CN110325186A - 用于治疗内皮素相关疾病的4-嘧啶磺酰胺衍生物与活性成分的组合 - Google Patents

用于治疗内皮素相关疾病的4-嘧啶磺酰胺衍生物与活性成分的组合 Download PDF

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Publication number
CN110325186A
CN110325186A CN201780087445.XA CN201780087445A CN110325186A CN 110325186 A CN110325186 A CN 110325186A CN 201780087445 A CN201780087445 A CN 201780087445A CN 110325186 A CN110325186 A CN 110325186A
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pharmaceutically acceptable
acceptable salt
aprocitentan
hypertension
combination
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CN201780087445.XA
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Chinese (zh)
Inventor
马克·贝列特
马汀·波利
马丁尼·克劳泽
马克·艾格拉尔兹
菲利普·科勒
伊凡·申德尔霍尔兹
马库斯·冯劳默尔
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Actelion Pharmaceuticals Ltd
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Actelion Pharmaceuticals Ltd
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Application filed by Actelion Pharmaceuticals Ltd filed Critical Actelion Pharmaceuticals Ltd
Publication of CN110325186A publication Critical patent/CN110325186A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/401—Proline; Derivatives thereof, e.g. captopril
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    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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    • 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
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    • 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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
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    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/549—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 sulfur as the ring hetero atoms, e.g. sulthiame having two or more nitrogen atoms in the same ring, e.g. hydrochlorothiazide
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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CN201780087445.XA 2017-02-27 2017-11-06 用于治疗内皮素相关疾病的4-嘧啶磺酰胺衍生物与活性成分的组合 Pending CN110325186A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EPPCT/EP2017/054489 2017-02-27
EP2017054489 2017-02-27
EP2017061487 2017-05-12
EPPCT/EP2017/061487 2017-05-12
PCT/EP2017/078371 WO2018153513A1 (en) 2017-02-27 2017-11-06 Combinations of a 4-pyrimidinesulfamide derivative with active ingredients for the treatment of endothelin related diseases

Publications (1)

Publication Number Publication Date
CN110325186A true CN110325186A (zh) 2019-10-11

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ID=60268369

Family Applications (3)

Application Number Title Priority Date Filing Date
CN201780087445.XA Pending CN110325186A (zh) 2017-02-27 2017-11-06 用于治疗内皮素相关疾病的4-嘧啶磺酰胺衍生物与活性成分的组合
CN201880014146.8A Pending CN110381948A (zh) 2017-02-27 2018-02-26 4-嘧啶磺酰胺衍生物的结晶形式
CN202311718027.XA Pending CN117946011A (zh) 2017-02-27 2018-02-26 4-嘧啶磺酰胺衍生物的结晶形式

Family Applications After (2)

Application Number Title Priority Date Filing Date
CN201880014146.8A Pending CN110381948A (zh) 2017-02-27 2018-02-26 4-嘧啶磺酰胺衍生物的结晶形式
CN202311718027.XA Pending CN117946011A (zh) 2017-02-27 2018-02-26 4-嘧啶磺酰胺衍生物的结晶形式

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US (5) US11174247B2 (enExample)
EP (3) EP3658140B1 (enExample)
JP (3) JP7223701B2 (enExample)
KR (3) KR102700778B1 (enExample)
CN (3) CN110325186A (enExample)
AU (2) AU2017400276B2 (enExample)
BR (2) BR112019017658A2 (enExample)
CA (2) CA3053991A1 (enExample)
CL (3) CL2019002464A1 (enExample)
DK (2) DK3658140T3 (enExample)
ES (2) ES3038007T3 (enExample)
FI (2) FI3658140T3 (enExample)
HR (2) HRP20250921T1 (enExample)
HU (2) HUE072288T2 (enExample)
IL (4) IL315563A (enExample)
LT (2) LT3658140T (enExample)
MA (2) MA49664A (enExample)
MX (3) MX392313B (enExample)
MY (2) MY199557A (enExample)
NZ (1) NZ757344A (enExample)
PH (2) PH12019501937A1 (enExample)
PL (2) PL3658140T3 (enExample)
PT (2) PT3658140T (enExample)
RS (2) RS67082B1 (enExample)
SG (3) SG11201907435PA (enExample)
SI (2) SI3658140T1 (enExample)
TW (2) TWI786089B (enExample)
UA (1) UA126122C2 (enExample)
WO (2) WO2018153513A1 (enExample)

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CN112679441A (zh) * 2019-10-18 2021-04-20 普济生物科技（台州）有限公司 阿普昔腾坦的晶型、制备方法及其用途
CN114644595A (zh) * 2020-12-19 2022-06-21 普济生物科技（台州）有限公司 阿普昔腾坦的无定型态、其药物组合物和用途
WO2024140425A1 (zh) * 2022-12-30 2024-07-04 苏州科睿思制药有限公司 一种阿普昔腾坦晶型及其制备方法和用途

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US20160045527A1 (en) * 2014-08-14 2016-02-18 Vivus, Inc. Treatment of sleep apnea with a combination of a carbonic anhydrase inhibitor and an aldosterone antagonist
LT3658140T (lt) 2017-02-27 2025-08-25 Idorsia Pharmaceuticals Ltd Aprocitentano ir kitų veikliųjų sudedamųjų dalių deriniai, skirti atsparios hipertenzijos gydymui
PL3716979T3 (pl) * 2017-11-30 2025-08-04 Idorsia Pharmaceuticals Ltd Połączenie pochodnej 4-pirymidynosulfamidu z inhibitorem sglt-2 do leczenia chorób związanych w endoteliną
WO2020069521A1 (en) 2018-09-28 2020-04-02 Flow Medical Corporation Catheter apparatus
MA54522B1 (fr) 2018-12-21 2024-07-31 Actelion Pharmaceuticals Ltd Macitentan pour le traitement de l'hypertension artérielle pulmonaire
TW202042818A (zh) 2019-01-25 2020-12-01 瑞士商艾克泰聯製藥有限公司 用於治療慢性血栓性肺高血壓之醫藥組成物
CN112569357B (zh) * 2019-09-30 2023-03-28 深圳奥萨制药有限公司 双重内皮素受体拮抗剂与利尿剂的组合物
EP4056182A1 (en) * 2019-11-07 2022-09-14 Crystal Pharmaceutical (Suzhou) Co., Ltd. Crystal form of aprocitentan, preparation method therefor and use thereof
WO2021237004A1 (en) 2020-05-21 2021-11-25 Teva Pharmaceuticals International Gmbh Solid state forms of aprocitentan and process for preparation thereof
US11730735B2 (en) 2020-07-10 2023-08-22 Astrazeneca Ab Combination of zibotentan and dapagliflozin for the treatment of endothelin related diseases
WO2023111797A1 (en) * 2021-12-17 2023-06-22 Janssen Biotech, Inc. Pyrimidine sulfamide derivatives and process for manufacturing them
WO2023227490A1 (en) 2022-05-22 2023-11-30 Idorsia Pharmaceuticals Ltd Aprocitentan for the treatment of hypertension
CA3251318A1 (en) 2022-05-25 2023-11-30 Idorsia Pharmaceuticals Ltd CRYSTALLINE FORMS OF (5-(4-BROMOPHENYL)-6-(2-((5-BROMOPYRIMIDIN-2-YL)OXY)ETHOXY)PYRIMIDIN-4-YL)(SULFAMOYL) SODIUM AMIDE
KR20250152723A (ko) 2024-04-16 2025-10-24 경북대학교 산학협력단 신규한 피리미딘 유도체 화합물 및 이의 용도

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