BR112017019286A2 - composto de fórmula (i) ou um sal farmaceuticamente aceitável deste - Google Patents

composto de fórmula (i) ou um sal farmaceuticamente aceitável deste

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Publication number
BR112017019286A2
BR112017019286A2 BR112017019286-1A BR112017019286A BR112017019286A2 BR 112017019286 A2 BR112017019286 A2 BR 112017019286A2 BR 112017019286 A BR112017019286 A BR 112017019286A BR 112017019286 A2 BR112017019286 A2 BR 112017019286A2
Authority
BR
Brazil
Prior art keywords
hydroperoxy
pyrazole derivative
cancer drugs
substituted
drugs substituted
Prior art date
Application number
BR112017019286-1A
Other languages
English (en)
Chinese (zh)
Other versions
BR112017019286B1 (pt
Inventor
Z. Ding Charles
Chen Shuhui
Zhao Baoping
Xu Zhaobing
Liu Yingchun
Lin Ruibin
Wang Fei
Li Jian
Original Assignee
Chia Tai Tianqing Pharmaceutical Group Co., Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Chia Tai Tianqing Pharmaceutical Group Co., Ltd filed Critical Chia Tai Tianqing Pharmaceutical Group Co., Ltd
Publication of BR112017019286A2 publication Critical patent/BR112017019286A2/pt
Publication of BR112017019286B1 publication Critical patent/BR112017019286B1/pt

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

é divulgado um derivado de 2h-pirazol substituído que serve como inibidor de cdk4/6 seletivo. especificamente, é divulgado um composto de fórmula (i) ou um sal farmaceuticamente aceitável deste, o qual serve como inibidor de cdk4/6 seletivo.
BR112017019286-1A 2015-03-11 2016-03-10 Derivados de 2h-pirazol substituídos ou um sal farmacêuticamente aceitável dos mesmos BR112017019286B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201510107436.5 2015-03-11
CN201510107436 2015-03-11
CN201610019047.1 2016-01-12
CN201610019047 2016-01-12
PCT/CN2016/076041 WO2016141881A1 (zh) 2015-03-11 2016-03-10 作为抗癌药物的取代的2-氢-吡唑衍生物

Publications (2)

Publication Number Publication Date
BR112017019286A2 true BR112017019286A2 (pt) 2018-05-02
BR112017019286B1 BR112017019286B1 (pt) 2023-02-14

Family

ID=56878940

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017019286-1A BR112017019286B1 (pt) 2015-03-11 2016-03-10 Derivados de 2h-pirazol substituídos ou um sal farmacêuticamente aceitável dos mesmos

Country Status (13)

Country Link
US (1) US9969719B2 (pt)
EP (1) EP3269715B1 (pt)
JP (1) JP6726677B2 (pt)
KR (1) KR102615733B1 (pt)
CN (2) CN107428731B (pt)
AU (1) AU2016228660B2 (pt)
BR (1) BR112017019286B1 (pt)
CA (1) CA2978363A1 (pt)
ES (1) ES2806206T3 (pt)
HK (1) HK1244803A1 (pt)
RU (1) RU2722363C2 (pt)
TW (1) TWI688559B (pt)
WO (1) WO2016141881A1 (pt)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI3464336T1 (sl) 2016-06-01 2022-06-30 Athira Pharma, Inc. Spojine
WO2017211303A1 (en) 2016-06-07 2017-12-14 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
CN109689641B (zh) * 2016-09-09 2020-11-03 正大天晴药业集团股份有限公司 一种取代的2-氢-吡唑衍生物的晶型、盐型及其制备方法
CN106588884B (zh) * 2016-11-10 2019-04-09 浙江大学 2-多取代芳环-嘧啶类衍生物及制备和医药用途
US10988466B2 (en) 2017-03-23 2021-04-27 Jacobio Pharmaceuticals Co., Ltd. Heterocyclic derivatives useful as SHP2 inhibitors
CN107382974B (zh) * 2017-06-08 2020-06-05 扬州市三药制药有限公司 一种嘧啶胺类化合物作为周期蛋白依赖性激酶4/6抑制剂的应用
CN111315379A (zh) * 2017-08-15 2020-06-19 北京轩义医药科技有限公司 Cdk4/6抑制剂及其用途
CN109503573A (zh) * 2017-09-14 2019-03-22 昆明圣加南生物科技有限公司 2-取代苯胺基嘧啶衍生物及其用途
AU2018354972B2 (en) 2017-10-27 2021-07-08 Fresenius Kabi Oncology Ltd. An improved process for the preparation of ribociclib and its salts
BR112020015405A2 (pt) * 2018-01-29 2020-12-08 Beta Pharma, Inc. Compostos de 2h-indazóis como inibidores cdk4 e cdk6, composições farmacêuticas que os compreendem, seus usos terapêuticos e métodos de preparação
BR112020015431A2 (pt) 2018-02-15 2020-12-08 Nuvation Bio Inc. Compostos heterocíclicos como inibidores de quinase
JP2022519205A (ja) * 2019-01-29 2022-03-22 ベータ・ファーマ・インコーポレイテッド 脳腫瘍および脳転移の治療剤としての２ｈ－インダゾール誘導体
TW202102487A (zh) * 2019-03-20 2021-01-16 美商貝達醫藥公司 N-(5-((4-乙基哌𠯤-1-基)甲基)吡啶-2-基)-5-氟-4-(3-異丙基-2-甲基-2h-吲唑-5-基)嘧啶-2-胺及其鹽的結晶與非晶型以及其製備方法與醫療用途
AU2020269469A1 (en) * 2019-05-05 2021-12-09 Regor Pharmaceuticals, Inc. CDK inhibitors
US20230331699A1 (en) 2020-06-22 2023-10-19 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Preparation method for cdk4/6 inhibitor
CN114539225B (zh) * 2020-11-11 2024-02-20 上海拓界生物医药科技有限公司 2-氨基-嘧啶类化合物
WO2022113003A1 (en) 2020-11-27 2022-06-02 Rhizen Pharmaceuticals Ag Cdk inhibitors
CN114605390B (zh) * 2020-12-04 2024-08-16 上海凌达生物医药有限公司 具有cdk激酶抑制活性的化合物、其药物组合物和用途
WO2022149057A1 (en) 2021-01-05 2022-07-14 Rhizen Pharmaceuticals Ag Cdk inhibitors
CN116940363A (zh) * 2021-03-03 2023-10-24 正大天晴药业集团股份有限公司 Cdk4/6抑制剂的联用药物组合物及其用途
CN118139844A (zh) 2021-09-27 2024-06-04 正大天晴药业集团股份有限公司 Cdk4/6抑制剂和芳香酶抑制剂的联用药物组合物
WO2023237055A1 (zh) * 2022-06-09 2023-12-14 正大天晴药业集团股份有限公司 一种cdk4/6抑制剂治疗去分化脂肪肉瘤的用途
WO2024032751A1 (zh) * 2022-08-12 2024-02-15 正大天晴药业集团股份有限公司 一种取代的2-氢-吡唑衍生物的晶型及其制备方法

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US8258129B2 (en) 2006-07-06 2012-09-04 Boehringer Ingelheim International Gmbh 4-heterocycloalkylpyri(mi)dines, process for the preparation thereof and their use as medicaments
RU2009108006A (ru) * 2006-09-08 2010-10-20 Пфайзер Продактс Инк. (Us) Синтез 2-(пиридин-2-иламино)-пиридо[2, 3-d]пиримидин-7-онов
US9259399B2 (en) * 2007-11-07 2016-02-16 Cornell University Targeting CDK4 and CDK6 in cancer therapy
SI2265607T1 (sl) * 2008-02-15 2017-06-30 Rigel Pharmaceuticals, Inc. Spojine pirimidin-2-amina in njihova uporaba kot inhibitorji JAK kinaz
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UY33227A (es) 2010-02-19 2011-09-30 Novartis Ag Compuestos de pirrolopirimidina como inhibidores de la cdk4/6
EP2558092B1 (en) * 2010-04-13 2018-06-27 Novartis AG Combination comprising a cyclin dependent kinase 4 or cyclin dependent kinase 6 (cdk4/6) inhibitor and an mtor inhibitor for treating cancer
WO2012129344A1 (en) 2011-03-23 2012-09-27 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3

Also Published As

Publication number Publication date
CN111333627B (zh) 2024-09-13
KR102615733B1 (ko) 2023-12-18
JP2018507883A (ja) 2018-03-22
US20180072707A1 (en) 2018-03-15
RU2722363C2 (ru) 2020-05-29
CN107428731A (zh) 2017-12-01
WO2016141881A1 (zh) 2016-09-15
TWI688559B (zh) 2020-03-21
AU2016228660B2 (en) 2020-05-07
CN107428731B (zh) 2020-05-05
CN111333627A (zh) 2020-06-26
BR112017019286B1 (pt) 2023-02-14
TW201639831A (zh) 2016-11-16
US9969719B2 (en) 2018-05-15
EP3269715A4 (en) 2018-08-08
KR20180005160A (ko) 2018-01-15
EP3269715A1 (en) 2018-01-17
HK1244803A1 (zh) 2018-08-17
CA2978363A1 (en) 2016-09-15
EP3269715B1 (en) 2020-05-13
AU2016228660A1 (en) 2017-10-19
JP6726677B2 (ja) 2020-07-22
ES2806206T3 (es) 2021-02-16
RU2017131559A3 (pt) 2019-04-11
RU2017131559A (ru) 2019-04-11

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

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