KR890012961A - N-(저급알킬)-2-(3'-우레이도벤질)피롤리딘 - Google Patents

N-(저급알킬)-2-(3'-우레이도벤질)피롤리딘 Download PDF

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Publication number
KR890012961A
KR890012961A KR1019890001859A KR890001859A KR890012961A KR 890012961 A KR890012961 A KR 890012961A KR 1019890001859 A KR1019890001859 A KR 1019890001859A KR 890001859 A KR890001859 A KR 890001859A KR 890012961 A KR890012961 A KR 890012961A
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KR
South Korea
Prior art keywords
compound
formula
propyl
lower alkyl
pyrrolidine
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KR1019890001859A
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English (en)
Inventor
엠. 마쵸우스키 조셉
디. 클라크 로빈
데비드 워터베리 엘.
Original Assignee
헤르뷕 본 모르제
신텍스(유.에스.에이.) 인코포레이티드
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Application filed by 헤르뷕 본 모르제, 신텍스(유.에스.에이.) 인코포레이티드 filed Critical 헤르뷕 본 모르제
Publication of KR890012961A publication Critical patent/KR890012961A/ko

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/06—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with radicals, containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/33—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/335—Radicals substituted by nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical

Abstract

내용 없음.

Description

N-(저급알킬)-2-(3'-우레이도벤질)피롤리딘
본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음

Claims (17)

  1. 하기 일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염, 또는 이들의 단일 이성체 또는이성체들의 혼합물:
    상기식에서, R1은 저급 알킬이고; R2는 저급알킬 또는 수소이다.
  2. 제1항에 있어서, R1이 탄소수 1내지 4의 저급알킬인 화합물.
  3. 제2항에 있어서, R2가 수소이거나 탄소수 1내지 3의 저급알킬인 화합물.
  4. 제3항에 있어서, 저급알킬이 직쇄 저급알킬인 화합물.
  5. 제4항에 있어서, R1이 메틸이고 R2가 수소인 화합물.
  6. 제4항에 있어서, R1이 에틸이고 R2가 수소인 화합물.
  7. 제4항에 있어서, R1이 프로필인 화합물.
  8. 제7항에 있어서, R2가 수소인 화합물, 즉(±)-1-프로필-2-(3'-우레이도벤질)피롤리딘; (2R)-1-프로필-2-(3'-우레이도벤질)피롤리딘; (2S)-1-프로필-2-(3'-우레이도벤질)피롤리딘; 또는 이들의 약제학적으로 허용되는 염, 특히 염산염.
  9. 제7항에 있어서, R2가 메틸, 바람직하게는 에틸, 더욱 바람직하게는 프로필인 화합물.
  10. 제4항에 있어서, R1이 부틸인 화합물.
  11. 제10항에 있어서, R2가 수소, 바람직하게는 메틸, 더욱 바람직하게는 에틸, 가장 바람직하게는 프로필인 화합물.
  12. 안과학적으로 허용되는 무독성 부형제 및 치료효과량의 제1항의 화합물을 포함하는, 안과용 약학 조성물.
  13. 제12항에 있어서, 제1항의 화합물이 1-프로필-2-(3'-우레이도벤질)피롤리딘 또는 그의 약제학적으로 허용되는 염, 또는 이들의 단일이성체 또는 이성체들의 혼합물인, 안과용 약학 조성물.
  14. 녹내장이 생긴 포유동물에게 치료효과량의 제1항의 화합물을 투여하는 것을 포함하는, 상기 포유동물의 녹내장 치료방법.
  15. (a) 일반식(12)의 화합물을 수소 공여체와 접촉시키거나; (b) 일반식(13)의 화합물을 시안산 또는 이의 유도체와 접촉시키거나; (c) 일반식(14)의 화합물을 환원제와 접촉시키거나; (d) 일반식(26)의 화합물을 암모니아와 접촉시키거나; (e) 수득된 일반식(Ⅰ)의 화합물을 그의 염으로 전환시키거나; (f) 일반식(Ⅰ)의 화합물의 염을 일반식(Ⅰ) 화합물의 유리 염기로 전환시키거나; (g) 일반식(Ⅰ)의 화합물의 염을 일반식(Ⅰ) 화합물의 다른 염으로 전환시키는 것을 포함하여; 일반식(Ⅰ)의 화합물 또는 이의 약제학적으로 허용되는 염, 또는 이들의 이성체 또는 이성체들의 혼합물을 제조하는 방법:
    상기식에서, R1은 저급알킬이고, R2는 수소 또는 저급알킬이다.
  16. 제15항에 있어서, (±)-1-프로필-2-(3'-우레이도벤질)피롤리딘; (2R)-1-프로필-2-(3'-우레도벤질)피롤리딘; (2S)-1-프로필-2-(3'-우레이도벤질)피롤리딘; 또는 이들의 약제학적으로 허용되는 염, 특히 염산염을 제조하는 방법.
  17. 제1항내지 11항중의 어느 한 항에 따른 화합물의 녹내장 치료용 약물의 제조에 있어서의 용도.
    ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
KR1019890001859A 1988-02-19 1989-02-17 N-(저급알킬)-2-(3'-우레이도벤질)피롤리딘 KR890012961A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/158,197 US4826869A (en) 1988-02-19 1988-02-19 N-(lower alkyl)-2-(3'ureidobenzyl)pyrrolidines
US158197 1988-02-19

Publications (1)

Publication Number Publication Date
KR890012961A true KR890012961A (ko) 1989-09-20

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019890001859A KR890012961A (ko) 1988-02-19 1989-02-17 N-(저급알킬)-2-(3'-우레이도벤질)피롤리딘

Country Status (7)

Country Link
US (1) US4826869A (ko)
EP (1) EP0329169A1 (ko)
JP (1) JPH01268674A (ko)
KR (1) KR890012961A (ko)
AU (1) AU3005589A (ko)
DK (1) DK75489A (ko)
ZA (1) ZA891257B (ko)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5629345A (en) * 1993-07-23 1997-05-13 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
US5965620A (en) * 1993-07-23 1999-10-12 Vide Pharmaceuticals Methods and compositions for ATP-sensitive K+ channel inhibition for lowering intraocular pressure
JP5524209B2 (ja) 2008-08-15 2014-06-18 エヌサーティー・ファーマシューティカルズ・インコーポレーテッド Ｓ−ニトロソグルタチオンレダクターゼのピロール阻害剤
WO2010019905A1 (en) * 2008-08-15 2010-02-18 N30 Pharmaceuticals, Llc Novel pyrrole inhibitors of s-nitrosoglutathione reductase as therapeutic agents
HUE031580T2 (en) 2008-08-15 2017-07-28 Nivalis Therapeutics Inc New pyrrole inhibitors of S-nitrosoglutathion reductase as therapeutic agents

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
LU75478A1 (ko) * 1976-07-28 1978-02-08
FR2460929A1 (fr) * 1979-07-06 1981-01-30 Roussel Uclaf Nouveaux derives de l'a-phenyl 2-pyrrolidinemethanol et leur sels, procede de preparation, application a titre de medicaments et compositions les renfermant
GR72841B (ko) * 1979-12-05 1983-12-07 Carlsson Arvid Emil
US4342692A (en) * 1980-10-20 1982-08-03 Usv Pharmaceutical Corporation Pyrrolidines
US4454151A (en) * 1982-03-22 1984-06-12 Syntex (U.S.A.) Inc. Use of pyrrolo pyrroles in treatment of ophthalmic diseases
US4558066A (en) * 1984-05-17 1985-12-10 Syntex (U.S.A.) Inc. Treatment and prevention of ocular hypertension
US4629730A (en) * 1985-04-11 1986-12-16 Syntex (U.S.A.) Inc. Method for treating intraocular hypertension
DK514585A (da) * 1984-11-08 1986-05-09 Syntex Inc Aminoethylanilinderivater
US4642378A (en) * 1985-04-11 1987-02-10 Syntex (U.S.A.) Inc. Arylalkyl amines useful for lowering intraocular pressure

Also Published As

Publication number Publication date
EP0329169A1 (en) 1989-08-23
DK75489D0 (da) 1989-02-17
JPH01268674A (ja) 1989-10-26
ZA891257B (en) 1990-10-31
US4826869A (en) 1989-05-02
AU3005589A (en) 1989-08-24
DK75489A (da) 1989-08-20

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