| 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 | VERFAHREN ZUR HERSTELLUNG VON 4-CHLORBENZOLSULFONSÄURE UND 4,4'-DICHLORDIPHENYLSULFON | PCT/EP2011/053010 | 2011-03-01 | WO2011107465A1 | 2011-09-09 | DECK, Patrick; SCHELLING, Heiner; GARLICHS, Florian |
Die Erfindung betrifft ein Verfahren zur Herstellung von 4-Chlorbenzolsulfonsäure aus 2-Chlorbenzolsulfonsäure und/oder 3-Chlorbenzolsulfonsäure umfassend die Umsetzung von 2-Chlorbenzolsulfonsäure und/oder 3-Chlorbenzolsulfonsäure zu 4-Chlorbenzolsulfonsäure in Gegenwart von Schwefelsäure bei einer Temperatur von 100 bis 300°C. Darüber hinaus betrifft die vorliegende Erfindung ein Verfahren zur Herstellung von 4,4'-Dichlordiphenylsulfon umfassend das genannte Verfahren zur Herstellung von 4-Chlorbenzolsulfonsäure. |
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| 62 | Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy | PCT/EP2010/051903 | 2010-02-16 | WO2010092180A1 | 2010-08-19 | AMBERG, Wilhelm; OCHSE, Michael; LANGE, Udo; KLING, Andreas; BEHL, Berthold; HORNBERGER, Wilfried; MEZLER, Mario; HUTCHINS, Charles |
The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GIyT1 inhibitors. |
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| 63 | TREATMENT OF DRUG-RESISTANT PROLIFERATIVE DISORDERS | PCT/US2006000059 | 2006-01-04 | WO2006074149A3 | 2007-11-15 | REDDY M V RAMANA; REDDY E PREMKUMAR; COSENZA STEPHEN C; BAKER STACEY J |
| a,ß-Unsaturated sulfones, sulfoxides and sulfonamides according to Formula I: wherein Ar1, Ar2, X, n, * and R are as defined herein are useful for the treatment of proliferative disorders which are resistant to treatment by ATP-competitive kinase inhibitors. | ||||||
| 64 | 11????-HSD1 INHIBITORS | PCT/EP2005011933 | 2005-11-08 | WO2006048330A8 | 2006-10-05 | COULTER THOMAS STEPHEN; STEVEN TAYLOR; FRYATT TARA; AICHER BABETTE; SCHNEIDER MARTIN |
| The invention relates to compounds of formula (I) wherein A, Y, Z1,Z2,R1 to R3 and X1 to X4 have the meaning as cited in the description and the claims. For example A is 4'-fluorobiphen-4-yl; Y is -S(O)2NH-; R1, R2 are H; X1,X2,X4 are CH; X3is C-F; Z' is =0; and Z2-R3 is N(CH2CH3)2. Said compounds are useful as 11ß-HSD1 inhibitors. The invention also relates to the preparation of such compounds as well as the production and use as medicament. | ||||||
| 65 | SYNTHESIS OF KETOSULFONE ESTERS | PCT/US0200995 | 2002-01-15 | WO02069909A3 | 2003-02-27 | CHEN CHENG YI; TAN LUSHI; CHEN WEIRONG; TILLYER RICHARD; DAGNEAU PHILIPPE; O'SHEA PAUL; XU FENG |
| This invention encompasses a process for making a compound of Formula A AThese compounds are intermediates useful in the preparation of certain non-steroidal anti-inflammatory agents. | ||||||
| 66 | (Z)-STYRYLBENZYLSULFONES AND PHARMACEUTICAL USES THEREOF | PCT/US0205817 | 2002-02-26 | WO02067913A8 | 2002-11-14 | REDDY E PREMKUMAR; REDDY M V RAMANA |
| Substituted (Z)-styrylbenzyl sulfones of the formulae (I, II, III, IV), pharmaceutically acceptable salts thereof, and compositions thereof are provided as cell antiproliferative agents, including, for example, anticancer agents. | ||||||
| 67 | SULFOXIDES OR SULFONES GRAFTED ONTO POLYMERS | PCT/EP2002/003381 | 2002-03-26 | WO2002081432A3 | 2002-10-17 | MEIER, Hans-Rudolf; KNOBLOCH, Gerrit; ROTA-GRAZIOSI, Pierre; EVANS, Samuel; DUBS, Paul; GERSTER, Michèle |
Polymers grafted with a compount of formula I, formula (I) wherein the general symbols are as defined in claim 1, have outstanding stability against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation. |
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| 68 | SULFOXIDES OR SULFONES GRAFTED ONTO POLYMERS | PCT/EP2002/003381 | 2002-03-26 | WO2002081432A2 | 2002-10-17 | MEIER, Hans-Rudolf; KNOBLOCH, Gerrit; ROTA-GRAZIOSI, Pierre; EVANS, Samuel; DUBS, Paul; GERSTER, Michèle |
Polymers grafted with a compount of formula I, formula (I) wherein the general symbols are as defined in claim 1, have outstanding stability against oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation. |
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| 69 | PURIFICATION OF 2-NITRO-4-METHYLSULPHONYLBENZOIC ACID | PCT/GB0201433 | 2002-03-25 | WO02076934A2 | 2002-10-03 | JAVDANI KAMBIZ; RODRIGUEZ GILBERT; MUXWORTHY JAMES PETER |
| A method for removing impurities from 2-nitro-4-methylsulfonylbenzoic acid which comprises at least two of the following steps, in any order, (a) dissolving 2-nitro-4-methylsulfonylbenzoic acid in water at a pH of about 2 to 10, followed by filtration; (b) contacting an aqueous solution of 2-nitro-4- methylsulfonylbenzoic acid with activated carbon at a pH of about 2 to 10; (c) treating an aqueous solution of 2-nitro-4-methylsulfonylbenzoic acid with sufficient base to hydrolyze undesired nitro and dinitro substituted impurities; followed by maintaining the resulting aqueous solution comprising 2-nitro-4-methylsulfonylbenzoic acid at a temperature of up to about 95 DEG C, and adjusting the pH of said solution to about a pH which is sufficient to effect crystallization of 2-nitro-4-methylsulfonylbenzoic acid upon cooling. | ||||||
| 70 | SUBSTITUTED (E)-STYRYL BENZYLSULFONES FOR TREATING PROLIFERATIVE DISORDERS | PCT/US2001/031337 | 2001-10-05 | WO02028828A1 | 2002-04-11 | |
| (E)-Styryl benzylsulfones useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: R1 is selected from the group consisting of halogen, C1-C6 alkoxy, nitro, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); and R2 and R3 are independently selected from the group consisting of halogen, C1-C6 alkoxy, C1-C6 alkyl, nitro, cyano, hydroxy, phosphonato, amino, sulfamyl, carboxy, acetoxy, and dimethylamino (C2-C6 alkoxy); provided: R1 may not be halogen when R2 and R3 are both halogen; R2 may not be 2-halogen when R3 is 4-halogen; or a pharmaceutically acceptable salt thereof; or formula II: whrein: R4 is selected from the group consisting of C1-C6 alkoxy, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); R6 is selected from the group consisting of nitro, hydrogen, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2-C6 alkoxy); and R7 is selected from the group consisting of halogen, C1-C6 alkoxy, C1-C6 alkyl, nitro, cyano, hydroxy, phosphonato, amino, sulfamyl, carboxy, acetoxy, dimethylamino (C2-C6 alkoxy) and trifluoromethyl; provided R5 and R6 may not be hydrogen in the same compound; or a pharmaceutically acceptable salt thereof. | ||||||
| 71 | SULFONYL ARYL OR HETEROARYL HYDROXAMIC ACID COMPOUNDS | PCT/US2001/014706 | 2001-05-07 | WO01085680A2 | 2001-11-15 | |
| 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. A contemplated compound corresponds in structure to the formula (I) wherein W and the R groups are defined elsewhere. | ||||||
| 72 | STYRYL SULFONE ANTICANCER AGENTS | PCT/US1999/007406 | 1999-04-02 | WO00059494A1 | 2000-10-12 | |
| Styryl sulfone compounds of the invention selectively inhibit proliferation of tumor cells, and induce apoptosis of tumor cells, while sparing normal cells. The compounds, which are useful in the treatment of cancer, have the formula (II) wherein n is zero or one; R1 is selected from the group consisting of hydrogen, chlorine, fluorine and bromine; R2 is selected from the group consisting of hydrogen, chlorine, fluorine, bromine, methyl and methoxy; and R3 is selected from the group consisting of hydrogen, chlorine and fluorine; provided, R2 may not be methyl or methoxy when R1 and R3 are both hydrogen and n is zero or one; and R1, R2 and R3 may not all be hydrogen when n is one, or formula (III) wherein R1 is selected from the group consisting of hydrogen, chlorine, fluorine and bromine; or formula (IV) wherein R1 is selected from the group consisting of fluorine and bromine, and R2 is selected from the group consisting of 2-chlorophenyl, 4-chlorophenyl, 4-fluorophenyl and 2-nitrophenyl. | ||||||
| 73 | CROSSLINKABLE BI-SULPHONYL DERIVATIVES AND THEIR USES FOR PREPARING ION-EXCHANGING MEMBRANES | PCT/CA1999/000083 | 1999-01-29 | WO99038842A1 | 1999-08-05 | |
| The invention concerns novel ion-exchanging membranes, the method for preparing them and their uses. The membranes are made up of a polymer obtained from a monomer or a bifunctional mixture of monomers of general formula [T-SO2-Y-SO2T']<-> M-<+>. Moreover said polymers are useful in electrochemical cells, in a chlorine-sodium electrolysis process, as separator in an electrochemical preparation of organic and inorganic compounds, as separator between an aqueous phase and an organic phase, or as catalyst for Diels-Alder additions, Friedel-Craft reactions, aldol condensations, cationic polymerisation, and acetal formation. | ||||||
| 74 | NOVEL P-AMINOPHENOL DERIVATIVES AND THE USE THEREOF | PCT/EP1998/007961 | 1998-12-08 | WO99031054A2 | 1999-06-24 | |
| Compounds of general formula (I), wherein A, B,C and D represent, independently from each other, an -OH- or -NHR- group, wherein R stands for a hydrogen atom or a C1-4 alkyl radical, with the proviso that A, B, C or D respectively stands for a hydroxy group, X stands for oxygen, sulphur, a sulfoxy or sulfoxyl group, R<1> and R<2> represent, independently from each other, hydrogen, fluorine, chlorine, a C1-4 alkyl or hydroxyalkyl group or a C2-4-dihydroxy-alkyl group, preferably a C2-dihydroxy alkyl group, and the physically acceptable salts of these compounds are highly suitable for use as developer components in oxidation coloring agents. | ||||||
| 75 | COMPOSITIONS AND METHODS FOR TREATING EYE DISORDERS | PCT/US2018/056429 | 2018-10-18 | WO2019079541A1 | 2019-04-25 | BESIRLI, Cagri Giray; WUBBEN, Thomas |
Provided herein are compositions and methods for treating eye disorders. In particular, provided herein are neuroprotective compositions and methods for treating vision loss and related disorders. |
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| 76 | DICHLORODIPHENYL SULFONE PASTILLES | PCT/EP2018/057778 | 2018-03-27 | WO2018188942A1 | 2018-10-18 | DOSI, Mahendra K.; HUSEIN, Ziad; MYSONA, Ronald |
Described herein are pastilles comprising a dicholorodiphenyl sulfone ("DCDPS"), corresponding formation methods and methods of synthesizing poly(aryl ether sulfone)s incorporating the DCDPS pastilles. It was surprisingly discovered that the use of pastilles comprising DCDPS as monomer source significantly increased the charge rate of the monomer into polymerization reactors during industrial scale poly(aryl ether sulfone) ("PAES") synthesis. The DCDPS pastilles can be formed by specifically adapted deposition approaches to achieve selected pastilles sizes with a narrow size distribution and, furthermore, can be desirably used in large scale PAES polymer synthesis to significantly improve polymer throughput. |
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| 77 | NONAQUEOUS ELECTROLYTE COMPOSITIONS COMPRISING FLUORINATED SULFONES | PCT/US2016/035734 | 2016-06-03 | WO2017209762A1 | 2017-12-07 | BURKHARDT, Stephen E.; KOURTAKIS, Kostantinos; ROELOFS, Mark Gerrit |
Disclosed herein are electrolyte compositions comprising a fluorinated solvent, a fluorinated sulfone, at least one component selected from a borate salt, and/or an oxalate salt, and/or a fluorinated cyclic carbonate, and at least one electrolyte salt. The fluorinated solvent may be a fluorinated acyclic carboxylic acid ester, a fluorinated acyclic carbonate, a fluorinated acyclic ether, or combinations thereof. The electrolyte compositions are useful in electrochemical cells, such as lithium ion batteries. |
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| 78 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC SYNDROME AND DIABETES | PCT/IB2013061384 | 2013-12-28 | WO2014106804A3 | 2017-04-13 | KANDULA MAHESH |
| The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing metabolic syndrome and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, neuropathic pain, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance. | ||||||
| 79 | PROCESS FOR THE ENANTIOMERIC RESOLUTION OF APREMILAST INTERMEDIATES | PCT/IN2016/050119 | 2016-04-22 | WO2016174685A1 | 2016-11-03 | DANDALA, Ramesh; JAYACHANDRA, Sureshbabu; KAUSHIK, Vipin Kumar; ACHANTA, Nageshwara Rao; DORASALA, Sivaprasad |
A process for the resolution of racemic 2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine using novel chiral salts is disclosed. An L-phenylalanine p-toluene-sulfonamide salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine and a di-p-toluoyl-L-tartaric acid salt of (S)-2-(3-ethoxy-4-methoxyphenyl)-1-(methylsulphonyl)-eth-2-ylamine are also provided. |
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| 80 | 4- { [ ( PYRIDIN- 3 - YL -METHYL) AMINOCARBONYL] AMINO} BENZENE - SULFONE DERIVATIVES AS NAMPT INHIBITORS FOR THERAPY OF DISEASES SUCH AS CANCER | PCT/US2011050320 | 2011-09-02 | WO2012031196A9 | 2013-06-13 | BAIR KENNETH W; BAUMEISTER TIMM R; BUCKMELTER ALEXANDRE J; CLODFELTER KARL H; HAN BINGSONG; LIN JIAN; REYNOLDS DOMINIC J; SMITH CHASE C; WANG ZHONGGUO; ZHENG XIAOZHANG; YUEN PO-WAI |
| The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An embodiment of the invention is the provision of a compound of Formula IIIA. | ||||||
