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1. 发明申请

WO2010055304A2 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2010055304A2
公开(公告)日：2010-05-20
申请号：PCT/GB2009/002662
申请日：2009-11-13
申请人： SAREUM LIMITED , READER, John, Charles
发明人： READER, John, Charles
IPC分类号： A61K31/4164 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K9/00 , A61P37/06
CPC分类号： A61K31/4164 , A61K9/0019 , A61K9/2018 , A61K9/4858 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/5377
摘要： The invention provides a compound for use in the treatment of an autoimmune disease such as multiple sclerosis, the compound being a compound of the formula (1) or a salt, solvate, N-oxide or tautomer thereof; wherein a is 0 or 1; b is 0 or 1 : provided that the sum of a and b is 0 or 1; T is O or NH; Ar 1 is an optionally substituted monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group; and Ar 2 is an optionally substituted monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group; provided that, when b is 0, a carbon atom of Ar 2 is attached directly to the 5-membered ring containing the moiety T.
摘要翻译：本发明提供了一种用于治疗自身免疫性疾病如多发性硬化的化合物，该化合物为式（1）化合物或其盐，溶剂合物，N-氧化物或其互变异构体; 其中a为0或1; b为0或1，条件是a和b之和为0或1; T是O或NH; Ar 1是任选取代的单环或双环5-至10-元芳基或杂芳基; 并且Ar 2是任选取代的单环或双环5-至10-元芳基或杂芳基; 条件是当b为0时，Ar 2的碳原子直接连接到含有部分T的5元环上。

2. 发明申请

WO2020074461A1 TYK2 KINASE INHIBITORS 审中-公开
公开(公告)号：WO2020074461A1
公开(公告)日：2020-04-16
申请号：PCT/EP2019/077118
申请日：2019-10-07
申请人： SAREUM LIMITED
发明人： READER, John Charles
IPC分类号： C07D263/48 , A61P29/00 , A61P37/00 , A61K31/541
摘要： The invention provides compounds of the formula (1): (1) or a salt or tautomer thereof; wherein R 1 is hydrogen or fluorine, pharmaceutical compositions containing the compounds and medical uses of the compounds (for example, in the treatment of inflammatory or immune disorders).

3. 发明申请

WO2013117522A1 AURORA AND FLT3 KINASES MODULATORS 审中-公开
标题翻译： AURORA和FLT3 KINASES调制器
公开(公告)号：WO2013117522A1
公开(公告)日：2013-08-15
申请号：PCT/EP2013/052182
申请日：2013-02-04
申请人： SAREUM LIMITED
发明人： READER, John Charles
IPC分类号： C07D413/14 , A61K31/496 , A61P35/00
CPC分类号： C07D413/14 , A61K31/496 , A61K45/06
摘要： The invention provides a compound having the formula (1) useful as modulator of the activity of Aurora kinases and FLT3 kinases: and salts thereof; wherein: R 1 is hydrogen or C 1-2 alkyl; and R 2 , R 3 and R 4 are the same or different and each is selected from hydrogen, C 1-2 alkyl, fluorine, chlorine, C 1-2 alkoxy and trifluoromethyl, provided that no more than two of R 2 , R 3 and R 4 are other than hydrogen. Also provided are pharmaceutical compositions containing the compounds and their use in medicine, and in particular in the treatment of cancer.
摘要翻译：本发明提供具有式（1）的化合物，其可用作Aurora激酶和FLT3激酶活性的调节剂：及其盐; 其中：R 1是氢或C 1-2烷基; R 2，R 3和R 4相同或不同，各自选自氢，C 1-2烷基，氟，氯，C 1-2烷氧基和三氟甲基，条件是R 2，R 3和R 4不超过氢。还提供含有这些化合物及其在药物中，特别是癌症治疗中的用途的药物组合物。

4. 发明申请

WO2021204762A1 CRYSTALLINE FORMS OF A TYK2 INHIBITOR 审中-公开
公开(公告)号：WO2021204762A1
公开(公告)日：2021-10-14
申请号：PCT/EP2021/058864
申请日：2021-04-06
申请人： SAREUM LIMITED
发明人： READER, John Charles , MARSHALL, Jamie Conor , MYKYTIUK, John , NORTHEN, Julian Scott
IPC分类号： A61P29/00 , A61K31/541 , A61P37/00 , C07D263/48
摘要： The invention provides crystalline forms of a compound having the formula (I) along with methods of making the crystalline forms and pharmaceutical formulations comprising the crystalline forms.

5. 发明申请

WO2018073438A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2018073438A1
公开(公告)日：2018-04-26
申请号：PCT/EP2017/076909
申请日：2017-10-20
申请人： SAREUM LIMITED
发明人： READER, John Charles
IPC分类号： A61K31/421 , A61P35/02
摘要： The invention provides a compound for use in the treatment of T-Cell Acute Lymphoblastic Leukaemia (T-ALL), the compound having the formula (1): or being a pharmaceutically acceptable salt thereof; wherein: n is 0, 1 or 2; Ar 1 is selected from an optionally subtituted phenyl, pyridyl, thienyl and furanyl; Q 1 is selected from C(=O), S(=O) and SO 2; A is absent or is NR 2 ; R 1 is selected from: -hydrogen; -an optionally substituted C 1-6 non-aromatic hydrocarbon group; and -optionally substituted 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are 1 nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings; R 2 is selected from hydrogen and C 1-4 alkyl; or NR 1 R 2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen- containing heterocyclic ring optionally containing a second heteroatom ring member selected from nitrogen and oxygen.
摘要翻译：本发明提供了用于治疗T细胞急性淋巴细胞白血病（T-ALL）的化合物，该化合物具有式（1）：或其可药用盐; 其中：n是0,1或2; Ar 1选自任选取代的苯基，吡啶基，噻吩基和呋喃基; Q 1选自C（= O），S（= O）和SO 2; A不存在或为NR 2; R 1选自： - 氢; - 任选取代的C 1-6非芳族烃基; 和任选取代的含有一个或两个选自O，N和S的杂原子环成员的3-至7-元非芳族碳环和杂环以及七至九个环成员的桥连二环杂环，其中一个或两个是1 氮原子，碳环和杂环以及桥连双环杂环; R 2选自氢和C 1-4烷基; 或NR 1 R 2 2形成任选取代的任选取代的4至7元非芳族含氮杂环，其任选地包含选自氮和氧的第二杂原子环成员。

6. 发明申请

WO2015032423A1 PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：药物化合物
公开(公告)号：WO2015032423A1
公开(公告)日：2015-03-12
申请号：PCT/EP2013/068198
申请日：2013-09-03
申请人： SAREUM LIMITED
发明人： READER, John Charles
IPC分类号： C07D263/48 , A61K31/421 , A61P37/00 , A61P37/06 , A61P37/08
CPC分类号： C07D263/48
摘要： The invention provides a compound which is an amide of the formula (2): or a salt or stereoisomer thereof; wherein: R 7 is selected from chlorine and fluorine; R 3 , R 4 , R 5 and R 6 are each independently selected from hydrogen, fluorine and chlorine; n is 0, 1 or 2; Q 1 is selected from C(=O), S(=O) and SO 2 ; A is absent or is NR 2 ; R 1 is selected from: - hydrogen; - an optionally substituted C 1-6 non-aromatic hydrocarbon group; and - 3- to 7-membered non-aromatic carbocyclic and heterocyclic rings containing one or two heteroatom ring members selected from O, N and S, and bridged bicyclic heterocyclic rings of seven to nine ring members of which one or two are nitrogen atoms, the carbocyclic and heterocyclic rings and bridged bicyclic heterocyclic rings being optionally substituted; R 2 is selected from hydrogen and C 1-4 alkyl; or NR 1 R 2 forms an optionally substituted 4- to 7-membered non-aromatic nitrogen- containing heterocyclic ring optionally containing a second heteroatom ring member selected from nitrogen and oxygen; with the provisos that: (i) no more than two of R 3 to R 6 are other than hydrogen; and (ii) when R 7 and R 6 are both fluorine, then one of R 3 to R 5 is chlorine or fluorine and/or R 1 -A-Q 1 is selected from ethylsulfonyl and isopropylsulfonyl. Also provided are pharmaceutical compositions containing the compounds and their therapeutic uses.
摘要翻译：本发明提供了一种化合物，它是式（2）的酰胺或其盐或立体异构体; 其中：R 7选自氯和氟; R3，R4，R5和R6各自独立地选自氢，氟和氯; n为0,1或2; Q1选自C（= O），S（= O）和SO2; A不存在或NR2; R1选自： - 氢; - 任选取代的C 1-6非芳族烃基; 和含有一个或两个选自O，N和S的杂原子环成员的3-7元非芳族碳环和杂环，以及七至九个环成员的桥连双环杂环，其中一个或两个是氮原子，碳环和杂环和桥连的双环杂环任选被取代; R2选自氢和C 1-4烷基; 或NR1R2形成任选含有选自氮和氧的第二杂原子环成员的任选取代的4-至7-元非芳族含氮杂环; 条件是：（i）R3至R6中不超过两个不是氢; 和（ii）当R 7和R 6均为氟时，R 3至R 5中的一个为氯或氟，和/或R 1 -A-Q 1选自乙基磺酰基和异丙基磺酰基。还提供含有该化合物及其治疗用途的药物组合物。

7. 发明申请

WO2008139161A1 OXAZOLE TYROSINE KINASE INHIBITORS 审中-公开
标题翻译：奥昔洛霉激酶激酶抑制剂
公开(公告)号：WO2008139161A1
公开(公告)日：2008-11-20
申请号：PCT/GB2008/001612
申请日：2008-05-09
申请人： SAREUM LIMITED , READER, John, Charles , ELLARD, John, Mark , BOFFEY, Helen , TAYLOR, Susanne , CARR, Andrew, David , CHERRY, Michael , WILSON, Michelle , OWOARE, Richard, Boakye
发明人： READER, John, Charles , ELLARD, John, Mark , BOFFEY, Helen , TAYLOR, Susanne , CARR, Andrew, David , CHERRY, Michael , WILSON, Michelle , OWOARE, Richard, Boakye
IPC分类号： C07D263/34 , C07D413/04 , C07D413/10 , C07D413/12
CPC分类号： C07D413/14 , C07D233/90 , C07D263/34 , C07D263/48 , C07D401/04 , C07D403/04 , C07D409/04 , C07D413/04 , C07D413/10 , C07D413/12 , C07D451/02 , C07D451/04 , C07D453/02 , C07D471/04
摘要： The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1 : provided that the sum of a and b is 0 or 1; T is O or NH Ar 1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R 1 ; Ar 2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R 2 ; and R 1 and R 2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
摘要翻译：本发明提供了一种化合物，它是式（1）的酰胺或其盐，溶剂合物，N-氧化物或其互变异构体; 其中：a为0或1; b为0或1，条件是a和b之和为0或1; T是O或NH Ar 1是含有至多4个选自O，N和S的杂原子的单环或双环5至10元芳基或杂芳基，并且任选地被一个或多个取代基R 1; Ar 2是含有至多4个选自O，N和S的杂原子并且任选被一个或多个取代基R 2取代的单环或双环5-至10-元芳基或杂芳基 ; R 1和R 2如权利要求中所定义。化合物是激酶抑制剂，特别是FLT3，FLT4和Aurora激酶。

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