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1. 发明授权

US08822707B2 Nucleophile assisting leaving groups 有权
标题翻译：亲核试剂帮助离群
公开(公告)号：US08822707B2
公开(公告)日：2014-09-02
申请号：US11667414
申请日：2005-11-14
申请人： Salvatore Lepore
发明人： Salvatore Lepore
IPC分类号： C07C309/77 , C07C309/89 , C07D323/00 , C07H11/00
CPC分类号： C07H11/00 , C07C309/77 , C07C309/89 , C07C2603/74 , C07D323/00
摘要： Sulfonate leaving groups include a cation chelating moiety, e.g. a polyether or crown ether. The chelating moiety stabilizes the sulfonate leaving group by forming a complex with a cation of a cation-nucleophile combination. The stabilized leaving group is more easily displaced under many conditions than are standard arylsulfonate leaving groups such as the toxyl group. The chelating moiety also favors certain cations depending on the identity of the moiety thereby enhancing the reaction rate with nucleophilic salts containing the preferred cation. Use of the inventive leaving groups results in improved yields, decreased reaction times and improved product purity.
摘要翻译：磺酸盐离去基团包括阳离子螯合部分，例如聚醚或冠醚。螯合部分通过与阳离子 - 亲核试剂组合的阳离子形成络合物来稳定磺酸根离去基团。稳定的离去基团在许多条件下比标准芳基磺酸盐离去基团如甲苯磺酰基更容易置换。取决于部分的同一性，螯合部分也有利于某些阳离子，从而增强与含有优选阳离子的亲核盐的反应速率。使用本发明的离去基团导致产率提高，反应时间缩短，产物纯度提高。

2. 发明授权

US5001163A Organic polymeric material and ion-exchange membrane with pendant carbocyclic exchanging groups produced 失效
标题翻译：生产有机聚合物材料和具有侧链碳环交换基团的离子交换膜
公开(公告)号：US5001163A
公开(公告)日：1991-03-19
申请号：US317369
申请日：1989-03-01
申请人： Harold C. Fielding , Philip H. Gamlen , Ian M. Shirley
发明人： Harold C. Fielding , Philip H. Gamlen , Ian M. Shirley
IPC分类号： B01J47/12 , C07C309/25 , C07C309/58 , C07C309/89 , C08F14/18 , C08F16/14 , C08F16/30 , C08F214/18 , C08F214/26 , C08F216/14 , C08F230/02 , C08F299/02 , C08J5/22 , C25B13/08 , H01M8/02
CPC分类号： C08J5/225 , C07C309/25 , C07C309/58 , C07C309/89 , C08F16/30 , H01M8/0289 , C07C2101/14 , C08J2327/18 , Y02P70/56
摘要： An organic polymeric material, which is preferably perfluorinated and which comprises a polymeric chain and at least one group pendant from the chain, in which the group pendant from the chain comprises a saturated cyclic group and at least one ion-exchange group or group convertible thereto, and in which the ion-exchange group or group convertible thereto is linked to the polymeric chain through the cyclic group. Also an ion-exchange membrane produced from the polymeric material, an electrolytic cell containing the membrane, vinyl monomers from which the organic polymeric material may be produced and intermediates useful in production of the monomers.

3. 发明授权

US4212819A Process for the preparation of benzoyl halide and halosulfonylbenzoyl halide 失效
标题翻译：苯甲酰卤和卤磺酰苯甲酰卤的制备方法
公开(公告)号：US4212819A
公开(公告)日：1980-07-15
申请号：US923411
申请日：1978-07-10
申请人： F. Howard Day
发明人： F. Howard Day
IPC分类号： C07C51/58 , C07C303/06 , C07C309/89 , C07C63/10 , C07C143/38 , C07C143/40
CPC分类号： C07C303/06 , C07C303/04 , C07C51/58
摘要： A process for the preparation of benzoyl halide and meta-halosulfonyl benzoyl halide comprises adding to sulfuric acid and reacting therewith a benzotrihalide compound characterized by the formula: ##STR1## wherein X is bromine or chlorine and Y is individually selected from the group consisting of fluorine, chlorine, bromine, iodine, alkyl, preferably of one to six carbon atoms, halosubstituted alkyl, preferably trichloromethyl or tribromomethyl, aryl, preferably phenyl, and hydrogen, with the proviso that at least one Y substituent at a meta position is hydrogen.
摘要翻译：制备苯甲酰卤和间卤代磺酰基苯甲酰卤的方法包括加入硫酸并与其反应，其特征在于以下结构式的苯并三卤化物：其中X是溴或氯，Y分别选自氟，氯，溴，碘，优选1-6个碳原子的烷基，卤代烷基，优选三氯甲基或三溴甲基，芳基，优选苯基和氢，条件是间位上至少有一个Y取代基是氢。

4. 发明申请

US20180230092A1 NOVEL ANTIVIRAL AGENTS AGAINST HBV INFECTION 审中-公开
公开(公告)号：US20180230092A1
公开(公告)日：2018-08-16
申请号：US15933098
申请日：2018-03-22
申请人： DREXEL UNIVERSITY , BARUCH S. BLUMBERG INSTITUTE , ARBUTUS BIOPHARMA, INC.
发明人： XIAODONG XU , JU-TAO GUO , TONG XIAO , YANMING DU , TIMOTHY BLOCK , SIMON DAVID PETER BAUGH , HONG YE
IPC分类号： C07C311/16 , C07D319/16 , C07D309/04 , C07D305/08 , C07D295/32 , C07D295/30 , C07D295/26 , C07D277/52 , C07D277/46 , C07D263/58 , C07D263/50 , C07D263/48 , C07D261/14 , C07D239/26 , C07D231/42 , C07D231/40 , C07D217/24 , C07D215/42 , C07D215/38 , C07D213/76 , C07D213/75 , C07D213/40 , C07D211/96 , C07D205/04 , C07D203/26 , C07C317/14 , C07C311/48 , C07C311/20 , C07C311/19 , C07C311/18 , C07C311/17 , C07C309/89 , C07C233/66 , C07D319/18
CPC分类号： C07C311/16 , C07B2200/07 , C07C233/66 , C07C309/89 , C07C311/17 , C07C311/18 , C07C311/19 , C07C311/20 , C07C311/48 , C07C317/14 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07D203/26 , C07D205/04 , C07D211/96 , C07D213/40 , C07D213/75 , C07D213/76 , C07D215/38 , C07D215/42 , C07D217/24 , C07D231/40 , C07D231/42 , C07D239/26 , C07D261/14 , C07D263/48 , C07D263/50 , C07D263/58 , C07D277/46 , C07D277/52 , C07D295/26 , C07D295/30 , C07D295/32 , C07D305/08 , C07D309/04 , C07D319/16 , C07D319/18
摘要： The present invention is directed toward novel compounds and novel methods of use of said compounds of the formula (I), useful as nucleocapsid assembly inhibitors for the treatment of viruses, especially but not exclusively, including pregenomic RNA encapsidation inhibitors of HBV for the treatment of Hepatitis B virus (HBV) infection and related conditions. including hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, wherein A, R1, R2, R3, R4, R5, R6, R7, and R8 are defined herein.

5. 发明授权

US5811571A Process for preparing aromatic or heteroaromatic sulfonyl halides 失效
标题翻译：制备芳族或杂芳族磺酰卤的方法
公开(公告)号：US5811571A
公开(公告)日：1998-09-22
申请号：US765246
申请日：1996-12-13
申请人： Hitoshi Karino , Hiroshi Goda , Jun-ichi Sakamoto , Katsuhiko Yoshida , Hideaki Nishiguchi
发明人： Hitoshi Karino , Hiroshi Goda , Jun-ichi Sakamoto , Katsuhiko Yoshida , Hideaki Nishiguchi
IPC分类号： C07C303/18 , C07C303/02 , C07C303/16 , C07C309/86 , C07C309/89 , C07C315/04 , C07C317/14 , C07C319/20 , C07C323/66 , C07D213/71 , C07D241/18 , C07D251/22 , C07D263/46 , C07D275/02 , C07D275/03 , C07D277/36 , C07C255/10
CPC分类号： C07D275/03 , C07C303/02 , C07C303/16 , C07C315/04 , C07C319/20 , C07D213/71 , C07D241/18 , C07D251/22 , C07D263/46
摘要： The present invention is directed to a process for preparing an aromatic or heteroaromatic sulfonyl halide represented by the formula (3), the process comprising halogenating an aromatic or heteroaromatic methyl sulfide represented by the formula (1) or an aromatic or heteroaromatic methyl sulfoxide represented by the formula (2) with a halogenating agent in the presence of water Ar.paren open-st.SCH.sub.3-m X.sub.m).sub.n (1) Ar.paren open-st.SOCH.sub.3-m X.sub.m).sub.n (2) Ar.paren open-st.SO.sub.2 Y).sub.n (3) wherein Ar is an aromatic ring or a heteroaromatic ring which is unsubstituted or which has an optional substituent or substituents, X and Y are halogen atoms, m is an integer of 0 to 3 and n is 1 or 2. According to the present invention, aromatic or heteroaromatic sulfonyl halides can be produced industrially cheaply and easily.
摘要翻译： PCT No.PCT / JP95 / 02675 Sec。 371日期1996年12月13日第 102（e）日期1996年12月13日PCT 1995年12月25日PCT PCT。公开号WO96 / 33167 日期：1996年10月24日本发明涉及一种由式（3）表示的芳族或杂芳族磺酰卤的制备方法，该方法包括将由式（1）表示的芳族或杂芳族甲基硫醚或芳族或（2）Ar + 545 SO 2 Y）n（3）其中，式（2）表示的杂芳香族甲基亚砜与卤化剂在水存在下反应，式中，Ar + 545 SCH3-mXm）n（1）Ar + 545 SOCH3-mXm） Ar是未取代的或具有任选的取代基的芳香环或杂芳环，X和Y是卤素原子，m是0-3的整数，n是1或2.根据本发明，芳香族或杂芳族磺酰卤可以在工业上廉价且容易地制备。

6. 发明授权

US5136043A Process for the preparation of aromatic sulfonyl chlorides 失效
标题翻译：芳香族磺酰氯的制备方法
公开(公告)号：US5136043A
公开(公告)日：1992-08-04
申请号：US746476
申请日：1991-08-16
申请人： Michael Meier , Wolfgang Tronich
发明人： Michael Meier , Wolfgang Tronich
IPC分类号： C07C303/08 , C07C309/86 , C07C309/88 , C07C309/89 , C07D263/58
CPC分类号： C07D263/58 , C07C303/08 , C07C303/22
摘要： A process for the preparation of aromatic sulfonyl chlorides of the formula I ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 are identical or different and are hydrogen, fluorine, chlorine, bromine or iodine atoms, alkyl(C.sub.1 -C.sub.4), acetamido, nitro or carboxyl groups, or R.sub.1 and R.sub.2 together form an aromatic or heteroaromatic ring having 5 or 6 ring members, which can be substituted by fluorine, chlorine, bromine or iodine atoms, alkyl(C.sub.1 -C.sub.4), acetamido, nitro or carboxyl groups, by reaction of aromatic compounds of the formula II ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 have the abovementioned meanings, with chlorosulfonic acid in excess or with chlorosulfonic acid or oleum and thionyl chloride, by reacting in the presence of sulfamic acid as a catalyst.
摘要翻译：其中R1，R2和R3相同或不同，为氢，氟，氯，溴或碘原子的芳基磺酰氯的方法，其中R1，R2和R3为氢，氟，氯，溴或碘原子，烷基（C1-C4），乙酰氨基，硝基或羧基，或R 1和R 2一起形成具有5或6个环成员的芳族或杂芳族环，其可被氟，氯，溴或碘原子取代，烷基（C1-C4），乙酰氨基，硝基或羧基，通过在氨基磺酸作为催化剂的存在下反应，通过在氨基磺酸作为催化剂的存在下反应，其中R1，R2和R3具有上述含义的芳族化合物与氯磺酸过量或与氯磺酸或发烟硫酸和亚硫酰氯反应。

7. 发明授权

US3897476A Sulfamylbenzoic acid derivatives 失效
标题翻译：磺酰基苯甲酸衍生物
公开(公告)号：US3897476A
公开(公告)日：1975-07-29
申请号：US34982673
申请日：1973-04-10
申请人： LEO PHARM PROD LTD
发明人： FEIT PETER WERNER , NIELSEN OLE BENT TVAERMOSE
IPC分类号： C07C67/00 , C07C205/61 , C07C301/00 , C07C303/38 , C07C309/89 , C07C311/16 , C07C311/29 , C07C313/00 , C07C319/20 , C07C323/66 , C07C323/67 , C07D213/30 , C07D213/32 , C07D275/04 , C07D275/06 , C07D277/24 , C07D277/26 , C07D307/38 , C07D307/40 , C07D333/16 , C07D333/18 , C07D333/24 , C07D333/34 , C07C143/78
CPC分类号： C07D213/30 , C07C205/61 , C07C309/89 , C07C311/29 , C07C323/66 , C07D213/32 , C07D275/04 , C07D275/06 , C07D277/26 , C07D307/38 , C07D333/16 , Y10S514/869
摘要： Compounds of the general formulae

IN WHICH R1 represents a straight or branched, optionally substituted alkyl, alkenyl or alkynyl radical; R2 stands for an optionally substituted phenyl radical; Y stands for oxygen, sulphur or a methylene radical; X stands for O or H2; their salts and esters and methods for their preparation. The compounds of the invention possess an outstanding diuretic and saluretic activity with a very low excretion of potassium ions and a low toxicity.
摘要翻译：通式为I的化合物，其中R 1表示直链或支链，任选取代的烷基，烯基或炔基; R2代表任选取代的苯基; Y代表氧，硫或亚甲基; X代表O或H2; 其盐和酯及其制备方法。

8. 发明授权

US3666771A M-(amino-s-triazolyl)benzene-sulfonamides and their production 失效
标题翻译： M-（氨基-S-三唑基）苯并噻吩及其生产
公开(公告)号：US3666771A
公开(公告)日：1972-05-30
申请号：US3666771D
申请日：1970-07-06
申请人： PARKE DAVIS & CO
发明人： HOEFLE MILTON L , HOLMES ANN
IPC分类号： C07C309/89 , C07C311/21 , C07D249/14 , C07D55/06
CPC分类号： C07C311/21 , C07C309/89 , C07D249/14
摘要： Amino-s-triazolybenzenesulfonamides having the formula WHERE EACH OF R1 and R2 is hydrogen or methyl, and X is hydrogen, methyl, methoxy, or halogen, and salts thereof are produced by cyclizing a sulfamoylbenzoic acid 2-amidinohydrazide. The compounds of the invention are useful as pharmacological agents having antiviral activity.
摘要翻译：具有下式的R 1和R 2的氨基-s-三唑聚苯磺酰胺是氢或甲基，X是氢，甲基，甲氧基或卤素，其盐是通过使氨磺酰基苯甲酸2-脒基 - 酰肼环化来制备的。本发明的化合物可用作具有抗病毒活性的药理学试剂。

9. 发明授权

US2667503A Method of preparing ortho sulfonyl chloride benzoic acid esters 失效
标题翻译：邻磺酰氯苯甲酸酯的制备方法
公开(公告)号：US2667503A
公开(公告)日：1954-01-26
申请号：US23900651
申请日：1951-07-27
申请人： MAUMEE DEV COMPANY
发明人： SENN OLIVER F
IPC分类号： C07C303/02 , C07C309/89
CPC分类号： C07C303/16 , C07C309/89

10. 发明授权

US11084784B2 ROR-gamma modulators and uses thereof 有权
公开(公告)号：US11084784B2
公开(公告)日：2021-08-10
申请号：US15128932
申请日：2015-03-25
申请人： PIRAMAL ENTERPRISES LIMITED
发明人： Rajiv Sharma , Bichismita Sahu , Sunil Vasantrao Mali , Deepak Singh , Pramod Bhaskar Kumar , Mahesh Dawange , Hitesh Mistry
IPC分类号： C07C317/32 , C07D311/22 , C07D335/06 , C07D265/36 , C07D207/27 , C07D295/26 , C07C233/29 , C07C237/22 , A61K31/18 , A61K31/351 , C07C217/88 , C07C317/24 , C07C311/08 , C07C255/46 , C07C233/54 , C07C217/48 , C07C211/45 , C07C215/70 , C07C255/50 , A61K31/277 , C07C309/89 , C07C225/22 , C07C229/42 , C07C317/44 , A61K31/165 , C07C323/09 , A61K31/5375 , C07C311/37 , C07F5/02 , A61K31/402 , C07D317/72 , C07C217/76 , C07C205/36 , A61K31/382 , C07F7/18 , C07C237/52 , C07C311/21 , C07C381/10 , C07D211/14 , C07D213/30 , C07D231/12 , C07D233/58 , C07D257/04 , C07D295/088 , C07D295/135 , C07D295/192 , C07D305/08
摘要： The present invention relates to a compound of formula I, or an isotopic form, stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate, a polymorph, a prodrug, N-oxide or S-oxide thereof; and processes for their preparation. The invention further relates to pharmaceutical compositions containing the compounds and their use in the treatment of diseases or disorders mediated by RORγ.

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