CO4950513A1 - Compuestos de pirazina - Google Patents

Compuestos de pirazina

Info

Publication number
CO4950513A1
CO4950513A1 CO98010500A CO98010500A CO4950513A1 CO 4950513 A1 CO4950513 A1 CO 4950513A1 CO 98010500 A CO98010500 A CO 98010500A CO 98010500 A CO98010500 A CO 98010500A CO 4950513 A1 CO4950513 A1 CO 4950513A1
Authority
CO
Colombia
Prior art keywords
4alkyl
substituted
hydrogen
group
halogen atoms
Prior art date
Application number
CO98010500A
Other languages
English (en)
Inventor
Brian Cox
Stuart Nobbs Malcolm
Punjabhai Shah Gita
Dean David Edney
Michael Simon Loft
Original Assignee
Glaxo Group Ltd
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
Priority claimed from GBGB9704275.8A external-priority patent/GB9704275D0/en
Priority claimed from GBGB9708183.0A external-priority patent/GB9708183D0/en
Application filed by Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of CO4950513A1 publication Critical patent/CO4950513A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings 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
    • C07D241/20—Nitrogen atoms
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings 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
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with nitrogen atoms directly attached to ring carbon atoms

Abstract

Un compuesto de fórmula (I)caracterizado porque R1 se selecciona del grupo que consiste de fenilo sustituido por uno o más átomos de halógeno, naftilo y naftilo sustituido por uno o más átomos de halógeno; R2 se selecciona del grupo que consiste de -NH2 y -NHC(=O)Ra ; R3 se selecciona del grupo que consiste de -NRb Rc , -NHC(=O)Ra e hidrógeno; R4 se selecciona del grupo que consiste de hidrógeno, -alquilo de C1-4 , -alquilo de C1-4 sustituido por uno o más átomos de halógeno, -CN, -CH2 OH, -CH2 ORd y -CH2 S(O)x Rd ; en la que Ra representa alquilo de C1-4 o cicloalquilo de C3-7 , y Rb y Rc , los cuales pueden ser los mismos o diferentes, se seleccionan de hidrógeno y alquilo de C1-4 , o junto con el átomo de nitrógeno al cual están unidos, forma un heterociclo de 6 miembros que contiene nitrógeno, el cual heterociclo puede ser además sustituido con uno o más de alquilo de C1-4 ; Rd se selecciona de alquilo C1-4 o alquilo de C1-4 sustituido por uno o más átomos de halógeno; x es un número entero de cero, uno o dos; y derivados farmacéuticamente aceptables de los mismos; con la condición de que R1 no represente; cuando R2 sea -NH2 , y ambos de R3 y R4 sean hidrógeno.
CO98010500A 1997-03-01 1998-02-26 Compuestos de pirazina CO4950513A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9704275.8A GB9704275D0 (en) 1997-03-01 1997-03-01 Pharmacologically active compound
GBGB9708183.0A GB9708183D0 (en) 1997-04-23 1997-04-23 Pharmacologically active compound

Publications (1)

Publication Number Publication Date
CO4950513A1 true CO4950513A1 (es) 2000-09-01

Family

ID=26311097

Family Applications (1)

Application Number Title Priority Date Filing Date
CO98010500A CO4950513A1 (es) 1997-03-01 1998-02-26 Compuestos de pirazina

Country Status (46)

Country Link
US (2) US6255307B1 (es)
EP (1) EP0966448B1 (es)
JP (1) JP3369189B2 (es)
KR (1) KR100544263B1 (es)
CN (1) CN1105111C (es)
AP (1) AP9901632A0 (es)
AR (1) AR011174A1 (es)
AT (1) ATE251143T1 (es)
AU (1) AU732915B2 (es)
BG (1) BG103723A (es)
BR (1) BR9807814B1 (es)
CA (1) CA2282585C (es)
CO (1) CO4950513A1 (es)
CZ (1) CZ295618B6 (es)
DE (1) DE69818643T2 (es)
DK (1) DK0966448T3 (es)
EA (1) EA002102B1 (es)
EE (1) EE9900376A (es)
ES (1) ES2205469T3 (es)
GE (1) GEP20012555B (es)
GT (1) GT199800046A (es)
HK (1) HK1023116A1 (es)
HN (2) HN1998000036A (es)
HR (1) HRP980107A2 (es)
HU (1) HU225852B1 (es)
ID (1) ID22850A (es)
IL (1) IL131293A (es)
IS (1) IS5163A (es)
JO (1) JO2035B1 (es)
MA (1) MA26473A1 (es)
MY (1) MY118612A (es)
NO (1) NO313383B1 (es)
NZ (1) NZ337121A (es)
OA (1) OA11151A (es)
PA (1) PA8448201A1 (es)
PE (1) PE58299A1 (es)
PL (1) PL192864B1 (es)
PT (1) PT966448E (es)
SI (1) SI0966448T1 (es)
SK (1) SK117399A3 (es)
SV (1) SV1998000029A (es)
TR (1) TR199902082T2 (es)
TW (1) TW513416B (es)
UY (1) UY24911A1 (es)
WO (1) WO1998038174A1 (es)
YU (1) YU40799A (es)

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US6420354B1 (en) 1998-06-08 2002-07-16 Advanced Medicine, Inc. Sodium channel drugs and uses
GB9818881D0 (en) 1998-08-28 1998-10-21 Glaxo Group Ltd Compounds
GB9907965D0 (en) * 1999-04-09 1999-06-02 Glaxo Group Ltd Medical use
US6479498B1 (en) 1999-06-04 2002-11-12 Theravance, Inc. Sodium channel drugs and uses
WO2001060806A2 (en) * 2000-02-16 2001-08-23 Neurogen Corporation Substituted arylpyrazines
EP1500653A1 (en) * 2000-02-16 2005-01-26 Neurogen Corporation Substituted arylpyrazines
GB0010971D0 (en) * 2000-05-05 2000-06-28 Glaxo Group Ltd Process
GB0016040D0 (en) * 2000-06-29 2000-08-23 Glaxo Group Ltd Novel process for preparing crystalline particles
SE0102439D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102438D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
EP1446387B1 (en) * 2001-11-21 2009-11-04 Pharmacia & Upjohn Company LLC Substituted aryl 1,4-pyrazine derivatives
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
EP1458386B1 (en) * 2001-12-27 2007-04-18 Ortho-McNeil Pharmaceutical, Inc. Aroyl pyrrole heteroeryl and methanols useful for treating a central nervous system disorder
JP2005533014A (ja) 2002-04-26 2005-11-04 ファルマシア・アンド・アップジョン・カンパニー・エルエルシー 置換ピラジン誘導体
CA2496197A1 (en) 2002-08-20 2004-03-04 Neurogen Corporation 5-substituted-2-arylpyrazines as modulators of crf receptors
SE0203754D0 (sv) * 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203753D0 (sv) * 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
CA2514574A1 (en) 2003-01-30 2004-08-12 Dynogen Pharmaceuticals, Inc. Use of sodium channel modulators for treating gastrointestinal tract disorders
TW200510373A (en) * 2003-07-14 2005-03-16 Neurogen Corp Substituted quinolin-4-ylamine analogues
CA2595855C (en) 2005-01-25 2017-07-04 Synta Pharmaceuticals Corp. Pyrazine compounds for inflammation and immune-related uses
MX2007009923A (es) * 2005-02-15 2008-03-04 Jazz Pharmaceuticals Forma farmaceutica y metodo para liberacion sostenida de un compuesto de pirazina sustituido.
NL2000284C2 (nl) * 2005-11-04 2007-09-28 Pfizer Ltd Pyrazine-derivaten.
WO2007083239A1 (en) * 2006-01-23 2007-07-26 Pfizer Limited Pyridine derivatives as sodium channel modulators
CA2685952C (en) * 2007-05-03 2012-03-13 Pfizer Limited N- [6-amino-5- (phenyl) pyrazin-2-yl] -isoxazole-4-carboxamide derivatives and related compounds as nav1.8 channel modulators for the treatment of pain
GB0800741D0 (en) 2008-01-16 2008-02-20 Univ Greenwich Cyclic triazo and diazo sodium channel blockers
GB201111712D0 (en) 2011-07-08 2011-08-24 Gosforth Ct Holdings Pty Ltd Pharmaceutical compositions
FR3001151B1 (fr) 2013-01-21 2016-04-08 Pf Medicament Association d'un bloqueur de courant sodique lent et d'un inhibiteur du courant if sinusal et les compositions pharmarceutiques la contenant
JO3517B1 (ar) * 2014-01-17 2020-07-05 Novartis Ag ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2
EA036446B1 (ru) 2016-06-14 2020-11-11 Новартис Аг Соединения и композиции для подавления активности shp2
US11602512B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11602513B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11504347B1 (en) 2016-07-22 2022-11-22 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
UY37341A (es) 2016-07-22 2017-11-30 Flamel Ireland Ltd Formulaciones de gamma-hidroxibutirato de liberación modificada con farmacocinética mejorada
CN108101857B (zh) * 2016-11-24 2021-09-03 韶远科技（上海)有限公司 制取2-氨基-3-溴-6-氯吡嗪的可放大工艺
CN107011273A (zh) * 2017-05-04 2017-08-04 无锡捷化医药科技有限公司 一种合成6‑碘‑3‑(2,3‑二氯苯基)吡嗪‑2‑胺的方法
CA3127871A1 (en) 2019-03-01 2020-09-10 Flamel Ireland Limited Gamma-hydroxybutyrate compositions having improved pharmacokinetics in the fed state
US11779557B1 (en) 2022-02-07 2023-10-10 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
US11583510B1 (en) 2022-02-07 2023-02-21 Flamel Ireland Limited Methods of administering gamma hydroxybutyrate formulations after a high-fat meal
CN115611700A (zh) * 2022-10-11 2023-01-17 辽宁东大光明化工科技有限责任公司 一种1-溴-2,5-二氯-3-氟苯的制备方法

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JPH08238778A (ja) * 1995-03-07 1996-09-17 Brother Ind Ltd インク噴射装置の電極形成方法

Also Published As

Publication number Publication date
EE9900376A (et) 2000-04-17
HUP0001802A2 (hu) 2001-05-28
AP9901632A0 (en) 1999-09-30
MY118612A (en) 2004-12-31
HU225852B1 (en) 2007-11-28
IS5163A (is) 1999-08-24
ATE251143T1 (de) 2003-10-15
US6599905B2 (en) 2003-07-29
HUP0001802A3 (en) 2001-07-30
TR199902082T2 (xx) 2000-04-21
CN1105111C (zh) 2003-04-09
EP0966448A1 (en) 1999-12-29
NO313383B1 (no) 2002-09-23
AU6823798A (en) 1998-09-18
HN1998000036A (es) 1999-08-23
MA26473A1 (fr) 2004-12-20
EA002102B1 (ru) 2001-12-24
EA199900687A1 (ru) 2000-04-24
BG103723A (bg) 2001-05-31
AU732915B2 (en) 2001-05-03
SV1998000029A (es) 1998-12-11
CZ311199A3 (cs) 2000-02-16
CN1253551A (zh) 2000-05-17
JP3369189B2 (ja) 2003-01-20
KR20000075859A (ko) 2000-12-26
PL192864B1 (pl) 2006-12-29
US20020169172A1 (en) 2002-11-14
PL335441A1 (en) 2000-04-25
CA2282585A1 (en) 1998-09-03
SK117399A3 (en) 2000-06-12
US6255307B1 (en) 2001-07-03
DE69818643T2 (de) 2004-10-07
JO2035B1 (en) 1999-05-15
DE69818643D1 (de) 2003-11-06
GEP20012555B (en) 2001-10-25
IL131293A0 (en) 2001-01-28
UY24911A1 (es) 2000-12-29
ES2205469T3 (es) 2004-05-01
AR011174A1 (es) 2000-08-02
EP0966448B1 (en) 2003-10-01
PA8448201A1 (es) 2000-05-24
TW513416B (en) 2002-12-11
IL131293A (en) 2003-07-31
WO1998038174A1 (en) 1998-09-03
HRP980107A2 (en) 1998-12-31
HK1023116A1 (en) 2000-09-01
OA11151A (en) 2003-04-22
DK0966448T3 (da) 2004-02-02
SI0966448T1 (en) 2004-04-30
JP2000511203A (ja) 2000-08-29
YU40799A (sh) 2001-09-28
BR9807814B1 (pt) 2009-01-13
CA2282585C (en) 2006-06-06
PT966448E (pt) 2004-02-27
NZ337121A (en) 2001-03-30
HN1999000019A (es) 1999-08-23
GT199800046A (es) 1999-08-20
BR9807814A (pt) 2000-02-22
KR100544263B1 (ko) 2006-01-23
NO994213L (no) 1999-10-29
CZ295618B6 (cs) 2005-09-14
NO994213D0 (no) 1999-08-31
ID22850A (id) 1999-12-09
PE58299A1 (es) 1999-06-23

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