used alone or in combination with estrogens in contraceptive preparations. In addition, they can be used for treating endometriosis. Together with estrogens, they can also be used in preparations for treating gynecological disorders, for treating premenstrual symptoms and for substitution therapy. Based on the androgenic action, they can also be used for male birth control, male HRT and hormone therapy and for treating andrological disease agents.Type: GrantFiled: July 27, 2001Date of Patent: April 15, 2003Assignee: Schering AktiengesellschaftInventors: Manfred Lehmann, Klaus Schoellkopf, Peter Strehlke, Nikolaus Heinrich, Karl-Heinrich Fritzemeier, Rolf Krattenmacher, Hans-Peter Muhn
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Publication number: 20030055076Abstract: Novel compounds of the general formula (I), the use of these compounds as medicaments, pharmaceuticaly compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR). The compounds exert their effects by modulating the PPAR&ggr; response in a partial agonist manner.Type: ApplicationFiled: July 30, 2002Publication date: March 20, 2003Inventors: Lone Jeppesen, Paul Stanley Bury, John Patrick Mogensen, Ingrid Pettersson, Per Sauerberg
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Patent number: 6498004Abstract: This invention provides a photographic element comprising at least one silver halide emulsion layer in which the silver halide is sensitized with a compound of the formula (a): &Dgr;−(t)m−XY′ (a) XY′−(t)m−&Dgr; (b) &Dgr;−(t)m−XY′−(t)m−&Dgr; (c) wherein &Dgr; is protective group that is eliminated during development of the photographic element, t is a timing group, m is an integer from 0 to 3, and XY′ is a fragmentable electron donor moiety in which X is an electron donor group and Y′ is a leaving proton H or a leaving group Y, with the proviso that if Y′ is a proton, a base, &bgr;−, is present in the emulsion or is covalently linked directly or indirectly to X, and wherein: 1) X—Y′ has an oxidation potential between 0 and about 1.Type: GrantFiled: December 28, 2000Date of Patent: December 24, 2002Assignee: Eastman Kodak CompanyInventors: Jerome R. Lenhard, Annabel A. Muenter, Stephen A. Godleski, Paul A. Zielinski, Deepak Shukla, Donald R. Diehl
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Patent number: 6495693Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 30, 1999Date of Patent: December 17, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Warren J. Porter, Eugene D. Thorsett, Jing Wu
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Patent number: 6489511Abstract: Disclosed is a process for forming an azomethine compound, comprising: (a) reacting a compound “A” having an active methylene group or methine group with an arylprimaryamine compound “B”; (b) in the presence of a base and an oxidizing agent and in a solvent medium containing a ketone compound having the formula R1C(O)R2 wherein R1 and R2 are independently C1-C4 alkyl groups; (c) at a temperature low enough to provide a yield of the azomethine product of at least 50 mole % based on compound A.Type: GrantFiled: August 16, 2001Date of Patent: December 3, 2002Assignee: Eastman Kodak CompanyInventor: Garry D. Jones
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Patent number: 6469199Abstract: New secondary amines are described which are prepared from inexpensive, commercially available raw materials, are stable at room temperature, and are reactive toward electrophiles. The secondary amines are prepared by the addition of one or more primary amines with one or more male (amide/ester) and fumar (amide/ester) Michael receptors. The above amines can be used as coreactants with aliphatic polyisocyanates for polyurea coatings. The novel secondary amines are also described as particularly useful as part of a two-part liquid pavement marking composition for pavement markings.Type: GrantFiled: August 24, 1999Date of Patent: October 22, 2002Assignee: 3M Innovative Properties CompanyInventors: Richard G. Hansen, Dean M. Moren, Mark D. Purgett
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Publication number: 20020115881Abstract: There are described 4-aminobut-2-ynecarboxylic acid derivatives of formula 1Type: ApplicationFiled: December 13, 2001Publication date: August 22, 2002Inventors: Werner Holzl, Wolfgang Haap, Jurgen Koppold, Dietmar Ochs, Karin Petzold, Marcel Schnyder
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Patent number: 6409995Abstract: Use of amino-substituted hydroxybenzophenones of the formula I in which the variables have the meanings explained in the description, as photostable UV filters in cosmetic and pharmaceutical preparations for protecting human skin or human hair from the sun's rays, alone or together with compounds which absorb in the UV region and are known per se for cosmetic and pharmaceutical preparations.Type: GrantFiled: April 20, 2000Date of Patent: June 25, 2002Assignee: BASF AktiengesellschaftInventors: Thorsten Habeck, Frank Prechtl, Thomas Wünsch, Horst Westenfelder, Sylke Haremza, Thorsten Bach, Anja Spiegel
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Patent number: 6407247Abstract: A method of using compounds of formula I in which the C═C double bond is present in E and/or Z configuration and the variables have the following meanings: R1 denotes COOR5, COR5, CONR5R6, CN, O═S(—R5)═O, O═S(═OR5)═O, R7O—P(—OR8)═O; R2 denotes COOR6, COR6, CONR5R6, CN, O═S(—R6)═O, O═S(═OR6)═O, R7O—P(—OR8)═O; R3 denotes hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms; R4 denotes an optionally substituted aromatic or heteroaromatic radical containing from 5 to 12 ring atoms; R5 to R8 independently denote hydrogen, an open-chain or branched-chain aliphatic, araliphatic, cycloaliphatic or optionally substituted aromatic radical containing in each case up to 18 carbon atoms, where the variables R3 to R8 may also form, together with the carbon atoms to which they are attached, a 5-membered or 6-memberedType: GrantFiled: January 31, 2000Date of Patent: June 18, 2002Assignee: BASF AktiengesellschaftInventors: Thorsten Habeck, Alexander Aumüller, Volker Schehlmann, Horst Westenfelder, Thomas Wünsch
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Patent number: 6399628Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: March 12, 1999Date of Patent: June 4, 2002Assignees: Athena Neurosciences, Inc., Eli Lilly & CompanyInventors: James E. Audia, Beverly K. Folmer, Varghese John, Lee H. Latimer, Jeffrey S. Nissen, Jon K. Reel, Eugene D. Thorsett, Celia A. Whitesitt
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Publication number: 20020065229Abstract: It is presently accepted that the mechanism of action for all anti-tumor tubulin ligands involves the perturbation of microtubule dynamics during the G2/M phase of cell division and subsequent entry into apoptosis (1). In this invention, we report a novel tubulin ligands which have a unique mechanism of action. These compounds,. halogenated derivatives of acetamido benzoyl ethyl ester (HAABE), arrest cancer cells in S-phase and cause cell death by a combination of apoptosis (DNA ladder) and necrosis (DNA degradation) type mechanisms. Normal cells are not affected at the same concentrations of compound. The ligands bind covalently to tubulin in vitro and in vivo and shows potent cancericidal activity in tissue culture assays and in animal tumor models. These compounds target early S-phase at the G1/S transition rather than the G2/M phase and mitotic arrest.Type: ApplicationFiled: November 29, 2000Publication date: May 30, 2002Inventors: Ashley Stuart Davis, Kim Maria Middleton, Jian-Dong Jiang, J George Bekesi
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Patent number: 6391915Abstract: This invention relates to new propanolamine derivatives presented by the following formula [I]: wherein R1 hydrogen or lower alkenyloxy, R2 is carboxy(lower)alkoxy or protected carboxy(lower)alkoxy, R3 is hydrogen or N-protective group, n is an integer of 1 or 2, and salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic and anti-pollakisuria activities, to processes for the preparation thereof and to a pharmaceutical composition comprising the same.Type: GrantFiled: September 15, 1999Date of Patent: May 21, 2002Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Norio Hashimoto, Takumi Okamoto, Kazunori Tsubaki, Yasuyo Tomishima, Hisashi Takasugi
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Patent number: 6392111Abstract: Olefins containing aromatic substituents are synthesized without the addition of phosphonium salts or phosphanes with the aid of a PdII compound as a catalyst in the presence of nitrogen-containing additives such as N,N-dimethylglycine and a base.Type: GrantFiled: March 21, 2001Date of Patent: May 21, 2002Assignee: Studiengesellschaft Kohle mbHInventors: Manfred T. Reetz, Gunther Lohmer, Renate Lohmer, Elke Westermann
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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
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Patent number: 6380256Abstract: Compounds having Formula 4 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 30, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Roshantha A. Chandraratna
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Patent number: 6369194Abstract: The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.Type: GrantFiled: November 9, 1998Date of Patent: April 9, 2002Assignee: Yale UniversityInventor: Harry H. Wasserman
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Patent number: 6369260Abstract: Process for the preparation of a pharmacologically active chemical combination constituted by the association, through chemical bonds, of units equal to one another, having each an own pharmacological activity, and with the general formula (I): M—A—X—B—M, where M indicates said unit having an own pharmacological activity, X indicates a “bidentate” structure suitable to interconnect the M units, A and B indicate functional groups either equal to or different from one another which allow the interconnection between M and X.Type: GrantFiled: May 16, 1997Date of Patent: April 9, 2002Assignees: Laboratori Alchemica S.r.l., Nicox SAInventors: Francesco Sannicolo′, Tiziana Benincori, Piero Del Soldato
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Patent number: 6348614Abstract: Novel aminobutyric acids derivatives and methods for protecting crops against fungal diseases by applying to the crops or their locus a composition containing an effective amount of said derivatives.Type: GrantFiled: June 25, 1999Date of Patent: February 19, 2002Assignee: Agrogene Ltd.Inventors: Yogal Cohen, Moshe Korat
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Publication number: 20020006956Abstract: This invention relates to new propanolamine derivatives presented by the following formula [I]: 1Type: ApplicationFiled: September 15, 1999Publication date: January 17, 2002Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Norio Hashimoto, Takumi Okamoto, Kazunori Tsubaki, Yasuyo Tomishima, Hisashi Takasugi
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Patent number: 6333432Abstract: Fungicidal compositions and methods comprising acylated aminosalicylamides (AASA) described herein. Novel amines and 3-nitrosalicylamides, and their use as pesticides and in the preparation of the antifungal AASA compounds are also disclosed.Type: GrantFiled: May 1, 2000Date of Patent: December 25, 2001Inventors: Gina M. Fitzpatrick, Ann B. Orth, Maurice C. H. Yap, Richard B. Rogers, Todd L. Werk, George E. Davis
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Patent number: 6326014Abstract: The invention relates to the use of oxamate derivatives in a composition, as agents for depigmenting and/or bleaching human skin, head hair and/or other hairs. The invention also relates to a process for depigmenting and/or bleaching the skin, head hair and/or other hairs, which includes applying a composition comprising oxamate derivatives to human skin, head hair and/or other hairs.Type: GrantFiled: May 16, 2000Date of Patent: December 4, 2001Assignee: L, OrealInventors: Remy Tuloup, Michel Philippe
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Patent number: 6303649Abstract: A compound of formula (I), wherein R1 is carboxy or protected carboxy, R2 and R3 are each independently hydrogen, hydroxy, or protected hydroxy, R4 is hydrogen or halogen, R5 is aryl substituted with halogen, amino, hydroxy or protected hydroxy, R6 is aryl optionally substituted with halogen, amino, hydroxy or protected hydroxy, A1 and A2 are each independently lower alkylene, and (II) is (III), (IV), (V) or (VI) or its salt, process for preparing it, a pharmaceutical composition including it, and a use thereof.Type: GrantFiled: August 4, 2000Date of Patent: October 16, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kouji Hattori, Hiromichi Itani, Akira Tanaka, Toshifumi Shiraga
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Publication number: 20010029306Abstract: The present invention is a process to prepare on of a phenylisoserine ester of the formula (II)Type: ApplicationFiled: February 28, 2001Publication date: October 11, 2001Inventor: Peter Guillaume Marie Wuts
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Patent number: 6294109Abstract: A new class of mesogenic compounds has the formula: where R1 is an ester (—COO—) group; R2 is H, NO2, CN, F, or Cl; R3 is H, CH2═CH, or (CH3)3Si; k is 1 or 2; q is 0 or 1; m is from 2 to 16; n is from 2 to 12; r is from 0 to n−1 (but not greater than 3 or 4); s=1 when r=0, s=0 when r≠0; x is from 0 to 4; and * denotes the position of a chiral carbon. Compounds within this class will have a smectic A* phase, and in some cases a smectic C* phase. Mixtures including one or more of these mesogenic compounds will be useful for a variety of applications.Type: GrantFiled: June 13, 1995Date of Patent: September 25, 2001Assignee: The United States of America as represented by the Secretary of the NavyInventors: Banahalli R. Ratna, Ranganathan Shashidhar, Jawad Naciri, Gregory P. Crawford, Joel M. Schnur
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Publication number: 20010020097Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: ApplicationFiled: March 30, 1999Publication date: September 6, 2001Inventors: JAMES E. AUDIA, BEVERLY K. FOLMER, VARGHESE JOHN, LEE H. LATIMER, JEFFREY S. NISSEN, WARREN J. PORTER, EUGENE D. THORSETT, JING WU
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Patent number: 6262302Abstract: Disclosed are compounds which inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed pharmaceutical compositions comprising a compound which inhibits &bgr;-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.Type: GrantFiled: September 17, 1999Date of Patent: July 17, 2001Assignees: Elan Pharmaceuticals, Inc., Eli Lilly & CompanyInventors: Jing Wu, Jay S. Tung, Jeffrey S. Nissen, Thomas E. Mabry, Lee H. Latimer, Clark N. Eid, James E. Audia
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Patent number: 6228884Abstract: If the R-enantiomer of metalaxyl, furalaxyl or benalaxyl is used, this results in a markedly increased biodegradability of these plant fungicides in the soil and a higher activity on the plants, as compared with the data of the racemic active ingredients. Fungicidal compositions exhibiting said improved properties comprise either of these fungicides with a content of R-enantiomer of more than 70 percent by weight based on the total amount of active ingredient.Type: GrantFiled: October 19, 1998Date of Patent: May 8, 2001Assignee: Syngenta Investment CorporationInventors: Cosima Nuninger, John Edward Nicholas Goggin, Dino Sozzi, Holm Ellgehausen
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Patent number: 6229020Abstract: A new reagent for preparation of a caged compound in accordance with the present invention is a compound having, as a basic structure, an N-succinimidyl cinnamate structure expressed by the following formula 1: Another reagent for preparation of a caged compound in accordance with the present invention is a compound having, as a basic structure, a p-nitrophenyl cinnamate structure expressed by the following formula 3:Type: GrantFiled: January 11, 2000Date of Patent: May 8, 2001Assignee: Laboratory of Molecular BiophotonicsInventor: Hirofumi Shiono
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Publication number: 20010000513Abstract: Biphenyl butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1 and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells.Type: ApplicationFiled: December 14, 2000Publication date: April 26, 2001Inventors: Claude Forsey Purchase, Bruce David Roth, Gerald Paul Schielke, Lary Craswell Walker, Andrew David White
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Patent number: 6187910Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.Type: GrantFiled: May 12, 1999Date of Patent: February 13, 2001Assignee: NeoRx CorporationInventor: Sudhakar Kasina
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Patent number: 6180815Abstract: The present invention provides compounds which inhibit an envelope virus by inhibiting the fusion of the virus with the host cell. The virus may be inhibited in an infected cell, a cell susceptible of infection or a mammal in need thereof.Type: GrantFiled: April 10, 2000Date of Patent: January 30, 2001Assignee: Eli Lilly and CompanyInventors: Scott C. Mauldin, John E. Munroe
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Patent number: 6172239Abstract: The invention relates to compounds of the formula The compounds have agreat affinity for the neurotensin receptors.Type: GrantFiled: August 16, 1999Date of Patent: January 9, 2001Assignee: SanofiInventors: Bernard Labeeuw, Danielle Gully, Francis JeanJean, Jean-Charles Molimard, Robert Boigegrain