The Chalcogen, X, Is In A -c(=x)- Group Patents (Class 546/340)
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Publication number: 20080115890Abstract: Various embodiments of the present invention are directed to molecular-film adhesives and methods and systems for using molecular-film adhesives. In one embodiment of the present invention, an amphipathic, biological-substrate-compatible adhesive is applied as a molecular-film. The amphipathic adhesive includes a first functional group, capable of bonding to a first substrate, and a second functional group, capable of bonding to a second, chemically dissimilar substrate.Type: ApplicationFiled: September 11, 2006Publication date: May 22, 2008Inventors: Sean X. Zhang, Patricia A. Beck
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Patent number: 7375121Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.Type: GrantFiled: September 23, 2002Date of Patent: May 20, 2008Assignee: AstraZeneca ABInventor: Magnus Polla
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Patent number: 7371867Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluoroleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbon-fluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.Type: GrantFiled: November 6, 2006Date of Patent: May 13, 2008Assignee: Trustees of Tufts CollegeInventors: Alfio Fichera, Zihni Bilgicer, Krishna Kumar, Xuechao Xing
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Patent number: 7342115Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptor. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: November 7, 2003Date of Patent: March 11, 2008Assignee: Neurogen CorporationInventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
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Patent number: 7297799Abstract: The invention relates to the use of compounds of formula for the preparation of medicines designed for the treatment of neuronal and cerebral disorders. The invention also relates to the compounds of formula: a process for their preparation and the pharmaceutical compositions containing them.Type: GrantFiled: November 1, 2006Date of Patent: November 20, 2007Assignee: Sanofi-AventisInventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi, Alessandra Ielmini
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Patent number: 7186722Abstract: Novel ?1-pyrrolines of the Formula (I) in which R1, R2, R3 and Het have the meanings given in the description, a plurality of processes for preparing these compounds and their use for controlling pests, and also novel intermediates and processes for their preparation.Type: GrantFiled: January 31, 2002Date of Patent: March 6, 2007Assignee: Bayer Cropscience AGInventors: Andrew Plant, Rüdiger Fischer, Thomas Seitz, Christoph Erdelen, Andreas Turberg, Olaf Hansen
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Patent number: 7151107Abstract: The invention relates to the use of compounds of formula for the preparation of medicines designed for the treatment of neuronal and cerebral disorders. The invention also relates to the compounds of formula: a process for their preparation and the pharmaceutical compositions containing them.Type: GrantFiled: May 24, 2005Date of Patent: December 19, 2006Assignee: Sanofi-aventisInventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi, Alessandra Ielmini
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Patent number: 7135574Abstract: The present invention relates to a process for the preparation of compounds of formula I wherein the substituents are as defined in claim 1, by conversion of a compound of formula II reaction of that compound with a compound of formula IV X—C(O)—Q,??(IV) wherein X is a leaving group, to form a compound of formula V and treatment of that compound in the presence of a base with catalytic amounts of cyanide ions.Type: GrantFiled: February 11, 2005Date of Patent: November 14, 2006Assignee: Syngenta Crop Protection, Inc.Inventors: Hermann Schneider, Christoph Lüthy, Andrew Edmunds
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Patent number: 7084278Abstract: The present invention provides a method for producing an optically active ?-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.Type: GrantFiled: March 5, 2003Date of Patent: August 1, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Toru Yamano, Naohiro Taya, Akio Ojida
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Patent number: 7078431Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.Type: GrantFiled: May 21, 2003Date of Patent: July 18, 2006Assignee: Atherogenics, Inc.Inventors: Charles Q. Meng, Liming Ni, James A. Sikorski, Lee K. Hoong
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Patent number: 6949656Abstract: A composition for use as an antiobestic agent and preventive or therapeutic agent for diabetes, containing a compound of the formula (I): wherein, A is substituted aryl or substituted heteroaryl with one or more group(s); (here, one of following groups is at least contained as the substituent: —RA—RB (RA is S, SO, SO2, NRC, NRCSO2 (RC is hydrogen or lower alkyl) or lower alkylene); RB is optionally substituted aryl); X is O, S, NR wherein R is hydrogen or lower alkyl, or single bond; m is an integer of 0 to 4; n is an integer of 1 to 6 p is an integer of 1 to 3, pharmaceutically acceptable salt, prodrug or hydrate thereof.Type: GrantFiled: August 2, 2001Date of Patent: September 27, 2005Assignee: Shionogi & Co., Ltd.Inventors: Toshisada Yano, Isako Sakaguchi, Goro Katsuura, Naoki Yoshikawa
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Patent number: 6936621Abstract: The invention relates to the use of compounds of formula for the preparation of medicines designed for the treatment of neuronal and cerebral disorders. The invention also relates to the compounds of formula: a process for their preparation and the pharmaceutical compositions containing them.Type: GrantFiled: December 5, 2003Date of Patent: August 30, 2005Assignee: Sanofi-AventisInventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi, Alessandra Ielmini
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Patent number: 6849741Abstract: A method for preparing a thiazolidinedione, oxazolidinedione or hydantoin compound of formula (I) from a compound of formula (II): wherein Q represents an oxygen atom or a sulfur atom; Q1 represents an oxygen atom or a sulfur atom; R1 and R2, which can be identical or different, represent a hydrogen atom, a C1-10 alkyl chain, a cycloalkyl, an alkylaryl, an arylalkyl; the alkyl, cycloalkyl, alkylaryl or arylalkyl groups being optionally substituted by an alkyl, an alkoxy or aryloxy, a halogen, a hydroxy, a sulfino, a sulfonyl, an amino such as NH2, NHR3, N(R3)2, wherein R3 represents an alkyl, an alkoxy or an alkylcarbonyl, reacting a compound of formula (II) with formic acid, either as a hydrogen donor in a hydrogen-transfer reaction or as a solvent in a hydrogenation reaction, in the presence of a catalyst containing a transition metal to obtain a corresponding compound of formula (I).Type: GrantFiled: August 7, 2003Date of Patent: February 1, 2005Assignee: PPG-SIPSYInventors: Michel Bulliard, Yvon Derrien, Tony Pintus
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Patent number: 6838564Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicidesType: GrantFiled: June 7, 2001Date of Patent: January 4, 2005Assignee: Syngenta Crop Protection, Inc.Inventors: Andrew Edmunds, Alain De Mesmaeker, Christoph Lüthy, Jürgen Schaetzer
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Patent number: 6794377Abstract: Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.Type: GrantFiled: December 5, 2001Date of Patent: September 21, 2004Assignee: Aventis Pharma Deutschland GmbHInventors: Stefan Peukert, Joachim Brendel, Horst Hemmerle, Heinz-Werner Kleemann
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Publication number: 20040171839Abstract: The invention relates to polycyclic aryl and heteroaryl substituted 1,4-quinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: ApplicationFiled: January 7, 2004Publication date: September 2, 2004Applicant: Pharmacia CorporationInventors: Michael S. South, John J. Parlow
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Patent number: 6765097Abstract: A process is described for the preparation of arylpyridine compounds by aryl-aryl cross-coupling reactions between a halopyridine and an arylmagnesium halide carried out in the presence of a catalytic amount of a zinc salt and a catalytic amount of palladium. The zinc salt is preferably selected from ZnCl2, ZnBr2 and/or Zn(OAc)2, while the palladium is preferably used in the form of Pd(PPh3)4 or Pd(OAc)2 +4 PPh3. The reaction can also be carried out in the presence of bidentate phosphines, such as, for example, 1,3-bis(diphenylphosphine)propane or 1,4-bis(diphenylphosphine)-butane. It is thus possible to obtain molar yields higher than 97% (calculated relative to the halopyridine) and a catalyticity of more than 2000.Type: GrantFiled: April 11, 2002Date of Patent: July 20, 2004Assignee: Euticals Prime European Therapeutical SpAInventors: Claudio Giordano, Claudio Pozzoli, Fabio Benedetti
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Patent number: 6749988Abstract: Novel amine compounds having a nitrogen-containing cyclic structure and a hydrating group such as a hydroxy, ether, ester, carbonyl, carbonate group or lactone ring are useful for use in resist compositions for preventing a resist film from thinning and also for enhancing the resolution and focus margin of resist.Type: GrantFiled: November 28, 2001Date of Patent: June 15, 2004Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Jun Hatakeyama, Tomohiro Kobayashi, Takeru Watanabe, Takeshi Nagata
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Patent number: 6720425Abstract: 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: December 9, 2002Date of Patent: April 13, 2004Assignee: Allergan, Inc.Inventors: 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: 6706741Abstract: The present invention provides an excellent acetylcholinesterase inhibitor. That is, it provides an acetylcholinesterase inhibitor comprising a 1-benzylpyridinium salt represented by the following formula: wherein R1, R2, R3 and R4 are the same as or different from each other and each represents a hydrogen atom, a halogen atom, a hydroxyl group, a nitrile group, a C1-6 alkyl group, a C1-6 alkoxy group etc.; R5 represents a hydrogen atom, a halogen atom etc.; the partial structure: is a group represented by the formula >C(R6)—CH2— (wherein R6 is a hydrogen atom or a halogen atom) or >C═CH—; X− represents a halide ion or organic sulfonic acid ion; and m is 0 or an integer from 1 to 5.Type: GrantFiled: September 18, 2002Date of Patent: March 16, 2004Assignee: Eisai Co., Ltd.Inventors: Yoichi Iimura, Takashi Kosasa
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Publication number: 20040029903Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, a trihalomethylcarbonyl group, such as a trifluoromethylcarbonyl group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.Type: ApplicationFiled: May 21, 2003Publication date: February 12, 2004Applicant: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
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Publication number: 20040024221Abstract: Nonmetallic, chiral organic catalysts are used to catalyze an enantioselective aldol coupling reaction between aldehyde substrates. The reaction may be carried out with a single enolizable aldehyde, resulting in dimerization to give a &bgr;-hydroxy aldehyde, or trimerization to give a dihydroxy tetrahydropyran. The reaction may also conducted with an enolizable aldehyde and a second aldehyde, which may or may not be enolizable, so that the coupling is a cross-aldol reaction in which the &agr;-carbon of the enolizable aldehyde adds to the carbonyl carbon of the second aldehyde in an enantioselective fashion. Reaction systems composed of at least one enolizable aldehyde, an optional additional aldehyde, and the nonmetallic chiral organic catalyst are also provided, as are methods of implementing the enantioselective aldol reaction in the synthesis of sugars.Type: ApplicationFiled: April 21, 2003Publication date: February 5, 2004Inventors: David W.C. MacMillan, Alan B. Northup
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Patent number: 6656711Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.Type: GrantFiled: January 29, 2002Date of Patent: December 2, 2003Assignee: Novartis AGInventors: Hans Hofmann, Marion Mahnke, Klaus Memmert, Frank Petersen, Thomas Schupp, Ernst Küsters, Michael Mutz
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Patent number: 6649623Abstract: A composition for use as an antiobestic agent and preventive or therapeutic agent for diabetes, containing a compound of the formula (I): wherein, A is optionally substituted aryl or optionally substituted heteroaryl; X is O, S, NR wherein R is hydrogen or lower alkyl, or single bond; m is an integer of 0 to 4; n is an integer of 1 to 5; p is an integer of 1 to 3, pharmaceutically acceptable salt, prodrug or hydrate thereof.Type: GrantFiled: July 20, 2001Date of Patent: November 18, 2003Assignee: Shionogi & Co., Ltd.Inventors: Toshisada Yano, Isako Sakaguchi, Goro Katsuura
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Patent number: 6638940Abstract: Compounds of formula are described, wherein R1 and R2 are for example, independently of each other, halogen, C1-C6-alkyl, C3-C6-cycloalkyl, halogen-C1-C6-alkyl, halogen-C3-C6-cycloalkyl, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl and halogen-C2-C4-alkinyl; R3 is hydrogen, OH, halogen, C1-C6-alkoxy, or —O—C(═O)—C1-C6-alkyl; R4 is for example phenyl, benzyl, phenoxy or benzyloxy, which is substituted by substituents selected from the group consisting of halogen, cyano, NO2, C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cyclalkyl-C1-C6-alkyl, halogen-C1-C6-alkyl, C1-C6-alkoxy, C3-C8-cycloalkoxy, C3-C8-cycloalkoxy-C1-C6-alkyl, C3-C8-cycloalkoxy-C1-C6-alkoxy, halogen-C1-C6-alkoxy, C2-C4-alkenyl, C2-C4-alkinyl, halogen-C2-C4-alkenyl, halogen-C2-C4-alkinyl, C2-C6-alkenyloxy, C2-C6-alkinyloxy, halogen-C2-C6-alkenyloxy, halogen-C2-C6-alkenyloxy, —NR6—C(═O)—O—C1-C6-alkyl, —NR6—C(═O)—O-halogen-C1-C6-alkyl, —C(R7)═N&Type: GrantFiled: February 25, 2002Date of Patent: October 28, 2003Assignee: Syngenta Crop Protection, Inc.Inventor: Stephan Trah
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Publication number: 20030191317Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: ApplicationFiled: December 1, 2000Publication date: October 9, 2003Applicant: G. D. Searle & Co.,Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo, Clara I. Villamil
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Publication number: 20030186941Abstract: A compound having a cyclopent-2-ene-1-one ring and also having a double bond directly attached to the ring (in addition to the C═O bond of the cyclopent-1-ene-1-one ring) may be useful in treating various disorders, including viral disorders, cancers, inflammatory disorders, etc.Type: ApplicationFiled: December 20, 2002Publication date: October 2, 2003Inventors: Stanley Michael Roberts, Maria Gabriella Santoro, Eric Emil Anggard
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Patent number: 6566379Abstract: Aminoguanidine and alkoxyguanidine compounds are described, including compounds of the Formula VII: wherein X is O or NR9 and Het, R1, R7, R8, R12-R15, Ra, Rb, Rc, Z, and n are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin. Also described are methods for preparing such compounds. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. The invention includes a composition for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation in a mammal, comprising a compound of the invention in a pharmaceutically acceptable carrier.Type: GrantFiled: September 12, 2002Date of Patent: May 20, 2003Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Thomas P. Markotan, Colleen Siedem
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Publication number: 20030087924Abstract: The invention provides dicarboxylic acid-substituted heteroaryl derivatives of the formulaType: ApplicationFiled: August 20, 2002Publication date: May 8, 2003Inventor: Roderick Joseph Sorenson
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Patent number: 6559100Abstract: Substituted 2-benzoylcyclohexane-1,3-diones of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3, —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen, C1-C6-alkyl, C1-C6-haloalkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl or phenyl-C1-C6-alkyl; where the abovementioned alkyl radicals may be partially or fully halogenated and/or may carry one to three of the following groups: hydroxyl, mercapto, amino, cyano, R3, —OR3, —SR3, —N(R3)2, ═NOR3, —OCOR3, —SCOR3, —NR3COR3, —CO2R3, —COSR3, —CON(R3)2, C1-C4-alkyliminooxy, C1-C4-alkoxyamino, C1-C4-alkylcarbonyl, C1-C4-alkoxy-C2-C6-alkoxycarbonyl, C1-C4-alkylsulfonyl, heterocyclyl, heterocyclyloxy, phenyl, benzyl, hetaryl, phenoxy, benzyloxy and hetaryloxy, where the eight last mentioned radicType: GrantFiled: February 7, 2000Date of Patent: May 6, 2003Assignee: BASF AktiengesellschaftInventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
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Publication number: 20030080323Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1Type: ApplicationFiled: July 26, 2002Publication date: May 1, 2003Applicant: FUJI PHOTO FILM CO., LTD.Inventors: Hisashi Okada, Terukazu Yanagi
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Patent number: 6555690Abstract: 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: May 8, 2002Date of Patent: April 29, 2003Assignee: Allergan, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20030069289Abstract: The present invention provides an excellent acetylcholinesterase inhibitor.Type: ApplicationFiled: September 18, 2002Publication date: April 10, 2003Inventors: Yoichi Iimura, Takashi Kosasa
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Patent number: 6541505Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: June 30, 2000Date of Patent: April 1, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Patent number: 6534445Abstract: Compounds of formula (I), in which the substituents are as defined in claim 1 and the agrochemically tolerated salts M+ and all stereoisomers and tautomers of the compounds of formula (I) are suitable for use as herbicides.Type: GrantFiled: June 22, 2001Date of Patent: March 18, 2003Assignee: Syngenta Participations AGInventors: Andrew Edmunds, Christoph Lüthy, Karl Seckinger, Alain De Mesmaeker, Walter Kunz, Jürgen Schaetzer
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Patent number: 6528533Abstract: The present invention relates to azo amino acid derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.Type: GrantFiled: January 3, 2002Date of Patent: March 4, 2003Assignee: Vertex Pharmaceuticals, IncorporatedInventors: David Lauffer, Michael Mullican
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Patent number: 6515134Abstract: It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethyl derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16).Type: GrantFiled: November 7, 2001Date of Patent: February 4, 2003Assignee: Kaneka CorporationInventors: Susumu Amano, Naoaki Taoka, Masaru Mitsuda, Kenji Inoue
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Patent number: 6498125Abstract: Compounds of formula (I) in which the substituents are as defined in claim 1 are suitable for use as herbicides.Type: GrantFiled: March 12, 2001Date of Patent: December 24, 2002Assignee: Syngenta Participations AGInventors: Andrew Edmunds, Karl Seckinger, Christoph Lüthy, Walter Kunz, Alain De Mesmaeker, Jürgen Schaetzer
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Publication number: 20020183342Abstract: Compounds of formula I: 1Type: ApplicationFiled: August 29, 2001Publication date: December 5, 2002Inventors: George Theodoridis, Edward Barron, Daniel H. Cohen, Ellen M. Crawford, Thomas G. Cullen, Hongyan Qi, Elizabeth Rowley, Syed F. Ali, Walter H. Yeager, Christina B. Duggan
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Patent number: 6476027Abstract: An N-hydroxy sulfonyl butanamide compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated N-hydroxy sulfonyl butanamide compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: December 6, 1999Date of Patent: November 5, 2002Assignee: Monsanto CompanyInventors: Clara I. Villamil, John N. Freskos, Brent V. Mischke, Patrick B. Mullins, Robert M. Heintz, Daniel P. Getman, Joseph J. McDonald, Gary A. DeCrescenzo, Thomas E. Barta, Daniel P. Becker
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Patent number: 6465646Abstract: Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: October 15, 2002Assignee: Allergan, Inc.Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
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Patent number: 6465647Abstract: Compounds of the Formula 1, Formula 2, Formula 3 and Formula 4 wherein the symbols have the meaning assigned to them in the disclosure have retinoid-like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: October 15, 2002Assignee: Allergan, Inc.Inventors: Richard L. Beard, Diana F. Colon, Roshantha A. Chandraratna
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Patent number: 6458957Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.Type: GrantFiled: July 12, 2000Date of Patent: October 1, 2002Assignee: Geneva Pharmaceuticals, Inc.Inventors: Anup K. Ray, Hiren Patel, Shilpa V. Merai, Mahendra R. Patel
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Patent number: 6444688Abstract: The instant invention provides compounds of formula I wherein R1 is OH, O—C(O)—(C1-C6 alkyl), O—C(O)—O(C1-C6 alkyl), O—C(O)—Ar, or O—C(O)—O—Ar; R2 is H, OH, O(C1-C6 alkyl), O—C(O)—(C1-C6 alkyl), O—C(O)—O(C1-C6 alkyl), O—C(O)—Ar, O—C(O)—O—Ar, O—SO2—(C4-C6 alkyl), chloro, fluoro, or bromo; V is S, O, or CH2CH2; W is CHOH, C(O), or CH2; X is (CH2)n; R3 and R4 each, independently, are H, C1-C6 alkyl, C(O)—(C1-C6 alkyl), C(O)—NH—(C1-C6 alkyl), C(O)—Ar, or together with the nitrogen to which they are attached form a 5- or 6-membered imide or cyclic amide; n is 1, 2, or 3; and Ar is optionally substituted phenyl; povided that at least one of R3 and R4 contains a carbonyl functional group, and their use in the treatment of estrogen deficiency pathologies.Type: GrantFiled: June 7, 1995Date of Patent: September 3, 2002Assignee: Eli Lilly and CompanyInventors: Jeffrey A. Dodge, Charles D. Jones, Kristin Marron, James P. Sluka, Mark G. Stocksdale
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Publication number: 20020087030Abstract: A process for preparing polymerizable biaryl derivatives comprises reacting an aromatic comprising a 6-membered ring which bears ester or benzylic OH groups in the 1,4 position with a second aromatic in a palladium-catalyzed cross-coupling reaction to give a biaryl and converting the ester or benzylic OH groups into polymerizable groups in one or more steps. The biaryls obtained are suitable for preparing polymers which are used as electroluminescence materials.Type: ApplicationFiled: October 16, 2001Publication date: July 4, 2002Inventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
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Publication number: 20020058672Abstract: The invention relates to the use of compounds of formula 1Type: ApplicationFiled: November 20, 2001Publication date: May 16, 2002Inventors: Marco Baroni, Rosanna Cardamone, Jacqueline Fournier, Umberto Guzzi, Alessandra Ielmini
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Patent number: 6380227Abstract: The invention relates to a new process for concentrating epothilones in culture media, a new process for the production of epothilones, a new process for separating epothilones A and B and a new strain obtained by mutagenesis for the production of epothilones, as well as aspects related thereto. New crystal forms of epothilone B are also described.Type: GrantFiled: September 7, 2000Date of Patent: April 30, 2002Assignee: Novartis AGInventor: Michael Mutz
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Publication number: 20020042376Abstract: This invention is directed to novel oxamyl dipeptide ICE/ced-3 family inhibitor compounds. The invention is also directed to pharmaceutical compositions containing these compounds, as well as to the use of such compositions in the treatment of patients suffering inflammatory, autoimmune and neurodegenerative diseases, for the prevention of ischemic injury, and for the preservation of organs that are to undergo a transplantation procedure.Type: ApplicationFiled: January 16, 2001Publication date: April 11, 2002Inventors: Donald S. Karanewsky, Robert J. Ternansky, Steven D. Linton, Thang Dinh
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Patent number: 6369227Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.Type: GrantFiled: December 22, 1999Date of Patent: April 9, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Patrick Y. S. Lam, Charles G. Clark, Renhau Li, Donald J. P. Pinto
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Patent number: 6358987Abstract: A compound of formula (I) wherein X is —COOH or —CONHOH Y is a group of formula (ID) or (IE) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.Type: GrantFiled: March 5, 2001Date of Patent: March 19, 2002Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker