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MX2021001565A - Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad). - Google Patents

Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad).

Info

Publication number
MX2021001565A
MX2021001565A MX2021001565A MX2021001565A MX2021001565A MX 2021001565 A MX2021001565 A MX 2021001565A MX 2021001565 A MX2021001565 A MX 2021001565A MX 2021001565 A MX2021001565 A MX 2021001565A MX 2021001565 A MX2021001565 A MX 2021001565A
Authority
MX
Mexico
Prior art keywords
indole
inhibitors
pad enzymes
azaindole
azaindole inhibitors
Prior art date
Application number
MX2021001565A
Other languages
English (en)
Inventor
Robert J Cherney
Anurag S Srivastava
Khehyong Ngu
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 MX2021001565A publication Critical patent/MX2021001565A/es

Links

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
    • C07D471/04—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
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

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, (ver Fórmula) 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.
MX2021001565A 2018-08-08 2019-08-07 Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad). MX2021001565A (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
MX2021001565A true MX2021001565A (es) 2021-04-19

Family

ID=67766306

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2021001565A MX2021001565A (es) 2018-08-08 2019-08-07 Inhibidores tipo indol y azaindol de enzimas peptidil arginina deiminasas (pad).

Country Status (18)

Country Link
US (1) US11524959B1 (es)
EP (1) EP3833440A1 (es)
JP (1) JP7651451B2 (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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202019415A (zh) 2018-08-08 2020-06-01 美商必治妥美雅史谷比公司 Pad酶之吲哚及氮雜吲哚抑制劑
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
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
TW202233174A (zh) * 2020-12-22 2022-09-01 美商基利科學股份有限公司 肽基精胺酸去亞胺酶之抑制劑
EP4267562A1 (en) 2020-12-22 2023-11-01 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
WO2025024265A1 (en) 2023-07-21 2025-01-30 Bristol-Myers Squibb Company Methods of assessing citrullination and activity of pad4 modulators

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104470919B (zh) 2012-07-26 2016-07-06 葛兰素集团有限公司 作为pad4抑制剂的2-(氮杂吲哚-2-基)苯并咪唑
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
AR107030A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores aza-bencimidazol de pad4
AR107032A1 (es) 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
KR20180098593A (ko) 2015-12-22 2018-09-04 칸세라 아베 포유류의 히스톤 탈아세틸화효소 활성에 대한 저해제로서 유용한 바이사이클릭 하이드록사믹산
CA3015482A1 (en) 2016-02-23 2017-08-31 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
ES2828623T3 (es) 2016-07-27 2021-05-27 Padlock Therapeutics Inc Inhibidores covalentes de PAD4
WO2018049296A1 (en) 2016-09-12 2018-03-15 Padlock Therapeutics, Inc. Heteroaryl inhibitors of pad4
JP7311228B2 (ja) 2017-06-30 2023-07-19 ベイジン タイド ファーマシューティカル カンパニー リミテッド Ｒｈｏ－関連プロテインキナーゼ阻害剤、それを含む医薬組成物並びにその調製方法及び使用
KR102782563B1 (ko) 2017-10-18 2025-03-14 주빌런트 에피파드 엘엘씨 Pad 억제제로서의 이미다조-피리딘 화합물
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
JP7483678B2 (ja) 2018-08-08 2024-05-15 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ベンズイミダゾール
KR20210042933A (ko) 2018-08-08 2021-04-20 브리스톨-마이어스 스큅 컴퍼니 Pad 효소의 벤즈이미다졸 억제제
TW202019415A (zh) 2018-08-08 2020-06-01 美商必治妥美雅史谷比公司 Pad酶之吲哚及氮雜吲哚抑制劑

Also Published As

Publication number Publication date
EA202190462A1 (ru) 2021-06-03
EP3833440A1 (en) 2021-06-16
KR20210042934A (ko) 2021-04-20
AR115920A1 (es) 2021-03-10
US11524959B1 (en) 2022-12-13
AU2019319835A1 (en) 2021-03-25
BR112021002091A2 (pt) 2021-05-04
JP7651451B2 (ja) 2025-03-26
PE20211068A1 (es) 2021-06-09
CL2021000296A1 (es) 2021-06-25
TW202019415A (zh) 2020-06-01
SG11202101174RA (en) 2021-03-30
CN112805067A (zh) 2021-05-14
CO2021001217A2 (es) 2021-02-26
CA3108791A1 (en) 2020-02-13
IL280650A (en) 2021-03-25
JP2021534108A (ja) 2021-12-09
WO2020033520A1 (en) 2020-02-13

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