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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • C07D241/14Heterocyclic 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
    • C07D241/20Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10Heterocyclic 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
    • C07D241/14Heterocyclic 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
    • C07D241/24Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D241/26Carbon 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
  • Detergent Compositions (AREA)

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
EP1500653A1 (en) * 2000-02-16 2005-01-26 Neurogen Corporation Substituted arylpyrazines
KR20080021603A (ko) * 2000-02-16 2008-03-07 뉴로젠 코포레이션 치환된 아릴피라진
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
SE0102438D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
SE0102439D0 (sv) * 2001-07-05 2001-07-05 Astrazeneca Ab New compounds
US6992087B2 (en) 2001-11-21 2006-01-31 Pfizer Inc Substituted aryl 1,4-pyrazine derivatives
MXPA04004714A (es) * 2001-11-21 2004-08-19 Upjohn Co Derivados de aril 1,4-pirazina sustituidos.
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
WO2003091225A1 (en) * 2002-04-26 2003-11-06 Pharmacia & Upjohn Company Substituted pyrazine derivatives
JP2006509729A (ja) 2002-08-20 2006-03-23 ニューロジェン・コーポレーション Crf受容体モジュレータとしての5−置換−2−アリールピラジン類
SE0203753D0 (sv) * 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
SE0203754D0 (sv) * 2002-12-17 2002-12-17 Astrazeneca Ab New compounds
WO2004066987A2 (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
ES2567853T3 (es) 2005-01-25 2016-04-26 Synta Pharmaceuticals Corporation Compuestos contra la inflamación y utilizaciones relacionadas con el sistema inmunitario
JP2008530131A (ja) * 2005-02-15 2008-08-07 ジャズ、ファーマシューティカルズ、インコーポレイテッド 置換ピラジン化合物の徐放のための投薬形態および方法
NL2000284C2 (nl) * 2005-11-04 2007-09-28 Pfizer Ltd Pyrazine-derivaten.
EP1984339A1 (en) * 2006-01-23 2008-10-29 Pfizer Limited Pyridine derivatives as sodium channel modulators
WO2008135830A1 (en) * 2007-05-03 2008-11-13 Pfizer Limited N- [6-amino-s- (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
PL3468972T3 (pl) 2016-06-14 2020-11-16 Novartis Ag Związki i kompozycje do hamowania aktywności shp2
US11986451B1 (en) 2016-07-22 2024-05-21 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
US11504347B1 (en) 2016-07-22 2022-11-22 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
US11602512B1 (en) 2016-07-22 2023-03-14 Flamel Ireland Limited Modified release gamma-hydroxybutyrate formulations having improved pharmacokinetics
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
BR112021013766A2 (pt) 2019-03-01 2021-09-21 Flamel Ireland Limited Composições de gama-hidroxibutirato com farmacocinética melhorada no estado alimentado
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
CN115611700B (zh) * 2022-10-11 2024-06-14 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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EP0288431B1 (de) 1987-04-07 1992-08-19 Ciba-Geigy Ag 3H-1,2,3-Triazolo[4,5-d]pyrimidine
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
SK117399A3 (en) 2000-06-12
CZ311199A3 (cs) 2000-02-16
GT199800046A (es) 1999-08-20
BR9807814A (pt) 2000-02-22
TW513416B (en) 2002-12-11
IL131293A (en) 2003-07-31
MY118612A (en) 2004-12-31
DE69818643T2 (de) 2004-10-07
PA8448201A1 (es) 2000-05-24
KR100544263B1 (ko) 2006-01-23
NZ337121A (en) 2001-03-30
BG103723A (bg) 2001-05-31
JO2035B1 (en) 1999-05-15
EP0966448A1 (en) 1999-12-29
NO313383B1 (no) 2002-09-23
WO1998038174A1 (en) 1998-09-03
MA26473A1 (fr) 2004-12-20
TR199902082T2 (xx) 2000-04-21
PL192864B1 (pl) 2006-12-29
CZ295618B6 (cs) 2005-09-14
PL335441A1 (en) 2000-04-25
DK0966448T3 (da) 2004-02-02
IL131293A0 (en) 2001-01-28
EE9900376A (et) 2000-04-17
HUP0001802A3 (en) 2001-07-30
AU732915B2 (en) 2001-05-03
AP9901632A0 (en) 1999-09-30
PT966448E (pt) 2004-02-27
BR9807814B1 (pt) 2009-01-13
DE69818643D1 (de) 2003-11-06
HUP0001802A2 (hu) 2001-05-28
HK1023116A1 (en) 2000-09-01
YU40799A (sh) 2001-09-28
US20020169172A1 (en) 2002-11-14
HN1998000036A (es) 1999-08-23
CA2282585A1 (en) 1998-09-03
CN1105111C (zh) 2003-04-09
IS5163A (is) 1999-08-24
EP0966448B1 (en) 2003-10-01
KR20000075859A (ko) 2000-12-26
GEP20012555B (en) 2001-10-25
SV1998000029A (es) 1998-12-11
ES2205469T3 (es) 2004-05-01
UY24911A1 (es) 2000-12-29
HU225852B1 (en) 2007-11-28
HRP980107A2 (en) 1998-12-31
CN1253551A (zh) 2000-05-17
US6599905B2 (en) 2003-07-29
CA2282585C (en) 2006-06-06
JP3369189B2 (ja) 2003-01-20
PE58299A1 (es) 1999-06-23
OA11151A (en) 2003-04-22
JP2000511203A (ja) 2000-08-29
NO994213D0 (no) 1999-08-31
HN1999000019A (es) 1999-08-23
ATE251143T1 (de) 2003-10-15
ID22850A (id) 1999-12-09
AR011174A1 (es) 2000-08-02
EA199900687A1 (ru) 2000-04-24
US6255307B1 (en) 2001-07-03
SI0966448T1 (en) 2004-04-30
AU6823798A (en) 1998-09-18
EA002102B1 (ru) 2001-12-24
NO994213L (no) 1999-10-29

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