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31. 发明授权

US4855424A Phenothiazine derivatives 失效
标题翻译：吩噻嗪衍生物
公开(公告)号：US4855424A
公开(公告)日：1989-08-08
申请号：US79315
申请日：1987-07-30
申请人： Paul O. Hong , Raymond C. De Wald
发明人： Paul O. Hong , Raymond C. De Wald
IPC分类号： C07D279/20 , C08F2/00
CPC分类号： C07D279/20 , C08F2/004 , C08F2/005
摘要： A composition having the formula ##STR1## wherein n has an average value of one to about five, is disclosed for use in reducing or eliminating the formation of reactor scale during the polymerization of vinyl chloride and comonomers. The composition is prepared by reacting phenothiazine with formaldehyde in the presence of a liquid diluent that is a solvent for the phenothiazine, but a non-solvent for the dimer of phenothiazine and formaldehyde. The process of the invention is preferably conducted in the presence of a strong acid catalyst. The formaldehyde is preferably added slowly to the reaction mixture over the course of the reaction. The product can be filtered and dried.
摘要翻译：公开了具有式“IMAGE”的组合物，其中n具有1至约5的平均值，用于在氯乙烯和共聚单体的聚合期间减少或消除反应器垢的形成。该组合物是通过吩噻嗪与甲醛在作为吩噻嗪的溶剂的液体稀释剂存在下制备的，但是吩噻嗪和甲醛的二聚体的非溶剂。本发明的方法优选在强酸催化剂的存在下进行。在反应过程中，甲醛优选缓慢加入到反应混合物中。产品可以过滤和干燥。

32. 发明授权

US4710570A Azine redox dyes and leuco azine dyes 失效
标题翻译： Azine氧化还原染料和无色吖嗪染料
公开(公告)号：US4710570A
公开(公告)日：1987-12-01
申请号：US781913
申请日：1985-09-30
申请人： Tran V. Thien
发明人： Tran V. Thien
IPC分类号： B41M5/136 , B41M5/323 , C07D241/46 , C07D265/36 , C07D279/20 , C07D413/04 , C07D417/12 , C07D513/04 , C09B17/00 , C09B17/02 , C09B19/00 , C09B21/00 , G03C1/498 , C07D265/38
CPC分类号： G03C1/49854 , B41M5/136 , B41M5/323 , C07D241/46 , C07D265/36 , C07D279/20 , C07D413/04 , C07D417/12 , C07D513/04 , C09B17/02 , C09B19/00 , C09B21/00
摘要： Azine redox dyes and their corresponding dyes of the formula: ##STR1## in which: X is O, S, NR.sup.2,Z completes a fused aromatic of heterocyclic ring system,n is 0 or 1 to allow one R.sup.1 ring substituent,Q represents CR.sup.4 R.sup.5 in which at least one of R.sup.4 and R.sup.5 is an electronegative group or R.sup.4 and R.sup.5 may complete a ring, orwhen X is S Q may represent NR.sup.3 in which R.sup.3 is an aromatic or heterocyclic group.The leuco dyes are useful as dye generators in pressure sensitive, thermographic or photothermographic imaging systems.
摘要翻译： Azine氧化还原染料及其相应的具有下式的染料：其中：X为O，S，NR 2，Z，完成杂环系统的稠合芳族化合物，n为0或1，以允许一个R 1 Q表示CR4R5，其中R4和R5中的至少一个是电负性基团，或者R4和R5可以完成环，或者当X是SQ时可以表示NR 3，其中R 3是芳族或杂环基。无色染料可用作压敏，热成像或光热成像系统中的染料发生器。

33. 发明授权

US4393206A Process for the production of 2,3-Dihydro-4H-1,4-benzothiazines 失效
标题翻译： 2,3-二氢-4H-1,4-苯并噻嗪的制备方法
公开(公告)号：US4393206A
公开(公告)日：1983-07-12
申请号：US359221
申请日：1982-03-18
申请人： Paul Uhrhan , Edmund Krauthausen
发明人： Paul Uhrhan , Edmund Krauthausen
IPC分类号： C08K5/00 , C07D279/16 , C07D279/20 , C08K5/36 , C08K5/372 , C08L7/00 , C08L21/00
CPC分类号： C07D279/20 , C07D279/16 , C08K5/3725
摘要： Process for the preparation of 2,3-Dihydro-4H-1,4-benzothiazines by cyclisation of suitable 2-(2-Hydroxyalkyl)-thioanilines under elimination of water in the presence of phosphorous acid.
摘要翻译：通过在亚磷酸存在下消除水而使合适的2-（2-羟烷基） - 硫代苯胺环化制备2,3-二氢-4H-1,4-苯并噻嗪的方法。

34. 发明授权

US4302582A Process for the preparation of a condensation product from phenothiazine and p-nitrosophenol 失效
标题翻译：从吩噻嗪和对亚硝基苯酚制备缩合产物的方法
公开(公告)号：US4302582A
公开(公告)日：1981-11-24
申请号：US117127
申请日：1980-01-31
申请人： Gert Nagl , Joachim Ribka , Ulrich Gotsmann , Heinz Dickmanns
发明人： Gert Nagl , Joachim Ribka , Ulrich Gotsmann , Heinz Dickmanns
IPC分类号： C07D279/20 , C07D279/34 , C09B49/10 , C07D513/00
CPC分类号： C07D279/34 , C07D279/20 , C09B49/10
摘要： An improved process for preparation of a condensed product of phenothiazine and p-nitrosophenol which contains more than 60% by weight of indophenol S-oxide of the formula ##STR1## by condensing phenothiazine with p-nitrosophenol in sulphuric acid wherein the improvement comprises the phenothiazine being in 60 to 90% strength sulphuric acid at the time of addition of the p-nitrosophenol.
摘要翻译：一种通过将吩噻嗪与对亚硝基苯酚在硫酸中缩合而制备吩噻嗪和对亚硝基苯酚的缩合产物的改进方法，其中含有超过60％（重量）的下式的靛酚S-氧化物，其中改进包括吩噻嗪在加入对亚硝基苯酚时，硫酸浓度为60〜90％。

35. 发明授权

US3644462A Preparation of aromatic isocyanates by catalytic carbonylation of nitro compounds 失效
标题翻译：通过硝基化合物的催化羰化制备芳族异氰酸酯
公开(公告)号：US3644462A
公开(公告)日：1972-02-22
申请号：US3644462D
申请日：1969-03-12
申请人： OLIN MATHIESON
发明人： SMITH ERIC , KOBER EHRENFRIED H
IPC分类号： C07D279/20 , B01J31/00 , B01J31/26 , B01J31/28 , C07B61/00 , C07C67/00 , C07C241/00 , C07C263/14 , C07C265/00 , C07C119/04 , C07F15/00
CPC分类号： B01J31/1805 , B01J31/1825 , B01J31/28 , B01J31/34 , B01J31/36 , B01J2531/82 , B01J2531/822 , B01J2531/824 , C07C263/14 , C07C265/14 , C07C265/12
摘要： THE PROCESS FOR PREPARING AN ORGAINC ISOCYANATE BY REACTING AN ORGANIC NITRO COMPOUND WITH CARBON MONOXIDE IN THE PRESENCE OF A CATALYST SYSTEM COMPRISING A HALIDE OF A NOBLE METAL AND AN AMINE COMPOSITION. USEFUL AMINE COMPOSITION INCLUDE COMPOUNDS OF THE FORMULA:

RR''R"N

WHEREIN R, R'' AND R" ARE EACH SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, CYCLOALKYL, ARALKYL, AND

R"''-BENZENE

AND WHEREIN NOT MORE THAN TWO OF THE R, R'' AND R" SUBSTITUENTS ARE HYDROGEN. PREFERRED AMINES INCLUDE TRI-NBUTYL AMINE, ANILINE, ANILINE-2-SULFONIC ACID, O-PHENYLENE DIAMINE, ANTHRANILIC ACID, N-PHENYL ANTHRANILIC ACID, ANTHRANILAMIDE, O-AMINOPHENOL, O-AMINOBENZENE THIOL, BENZYL AMINE, DIPHENYL AMINE, AND TRIPHENYL AMINE. THE NOBLE METAL HALIDE IS PREFERABLY A HALIDE OF PALLADIUM, RODIUM, IRIDIUM, RHENIUM, PATINUM, AND MIXTURES THEREOF. THE CATALST SYSTEM MAY ALSO INCLUDE MOLYBDENUM TRIOXIDE OR ANOTHER METAL OXIDE.

36. 发明授权

US2483838A Diisobutyl substituted heterocyclic compounds 失效
标题翻译：二异丁基取代杂环化合物
公开(公告)号：US2483838A
公开(公告)日：1949-10-04
申请号：US56471144
申请日：1944-11-22
申请人： NIEDERL JOSEPH B
发明人： NIEDERL JOSEPH B
IPC分类号： C07D215/26 , C07D241/46 , C07D263/56 , C07D265/38 , C07D279/20
CPC分类号： C07D263/56 , C07D215/26 , C07D241/46 , C07D265/38 , C07D279/20

37. 发明授权

US1766403A Weener schtjlemann 失效
公开(公告)号：US1766403A
公开(公告)日：1930-06-24
申请号：US1766403D
IPC分类号： C07D219/08 , C07D219/10 , C07D265/38 , C07D279/20 , C07D311/82 , C09B11/24
CPC分类号： C09B11/24 , C07D219/08 , C07D219/10 , C07D265/38 , C07D279/20 , C07D311/82

38. 发明授权

US12064439B2 Phenothiazine diaminium salts and their use 有权
公开(公告)号：US12064439B2
公开(公告)日：2024-08-20
申请号：US17499498
申请日：2021-10-12
申请人： WisTa Laboratories Ltd.
发明人： Colin Marshall , Scott Clunas , John Mervyn David Storey , James Peter Sinclair , Thomas Craven Baddeley , Ahtsham Ishaq , Michael Simpson , Craig Williamson , Barry Alan Wood , Claude Michel Wischik , Charles Robert Harrington , Janet Elizabeth Rickard , David Horsley , Yin Sze Loh , Karrar Ahmad Khan , Christopher Paul Larch
IPC分类号： A61K31/5415 , A61K9/00 , A61K9/20 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/18 , A61P33/02 , A61P33/06 , A61P35/00 , C07D279/20 , A61K9/28 , A61L2/00 , C07C303/32 , C07C309/04 , C07C309/05 , C07C309/30 , C07C309/35
CPC分类号： A61K31/5415 , A61K9/0053 , A61K9/2095 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/18 , A61P33/02 , A61P33/06 , A61P35/00 , C07D279/20 , A61K9/2893 , A61L2/0052 , C07C303/32 , C07C309/04 , C07C309/05 , C07C309/30 , C07C309/35 , Y02A50/30
摘要： Disclosed are compounds of general formula (I):

and pharmaceutically acceptable salts thereof, formulations, methods and uses in, for example, the treatment of disease.

39. 发明公开

US20240115580A1 METHODS OF SYNTHESIS AND/OR PURIFICATION OF DIAMINOPHENOTHIAZINIUM COMPOUNDS 审中-公开
公开(公告)号：US20240115580A1
公开(公告)日：2024-04-11
申请号：US18533515
申请日：2023-12-08
申请人： WisTa Laboratories Ltd.
发明人： Claude Michel Wischik , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： A61K31/5415 , C07D279/18 , C07D279/20
CPC分类号： A61K31/5415 , C07D279/18 , C07D279/20 , Y02A50/30
摘要： Disclosed are methods of synthesis and/or purification of certain 3,7-diamino-phenothiazin-5-ium compounds (“diaminophenothiazinium compounds”) including Methylthioninium Chloride (MTC) (Methylene Blue), and the resulting high purity characterized by a purity greater than 98%, and very low levels of heavy metals and organic impurities Azure A, B, C and MVB. Also disclosed are methods of treatment of a tauopathy or methemoglobinemia in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of the high-purity diaminophenothiazinium compound.

40. 发明授权

US11951110B2 3, 7-diamino-10H-phenothiazine salts and their use 有权
公开(公告)号：US11951110B2
公开(公告)日：2024-04-09
申请号：US17591306
申请日：2022-02-02
申请人： WisTa Laboratories Ltd.
发明人： Claude Michel Wischik , Janet Elizabeth Rickard , Charles Robert Harrington , David Horsley , John Mervyn David Storey , Colin Marshall , James Peter Sinclair , Thomas Craven Baddeley
IPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00
CPC分类号： A61K31/5415 , C07D279/20 , C07D279/22 , C09B21/00 , Y02A50/30
摘要： Described are methods of preparing reduced 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of formula:

wherein: R1 and R9 are independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of HX1 and HX2 is independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These methods are particularly useful for producing stable reduced forms, and with high purity. The stability and purity are especially relevant for pharmaceutical compositions for the treatment of disease. The compounds are useful for treatment of e.g. tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs.

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