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1. 发明授权

US09872874B2 Dosage regimen for sapacitabine and seliciclib 有权
公开(公告)号：US09872874B2
公开(公告)日：2018-01-23
申请号：US14401357
申请日：2013-05-14
申请人： Cyclacel Limited
发明人： Judy H. Chiao , David Blake , Daniella Zheleva , Susan Davis , Simon Green , Geoffrey Shapiro
IPC分类号： A61K31/7068 , A61K31/52 , A61K9/00
CPC分类号： A61K31/7068 , A61K9/0053 , A61K31/52 , A61P35/00 , A61P35/02 , A61K2300/00
摘要： A first aspect of the invention relates to a method of treating a proliferative disorder in a subject, said method comprising administering to the subject a therapeutically effective amount of (i) sapacitabine, or a metabolite thereof; and (ii) seliciclib; in accordance with a dosing regimen comprising at least one first treatment cycle and at least one second treatment cycle, wherein said first treatment cycle comprises: (a) administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 3 to 5 consecutive days for 2 weeks, starting on day d, where d is the first day of treatment with sapacitabine, or the metabolite thereof, in said first treatment cycle; and (b) optionally administering a therapeutically effective amount of seliciclib for 3 to 5 consecutive days for 2 weeks, starting on day (d−1) relative to the administration of sapacitabine or the metabolite thereof, in said first treatment cycle; followed by a rest period of at least 2 weeks, or until treatment-related toxicities are resolved, whichever is longer; and wherein said second treatment cycle comprises: (a) administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 3 to 5 consecutive days for 2 weeks, starting on day d, where d is the first day of treatment with sapacitabine, or the metabolite thereof, in said second treatment cycle; and (b) administering a therapeutically effective amount of seliciclib for 3 to 5 consecutive days for 2 weeks, starting on day (d−1) relative to the administration of sapacitabine or the metabolite thereof, in said second treatment cycle; followed by a rest period of at least 2 weeks, or until treatment-related toxicities are resolved, whichever is longer. Further aspects of the invention relate to a kit of parts, and corresponding uses.

2. 发明申请

US20150344486A1 PYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS 有权
标题翻译：吡啶衍生物作为蛋白激酶抑制剂
公开(公告)号：US20150344486A1
公开(公告)日：2015-12-03
申请号：US14820711
申请日：2015-08-07
申请人： Cyclacel Limited
发明人： Jonathan James HOLLICK , Stuart Donald JONES , Claire June FLYNN , Michael George THOMAS
IPC分类号： C07D487/04 , C07D487/10 , A61K31/551
CPC分类号： C07D487/04 , A61K31/551 , C07D453/02 , C07D487/10 , C07D519/00 , Y02A50/411
摘要： The present invention relates to pyrimidine derivatives capable of inhibiting one or more protein kinases. Further aspects relate to pharmaceutical compositions comprising the pyrimidine derivatives and the use thereof in the treatment of proliferative disorders.
摘要翻译：本发明涉及能够抑制一种或多种蛋白激酶的嘧啶衍生物。其它方面涉及包含嘧啶衍生物的药物组合物及其在治疗增殖性疾病中的用途。

3. 发明申请

US20150320762A1 TREATMENT OF PROLIFERATIVE DISEASES WITH PYRIMIDODIAZEPINONES 审中-公开
标题翻译：用吡咯烷酮治疗增殖性疾病
公开(公告)号：US20150320762A1
公开(公告)日：2015-11-12
申请号：US14387963
申请日：2013-03-28
申请人： Cyclacel limited
发明人： Susan DAVIS , Daniella I. ZHELEVA
IPC分类号： A61K31/551 , A61K9/00
CPC分类号： A61K9/0019 , A61K31/551
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in treating a proliferative disorder, wherein: X is NR7; R1 and R2 are each independently H, alkyl or cycloalkyl; R3 is a 6-membered heterocycloalkyl group selected from piperidinyl, piperazinyl, morpholinyl and tetrahydropyranyl, wherein said heterocycloalkyl group is optionally further substituted by one or more (CH2)—R19 groups; R4 and R4′ are each independently H or alkyl; or R4 and R4′ together form a spiro cycloalkyl group; Q is CH or N; R6 is OR8 or halogen; n is 1, 2 or 3; R19 is H, alkyl, aryl or a cycloalkyl group; R7 and R8 are each independently H or alkyl; and wherein said compound is administered in accordance with a dosing regimen which: (i) maintains a plasma concentration of from about 50 to about 500 nM for a period of up to about 16 hours; or (ii) maintains a plasma concentration of from about 0.5 μM to about 1 μM for a period of up to about 6 hours; or (iii) achieves a maximum plasma concentration (Cmax) of no more than about 500 nM within a period of about 6 hours; or (iv) achieves a maximum plasma concentration (Cmax) of no more than about 200 nM within a period of about 16 hours; or (v) achieves a maximum plasma concentration (Cmax) of about 0.5 μM to about 1 μM within about 6 hours. Further claims relate to a method of treatment based on this dosing regimen, and kits relating to the same.
摘要翻译：本发明的第一方面涉及用于治疗增殖性疾病的式（I）化合物或其药学上可接受的盐，其中：X为NR7; R1和R2各自独立地为H，烷基或环烷基; R3是选自哌啶基，哌嗪基，吗啉基和四氢吡喃基的6元杂环烷基，其中所述杂环烷基任选进一步被一个或多个（CH 2）R 19基团取代; R4和R4'各自独立地为H或烷基; 或R 4和R 4'一起形成螺环烷基; Q是CH或N; R6为OR8或卤素; n为1,2或3; R19是H，烷基，芳基或环烷基; R 7和R 8各自独立地为H或烷基; 并且其中所述化合物根据给药方案给药，所述给药方案：（i）维持约50至约500nM的血浆浓度达约16小时; 或（ii）维持约0.5μM至约1μM的血浆浓度达约6小时; 或（iii）在约6小时内达到不超过约500nM的最大血浆浓度（C max）; 或（iv）在约16小时内达到不大于约200nM的最大血浆浓度（C max）; 或（v）在约6小时内达到约0.5μM至约1μM的最大血浆浓度（C max）。进一步的权利要求涉及基于该给药方案的治疗方法和与其相关的试剂盒。

4. 发明授权

US10927113B2 Process for preparing purine derivatives 有权
公开(公告)号：US10927113B2
公开(公告)日：2021-02-23
申请号：US16480858
申请日：2018-01-25
申请人： Cyclacel Limited
发明人： Benjamin Mark Skead , Robert Westwood , Derek Londesbrough , Julian Scott Northen , Jonathan Charles Christian Atherton
IPC分类号： C07D473/16 , C07D473/40
摘要： The present invention relates to a process for preparing a compound of formula [I], said process comprising the steps of: formula [II]+formula [III]→formula [I] (i) forming a reaction mixture comprising (a) a compound of formula [II], (b) a compound of formula [III] and (c) 1,2-propanediol or polyethylene glycol, or a mixture thereof, and optionally (d) a base; (ii) heating said reaction mixture to a temperature of at least about 150° C. to form a compound of formula [I]; (iii) isolating said compound of formula [I]; and (iv) optionally converting said compound of formula [I] into salt form; wherein: R1 and R2 are each independently H, alkyl or haloalkyl; R3 and R4 are each independently H, alkyl, haloalkyl or aryl; R5 is alkyl, alkenyl, cycloalkyl or cycloalkyl-alkyl, each of which may be optionally substituted with one or more OH groups; R6 is selected from cyclopropylamino, cyclopropylmethylamino, cyclobutylamino, cyclobutylmethylamino and formula (A) where one of X, Y and Z is N and the remainder are CR9; R7, R8 and each R9 are independently H, alkyl or haloalkyl, wherein at least one of R7, R8 and R9 is other than H. Further aspects of the invention relate to a highly diastereoselective process for the preparation of compounds of formula [III], a process for preparing intermediates of formula [II], and other intermediates useful in the synthesis of compounds of formula [I], and to a process for preparing the crystalline tartrate salt and free base of compounds of formula [I].

5. 发明授权

US09675631B2 Dosing regimens for treatment of proliferative disorders comprising administration of sapacitabine 有权
公开(公告)号：US09675631B2
公开(公告)日：2017-06-13
申请号：US13967901
申请日：2013-08-15
申请人： Cyclacel Limited
发明人： Judy H. Chiao
IPC分类号： A61K31/7068 , A61K31/513
CPC分类号： A61K31/7068 , A61K31/513
摘要： One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).

6. 发明申请

US20150164933A1 DOSAGE REGIMEN FOR SAPACITABINE AND SELICICLIB 有权
标题翻译：用于SAPACITABINE和SELICICLIB的剂量计
公开(公告)号：US20150164933A1
公开(公告)日：2015-06-18
申请号：US14401357
申请日：2013-05-14
申请人： Cyclacel Limited
发明人： Judy H. Chiao , David Blake , Daniella Zheleva , Susan Davis , Simon Green , Geoffrey Shapiro
IPC分类号： A61K31/7068 , A61K9/00 , A61K31/52
CPC分类号： A61K31/7068 , A61K9/0053 , A61K31/52 , A61P35/00 , A61P35/02 , A61K2300/00
摘要： A first aspect of the invention relates to a method of treating a proliferative disorder in a subject, said method comprising administering to the subject a therapeutically effective amount of (i) sapacitabine, or a metabolite thereof; and (ii) seliciclib; in accordance with a dosing regimen comprising at least one first treatment cycle and at least one second treatment cycle, wherein said i first treatment cycle comprises: (a) administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 3 to 5 consecutive days for 2 weeks, starting on day d, where d is the first day of treatment with sapacitabine, or the metabolite thereof, in said first treatment cycle; and (b) optionally administering a therapeutically effective amount of seliciclib for 3 to 5 consecutive days for 2 weeks, starting on day (d−1) relative to the administration of sapacitabine or the metabolite thereof, in said first treatment cycle; followed by a rest period of at least 2 weeks, or until treatment-related toxicities are resolved, whichever is longer; and wherein said second treatment cycle comprises: (a) administering a therapeutically effective amount of sapacitabine, or a metabolite thereof, for 3 to 5 consecutive days for 2 weeks, starting on day d, where d is the first day of treatment with sapacitabine, or the metabolite thereof, in said second treatment cycle; and (b) administering a therapeutically effective amount of seliciclib for 3 to 5 consecutive days for 2 weeks, starting on day (d−1) relative to the administration of sapacitabine or the metabolite thereof, in said second treatment cycle; followed by a rest period of at least 2 weeks, or until treatment-related toxicities are resolved, whichever is longer. Further aspects of the invention relate to a kit of parts, and corresponding uses.
摘要翻译：本发明的第一方面涉及治疗受试者中增殖性疾病的方法，所述方法包括给予受试者治疗有效量的（i）西他滨或其代谢物; 和（ii）seliciclib; 根据包含至少一个第一治疗周期和至少一个第二治疗周期的给药方案，其中所述第一治疗周期包括：（a）将治疗有效量的西他滨或其代谢物施用连续3至5次天为期2周，从第d天开始，其中d是在所述第一治疗周期中用西他滨或其代谢物治疗的第一天; 和（b）在所述第一个治疗周期中相对于施用西来昔布或其代谢物，在第（d-1）天开始，任选地施用治疗有效量的西拉替尼连续3至5天，持续2周; 之后休息至少2周，或直到治疗相关毒性得到解决，以较长者为准; 并且其中所述第二治疗周期包括：（a）从第d天开始，给予治疗有效量的沙美他滨或其代谢物连续3至5个星期，其中d是用西他滨的第一天治疗，或其代谢物，在所述第二处理循环中; 和（b）在所述第二治疗周期中相对于施用西他滨或其代谢物，在第（d-1）天开始，施用治疗有效量的联用西拉霉3至5个连续2周。其次是至少2周的休息期，或直到治疗相关的毒性被解决为止，以较长者为准。本发明的其它方面涉及一组零件和相应的用途。

7. 发明申请

US20140142058A1 DOSING REGIMENS FOR TREATMENT OF PROLIFERATIVE DISORDERS COMPRISING ADMINISTRATION OF SAPACITABINE 有权
标题翻译：治疗包含SAPACITABINE治疗的增殖性疾病的剂量方案
公开(公告)号：US20140142058A1
公开(公告)日：2014-05-22
申请号：US13967901
申请日：2013-08-15
申请人： Cyclacel Limited
发明人： Judy H. CHIAO
IPC分类号： A61K31/7068
CPC分类号： A61K31/7068 , A61K31/513
摘要： One aspect of the present invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating a proliferative disorder, wherein the sapacitabine or metabolite thereof is administered in a dosing regimen comprising at least one treatment cycle, wherein said treatment cycle comprises administering a therapeutically effective amount of sapacitabine or metabolite thereof for about 2 to about 6 days per week, for 2 weeks out of 3 weeks. Another aspect of the invention relates to the use of sapacitabine, or a metabolite thereof, in the preparation of a medicament for treating cutaneous T-cell lymphoma (CTCL).
摘要翻译：本发明的一个方面涉及用于制备用于治疗增殖性病症的药物中的西他滨或其代谢物的用途，其中所述的沙美他滨或其代谢物以包含至少一个治疗周期的给药方案施用，其中所述治疗周期包括在3周内给予治疗有效量的每周约2至约6天的治疗有效量的沙美他滨或其代谢物2周。本发明的另一方面涉及用于制备用于治疗皮肤T细胞淋巴瘤（CTCL）的药物的西他滨或其代谢物的用途。

8. 发明申请

US20220289755A1 PROCESS FOR THE PREPARATION OF A PYRIMIDINO-DIAZEPINE DERIVATIVE 有权
公开(公告)号：US20220289755A1
公开(公告)日：2022-09-15
申请号：US17634693
申请日：2020-08-14
申请人： CYCLACEL LIMITED
发明人： Benjamin SKEAD , Derek LONDESBROUGH , Michal CZYZEWSKI , Chris ATHERTON , Chris GILL , Alex HUDSON
IPC分类号： C07D487/04
摘要： In one aspect, the invention relates to a process for preparing a compound of formula (XII), wherein PG is a protecting group, or a compound of formula (XI), comprising the steps of: (i) treating a compound of formula XIII, wherein PG is a protecting group, with N-methylpiperazine to form a compound of formula XII, wherein said compound of formula XII is in the form of a mixture of cis and trans isomers; (ii) combining the mixture formed in step (i) with an organic solvent and heating the solvent mixture so formed; (iii) isolating the trans-isomer of the compound of formula XII from the solvent mixture formed in step (ii); and (iv) optionally treating said trans-isomer of the compound of formula XII with an acid to form a compound of formula XI; and isolating said compound of formula XI. Further aspects of the invention relate to processes for preparing pyrimido-diazepinone derivatives using the above process and intermediates.

9. 发明申请

US20190298718A1 DOSING REGIMEN 审中-公开
公开(公告)号：US20190298718A1
公开(公告)日：2019-10-03
申请号：US16173127
申请日：2018-10-29
申请人： Cyclacel Limited
发明人： Judy H. CHIAO
IPC分类号： A61K31/506 , A61K31/7068 , A61P35/02 , A61K9/00
摘要： The invention relates to a method of treating AML in a subject having a white blood cell (WBC) count of less than about 10,000 cells/microliter, and/or a cytogenetic risk classification according to the US Southwest Oncology Group (SWOG) that is not unfavourable, and/or the subject falls within a classification selected from antecedent myelodysplastic syndrome (MDS), antecedent myeloproliferative neoplasm (MPN), and antecedent myelodysplastic/myeloproliferative neoplasm (MDS/MPN), wherein the method comprises (i) a first treatment cycle comprising administering decitabine for 5 to 10 consecutive days followed by a rest period of from 3 to 5 weeks, or until treatment-related toxicities are resolved, whichever is longer; and (ii) a second treatment cycle comprising administering sapacitabine, or a metabolite thereof, for 3 consecutive days per week, for 2 weeks followed by a rest period of from 2 to 4 weeks, or until treatment-related toxicities are resolved, whichever is longer.

10. 发明授权

US09133199B2 Pyrimidine derivatives as protein kinase inhibitors 有权
标题翻译：嘧啶衍生物作为蛋白激酶抑制剂
公开(公告)号：US09133199B2
公开(公告)日：2015-09-15
申请号：US13910349
申请日：2013-06-05
申请人： Cyclacel Limited
发明人： Jonathan James Hollick , Stuart Donald Jones , Claire June Flynn , Michael George Thomas
IPC分类号： A61K31/551 , C07D487/04 , C07D519/00 , C07D453/02
CPC分类号： C07D487/04 , A61K31/551 , C07D453/02 , C07D487/10 , C07D519/00 , Y02A50/411
摘要： The present invention relates to a compound of formula (VII)I, or pharmaceutically acceptable salt or ester thereof, wherein: X is NR7; Y is O or N—(CH2)nR19; n is 1, 2 or 3; m is 1 or 2; R1 and R2 are each independently H, alkyl or cycloalkyl; R4 and R4′ are each independently H or alkyl; or R4 and R4′ together form a spiro cycloalkyl group; R19 is H, alkyl, aryl or a cycloalkyl group; R6 is OR8 or halogen; and R7 and R8 are each independently H or alkyl. Further aspects relate to pharmaceutical compositions comprising said compounds and use therefore in the treatment of proliferative disorders and the like.
摘要翻译：本发明涉及式（VII）I化合物或其药学上可接受的盐或酯，其中：X为NR7; Y是O或N-（CH 2）n R 19; n为1,2或3; m为1或2; R1和R2各自独立地为H，烷基或环烷基; R4和R4'各自独立地为H或烷基; 或R 4和R 4'一起形成螺环烷基; R19是H，烷基，芳基或环烷基; R6为OR8或卤素; 并且R 7和R 8各自独立地为H或烷基。其它方面涉及包含所述化合物的药物组合物，因此用于治疗增殖性疾病等。

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