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AR091176A1 - Pirrodilina-2-carboxamidas sustituidas - Google Patents

Pirrodilina-2-carboxamidas sustituidas

Info

Publication number
AR091176A1
AR091176A1 ARP130101851A AR091176A1 AR 091176 A1 AR091176 A1 AR 091176A1 AR P130101851 A ARP130101851 A AR P130101851A AR 091176 A1 AR091176 A1 AR 091176A1
Authority
AR
Argentina
Prior art keywords
substituted
och2ch2
group
och2c
cycloalkenyl
Prior art date
Application number
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR091176A1 publication Critical patent/AR091176A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H13/00Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
    • C07H13/02Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
    • C07H13/08Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to carbocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Métodos para la obtención de los compuestos así como el uso de tales compuestos como antagonistas de MDM2. Reivindicación 1: Un compuesto de la fórmula (1) en la que: X se elige entre el grupo formado por H, F, Cl, Br, I, ciano, nitro, etinilo, ciclopropilo, metilo, etilo, isopropilo, vinilo y metoxi; Y es de uno a cuatro grupos elegidos con independencia entre el grupo formado por -H, -F, -Cl, -Br, -I, -CN, -OH, nitro, alquilo inferior, cicloalquilo, alcoxi inferior, alquenilo inferior, cicloalquenilo y alquinilo inferior; Z es alcoxi inferior; R¹ se elige entre el grupo formado por alquilo inferior, alquilo inferior sustituido, alquenilo inferior, alquenilo inferior sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, heterociclo, heterociclo sustituido, cicloalquilo, cicloalquilo sustituido, cicloalquenilo y cicloalquenilo sustituido; R² es un fenilo sustituido elegido entre los restos del grupo de fórmulas (2); W es -F, -Cl o -Br; V es -H o -F; R³ se elige entre el grupo formado por alcoxi inferior, alcoxi inferior sustituido, alquilamino, dialquilamino, ácido glucurónico, hexosas, aminohexosas, piranosas, aminoglicósidos, aminoácidos naturales y no naturales, -OCH₂C(O)N(CH₃)₂, -(OCH₂CH₂)ₙ-OH, -(OCH₂CH₂)ₙ-OCH₃, -(OCH₂CH₂)ₙ-OP(O)(OR⁴)₂, -OCH₂-C(O)-(OCH₂CH₂)ₙ-OH, -OCH₂C(O)-(OCH₂CH₂)ₙ-OCH₃, -NH(CH₂-CH₂O)ₙ-CH₃, -NH(CH₂CH₂O)ₙ-H, -OCH₂C(O)NH(CH₂CH₂O)ₙ-CH₃, -O-R⁵, -OCH₂-R⁵, OCH₂CH₂-R⁵, -OCH₂C(O)-R⁵, -NH(OCH₂CH₂)ₙ-NH₂ y -OCH₂CH₂-aminoácido, en los que n es un número de 3 a 80; R⁴ es hidrógeno o bencilo; R⁵ se elige entre el grupo formado por los heterociclos, heterociclos sustituidos, dialquilamino, alquilamino y aminoalquilalcoholes; o una sal o éster farmacéuticamente aceptable de los mismos.
ARP130101851 2012-05-30 2013-05-28 Pirrodilina-2-carboxamidas sustituidas AR091176A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201261653133P 2012-05-30 2012-05-30

Publications (1)

Publication Number Publication Date
AR091176A1 true AR091176A1 (es) 2015-01-14

Family

ID=48536854

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101851 AR091176A1 (es) 2012-05-30 2013-05-28 Pirrodilina-2-carboxamidas sustituidas

Country Status (17)

Country Link
US (1) US9371280B2 (es)
EP (1) EP2854800B1 (es)
JP (1) JP6067108B2 (es)
KR (1) KR101714856B1 (es)
CN (2) CN104349774A (es)
AR (1) AR091176A1 (es)
AU (1) AU2013269798A1 (es)
BR (1) BR112014029530A2 (es)
CA (1) CA2869101A1 (es)
HK (2) HK1201200A1 (es)
IL (1) IL235019A0 (es)
MX (1) MX2014014229A (es)
NZ (1) NZ631477A (es)
RU (1) RU2014150492A (es)
SG (1) SG11201406889WA (es)
WO (1) WO2013178570A1 (es)
ZA (1) ZA201407694B (es)

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US8993614B2 (en) * 2012-03-15 2015-03-31 F. Hoffmann-La Roche Ag Substituted pyrrolidine-2-carboxamides
GB201311888D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compounds
GB201311891D0 (en) 2013-07-03 2013-08-14 Glaxosmithkline Ip Dev Ltd Novel compound
US20180228907A1 (en) 2014-04-14 2018-08-16 Arvinas, Inc. Cereblon ligands and bifunctional compounds comprising the same
MA39877A (fr) * 2014-04-15 2017-02-22 Hoffmann La Roche Formes solides d'un composé pharmaceutiquement actif
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
BR112017015497A2 (pt) 2015-01-20 2018-01-30 Arvinas, Inc. composto, e, composição
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
BR112017028394A2 (pt) * 2015-07-10 2018-08-28 Arvinas Inc composto, composição, e, métodos para induzir a degradação de uma proteína-alvo em uma célula e para tratar um estado doente ou uma condição doente.
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WO2017201449A1 (en) 2016-05-20 2017-11-23 Genentech, Inc. Protac antibody conjugates and methods of use
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MX2019005007A (es) 2016-11-01 2019-07-18 Arvinas Inc Protac dirigidos a la proteína tau y métodos asociados de uso.
PL3689868T3 (pl) 2016-12-01 2024-03-11 Arvinas Operations, Inc. Pochodne tetrahydronaftalenu i tetrahydroizochinoliny jako degradery receptorów estrogenowych
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BR112019015312A2 (pt) 2017-01-26 2020-03-10 Arvinas Operations, Inc. Moduladores da proteólise pelo receptor de estrogênio e métodos de uso associados
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UA130303C2 (uk) 2019-12-06 2026-01-14 Вертекс Фармасьютикалз Інкорпорейтед Заміщені тетрагідрофурани як модулятори натрієвих каналів
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Also Published As

Publication number Publication date
KR20150013215A (ko) 2015-02-04
JP6067108B2 (ja) 2017-01-25
KR101714856B1 (ko) 2017-03-09
HK1201200A1 (en) 2015-08-28
AU2013269798A1 (en) 2014-10-02
MX2014014229A (es) 2015-02-17
US20130324531A1 (en) 2013-12-05
US9371280B2 (en) 2016-06-21
IL235019A0 (en) 2014-12-31
HK1248702A1 (zh) 2018-10-19
CN104349774A (zh) 2015-02-11
SG11201406889WA (en) 2015-02-27
RU2014150492A (ru) 2016-07-20
BR112014029530A2 (pt) 2017-06-27
CA2869101A1 (en) 2013-12-05
EP2854800B1 (en) 2018-03-28
JP2015519351A (ja) 2015-07-09
NZ631477A (en) 2016-12-23
ZA201407694B (en) 2015-05-27
CN107540594A (zh) 2018-01-05
EP2854800A1 (en) 2015-04-08
WO2013178570A1 (en) 2013-12-05

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