PE20110163A1 - Proceso para la preparacion de derivados de pirimidina sustituidos - Google Patents

Proceso para la preparacion de derivados de pirimidina sustituidos

Info

Publication number
PE20110163A1
PE20110163A1 PE2010001216A PE2010001216A PE20110163A1 PE 20110163 A1 PE20110163 A1 PE 20110163A1 PE 2010001216 A PE2010001216 A PE 2010001216A PE 2010001216 A PE2010001216 A PE 2010001216A PE 20110163 A1 PE20110163 A1 PE 20110163A1
Authority
PE
Peru
Prior art keywords
formula
compound
alkyl
preparation
produce
Prior art date
Application number
PE2010001216A
Other languages
English (en)
Inventor
Sergio Cesco-Cancian
Hongfeng Chen
Jeffrey S Grimm
Neelakandha S Mani
Christopher M Mapes
David C Palmer
Daniel J Pippel
Kirk L Sorgi
Tong Xiao
Original Assignee
Janssen Pharmaceutica Nv
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41464882&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20110163(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of PE20110163A1 publication Critical patent/PE20110163A1/es

Links

Classifications

    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/20—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton
    • C07C211/22—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton containing at least two amino groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C211/00—Compounds containing amino groups bound to a carbon skeleton
    • C07C211/01—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms
    • C07C211/26—Compounds containing amino groups bound to a carbon skeleton having amino groups bound to acyclic carbon atoms of an unsaturated carbon skeleton containing at least one six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/18—Heterocyclic 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
    • C07D211/20—Heterocyclic 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 singly bound oxygen or sulphur atoms
    • C07D211/22—Heterocyclic 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 singly bound oxygen or sulphur atoms by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/08—Heterocyclic 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
    • C07D211/18—Heterocyclic 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
    • C07D211/26—Heterocyclic 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 nitrogen atoms

Landscapes

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

Abstract

REFERIDA A UN PROCESO DE PREPARACION DE DERIVADOS DE PIRIMIDINA DE FORMULA (I) QUE COMPRENDE: a) HACER REACCIONAR UN COMPUESTO DE FORMULA (V) CON UN COMPUESTO DE FORMULA (VI), EN PRESENCIA DE UN SISTEMA DE AGENTES DE ACOPLAMIENTO TALES COMO DIISOPROPILAZODICARBOXILATO Y TRIFENILFOSFINA, O EN UN PRIMER SOLVENTE ORGANICO TAL COMO 2-METIL-TETRAHIDROFURANO, PARA PRODUCIR EL COMPUESTO DE FORMULA (VII), b) DESPROTEGER EL COMPUESTO (VII) PARA PRODUCIR EL COMPUESTO DE FORMULA (VIII), c) HACER REACCIONAR EL COMPUESTO (VIII) CON UN COMPUESTO DE FORMULA (IX), EN UN SEGUNDO SOLVENTE ORGANICO TAL COMO ETANOL, PARA PRODUCIR EL COMPUESTO DE FORMULA (I); EN DONDE L1 ES CN; Rc ES H, METILO, ETILO, PROPILO, ISOPROPILO, CF3, CICLOPROPILO Y CICLOBUTILO; R6 ES H; R8 ES H O ALQUILO C1-C4; Z ES N O CH; n ES 1 O 2; R9, R10 Y R11 SON H O ALQUILO C1-C4; PG1 Y PG2 SON UN GRUPO DE PROTECCION DE NITROGENO TAL COMO BENCILOXICARBONIL; LG1 ES UN GRUPO DE SALIDA TAL COMO TOSILATO, OH, ENTRE OTROS; X ES N(R20)2 U OR21; R20 ES ALQUILO C1-C4; R21 ES ALQUILO C1-C4 O BENCILO. DICHOS COMPUESTOS DE FORMULA (I) SON UTILES COMO INTERMEDIARIOS EN LA SINTESIS DE MODULADORES DEL RECEPTOR H4 DE HISTAMINA
PE2010001216A 2008-06-30 2009-06-29 Proceso para la preparacion de derivados de pirimidina sustituidos PE20110163A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US7675208P 2008-06-30 2008-06-30

Publications (1)

Publication Number Publication Date
PE20110163A1 true PE20110163A1 (es) 2011-03-28

Family

ID=41464882

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2010001216A PE20110163A1 (es) 2008-06-30 2009-06-29 Proceso para la preparacion de derivados de pirimidina sustituidos

Country Status (36)

Country Link
US (6) US8309720B2 (es)
EP (5) EP2769721A3 (es)
JP (1) JP5416768B2 (es)
KR (1) KR101675354B1 (es)
CN (1) CN102137672B (es)
AR (1) AR072396A1 (es)
AU (1) AU2009267156B2 (es)
BR (1) BRPI0913644A2 (es)
CA (1) CA2729733C (es)
CO (1) CO6341560A2 (es)
CY (1) CY1116134T1 (es)
DK (1) DK2310012T3 (es)
EA (1) EA019361B1 (es)
EC (1) ECSP11010745A (es)
ES (1) ES2538135T3 (es)
HK (4) HK1156857A1 (es)
HR (1) HRP20150576T1 (es)
HU (1) HUE024949T2 (es)
IL (4) IL210214A (es)
JO (1) JO3043B1 (es)
ME (1) ME02154B (es)
MX (1) MX2011000080A (es)
MY (1) MY150601A (es)
NI (1) NI201000232A (es)
NZ (1) NZ590170A (es)
PE (1) PE20110163A1 (es)
PL (1) PL2310012T3 (es)
PT (1) PT2310012E (es)
RS (1) RS53985B1 (es)
SI (1) SI2310012T1 (es)
SV (1) SV2011003788A (es)
TW (3) TWI498326B (es)
UA (1) UA106724C2 (es)
UY (1) UY31949A (es)
WO (1) WO2010002774A1 (es)
ZA (1) ZA201100759B (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT2007752E (pt) 2006-03-31 2010-10-18 Janssen Pharmaceutica Nv Benzoimidazol-2-il pirimidinas e pirazinas como moduladores do receptor de histamina h4
US9371311B2 (en) 2008-06-30 2016-06-21 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine derivatives
UA106724C2 (uk) * 2008-06-30 2014-10-10 Янссен Фармацевтика Нв Спосіб отримання заміщених піримідинових похідних
JP5574294B2 (ja) * 2010-11-04 2014-08-20 独立行政法人科学技術振興機構 光磁気記録媒体及び光磁気記録方法
MY180726A (en) 2013-03-06 2020-12-08 Janssen Pharmaceutica Nv Benzoimidazol-2-yl pyrimidine modulators of the histamine h4 receptor
CN106132926B (zh) * 2014-03-28 2019-05-21 株式会社钟化 三苄氧羰基精氨酸的制造方法
US10723723B2 (en) 2016-11-03 2020-07-28 Bristol-Myers Squibb Company Substituted bicycle heterocyclic derivatives useful as ROMK channel inhibitors

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PT2007752E (pt) * 2006-03-31 2010-10-18 Janssen Pharmaceutica Nv Benzoimidazol-2-il pirimidinas e pirazinas como moduladores do receptor de histamina h4
UA106724C2 (uk) 2008-06-30 2014-10-10 Янссен Фармацевтика Нв Спосіб отримання заміщених піримідинових похідних
UA102855C2 (ru) * 2008-06-30 2013-08-27 Янссен Фармацевтика Нв Способ получения бензоимидазол-2-илпиримидиновых производных

Also Published As

Publication number Publication date
CY1116134T1 (el) 2017-02-08
US9079882B2 (en) 2015-07-14
US20100004450A1 (en) 2010-01-07
US20130225816A1 (en) 2013-08-29
US20130053561A1 (en) 2013-02-28
IL210214A0 (en) 2011-03-31
JP2011526910A (ja) 2011-10-20
EP2924035A1 (en) 2015-09-30
US20140073795A1 (en) 2014-03-13
US8309720B2 (en) 2012-11-13
PL2310012T3 (pl) 2015-08-31
CA2729733A1 (en) 2010-01-07
HK1214590A1 (zh) 2016-07-29
US9079884B2 (en) 2015-07-14
IL210214A (en) 2016-07-31
BRPI0913644A2 (pt) 2015-11-24
MX2011000080A (es) 2011-03-02
US9359327B2 (en) 2016-06-07
TW201420583A (zh) 2014-06-01
SV2011003788A (es) 2011-02-08
US20140066624A1 (en) 2014-03-06
TWI498326B (zh) 2015-09-01
US9079883B2 (en) 2015-07-14
HK1201441A1 (en) 2015-09-04
HUE024949T2 (en) 2016-02-29
US9006432B2 (en) 2015-04-14
SI2310012T1 (sl) 2015-06-30
UY31949A (es) 2010-01-29
ME02154B (me) 2015-10-20
WO2010002774A1 (en) 2010-01-07
ECSP11010745A (es) 2011-02-28
EP2924025A1 (en) 2015-09-30
UA106724C2 (uk) 2014-10-10
US20140121374A1 (en) 2014-05-01
DK2310012T3 (da) 2015-03-30
TWI481603B (zh) 2015-04-21
EA201170113A1 (ru) 2011-08-30
EP2310012A1 (en) 2011-04-20
RS53985B1 (en) 2015-10-30
EP2924023A1 (en) 2015-09-30
PT2310012E (pt) 2015-04-02
EP2769721A2 (en) 2014-08-27
KR20110023901A (ko) 2011-03-08
CN102137672B (zh) 2014-03-26
CO6341560A2 (es) 2011-11-21
ZA201100759B (en) 2012-07-25
EP2310012A4 (en) 2012-06-20
CA2729733C (en) 2016-10-25
HK1215434A1 (zh) 2016-08-26
JP5416768B2 (ja) 2014-02-12
HK1156857A1 (en) 2012-06-22
NZ590170A (en) 2012-04-27
AR072396A1 (es) 2010-08-25
EP2769721A3 (en) 2015-04-01
NI201000232A (es) 2011-09-07
JO3043B1 (ar) 2016-09-05
HRP20150576T1 (hr) 2015-09-11
MY150601A (en) 2014-01-30
EP2310012B1 (en) 2015-03-04
AU2009267156A1 (en) 2010-01-07
IL235570A (en) 2016-08-31
TW201433568A (zh) 2014-09-01
CN102137672A (zh) 2011-07-27
IL235572A (en) 2016-09-29
EA019361B1 (ru) 2014-03-31
AU2009267156B2 (en) 2015-05-28
KR101675354B1 (ko) 2016-11-11
TW201012810A (en) 2010-04-01
IL235571A (en) 2016-09-29
ES2538135T3 (es) 2015-06-17

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