DOP2022000235A - Inhibidores macrocíclicos de las peptidilarginina deiminasas - Google Patents

Inhibidores macrocíclicos de las peptidilarginina deiminasas

Info

Publication number
DOP2022000235A
DOP2022000235A DO2022000235A DO2022000235A DOP2022000235A DO P2022000235 A DOP2022000235 A DO P2022000235A DO 2022000235 A DO2022000235 A DO 2022000235A DO 2022000235 A DO2022000235 A DO 2022000235A DO P2022000235 A DOP2022000235 A DO P2022000235A
Authority
DO
Dominican Republic
Prior art keywords
compounds
peptidylarginine
deiminases
macrocyclic inhibitors
peptidylarginine deiminases
Prior art date
Application number
DO2022000235A
Other languages
English (en)
Inventor
G Taylor James
A Loyer-Drew Jennifer
B Phillips Gary
J Van Veldhuizen Joshua
D Saito Roland
Y Canales Eda
K Chang Weng
P Debien Laurent
Jansa Petr
P Martinez Luisruben
Perreault Stephane
Pyun Hyung-Jung
S Sangi Michael
J Schrier Adam
E Shatskikh Marina
A Treiberg Jennifer
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of DOP2022000235A publication Critical patent/DOP2022000235A/es

Links

Classifications

    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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
    • 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
    • A61K31/439Heterocyclic 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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D471/12Heterocyclic 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 three hetero rings
    • C07D471/14Ortho-condensed systems
    • 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
    • C07D471/22Heterocyclic 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 systems contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18Bridged systems

Landscapes

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

Abstract

La presente divulgación se refiere a compuestos novedosos para su uso en el tratamiento terapéutico de una enfermedad asociada con peptidilarginina deiminasas (PAD), tales como peptidilarginina deiminasa tipo 4 (PAD4). La presente divulgación también se refiere a procesos e intermediarios para la preparación de tales compuestos, métodos para usar tales compuestos y composiciones farmacéuticas que comprenden los compuestos descritos en este documento.
DO2022000235A 2020-04-30 2022-10-27 Inhibidores macrocíclicos de las peptidilarginina deiminasas DOP2022000235A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063018411P 2020-04-30 2020-04-30
US202063129430P 2020-12-22 2020-12-22
PCT/US2021/029557 WO2021222353A1 (en) 2020-04-30 2021-04-28 Macrocyclic inhibitors of peptidylarginine deiminases

Publications (1)

Publication Number Publication Date
DOP2022000235A true DOP2022000235A (es) 2022-11-30

Family

ID=76181198

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2022000235A DOP2022000235A (es) 2020-04-30 2022-10-27 Inhibidores macrocíclicos de las peptidilarginina deiminasas

Country Status (17)

Country Link
US (1) US11976083B2 (es)
EP (1) EP4143189A1 (es)
JP (1) JP7507251B2 (es)
KR (1) KR20230004810A (es)
CN (1) CN115551862B (es)
AU (1) AU2021265110B2 (es)
BR (1) BR112022021963A2 (es)
CA (1) CA3177532A1 (es)
CL (1) CL2022002990A1 (es)
CO (1) CO2022015307A2 (es)
CR (1) CR20220550A (es)
DO (1) DOP2022000235A (es)
IL (1) IL296923A (es)
MX (1) MX2022013615A (es)
PE (1) PE20230488A1 (es)
TW (1) TWI815110B (es)
WO (1) WO2021222353A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11878965B2 (en) 2020-12-22 2024-01-23 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
CN118679162A (zh) 2021-11-15 2024-09-20 锐格药业公司 Pad4抑制剂及其用途
WO2024008745A1 (en) 2022-07-05 2024-01-11 Institut National de la Santé et de la Recherche Médicale Methods and composition to identify and treat subjects resisting to chemotherapy treatment
CN115960124A (zh) * 2023-02-23 2023-04-14 康化(上海)新药研发有限公司 一种2-氟-3-甲酰基-吡啶-4-硼酸频哪醇酯的合成方法

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3821540A1 (de) 1988-06-25 1989-12-28 Boehringer Mannheim Gmbh Neue sulfonamide, verfahren zu ihrer herstellung sowie solche sulfonamide enthaltende arzneimittel
KR20150043565A (ko) 2007-03-12 2015-04-22 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 페닐 아미노 피리미딘 화합물 및 이의 용도
BRPI0809238A2 (pt) 2007-03-15 2014-09-09 Schering Corp Derivados de piridazinonas úteis como inibidores de glican sintase
GB201106520D0 (en) 2011-04-18 2011-06-01 Numedicus Ltd Pharmaceutical compounds
HUE033294T2 (en) 2012-07-26 2017-11-28 Glaxo Group Ltd 2- (azaindol-2-yl) benzimidazoles as PAD4 inhibitors
CA2986199C (en) * 2015-05-21 2023-07-18 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
AR107032A1 (es) * 2015-12-09 2018-03-14 Padlock Therapeutics Inc Inhibidores bicíclicos de pad4
MX2018009773A (es) 2016-02-23 2018-11-29 Padlock Therapeutics Inc Heteroarilos inhibidores de peptidilarginina desiminasa 4 (pad4).
WO2018022897A1 (en) 2016-07-27 2018-02-01 Padlock Therapeutics, Inc. Covalent inhibitors of pad4
MA46193A (fr) 2016-09-12 2019-07-17 Padlock Therapeutics Inc Inhibiteurs hétéroaryles de pad4
EP3685149B1 (en) 2017-09-21 2023-08-16 F. Hoffmann-La Roche AG Use of a solid fraction sensor to evaluate a solid fraction of a target pharmaceutical sample and solid fraction sensor
PL3684767T3 (pl) 2017-09-22 2024-10-14 Jubilant Epipad LLC Związki heterocykliczne jako inhibitory pad
JP7307723B2 (ja) 2017-10-18 2023-07-12 ジュビラント エピパッド エルエルシー Pad阻害剤としてのイミダゾ-ピリジン化合物
US11453676B2 (en) 2018-02-02 2022-09-27 Forward Therapeutics, Inc. Inhibitors of protein arginine deiminases
CN110194770B (zh) * 2018-02-26 2022-08-09 药捷安康(南京)科技股份有限公司 肽酰精氨酸脱亚胺酶抑制剂及其用途
US20220348562A1 (en) 2018-08-08 2022-11-03 Bristol-Myers Squibb Company Benzimidazole inhibitors of pad enzymes
WO2020033488A1 (en) 2018-08-08 2020-02-13 Bristol-Myers Squibb Company Substituted benzimidazoles as pad4 inhibitors
KR20210042935A (ko) 2018-08-08 2021-04-20 브리스톨-마이어스 스큅 컴퍼니 Pad4 억제제로서의 치환된 티에노피롤
CN112805067A (zh) 2018-08-08 2021-05-14 百时美施贵宝公司 Pad酶的吲哚及氮杂吲哚抑制剂
CN116574099A (zh) 2019-09-23 2023-08-11 南京征祥医药有限公司 磷酸二酯酶抑制剂及用途
CN112574230B (zh) 2019-09-27 2022-10-28 药捷安康(南京)科技股份有限公司 肽酰精氨酸脱亚胺酶抑制剂及其用途
KR20220137694A (ko) 2020-02-06 2022-10-12 브리스톨-마이어스 스큅 컴퍼니 면역억제제로서 유용한 마크로시클릭 pad4 억제제
TW202140477A (zh) 2020-02-12 2021-11-01 美商必治妥美雅史谷比公司 雜環pad4抑制劑

Also Published As

Publication number Publication date
CN115551862A (zh) 2022-12-30
JP7507251B2 (ja) 2024-06-27
AU2021265110B2 (en) 2023-08-17
CL2022002990A1 (es) 2023-07-14
CN115551862B (zh) 2024-04-12
MX2022013615A (es) 2022-11-16
CA3177532A1 (en) 2021-11-04
WO2021222353A1 (en) 2021-11-04
PE20230488A1 (es) 2023-03-21
EP4143189A1 (en) 2023-03-08
TWI815110B (zh) 2023-09-11
CR20220550A (es) 2022-12-15
US20230002412A1 (en) 2023-01-05
AU2021265110A1 (en) 2022-10-27
US11976083B2 (en) 2024-05-07
IL296923A (en) 2022-12-01
KR20230004810A (ko) 2023-01-06
CO2022015307A2 (es) 2023-02-16
BR112022021963A2 (pt) 2022-12-13
TW202206431A (zh) 2022-02-16
JP2023524036A (ja) 2023-06-08

Similar Documents

Publication Publication Date Title
DOP2022000235A (es) Inhibidores macrocíclicos de las peptidilarginina deiminasas
CL2022003510A1 (es) Inhibidores de cisteína proteasas y sus métodos de uso
CL2008002916A1 (es) Compuestos derivados de triazolopiridina, inhibidores 11-beta-hidroxiesteroide deshidrogenasa tipo i; composicion farmaceutica que los comprende; y su uso en el tratamiento y/o prevencion de la diabetes, dislipidemia, obesidad, entre otros.
ECSP099706A (es) Nuevos derivados de n-(8-heteroariltetrahidronaftalen-2yl) y n-(5-heteroarilcroman-3-il) carboxamida para el tratamiento del dolor
GT200600045A (es) Derivados de piridizina y su uso como agentes terapeuticos
GT200500237A (es) Derivados de pirimidina
AR107871A1 (es) Combinaciones de inhibidores de lsd1 para su uso en el tratamiento de tumores sólidos
GT200500325A (es) Pirazolo-pirimidinas 1,4-sustituidas como inhibidores de quinasa
BR112014026057A2 (pt) análogos limitados por anel como inibidores de arginase
ECSP11011113A (es) Piridiloxi-indoles inhibidores del vegf-r2 y uso de los mismos para el tratamiento de enfermedades
ECSP13013048A (es) Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores
GT200600096A (es) Composicion farmaceutica para el tratamiento del cancer
ECSP109903A (es) Derivados de pirazinona y su uso en el tratamiento de enfermedades pulmonares
UY32462A (es) Derivados de bifenilo novedosos para el tratamiento de infección por virus de hepatitis c 644
AR054347A1 (es) Combinaciones terapeuticas para el tratamiento o la prevencion de la depresion
ECSP10010489A (es) Nuevas formulaciones, comprimidos que comprenden tales formulaciones, su uso y procedimiento para su preparación
DOP2011000264A (es) Derivados de aminotetralina, composiciones farmaceuticas que los contienen y sus usos en terapia
UY28990A1 (es) Nuevos derivados de benceno 1, 3-amino carbonilo como inhibidores de b-raf, composiciones farmacéuticas que los contienen, procesos de preparación y uso.
CL2008001560A1 (es) Compuestos derivados de heterociclo de nitrogenado, moduladores de gamma secretasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de enfermedades neurodegenerativas como el alzheimer, sindrome de down; kit farmaceutico.
CO6640335A2 (es) Tratamiento terapéutico para síndrome metabólico, diabetes de tipo 2, obesidad o prediabetes
AR047928A1 (es) Derivados de tetrahidropiridoindol
CR20120062A (es) Terapia combinada para el tratamiento de la diabetes
UY27872A1 (es) Inhibidores de caspasa y usos de los mismos.
UY31141A1 (es) Compuestos de piperidina y sus usos
UY29092A1 (es) Derivados de 4-oxo-3,4-dihidroquinazolin-6-carboxamida, inhibidores de b-raf, composiciones farmacéuticas que los contienen, procedimientos de preparación y aplicaciones