TWI853965B - 神經激肽-1拮抗劑 - Google Patents

神經激肽-1拮抗劑 Download PDF

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TWI853965B
TWI853965B TW109121881A TW109121881A TWI853965B TW I853965 B TWI853965 B TW I853965B TW 109121881 A TW109121881 A TW 109121881A TW 109121881 A TW109121881 A TW 109121881A TW I853965 B TWI853965 B TW I853965B
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compound
alkyl
cycloalkyl
hydrogen
pharmaceutically acceptable
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TW109121881A
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Chinese (zh)
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TW202115064A (zh
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黃建
祝令建
鄒洋
唐應剛
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大陸商上海盛迪醫藥有限公司
大陸商上海森輝醫藥有限公司
大陸商江蘇恆瑞醫藥股份有限公司
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    • C—CHEMISTRY; METALLURGY
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    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/06—Phosphorus compounds without P—C bonds
    • C07F9/08—Esters of oxyacids of phosphorus
    • C07F9/09—Esters of phosphoric acids
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
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    • 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
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    • 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
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    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
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    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
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    • C07F9/65615—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing a spiro condensed ring system of the formula where at least one of the atoms X or Y is a hetero atom, e.g. S
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  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Addiction (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biotechnology (AREA)
TW109121881A 2019-06-28 2020-06-29 神經激肽-1拮抗劑 TWI853965B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201910572272.1 2019-06-28
CN201910572272 2019-06-28
CN201911375262.5 2019-12-27
CN201911375262 2019-12-27

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TW202115064A TW202115064A (zh) 2021-04-16
TWI853965B true TWI853965B (zh) 2024-09-01

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EP (1) EP3991730A4 (https=)
JP (2) JP7702887B2 (https=)
KR (1) KR102940508B1 (https=)
CN (2) CN113905735B (https=)
AU (1) AU2020308397B2 (https=)
BR (1) BR112021026554A2 (https=)
CA (1) CA3144247A1 (https=)
MX (1) MX2021015827A (https=)
TW (1) TWI853965B (https=)
WO (1) WO2020259675A1 (https=)

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Publication number Priority date Publication date Assignee Title
AU2021407138A1 (en) * 2020-12-25 2023-06-29 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Use of nk1 antagonist prodrug compound in combination with 5-ht3 receptor antagonist
CN114671913A (zh) * 2020-12-25 2022-06-28 上海盛迪医药有限公司 一种神经激肽-1拮抗剂的晶型及其制备方法
JP2025500688A (ja) * 2022-01-12 2025-01-09 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 ニューロキニン－１アンタゴニストプロドラッグ化合物の医薬組成物
CN118475589A (zh) 2022-01-12 2024-08-09 江苏恒瑞医药股份有限公司 一种神经激肽-1拮抗剂前药化合物的晶型
CN119528985A (zh) 2023-08-28 2025-02-28 科睿迪(南京)医药科技有限公司 神经激肽-1受体拮抗剂化合物

Citations (1)

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TW201604195A (zh) * 2009-08-14 2016-02-01 歐科生醫股份有限公司 神經激酶-１拮抗劑之靜脈注射劑型

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AU678409B2 (en) 1992-10-28 1997-05-29 Merck Sharp & Dohme Limited 4-arylmethyloxymethyl piperidines as tachykinin antagonists
US5661162A (en) 1992-12-14 1997-08-26 Merck Sharp & Dohme Limited 4-aminomethyl/thiomethyl/sulfonylmethyl-4-phenylpiperdines as tachykinin receptor antagonists
ES2120170T3 (es) 1994-01-13 1998-10-16 Merck Sharp & Dohme Antagonistas azaciclicos gem-disustituidos de taquiquininas.
WO1998022542A2 (en) * 1996-11-08 1998-05-28 Ikonos Corporation Chemical functionalization of surfaces
PE20030762A1 (es) 2001-12-18 2003-09-05 Schering Corp Compuestos heterociclicos como antagonistas nk1
CN1678317B (zh) * 2002-07-03 2010-10-27 先灵公司 用作治疗呕吐、抑郁症、焦虑症和咳嗽的神经激肽-1(nk-1)拮抗剂的1-酰氨基-4-苯基-4-苄氧基甲基-哌啶衍生物和相关化合物
AR046769A1 (es) * 2003-12-22 2005-12-21 Schering Corp Composiciones farmaceuticas
CA3123900A1 (en) * 2011-07-28 2013-01-31 Kempharm Inc. Methylphenidate-prodrugs, processes of making and using the same
CN102775401B (zh) 2012-08-15 2015-01-07 青岛农业大学 一种美洛昔康的合成方法
CN108148060B (zh) * 2016-12-05 2020-06-19 四川科伦博泰生物医药股份有限公司 取代的杂环化合物及其衍生物，其药物组合物、制备方法及用途
CN107383008A (zh) * 2017-08-14 2017-11-24 苏州信恩医药科技有限公司 一种罗拉匹坦的合成方法

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TW201604195A (zh) * 2009-08-14 2016-02-01 歐科生醫股份有限公司 神經激酶-１拮抗劑之靜脈注射劑型

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CN113905735B (zh) 2024-03-15
US12421260B2 (en) 2025-09-23
US20220380393A1 (en) 2022-12-01
TW202115064A (zh) 2021-04-16
CN113905735A (zh) 2022-01-07
MX2021015827A (es) 2022-04-11
AU2020308397B2 (en) 2026-01-08
KR20220054287A (ko) 2022-05-02
CA3144247A1 (en) 2020-12-30
JP7702887B2 (ja) 2025-07-04
EP3991730A4 (en) 2023-08-09
CN118324811A (zh) 2024-07-12
BR112021026554A2 (pt) 2022-05-24
EP3991730A1 (en) 2022-05-04
JP2025111616A (ja) 2025-07-30
AU2020308397A1 (en) 2022-02-17
WO2020259675A1 (zh) 2020-12-30
JP2022539570A (ja) 2022-09-12
KR102940508B1 (ko) 2026-03-16

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