ES2157366T3 - Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos. - Google Patents

Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos.

Info

Publication number
ES2157366T3
ES2157366T3 ES96108493T ES96108493T ES2157366T3 ES 2157366 T3 ES2157366 T3 ES 2157366T3 ES 96108493 T ES96108493 T ES 96108493T ES 96108493 T ES96108493 T ES 96108493T ES 2157366 T3 ES2157366 T3 ES 2157366T3
Authority
ES
Spain
Prior art keywords
sub
rent
arilo
sup
heteroarilo
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES96108493T
Other languages
English (en)
Inventor
Gary W Bantle
Todd R Elworthy
Angel Guzman
Saul Jaime-Figueroa
Francisco J Lopez-Tapia
David J Morgans Jr
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2157366T3 publication Critical patent/ES2157366T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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 with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C07D239/557—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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 with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms, e.g. orotic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic 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
    • C07D239/28—Heterocyclic 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • C07D239/96—Two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D253/00—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00
    • C07D253/02—Heterocyclic compounds containing six-membered rings having three nitrogen atoms as the only ring hetero atoms, not provided for by group C07D251/00 not condensed with other rings
    • C07D253/06—1,2,4-Triazines
    • C07D253/065—1,2,4-Triazines having three double bonds between ring members or between ring members and non-ring members
    • C07D253/07—1,2,4-Triazines having three 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
    • C07D253/075—Two hetero atoms, in positions 3 and 5
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

LA PRESENTE INVENCION SE REFIERE A NUEVOS AGONISTAS AL SUB,3}-ADRENOCEPTORES DE LA FORMULA (I) EN LA CUAL: R{SUP,1} ES ACETILAMINO, AMINO, CIANO, TRIFLUOACETILAMINO, HALO, HIDRO, HIDROXI, NITRO, METILSULFONILAMINO, 2-PROPINILOXI, UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,1-6}), CICLOALQUILO(C{SUB,36}), ALQUIL(C{SUB,1-4})CICLOALQUILO(C{SUB,3-6}, ALQUILOXI(C{SUB,1-6}), CICLOALQUILOXI(C{SUB,3-6}, ALQUILOXI(C{SUB,1-4})CICLOALQUILO(C{SUB,3-6}) Y ALQUILTIO(C{SUB,1-4}) (CUYO GRUPO ESTA ADEMAS OPCIONALMENTE SUBSTITUIDO CON DE 1 A 3 ATOMOS DE HALO) O UN GRUPO SELECCIONADO DE ARILO, ALQUIL(C{SUB,1-4})ARILO, HETEROARILO, ALQUIL(C{SUB,14})HETEROARILO, ARILOXI, ALQUILOXI(C{SUB,1-4})ARILO, HETEROARILOXI Y ALQUILOXI(C{SUB,1-4})HETEROARILO (CUYO ARILO Y HETEROARILO ESTAN ADEMAS OPCIONALMENTE SUBSTITUIDOS CON DE 1 A 2 RADICALES INDEPENDIENTEMENTE SELECCIONADOS DE HALO Y CIANO); R{SUP,2} ES CIANO, HALO, HIDRO, HIDROXI O UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,1-6}) Y ALQUILOXI(C{SUB,1-6}) (CUYO GRUPO ESTA ADEMASOPCIONALMENTE SUBSTITUIDO CON DE 1 A 3 ATOMOS DE HALOGENO); R{SUP,3} Y R{SUP,4} SON AMBOS HIDRO O METILO O JUNTOS SON ETILENO; Y R{SUP,5} ES UN GRUPO SELECCIONADO DE LAS FORMULAS (A), (B), (C) Y (D): EN QUE: X ES C(O), CH{SUB,2} O CH(OH); Y ES CH{SUB,2} O CH(OH); Z ES N O C(R{SUP,9}), EN DONDE R{SUP,9} ES HIDRO, ALQUILO(C{SUB,1-6}) O HIDROXI; R{SUP,6} ES HIDRO, UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,1-6}), CICLOALQUILO(C{SUB,3-6}), ALQUIL(C{SUB,1-4})CICLOALQUILO(C{SUB,36}) (CUYO GRUPO ESTA OPCIONALMENTE SUBSTITUIDO CON DE 1 A 3 ATOMOS DE HALO) O UN GRUPO SELECCIONADO DE ARILO, HETEROARILO, ALQUIL(C{SUB,1-4})ARILO Y ALQUIL(C{SUB,1-4}HETEROARILO (CUYO ARILO Y HETEROARILO ESTAN ADEMAS OPCIONALMENTE SUBSTITUIDOS CON DE UNO A TRES RADICALES SELECCIONADOS DE HALO, CIANO, ALQUILOXI(C{SUB,1-6}), ALQUILO(C{SUB,1-6}) Y ARILO); R{SUP,7} ES ALCANOILO(C{SUB,1-6}), CARBAMOILO, CIANO, DIALQUILAMINO(C{SUB,1-6}), HALO, HIDRO, HIDROXI, HIDROXIIMINOMETILO, ALQUIL(C{SUB,1-6})-SULFONILO, ALQUILTIO(C{SUB,1-6}),UN GRUPO SELECCIONADO DE ALQUILO(C{SUB,16}), CICLOALQUILO(C{SUB,3-6}), ALQUILOXI(C{SUB,1-6}) Y ALQUIL(C{SUB,1-4})ALQUILOXI(C{SUB,1-6}) (CUYO GRUPO ESTA OPCIONALMENTE SUBSTITUIDO CON DE UNO A TRES RADICALES SELECCIONADOS DE HALO, HIDROXI O ALQUILOXI(C{SUB,1-6})) O UN GRUPO SELECCIONADO DE ARILO, HETEROARILO, ALQUIL(C{SUB,1-4})ARILO Y ALQUIL(C{SUB,1-4})HETEROARILO (CUYO ARILO Y HETEROARILO ESTAN ADEMAS OPCIONALMENTE SUBSTITUIDOS CON DE UNO A TRES RADICALES SELECCIONADOS DE HALO, CIANO, ALQUILOXI(C{SUB,1-6}), ALQUILO(C{SUB,1-6}) Y ARILO) O R{SUP,7} Y R{SUP,9} JUNTOS SON TETRAMETILENO, Y CADA R{SUP,8} ES INDEPENDIENTEMENTE HIDRO, HIDROXI, METILO O ETILO; Y LAS SALES FARMACEUTICAMENTE ACEPTABLES Y N-OXIDOS DE LOS MISMOS.
ES96108493T 1995-06-09 1996-05-28 Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos. Expired - Lifetime ES2157366T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US48918395A 1995-06-09 1995-06-09

Publications (1)

Publication Number Publication Date
ES2157366T3 true ES2157366T3 (es) 2001-08-16

Family

ID=23942748

Family Applications (1)

Application Number Title Priority Date Filing Date
ES96108493T Expired - Lifetime ES2157366T3 (es) 1995-06-09 1996-05-28 Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos.

Country Status (31)

Country Link
EP (1) EP0748800B1 (es)
JP (1) JP2721147B2 (es)
KR (1) KR100446877B1 (es)
CN (1) CN1118459C (es)
AR (1) AR003428A1 (es)
AT (1) ATE201016T1 (es)
AU (1) AU710754B2 (es)
BR (1) BR9602705A (es)
CA (1) CA2178548A1 (es)
CO (1) CO4700472A1 (es)
CZ (1) CZ290004B6 (es)
DE (1) DE69612698T2 (es)
DK (1) DK0748800T3 (es)
ES (1) ES2157366T3 (es)
GR (1) GR3036307T3 (es)
HU (1) HU223594B1 (es)
IL (1) IL118519A (es)
MA (1) MA23899A1 (es)
MY (1) MY113499A (es)
NO (1) NO309424B1 (es)
NZ (1) NZ286720A (es)
PE (1) PE46497A1 (es)
PL (1) PL188061B1 (es)
PT (1) PT748800E (es)
RU (1) RU2175322C2 (es)
SA (1) SA96170263B1 (es)
SG (1) SG45486A1 (es)
TR (1) TR970073A2 (es)
TW (1) TW340846B (es)
UY (1) UY24257A1 (es)
ZA (1) ZA964561B (es)

Families Citing this family (43)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6271234B1 (en) 1997-08-01 2001-08-07 Recordati S.A., Chemical And Pharmaceutical Company 1,4-disubstituted piperazines
HU226767B1 (en) 1997-10-31 2009-09-28 Asubio Pharma Co Arylpiperidinopropanol and arylpiperazinopropanol derivatives and pharmaceuticals containing the same
US6083950A (en) * 1997-11-13 2000-07-04 Ranbaxy Laboratories Limited 1-(4-arylpiperazin-1-yl)-ω-[n-(α,ω-dicarboximido)]-alka nes useful as uro-selective α1-adrenoceptor blockers
EP0949250B1 (en) * 1998-03-30 2006-05-03 F. Hoffmann-La Roche Ag Process for manufacturing alpha1L-adrenoceptor antagonists
AU1979799A (en) * 1998-07-21 2000-02-14 Ranbaxy Laboratories Limited Arylpiperazine derivatives useful as uro-selective alpha-1-adrenoceptor blockers
HUP0102980A3 (en) * 1998-07-21 2003-02-28 Ranbaxy Lab Ltd Arylpiperazine derivatives useful as uroselective alpha1-adrenoceptor blockers, pharmaceutical compositions containing them and their use
AU1345600A (en) 1998-11-12 2000-06-05 Merck & Co., Inc. Pyrimidinedione derivatives useful as alpha 1a adrenoceptor antagonists
US6358959B1 (en) 1999-01-26 2002-03-19 Merck & Co., Inc. Polyazanaphthalenone derivatives useful as alpha 1a adrenoceptor antagonists
US6306861B1 (en) 1999-07-30 2001-10-23 Recordati S.A. Chemical And Pharmaceutical Company Thienopyrancecarboxamide derivatives
US6387909B1 (en) 1999-07-30 2002-05-14 Recordati S.A. Chemical And Pharmaceutical Company Thienopyranecarboxamide derivatives
GB2355456A (en) 1999-09-30 2001-04-25 Merck & Co Inc Novel arylhydantoin derivatives useful as alpha 1a adrenoceptor antagonists
GB2355263A (en) 1999-09-30 2001-04-18 Merck & Co Inc Lactam and cyclic urea derivatives useful as alpha 1a adrenoceptor antagonists
GB2355457A (en) 1999-09-30 2001-04-25 Merck & Co Inc Novel spirotricyclic substituted azacycloalkane derivatives useful as alpha 1a adrenoceptor antagonists
GB2355264A (en) 1999-09-30 2001-04-18 Merck & Co Inc Spirohydantoin derivatives useful as alpha 1a adrenoceptor antagonists
US6365591B1 (en) 1999-10-18 2002-04-02 Recordati, S.A., Chemical And Pharmacueticals Company Isoxazolecarboxamide derivatives
US6403594B1 (en) 1999-10-18 2002-06-11 Recordati, S.A. Chemical And Pharmaceutical Company Benzopyran derivatives
KR100814269B1 (ko) 2000-01-25 2008-03-18 뉴로크린 바이오사이언시즈 인코퍼레이티드 고나도트로핀-분비 호르몬 수용체 길항제 및 이를 포함하는 약제학적 조성물
AP2003002810A0 (en) * 2000-11-30 2003-06-30 Ranbaxy Laboratories Ltd 1,4-Disubstituted piperazine derivatives useful as uro-selective a, - adrenoceptor blockers
JP2005500352A (ja) 2001-08-02 2005-01-06 ニューロクライン バイオサイエンシーズ， インコーポレイテッド ゴナドトロピン放出ホルモンレセプター（ＧｎＲＨ）アンタゴニストとしての１，２，４−トリアジン−３，５−ジオン
DE10311065A1 (de) 2003-03-13 2004-09-23 Abbott Gmbh & Co. Kg Pyrimidin-2-on-Verbindungen und ihre therapeutische Verwendung
KR20050122220A (ko) 2003-03-25 2005-12-28 다케다 샌디에고, 인코포레이티드 디펩티딜 펩티다제 억제제
KR20060041309A (ko) 2003-08-13 2006-05-11 다케다 야쿠힌 고교 가부시키가이샤 ４-피리미돈 유도체 및 펩티딜 펩티다제 저해제로서의 그의용도
US7790734B2 (en) 2003-09-08 2010-09-07 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
MY140489A (en) * 2003-12-26 2009-12-31 Eisai R&D Man Co Ltd 1,2-di (cyclic) substituted benzene compounds
GB0400290D0 (en) 2004-01-08 2004-02-11 Medivir Ab dUTPase inhibitors
EA013427B1 (ru) 2004-03-15 2010-04-30 Такеда Фармасьютикал Компани Лимитед Ингибиторы дипептидилпептидазы
EP1655288A1 (en) * 2004-11-05 2006-05-10 Institut Pasteur Aryl pyrimidyl compounds, pharmaceutical compositions comprising them, their use as antimicrobial agents
WO2006068058A1 (ja) 2004-12-20 2006-06-29 Eisai R & D Management Co., Ltd. １－シクロプロピルメチル－４－［２－（３，３，５，５－テトラメチルシクロヘキシル）フェニル］ピペラジンの塩および結晶
EP1828192B1 (en) 2004-12-21 2014-12-03 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
EP1889827B1 (en) * 2005-05-25 2010-08-25 Eisai R&D Management Co., Ltd. Process for producing [2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine
PT1942898E (pt) 2005-09-14 2011-12-20 Takeda Pharmaceutical Inibidores da dipeptidilpeptidase para o tratamento da diabetes
CN101360723A (zh) * 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
DE102008030091B4 (de) 2008-06-25 2011-03-03 Resprotect Gmbh Uracilderivate und deren Verwendung
US9452980B2 (en) 2009-12-22 2016-09-27 Hoffmann-La Roche Inc. Substituted benzamides
RU2449994C1 (ru) * 2011-03-10 2012-05-10 Светлана Алексеевна Мещерякова 6-(4-бензилпиперазино)-1,3-диметилурацила дигидрохлорид, проявляющий биологическую активность
CN103596431B (zh) * 2011-03-18 2016-06-22 科赛普特治疗公司 嘧啶环己基糖皮质激素受体调节剂
GB201318886D0 (en) * 2013-10-25 2013-12-11 Givaudan Sa Improvements i or relating to organic compounds
BR112018015389B1 (pt) 2016-03-17 2023-12-19 F. Hoffmann-La Roche Ag Derivado de 5-etil-4-metil-pirazol-3-carboxamida, seu processo de fabricação, preparação farmacêutica oral e uso
MX2022004804A (es) * 2019-10-28 2022-05-16 Nippon Soda Co Compuesto de 2,6-dioxo-3,6-dihidropirimidina, bactericida agricola y horticola, nematicida y agente antifungico medico y veterinario.
US20240260575A1 (en) * 2021-04-28 2024-08-08 Nippon Soda Co., Ltd. Agricultural and horticultural fungicidal composition

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE2727469A1 (de) * 1977-06-18 1978-12-21 Hoechst Ag Neue hexahydropyrimidine, verfahren zu ihrer herstellung und arzneimittel, die diese verbindungen enthalten
JPH02184667A (ja) * 1989-01-11 1990-07-19 Meiji Seika Kaisha Ltd Ｎ，ｎ’―ジ置換ピペラジル誘導体及びそれを有効成分とする排尿障害改善剤
JPH0344379A (ja) * 1989-07-13 1991-02-26 Yamasa Shoyu Co Ltd Ｎ↑３―ピペラジノウラシル誘導体
JP2814600B2 (ja) * 1989-08-31 1998-10-22 正幸 石川 排尿障害治療剤
FR2673628B1 (fr) * 1991-03-07 1993-07-09 Esteve Labor Dr Procede de preparation de derives d'aryl (ou heteroaryl)-piperazinyl-butyl-azoles.
SG65570A1 (en) * 1992-02-25 1999-06-22 Recordati Chem Pharm Heterobicyclic compounds
GB9305623D0 (en) * 1993-03-18 1993-05-05 Merck Sharp & Dohme Therapeutic agents
IL111730A (en) * 1993-11-29 1998-12-06 Fujisawa Pharmaceutical Co Piperazine derivatives processes for the preparation thereof and pharmaceutical compositions containing the same
FR2727682A1 (fr) * 1994-12-02 1996-06-07 Pf Medicament Nouveaux derives de 3,5-dioxo-(2h,4h)-1,2,4-triazines, leur preparation et leur application a titre de medicament

Also Published As

Publication number Publication date
ATE201016T1 (de) 2001-05-15
PT748800E (pt) 2001-10-30
NO962412L (no) 1996-12-10
PE46497A1 (es) 1997-12-04
HUP9601529A2 (hu) 1998-09-28
NO309424B1 (no) 2001-01-29
NO962412D0 (no) 1996-06-07
DK0748800T3 (da) 2001-08-27
GR3036307T3 (en) 2001-10-31
EP0748800A2 (en) 1996-12-18
ZA964561B (en) 1996-12-09
MA23899A1 (fr) 1996-12-31
IL118519A0 (en) 1996-09-12
UY24257A1 (es) 2000-12-29
PL314635A1 (en) 1996-12-23
IL118519A (en) 1999-12-22
CZ290004B6 (cs) 2002-05-15
CN1149051A (zh) 1997-05-07
AR003428A1 (es) 1998-08-05
NZ286720A (en) 1998-08-26
BR9602705A (pt) 1998-09-08
CZ169696A3 (en) 1997-01-15
KR100446877B1 (ko) 2004-11-06
PL188061B1 (pl) 2004-12-31
TR970073A2 (tr) 1997-02-21
AU710754B2 (en) 1999-09-30
SG45486A1 (en) 1998-01-16
EP0748800A3 (en) 1996-12-27
HK1013065A1 (en) 1999-08-13
HU223594B1 (hu) 2004-09-28
HUP9601529A3 (en) 2000-02-28
HU9601529D0 (en) 1996-07-29
RU2175322C2 (ru) 2001-10-27
AU5469096A (en) 1996-12-19
CO4700472A1 (es) 1998-12-29
KR970001344A (ko) 1997-01-24
TW340846B (en) 1998-09-21
JPH09100269A (ja) 1997-04-15
MY113499A (en) 2002-03-30
SA96170263B1 (ar) 2006-05-23
DE69612698D1 (de) 2001-06-13
CN1118459C (zh) 2003-08-20
DE69612698T2 (de) 2001-12-06
JP2721147B2 (ja) 1998-03-04
EP0748800B1 (en) 2001-05-09
CA2178548A1 (en) 1996-12-10

Similar Documents

Publication Publication Date Title
ES2157366T3 (es) Derivados de pirimidindiona, pirimidintriona, triacindiona como antagonistas de receptores alfa-1-adrenergicos.
ES2191870T3 (es) Pirazoles parasiticidas.
ES2170211T3 (es) Compuestos azaheterociclicos que tienen actividad antagonista de los receptores de taquiquinina; nk1 y nk2.
ES2164758T3 (es) Derivados de morfolina sustituidos y su uso como agentes terapeuticos.
ES2113368T3 (es) Antagonistas de serotonina.
DK0640592T3 (da) N-acylerede tricycliske azaheteroringe anvendelige som vasopressin-antagonister
ES2159760T3 (es) Derivados de aril purina y piridopirimidina y de heteroaril purina y piridopirimidina.
ES2191838T3 (es) Derivados de tetrahidroisoquinoleina como moduladores de los receptores d3 de la dopamina.
ES2180625T3 (es) Derivados de camptotecina solubles en agua, proceso para su preparacion y su uso como agentes antitumorales.
ES2143238T3 (es) Derivados de 1-(piperidinil disustituido en posiciones 1,2)-piperazinas sustituidas en posicion 4.
ES2153118T3 (es) Analogos heterociclicos de 1,2,4-triazolo 1,5-c)pirimidina que tienen una actividad antagonista sobre los receptores de adenosina a 2a?.
AR245700A1 (es) Nuevos derivados de la 2-anilino-pirimidina como agentes antiparasitarios.
AR248013A1 (es) Compuesto de imidazol y composicion biocida que los contiene, excluidos sus usos medicinales y veterinarios, y el procedimiento de preparacion de los compuestos i y sus intermediarios.
ES2176329T3 (es) Procedimientos para preparar formas anhidras e hidratadas de derivados antihistaminicos de piperidina, sus polimeros y pseudomorfos.
DE69903333D1 (de) Crf rezeptor-antagonisten und darauf bezogene methoden
PT91336A (pt) Processo para a preparacao de derivados lactamicos
ES2164881T3 (es) Derivados de 6-carboxamido dihidropirano.
ES2123873T3 (es) Pirrolocarbazol.
ES2166128T3 (es) Mezcla fungicida.
MXPA94001345A (es) Derivados de poliamina como agentes radioprotectores.
BR0209719A (pt) Derivados de aminoquinolina e aminopiridina e seu uso como ligandos de adenosina a3
BR9714215A (pt) Derivados de benzoato de 1,4-diazabiciclo[2.2.2]oct-2-ilmetila, seu preparo e sua aplicação em terapêutica
MX9300602A (es) Analogos de fenilalanina de bombesina.
ES2177727T3 (es) Derivados de 4-indolilpiperazinilo.
PT90716A (pt) Processo aperfeicoado para a preparacao de derivados de ariloxipropanolamina uteis como antagonistas de serotonina

Legal Events

Date Code Title Description
FG2A Definitive protection

Ref document number: 748800

Country of ref document: ES