CO2021001217A2 - Inhibidores tipo indol y azaindol de enzimas pad - Google Patents

Inhibidores tipo indol y azaindol de enzimas pad

Info

Publication number
CO2021001217A2
CO2021001217A2 CONC2021/0001217A CO2021001217A CO2021001217A2 CO 2021001217 A2 CO2021001217 A2 CO 2021001217A2 CO 2021001217 A CO2021001217 A CO 2021001217A CO 2021001217 A2 CO2021001217 A2 CO 2021001217A2
Authority
CO
Colombia
Prior art keywords
indole
inhibitors
pad enzymes
azaindole
azaindole inhibitors
Prior art date
Application number
CONC2021/0001217A
Other languages
English (en)
Inventor
Anurag S Srivastava
Khehyong Ngu
Robert J Cherney
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CO2021001217A2 publication Critical patent/CO2021001217A2/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

La presente invención proporciona compuestos de la Fórmula (I) útiles como inhibidores de PAD4, composiciones de los mismos y métodos para tratar trastornos relacionados con PAD4., (I) en donde cada uno de Anillo A, L, Q, R1, R2, R3, R4, R7, y R8 junto con otras variables son como se definen en la presente.
CONC2021/0001217A 2018-08-08 2021-02-03 Inhibidores tipo indol y azaindol de enzimas pad CO2021001217A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201862715850P 2018-08-08 2018-08-08
PCT/US2019/045466 WO2020033520A1 (en) 2018-08-08 2019-08-07 Indole and azaindole inhibitors of pad enzymes

Publications (1)

Publication Number Publication Date
CO2021001217A2 true CO2021001217A2 (es) 2021-02-26

Family

ID=67766306

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2021/0001217A CO2021001217A2 (es) 2018-08-08 2021-02-03 Inhibidores tipo indol y azaindol de enzimas pad

Country Status (18)

Country Link
US (1) US11524959B1 (es)
EP (1) EP3833440A1 (es)
JP (1) JP2021534108A (es)
KR (1) KR20210042934A (es)
CN (1) CN112805067A (es)
AR (1) AR115920A1 (es)
AU (1) AU2019319835A1 (es)
BR (1) BR112021002091A2 (es)
CA (1) CA3108791A1 (es)
CL (1) CL2021000296A1 (es)
CO (1) CO2021001217A2 (es)
EA (1) EA202190462A1 (es)
IL (1) IL280650A (es)
MX (1) MX2021001565A (es)
PE (1) PE20211068A1 (es)
SG (1) SG11202101174RA (es)
TW (1) TW202019415A (es)
WO (1) WO2020033520A1 (es)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA202190462A1 (ru) 2018-08-08 2021-06-03 Бристол-Маерс Сквибб Компани Индольные и азаиндольные ингибиторы ферментов pad
PE20230488A1 (es) * 2020-04-30 2023-03-21 Gilead Sciences Inc Inhibidores macrociclicos de las peptidilarginina deiminasas
CN111943947B (zh) * 2020-07-24 2021-04-30 重庆文理学院 1H-吡咯[2,3-b]吡啶衍生物及其合成方法与应用
WO2022140390A1 (en) * 2020-12-22 2022-06-30 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
WO2022140428A2 (en) * 2020-12-22 2022-06-30 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2877467T3 (pl) * 2012-07-26 2017-08-31 Glaxo Group Limited 2-(azaindolo-2-ylo)benzoimidazole jako inhibitory pad4
CN107849015B (zh) 2015-05-21 2021-03-19 葛兰素知识产权发展有限公司 作为pad4抑制剂的苯并咪唑衍生物
AR107032A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
AR107030A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
KR20180098593A (ko) 2015-12-22 2018-09-04 칸세라 아베 포유류의 히스톤 탈아세틸화효소 활성에 대한 저해제로서 유용한 바이사이클릭 하이드록사믹산
EP3419969B1 (en) 2016-02-23 2019-12-18 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
EP3490989B1 (en) 2016-07-27 2020-09-09 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
JP7118951B2 (ja) 2016-09-12 2022-08-16 パドロック・セラピューティクス・インコーポレイテッド Ｐａｄ４のヘテロアリール阻害剤
CN117343049A (zh) 2017-06-30 2024-01-05 北京泰德制药股份有限公司 Rho相关蛋白激酶抑制剂、包含其的药物组合物及其制备方法和用途
HUE061607T2 (hu) 2017-10-18 2023-07-28 Jubilant Epipad LLC Imidazopiridin vegyületek mint PAD inhibitorok
JP7447080B2 (ja) 2018-08-08 2024-03-11 ブリストル－マイヤーズ スクイブ カンパニー Ｐａｄ４阻害剤としての置換チエノピロール
EA202190462A1 (ru) 2018-08-08 2021-06-03 Бристол-Маерс Сквибб Компани Индольные и азаиндольные ингибиторы ферментов pad
CN112789087A (zh) 2018-08-08 2021-05-11 百时美施贵宝公司 Pad酶的苯并咪唑抑制剂
MX2021001471A (es) 2018-08-08 2021-04-28 Bristol Myers Squibb Co Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4).

Also Published As

Publication number Publication date
PE20211068A1 (es) 2021-06-09
MX2021001565A (es) 2021-04-19
IL280650A (en) 2021-03-25
EP3833440A1 (en) 2021-06-16
TW202019415A (zh) 2020-06-01
US11524959B1 (en) 2022-12-13
CA3108791A1 (en) 2020-02-13
JP2021534108A (ja) 2021-12-09
CL2021000296A1 (es) 2021-06-25
KR20210042934A (ko) 2021-04-20
BR112021002091A2 (pt) 2021-05-04
EA202190462A1 (ru) 2021-06-03
WO2020033520A1 (en) 2020-02-13
AR115920A1 (es) 2021-03-10
CN112805067A (zh) 2021-05-14
AU2019319835A1 (en) 2021-03-25
SG11202101174RA (en) 2021-03-30

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