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AR063101A1 - Derivados de pirazina-2-carboxiamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento o profilaxis de enfermedades asociadas con la modulacion de receptores del cb2. - Google Patents

Derivados de pirazina-2-carboxiamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento o profilaxis de enfermedades asociadas con la modulacion de receptores del cb2.

Info

Publication number
AR063101A1
AR063101A1 ARP070104363A ARP070104363A AR063101A1 AR 063101 A1 AR063101 A1 AR 063101A1 AR P070104363 A ARP070104363 A AR P070104363A AR P070104363 A ARP070104363 A AR P070104363A AR 063101 A1 AR063101 A1 AR 063101A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
group
formula
heterocyclic ring
chosen
Prior art date
Application number
ARP070104363A
Other languages
English (en)
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=39166552&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR063101(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR063101A1 publication Critical patent/AR063101A1/es

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    • 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
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos son utiles para el tratamiento y/o profilaxis de enfermedades asociadas con la modulacion de receptores del CB2. Se proveen además, composiciones farmacéuticas que los contienen. Reivindicacion 1: Compuestos de la formula general (1) en la que se elige entre el grupo formado por alquilo inferior, hidroxialquilo inferior, cicloalquilo que está sin sustituir o sustituido con un grupo elegido entre hidroxi, alcoxi inferior e hidroxialquilo inferior, cicloalquilalquilo inferior, heterociclilalquilo inferior, -CR5R6-COOR7 y -CR5R6-CONH2; R5 y R6 con independencia entre sí son hidrogeno o alquilo inferior; R7 es alquilo inferior; R2 es hidrogeno; o R1 y R2 junto con el átomo de nitrogeno al que están unidos forman un anillo heterocíclico de 4, 5, 6 o 7 eslabones que contiene opcionalmente otro heteroátomo elegido entre nitrogeno, oxígeno o azufre; uno de R3 o R4 se elige entre el grupo formado por alquilamino inferior, di(alquilo inferior)amino, cicloalquilamino.y halogenofenilo, o es un anillo heterocíclico elegido entre azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, tiomorfolinilo y azepanilo, dicho anillo heterocíclico está sin sustituir o sustituido con halogeno; y el otro de R3 o R4 es -OR8 o - NRR10, en los que R8 se elige entre el grupo formado por alquilo inferior, halogenoalquilo inferior, cicloalquilo, cicloalquilalquilo inferior, fenilalquilo inferior, dicho fenilo está sin sustituir o sustituido con un grupo elegido entre alquilo inferior, alcoxi inferior y halogeno, heterociclilalquilo inferior, heteroarilalquilo inferior, alcoxialquilo inferior e hidroxialquilo inferior; R9 es alquilo inferior y R10 es alquilo inferior o alcoxialquilo inferior; o bien en el caso de que uno de R3 o R4 sea halogenofenilo, R9 y R10 junto con el átomo de nitrogeno al que están unidos pueden formar también un anillo heterocíclico elegido entre pirrolidinilo y piperidinilo; y sus sales farmacéuticamente aceptables. 19. Un proceso de obtencion de los compuestos de la formula 1 ya definida en una cualquiera de las reivindicaciones de 1 a 18, dicho proceso consiste en: hacer reaccionar un compuesto de la formula (2) en la que R3 y R4 tienen los significados definidos en la reivindicacion 1, con una amina de la formula H-NR1R2 en la que R1 y R2 tienen los significados definidos en la reivindicacion 1, con la intervencion de un agente de adicion, en condiciones básicas, y, si se desea, convertir el compuesto resultante de la formula 1 en una sal farmacéuticamente aceptable.
ARP070104363A 2006-10-04 2007-10-02 Derivados de pirazina-2-carboxiamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento o profilaxis de enfermedades asociadas con la modulacion de receptores del cb2. AR063101A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06121749 2006-10-04

Publications (1)

Publication Number Publication Date
AR063101A1 true AR063101A1 (es) 2008-12-30

Family

ID=39166552

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP070104363A AR063101A1 (es) 2006-10-04 2007-10-02 Derivados de pirazina-2-carboxiamida, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en la preparacion de medicamentos para el tratamiento o profilaxis de enfermedades asociadas con la modulacion de receptores del cb2.

Country Status (18)

Country Link
US (1) US7691863B2 (es)
EP (1) EP2076499B1 (es)
JP (1) JP5064506B2 (es)
KR (1) KR101114704B1 (es)
CN (1) CN101522644B (es)
AR (1) AR063101A1 (es)
AT (1) ATE467622T1 (es)
AU (1) AU2007304363B2 (es)
BR (1) BRPI0717822A2 (es)
CA (1) CA2664621A1 (es)
CL (1) CL2007002834A1 (es)
DE (1) DE602007006531D1 (es)
ES (1) ES2344128T3 (es)
IL (1) IL197763A0 (es)
MX (1) MX2009003316A (es)
PE (1) PE20080855A1 (es)
TW (1) TW200825065A (es)
WO (1) WO2008040649A2 (es)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7629346B2 (en) * 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
US7781593B2 (en) 2006-09-14 2010-08-24 Hoffmann-La Roche Inc. 5-phenyl-nicotinamide derivatives
AU2007304365A1 (en) * 2006-10-04 2008-04-10 F. Hoffmann-La Roche Ag 3-pyridinecarboxamide and 2-pyrazinecarboxamide derivatives as HDL-cholesterol raising agents
US8088920B2 (en) 2008-03-31 2012-01-03 Hoffmann-La Roche Inc. 3-trifluoromethyl-pyrazine-2-carboxylic acid amide derivatives as HDL-cholesterol raising agents
US7897621B2 (en) 2008-03-31 2011-03-01 Hoffmann-La Roche Inc. 2-trifluoromethylnicotinamide derivatives as HDL-cholesterol raising agents
US8354441B2 (en) 2009-11-11 2013-01-15 Hoffmann-La Roche Inc. Oxazoline derivatives
WO2012031817A1 (en) 2010-09-09 2012-03-15 F. Hoffmann-La Roche Ag Determination of abca1 protein levels in cells
US8410107B2 (en) 2010-10-15 2013-04-02 Hoffmann-La Roche Inc. N-pyridin-3-yl or N-pyrazin-2-yl carboxamides
US8669254B2 (en) 2010-12-15 2014-03-11 Hoffman-La Roche Inc. Pyridine, pyridazine, pyrimidine or pyrazine carboxamides as HDL-cholesterol raising agents
US9321727B2 (en) 2011-06-10 2016-04-26 Hoffmann-La Roche Inc. Pyridine derivatives as agonists of the CB2 receptor
US9403808B2 (en) * 2011-10-28 2016-08-02 Hoffmann-La Roche Inc. Pyrazine derivatives
CN104837831B (zh) * 2012-12-07 2017-10-31 霍夫曼-拉罗奇有限公司 新的吡啶衍生物
RS56424B1 (sr) * 2012-12-07 2018-01-31 Hoffmann La Roche Piridin-2-amidi korisni kao cb2-agonisti
CA2885987A1 (en) * 2012-12-07 2014-06-12 F. Hoffmann-La Roche Ag Pyridine-2-amides useful as cb2 agonists
US9512141B2 (en) * 2012-12-07 2016-12-06 Hoffmann-La Roche Inc. Pyrazine derivatives as CB2 receptor agonists
SG11201608246VA (en) * 2014-04-04 2016-10-28 Hoffmann La Roche 5,6-disubstituted pyridine-2-carboxamides as cannabinoid receptor agonists
JP6751203B2 (ja) 2016-06-07 2020-09-02 ジャコバイオ ファーマスーティカルズ カンパニー リミテッドJacobio Pharmaceuticals Co., Ltd. Shp2阻害剤として有用な新規複素環式誘導体
SG11201908820VA (en) 2017-03-23 2019-10-30 Jacobio Pharmaceuticals Co Ltd Novel heterocyclic derivatives useful as shp2 inhibitors
CN109384734B (zh) * 2017-08-14 2023-04-11 上海科胜药物研发有限公司 一种塞尔西帕中间体的制备方法
EP3814337B1 (en) * 2018-06-27 2025-05-14 F. Hoffmann-La Roche AG Pyridine and pyrazine derivatives as preferential cannabinoid 2 agonists
SG11202009103WA (en) * 2018-06-27 2020-10-29 Hoffmann La Roche Novel pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
EP3814328A1 (en) 2018-06-27 2021-05-05 F. Hoffmann-La Roche AG Novel azetidine-substituted pyridine and pyrazine compounds as inhibitors of cannabinoid receptor 2
WO2020002314A1 (en) 2018-06-27 2020-01-02 F. Hoffmann-La Roche Ag Radiolabeled cannabinoid receptor 2 ligand
WO2020063760A1 (en) 2018-09-26 2020-04-02 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
WO2023082145A1 (en) * 2021-11-11 2023-05-19 4B Technologies (Suzhou) Limited Intermediate compound of quinoxaline and preparation process thereof

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US7629346B2 (en) * 2006-06-19 2009-12-08 Hoffmann-La Roche Inc. Pyrazinecarboxamide derivatives as CB1 antagonists
US7781593B2 (en) 2006-09-14 2010-08-24 Hoffmann-La Roche Inc. 5-phenyl-nicotinamide derivatives

Also Published As

Publication number Publication date
AU2007304363A1 (en) 2008-04-10
AU2007304363B2 (en) 2013-01-17
WO2008040649A3 (en) 2008-05-29
CL2007002834A1 (es) 2008-05-16
TW200825065A (en) 2008-06-16
CN101522644B (zh) 2013-04-24
KR20090084842A (ko) 2009-08-05
EP2076499A2 (en) 2009-07-08
MX2009003316A (es) 2009-04-09
KR101114704B1 (ko) 2012-03-14
JP2010505788A (ja) 2010-02-25
ATE467622T1 (de) 2010-05-15
BRPI0717822A2 (pt) 2013-11-12
ES2344128T3 (es) 2010-08-18
DE602007006531D1 (de) 2010-06-24
US7691863B2 (en) 2010-04-06
CA2664621A1 (en) 2008-04-10
IL197763A0 (en) 2009-12-24
EP2076499B1 (en) 2010-05-12
CN101522644A (zh) 2009-09-02
US20080085905A1 (en) 2008-04-10
JP5064506B2 (ja) 2012-10-31
WO2008040649A2 (en) 2008-04-10
PE20080855A1 (es) 2008-06-28

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