AR081832A1 - Derivados de 3,4-dihidropirrolo[1,2-a]pirazina-2,8(1h)-dicarboxamida, su preparacion y su aplicacion en terapeutica - Google Patents

Derivados de 3,4-dihidropirrolo[1,2-a]pirazina-2,8(1h)-dicarboxamida, su preparacion y su aplicacion en terapeutica

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Publication number
AR081832A1
AR081832A1 ARP110101901A ARP110101901A AR081832A1 AR 081832 A1 AR081832 A1 AR 081832A1 AR P110101901 A ARP110101901 A AR P110101901A AR P110101901 A ARP110101901 A AR P110101901A AR 081832 A1 AR081832 A1 AR 081832A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
group
hydroxy
fluoroalkyl
Prior art date
Application number
ARP110101901A
Other languages
English (en)
Inventor
Jean Gibert
Jean-François Gibert
Frank Marguet
Christophe Pacaud
Des Combes Sylvain Cote
Jacques Froissant
Original Assignee
Ravet Antoine
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=42697541&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR081832(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ravet Antoine filed Critical Ravet Antoine
Publication of AR081832A1 publication Critical patent/AR081832A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • 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
    • 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

Landscapes

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

Abstract

Reivindicación 1: Compuestos que responden a la fórmula general (1) en la que R2 representa: un grupo alquilo C1-10, cicloalquil C3-7-alquilo C1-6, alquiltio C1-6-alquilo C1-10, alcoxi C1-6-alquilo C1-10, hidroxi-alquilo C1-10, hidroxi-alquil C1-6-cicloalquilo C3-7-alquilo C1-6, fluoroalquilo C1-10, alquil C1-10-oxiimino-alquilo C1-10; un grupo cicloalquilo C3-10, fluorocicloalquilo C3-10, hidroxi-cicloalquilo C3-10; un grupo cicloalquilo C3-7 que puede estar sustituido con uno o dos grupos elegidos independientemente entre alquilo C1-6, cicloalquilo C3-7, hidroxi, fluoroalquilo C1-10 o alquil C1-10-oxiimino; un grupo heterocíclico que contiene de 3 a 8 átomos de carbono y al menos un heteroátomo elegido entre nitrógeno, oxigeno, azufre y la forma oxidada o dioxidada del azufre, pudiendo estar este grupo heterocíclico sustituido con uno o varios grupos hidroxi, alquilo C1-6, hidroxi-alquilo C1-6, fluoroalquilo C1-6; un grupo alquilo C1-10 sustituido con un grupo heterocíclico que contiene de 3 a 8 átomos de carbono y al menos un heteroátomo elegido entre nitrógeno, oxígeno, azufre y la forma oxidada o dioxidada del azufre, pudiendo estar este grupo heterocíclico sustituido con uno o varios grupos hidroxi, alquilo C1-6, hidroxi-alquilo C1-6, fluoroalquilo C1-6; X6 representa un átomo de hidrógeno, de flúor, de cloro, de bromo o un grupo alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6, fluoroalquilo C1-6 o ciano; R7 representa un grupo fenilo o un grupo naftilo, sustituido opcionalmente con uno o varios sustituyentes X7, idénticos o diferentes, elegidos independientemente; X7 representa: un átomo de halógeno elegido entre el átomo de flúor, cloro o bromo, o un grupo elegido entre: hidroxi; alquilo C1-6, cicloalquilo C3-7, cicloalquil C3-7-alquilo C1-6; hidroxi-alquilo C1-6, hidroxi-cicloalquilo C3-7, hidroxi-cicloalquil C3-7-alquilo C1-6; alcoxi C1-6, cicloalcoxi C3-7, cicloalquil C3-7-alcoxi C1-6; alquiltio C1-6, cicloalquiltio C3-7, cicloalquil C3-7-alquiltio C1-6; arilo, aril-alquilo C1-6; ariloxi, aril-alcoxi C1-6; fluoroalquilo C1-6, fluorocicloalquilo C3-7, fluorocicloalquil C3-7-alquilo C1-6; fluoroalcoxi C1-6, fluorocicloalcoxi C3-7, fluorocicloalquil C3-7-alcoxi C1-6; ciano, ciano-alquilo C1-6, ciano-alcoxi C1-6; NRaRb, NRcCORd, NRcSO2Rd, NRcSO2NRaRb, CONRaRb, CON(ORc)Rd; un grupo heteroarilo, estando los grupos arilo o heteroarilo sustituidos opcionalmente con uno o varios sustituyentes elegidos entre el átomo de flúor, de cloro o de bromo o un grupo alquilo C1-6, cicloalquilo C3-7, alcoxi C1-6, fluoroalquilo C1-6, fluoroalcoxi C1-6 o ciano; Ra y Rb representan independientemente el uno del otro un átomo de hidrógeno o un grupo alquilo C1-6, cicloalquilo C3-7 o cicloalquil C3-7-alquilo C1-6, o bien forman con el átomo al que están unidos un ciclo elegido entre azetidina, pirrolidina, piperidina, morfolina, tiomorfolina, azepina, piperazina, estando este ciclo sustituido opcionalmente con uno o varios grupos alquilo C1-6; Rc y Rd representan independientemente el uno del otro un átomo de hidrógeno o un grupo alquilo C1-6, cicloalquilo C3-7 o cicloalquil C3-7-alquilo C1-6; en el estado de base o de sal de adición a un ácido.
ARP110101901A 2010-06-03 2011-06-02 Derivados de 3,4-dihidropirrolo[1,2-a]pirazina-2,8(1h)-dicarboxamida, su preparacion y su aplicacion en terapeutica AR081832A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
FR1054372A FR2960876B1 (fr) 2010-06-03 2010-06-03 Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique.

Publications (1)

Publication Number Publication Date
AR081832A1 true AR081832A1 (es) 2012-10-24

Family

ID=42697541

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110101901A AR081832A1 (es) 2010-06-03 2011-06-02 Derivados de 3,4-dihidropirrolo[1,2-a]pirazina-2,8(1h)-dicarboxamida, su preparacion y su aplicacion en terapeutica

Country Status (38)

Country Link
US (2) US8791119B2 (es)
EP (1) EP2588480B1 (es)
JP (1) JP5995841B2 (es)
KR (1) KR20130113928A (es)
CN (1) CN103168041B (es)
AR (1) AR081832A1 (es)
AU (1) AU2011268651B2 (es)
BR (1) BR112012030697A2 (es)
CA (1) CA2801154C (es)
CL (1) CL2012003360A1 (es)
CO (1) CO6602113A2 (es)
CR (1) CR20120595A (es)
CY (1) CY1118512T1 (es)
DK (1) DK2588480T3 (es)
DO (1) DOP2012000296A (es)
EA (1) EA201291364A1 (es)
EC (1) ECSP12012322A (es)
ES (1) ES2603420T3 (es)
FR (1) FR2960876B1 (es)
GT (1) GT201200319A (es)
HR (1) HRP20161494T1 (es)
HU (1) HUE030650T2 (es)
IL (1) IL223364A (es)
LT (1) LT2588480T (es)
MA (1) MA34360B1 (es)
MX (1) MX2012014084A (es)
NI (1) NI201200176A (es)
NZ (1) NZ603947A (es)
PE (1) PE20130259A1 (es)
PL (1) PL2588480T3 (es)
PT (1) PT2588480T (es)
SG (1) SG186143A1 (es)
SI (1) SI2588480T1 (es)
TN (1) TN2012000520A1 (es)
TW (1) TWI487707B (es)
UY (1) UY33428A (es)
WO (1) WO2011161537A2 (es)
ZA (1) ZA201209071B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2960876B1 (fr) * 2010-06-03 2012-07-27 Sanofi Aventis Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique.
UY35834A (es) * 2013-11-14 2015-05-29 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon
JP6307989B2 (ja) * 2014-04-02 2018-04-11 住友化学株式会社 塩、酸発生剤、レジスト組成物及びレジストパターンの製造方法
CN110709523B (zh) * 2017-04-12 2023-07-11 豪夫迈·罗氏有限公司 使用经pictet spengler反应获得的加标签的核苷的测序反应方法
JP2020528062A (ja) * 2017-07-27 2020-09-17 江蘇恒瑞医薬股▲ふん▼有限公司 ピペラジンヘテロアリール誘導体、その製造方法、およびその医薬での使用
TW202412758A (zh) * 2022-06-29 2024-04-01 香港商英矽智能科技知識產權有限公司 Fgfr2與fgfr3抑制劑及其用途

Family Cites Families (10)

* Cited by examiner, † Cited by third party
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EP1150991B1 (en) 1999-02-01 2004-04-07 University of Virginia Patent Foundation Compositions for treating inflammatory response
MXPA04002243A (es) * 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.
GB0202015D0 (en) * 2002-01-29 2002-03-13 Hoffmann La Roche Piperazine Derivatives
ATE428711T1 (de) 2003-12-11 2009-05-15 Aventis Pharma Inc Substituierte 1h-pyrroloä3,2-b, 3,2-c und 2,3- cüpyridin-2-carbonsäureamide und verwandte analoga als inhibitoren von caseinkinase-i- epsilon
GB0328900D0 (en) 2003-12-12 2004-01-14 Glaxo Group Ltd Novel compounds
US8304408B2 (en) * 2007-05-24 2012-11-06 The Regents Of The University Of California Wnt signaling inhibitors, and methods for making and using them
NZ582871A (en) 2007-07-27 2011-09-30 Sanofi Aventis 1,2,3,4-Tetrahydropyrrolo[1,2-a]pyrazine-6-carboxamide and 2,3,4,5- tetrahydropyrrolo[1,2-a][1,4]-diazepine-7-carboxamide derivatives, preparation and therapeutic use thereof
EP2229395A1 (en) * 2008-01-17 2010-09-22 Grünenthal GmbH Substituted sulfonamide derivatives
WO2009097515A2 (en) * 2008-01-30 2009-08-06 Wyeth [a]-fused indole compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses
FR2960876B1 (fr) * 2010-06-03 2012-07-27 Sanofi Aventis Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique.

Also Published As

Publication number Publication date
CN103168041B (zh) 2015-08-26
MA34360B1 (fr) 2013-07-03
CO6602113A2 (es) 2013-01-18
CA2801154A1 (en) 2011-12-29
ECSP12012322A (es) 2013-03-28
CL2012003360A1 (es) 2013-04-01
US9233965B2 (en) 2016-01-12
SG186143A1 (en) 2013-01-30
DK2588480T3 (en) 2016-12-12
EA201291364A1 (ru) 2013-05-30
HRP20161494T1 (hr) 2016-12-16
AU2011268651A1 (en) 2012-12-20
PL2588480T3 (pl) 2017-08-31
NI201200176A (es) 2013-02-06
TWI487707B (zh) 2015-06-11
FR2960876A1 (fr) 2011-12-09
SI2588480T1 (sl) 2016-12-30
DOP2012000296A (es) 2013-02-28
CA2801154C (en) 2018-01-09
KR20130113928A (ko) 2013-10-16
JP2013527226A (ja) 2013-06-27
UY33428A (es) 2011-12-30
TN2012000520A1 (en) 2014-04-01
PE20130259A1 (es) 2013-03-22
US8791119B2 (en) 2014-07-29
CN103168041A (zh) 2013-06-19
AU2011268651B2 (en) 2016-09-01
GT201200319A (es) 2014-01-17
FR2960876B1 (fr) 2012-07-27
MX2012014084A (es) 2013-01-29
TW201202248A (en) 2012-01-16
HUE030650T2 (en) 2017-05-29
CY1118512T1 (el) 2017-07-12
CR20120595A (es) 2013-01-03
PT2588480T (pt) 2016-11-21
WO2011161537A2 (en) 2011-12-29
WO2011161537A3 (en) 2012-03-01
EP2588480B1 (en) 2016-08-17
US20140336189A1 (en) 2014-11-13
ES2603420T3 (es) 2017-02-27
NZ603947A (en) 2014-12-24
BR112012030697A2 (pt) 2019-09-24
EP2588480A2 (en) 2013-05-08
LT2588480T (lt) 2016-12-12
ZA201209071B (en) 2014-02-26
US20130090340A1 (en) 2013-04-11
IL223364A (en) 2015-06-30
JP5995841B2 (ja) 2016-09-21

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