CN114302886A - ***并哒嗪类衍生物、其制备方法、药物组合物和用途 - Google Patents

***并哒嗪类衍生物、其制备方法、药物组合物和用途 Download PDF

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CN114302886A
CN114302886A CN202080061283.4A CN202080061283A CN114302886A CN 114302886 A CN114302886 A CN 114302886A CN 202080061283 A CN202080061283 A CN 202080061283A CN 114302886 A CN114302886 A CN 114302886A
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alkyl
group
membered
heteroaryl
methyl
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CN114302886B (zh
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金赟
王非
吴金华
陈南阳
孙勇
李帅
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Shanghai Semerode Biotechnology Co ltd
Shanghai Simr Biotechnology Co ltd
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Shanghai Semerode Biotechnology Co ltd
Shanghai Simr Biotechnology Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with 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
    • A61K31/54—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
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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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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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

提供了一种***并哒嗪类衍生物、其制备方法、药物组合物和用途。该类***并哒嗪类衍生物如式I所示。所述***并哒嗪类衍生物具有良好的反向激动活性、反向激动活性、热力学溶解度、生物利用度和和药代动力学性质，具有较好的应用前景。

Description

PCT国内申请，说明书已公开。

Claims (20)

  1. PCT国内申请，权利要求书已公开。
CN202080061283.4A 2019-12-16 2020-12-16 ***并哒嗪类衍生物、其制备方法、药物组合物和用途 Active CN114302886B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201911296884.9A CN112979655A (zh) 2019-12-16 2019-12-16 ***并哒嗪类衍生物、其制备方法、药物组合物和用途
CN2019112968849 2019-12-16
PCT/CN2020/136998 WO2021121294A1 (zh) 2019-12-16 2020-12-16 ***并哒嗪类衍生物、其制备方法、药物组合物和用途

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CN114302886A true CN114302886A (zh) 2022-04-08
CN114302886B CN114302886B (zh) 2024-03-22

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CN202080061283.4A Active CN114302886B (zh) 2019-12-16 2020-12-16 ***并哒嗪类衍生物、其制备方法、药物组合物和用途

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US (1) US20230136194A1 (zh)
EP (1) EP4079734A4 (zh)
JP (1) JP7417742B2 (zh)
KR (1) KR20220140710A (zh)
CN (2) CN112979655A (zh)
AU (1) AU2020410470B2 (zh)
BR (1) BR112022011946A2 (zh)
CA (1) CA3161739A1 (zh)
CO (1) CO2022009489A2 (zh)
IL (1) IL293959A (zh)
MX (1) MX2022007426A (zh)
PE (1) PE20221517A1 (zh)
WO (1) WO2021121294A1 (zh)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117069725A (zh) * 2022-05-10 2023-11-17 上海赛默罗生物科技有限公司 咪唑并哒嗪取代苯环类衍生物、制备方法、药物组合物及用途
CN114591352B (zh) * 2022-05-11 2022-09-09 上海赛默罗生物科技有限公司 一种***并哒嗪类化合物及其应用
CN114773352B (zh) * 2022-06-20 2023-03-17 上海赛默罗生物科技有限公司 制备取代的烟酰胺的方法
CN116008443B (zh) * 2023-03-28 2023-06-30 上海赛默罗生物科技有限公司 α5-GABAA受体调节剂类药物中有关物质的检测方法

Citations (8)

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GB2345443A (en) * 1999-01-08 2000-07-12 Merck Sharp & Dohme Use of triazolo-pyridazines for treating premenstrual syndrome
US6110915A (en) * 1997-12-18 2000-08-29 Merck & Co., Inc. Antiemetic use of triazolo-pyridazine derivatives
US6174886B1 (en) * 1997-11-13 2001-01-16 Merck Sharp & Dohme Ltd. Antipsychotic use of triazolo-pyridazine derivatives
US6444666B1 (en) * 1997-08-28 2002-09-03 Merck Sharp & Dohme Ltd. Triazolopyridazine Derivatives for treating anxiety and enhancing cognition
CN1871008A (zh) * 2003-10-21 2006-11-29 默克公司 用于治疗神经病变性疼痛的***并－哒嗪化合物和它们的衍生物
CN101868458A (zh) * 2007-12-04 2010-10-20 弗·哈夫曼-拉罗切有限公司 异*唑并-哒嗪衍生物
CN107344936A (zh) * 2016-05-06 2017-11-14 如东赛默罗生物科技有限公司 ***哒嗪类衍生物、其制备方法、药物组合物和用途
CN110256441A (zh) * 2019-06-24 2019-09-20 江苏君若医药有限公司 一种巴瑞克替尼的制备方法

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GB9112504D0 (en) 1991-06-11 1991-07-31 Merck Sharp & Dohme Cell line
EP1605046B1 (en) 1992-12-10 2007-11-21 Merck Sharp & Dohme Limited Stably transfected cell lines expressing human GABA-A receptors with the subunit combination alpha-2, beta-3 and gamma-2
US10206921B2 (en) 2009-06-03 2019-02-19 The Regents Of The University Of California Methods and compositions for treating a subject for central nervous system (CNS) injury
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US9371282B2 (en) 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists
CN106854207B (zh) 2015-12-08 2019-10-29 上海赛默罗生物科技有限公司 呔嗪类衍生物、其制备方法、药物组合物和用途
CN107344938B (zh) * 2016-05-06 2022-05-06 上海赛默罗生物科技有限公司 吡唑-三嗪类衍生物、其制备方法、药物组合物和用途
AU2019233183B2 (en) * 2018-03-12 2024-02-01 Shanghai SIMR Biotechnology Co., Ltd Phthalazine isoxazole alkoxy derivatives, preparation method thereof, pharmaceutical composition and use thereof

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6444666B1 (en) * 1997-08-28 2002-09-03 Merck Sharp & Dohme Ltd. Triazolopyridazine Derivatives for treating anxiety and enhancing cognition
US6174886B1 (en) * 1997-11-13 2001-01-16 Merck Sharp & Dohme Ltd. Antipsychotic use of triazolo-pyridazine derivatives
US6110915A (en) * 1997-12-18 2000-08-29 Merck & Co., Inc. Antiemetic use of triazolo-pyridazine derivatives
GB2345443A (en) * 1999-01-08 2000-07-12 Merck Sharp & Dohme Use of triazolo-pyridazines for treating premenstrual syndrome
CN1871008A (zh) * 2003-10-21 2006-11-29 默克公司 用于治疗神经病变性疼痛的***并－哒嗪化合物和它们的衍生物
CN101868458A (zh) * 2007-12-04 2010-10-20 弗·哈夫曼-拉罗切有限公司 异*唑并-哒嗪衍生物
CN107344936A (zh) * 2016-05-06 2017-11-14 如东赛默罗生物科技有限公司 ***哒嗪类衍生物、其制备方法、药物组合物和用途
CN110256441A (zh) * 2019-06-24 2019-09-20 江苏君若医药有限公司 一种巴瑞克替尼的制备方法

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MX2022007426A (es) 2022-07-27
CO2022009489A2 (es) 2022-07-08
AU2020410470A1 (en) 2022-07-28
EP4079734A4 (en) 2023-01-25
WO2021121294A1 (zh) 2021-06-24
EP4079734A1 (en) 2022-10-26
PE20221517A1 (es) 2022-10-04
CA3161739A1 (en) 2021-06-24
CN114302886B (zh) 2024-03-22
JP7417742B2 (ja) 2024-01-18
AU2020410470B2 (en) 2023-07-27
JP2023508858A (ja) 2023-03-06
CN112979655A (zh) 2021-06-18
BR112022011946A2 (pt) 2022-09-06
US20230136194A1 (en) 2023-05-04
IL293959A (en) 2022-08-01
KR20220140710A (ko) 2022-10-18

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