PE10997A1 - NUEVOS DERIVADOS DE [3-(4-FENILPIPERACIN-1-i1)PROPILAMINO]-PIRIDINA, PIRIMIDINA Y BENCENO COMO ANTAGONISTAS DE a1-ADRENOCEPTORES, SUS EMPLEOS COMO AGENTES TERAPEUTICOS Y LOS METODOS PARA SU PREPARACION - Google Patents

NUEVOS DERIVADOS DE [3-(4-FENILPIPERACIN-1-i1)PROPILAMINO]-PIRIDINA, PIRIMIDINA Y BENCENO COMO ANTAGONISTAS DE a1-ADRENOCEPTORES, SUS EMPLEOS COMO AGENTES TERAPEUTICOS Y LOS METODOS PARA SU PREPARACION

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Publication number
PE10997A1
PE10997A1 PE1995283893A PE28389395A PE10997A1 PE 10997 A1 PE10997 A1 PE 10997A1 PE 1995283893 A PE1995283893 A PE 1995283893A PE 28389395 A PE28389395 A PE 28389395A PE 10997 A1 PE10997 A1 PE 10997A1
Authority
PE
Peru
Prior art keywords
alkyl
pirimidine
substitute
formula
phenylpiperacin
Prior art date
Application number
PE1995283893A
Other languages
English (en)
Inventor
Jurg Roland Pfister
Jr David John Morgans
David Bruce Repke
Eric Brian Sjogren
David Ernest Clarke
Helen Yen-Hui Wu
Todd Richard Elworthy
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of PE10997A1 publication Critical patent/PE10997A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/74Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/02Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84Nitriles
    • C07D213/85Nitriles in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/89Heterocyclic 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 with hetero atoms directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS ANTAGONISTAS DE O1-ADRENOCEPTORES DE FORMULA (I), DONDE: p=0,1; t=0,1,2; X=O,S,NR6; R6=H,(C1-6)ALQUILO; Y,Z=INDEPENDIENTEMENTE CH,N; R1=H,(C1-4)ALQUILTIO,(C1-6)ALQUILO,OXAZOL-2-ILO,(C3-6)CICLOALQUILO, ENTRE OTROS; R2=H,OH,HALO,(C1-6)ALQUILO,ENTRE OTROS, EN DONDE EL ALQUILO ESTA OPCIONALMENTE SUSTITUIDO POR 1,2 O 3 HALOGENOS; R3=C(0)R7; R7=DI(C1-4)ALQUILAMINO, N-(C1-4)ALQUIL-N-(C1-4)ALQUILOXIAMINO,ENTRE OTROS; R4=H,OH,CN,ENTRE OTROS; R5=(C1-6)ALQUILO; ADEMAS DE SUS N-OXIDOS Y SALES FARMACEUTICAMENTE ACEPTABLES. TAMBIEN SE REFIERE AL PROCEDIMIENTO DE OBTENCION DE UN COMPUESTO DE FORMULA (I), QUE COMPRENDE: (A) UNA REACCION PARA LA FORMACION DE UN COMPUESTO DE FORMULA (I) QUE OCURRE EN EL SUSTITUYENTE X, ENTRE L Y -OH,-SH,-NHR6 DONDE L=GRUPO PARTIENTE Y SI Y,Z=N, L ES SUSTITUYENTE DE LA PIRIMIDINA Y SI Y,Z=CH, L ES SUSTITUYENTE DEL PROPILPIPERACINFENILO; (B) SI Y,Z=CH, X=-0H,-SH,-NHR6 QUE REACCIONA CON 3-BR-1-PROPANOL, AL QUE SE LE SUSTITUYE CON UN GRUPO PARTIENTE QUE LUEGO SE HACE REACCIONAR CON EL NITROGENO DEL PIPERACINFENILO R1,R2 SUSTITUIDO; (C) TAMBIEN REACCIONES OPCIONALES DE HALOGENACION, DEMETILACION, ENTRE OTRAS. ES USADO EN EL TRATAMIENTO DE LA OBSTRUCCION DEL TRACTO URINARIO INFERIOR CAUSADO POR HIPERPLASIA PROSTATICA BENIGNA
PE1995283893A 1994-11-08 1995-11-06 NUEVOS DERIVADOS DE [3-(4-FENILPIPERACIN-1-i1)PROPILAMINO]-PIRIDINA, PIRIMIDINA Y BENCENO COMO ANTAGONISTAS DE a1-ADRENOCEPTORES, SUS EMPLEOS COMO AGENTES TERAPEUTICOS Y LOS METODOS PARA SU PREPARACION PE10997A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US08/336,368 US5688795A (en) 1994-11-08 1994-11-08 3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine, pyrimidine and benzene derivatives as α1 -adrenoceptor antagonists

Publications (1)

Publication Number Publication Date
PE10997A1 true PE10997A1 (es) 1997-04-26

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ID=23315765

Family Applications (1)

Application Number Title Priority Date Filing Date
PE1995283893A PE10997A1 (es) 1994-11-08 1995-11-06 NUEVOS DERIVADOS DE [3-(4-FENILPIPERACIN-1-i1)PROPILAMINO]-PIRIDINA, PIRIMIDINA Y BENCENO COMO ANTAGONISTAS DE a1-ADRENOCEPTORES, SUS EMPLEOS COMO AGENTES TERAPEUTICOS Y LOS METODOS PARA SU PREPARACION

Country Status (22)

Country Link
US (1) US5688795A (es)
EP (1) EP0711757A1 (es)
JP (1) JPH08208614A (es)
KR (1) KR960017658A (es)
CN (1) CN1136039A (es)
AR (1) AR002244A1 (es)
AU (1) AU3459995A (es)
BR (1) BR9505107A (es)
CA (1) CA2162089A1 (es)
CO (1) CO4520230A1 (es)
CZ (1) CZ291095A3 (es)
FI (1) FI955376A (es)
HU (1) HUT73843A (es)
IL (1) IL115844A0 (es)
MA (1) MA23717A1 (es)
NO (1) NO954453L (es)
NZ (1) NZ280396A (es)
PE (1) PE10997A1 (es)
PL (1) PL311261A1 (es)
SG (1) SG70950A1 (es)
TR (1) TR199501387A2 (es)
ZA (1) ZA959268B (es)

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IL165220A0 (en) 2002-06-19 2005-12-18 Biovitrum Ab Novel compounds, their use and preparation
UA89035C2 (ru) * 2003-12-03 2009-12-25 Лео Фарма А/С Эфиры гидроксамовых кислот и их фармацевтическое применение
MY140489A (en) * 2003-12-26 2009-12-31 Eisai R&D Man Co Ltd 1,2-di (cyclic) substituted benzene compounds
WO2005112538A2 (en) * 2004-05-20 2005-12-01 Universidade Federal Do Rio De Janeiro-Ufrj Use of adrenergic n-phenylpiperazine antagonists, pharmaceutical compositions containing them, and methods of preparing them.
EP2077262A4 (en) * 2006-10-23 2011-12-28 Takeda Pharmaceutical IMINOPYRIDINE DERIVATIVES AND THEIR USE
JP5441705B2 (ja) * 2007-10-15 2014-03-12 武田薬品工業株式会社 アミド化合物およびその用途
US8481569B2 (en) 2008-04-23 2013-07-09 Takeda Pharmaceutical Company Limited Iminopyridine derivatives and use thereof
CL2009000964A1 (es) * 2008-04-23 2010-03-26 Takeda Pharmaceuticals Co Compuestos derivados de 1-aril-2-imino-1,2-dihidropiridina-3-carboxamida, antagonista del receptor adrenergico alfa 1d, composicion farmaceutica que los comprende; y su uso para el tratamiento o profilaxis de enfermedades del tracto urinario inferior.
US20110039892A1 (en) * 2008-04-23 2011-02-17 Takeda Pharmaceutical Company Limited Iminopyridine derivative and use thereof
CN101585781B (zh) * 2009-07-08 2012-08-08 北京颖新泰康国际贸易有限公司 一种邻氨基-n,n-二甲基苯甲酰胺的制备方法
CN103387531A (zh) * 2012-05-10 2013-11-13 广州医学院 酰胺类芳基哌嗪衍生物及其制备方法和在抗良性***增生中的应用
CN114163383A (zh) * 2021-12-24 2022-03-11 江苏丰山集团股份有限公司 一种烟嘧磺隆中间体烟酰胺和磺酰胺的绿色生产工艺
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Also Published As

Publication number Publication date
AU3459995A (en) 1996-05-16
FI955376A (fi) 1996-05-09
NZ280396A (en) 1997-05-26
NO954453D0 (no) 1995-11-07
JPH08208614A (ja) 1996-08-13
KR960017658A (ko) 1996-06-17
CA2162089A1 (en) 1996-05-09
EP0711757A1 (en) 1996-05-15
MA23717A1 (fr) 1996-07-01
IL115844A0 (en) 1996-01-31
CN1136039A (zh) 1996-11-20
HUT73843A (en) 1996-09-30
ZA959268B (en) 1997-01-31
BR9505107A (pt) 1997-09-09
CZ291095A3 (en) 1996-09-11
CO4520230A1 (es) 1997-10-15
TR199501387A2 (tr) 1996-07-21
HU9503178D0 (en) 1996-01-29
PL311261A1 (en) 1996-05-13
NO954453L (no) 1996-05-09
AR002244A1 (es) 1998-03-11
FI955376A0 (fi) 1995-11-08
SG70950A1 (en) 2000-03-21
US5688795A (en) 1997-11-18

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