AU2020308397B2 - Neurokinin-1 antagonist - Google Patents

Neurokinin-1 antagonist

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Publication number
AU2020308397B2
AU2020308397B2 AU2020308397A AU2020308397A AU2020308397B2 AU 2020308397 B2 AU2020308397 B2 AU 2020308397B2 AU 2020308397 A AU2020308397 A AU 2020308397A AU 2020308397 A AU2020308397 A AU 2020308397A AU 2020308397 B2 AU2020308397 B2 AU 2020308397B2
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Australia
Prior art keywords
compound
disorder
alkyl
group
disease
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AU2020308397A
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AU2020308397A1 (en
Inventor
Jian Huang
Yinggang TANG
Lingjian ZHU
Yang Zou
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Jiangsu Hengrui Medicine Co Ltd
Shanghai Shengdi Pharmaceutical Co Ltd
Shanghai Senhui Medicine Co Ltd
Original Assignee
Jiangsu Hengrui Medicine Co Ltd
Shanghai Shengdi Pharmaceutical Co Ltd
Shanghai Senhui Medicine Co Ltd
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Application filed by Jiangsu Hengrui Medicine Co Ltd, Shanghai Shengdi Pharmaceutical Co Ltd, Shanghai Senhui Medicine Co Ltd filed Critical Jiangsu Hengrui Medicine Co Ltd
Publication of AU2020308397A1 publication Critical patent/AU2020308397A1/en
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Publication of AU2020308397B2 publication Critical patent/AU2020308397B2/en
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • 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
    • A61K31/495—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
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/14—Antitussive agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P25/32—Alcohol-abuse
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Otolaryngology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Addiction (AREA)
  • Obesity (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
AU2020308397A 2019-06-28 2020-06-28 Neurokinin-1 antagonist Active AU2020308397B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CN201910572272 2019-06-28
CN201910572272.1 2019-06-28
CN201911375262 2019-12-27
CN201911375262.5 2019-12-27
PCT/CN2020/098460 WO2020259675A1 (zh) 2019-06-28 2020-06-28 神经激肽-1拮抗剂

Publications (2)

Publication Number Publication Date
AU2020308397A1 AU2020308397A1 (en) 2022-02-17
AU2020308397B2 true AU2020308397B2 (en) 2026-01-08

Family

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Family Applications (1)

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AU2020308397A Active AU2020308397B2 (en) 2019-06-28 2020-06-28 Neurokinin-1 antagonist

Country Status (10)

Country Link
US (1) US12421260B2 (enExample)
EP (1) EP3991730A4 (enExample)
JP (2) JP7702887B2 (enExample)
KR (1) KR102940508B1 (enExample)
CN (2) CN113905735B (enExample)
AU (1) AU2020308397B2 (enExample)
BR (1) BR112021026554A2 (enExample)
MX (1) MX2021015827A (enExample)
TW (1) TWI853965B (enExample)
WO (1) WO2020259675A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024501994A (ja) * 2020-12-25 2024-01-17 上海盛迪医▲葯▼有限公司 Nk1拮抗剤プロドラッグ化合物と5-ht3受容体拮抗剤との併用使用
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
CA3247908A1 (en) * 2022-01-12 2025-07-10 Jiangsu Hengrui Pharmaceuticals Co., Ltd. PHARMACEUTICAL COMPOSITION COMPRISING A NEUROKIN-1 ANTAGONIST PROMEDICINE COMPOUND
CA3247898A1 (en) 2022-01-12 2025-07-10 Jiangsu Hengrui Pharmaceuticals Co., Ltd. CRYSTALLINE FORM OF A NEUROKIN-1 ANTAGONIST PRODIGITANT COMPOUND
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160024092A1 (en) * 2009-08-14 2016-01-28 Opko Health, Inc. Intravenous formulations of neurokinin-1 antagonists

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EP0666856B1 (en) 1992-10-28 2000-01-05 MERCK SHARP & DOHME LTD. 4-arylmethyloxymethyl piperidines as tachykinin antagonists
JPH08504435A (ja) 1992-12-14 1996-05-14 メルク シヤープ エンド ドーム リミテツド タキキニン受容体拮抗剤としての4−アミノメチル/チオメチル/スルホニルメチル−4−フェニルピペリジン
JPH09507500A (ja) 1994-01-13 1997-07-29 メルク シヤープ エンド ドーム リミテツド gem二置換アザシクロ系のタキキニン拮抗薬
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
US7041682B2 (en) * 2002-07-03 2006-05-09 Schering Corporation NK1 antagonists
KR20060113737A (ko) * 2003-12-22 2006-11-02 쉐링 코포레이션 약제학적 조성물
KR20180069934A (ko) 2011-07-28 2018-06-25 켐팜 인코포레이티드 메틸페니데이트 프로드러그, 이의 제조 방법 및 사용 방법
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

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20160024092A1 (en) * 2009-08-14 2016-01-28 Opko Health, Inc. Intravenous formulations of neurokinin-1 antagonists

Also Published As

Publication number Publication date
JP7702887B2 (ja) 2025-07-04
CN113905735B (zh) 2024-03-15
KR20220054287A (ko) 2022-05-02
US12421260B2 (en) 2025-09-23
JP2025111616A (ja) 2025-07-30
CA3144247A1 (en) 2020-12-30
CN113905735A (zh) 2022-01-07
MX2021015827A (es) 2022-04-11
JP2022539570A (ja) 2022-09-12
TWI853965B (zh) 2024-09-01
TW202115064A (zh) 2021-04-16
US20220380393A1 (en) 2022-12-01
EP3991730A4 (en) 2023-08-09
AU2020308397A1 (en) 2022-02-17
WO2020259675A1 (zh) 2020-12-30
KR102940508B1 (ko) 2026-03-16
BR112021026554A2 (pt) 2022-05-24
EP3991730A1 (en) 2022-05-04
CN118324811A (zh) 2024-07-12

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