AR117229A1 - Compuestos heteroaromáticos como inhibidores de vanina - Google Patents

Compuestos heteroaromáticos como inhibidores de vanina

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Publication number
AR117229A1
AR117229A1 ARP190103518A ARP190103518A AR117229A1 AR 117229 A1 AR117229 A1 AR 117229A1 AR P190103518 A ARP190103518 A AR P190103518A AR P190103518 A ARP190103518 A AR P190103518A AR 117229 A1 AR117229 A1 AR 117229A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
membered
optionally substituted
cycloalkyl
Prior art date
Application number
ARP190103518A
Other languages
English (en)
Inventor
Hannes Fiepko Koolman
Cdrickx Godbout
Martin Thomas Fleck
Original Assignee
Boehringer Ingelheim Int
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 Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR117229A1 publication Critical patent/AR117229A1/es

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    • 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/44Iso-indoles; Hydrogenated iso-indoles
    • C07D209/48Iso-indoles; Hydrogenated iso-indoles with oxygen atoms in positions 1 and 3, e.g. phthalimide
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D211/78Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • 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
    • 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • 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
    • C07D409/14Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/056Triazole or tetrazole radicals

Abstract

Los compuestos de la fórmula (1), que son adecuados para el tratamiento de enfermedades relacionadas con vanina, y los procesos para fabricar estos compuestos, las preparaciones farmacéuticas que contienen estos compuestos y sus métodos de uso. Reivindicación 1: Un compuesto caracterizado por la fórmula (1), o una sal de este aceptable desde el punto de vista farmacéutico, en donde n indica 1 ó 2; R¹, R² y R³ se seleccionan, independientemente entre sí, del grupo que consiste en C₁₋₄-alquilo opcionalmente sustituido con hidroxi, CH₃-O-, CH₃-SO₂-, fenil-CH₂- opcionalmente sustituido con 1 a 3 átomos de halógeno y heteroaril-C₁₋₂- alquil- de 5 - 6 miembros, o R² y R³ juntos forman un carbociclo de 3 - 6 miembros o un heterociclilo de 4 - 6 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N y O; o R¹, R² y R³ juntos pueden formar un carbociclo bicíclico de 5 - 8 miembros o un heterociclilo bicíclico de 6 - 8 miembros que contiene un heteroátomo seleccionado del grupo que consiste en N y O; en donde, en la definición de R¹, R² y R³ mencionada, alquilo, cicloalquilo, heteroarilo y heterociclilo se sustituyen opcionalmente con 1 a 3 átomos de halógeno; R⁴ indica R⁴.¹R⁴.²N-, heteroarilo de 5 - 6 miembros, NC- o heterociclilo de 5 - 6 miembros; o R⁴ indica un grupo de la fórmula R⁴.ᵃ o R⁴.ᵇ en donde X indica CH₂, -NRX u O; en donde RX indica H o C₁₋₃-alquilo; R⁴.ᵃ y R⁴.ᵇ, independientemente entre sí, se sustituyen opcionalmente con metilo; R⁴.¹ se selecciona del grupo que consiste en C₁₋₄-alquil-CO- opcionalmente sustituido con 1 - 3 átomos de F, C₃₋₄-cicloalquilo o C₁₋₂-alcoxi, C₃₋₅-cicloalquil-CO- sustituido con R⁴.¹.¹ y R⁴.¹.², heterociclil-CO- de 4 - 6 miembros sustituido con R⁴.¹.³ y R⁴.¹.⁴, heterociclil-CH₂-CO- de 4 - 6 miembros, heteroaril-CO- de 5 - 6 miembros opcionalmente sustituido con 1 átomo de halógeno, H₃C-O- o 1 a 2 metilo, fenil-CO- sustituido con R⁴.¹.⁵ y R⁴.¹.⁶, (C₁₋₃-alquil)(C₁₋₃alquil)N-CO- y heteroarilo de 5 - 6 miembros; en donde R⁴.¹.¹, R⁴.¹.² se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, F, CF₃ y -CN; R⁴.¹.³, R⁴.¹.⁴ se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, F, CF₃ y -CN; R⁴.¹.⁵, R⁴.¹.⁶ se seleccionan, independientemente entre sí, del grupo que consiste en H, -CH₃, F, CF₃ y -CN; R⁴.² se selecciona del grupo que consiste en H, C₁₋₄-alquilo, C₃₋₄-cicloalquilo, C₃₋₄-cicloalquil-C₁₋₂-alquil- y fenil-C₁₋₂-alquil-; en donde, en la definición de R⁴.² mencionada, alquilo, cicloalquilo y fenilo se sustituyen opcionalmente con 1 - 3 átomos de F o un C₁₋₂-alquil-O; R⁵ indica H o C₁₋₂-alquilo; o R⁴ y R⁵ juntos forman un heterociclilo de 4 - 6 miembros que contiene 1 heteroátomo seleccionado del grupo que consiste en N y O; o una sal de aquel aceptable desde el punto de vista farmacéutico.
ARP190103518A 2018-12-03 2019-12-02 Compuestos heteroaromáticos como inhibidores de vanina AR117229A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP18209721 2018-12-03

Publications (1)

Publication Number Publication Date
AR117229A1 true AR117229A1 (es) 2021-07-21

Family

ID=64572152

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP190103518A AR117229A1 (es) 2018-12-03 2019-12-02 Compuestos heteroaromáticos como inhibidores de vanina

Country Status (23)

Country Link
US (3) US11078182B2 (es)
EP (1) EP3891139A1 (es)
JP (2) JP7130873B2 (es)
KR (1) KR20210100150A (es)
CN (2) CN114478485B (es)
AR (1) AR117229A1 (es)
AU (1) AU2019391279A1 (es)
BR (1) BR112021007915A2 (es)
CA (1) CA3116830A1 (es)
CL (2) CL2021001198A1 (es)
CO (1) CO2021007173A2 (es)
CR (1) CR20210294A (es)
DO (1) DOP2021000071A (es)
EA (1) EA202191476A1 (es)
EC (1) ECSP21040278A (es)
IL (1) IL283397A (es)
JO (2) JOP20210128A1 (es)
MA (1) MA54378A (es)
MX (1) MX2021006520A (es)
PE (1) PE20211769A1 (es)
PH (1) PH12021551280A1 (es)
SG (1) SG11202104437XA (es)
WO (1) WO2020114943A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20210478A1 (es) 2018-08-28 2021-03-11 Boehringer Ingelheim Int Compuestos heteroaromaticos como inhibidores de vanina
EP3890828A1 (en) * 2018-12-03 2021-10-13 Boehringer Ingelheim International GmbH Heteroaromatic compounds as vanin inhibitors
JP7130873B2 (ja) 2018-12-03 2022-09-05 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング バニン阻害剤としてのヘテロ芳香族化合物
US20230107927A1 (en) 2020-02-28 2023-04-06 First Wave Bio, Inc. Methods of treating iatrogenic autoimmune colitis
CN116768909A (zh) * 2022-03-18 2023-09-19 上海美悦生物科技发展有限公司 Vanin酶抑制剂的盐型、晶型及其制备方法和应用

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030195192A1 (en) * 2002-04-05 2003-10-16 Fortuna Haviv Nicotinamides having antiangiogenic activity
WO2005035524A1 (en) 2003-10-09 2005-04-21 Abbott Laboratories Pyrrolidinyl urea derivatives as angiogensis inhibitors
CN104703965A (zh) * 2012-09-25 2015-06-10 默克专利股份有限公司 α羟基酰胺
EP3303303A1 (en) 2015-05-29 2018-04-11 Pfizer Inc Novel heterocyclic compounds as inhibitors of vanin-1 enzyme
US10906888B2 (en) 2016-07-14 2021-02-02 Pfizer Inc. Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme
WO2018228934A1 (en) 2017-06-12 2018-12-20 Boehringer Ingelheim International Gmbh Heteroaromatic compounds as vanin inhibitors
PE20210478A1 (es) 2018-08-28 2021-03-11 Boehringer Ingelheim Int Compuestos heteroaromaticos como inhibidores de vanina
PL3891142T3 (pl) * 2018-12-03 2023-01-02 Boehringer Ingelheim International Gmbh Związki heteroaromatyczne jako inhibitory waniny
EP3890828A1 (en) * 2018-12-03 2021-10-13 Boehringer Ingelheim International GmbH Heteroaromatic compounds as vanin inhibitors
JP7130873B2 (ja) 2018-12-03 2022-09-05 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング バニン阻害剤としてのヘテロ芳香族化合物

Also Published As

Publication number Publication date
EA202191476A1 (ru) 2021-10-26
CL2021001198A1 (es) 2021-12-24
EP3891139A1 (en) 2021-10-13
SG11202104437XA (en) 2021-05-28
WO2020114943A1 (en) 2020-06-11
PH12021551280A1 (en) 2021-12-06
US20230295112A1 (en) 2023-09-21
BR112021007915A2 (pt) 2021-07-27
US20220048885A1 (en) 2022-02-17
MA54378A (fr) 2022-03-09
CA3116830A1 (en) 2020-06-11
KR20210100150A (ko) 2021-08-13
MX2021006520A (es) 2021-07-07
CN114478485B (zh) 2024-04-05
CN114478485A (zh) 2022-05-13
US20200172508A1 (en) 2020-06-04
CN113166104A (zh) 2021-07-23
JP7130873B2 (ja) 2022-09-05
CL2021003568A1 (es) 2022-11-04
DOP2021000071A (es) 2021-05-31
JOP20210128A1 (ar) 2023-01-30
PE20211769A1 (es) 2021-09-07
TW202039461A (zh) 2020-11-01
JOP20210127A1 (ar) 2023-01-30
IL283397A (en) 2021-07-29
JP2022509317A (ja) 2022-01-20
ECSP21040278A (es) 2021-07-30
CO2021007173A2 (es) 2021-06-21
JP2022188014A (ja) 2022-12-20
CR20210294A (es) 2021-08-13
US11078182B2 (en) 2021-08-03
AU2019391279A1 (en) 2021-05-13

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