KR950704322A - Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders - Google Patents

Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders

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Publication number
KR950704322A
KR950704322A KR1019950702268A KR19950702268A KR950704322A KR 950704322 A KR950704322 A KR 950704322A KR 1019950702268 A KR1019950702268 A KR 1019950702268A KR 19950702268 A KR19950702268 A KR 19950702268A KR 950704322 A KR950704322 A KR 950704322A
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KR
South Korea
Prior art keywords
alkyl
compound
formula
pharmaceutically acceptable
optionally substituted
Prior art date
Application number
KR1019950702268A
Other languages
Korean (ko)
Inventor
알렉산더 코버
제임스 3세 로크
죠지 뮬렌
에드윈 쉔-쵸우 우
Original Assignee
로버트 고든 맥레어 라이트
피존스 코포레이션
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
Priority claimed from GB929225498A external-priority patent/GB9225498D0/en
Priority claimed from GB929225497A external-priority patent/GB9225497D0/en
Priority claimed from GB939316531A external-priority patent/GB9316531D0/en
Application filed by 로버트 고든 맥레어 라이트, 피존스 코포레이션 filed Critical 로버트 고든 맥레어 라이트
Publication of KR950704322A publication Critical patent/KR950704322A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61P25/28—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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Veterinary Medicine (AREA)
  • Neurology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

하기 일반식(I)의 화합물 및 제약상 허용되는 그의 염은 신셩변성 질환의 치료에 유용하다.The compounds of formula (I) below and pharmaceutically acceptable salts thereof are useful for the treatment of degenerative diseases.

상기 식 중, 고리 A는 하기 일반식(AI) 또는 (AII)(여기서, 스피로 원자는 ＊로 나타냄)의 고리이고,In said formula, ring A is a ring of the following general formula (AI) or (AII) (wherein a spiro atom is represented by *),

R1은 H 또는 알킬 C1-6이고, R2는 -(CH2)n-OR3,-(CH2)m-C(O)R4, 플루오로알킬 C1-6, 시아코알킬 C1-6또는 임의로 불포화된 4내지 7원 헤테로시클릭 고기로 치환된 알킬 C1-6이고, R3은 H, 알킬 C1-6(임의로 알콕시 C1-6으로 치환됨), 시클로알킬 C4-7, 임의로 불포화된 4 내지 7원 헤테로시클릭 고리, 페닐(임의로 할로겐, 히드록시 또는 알킬 C1-6으로 치환됨) 또는 벤질 (임으로 할로겐, 히드록시 또는 알킬 C1-6으로 치환됨)이고, R4는 OR5, NR6R7, N(OR6)R7또는 알킬 C1-6이고, R5는 H, 알케닐 C2-6, 알키닐 C2-6또는 알킬 C1-6(임의로 페닐로 치환됨)이고, R6및 R7은 독립적으로 H 또는 알킬 C1-6을 나타내고, R6은 H 또는 알킬 C1-6이고, n은 2 내지 5이고, m은 1 내지 3이고, p는 1 또는 2 이다.R 1 is H or alkyl C 1-6 , R 2 is — (CH 2 ) n -OR 3 ,-(CH 2 ) m -C (O) R 4 , fluoroalkyl C 1-6 , cyaalkyl Alkyl C 1-6 substituted with C 1-6 or optionally unsaturated 4-7 membered heterocyclic meat, R 3 is H, alkyl C 1-6 (optionally substituted with alkoxy C 1-6 ), cycloalkyl C 4-7 , an optionally unsaturated 4-7 membered heterocyclic ring, phenyl (optionally substituted with halogen, hydroxy or alkyl C 1-6 ) or benzyl (optionally substituted with halogen, hydroxy or alkyl C 1-6 R 4 is OR 5 , NR 6 R 7 , N (OR 6 ) R 7 or alkyl C 1-6 , R 5 is H, alkenyl C 2-6 , alkynyl C 2-6 or alkyl C 1-6 (optionally substituted with phenyl), R 6 and R 7 independently represent H or alkyl C 1-6 , R 6 is H or alkyl C 1-6 , n is 2 to 5, m is 1 to 3 and p is 1 or 2.

Description

스피로푸라논 유도체 및 그의 신경변성 질환 치료 용도(Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders)Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (12)

하기 일반식(I)의 화합물 및 제약상 허용되는 그의 염.Compounds of formula (I) and pharmaceutically acceptable salts thereof. 상기 식 중, 고리 A는 하기 일반식(AI) 또는 (AII)(여기서, 스피로 원자는 ＊로 나타냄)의 고리이고,In said formula, ring A is a ring of the following general formula (AI) or (AII) (wherein a spiro atom is represented by *), R1은 H 또는 알킬 C1-6이고, R2는 -(CH2)n-OR3,-(CH2)m-C(O)R4, 플루오로알킬 C1-6, 시아코알킬 C1-6또는 임의로 불포화된 4내지 7원 헤테로시클릭 고기로 치환된 알킬 C1-6이고, R3은 H, 알킬 C1-6(임의로 알콕시 C1-6으로 치환됨), 시클로알킬 C4-7, 임의로 불포화된 4 내지 7원 헤테로시클릭 고리, 페닐(임의로 할로겐, 히드록시 또는 알킬 C1-6으로 치환됨) 또는 벤질 (임으로 할로겐, 히드록시 또는 알킬 C1-6으로 치환됨)이고, R4는 OR5, NR6R7, N(OR6)R7또는 알킬 C1-6이고, R5는 H, 알케닐 C2-6, 알키닐 C2-6또는 알킬 C1-6(임의로 페닐로 치환됨)이고, R6및 R7은 독립적으로 H 또는 알킬 C1-6을 나타내고, R6은 H 또는 알킬 C1-6이고, n은 2 내지 5이고, m은 1 내지 3이고, p는 1 또는 2 이다.R 1 is H or alkyl C 1-6 , R 2 is — (CH 2 ) n -OR 3 ,-(CH 2 ) m -C (O) R 4 , fluoroalkyl C 1-6 , cyaalkyl Alkyl C 1-6 substituted with C 1-6 or optionally unsaturated 4-7 membered heterocyclic meat, R 3 is H, alkyl C 1-6 (optionally substituted with alkoxy C 1-6 ), cycloalkyl C 4-7 , an optionally unsaturated 4-7 membered heterocyclic ring, phenyl (optionally substituted with halogen, hydroxy or alkyl C 1-6 ) or benzyl (optionally substituted with halogen, hydroxy or alkyl C 1-6 R 4 is OR 5 , NR 6 R 7 , N (OR 6 ) R 7 or alkyl C 1-6 , R 5 is H, alkenyl C 2-6 , alkynyl C 2-6 or alkyl C 1-6 (optionally substituted with phenyl), R 6 and R 7 independently represent H or alkyl C 1-6 , R 6 is H or alkyl C 1-6 , n is 2 to 5, m is 1 to 3 and p is 1 or 2. 제1항에 있어서, R1이 메틸인 화합물.The compound of claim 1, wherein R 1 is methyl. 제1 또는 2항에 있어서, R2가 -(CH2)n-OR3 또는 -(CH2)m-C(O)R4인 화합물.The compound of claim 1 or 2, wherein R2Is-(CH2)n-OR3 Or-(CH2)m-C (O) R4Phosphorus compounds. 제1 내지 3항 중 어느 한항에 있어서, R3이 알킬 C1-6(임의로 알콕시 C1-6으로 치환됨)인 화합물.The compound of any one of claims 1-3, wherein R 3 is alkyl C 1-6 (optionally substituted with alkoxy C 1-6 ). 제1 내지 4항 중 어느 한항에 있어서, R4가 O-(알킬 C1-6) 또는 N(알킬 C1-6)인 화합물.The compound of any one of claims 1-4, wherein R 4 is O- (alkyl C 1-6 ) or N (alkyl C 1-6 ). 제1 내지 5항 중 어느 한항에 있어서, R8이 메틸인 화합물.The compound of any one of claims 1-5, wherein R 8 is methyl. 제1 내지 6항 중 어느 한항에 있어서, 고리 A가 일반식(AI)의 고리인 화합물.The compound of any one of claims 1-6, wherein ring A is a ring of formula (AI). 약제로 사옹하기 위한 제1항 기재의 일반식(I)의 화합물 또는 제약상 허용되는 그의 염.A compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 for use as a medicament. 제1항 기재의 일반식(I)의 화합물 또는 제약상 허용되는 그의 염과 제약상 허용되는 보조제, 희석제 또는 담체의 혼합물을 포함하는 제약 조성물.A pharmaceutical composition comprising a mixture of a compound of formula (I) or a pharmaceutically acceptable salt thereof as described in claim 1 with a pharmaceutically acceptable adjuvant, diluent or carrier. 신경변성 질환 치료용 의약의 제조에 사용하기 위한 제1항 기재의 일반식(I)의 화합물 또는 제약상 허용되는 그의 염.A compound of formula (I) according to claim 1, or a pharmaceutically acceptable salt thereof, for use in the manufacture of a medicament for the treatment of neurodegenerative diseases. 신경변성 질환을 앓는 환자에게 치료 유효량의 제1항 기재의 일반식(I)의 화합물 또는 제약상 허용되는 그의 염을 투여하는 것을 포함하는 신경변성 질환의 치료 방법.A method of treating neurodegenerative disease comprising administering to a patient suffering from a neurodegenerative disease a therapeutically effective amount of a compound of formula (I) as described in claim 1 or a pharmaceutically acceptable salt thereof. (a) 하기 일반식(II)의 화합물을 하기 일반식(III)의 화합물과 반응시키거나, 또는 (b) 하기 일반식(V)의 화합물을 염기 존재하게 하기 일반식(VI)의 화합물과 반응시키고, 경우에 따라 생성된 화합물을 제약상 허용되는 염으로 전환시키는 것을 포함하는 제1항 기재의 일반식(I)의 화합물 또는 제약상 허용되는 그의 염의 제조 방법.(a) reacting a compound of the general formula (II) with a compound of the general formula (III), or (b) a compound of the general formula (V) A process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof according to claim 1 comprising reacting and optionally converting the resulting compound into a pharmaceutically acceptable salt. 상기 식 중, A, R1및 R2는 제1항에서 정의한 바와 같고, X는 이탈기이다.In the above formula, A, R 1 and R 2 are as defined in claim 1, and X is a leaving group. ※ 참고사항:최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019950702268A 1992-12-05 1993-12-06 Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders KR950704322A (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
GB9225498.6 1992-12-05
GB929225498A GB9225498D0 (en) 1992-12-05 1992-12-05 Pharmacologically active compounds
GB929225497A GB9225497D0 (en) 1992-12-05 1992-12-05 Pharmacologically active compounds
GB9225497.8 1992-12-05
GB9316531.4 1993-08-10
GB939316531A GB9316531D0 (en) 1993-08-10 1993-08-10 Pharmacologically active compounds
PCT/GB1993/002500 WO1994013678A1 (en) 1992-12-05 1993-12-06 Spirofuranone derivatives and their use in the treatment of neurodegenerative disorders

Publications (1)

Publication Number Publication Date
KR950704322A true KR950704322A (en) 1995-11-17

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ID=27266497

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019950702268A KR950704322A (en) 1992-12-05 1993-12-06 Spirofuranone Derivatives and Their Use in the Treatment of Neurodegenerative Disorders

Country Status (10)

Country Link
EP (1) EP0672046A1 (en)
JP (1) JPH08503955A (en)
KR (1) KR950704322A (en)
AU (1) AU5655394A (en)
CA (1) CA2150947A1 (en)
FI (1) FI952733A0 (en)
IL (1) IL107881A0 (en)
MX (1) MX9307679A (en)
NO (1) NO952194L (en)
WO (1) WO1994013678A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2270884A1 (en) * 1997-01-27 1998-07-30 Haile Tecle Single pot process for producing (z)-azabicyclo oxime ethers
TWI243173B (en) 1999-11-17 2005-11-11 Akzo Nobel Nv Spiro[2H-1-benzopyran-2,4'-piperidine] derivatives
KR100783836B1 (en) 2004-01-08 2007-12-10 에프. 호프만-라 로슈 아게 Diaza-spiropiperidine derivatives as inhibitors of glycine transporter 1 and glycine transporter 2

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5075317A (en) * 1989-06-21 1991-12-24 Fisons Corporation Spirofurane derivatives
JPH03153690A (en) * 1989-11-10 1991-07-01 Yamanouchi Pharmaceut Co Ltd Heterocyclic spiro derivative and production thereof
IE914238A1 (en) * 1990-12-19 1992-07-01 Fisons Corp Novel spirofurane derivatives

Also Published As

Publication number Publication date
FI952733A (en) 1995-06-05
FI952733A0 (en) 1995-06-05
IL107881A0 (en) 1994-04-12
EP0672046A1 (en) 1995-09-20
JPH08503955A (en) 1996-04-30
CA2150947A1 (en) 1994-06-23
AU5655394A (en) 1994-07-04
NO952194D0 (en) 1995-06-02
MX9307679A (en) 1994-06-30
NO952194L (en) 1995-06-02
WO1994013678A1 (en) 1994-06-23

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