CL2022002990A1 - Inhibidores macrocíclicos de las peptidilarginina deiminasas - Google Patents

Inhibidores macrocíclicos de las peptidilarginina deiminasas

Info

Publication number
CL2022002990A1
CL2022002990A1 CL2022002990A CL2022002990A CL2022002990A1 CL 2022002990 A1 CL2022002990 A1 CL 2022002990A1 CL 2022002990 A CL2022002990 A CL 2022002990A CL 2022002990 A CL2022002990 A CL 2022002990A CL 2022002990 A1 CL2022002990 A1 CL 2022002990A1
Authority
CL
Chile
Prior art keywords
compounds
peptidylarginine
deiminases
macrocyclic inhibitors
peptidylarginine deiminases
Prior art date
Application number
CL2022002990A
Other languages
English (en)
Inventor
Roland D Saito
Hyung-Jung Pyun
James G Taylor
Stephane Perreault
Veldhuizen Joshua J Van
Eda Y Canales
Weng K Chang
Laurent P Debien
Petr Jansa
Jennifer A Loyer-Drew
Luisruben P Martinez
Gary B Phillips
Michael S Sangi
Adam J Schrier
Marina E Shatskikh
Jennifer A Treiberg
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 CL2022002990A1 publication Critical patent/CL2022002990A1/es

Links

Classifications

    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed 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
    • C07D471/22—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 systems contains four 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
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic 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
    • C07D513/12—Heterocyclic 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
    • C07D513/18—Bridged 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.
CL2022002990A 2020-04-30 2022-10-27 Inhibidores macrocíclicos de las peptidilarginina deiminasas CL2022002990A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063018411P 2020-04-30 2020-04-30
US202063129430P 2020-12-22 2020-12-22

Publications (1)

Publication Number Publication Date
CL2022002990A1 true CL2022002990A1 (es) 2023-07-14

Family

ID=76181198

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2022002990A CL2022002990A1 (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) JP2023524036A (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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2022140390A1 (en) * 2020-12-22 2022-06-30 Gilead Sciences, Inc. Inhibitors of peptidylarginine deiminases
WO2023083365A1 (en) 2021-11-15 2023-05-19 Qilu Regor Therapeutics Inc. Pad4 inhibitors and use thereof
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

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
KR101737753B1 (ko) 2007-03-12 2017-05-18 와이엠 바이오사이언시즈 오스트레일리아 피티와이 엘티디 페닐 아미노 피리미딘 화합물 및 이의 용도
PE20081882A1 (es) 2007-03-15 2008-12-27 Schering Corp Derivados de piridazinona utiles como inhibidores de glucano sintasa
GB201106520D0 (en) 2011-04-18 2011-06-01 Numedicus Ltd Pharmaceutical compounds
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
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
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
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
NZ762985A (en) 2017-09-22 2024-03-22 Jubilant Epipad LLC Heterocyclic compounds as pad inhibitors
HUE061607T2 (hu) * 2017-10-18 2023-07-28 Jubilant Epipad LLC Imidazopiridin vegyületek mint PAD inhibitorok
EP3746430A4 (en) 2018-02-02 2021-11-03 Padforward LLC INHIBITORS OF PROTEIN ARGININE DEIMINASES
JP2021515043A (ja) * 2018-02-26 2021-06-17 南京薬捷安康生物科技有限公司Ｎａｎｊｉｎｇ Ｔｒａｎｓｔｈｅｒａ Ｂｉｏｓｃｉｅｎｃｅｓ Ｃｏ．， Ｌｔｄ． ペプチジルアルギニンデイミナーゼ阻害剤及びその使用
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
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
EA202190462A1 (ru) * 2018-08-08 2021-06-03 Бристол-Маерс Сквибб Компани Индольные и азаиндольные ингибиторы ферментов pad
MX2021001471A (es) 2018-08-08 2021-04-28 Bristol Myers Squibb Co Benzimidazoles sustituidos como inhibidores de peptidil arginina deiminasa 4 (pad4).
CN115151253A (zh) 2019-09-23 2022-10-04 南京征祥医药有限公司 磷酸二酯酶抑制剂及用途
TW202115083A (zh) 2019-09-27 2021-04-16 大陸商南京藥捷安康生物科技有限公司 肽醯精胺酸脫亞胺酶抑制劑及其用途
JP2023512557A (ja) * 2020-02-06 2023-03-27 ブリストル－マイヤーズ スクイブ カンパニー 免疫抑制剤として有用な大環状ｐａｄ４阻害剤
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
PE20230488A1 (es) 2023-03-21
CN115551862A (zh) 2022-12-30
US20230002412A1 (en) 2023-01-05
MX2022013615A (es) 2022-11-16
KR20230004810A (ko) 2023-01-06
TW202206431A (zh) 2022-02-16
TWI815110B (zh) 2023-09-11
BR112022021963A2 (pt) 2022-12-13
CA3177532A1 (en) 2021-11-04
CO2022015307A2 (es) 2023-02-16
JP2023524036A (ja) 2023-06-08
AU2021265110A1 (en) 2022-10-27
US11976083B2 (en) 2024-05-07
DOP2022000235A (es) 2022-11-30
AU2021265110B2 (en) 2023-08-17
IL296923A (en) 2022-12-01
CR20220550A (es) 2022-12-15
EP4143189A1 (en) 2023-03-08
CN115551862B (zh) 2024-04-12
WO2021222353A1 (en) 2021-11-04

Similar Documents

Publication Publication Date Title
CO2022015307A2 (es) Inhibidores macrocíclicos de las peptidilarginina deiminasas
CL2022003510A1 (es) Inhibidores de cisteína proteasas y sus métodos de uso
AR107871A1 (es) Combinaciones de inhibidores de lsd1 para su uso en el tratamiento de tumores sólidos
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
ECSP13013048A (es) Spiro-[1,3]-oxacinas y spiro-[1,4]-oxacepinas como inhibidores
BR112014026057A2 (pt) análogos limitados por anel como inibidores de arginase
ECSP109903A (es) Derivados de pirazinona y su uso en el tratamiento de enfermedades pulmonares
AR054347A1 (es) Combinaciones terapeuticas para el tratamiento o la prevencion de la depresion
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.
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
CL2011000306A1 (es) Compuestos derivados de di-alquilamida del acido 7-ciclopentil-2-[5-(piperidin o piperazin sustituido)-piridin-2-il amino]-7h-pirrolo-[2,3-d]-pirimidin-6-carboxilico, inhibidores de cdk4; composicion farmaceutica; y su uso para el tratamiento del cancer o la inflamacion.
AR047928A1 (es) Derivados de tetrahidropiridoindol
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.
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
UY30267A1 (es) Nuevos derivados de la tioxantina , composiciones farmacéuticas que los contienen, procedimientos de preparacion y aplicaciones
CO6640335A2 (es) Tratamiento terapéutico para síndrome metabólico, diabetes de tipo 2, obesidad o prediabetes
CR20120062A (es) Terapia combinada para el tratamiento de la diabetes
UY28979A1 (es) Derivados de hidrocloruros de 3-carboxamida, composiciones farmacéuticas que los contienen, procedimiento de preparación y su uso, útiles como inhibidores selectivos de gsk3
UY32315A (es) Compuestos de piperidina y usos de los mismo-596
UY31141A1 (es) Compuestos de piperidina y sus usos
CR9722A (es) Derivados de benzilpiperazina y su uso medico