RO82508B - PROCEDEU PENTRU PREPARAREA UNOR DERIVATI DE 3-(1-PIPERIDINILACHIL)-4H-PIRIDO-(1,2-a)- PIRIMIDIN-4-ONA - Google Patents

PROCEDEU PENTRU PREPARAREA UNOR DERIVATI DE 3-(1-PIPERIDINILACHIL)-4H-PIRIDO-(1,2-a)- PIRIMIDIN-4-ONA

Info

Publication number
RO82508B
RO82508B RO103848A RO10384881A RO82508B RO 82508 B RO82508 B RO 82508B RO 103848 A RO103848 A RO 103848A RO 10384881 A RO10384881 A RO 10384881A RO 82508 B RO82508 B RO 82508B
Authority
RO
Romania
Prior art keywords
lower alkyl
hydrogen
pyrido
pyrimidin
derivatives
Prior art date
Application number
RO103848A
Other languages
English (en)
Other versions
RO82508A (ro
Inventor
Ludo Edmond Josephine Kennis
Josephus Carolus Mertens
Original Assignee
Janssen Pharmaceutica N.V.
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 N.V. filed Critical Janssen Pharmaceutica N.V.
Publication of RO82508B publication Critical patent/RO82508B/ro
Publication of RO82508A publication Critical patent/RO82508A/ro

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/08Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/34Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/70Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Inventia se refera la un procedeu pentru prepararea unor derivati de 3-(1-piperidinilalchil)-4H-pirido-[1,2-a] pirimidin-4-ona cu formula generala I: (vezi formula) în care R1 si R2 sunt alesi independent unul de altul din grupul constând din hidrogen, alchil inferior, alchiloxi inferior, halogen si trifluormetil, R3 reprezinta hidrogen, alchil inferior si aril, Alc reprezinta un radical de alchilen inferior, R reprezinta un hidrogen, alchil inferior si hidroximetil în pozitia 2,3 sau 4 a inelului piperidinic; x reprezinta una din grupele: (vezi formula) unde R4 este hidrogen sau alchil inferior si q este un numar întreg 2 sau 3, iar Ar reprezinta o grupa aril; fenil, fenil substituit, tienil, furanil si piridinil , grupa fenil substituit, are între 1 si 3 substituenti, fiecare reprezentând halogen alchil inferior, alchiloxi inferior, trifluormetil, nitro, amino si hidroxi.
RO81103848A 1980-03-28 1981-03-28 Procedeu pentru prepararea unor derivati de 3-(1-piperidinilalchil)-4procedeu pentru prepararea unor derivati de 3-(1-piperidinilalchil)-4h-pirido-(1,2,-a)-pirimidin-4-ona RO82508A (ro)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US13484580A 1980-03-28 1980-03-28
US06/191,632 US4342870A (en) 1980-03-28 1980-09-29 Novel 3-(1-piperidinylalkyl)-4H-pyrido[1,2-a]pyrimidin-4-one derivatives

Publications (2)

Publication Number Publication Date
RO82508B true RO82508B (ro) 1983-08-30
RO82508A RO82508A (ro) 1983-09-26

Family

ID=26832744

Family Applications (1)

Application Number Title Priority Date Filing Date
RO81103848A RO82508A (ro) 1980-03-28 1981-03-28 Procedeu pentru prepararea unor derivati de 3-(1-piperidinilalchil)-4procedeu pentru prepararea unor derivati de 3-(1-piperidinilalchil)-4h-pirido-(1,2,-a)-pirimidin-4-ona

Country Status (22)

Country Link
US (1) US4342870A (ro)
EP (1) EP0037265B1 (ro)
AU (1) AU537700B2 (ro)
BG (1) BG36199A3 (ro)
CA (1) CA1163994A (ro)
CS (1) CS256366B2 (ro)
DE (1) DE3168433D1 (ro)
DK (1) DK159390C (ro)
ES (1) ES500814A0 (ro)
FI (1) FI71737C (ro)
GR (1) GR72488B (ro)
HU (1) HU187329B (ro)
IE (1) IE51319B1 (ro)
IL (1) IL62494A (ro)
MA (1) MA19107A1 (ro)
NO (1) NO156752C (ro)
NZ (1) NZ196522A (ro)
PH (1) PH16530A (ro)
PT (1) PT72740B (ro)
RO (1) RO82508A (ro)
SU (1) SU1068037A3 (ro)
YU (1) YU43010B (ro)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
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US4443451A (en) 1981-07-15 1984-04-17 Janssen Pharmaceutica N.V. Bicyclic pyrimidin-5-one derivatives
US4548938A (en) * 1981-07-15 1985-10-22 Janssen Pharmaceutica N.V. 5-H-1,3,4-thiadiazolo[3,2-a]pyrimidin-5-one compounds
US4355037A (en) * 1981-11-12 1982-10-19 Hoechst-Roussel Pharmaceuticals 3-(4-Piperidyl)-1,2-benzisoxales
US4485107A (en) * 1982-11-01 1984-11-27 Janssen Pharmaceutica N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones
US4581171A (en) * 1983-07-27 1986-04-08 Janssen Pharmaceutica, N.V. [[Bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones useful for treating psychotropic disorders
US4695569A (en) * 1983-11-30 1987-09-22 Janssen Pharmaceutica N.V. Bicyclic heterocyclyl containing N-(bicyclic heterocyclyl)-4-piperidinamines
US4888426A (en) * 1983-11-30 1989-12-19 Janssen Pharmaceutica N.V. 1-(5-methyl-furan-2-ylmethyl)-N-(4-piperidinyl)imidazo [4,5-6]pyridine-2-amine
PH23995A (en) * 1984-01-09 1990-02-09 Janssen Pharmaceutica Nv 4((bicycle heterocyclyl)-methyl and hetero)piperidines
US4548939A (en) * 1984-10-01 1985-10-22 Janssen Pharmaceutica N. V. 1H-Indol-3-yl containing 1,3-dimethyl-1H-purine-2,6-diones
US4804663A (en) * 1985-03-27 1989-02-14 Janssen Pharmaceutica N.V. 3-piperidinyl-substituted 1,2-benzisoxazoles and 1,2-benzisothiazoles
EP0268309B1 (en) * 1986-09-22 1996-12-11 Janssen Pharmaceutica N.V. Serotonin antagonists for treating wounds
IL90879A0 (en) * 1988-09-02 1990-02-09 Janssen Pharmaceutica Nv 3-piperidinyl-indazole derivatives,their preparation and antihypertensive compositions containing them
CA2000786C (en) * 1988-11-07 1999-01-26 Cornelus G. M. Janssen 3-piperidinyl-1,2-benzisoxazoles
US5153206A (en) * 1988-12-02 1992-10-06 Pfizer Inc. Arylpiperidine derivatives
WO1990011093A1 (en) * 1989-03-23 1990-10-04 Mallinckrodt, Inc. Radioactive iodine- or bromine labelled piperidine compound as well as method of preparing same and composition comprising said compound
DE4138756A1 (de) * 1991-11-26 1993-05-27 Troponwerke Gmbh & Co Kg Kombination mit neuroprotektiver wirkung
US5266571A (en) * 1992-01-09 1993-11-30 Amer Moh Samir Treatment of hemorrhoids with 5-HT2 antagonists
AU669156B2 (en) * 1992-02-13 1996-05-30 Merrell Dow Pharmaceuticals Inc. Piperidinyl thiacyclic derivatives
JPH07508741A (ja) * 1992-07-13 1995-09-28 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ 新規4−(3−ベンゾフラニル)ピペリジニル及び4−(3−ベンゾチエニル)ピペリジニル誘導体,ならびにそれらを含む製薬学的組成物
ES2236700T3 (es) * 1993-11-19 2005-07-16 Janssen Pharmaceutica N.V. 1,2-benzazoles microencapsulados.
ES2085234B1 (es) * 1994-02-24 1997-01-16 Vita Invest Sa Agente activo sobre el sistema nervioso central, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
TW421649B (en) * 1995-01-31 2001-02-11 Janssen Pharmaceutica Nv 4-(1H-indol-1yl)-1-piperidinyl derivatives
US5753664A (en) * 1995-03-16 1998-05-19 Takeda Chemical Industries, Ltd. Heterocyclic compounds, their production and use
EP1560814A1 (en) * 2002-11-13 2005-08-10 Synthon B.V. Process for making risperidone and intermediates therefor
WO2004094415A1 (en) * 2003-04-22 2004-11-04 Synthon B.V. Risperidone monohydrochloride
DK3106166T3 (da) 2008-02-29 2021-01-11 Vm Therapeutics Llc Forbindelser til behandling af smertesyndrom og andre lidelser
PE20142364A1 (es) 2012-02-10 2015-01-10 Hoffmann La Roche Compuestos para tratar atrofia muscular espinal
KR102099997B1 (ko) 2012-03-01 2020-04-13 피티씨 테라퓨틱스, 인크. 척수성 근위축증을 치료하기 위한 화합물
EA028382B1 (ru) 2012-03-23 2017-11-30 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Соединения для лечения спинальной мышечной атрофии
WO2014143915A1 (en) * 2013-03-15 2014-09-18 Vm Therapeutics Llc Novel crystalline forms
EP3082820B1 (en) 2013-12-19 2022-07-20 PTC Therapeutics, Inc. Methods for modulating the amount of rna transcripts
EP4249472A3 (en) 2015-05-30 2023-12-13 PTC Therapeutics, Inc. Methods for modulating rna splicing
IL281633B (en) 2015-12-10 2022-07-01 Ptc Therapeutics Inc Methods for treating Huntington's disease
EP3544435A4 (en) 2016-11-28 2020-11-04 PTC Therapeutics, Inc. RNA SPLICE MODULATION PROCESSES
EP3634953B1 (en) 2017-06-05 2024-01-03 PTC Therapeutics, Inc. Compounds for treating huntington's disease
CN111372611A (zh) 2017-06-14 2020-07-03 Ptc医疗公司 修饰rna剪接的方法
US11395822B2 (en) 2017-06-28 2022-07-26 Ptc Therapeutics, Inc. Methods for treating Huntington's disease
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US3412094A (en) * 1967-06-21 1968-11-19 Searle & Co 5-alkyl-2-amino-4-azido-6-phenylpyrimidines and congeners
US3960863A (en) * 1974-06-25 1976-06-01 Sankyo Company Limited Pyrido[1,2-a]pyrimidinone derivatives
JPS5146497A (en) * 1974-10-19 1976-04-20 Masato Aiura Hobuban
JPS525795A (en) * 1975-06-28 1977-01-17 Sankyo Co Ltd Preparation of tetrahydro pyridopyrimidinone derivatives
HU173438B (hu) * 1975-11-27 1979-05-28 Chinoin Gyogyszer Es Vegyeszet Sposob poluchenija novykh proizvodnykh 4-okso-1,6,7,8-/tetragidro-4h-pirido/1,2/pirimidina s zaderzhivajuhhejj vozgoranie aktivnot'ju i protivosvertivajuhhem effektom

Also Published As

Publication number Publication date
YU81081A (en) 1983-12-31
EP0037265B1 (en) 1985-01-23
IL62494A0 (en) 1981-05-20
GR72488B (ro) 1983-11-14
BG36199A3 (en) 1984-09-14
NZ196522A (en) 1985-10-11
DK138281A (da) 1981-09-29
IL62494A (en) 1984-08-31
CS256366B2 (en) 1988-04-15
FI71737C (fi) 1987-02-09
AU537700B2 (en) 1984-07-05
MA19107A1 (fr) 1981-10-01
AU6842981A (en) 1981-10-01
FI810956L (fi) 1981-09-29
IE810706L (en) 1981-09-28
NO156752C (no) 1987-11-18
DK159390C (da) 1991-03-04
IE51319B1 (en) 1986-12-10
NO811058L (no) 1981-09-29
EP0037265A1 (en) 1981-10-07
FI71737B (fi) 1986-10-31
DE3168433D1 (de) 1985-03-07
ES8300763A1 (es) 1982-11-01
SU1068037A3 (ru) 1984-01-15
HU187329B (en) 1985-12-28
US4342870A (en) 1982-08-03
PT72740A (en) 1981-04-01
ES500814A0 (es) 1982-11-01
YU43010B (en) 1989-02-28
NO156752B (no) 1987-08-10
PT72740B (en) 1982-11-16
DK159390B (da) 1990-10-08
RO82508A (ro) 1983-09-26
CA1163994A (en) 1984-03-20
PH16530A (en) 1983-11-10

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