PE20230679A1 - Inhibidores heterociclicos de pad4 - Google Patents

Inhibidores heterociclicos de pad4

Info

Publication number
PE20230679A1
PE20230679A1 PE2022001712A PE2022001712A PE20230679A1 PE 20230679 A1 PE20230679 A1 PE 20230679A1 PE 2022001712 A PE2022001712 A PE 2022001712A PE 2022001712 A PE2022001712 A PE 2022001712A PE 20230679 A1 PE20230679 A1 PE 20230679A1
Authority
PE
Peru
Prior art keywords
independently
alkyl
optionally substituted
selected independently
heterocyclic
Prior art date
Application number
PE2022001712A
Other languages
English (en)
Inventor
Kumaravel Selvakumar
Venkatram Reddy Paidi
Srinivasan Thangathirupathy
Cm Vijaya Kumar
Tirupathi Rao Alajangi
Mallikarjun Reddy Sura
Krishna Mahadevu
Ramesh Kumar Sistla
Piyush Agarwal
Karuppiah Arul Mozhi Subbiah
Jalathi S Nair
Ooha Morampudi
Manoranjan Panda
Joseph A Tino
Robert J Cherney
John V Duncia
Daniel S Gardner
T G Murali Dhar
Audrey Graham Ross
Paul E Gormisky
Xiao Zhu
Boris M Seletsky
Alyssa H Antropow
Deqiang Niu
Zhengdong Zhu
Guobin Miao
Julio Hernan Cuervo
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 PE20230679A1 publication Critical patent/PE20230679A1/es

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Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61P25/28—Drugs 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic 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
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

Landscapes

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

Abstract

Referido a un compuesto de la Formula I, en donde: X1 se selecciona independientemente de CR2 y N; X2 se selecciona independientemente de CR4 y N; X3 se selecciona independientemente de O y S; X4 se selecciona independientemente de CR2 y N; siempre que X1 y X4 no sean ambos N; X5 se selecciona independientemente de O y S; X6 se selecciona independientemente de CR4, y N; siempre que X2 y X6 no sean ambos N; cuando X2 y X6 son ambos CR4, uno de R4 es H; R1 se selecciona independientemente de -NH- alquilo C1-C5 opcionalmente sustituido por uno o mas sustituyentes seleccionados de F, Cl, heterociclilo de 4-10 miembros, entre otros; R2 se selecciona independientemente de H, F, Cl, alquilo C1-C4 opcionalmente sustituido por uno o mas sustituyentes seleccionados de F, Cl, y OH, y -O alquiloC1-C4; R3 se selecciona independientemente de H, F, Cl, CN, entre otros; R4 se selecciona independientemente de H, F, Cl, Br, entre otros; R5 se selecciona independientemente de H, F, Cl, Br, CN, =O, alquilo C1-C4 opcionalmente sustituido, entre otros; R6 se selecciona independientemente de H, alquilo C1-C6; R7 se selecciona independientemente de H, F, y Cl; R8 se selecciona independientemente de H, y alquilo C1-C6 opcionalmente sustituido. Un compuesto seleccionado es 5-(2-(6-((7R)-7-Amino-2-azabiciclo[2.2.1]- heptano-2-carbonil)-4-metoxi-3-metilpirazolo[1,5-a]piridin-2-il)-1-(ciclopropilmetil)-1H-pirrolo[2,3-b]piridin-6-il)isoindolin-1-ona (5). Estos compuestos heterociclicos son inhibidores de PAD4. Tambien se refiere a metodo para preparar estos compuestos y su uso de estos compuestos en el tratamiento de una enfermedad o trastorno asociado con la actividad de la enzima PAD4.
PE2022001712A 2020-02-12 2021-02-11 Inhibidores heterociclicos de pad4 PE20230679A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN202041006146 2020-02-12
PCT/US2021/017554 WO2021163254A1 (en) 2020-02-12 2021-02-11 Heterocyclic pad4 inhibitors

Publications (1)

Publication Number Publication Date
PE20230679A1 true PE20230679A1 (es) 2023-04-21

Family

ID=74856949

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022001712A PE20230679A1 (es) 2020-02-12 2021-02-11 Inhibidores heterociclicos de pad4

Country Status (16)

Country Link
US (1) US20230167131A1 (es)
EP (1) EP4103559A1 (es)
JP (1) JP2023515780A (es)
KR (1) KR20220140795A (es)
CN (1) CN115348961A (es)
AR (1) AR121299A1 (es)
AU (1) AU2021219710A1 (es)
BR (1) BR112022015792A2 (es)
CA (1) CA3167753A1 (es)
CL (1) CL2022002148A1 (es)
CO (1) CO2022011388A2 (es)
IL (1) IL295506A (es)
MX (1) MX2022009874A (es)
PE (1) PE20230679A1 (es)
TW (1) TW202140477A (es)
WO (1) WO2021163254A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112022021963A2 (pt) * 2020-04-30 2022-12-13 Gilead Sciences Inc Inibidores macrocíclicos de peptidilarginina desiminases
US11878965B2 (en) 2020-12-22 2024-01-23 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7842713B2 (en) 2006-04-20 2010-11-30 Pfizer Inc Fused phenyl amido heterocyclic compounds
WO2014015905A1 (en) * 2012-07-26 2014-01-30 Glaxo Group Limited 2 - (azaindol- 2 -yl) benz imidazoles as pad4 inhibitors
EP3298003B1 (en) * 2015-05-21 2023-04-19 GlaxoSmithKline Intellectual Property Development Limited Benzoimidazole derivatives as pad4 inhibitors
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
US11390609B2 (en) * 2017-06-30 2022-07-19 Beijing Tide Pharmaceutical Co., Ltd. Rho-associated protein kinase inhibitor, pharmaceutical composition comprising same, and preparation method and use thereof
BR112020007607A2 (pt) * 2017-10-18 2020-09-29 Jubilant Epipad LLC compostos das fórmulas (i), (ii) e (iii); processos de preparação de compostos das fórmulas (i), (ii) e (iii); composição farmacêutica; compostos; método para a inibição de uma ou mais famílias de pad em uma célula; método de tratamento de uma afecção mediada por uma ou mais pad; composto da fórmula (i), fórmula (ii) e fórmula (iii); uso do composto; método para o tratamento e/ou prevenção de uma afecção; método para o tratamento de artrite reumatoide; e método de tratamento de câncer

Also Published As

Publication number Publication date
KR20220140795A (ko) 2022-10-18
TW202140477A (zh) 2021-11-01
US20230167131A1 (en) 2023-06-01
CL2022002148A1 (es) 2023-02-24
IL295506A (en) 2022-10-01
AU2021219710A1 (en) 2022-10-06
EP4103559A1 (en) 2022-12-21
BR112022015792A2 (pt) 2022-10-11
WO2021163254A1 (en) 2021-08-19
AR121299A1 (es) 2022-05-04
CN115348961A (zh) 2022-11-15
MX2022009874A (es) 2022-08-22
JP2023515780A (ja) 2023-04-14
CA3167753A1 (en) 2021-08-19
CO2022011388A2 (es) 2022-08-30

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