CN106458929A - N‑(氰基甲基)‑4‑(2‑(4‑吗啉代苯基氨基)嘧啶‑4‑基)苯甲酰胺盐酸盐 - Google Patents

N‑(氰基甲基)‑4‑(2‑(4‑吗啉代苯基氨基)嘧啶‑4‑基)苯甲酰胺盐酸盐 Download PDF

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Publication number
CN106458929A
CN106458929A CN201580031169.6A CN201580031169A CN106458929A CN 106458929 A CN106458929 A CN 106458929A CN 201580031169 A CN201580031169 A CN 201580031169A CN 106458929 A CN106458929 A CN 106458929A
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Prior art keywords
cyt
cyanomethyl
pyrimidin
morpholinophenylamino
benzamide
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Pending
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CN201580031169.6A
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English (en)
Chinese (zh)
Inventor
B.H.布朗
E.A.卡拉
J.N.海明威
H.莫里森
T.雷诺兹
B.史
D.斯蒂芬尼迪斯
F.王
M.R.瓦尔
J.A.惠特尼
Y.辛
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Gilead Sciences Inc
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Gilead Sciences Inc
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=53674249&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN106458929(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Priority to CN201910920874.1A priority Critical patent/CN110627728A/zh
Publication of CN106458929A publication Critical patent/CN106458929A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/301,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201580031169.6A 2014-06-12 2015-06-11 N‑(氰基甲基)‑4‑(2‑(4‑吗啉代苯基氨基)嘧啶‑4‑基)苯甲酰胺盐酸盐 Pending CN106458929A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201910920874.1A CN110627728A (zh) 2014-06-12 2015-06-11 N-(氰基甲基)-4-(2-(4-吗啉代苯基氨基)嘧啶-4-基)苯甲酰胺盐酸盐

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462011315P 2014-06-12 2014-06-12
US62/011,315 2014-06-12
PCT/US2015/035316 WO2015191846A1 (en) 2014-06-12 2015-06-11 N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide hydrochloride salts

Related Child Applications (1)

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CN201910920874.1A Division CN110627728A (zh) 2014-06-12 2015-06-11 N-(氰基甲基)-4-(2-(4-吗啉代苯基氨基)嘧啶-4-基)苯甲酰胺盐酸盐

Publications (1)

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CN106458929A true CN106458929A (zh) 2017-02-22

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CN201580031169.6A Pending CN106458929A (zh) 2014-06-12 2015-06-11 N‑(氰基甲基)‑4‑(2‑(4‑吗啉代苯基氨基)嘧啶‑4‑基)苯甲酰胺盐酸盐
CN201910920874.1A Pending CN110627728A (zh) 2014-06-12 2015-06-11 N-(氰基甲基)-4-(2-(4-吗啉代苯基氨基)嘧啶-4-基)苯甲酰胺盐酸盐

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US (5) US9469613B2 (https=)
EP (3) EP3907219A1 (https=)
JP (5) JP6600649B2 (https=)
KR (1) KR101928225B1 (https=)
CN (2) CN106458929A (https=)
AP (1) AP2016009551A0 (https=)
AR (1) AR100818A1 (https=)
AU (1) AU2015274554B9 (https=)
BR (1) BR112016028749A2 (https=)
CA (1) CA2951883C (https=)
CR (1) CR20160575A (https=)
CU (1) CU20160183A7 (https=)
CY (2) CY1123604T1 (https=)
DK (1) DK3154950T3 (https=)
EA (1) EA032639B1 (https=)
EC (1) ECSP16093323A (https=)
ES (1) ES2822773T3 (https=)
FI (1) FIC20240025I1 (https=)
FR (1) FR24C1030I2 (https=)
HR (1) HRP20201492T1 (https=)
HU (2) HUE051360T2 (https=)
IL (3) IL249038B (https=)
LT (2) LT3154950T (https=)
MA (1) MA40067A (https=)
MX (3) MX374541B (https=)
NL (1) NL301282I2 (https=)
NZ (1) NZ725966A (https=)
PH (1) PH12016502461A1 (https=)
PL (1) PL3154950T3 (https=)
PT (1) PT3154950T (https=)
RS (1) RS61065B1 (https=)
SG (2) SG10201911925TA (https=)
SI (1) SI3154950T1 (https=)
TW (3) TWI729644B (https=)
UY (1) UY36166A (https=)
WO (1) WO2015191846A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106316963B (zh) * 2015-06-26 2021-06-08 苏州泽璟生物制药股份有限公司 吗啡啉苯基氨基嘧啶化合物或其盐的多晶型物
CN115957221A (zh) * 2021-10-09 2023-04-14 广东东阳光药业有限公司 抗纤维化组合物

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TWI729644B (zh) 2014-06-12 2021-06-01 美商西爾拉癌症醫學公司 N-(氰基甲基)-4-(2-(4-𠰌啉基苯基胺基)嘧啶-4-基)苯甲醯胺
CN106316964B (zh) * 2015-06-26 2019-06-25 苏州泽璟生物制药股份有限公司 苯基氨基嘧啶化合物或其盐的多晶型物
TWI808055B (zh) 2016-05-11 2023-07-11 美商滬亞生物國際有限公司 Hdac 抑制劑與 pd-1 抑制劑之組合治療
TWI794171B (zh) 2016-05-11 2023-03-01 美商滬亞生物國際有限公司 Hdac抑制劑與pd-l1抑制劑之組合治療
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CN115957221A (zh) * 2021-10-09 2023-04-14 广东东阳光药业有限公司 抗纤维化组合物
CN115957221B (zh) * 2021-10-09 2026-01-06 广东东阳光药业股份有限公司 抗纤维化组合物

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USRE50497E1 (en) 2025-07-22
CY2024024I1 (el) 2025-03-28
KR101928225B1 (ko) 2018-12-11
TW201617323A (zh) 2016-05-16
CY1123604T1 (el) 2022-03-24
UY36166A (es) 2016-01-29
JP2021107465A (ja) 2021-07-29
CA2951883C (en) 2020-05-05
ECSP16093323A (es) 2017-01-31
BR112016028749A2 (pt) 2017-08-22
TWI729644B (zh) 2021-06-01
CU20160183A7 (es) 2017-05-10
IL276948B (en) 2021-09-30
US20160347719A1 (en) 2016-12-01
LTPA2024523I1 (https=) 2024-07-25
IL249038A0 (en) 2017-01-31
EP3907219A1 (en) 2021-11-10
US9469613B2 (en) 2016-10-18
EP3719005A1 (en) 2020-10-07
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