序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
61 JPS50134987A - JP3737875 1975-03-27 JPS50134987A 1975-10-25
62 JPS5040536A - JP7549374 1974-07-03 JPS5040536A 1975-04-14
63 JPS5037747A - JP7548974 1974-07-03 JPS5037747A 1975-04-08
64 JPS508095B1 - JP11788270 1970-12-25 JPS508095B1 1975-04-02
65 PROCESS FOR THE PREPARATION OF THIADIAZOLE DERIVATIVES PCT/IB2019/054672 2019-06-05 WO2019234651A1 2019-12-12 BELLANDI, Paolo; GUSMEROLI, Marilena; MORMILE, Silvia; ZANARDI, Giampaolo; MEREGHETTI, Pierangelo

A process is described for the preparation of thiadiazole derivatives and more specifically a new synthetic process of compounds having general formula (I) and intermediate compounds having general formula (XVI).

66 TRANSITION METAL COMPLEXES OF BIS[THIOHYDRAZIDE AMIDE] COMPOUNDS PCT/US2009/061480 2009-10-21 WO2010048284A1 2010-04-29 NAGAI, Masazumi; SHEN, Jianhua

The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I):, or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. In one embodiment, the compound is represented by Structural Formula (II):, or a prodrug, isomer, ester, salt, hydrate, solvate or polymorph thereof. The present invention also provides a pharmaceutical composition comprising the compound of the invention and method of use thereof.

67 THIOAMIDE COMPOUNDS, METHOD OF MAKING AND METHOD OF USING THEREOF PCT/US2009/061337 2009-10-20 WO2010048191A1 2010-04-29 LE HIR DE FALLOIS, Loïc, Patrick; LEE, Hyoung, Ik; TIMMONS, Philip, Reid

The present invention relates to novel thioamide derivatives of formula (I) and formula (Ia): wherein, R3, R4, R5, R6, R7, P, Q, T, V, W, X, Y, Z, a, m and n are as defined in the description, compositions thereof, processes for their preparation and their uses as pesticides.

68 COMPOUNDS FOR TREATING PROLIFERATIVE DISORDERS PCT/US2007018362 2007-08-20 WO2008024302A2 2008-02-28 SUN LIJUN; KOYA KEIZO; CHEN SHOUJUN; DEMKO ZACHARY; XIA ZHI-QIANG
Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
69 SITE AND RATE SELECTIVE PRODRUG FORMULATIONS OF D609 WITH ANTIOXIDANT AND ANTICANCER ACTIVITY PCT/US2004033255 2004-10-08 WO2005032492A3 2007-04-12 MEIER G PATRICK; BAI AIPING; ZHOU DAOHONG
Compounds that are heteroatom substituted alkyl derivatives of tricyclodecan-9-yl-xanthogenate, and pharmaceutical compositions of these compounds, are disclosed. Methods of treating a disease or disorder in a subject and methods of protecting normal tissues in a subject from toxicity associated ionizing radiation or chemotherapy using compositions comprising these novel compounds are also disclosed. The invention also concerns methods of treating a disease or disorder in a subject using compositions that include these novel compounds while concurrently or consecutively treating the subject with ionizing radiation or a chemotherapeutic agent.
70 SYNTHESIS OF LABELED OXALIC ACID DERIVATIVES PCT/US2004017751 2004-06-04 WO2005000228A3 2005-03-17 MARTINEZ RODOLFO A; ALVAREZ MARC A; UNKEFER CLIFFORD J
The present invention is directed to labeled compounds, specifically (F) where each C<*> is selected from the group consisting of a carbon-12, i.e., <12>C, or a carbon-13, i.e., <13>C< >and at least one C<*> is <13>C, R<1> is selected from the group of C1-C4 lower alkyls and aryl, and X is selected from the group of -NR<2>R<3 >where R<2> and R<3> are each independently selected from the group of C1-C4 lower alkyl, alkoxy and aryl, -SR<4> where R<4> is selected from the group of CI-C4 lower alkyl, alkoxy and aryl, and -OR<5> where R<5> is selected from the group of C1-C4 lower alkyl, alkoxy and aryl with the proviso that when R<1> is methyl then R<5> is other than methyl, when R<1> is ethyl then R<5> is other than ethyl, and when R<1> is benzyl then R<5> is other than benzyl.
71 3,4-DIHYDROXYBENZYL-SUBSTITUTED CARBONIC ACID DERIVATIVES AND THE USE THEREOF AS ANTIOXIDANTS PCT/EP0106568 2001-06-11 WO0198235A3 2002-05-23 LEY JAKOB PETER; JOHNCOCK WILLIAM; LANGNER ROLAND
The invention relates to 3,4-dihydroxybenzyl-substituted carbonic acid derivatives, to their production, and to their use as antioxidants or free-radical scavengers, especially in cosmetic and pharmaceutical preparations and in foodstuffs and stimulants, to protect cells and tissues from the harmful effects of radicals and reactive oxygen compounds that accelerate aging. The invention further relates to cosmetic and pharmaceutical preparations and to foodstuffs and stimulants that comprises the inventive 3,4-dihydroxybenzyl-substituted carbonic acid derivatives.
72 AMPHIPHILIC RAFT AGENT PCT/AU2016/050643 2016-07-20 WO2017035570A1 2017-03-09 FRANCIS, Craig L; GARDINER, James; MARTINEZ BOTELLA, Ivan; TSANAKTSIDIS, John

This invention relates to a RAFT agent formula (I).

73 SYNTHESIS OF ACYL-PANTETHEINE DERIVATIVES AND THE USE THEREOF IN THE SYNTHESIS OF ACYL-COENZYME A DERIVATIVES PCT/IB2011/053458 2011-08-03 WO2012017400A1 2012-02-09 VAN DIJK, Alberdina Aike; BADENHORST, Christoffel Petrus Stephanus

The present invention relates to a novel synthesis method for acyl-pantetheine derivatives. The present invention further relates to the use of said synthesized acyl-pantetheine derivatives as a starting material in the enzymatic synthesis of acyl-coenzyme A derivatives. According to a first aspect thereof, the present invention provides a method for the synthesis of acyl-pantetheine derivatives, the method including the steps of: a) providing a source of pantetheine; b) providing a source of acyl ester; and c) contacting the source of pantetheine with the source of acyl ester to form the corresponding acyl-pantetheine derivative, having the general formula (I), wherein R is an acyl group.The present invention also provides a method for the synthesis of acyl-coenzyme A derivatives as well as the use of a source of pantetheine and a source of acyl ester in the preparation steps of these two methods.

74 TRANSITION METAL COMPLEXES OF A BIS[THIOHYDRAZIDE AMIDE] COMPOUND PCT/US2009/061491 2009-10-21 WO2010048293A1 2010-04-29 NAGAI, Masazumi; SHEN, Jianhua

The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof.

75 NOVEL MODULATORS OF PROTEIN KINASE SIGNALING PCT/IL2009/000568 2009-06-07 WO2009147682A1 2009-12-10 REUVENI, Hadas; LEVITZKI, Alexander; SASSON, Revital; LUCASSEN, Andre C. B.

The present invention provides new tyrphostin derivatives acting as protein kinase (PK) and receptor kinase (RK) signaling modulators. The invention further provides methods of their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as chemotherapeutic agents for preventions and treatments of PK and RK related disorders such as metabolic, inflammatory, fibrotic, and cell proliferative disorders, in particular cancer.

76 METHOXYPOLYETHYLENE GLYCOL THIOESTER CHELATE AND USES THEREOF PCT/US2007003682 2007-02-14 WO2007095178A3 2008-04-17 SCHELLENBERG KARL A; LATTANZIO FRANK A; SHAEFER JAMES
The present invention is directed generally to protecting cells, tissues and organs against the damaging effects of ionizing or other damaging agents associated with radiation or chemotherapy, or degenerative diseases or processes of various organs that elicit the production of free radicals or oxidants such as peroxides, superoxide anions, hydroxyl radicals or nitric oxides, or heavy metal cations. More particularly, the present invention is concerned with methoxypolyethylene glycol thioester chelate methyl esters that are useful as protectors against tissue damage by penetrating the cell membrane to remove electrons from free radical oxidants and remove heavy metals that may react with peroxides to produce the reactive hydroxyl radical, or remove Ca++ that may be released from organelles. These chelate esters will also have utility in reducing intraocular pressure in glaucoma patients.
77 NOVEL ALKYL- AND ARYL-THIOTRIFLUOROACETATES AND PROCESS PCT/US2005/001012 2005-01-12 WO2005073185A1 2005-08-11 SHARMA, Padam N.; GUBLO, Edward J.; BOETTGER, Susan D.; RACHA, Saibaba; USHER, John

Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure [Formula (I)], wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate. In addition, a process for protecting a primary or secondary amino group or a primary or secondary hydroxyl group or an amino alcohol with a trifluoroacetyl protecting group is provided wherein a primary or secondary amine, amino acid, a primary or secondary alcohol or an amino alcohol is treated with a C3 to C19 alkyl- or aryl-thiotrifluoroacetate in basic aqueous solution.

78 3,4-DIHYDROXYBENZYL-SUBSTITUTED CARBONIC ACID DERIVATIVES AND THE USE THEREOF AS ANTIOXIDANTS PCT/EP2001/006568 2001-06-11 WO01098235A2 2001-12-27
The invention relates to 3,4-dihydroxybenzyl-substituted carbonic acid derivatives, to their production, and to their use as antioxidants or free-radical scavengers, especially in cosmetic and pharmaceutical preparations and in foodstuffs and stimulants, to protect cells and tissues from the harmful effects of radicals and reactive oxygen compounds that accelerate aging. The invention further relates to cosmetic and pharmaceutical preparations and to foodstuffs and stimulants that comprises the inventive 3,4-dihydroxybenzyl-substituted carbonic acid derivatives.
79 SYNTHESIS OF OLIGOKETIDES PCT/US0002397 2000-01-27 WO0044717A2 2000-08-03 ASHLEY GARY; CHAN-KAI ISAAC CHU-WAH; BURLINGAME MARK ALMA
Facile methods for preparing diketide and triketide thioesters are disclosed. The resulting thioesters may be used as intermediates in the synthesis of desired polyketides, and may contain functional groups which ultimately reside in side chains on the resulting polyketide and thus can be used further to manipulate the polyketide so as to form derivatives. The polyketides produced may also be tailored by glycosylation, hydroxylation and the like. New polyketides and their derivatives and tailored forms are thereby produced.
80 METHODS AND COMPOSITIONS TO PROTECT CROPS AGAINST PLANT-PARASITIC NEMATODES PCT/US1998/011795 1998-06-09 WO98056234A1 1998-12-17
A method for protecting a crop against plant-parasitic nematode attack by inducing local and systemic resistance of the crop comprising the application of a composition containing an effective amount of beta -amino butyric acid or derivatives thereof to the crop or its locus.
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