WO2019141096A1 - Composé d'urée substitué, son procédé de préparation et son utilisation - Google Patents

Composé d'urée substitué, son procédé de préparation et son utilisation Download PDF

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Publication number
WO2019141096A1
WO2019141096A1 PCT/CN2019/070390 CN2019070390W WO2019141096A1 WO 2019141096 A1 WO2019141096 A1 WO 2019141096A1 CN 2019070390 W CN2019070390 W CN 2019070390W WO 2019141096 A1 WO2019141096 A1 WO 2019141096A1
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WO
WIPO (PCT)
Prior art keywords
group
compound
alkyl
membered
nitrogen
Prior art date
Application number
PCT/CN2019/070390
Other languages
English (en)
Chinese (zh)
Inventor
刘金明
何婷
蔡家强
王利春
王晶翼
Original Assignee
四川科伦博泰生物医药股份有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 四川科伦博泰生物医药股份有限公司 filed Critical 四川科伦博泰生物医药股份有限公司
Publication of WO2019141096A1 publication Critical patent/WO2019141096A1/fr

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Classifications

    • 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
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

Abstract

L'invention concerne un composé d'urée substitué, son procédé de préparation et son utilisation. Plus particulièrement, l'invention concerne un composé d'urée substitué ou un sel pharmaceutiquement acceptable, un stéréoisomère, une substance polymorphe, un solvate, un N-oxyde, un composé marqué par un isotope, un métabolite ou un promédicament de celui-ci. L'invention concerne également un procédé de préparation du composé, un intermédiaire, une composition pharmaceutique comprenant le composé, et des utilisations thérapeutiques associées. Le composé ou la composition pharmaceutique de celui-ci est capable d'inhiber l'activité du récepteur A2a de l'adénosine et peut être utilisé pour traiter ou prévenir une maladie associée au récepteur A2a de l'adénosine, en particulier pour traiter une tumeur.
PCT/CN2019/070390 2018-01-19 2019-01-04 Composé d'urée substitué, son procédé de préparation et son utilisation WO2019141096A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201810051542 2018-01-19
CN201810051542.X 2018-01-19

Publications (1)

Publication Number Publication Date
WO2019141096A1 true WO2019141096A1 (fr) 2019-07-25

Family

ID=67302002

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2019/070390 WO2019141096A1 (fr) 2018-01-19 2019-01-04 Composé d'urée substitué, son procédé de préparation et son utilisation

Country Status (1)

Country Link
WO (1) WO2019141096A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113166119A (zh) * 2018-12-28 2021-07-23 四川科伦博泰生物医药股份有限公司 取代芳基化合物及其制备方法和用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1602196A (zh) * 2001-12-10 2005-03-30 弗·哈夫曼-拉罗切有限公司 作为腺苷调节剂的2－氨基苯并噻唑脲
CN1791600A (zh) * 2003-05-19 2006-06-21 弗·哈夫曼-拉罗切有限公司 用作腺苷受体的配体的苯并噻唑衍生物
CN1956983A (zh) * 2004-05-24 2007-05-02 弗·哈夫曼-拉罗切有限公司 4－羟基－4－甲基－哌啶－1－甲酸(4－甲氧基－7－吗啉－4－基－苯并噻唑－2－基)－酰胺
CN103664908A (zh) * 2013-12-10 2014-03-26 苏州大学 一种具有腺苷受体拮抗活性的氨基嘧啶杂环化合物

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1602196A (zh) * 2001-12-10 2005-03-30 弗·哈夫曼-拉罗切有限公司 作为腺苷调节剂的2－氨基苯并噻唑脲
CN1791600A (zh) * 2003-05-19 2006-06-21 弗·哈夫曼-拉罗切有限公司 用作腺苷受体的配体的苯并噻唑衍生物
CN1956983A (zh) * 2004-05-24 2007-05-02 弗·哈夫曼-拉罗切有限公司 4－羟基－4－甲基－哌啶－1－甲酸(4－甲氧基－7－吗啉－4－基－苯并噻唑－2－基)－酰胺
CN103664908A (zh) * 2013-12-10 2014-03-26 苏州大学 一种具有腺苷受体拮抗活性的氨基嘧啶杂环化合物
CN104447708A (zh) * 2013-12-10 2015-03-25 苏州大学 一种具有腺苷受体拮抗活性的氨基嘧啶杂环化合物

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113166119A (zh) * 2018-12-28 2021-07-23 四川科伦博泰生物医药股份有限公司 取代芳基化合物及其制备方法和用途
CN113166119B (zh) * 2018-12-28 2024-01-05 四川科伦博泰生物医药股份有限公司 取代芳基化合物及其制备方法和用途

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