CN106456773A - 用于治疗骨髓增生异常综合征的jak1抑制剂 - Google Patents

用于治疗骨髓增生异常综合征的jak1抑制剂 Download PDF

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Publication number
CN106456773A
CN106456773A CN201580017178.XA CN201580017178A CN106456773A CN 106456773 A CN106456773 A CN 106456773A CN 201580017178 A CN201580017178 A CN 201580017178A CN 106456773 A CN106456773 A CN 106456773A
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pyrrolo
pyrimidin
pyrazol
trifluoromethyl
methyl
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Chinese (zh)
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K·瓦迪
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Incyte Corp
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Incyte Corp
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P7/06Antianaemics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
CN201580017178.XA 2014-02-28 2015-02-27 用于治疗骨髓增生异常综合征的jak1抑制剂 Pending CN106456773A (zh)

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CN202010986614.7A CN112494652A (zh) 2014-02-28 2015-02-27 用于治疗骨髓增生异常综合征的jak1抑制剂

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461946124P 2014-02-28 2014-02-28
US61/946,124 2014-02-28
PCT/US2015/017963 WO2015131031A1 (en) 2014-02-28 2015-02-27 Jak1 inhibitors for the treatment of myelodysplastic syndromes

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CN202010986614.7A Pending CN112494652A (zh) 2014-02-28 2015-02-27 用于治疗骨髓增生异常综合征的jak1抑制剂

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US (4) US20150246046A1 (https=)
EP (1) EP3110409B1 (https=)
JP (1) JP6576941B2 (https=)
KR (1) KR20160136323A (https=)
CN (2) CN106456773A (https=)
AU (1) AU2015222913B2 (https=)
CA (1) CA2940659C (https=)
CL (1) CL2016002144A1 (https=)
CR (1) CR20160449A (https=)
CY (1) CY1120857T1 (https=)
DK (1) DK3110409T3 (https=)
EA (1) EA201691745A1 (https=)
ES (1) ES2688553T3 (https=)
HR (1) HRP20181661T1 (https=)
HU (1) HUE041456T2 (https=)
IL (1) IL247475B (https=)
LT (1) LT3110409T (https=)
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PE (1) PE20161388A1 (https=)
PL (1) PL3110409T3 (https=)
PT (1) PT3110409T (https=)
RS (1) RS57723B1 (https=)
SG (2) SG10201807952PA (https=)
SI (1) SI3110409T1 (https=)
SM (1) SMT201800551T1 (https=)
UA (1) UA121857C2 (https=)
WO (1) WO2015131031A1 (https=)
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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109867676A (zh) * 2017-12-01 2019-06-11 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
CN111358791A (zh) * 2020-03-13 2020-07-03 深圳百奥捷生物科技有限公司 Jak/stat信号通路磷酸盐抑制剂在制备治疗dba疾病的药物中的应用
CN113490484A (zh) * 2018-10-31 2021-10-08 因赛特公司 治疗血液疾病的组合疗法
CN114007621A (zh) * 2019-03-05 2022-02-01 因赛特公司 用于治疗慢性肺同种异体移植物功能障碍的jak1途径抑制剂
WO2024222835A1 (en) * 2023-04-27 2024-10-31 Sironax Ltd. Sarm1 modulators, preparations, and uses thereof

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EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
PT3354652T (pt) 2010-03-10 2020-07-20 Incyte Holdings Corp Derivados de piperidin-4-ilazetidina como inibidores de jak1
RS54824B1 (sr) 2010-05-21 2016-10-31 Incyte Holdings Corp Topikalna formulacija za inhibiciju jak-a
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CN104918945B (zh) 2012-11-01 2018-01-05 因赛特公司 作为jak抑制剂的三环稠合噻吩衍生物
CN113384546A (zh) 2012-11-15 2021-09-14 因赛特公司 鲁索利替尼的缓释剂型
JP6437452B2 (ja) 2013-01-14 2018-12-12 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Pimキナーゼ阻害剤として有用な二環式芳香族カルボキサミド化合物
RS60244B1 (sr) 2013-01-15 2020-06-30 Incyte Holdings Corp Jedinjenja tiazolkarboksamida i piridinkarboksamida korisna kao inhibitori pim kinaze
WO2014138168A1 (en) 2013-03-06 2014-09-12 Incyte Corporation Processes and intermediates for making a jak inhibitor
SMT201900223T1 (it) 2013-05-17 2019-07-11 Incyte Corp Sale di bipirazolo come inibitore di jak
SG10201801069QA (en) 2013-08-07 2018-03-28 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
CN105658653A (zh) 2013-08-23 2016-06-08 因赛特公司 可用作pim激酶抑制剂的呋喃并-和噻吩并-吡啶甲酰胺化合物
PH12020552277A1 (en) 2014-04-08 2023-07-17 Incyte Holdings Corp Treatment of b-cell malignancies by a combination jak and pi3k inhibitor
CN106687462A (zh) 2014-04-30 2017-05-17 因赛特公司 Jak1抑制剂的制备方法以及其新形式
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US9580418B2 (en) 2014-07-14 2017-02-28 Incyte Corporation Bicyclic aromatic carboxamide compounds useful as Pim kinase inhibitors
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WO2016196244A1 (en) 2015-05-29 2016-12-08 Incyte Corporation Pyridineamine compounds useful as pim kinase inhibitors
TWI734699B (zh) 2015-09-09 2021-08-01 美商英塞特公司 Pim激酶抑制劑之鹽
US9920032B2 (en) 2015-10-02 2018-03-20 Incyte Corporation Heterocyclic compounds useful as pim kinase inhibitors
EP3461887A4 (en) * 2016-03-09 2020-01-22 University Of Ulsan Foundation For Industry Cooperation COMPOSITION FOR PROLIFERATION, PROMOTION OF DIFFERENTIATION OR SENESCENCE INHIBITION OF STEM CELLS WITH JAK1 INHIBITOR AS AN ACTIVE SUBSTANCE
KR101934107B1 (ko) * 2016-12-15 2018-12-31 가톨릭대학교산학협력단 골수형성이상 증후군 환자의 저메틸화 제제 치료 반응성 및 생존 예후 예측용 조성물
JP7112755B2 (ja) 2017-01-23 2022-08-04 シャンハイ ロングウッド バイオファーマシューティカルズ カンパニー リミテッド Jak酵素阻害剤及びその製造方法と用途
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EP4085965A1 (en) 2018-02-01 2022-11-09 Shifamed Holdings, LLC Intravascular blood pumps and methods of use and manufacture
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MD3773593T2 (ro) 2018-03-30 2024-10-31 Incyte Corp Tratament hidradenitei supurative utilizând inhibitori ai JAK
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KR102900540B1 (ko) * 2018-10-31 2025-12-17 스템라인 테라퓨틱스, 인코포레이티드 디프테리아 독소-인간 인터루킨-3 접합체를 다른 제제와 조합하여 사용해서 골수증식성 신생물을 치료하는 조합 치료 방법
CN111320633B (zh) * 2018-12-14 2022-09-27 中国医药研究开发中心有限公司 吡咯/咪唑并六元杂芳环类化合物及其制备方法和医药用途
CN114761013A (zh) 2019-09-27 2022-07-15 迪斯克医药公司 治疗骨髓纤维化和相关病症的方法
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FI4157831T3 (fi) 2020-06-02 2024-12-02 Incyte Corp Menetelmiä jak1-estäjän valmistamiseksi
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WO2022125670A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
KR20230133317A (ko) * 2021-01-18 2023-09-19 액티브 바이오테크 에이비 골수이형성 증후군의 치료에 이용하기 위한 타스퀴니모드또는 이의 약제학적으로 허용가능한 염
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Publication number Priority date Publication date Assignee Title
CN109867676A (zh) * 2017-12-01 2019-06-11 北京普祺医药科技有限公司 一种吡咯并嘧啶衍生的化合物、药物组合物以及其用途
CN113490484A (zh) * 2018-10-31 2021-10-08 因赛特公司 治疗血液疾病的组合疗法
CN114007621A (zh) * 2019-03-05 2022-02-01 因赛特公司 用于治疗慢性肺同种异体移植物功能障碍的jak1途径抑制剂
CN111358791A (zh) * 2020-03-13 2020-07-03 深圳百奥捷生物科技有限公司 Jak/stat信号通路磷酸盐抑制剂在制备治疗dba疾病的药物中的应用
WO2024222835A1 (en) * 2023-04-27 2024-10-31 Sironax Ltd. Sarm1 modulators, preparations, and uses thereof

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JP6576941B2 (ja) 2019-09-18
SG10201807952PA (en) 2018-10-30
SI3110409T1 (sl) 2018-11-30
CA2940659C (en) 2023-01-03
MY185392A (en) 2021-05-17
MX2016011103A (es) 2017-02-28
US20150246046A1 (en) 2015-09-03
SMT201800551T1 (it) 2019-01-11
EP3110409A1 (en) 2017-01-04
UA121857C2 (uk) 2020-08-10
US20210069193A1 (en) 2021-03-11
CR20160449A (es) 2016-12-20
US20220378791A1 (en) 2022-12-01
KR20160136323A (ko) 2016-11-29
PE20161388A1 (es) 2016-12-28
IL247475B (en) 2020-05-31
ES2688553T3 (es) 2018-11-05
PT3110409T (pt) 2018-11-07
CY1120857T1 (el) 2019-12-11
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MX372939B (es) 2020-04-03
EP3110409B1 (en) 2018-08-15
BR112016019511A2 (https=) 2017-08-15
CA2940659A1 (en) 2015-09-03
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AU2015222913A1 (en) 2016-09-29
CN112494652A (zh) 2021-03-16
PL3110409T3 (pl) 2018-12-31
ZA201606610B (en) 2020-08-26
CL2016002144A1 (es) 2016-12-16
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AU2015222913B2 (en) 2019-12-12
US20190111058A1 (en) 2019-04-18
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WO2015131031A1 (en) 2015-09-03
HUE041456T2 (hu) 2019-05-28

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