Polycyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 549/354)
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Publication number: 20080262076Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain with binding affinities towards dopamine receptors, in particular dopamine D2 receptors, towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also a pharmaceutically acceptable acid or base addition salt thereof, an N-oxide form thereof or a quaternary ammonium salt thereof, wherein all substituents are defined as in Claim 1.Type: ApplicationFiled: June 16, 2006Publication date: October 23, 2008Inventors: Jose Maria Cid-Nunez, Andres Avelino Trabanco-Suarez
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Publication number: 20080214832Abstract: Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine.Type: ApplicationFiled: December 21, 2007Publication date: September 4, 2008Inventors: Jie Zhu, Rolf Keltjens, Judith Firet
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Patent number: 7417155Abstract: A new artemisinin derivatives, of following general formula (I): In which: a and b represent a single or a double bond, n1 and n2 represent 0 or 1, R1 represents a fluoroalkyl group or a fluoroaryl group, R2 represents a hydrogen atom, or a halogen atom, or a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R3 represents a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R4 represents H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.Type: GrantFiled: October 25, 2002Date of Patent: August 26, 2008Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Michèle Ourevitch, Fatima Chorki, Fabienne Grellepois, Guillaume Magueur
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Publication number: 20080194764Abstract: The present invention relates to a novel fluorine-containing cyclic compound that is derived from a norbornadiene and hexafluoroacetone and has an oxacyclopentane structure. This compound may be represented by the following formula (1) or (2). Furthermore, the present invention relates to a fluorine-containing polymer compound prepared by a polymerization or copolymerization using this fluorine-containing cyclic compound or its derivative. By using such fluorine-containing polymer compound, it is possible to provide a superior resist material and a fine pattern forming process using the same.Type: ApplicationFiled: November 16, 2007Publication date: August 14, 2008Applicant: Central Glass Company LimitedInventors: Haruhiko KOMORIYA, Shinichi SUMIDA, Katsunori KAWAMURA, Satoru KOBAYASHI, Satoru MIYAZAWA, Kazuhiko MAEDA
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Patent number: 7410997Abstract: Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR? (wherein R and R? are the same as the above defined R); Y is, for example, CH, CH2 or C?O; Z is, for example, O, S, S?O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided. These compounds are characterized in having a wide range of pharmacological actions such as an excellent relaxing action of tracheal smooth muscles, an inhibition of airway hypersensitivity and an inhibition of infiltration of inflammatory cells into the airway and, in addition, high safety.Type: GrantFiled: December 5, 2003Date of Patent: August 12, 2008Assignee: Nippon Sulsan Kaisha, Ltd.Inventors: Shuji Jinno, Takaaki Okita, Naomi Ohtsuka, Shinya Yamashita, Junichiro Hata, Jiro Takeo
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Patent number: 7390831Abstract: The present invention is directed to tetracyclic steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.Type: GrantFiled: February 16, 2007Date of Patent: June 24, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Ningyi Chen, Nareshkumar F. Jain, Zhihua Sui
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Publication number: 20080139642Abstract: The invention provides a type of artemisinin derivatives having following structure I, its preparation method and use, as well as a pharmaceutical composition containing such artemisinin derivatives and its use. The artemisinin derivatives of the present invention and their pharmaceutical composition containing the artemisinin derivatives. have immunosuppressive activities and can be used more safely. The composition which comprises the artemisinin derivatives can be formulated into long-term dosage forms such as tablet, pellet and the like, and have wider productive and use value.Type: ApplicationFiled: January 27, 2006Publication date: June 12, 2008Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Ying Li, Jianping Zuo, Zhongshun Yang, Wenliang Zhou, Yi Sui, Junxia Wang, Yu Zhang, Yu Zhou, Jinming Wu
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Patent number: 7375099Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds are ?-secretase inhibitors. Thus, the invention also relates to pharmaceutical compositions containing these compounds and to a method of treating Alzheimer's disease by administering the compounds of the invention.Type: GrantFiled: January 29, 2004Date of Patent: May 20, 2008Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Helmut Jacobsen, Eric Argirios Kitas, Jens-Uwe Peters
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Publication number: 20080090026Abstract: The present invention relates to a liquid-crystal display of the PSA (polymer sustained alignment) type, and to novel liquid-crystal media and novel polymerizable compounds for use in PSA displays.Type: ApplicationFiled: October 11, 2007Publication date: April 17, 2008Inventors: Georg Bernatz, Andreas Taugerbeck
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Patent number: 7312203Abstract: The present invention relates to 1-aza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: May 20, 2003Date of Patent: December 25, 2007Assignee: GlaxoSmithKline istraziva{hacek over (c)}ki Centar Zagreb d.o.o.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic
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Patent number: 7288543Abstract: A compound of the formula (I) (I) wherein the variables X1 to X6, Ra, Rb, R1 to R7 including R3?, E, p, j, y, z, A, B and C are as described or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosedType: GrantFiled: March 8, 2005Date of Patent: October 30, 2007Assignee: Eli Lilly and CompanyInventors: Howard Barff Broughton, Nuria Diaz Buezo, Charles Howard Mitch, Concepcion Pedregal-Tercero
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Patent number: 7282598Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having “n” procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4?8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8?8), (8?6), and (6?6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (?)-epicatechin is produced under certain conditions.Type: GrantFiled: March 11, 2004Date of Patent: October 16, 2007Inventors: Leo J. Romanczyk, Jr., Amit Basak, Craig A. Townsend
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Publication number: 20070197634Abstract: The present invention is directed to tetracyclic steroid derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by a progesterone or glucocorticoid receptor.Type: ApplicationFiled: February 16, 2007Publication date: August 23, 2007Inventors: Ningyi Chen, Nareshkumar F. Jain, Zhihua Sui
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Patent number: 7205332Abstract: The present invention relates to a new deoxoartemisinin dimer and trimer, which have excellent anticancer activity and lower toxicity and are stable to acids, to a new deoxoartemisinin monomer of intermediate thereof, to preparations thereof, and to anticancer agents comprising the deoxoartemisinin dimer or trimer.Type: GrantFiled: January 19, 2004Date of Patent: April 17, 2007Assignee: Industry-Academic Cooperation Foundation, Yonsei UniversityInventor: Man-Kil Jung
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Patent number: 7202271Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: GrantFiled: September 20, 2004Date of Patent: April 10, 2007Assignee: University of North CarolinaInventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais
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Patent number: 7166583Abstract: The present invention relates to 1,3-diaza-dibenzoazulene derivatives, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: May 20, 2003Date of Patent: January 23, 2007Assignee: Pliva-Istrazivacki Institut d.o.o.Inventors: Mladen Mercep, Milan Mesic, Renata Rupcic, Dijana Pesic
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Patent number: 7160875Abstract: The invention relates to malonamide derivatives of formula wherein each of the variables are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates and diastereomeric mixtures thereof. These compounds are ?-secretase inhibitors and may be used for the treatment of Alzheimer's disease.Type: GrantFiled: September 2, 2004Date of Patent: January 9, 2007Assignee: Hoffmann-La Rache Inc.Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Jens-Uwe Peters, Wolfgang Wostl
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Patent number: 7087765Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: March 9, 2004Date of Patent: August 8, 2006Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Patent number: 7067510Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), or —OSO2(C2–C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1–C4 alkyl), —OCOC6H5, —OCO(C1–C6 alkyl), —OSO2(C2–C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3; X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1–C4 alkyl; and Y is —O—, —S—, —NH—, —NMe-, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.Type: GrantFiled: July 11, 2003Date of Patent: June 27, 2006Assignee: Eli Lilly and CompanyInventor: Owen Brendan Wallace
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Patent number: 7022664Abstract: The invention relates to 1,2-substituted 2,3-dihydro-1H-5,9-dioxacyclohepta[f]inden-7-ones and 7-substituted benzo[b][1,4]dioxepin-3-ones and to the use of these compounds in fragrance compositions.Type: GrantFiled: April 28, 2003Date of Patent: April 4, 2006Assignee: Givaudan SAInventor: Philip Kraft
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Patent number: 7015338Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having “n” procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4?8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8?8), (8?6), and (6?6) dimers and doubly branched oligomers. Crystalline 8-bromo-tetra-O-benzyl-(?)-epicatechin is produced under certain conditions.Type: GrantFiled: April 15, 1999Date of Patent: March 21, 2006Assignee: Mars IncorporatedInventors: Leo J. Romancyzk, Jr., Amit Basak, Craig A. Townsend
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Patent number: 7008568Abstract: A photochromic naphthopyran displays good color distribution when the naphthopyran has a central nucleus of the formula: wherein F is a 5-member, 6-member, or 7-member heterocyclic ring group having only one heteroatom, the heteroatom selected from the group consisting of oxygen, sulfur, and nitrogen, the 2,3 or 3,2 positions of the heterocyclic ring fused to the g, h, or i side; R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.Type: GrantFiled: November 20, 2001Date of Patent: March 7, 2006Assignee: Vision-Ease Lens, Inc.Inventor: Xuzhi Qin
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Patent number: 7009061Abstract: The present invention provides a novel diterpene compounds with antineoplastic activities. The novel diterpene compounds of the present invention are represented by the general formula (I). R1 to R6 in the formula represent an aliphatic group, or a radical represented by the general formula RCO—, wherein R represents an aliphatic, an aromatic or a heteroaromatic group. The compounds of the present invention may be prepared by extracting roots of Euphorbia kansui L. with an organic solvent such as chloroform, ethyl acetate and butanol. These extracted compounds may be used as starting materials for the preparation of the compounds represented by the general formula (I). The compounds of the present invention have antineoplastic activities, and therefore, useful as antineoplastic agents.Type: GrantFiled: January 30, 2004Date of Patent: March 7, 2006Assignee: Nihon UniversityInventors: Susumu Kitanaka, Syohei Miyata, Liyan Wang, Naili Wang, Xinsheng Yao
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Patent number: 6933260Abstract: A compound of formula (I) wherein the bond marked by formula (II) indicates either the S or the R isomer at the 4?-position; and wherein R1 is C1-C12alkyl, C3-C8cycloalkyl; or C2-C12alkenyl; R2 is, for example, hydrogen, unsubstituted or mono- to penta-substituted C1-C12alkyl or unsubstituted or mono- to penta-substituted C2-C12alkenyl; R3 is, for example, hydrogen, C1-C12alkyl, mono- to penta-substituted C1-C12alkyl, unsubstituted or mono- to penta-substituted C3-C12cycloalkyl, or unsubstituted or mono- to penta-substituted C2-C12alkenyl; and wherein the substituents of the alkyl, alkenyl, alkynyl, alkylene, alkenylene and cycloalkyl radicals defined under R2 and R3 are selected, for example, from the group consisting of OH, halogen, halo-C1-C2alkyl, CN, NO2 and C2-C6alkynyl; and, where applicable, E/Z isomers, mixtures of E/Z isomers and/or tautomers, in each case in free form or in salt form; a process for the preparation of and the use of those compounds, their isomers and tautomers; starting materials foType: GrantFiled: December 20, 2002Date of Patent: August 23, 2005Assignee: Syngenta Crop Protection, Inc.Inventor: Jérôme Cassayre
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Patent number: 6887700Abstract: A process is provided for preparing an enantiopure 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivative, which includes bringing a mixture containing enantiomeric 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivatives and an enzyme with hydrolytic activity into contact in the presence of a nucleophile. Cleaving a dioxolanone/oxathiolanone ring of one enantiomer occurs by the enzyme with hydrolytic activity and, after the cleavage of one enantiomer has taken place, the uncleaved enantiomer of the 1,3-dioxolan-4-one or 1,3-oxathiolan-5-one derivative is isolated.Type: GrantFiled: January 30, 2002Date of Patent: May 3, 2005Assignee: Consortium für Elektrochemische Industrie GmbHInventors: Alfred Popp, Jürgen Stohrer, Hermann Petersen, Andrea Gilch, Jodoca Rockinger-Mechlem
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Patent number: 6864377Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having “n” procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4?8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8?8), (8?6), and (6?6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (?)-epicatechin is produced under certain conditions.Type: GrantFiled: August 6, 2002Date of Patent: March 8, 2005Assignee: Mars IncorporatedInventors: Leo J Romanczyk, Jr., Amit Basak, Craig A Townsend
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Patent number: 6858732Abstract: Benzodioxino-naphtho[1,2-b]pyran compounds having particularly advantageous photochromic properties, such as, high sensitivity/coloration, two distinct absorption bands in the 430-500 nm range and 520-620 nm range of the visible spectrum may be generally described as a naphthopyran having a central nucleus of the formula: wherein F is a 1,4-benzodioxine ring with its 2,3 positions fused to the i, j, or k faces; and R1 and R2 are the atoms or groups providing photochromic properties to the naphthopyran.Type: GrantFiled: March 1, 2002Date of Patent: February 22, 2005Assignee: Vision-Ease Lens, Inc.Inventors: Xuzhi Qin, J. Thomas Ippoliti
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Patent number: 6849746Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.Type: GrantFiled: January 31, 2003Date of Patent: February 1, 2005Assignee: Mars, Inc.Inventors: Leo J. Romanczyk, Jr., Alan P. Kozikowski, Werner Tueckmantel, Marc E. Lippman
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Patent number: 6790966Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.Type: GrantFiled: January 15, 2003Date of Patent: September 14, 2004Assignee: Mars IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Publication number: 20040171670Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: March 9, 2004Publication date: September 2, 2004Applicant: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Publication number: 20040127713Abstract: Compounds represented by formula (1), 1Type: ApplicationFiled: December 5, 2003Publication date: July 1, 2004Applicant: Nippon Suisan Kaisha, Ltd.Inventors: Shuji Jinno, Takaaki Okita, Naomi Ohtsuka, Shinya Yamashita, Junichiro Hata, Jiro Takeo
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Patent number: 6750244Abstract: Method and compositions for treating a patient having a neurological disease or disorder, such as stroke, head trauma, spinal cord injury, spinal cord ischemia, ischemia- or hypoxia-induced nerve cell damage, epilepsy, anxiety, neuropsychiatric or cognitive deficits due to ischemia or hypoxia such as those that frequently occur as a consequence of cardiac surgery under cardiopulmonary bypass, or neurodegenerative diseases such as Alzheimer's Disease, Huntington's Disease, Parkinson's Disease, or amyotrophic lateral sclerosis (ALS).Type: GrantFiled: April 2, 2001Date of Patent: June 15, 2004Assignee: NPS Pharmaceuticals, Inc.Inventors: Alan L. Mueller, Scott T. Moe
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Patent number: 6750356Abstract: The present invention provides a method for the preparation of arteether from artemisinin in one pot in just about 4 hours comprising reduction of artemisinin into dihydroartemisinin by less quantity of sodium borohydride in ethanol at room temperature in the presence of a novel polyhydroxy catalyst, acylation of dihydroartemisinin in the presence of an acid catalyst, extraction of arteether from an aqueous reaction mixture using 1% ethyl acetate in n-hexane followed by workup and purification of the impure arteether to yield 80-86% (w/w) pure alpha, beta arteether.Type: GrantFiled: December 2, 2002Date of Patent: June 15, 2004Assignee: Council of Scientific and Industrial ResearchInventors: Rajendra Singh Bhakuni, Amit Tewari, Tarun Singh, Suman P. S. Khanuja
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Patent number: 6723858Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.Type: GrantFiled: February 21, 2002Date of Patent: April 20, 2004Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Patent number: 6723731Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, Ar, X, Q, A, Y and Z are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: April 13, 2001Date of Patent: April 20, 2004Assignees: Novo Nordisk A/S, Dr. Reddy's Research FoundationInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6709642Abstract: The invention concerns derivatives of calixarene having the formula: in which: R1 represents various hydrocarbon groups, R2 and R3 represent an alkyl, cycloalkyl or aryl group or a group having the formula: O(CH2)n[O(CH2)p]q OR4, or form a heterocyclic group with the nitrogen atom, and, n equals 6, 7 or 8. These derivatives can be used for extracting strontium from aqueous solutions.Type: GrantFiled: February 12, 2002Date of Patent: March 23, 2004Assignee: Commissariat a l'Energie AtomiguieInventors: Jean-François Dozol, Rocco Ungaro, Alessandro Casnati
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Publication number: 20030220360Abstract: Compounds represented by formula (1), 1Type: ApplicationFiled: November 12, 2002Publication date: November 27, 2003Applicant: Nippon Suisan Kaisha, Ltd., a Japan corporationInventors: Shuji Jinno, Takaaki Okita, Naomi Ohtsuka, Shinya Yamashita, Junichiro Hata, Jiro Takeo
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Publication number: 20030176493Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.Type: ApplicationFiled: January 15, 2003Publication date: September 18, 2003Applicant: Mars IncorporatedInventors: Leo J. Romanczyk, John F. Hammerstone, Margaret M. Buck
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Publication number: 20030114691Abstract: Processes are disclosed for the production of linear and branched procyanidin oligomers having “n” procyanidin monomeric units where n is 2 to 18. The processes include coupling protected, activated monomers with an unprotected monomer to produce a partially protected (4→8) dimer. The dimer is optionally blocked, coupled with an activated protected monomer to produce a partially protected, optionally blocked trimer, and deprotected. The steps can be repeated to produce higher oligomers. Processes are also provided for producing (8→8), (8→6), and (6→6) dimers and doubly branched oligomers. Crystalline 8-bromo tetra-O-benzyl (−)-epicatechin is produced under certain conditions.Type: ApplicationFiled: August 6, 2002Publication date: June 19, 2003Applicant: Mars IncorporatedInventors: Leo J. Romanczyk, Amit Basak, Craig A. Townsend
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Patent number: 6562863Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.Type: GrantFiled: January 24, 2001Date of Patent: May 13, 2003Assignee: Mars IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Patent number: 6562864Abstract: Described herein are catechin multimers, and particularly substituted catechin multimers, and their use as carrier moieties for the delivery of nucleophilic and cationic bioactive therapeutic agents to target sites in vivo. For example, substituted catechin multimers of the present invention may be administered alone, for the treatment of stenotic vascular diseases and disorders, such as atherosclerosis (also known as arteriosclerosis) and coronary heart disease (also known as coronary artery disease and ischemic heart disease).Type: GrantFiled: May 3, 2002Date of Patent: May 13, 2003Inventor: Drake Larson
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Patent number: 6525086Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, A, X, T, Q, Z, U, Y, Ar, p and n are as defined in the specification. These compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).Type: GrantFiled: March 14, 2001Date of Patent: February 25, 2003Assignee: Novo Nordisk A/SInventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6512123Abstract: Compounds of formula I wherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC inhibitory activity for inhibiting cell proliferation. Also provided is a process of manufacturing these compounds.Type: GrantFiled: April 22, 2002Date of Patent: January 28, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Adelbert Grossmann, Wolfgang von der Saal, Tim Sattelkau, Ulrich Tibes
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Patent number: 6479539Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins-and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.Type: GrantFiled: April 22, 1997Date of Patent: November 12, 2002Assignee: Mars, IncorporatedInventors: Leo J. Romanczyk, Jr., John F. Hammerstone, Jr., Margaret M. Buck
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Publication number: 20020137951Abstract: The present invention relates to a process for the transformation of tricyclopentabenzene to 12-hydrox-16-oxatetracyclo [10.3. 1.01,5.Type: ApplicationFiled: March 20, 2001Publication date: September 26, 2002Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Ranganathan Subramania, Manjheri Muraleedharan Kannoth
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Publication number: 20020115654Abstract: The present invention relates to compounds of the general formula (I) 1Type: ApplicationFiled: October 25, 2001Publication date: August 22, 2002Inventors: Lone Jeppesen, Paul Stanley Bury, Per Sauerberg
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Patent number: 6437152Abstract: An enantiomerically enriched compound of formula 1, wherein Ar is phenyl optionally substituted with one or more groups selected from haloalkyl, alkyl and halide. This compound can be isolated in crystalline form, and used in the preparation of (+)-16-[3-trifluoromethyl)phenoxy]-17,18,19,20-tetranor PGF2&agr; isopropyl ester.Type: GrantFiled: July 3, 2001Date of Patent: August 20, 2002Assignee: Chirotech Technology, Inc.Inventors: Philip Mark Jackson, Ian Campbell Lennon
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Publication number: 20020035104Abstract: Provided are compounds of formula (I) 1Type: ApplicationFiled: August 16, 2001Publication date: March 21, 2002Applicant: GENENTECH, INC.Inventors: Dean R. Artis, David Y. Jackson, Thomas E. Rawson, Mark E. Reynolds, Daniel P. Sutherlin, Mark S. Stanley
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Publication number: 20020004523Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.Type: ApplicationFiled: January 24, 2001Publication date: January 10, 2002Applicant: Mars, IncorporatedInventors: Leo J. Romanczyk, John F. Hammerstone, Margaret M. Buck
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Patent number: 6316491Abstract: Radioicol derivatives represented by the following formula (I) having tyrosine kinase inhibition activity or pharmacologically acceptable salts thereof: wherein R1 and R2 are the same or different, and each represents hydrogen, alkanoyl, alkenoyl, tert-butyldiphenylsilyl or tert-butyldimethylsilyl; R3 represents Y—R5 (wherein Y represents substituted or unsubstituted alkylene; and R5 represents CONR6R7 (wherein R6 represents hydrogen, hydroxyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted higher alkyl, and the like; R7 represents hydroxyl, substituted lower alkyl, and the like), CO2R12 (wherein R12 represents substituted lower alkyl, substituted or unsubstituted higher alkyl, and the like), and the like) and the like; X represents halogen or is combined together with R4 to represent a single bond; and R4 is combined together with X to represent a single bond, or represents hydrogen, alkanoyl, and the like.Type: GrantFiled: June 24, 1998Date of Patent: November 13, 2001Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Yoji Ino, Nobuyoshi Amishiro, Mayumi Miyata, Chikara Murakata, Harumi Ogawa, Tadakazu Akiyama, Shiro Akinaga, Shiro Soga, Yukimasa Shiotsu