CN101676267B - N-[4-(1-氰基环戊基)苯基]-2-(4-吡啶甲基)氨基-3-吡啶甲酰胺的盐 - Google Patents

N-[4-(1-氰基环戊基)苯基]-2-(4-吡啶甲基)氨基-3-吡啶甲酰胺的盐 Download PDF

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Publication number
CN101676267B
CN101676267B CN2008101496511A CN200810149651A CN101676267B CN 101676267 B CN101676267 B CN 101676267B CN 2008101496511 A CN2008101496511 A CN 2008101496511A CN 200810149651 A CN200810149651 A CN 200810149651A CN 101676267 B CN101676267 B CN 101676267B
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compd
mesylate
salt
administration
rat
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Chinese (zh)
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CN101676267A (zh
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袁开红
孙飘扬
周云曙
陈永江
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Jiangsu Hengrui Medicine Co Ltd
Shanghai Hengrui Pharmaceutical Co Ltd
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Jiangsu Hengrui Medicine Co Ltd
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Priority to CN2008101496511A priority Critical patent/CN101676267B/zh
Application filed by Jiangsu Hengrui Medicine Co Ltd filed Critical Jiangsu Hengrui Medicine Co Ltd
Priority to AU2009295168A priority patent/AU2009295168B2/en
Priority to CA2736664A priority patent/CA2736664C/en
Priority to JP2011526364A priority patent/JP5649132B2/ja
Priority to US13/063,850 priority patent/US8362256B2/en
Priority to BRPI0919018A priority patent/BRPI0919018A2/pt
Priority to KR1020117008504A priority patent/KR101674227B1/ko
Priority to RU2011113229/04A priority patent/RU2499796C2/ru
Priority to EP09813987.6A priority patent/EP2327697B1/en
Priority to MX2011002816A priority patent/MX2011002816A/es
Priority to PCT/CN2009/072239 priority patent/WO2010031266A1/zh
Publication of CN101676267A publication Critical patent/CN101676267A/zh
Priority to HK10107871.7A priority patent/HK1141514B/xx
Priority to ZA2011/01891A priority patent/ZA201101891B/en
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
CN2008101496511A 2008-09-16 2008-09-16 N-[4-(1-氰基环戊基)苯基]-2-(4-吡啶甲基)氨基-3-吡啶甲酰胺的盐 Active CN101676267B (zh)

Priority Applications (13)

Application Number Priority Date Filing Date Title
CN2008101496511A CN101676267B (zh) 2008-09-16 2008-09-16 N-[4-(1-氰基环戊基)苯基]-2-(4-吡啶甲基)氨基-3-吡啶甲酰胺的盐
PCT/CN2009/072239 WO2010031266A1 (zh) 2008-09-16 2009-06-11 N-[4-(1-氰基环戊基)苯基]-2-（4-吡啶甲基）氨基-3-吡啶甲酰胺的盐
JP2011526364A JP5649132B2 (ja) 2008-09-16 2009-06-11 Ｎ−［４−（１−シアノシクロペンチル）フェニル］−２−（４−ピリジルメチル）アミノ−３−ピリジンカルボキサミドの塩
US13/063,850 US8362256B2 (en) 2008-09-16 2009-06-11 Salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide
BRPI0919018A BRPI0919018A2 (pt) 2008-09-16 2009-06-11 sal farmaceuticamente aceitável, uso de sal, e, processo para a preparação de sal
KR1020117008504A KR101674227B1 (ko) 2008-09-16 2009-06-11 Ｎ-[4-(1-사이아노사이클로펜틸)페닐]-2-(4-피리딜메틸)아미노-3-피리딘카복스아마이드의 염
AU2009295168A AU2009295168B2 (en) 2008-09-16 2009-06-11 The salts of N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridyl methyl)amino-3-pyridinecarboxamide
EP09813987.6A EP2327697B1 (en) 2008-09-16 2009-06-11 The salts of n-(4-(1-cyanocyclopentyl)phenyl)-2-(4-pyridyl methyl)amino-3-pyridinecarboxamide
MX2011002816A MX2011002816A (es) 2008-09-16 2009-06-11 Sales de n-[4-(1-cianociclopentil)fenil]-2-(4-piridimetil) amino-3-piridinacarboxamida.
CA2736664A CA2736664C (en) 2008-09-16 2009-06-11 The salts of n-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide
RU2011113229/04A RU2499796C2 (ru) 2008-09-16 2009-06-11 Соли n-[4-(1-цианоциклопентил)фенил]-2-(4-пиридилметил)амино-3-пиридинкарбоксамида
HK10107871.7A HK1141514B (en) 2010-08-18 The salts of n-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridyl methyl)amino-3-pyridinecarboxamide
ZA2011/01891A ZA201101891B (en) 2008-09-16 2011-03-11 The salts of n-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridyl methyl)amino-3-pyridinecarboxamide

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2008101496511A CN101676267B (zh) 2008-09-16 2008-09-16 N-[4-(1-氰基环戊基)苯基]-2-(4-吡啶甲基)氨基-3-吡啶甲酰胺的盐

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CN101676267A CN101676267A (zh) 2010-03-24
CN101676267B true CN101676267B (zh) 2012-12-26

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US (1) US8362256B2 (enExample)
EP (1) EP2327697B1 (enExample)
JP (1) JP5649132B2 (enExample)
KR (1) KR101674227B1 (enExample)
CN (1) CN101676267B (enExample)
AU (1) AU2009295168B2 (enExample)
BR (1) BRPI0919018A2 (enExample)
CA (1) CA2736664C (enExample)
MX (1) MX2011002816A (enExample)
RU (1) RU2499796C2 (enExample)
WO (1) WO2010031266A1 (enExample)
ZA (1) ZA201101891B (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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CN109381436A (zh) * 2017-08-14 2019-02-26 江苏恒瑞医药股份有限公司 阿帕替尼药物组合物及其制备方法

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CN104072412A (zh) * 2014-07-08 2014-10-01 上海宣创生物科技有限公司 烟酰胺类衍生物的甲磺酸盐b晶型及其制备方法和应用
CN104086484B (zh) * 2014-07-08 2016-05-25 上海宣创生物科技有限公司 烟酰胺类衍生物的甲磺酸盐溶剂化物晶体及其制备方法和应用
CN104072411A (zh) * 2014-07-08 2014-10-01 上海宣创生物科技有限公司 烟酰胺类衍生物的甲磺酸盐c晶型及其制备方法和应用
CN104072413A (zh) * 2014-07-08 2014-10-01 上海宣创生物科技有限公司 烟酰胺类衍生物的甲磺酸盐a晶型及其制备方法和应用
CN104072410B (zh) * 2014-07-08 2017-02-08 上海宣创生物科技有限公司 烟酰胺类衍生物的甲磺酸盐d晶型及其制备方法和应用
CN104086483A (zh) * 2014-07-08 2014-10-08 上海宣创生物科技有限公司 烟酰胺类衍生物的甲磺酸盐f晶型及其制备方法和应用
CN105622499A (zh) * 2014-10-28 2016-06-01 华东理工常熟研究院有限公司 硫酸阿帕替尼的新晶型
CN105541708A (zh) * 2014-10-28 2016-05-04 华东理工常熟研究院有限公司 硫酸阿帕替尼的新晶型
CN105622498A (zh) * 2014-10-28 2016-06-01 华东理工常熟研究院有限公司 硫酸阿帕替尼的新晶型
JP6714017B6 (ja) 2015-04-15 2020-07-22 ダウ グローバル テクノロジーズ エルエルシー 垂直方向に伸長された気泡を有する断熱発泡体
CN105801476A (zh) * 2016-04-13 2016-07-27 上海宣创生物科技有限公司 阿帕替尼甲磺酸盐ii晶型及其制备方法和应用
CN106243031B (zh) * 2016-07-26 2017-09-08 江苏恒瑞医药股份有限公司 一种阿帕替尼的制备方法
TWI764943B (zh) 2016-10-10 2022-05-21 大陸商蘇州盛迪亞生物醫藥有限公司 一種抗pd-1抗體和vegfr抑制劑聯合在製備治療癌症的藥物中的用途
TWI771344B (zh) * 2016-12-01 2022-07-21 大陸商江蘇恆瑞醫藥股份有限公司 一種ｖｅｇｆｒ抑制劑與ｐａｒｐ抑制劑聯合在製備治療胃癌的藥物中的用途
CN108250138A (zh) * 2016-12-28 2018-07-06 上海宣创生物科技有限公司 阿帕替尼a晶型及其制备方法和应用
CN106963948A (zh) * 2017-05-12 2017-07-21 顾艳宏 阿帕替尼与Anti‑PD‑1抗体联用在制备结肠癌药物中的应用
CN109394685B (zh) * 2017-08-15 2021-04-06 江苏恒瑞医药股份有限公司 一种vegfr抑制剂的药物组合物及其制备方法
WO2019034048A1 (zh) * 2017-08-15 2019-02-21 江苏恒瑞医药股份有限公司 一种vegfr抑制剂晶型及其制备方法
WO2019094832A1 (en) * 2017-11-10 2019-05-16 Lsk Biopharma A combination therapy with apatinib for the treatment of cancer
BR112020010435A2 (pt) 2017-12-06 2020-11-24 Jiangsu Hengrui Medicine Co., Ltd. uso de inibidor da parp no tratamento de câncer de ovário ou câncer de mama resistente à quimioterapia
CN109942487A (zh) * 2017-12-21 2019-06-28 江苏恒瑞医药股份有限公司 一种吡啶类化合物及其制备方法、用途
TW201929900A (zh) 2017-12-29 2019-08-01 大陸商江蘇恆瑞醫藥股份有限公司 Ｐｄ－１抗體和阿帕替尼聯合治療三陰性乳腺癌的用途
WO2020051173A1 (en) * 2018-09-05 2020-03-12 Assia Chemical Industries Ltd New crystalline polymorphs of rivoceranib and rivoceranib mesylate
WO2021203769A1 (zh) * 2020-04-10 2021-10-14 江苏恒瑞医药股份有限公司 一种抗pd-1抗体在制备治疗肢端黑色素瘤的药物中的用途

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CA2736664C (en) 2016-05-24
EP2327697B1 (en) 2014-03-12
BRPI0919018A2 (pt) 2015-12-08
JP5649132B2 (ja) 2015-01-07
EP2327697A4 (en) 2012-06-06
RU2499796C2 (ru) 2013-11-27
MX2011002816A (es) 2011-04-05
US8362256B2 (en) 2013-01-29
ZA201101891B (en) 2012-05-30
RU2011113229A (ru) 2012-10-27
CA2736664A1 (en) 2010-03-25
AU2009295168A1 (en) 2010-03-25
KR101674227B1 (ko) 2016-11-08
HK1141514A1 (en) 2010-11-12
CN101676267A (zh) 2010-03-24
EP2327697A1 (en) 2011-06-01
AU2009295168B2 (en) 2014-02-13
KR20110059877A (ko) 2011-06-07
JP2012502885A (ja) 2012-02-02
WO2010031266A1 (zh) 2010-03-25
US20110184023A1 (en) 2011-07-28

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Address after: 222047 No. 7 Kunlun Shan Road, Lianyungang economic and Technological Development Zone, Jiangsu

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Patentee before: Jiangsu Shengdi Pharmaceutical Co.,Ltd.