FI87456B - Foerfarande foer framstaellning av terapeutiskt anvaendbara pyrrolidinfoereningar. - Google Patents

Foerfarande foer framstaellning av terapeutiskt anvaendbara pyrrolidinfoereningar. Download PDF

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Publication number
FI87456B
FI87456B FI881612A FI881612A FI87456B FI 87456 B FI87456 B FI 87456B FI 881612 A FI881612 A FI 881612A FI 881612 A FI881612 A FI 881612A FI 87456 B FI87456 B FI 87456B
Authority
FI
Finland
Prior art keywords
formula
alkyl
phenyl
compound
nitrogen atom
Prior art date
Application number
FI881612A
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English (en)
Finnish (fi)
Other versions
FI87456C (sv
FI881612A (fi
FI881612A0 (fi
Inventor
Hansjoerg Urbach
Rainer Henning
Franz Hock
Original Assignee
Hoechst Ag
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Publication date
Application filed by Hoechst Ag filed Critical Hoechst Ag
Publication of FI881612A0 publication Critical patent/FI881612A0/fi
Publication of FI881612A publication Critical patent/FI881612A/fi
Application granted granted Critical
Publication of FI87456B publication Critical patent/FI87456B/fi
Publication of FI87456C publication Critical patent/FI87456C/sv

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Classifications

    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D207/10—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 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • C07D401/14—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 three or more hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (4)

1. Förfarande för framställning av terapeutiskt användbara pyrrolidinföreningar med formeln I och fysiolo-5 giskt godtagbara salter därav CH-O-C-N-CH-C-N (I)
0 I 0 10 kk ?° H6 cf2-corö där R1 betecknar (C6-C12)-aryl, R6 betecknar (C^-CjJ-alkoxi eller en rest med formeln 15 -NR7R8, där R7 och R® är lika eller olika och betecknar väte, fenyl-(Cx—C4)-alkyl, 2-, 3- eller 4-pyrldyl-(C1-C4)-alkyl, amino-(Ci-C4)-alkyl, (Ci-Cji-alkylamino-fC^Ce)-alkyl eller di-(C1-C2)-alkylamino-(C1-C4)-alkyl, eller R7 och R® bildar 20 tillsammans med kväveatomen, tili vilken de är bundna, en 5-9-ledad heterocyklisk ring, vilken som ringatomer inne-häller 3-8 kolatomer och eventuellt ytterligare en syre-eller kväveatom och vilken eventuellt som substituent in-nehäller en rest ur serlen (C^-C^)-alkyl, fenyl, fenyl-25 (Cj-C*)-alkyl, varvid fenyldelen i fenylen och fenylalkylen kan som substituenter innehälla en, tvä eller tre likadana eller olika rester ur serien metyl, etyl och metoxi, kännetecknat därav, att en förening med formeln IV oxideras, 30 R \ O CHOH \ • 35 CF2-COR6 17 87456 där symbolerna R1 och R6 har samma betydelser som ovan, den sä erhällna föreningen omvandlas eventuellt tili ett fy-siologiskt godtagbart sait.
2. Förfarande enligt patentkravet 1, k ä n n e -5 tecknat därav, att man framställer en förening med formeln I, där R1 betecknar fenyl, R6 betecknar metoxi el-ler en rest med formeln -NR7R8, där R7 och R8 är olika och betecknar väte, fenyl-(Cj-C4)-alkyl, 2-pyridylmetyl eller dimetylaminopropyl, eller R7 och R8 betecknar tillsammans 10 med kväveatomen, tili vilken de är bundna, pyrrolidino, morfolino eller piperazino, varvid piperazinet är substi-tuerat med en tili den andra kväveatomen bunden metyl-eller 3,4,5-trimetoxifenyletylgrupp, eller ett fysiolo-giskt godtagbart sait därav. 15 3. Förfarande enligt patentkravet 1 eller 2, k ä n- netecknat därav, att man framställer [3-N-(ben-syloxikarbonyl-S-propyl)-pyrrolidin-2-S-yl]-3-OXO-2,2-di-. fluorpropionsyra-N-bensylamid.
4. Förfarande enligt patentkravet 1 eller 2, k ä n-20 netecknat därav, att man framställer en förening med formeln . 25 \ f CH'C6H5 : : 30 C6H5-CH2-0'^Vs 0
FI881612A 1987-04-11 1988-04-07 Förfarande för framställning av terapeutiskt användbara pyrrolidinföre ningar FI87456C (sv)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19873712364 DE3712364A1 (de) 1987-04-11 1987-04-11 Neue pyrrolidin-2-(1,3-dicarbonyl)-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung
DE3712364 1987-04-11

Publications (4)

Publication Number Publication Date
FI881612A0 FI881612A0 (fi) 1988-04-07
FI881612A FI881612A (fi) 1988-10-12
FI87456B true FI87456B (fi) 1992-09-30
FI87456C FI87456C (sv) 1993-01-11

Family

ID=6325456

Family Applications (1)

Application Number Title Priority Date Filing Date
FI881612A FI87456C (sv) 1987-04-11 1988-04-07 Förfarande för framställning av terapeutiskt användbara pyrrolidinföre ningar

Country Status (15)

Country Link
US (1) US4912128A (sv)
EP (1) EP0286927A3 (sv)
JP (1) JPS63258852A (sv)
KR (1) KR880012542A (sv)
AU (1) AU607987B2 (sv)
DE (1) DE3712364A1 (sv)
DK (1) DK191988A (sv)
FI (1) FI87456C (sv)
HU (1) HU199785B (sv)
IL (1) IL86028A (sv)
NO (1) NO881545L (sv)
NZ (1) NZ224181A (sv)
PH (1) PH26048A (sv)
PT (1) PT87194B (sv)
ZA (1) ZA882460B (sv)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3712365A1 (de) * 1987-04-11 1988-10-27 Hoechst Ag Neue 2-acylpyrrolidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung
DE3742431A1 (de) * 1987-12-15 1989-07-13 Hoechst Ag Neue derivate cyclischer aminosaeuren, verfahren zu ihrer herstellung, sie enthaltende mittel und deren verwendung
US5053414A (en) * 1988-04-08 1991-10-01 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
US5212191A (en) * 1988-04-08 1993-05-18 Ono Pharmaceutical Co., Ltd. Heterocyclic compounds
AU643300B2 (en) * 1990-06-07 1993-11-11 Zeria Pharmaceutical Co., Ltd. Novel arylalkanoylamine derivative and drug containing the same
JPH05186498A (ja) * 1991-12-27 1993-07-27 Japan Tobacco Inc プロリン誘導体
US5506256A (en) * 1990-07-27 1996-04-09 Yoshitomi Pharmaceutical Industries, Ltd. Proline derivatives possessing prolyl endopeptidase-inhibitory activity
DE4029054A1 (de) * 1990-09-13 1992-03-19 Bayer Ag N-acylpyrrolidin-derivate
US5254696A (en) * 1990-09-13 1993-10-19 Bayer Aktiengesellschaft N-acylpyrrolidine derivatives
JP3810097B2 (ja) * 1993-01-15 2006-08-16 明治製菓株式会社 ピロリジン−２−イルカルボニル複素環式化合物誘導体
US6218424B1 (en) * 1996-09-25 2001-04-17 Gpi Nil Holdings, Inc. Heterocyclic ketone and thioester compounds and uses

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1492640A (en) * 1975-07-08 1977-11-23 Ucb Sa L-pyroglutamyl-l-prolinamide
US4560795A (en) * 1979-04-10 1985-12-24 Merrell Dow France et Cie. α-Halomethyl derivatives of α-amino acids
US4499102A (en) * 1979-12-13 1985-02-12 Santen Pharmaceutical Co., Ltd. Thiazolidine and pyrrolidine compounds and pharmaceutical compositions containing them
US4277395A (en) * 1980-06-16 1981-07-07 Richardson-Merrell Inc. Novel enzyme inhibitors
GB2083030B (en) * 1980-08-23 1984-03-07 Merrell Toraude & Co Fluorinated pentene diamine derivatives
US4456594A (en) * 1981-11-06 1984-06-26 Smithkline Beckman Corporation N-Carboxyalkylproline-containing tripeptides
US4483991A (en) * 1983-01-17 1984-11-20 American Home Products Corporation Hypotensive agents
US4518528A (en) * 1983-05-19 1985-05-21 Rasnick David W α Amino fluoro ketones
JPS6137764A (ja) * 1984-07-31 1986-02-22 Suntory Ltd 抗プロリルエンドペプチダ−ゼ活性を有する新規生理活性化合物
JPH0655758B2 (ja) * 1984-08-24 1994-07-27 味の素株式会社 アミノ酸誘導体
US4626545A (en) * 1984-08-27 1986-12-02 Merck & Co., Inc. Amino acid derivatives as enzyme inhibitors
US4762821A (en) * 1985-03-22 1988-08-09 Syntex (U.S.A.) Inc. N',N"-dialkylguanidino dipeptides
EP0201741B1 (en) * 1985-04-16 1991-07-31 Suntory Limited Dipeptide derivatives, processes for preparing them, pharmaceutical composition and use
JPH0623190B2 (ja) * 1985-04-16 1994-03-30 サントリー株式会社 インヒビタ−活性を有するｎ−アシルピロリジン誘導体及びその製法並びに用途
JPH0653757B2 (ja) * 1985-12-06 1994-07-20 味の素株式会社 プロリン誘導体の芳香族スルホン酸塩
JPH08806B2 (ja) * 1986-11-18 1996-01-10 サントリー株式会社 プロリルエンドペプチダ−ゼ阻害作用を有する新規ピロリジンアミド誘導体
DE3712363A1 (de) * 1987-04-11 1988-10-27 Hoechst Ag Neue pyrrolidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung
DE3712365A1 (de) * 1987-04-11 1988-10-27 Hoechst Ag Neue 2-acylpyrrolidin-derivate, verfahren zu ihrer herstellung, sie enthaltende mittel sowie deren verwendung

Also Published As

Publication number Publication date
IL86028A (en) 1993-03-15
DK191988A (da) 1988-10-12
IL86028A0 (en) 1988-09-30
FI87456C (sv) 1993-01-11
ZA882460B (en) 1988-09-29
PT87194A (pt) 1988-05-01
KR880012542A (ko) 1988-11-28
JPS63258852A (ja) 1988-10-26
DE3712364A1 (de) 1988-10-27
FI881612A (fi) 1988-10-12
EP0286927A2 (de) 1988-10-19
PT87194B (pt) 1992-07-31
AU1446588A (en) 1988-10-13
DK191988D0 (da) 1988-04-08
FI881612A0 (fi) 1988-04-07
EP0286927A3 (de) 1991-05-08
NO881545D0 (no) 1988-04-08
US4912128A (en) 1990-03-27
NZ224181A (en) 1990-07-26
HU199785B (en) 1990-03-28
NO881545L (no) 1988-10-12
AU607987B2 (en) 1991-03-21
HUT46659A (en) 1988-11-28
PH26048A (en) 1992-01-29

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Owner name: HOECHST AKTIENGESELLSCHAFT