CN108026069A - 2,3,4,5-四氢吡啶-6-胺衍生物 - Google Patents

2,3,4,5-四氢吡啶-6-胺衍生物 Download PDF

Info

Publication number
CN108026069A
CN108026069A CN201680055231.XA CN201680055231A CN108026069A CN 108026069 A CN108026069 A CN 108026069A CN 201680055231 A CN201680055231 A CN 201680055231A CN 108026069 A CN108026069 A CN 108026069A
Authority
CN
China
Prior art keywords
alkyloxy
alkyl
mmol
cyclopropyl
compound
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201680055231.XA
Other languages
English (en)
Chinese (zh)
Inventor
F.J.R.罗姆布茨
H.J.M.吉森
S.F.A.范布兰特
A.A.特拉班科-苏亚雷斯
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.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
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 Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Publication of CN108026069A publication Critical patent/CN108026069A/zh
Pending legal-status Critical Current

Links

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
    • A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • 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
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CN201680055231.XA 2015-09-23 2016-09-23 2,3,4,5-四氢吡啶-6-胺衍生物 Pending CN108026069A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP15186394 2015-09-23
EP15186394.1 2015-09-23
EP16172005 2016-05-30
EP16172005.7 2016-05-30
PCT/EP2016/072710 WO2017050978A1 (en) 2015-09-23 2016-09-23 2,3,4,5-tetrahydropyridin-6-amine derivatives

Publications (1)

Publication Number Publication Date
CN108026069A true CN108026069A (zh) 2018-05-11

Family

ID=56985626

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680055231.XA Pending CN108026069A (zh) 2015-09-23 2016-09-23 2,3,4,5-四氢吡啶-6-胺衍生物

Country Status (14)

Country Link
US (1) US20180334447A1 (https=)
EP (1) EP3353163B1 (https=)
JP (1) JP2018527387A (https=)
KR (1) KR20180053357A (https=)
CN (1) CN108026069A (https=)
AU (1) AU2016328589A1 (https=)
BR (1) BR112018005591A2 (https=)
CA (1) CA2995161A1 (https=)
EA (1) EA035026B1 (https=)
HK (1) HK1254800A1 (https=)
IL (1) IL258217A (https=)
MX (1) MX2018003565A (https=)
TW (1) TW201726651A (https=)
WO (1) WO2017050978A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114380736A (zh) * 2020-10-21 2022-04-22 复旦大学 一种2,3,4,5-四氢吡啶类化合物的合成方法

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019208509A1 (en) * 2018-04-23 2019-10-31 Shionogi & Co., Ltd. Bicyclic heterocycle derivatives having selective bace1 inhibitory activity
TW202014191A (zh) 2018-04-27 2020-04-16 日商鹽野義製藥股份有限公司 具有選擇性ｂａｃｅ１抑制活性的四氫哌喃并衍生物

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102471293A (zh) * 2009-07-24 2012-05-23 诺瓦提斯公司 *嗪衍生物及其作为bace抑制剂用于治疗神经障碍的用途
WO2014059185A1 (en) * 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2015124576A1 (en) * 2014-02-19 2015-08-27 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120258961A1 (en) * 2009-12-24 2012-10-11 Shionogi & Co., Ltd. 4-amino-1,3-thiazine or oxazine derivative
US8673894B2 (en) 2010-05-07 2014-03-18 Hoffmann-La Roche Inc. 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds
KR101730937B1 (ko) * 2010-06-09 2017-04-27 얀센 파마슈티카 엔.브이. 베타-세크레타아제(ｂａｃｅ) 저해제로 유용한 5,6-디하이드로-2ｈ-[1,4]옥사진-3-일-아민 유도체
JP5766198B2 (ja) 2010-10-29 2015-08-19 塩野義製薬株式会社 縮合アミノジヒドロピリミジン誘導体
US8815841B2 (en) 2011-02-18 2014-08-26 Hoffmann-La Roche Inc. 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors
US8785436B2 (en) 2011-05-16 2014-07-22 Hoffmann-La Roche Inc. 1,3-oxazines as BACE 1 and/or BACE2 inhibitors
CA2902212C (en) 2013-03-01 2020-10-13 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102471293A (zh) * 2009-07-24 2012-05-23 诺瓦提斯公司 *嗪衍生物及其作为bace抑制剂用于治疗神经障碍的用途
WO2014059185A1 (en) * 2012-10-12 2014-04-17 Amgen Inc. Amino - dihydrothiazine and amino - dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
WO2015124576A1 (en) * 2014-02-19 2015-08-27 H. Lundbeck A/S 2-amino-3, 5, 5-trifluoro-3, 4, 5, 6-tetrahydropyridines as bace1 inhibitors for treatment of alzheimer's disease

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114380736A (zh) * 2020-10-21 2022-04-22 复旦大学 一种2,3,4,5-四氢吡啶类化合物的合成方法
CN114380736B (zh) * 2020-10-21 2023-10-03 复旦大学 一种2,3,4,5-四氢吡啶类化合物的合成方法

Also Published As

Publication number Publication date
EP3353163A1 (en) 2018-08-01
TW201726651A (zh) 2017-08-01
WO2017050978A1 (en) 2017-03-30
EP3353163B1 (en) 2020-02-05
BR112018005591A2 (pt) 2018-10-09
HK1254800A1 (zh) 2019-07-26
CA2995161A1 (en) 2017-03-30
AU2016328589A1 (en) 2018-03-01
US20180334447A1 (en) 2018-11-22
JP2018527387A (ja) 2018-09-20
EA035026B1 (ru) 2020-04-20
EA201890769A1 (ru) 2018-09-28
MX2018003565A (es) 2018-06-18
IL258217A (en) 2018-05-31
KR20180053357A (ko) 2018-05-21

Similar Documents

Publication Publication Date Title
JP7840517B2 (ja) 二環式複素環誘導体およびオレキシン－２受容体アゴニストとしてのそれらの使用
CN103415521B (zh) 用作β分泌酶（BACE）抑制剂的3,4-二氢-吡咯并[1,2-a]吡嗪-1-基胺衍生物
US10266529B2 (en) Salts, co-crystals, and polymorphs of an anxiolytic compound
CN107108582B (zh) β-分泌酶的2，3，4，5-四氢吡啶-6-胺化合物抑制剂
JP2013531644A (ja) βセクレターゼ（ＢＡＣＥ）の阻害剤として有用な５−アミノ−３，６−ジヒドロ−１Ｈ−ピラジン−２−オン誘導体
TW201300358A (zh) 含氮縮合雜環化合物
CN106211770B (zh) 作为γ‑分泌酶调节剂的色烯和1,1A,2,7B‑四氢环丙烷并[c]色烯吡啶并吡嗪二酮
CN107148409B (zh) 经取代的二环化合物
SG186408A1 (en) 3-amino-5, 6-dihydro-1h-pyrazin-2-one derivatives useful for the treatment of alzheimer's disease and other forms of dementia
JP2017519836A (ja) シクロヘキセン−１−イル−ピリジン−２−イル−１ｈ−ピラゾール−４−カルボン酸誘導体、および可溶性グアニル酸シクラーゼ活性化剤としてのその使用
JP2023521237A (ja) 抗ウイルス１，３－ジ－オキソ－インデン化合物
CN108026069A (zh) 2,3,4,5-四氢吡啶-6-胺衍生物
CN117062804A (zh) 1,3-取代的环丁基衍生物及其用途
EP4065228A1 (en) 1,2,4-oxadiazole derivatives as liver x receptor agonists
CN111566091A (zh) 用于治疗疼痛和疼痛相关病症的新的烷氧基氨基衍生物
HK40126954A (zh) 募集cereblon的bcl-xl/bcl-2双重降解剂
KR20250030474A (ko) 화합물, 조성물 및 이의 사용 방법
HK40085749A (en) P2x3 modulators
HK1193601B (en) Cyclohexyl-4h,6h-5-oxa-2,3,10b-triaza-benzo[e]azulenes as v1a antagonists

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1254800

Country of ref document: HK

WD01 Invention patent application deemed withdrawn after publication
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20180511

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1254800

Country of ref document: HK