| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 81 | INDOLINE DERIVATIVES AS PROGESTERONE ANTAGONISTS | PCT/US2000/011847 | 2000-05-01 | WO00066556A1 | 2000-11-09 | |
| This invention comprises compounds of formula (I), which are antagonists of the progesterone receptor, their preparation and utility. | ||||||
| 82 | SYNTHESIS OF POLYSUBSTITUTED AROMATIC COMPOUNDS AND AROMATISATION PROCESS FOR USE THEREIN | PCT/GB1999/001009 | 1999-03-31 | WO99050259A2 | 1999-10-07 | |
| In a retro-Diels-Alder reaction the starting cycloadduct is protected by -OH or -OP groups to form a desired benzene derivative or heteroaromatic compound, with the concomitant elimination of a dioxolene species. The protecting groups P are preferably comprised in a cyclic thiocarbonate or cis-isopropyldienedioxy group. The cycloadduct may be prepared by Diels-Alder cycloaddition of an acetylenic dienophile to a cyclohexadiene-cis-diol, and the cyclohexadiene may be formed by biological oxidation of an arene. The process allows desired aromatised products to be produced in uniformly high yields and the reaction is generally initiated at lower temperatures than known methods of synthesis which evolve ethylene. The by-products are usually non-volatile and may spontaneously polymerise. | ||||||
| 83 | METHOD FOR SUSTAINABLE CHEMICAL FIXATION OF CO2 | PCT/IN2020/050708 | 2020-08-12 | WO2021028946A1 | 2021-02-18 | H. JADHAV, Arvind; NAGARAJA, Bhari Mallanna; PRASAD, Divya; N. PATIL, Komal; T. BHANUSHALI, Jayesh |
A method for sustainable fixation of CO2, is disclosed herein. A sustainable chemical fixation of CO2 into epoxide to form value added product such as cyclic carbonates using bimetallic spinel oxide hollow microspheres as an efficient and recyclable catalyst under solvent free and mild reaction conditions. |
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| 84 | COMPOUNDS AND THERAPEUTIC USES THEREOF | PCT/US2018/064584 | 2018-12-07 | WO2019113523A1 | 2019-06-13 | BAJJI, Ashok |
The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, diseases associated with over production of IL12/IL23, lysosomal storage disorders, filovirus infections, ischemia, and other complications associated with these diseases and disorders. |
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| 85 | A NOVEL ROUTE FOR PREPARATION OF L,3:2,4-BIS-(3,4- D IM ETH YLB ENZYLIDENE)SO RB ITO L | PCT/IN2015/000393 | 2015-10-16 | WO2016071921A2 | 2016-05-12 | SHROFF Ravi Ashwin; PATIL, Mahesh Laxmikant; VAISHNAV Ujval Hemantkumar; PILLAI Vivekanand Bhaskar |
A new route for preparation of 3:2,4-bis-(3,4- dimethylbenzylidene) sorbitol [DMDBS] has been disclosed which is comprising: bromination of o-xylene to obtain a mixture of 4-bromo- o-xylene as a major product and 3-bromo-o-xylene; conversion of bromo-o-xylenes into corresponding dimethylbenzaldehyde by Grignard reaction; and reaction of 3,4-dimethylbenzaldehyde with sorbitol in presence of catalyst and solvent to obtain DMDBS. The invented route is cost-effective and it obviates the need to separate 3,4-dimethylbenzaldehyde from its 2,3-isomer. |
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| 86 | METHODS OF TREATING SKIN CONDITIONS USING CYCLOLIGNAN COMPOUNDS | PCT/US2014/037523 | 2014-05-09 | WO2014183055A1 | 2014-11-13 | FEIN, Howard; BERLIN, Joshua, M. |
The present invention includes compositions and methods for the treatment of skin conditions by administration of a cyclolignan such as picropodophyllin and/or a derivative, metabolite, analog, prodrug, pharmaceutically acceptable salt, or hydrate thereof. |
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| 87 | VANILLIN ACETALS AND SENSORY STIMULANT COMPOSITION CONTAINING THE SAME | PCT/JP2006/313799 | 2006-07-05 | WO2007004740A1 | 2007-01-11 | ISHIDA, Kenya; AIDA, Takashi |
The invention relates to a sensory stimulant composition containing one or more of vanillin acetals represented by the general formula (1), and a flavor and fragrance composition, a beverage or food product, a fragrance or cosmetic product, a daily utensil product, an oral composition, or a pharmaceutical product containing the sensory stimulant composition with a warming sensation agent or cooling sensation substance, if necessary. Vanillin acetals represented by the general formula (1) show an excellent pungent and/or warming sensation effect and a cooling sensation-emphasizing effect. |
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| 88 | VERFAHREN ZUR HERSTELLUNG VON GLYCERINCARBONATMETHACRYLAT | PCT/EP2004/009423 | 2004-08-24 | WO2005058862A2 | 2005-06-30 | SCHMITT, Bardo; CASPARI, Maik |
Die Erfindung betrifft ein Verfahren zur Herstellung von Glycerincarbonatmethacrylat in Gegenwart von Metall-Chelat-Katalysatoren vom Typ Metallion-1,3-Diketonat. |
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| 89 | METHOD OF AFFINITY PURIFYING PROTEINS USING MODIFIED BIS-ARSENICAL FLUORESCEIN | PCT/US0102214 | 2001-01-22 | WO0153325A3 | 2002-03-07 | VALE RONALD D; THORN KURT; COOKE ROGER; MATUSKA MARIJA; NABER NARIMAN |
| The present invention features methods for purifying polypeptides of interest using a modified Fluorescein arsenical helix binder (F1AsH) compound immobilized on a solid support. An exemplary F1AsH target sequence motif is also presented. Examples of modification of the F1AsH compound which allow immobilization to a solid support are also provided. The present invention also provides DNA constructs for producing a dual affinity tagged polypeptide and methods for purification thereof. | ||||||
| 90 | METHOD FOR THE PRODUCTION OF IMIDAZO-(1,2-C)(2,3)-BENZODIAZEPINES AND INTERMEDIATES IN THE PRODUCTION THEREOF | PCT/EP2001/008661 | 2001-07-26 | WO02012247A1 | 2002-02-14 | |
| The invention relates to a method for the preparation of compound of formula (1). The invention further relates to the previously unknown compounds of formulas (5 and 6) as intermediates in the production of benzodiazepines of formula (1). | ||||||
| 91 | CARBOCYCLIC SIDE CHAIN CONTAINING, N-SUBSTITUTED METALLOPROTEASE INHIBITORS | PCT/US2001/008782 | 2001-03-20 | WO01070720A2 | 2001-09-27 | |
| Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I): where R<1>, R<2>, R<3>, n, A, E, E', L, L', G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions. | ||||||
| 92 | NEW 2,3-BENZODIAZEPINE DERIVATIVES | PCT/HU0000074 | 2000-07-04 | WO0104122A3 | 2001-05-10 | GREFF ZOLTAN; SZABO GEZA; BARKOCZY JOZSEF; RATKAI ZOLTAN; BLASKO GABOR; SIMIG GYULA; GIGLER GABOR; MARTONNE MARKO BERNADETT; LEVAY GYOERGY; TIHANYI KAROLY; EGYED ANDRAS; SIMO ANNAMARIA |
| The invention relates to new 2,3-benzodiazepine derivatives of general Formula (I), (wherein R<1> stands for methyl, formyl, carboxy, cyano, -CH=NOH, -CH=NNHCONH2 or -NR<5>R<6>, wherein R<5> and R<6> independently from each other represent hydrogen or lower alkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R<2> is nitro or amino; R<3> stands for hydrogen, lower alkanoyl or CO-NR<7>R<8>, wherein R<7> and R<8> independently from each other stand for hydrogen, lower alkoxy, lower alkyl or lower cycloalkyl or together with the nitrogen atom, they are attached to, form a 5- or 6-membered, saturated or unsaturated heterocyclic ring optionally containing one or more further nitrogen, sulfur and/or oxygen atom(s); R<4> is hydrogen or lower alkyl; the dotted lines have the following meaning: if R<3> and R<4> are not present, the bond between positions C<8> and C<9> is a single bond and the bond between positions C<8> and N<7> is a double bond; if R<3> and R<4> are present, the bonds between positions C<8> and C<9> and between position C<8> and N<7> are single bonds; and if R<3> is present and R<4> is missing, the bond between positions C<8> and C<9> is a double bond and the bond between positions C<8> and N<7> is a single bond) and salts thereof. The invention compounds have neuroprotective effect. | ||||||
| 93 | HEMISYNTHETIC METHOD AND NEW COMPOUNDS | PCT/GB2000/001852 | 2000-05-15 | WO00069862A2 | 2000-11-23 | |
| Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically: R<1> is an amidomethylene group or an acyloxymethylene group; R<5> and R<8> are independently chosen from -H, -OH or -OCOCH2OH, or R<5> and R<8> are both keto and the ring A is a p-benzoquinone ring; R<14a> and R<14b> are both -H ozone is -H and the other is -OH, -OCH3 or -OCH2CH3, or R<14a> and R<14b> together form a keto group; and R<15> and R<18> are independently chosen from -H or -OH, or R<5> and R<8> are both keto and the ring A is a p-benzoquinone ring. In modified starting materials, the 21-cyano group can be replaced by other groups introduced using nucleophilic reagents. | ||||||
| 94 | SUBSTITUTED BENZOPYRAN ANALOGS FOR THE TREATMENT OF INFLAMMATION | PCT/US9921460 | 1999-10-15 | WO0023433A8 | 2000-07-27 | CARTER JEFFREY S; DEVADAS BALEKUDRU; TALLEY JOHN J; BROWN DAVID L; GRANETO MATTHEW J; ROGIER DONALD J JR; NAGARAJAN SRINIVASAN R; HANAU CATHLEEN E; HARTMANN SUSAN J; LUDWIG CINDY L; METZ SUZANNE; KORTE DONALD E; BERTENSHAW STEPHEN R; OBUKOWICZ MARK G |
| A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I') wherein X, A<1>, A<2>, A<3>, A<4>, R, R'', R<1> and R<2> are as described in the specification. | ||||||
| 95 | (+)-NORCISAPRIDE USEFUL FOR 5-HT3 AND 5-HT4 MEDIATED DISORDERS | PCT/EP1998/004193 | 1998-07-07 | WO99002496A1 | 1999-01-21 | |
| The present invention concerns (+)-norcisapride of formula (I) and compounds (V), and its pharmaceutically acceptable acid additions salts, a process for preparing said compound, and its use for the manufacture of a medicament for treating gastro-intestinal disorders while avoiding central nervous system effects. Also provided are method of treating gastro-intestinal disorders. Compounds of formula (V) wherein the piperidine ring has the absolute configuration (3S, 4R) and PG is methyloxycarbonyl, ethyloxycarbonyl, tert-butyloxycarbonyl or phenylmethyl. | ||||||
| 96 | ANTIMICROBIAL COMPOSITIONS CONTAINING PROPYLENE CARBONATE AND/OR ETHYLENE CARBONATE AS THE CARRIER SOLVENT | PCT/US1992007480 | 1992-09-03 | WO1993005032A1 | 1993-03-18 | GREAT LAKES CHEMICAL CORPORATION; McCOY, William, F.; SUMMERFIELD, James, M. |
| Antimicrobial compositions of bromonitrostyrene or bromonitroethenylfuran are formed in a carrier solvent system comprising propylene carbonate, ethylene carbonate or mixtures thereof. The propylene carbonate system may additionally include tetrahydrofurfuryl alcohol. | ||||||
| 97 | PROCESS FOR PREPARING SOLKETAL AMINE VIA DIRECT AMINATION | PCT/CN2018/103226 | 2018-08-30 | WO2020042079A1 | 2020-03-05 | KUSEMA, Bright; STREIFF, Stéphane; YAN, Zhen; MALHEIRO, Arthur |
Disclosed a process for preparing a solketal amine via direct amination. It is possible to obtain solketal amines by very simple procedure with desired characteristics such as simplicity, inexpensiveness, high yield and conversion, as well as low environmental impact. |
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| 98 | 1-O-咖啡酰奎宁酸、其衍生物、制备方法及其用途 | PCT/CN2018/090091 | 2018-06-06 | WO2019128113A1 | 2019-07-04 | 廖杰远; 孙志国; 邹德超; 陈先红; 季鸣; 谈敦潮; 陈晓光 |
本发明提供了式(II)所示的1-O-咖啡酰奎宁酸衍生物，以及1-O-咖啡酰奎宁酸、式(II)所示的1-O-咖啡酰奎宁酸衍生物及其盐的应用。1-O-咖啡酰奎宁酸、如式(II)所示的1-O-咖啡酰奎宁酸衍生物及其盐具有抑制白介素17，尤其是白介素17F的分泌的作用，并且能够预防和治疗肿瘤。实验结果表明，1-O-咖啡酰奎宁酸浓度为0.5μM/L时对白介素17F的抑制率接近70％；1-O-咖啡酰奎宁酸在20mg/kg的剂量下对黑色素瘤、胰腺癌、结直肠癌、肺癌等肿瘤有较好的抑制作用，均超过50％，而其衍生物对黑色素瘤、胰腺癌、结直肠癌、肺癌等肿瘤也具有较好的抑制作用。 |
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| 99 | A NOVEL ROUTE FOR PREPARATION OF L,3:2,4-BIS-(3,4- D IM ETH YLB ENZYLIDENE)SO RB ITO L | PCT/IN2015000393 | 2015-10-16 | WO2016071921A3 | 2016-07-28 | SHROFF RAVI ASHWIN; PATIL MAHESH LAXMIKANT; VAISHNAV UJVAL HEMANTKUMAR; PILLAI VIVEKANAND BHASKAR |
| A new route for preparation of 3:2,4-bis-(3,4- dimethylbenzylidene) sorbitol [DMDBS] has been disclosed which is comprising: bromination of o-xylene to obtain a mixture of 4-bromo- o-xylene as a major product and 3-bromo-o-xylene; conversion of bromo-o-xylenes into corresponding dimethylbenzaldehyde by Grignard reaction; and reaction of 3,4-dimethylbenzaldehyde with sorbitol in presence of catalyst and solvent to obtain DMDBS. The invented route is cost-effective and it obviates the need to separate 3,4-dimethylbenzaldehyde from its 2,3-isomer. | ||||||
| 100 | STEREOCHEMICALLY DEFINED POLYPROPIONATES AND METHODS FOR MAKING AND USING THE SAME | PCT/US2015/043535 | 2015-08-04 | WO2016022519A1 | 2016-02-11 | FANG, Francis G.; CHOI, Hyeong-Wook; CAMPAGNA, Silvio; MATHIEU, Steven |
The present invention relates to stereochemically defined polypropionates and methods for preparing and using the same. The stereochemically defined polypropionates may be useful in the synthesis of natural products and/or natural product-like libraries. |
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