PE20221829A1 - Inhibicion de integrina alfa4 beta7 humana - Google Patents

Inhibicion de integrina alfa4 beta7 humana

Info

Publication number
PE20221829A1
PE20221829A1 PE2022000633A PE2022000633A PE20221829A1 PE 20221829 A1 PE20221829 A1 PE 20221829A1 PE 2022000633 A PE2022000633 A PE 2022000633A PE 2022000633 A PE2022000633 A PE 2022000633A PE 20221829 A1 PE20221829 A1 PE 20221829A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibition
acid
human integrin
integrin alpha4
Prior art date
Application number
PE2022000633A
Other languages
English (en)
Inventor
Matthew G Bursavich
Dan Cui
James E Dowling
Kristopher N Hahn
Bryce A Harrison
fu-yang Lin
Blaise S Lippa
Bruce N Rogers
Dawn M Troast
Cheng Zhong
Kyle D Konze
Aleksey I Gerasyuto
Byungchan Kim
Salma Rafi
Tyler Day
Eugene Hickey
Evelyne Houang
Robert Zahler
Original Assignee
Morphic Therapeutic 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 Morphic Therapeutic Inc filed Critical Morphic Therapeutic Inc
Publication of PE20221829A1 publication Critical patent/PE20221829A1/es

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Classifications

    • 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
    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Radio Relay Systems (AREA)
  • Air Conditioning Control Device (AREA)

Abstract

Esta referido a un compuesto de Formula (Ia), en donde: R1 es alquilo sustituido o no sustituido; R3a y R3b son H, alquilo, cicloalquilo, OH, CN, entre otras opciones; R3c es H; R3d es haluro; R4 es H; R5a y R5e son alquilo; R5b, R5c y R5d son H, CN, haluro, CF3, alquilo, entre otras opciones; Ra es CF3; Rb es -(C1-C5)alquilen-N-(Rx)(Ry) sustituido o no sustituido; y, Rc es H. entre los compuestos preferidos tenemos los siguientes: acido (3S)-3-(4,5-difluoro-2',6'-dimetilbifenil-3-il)-3-(2-(5-(2-(3- fluoroazetidin-1-il)etil)-4-metil-2-oxopiridin-1(2H)-il)-4-metilpentanamido)propanoico; acido (3S)-3-(3-ciclopropil-2-(5-(2-(3-fluoroazetidin-1-il)etil)-2- oxopiridin-1(2H)-il)propanamido)-3-(4,5-difluoro-2',6'-dimetil-[1,1'-bifenil]-3-il)propanoico; entre otros. Estos compuestos son antagonistas de la integrina humana alfa4beta7 y se emplean en el tratamiento de diversas afecciones, tales como: enfermedad inflamatoria intestinal (IBD), colitis ulcerosa (UC) y enfermedad de Crohn (CD).
PE2022000633A 2019-10-16 2020-10-16 Inhibicion de integrina alfa4 beta7 humana PE20221829A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962916062P 2019-10-16 2019-10-16
PCT/US2020/055986 WO2021076890A1 (en) 2019-10-16 2020-10-16 INHIBITING HUMAN INTEGRIN α4β7

Publications (1)

Publication Number Publication Date
PE20221829A1 true PE20221829A1 (es) 2022-11-29

Family

ID=73198501

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000633A PE20221829A1 (es) 2019-10-16 2020-10-16 Inhibicion de integrina alfa4 beta7 humana

Country Status (22)

Country Link
US (3) US11104661B1 (es)
EP (2) EP4045039A4 (es)
JP (7) JP7437495B2 (es)
KR (2) KR20220102669A (es)
CN (2) CN115087444B (es)
AR (1) AR120244A1 (es)
AU (2) AU2020366435A1 (es)
BR (1) BR112022007284A2 (es)
CA (1) CA3154269A1 (es)
CL (1) CL2022000959A1 (es)
CO (1) CO2022005759A2 (es)
CR (1) CR20220205A (es)
CU (1) CU20220027A7 (es)
DO (1) DOP2022000081A (es)
EC (1) ECSP22038978A (es)
IL (1) IL292296A (es)
MX (1) MX2022004406A (es)
PE (1) PE20221829A1 (es)
TW (4) TWI802477B (es)
UY (1) UY38926A (es)
WO (3) WO2021076902A1 (es)
ZA (2) ZA202203872B (es)

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AR114489A1 (es) 2018-04-12 2020-09-09 Morphic Therapeutic Inc ANTAGONISTAS DE LA INTEGRINA a4b7 HUMANA
KR20240015737A (ko) 2018-10-30 2024-02-05 길리애드 사이언시즈, 인코포레이티드 알파4베타7 인테그린 억제제로서의 퀴놀린 유도체
US11578069B2 (en) 2019-08-14 2023-02-14 Gilead Sciences, Inc. Compounds for inhibition of α4 β7 integrin
MX2022004450A (es) 2019-10-16 2022-05-03 Chemocentryx Inc Aminas de heteroaril-bifenilo para el tratamiento de enfermedades pd-l1.
JP7437495B2 (ja) * 2019-10-16 2024-02-22 モーフィック セラピューティック，インコーポレイテッド ヒトインテグリンα４β７の阻害
CN118591535A (zh) * 2021-12-27 2024-09-03 西藏海思科制药有限公司 一种丙酸衍生物及其在医药上的应用
WO2024051819A1 (zh) * 2022-09-09 2024-03-14 西藏海思科制药有限公司 一种丙酸衍生物及其在医药上的应用
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US20240174632A1 (en) 2024-05-30
TW202126624A (zh) 2021-07-16
JP2022542184A (ja) 2022-09-29
TW202332675A (zh) 2023-08-16
WO2021076890A1 (en) 2021-04-22
JP7437490B2 (ja) 2024-02-22
WO2021076902A1 (en) 2021-04-22
UY38926A (es) 2021-05-31
TWI840047B (zh) 2024-04-21
JP2024054293A (ja) 2024-04-16
CN116783161A (zh) 2023-09-19
DOP2022000081A (es) 2022-07-31
WO2022081983A1 (en) 2022-04-21
EP4228634A1 (en) 2023-08-23
WO2021076890A4 (en) 2021-06-10
CA3154269A1 (en) 2021-04-22
TWI775182B (zh) 2022-08-21
ZA202303992B (en) 2024-06-26
KR20220102669A (ko) 2022-07-20
JP2024116230A (ja) 2024-08-27
CU20220027A7 (es) 2022-12-12
JP2022548809A (ja) 2022-11-22
MX2022004406A (es) 2022-08-25
CL2022000959A1 (es) 2023-04-28
ZA202203872B (en) 2024-01-31
CR20220205A (es) 2022-07-22
US11370773B1 (en) 2022-06-28
AU2020366435A1 (en) 2022-04-21
TW202244040A (zh) 2022-11-16
JP2023036958A (ja) 2023-03-14
ECSP22038978A (es) 2022-06-30
TWI791304B (zh) 2023-02-01
CN115087444A (zh) 2022-09-20
KR20230088376A (ko) 2023-06-19
JP2023500437A (ja) 2023-01-06
EP4045039A1 (en) 2022-08-24
JP2024054296A (ja) 2024-04-16
TW202315868A (zh) 2023-04-16
US11104661B1 (en) 2021-08-31
AR120244A1 (es) 2022-02-09
CO2022005759A2 (es) 2022-05-20
BR112022007284A2 (pt) 2022-07-05
JP7437495B2 (ja) 2024-02-22
TWI802477B (zh) 2023-05-11
IL292296A (en) 2022-06-01
TW202222793A (zh) 2022-06-16
AU2021361031A1 (en) 2023-06-08
EP4045039A4 (en) 2023-12-13
CN115087444B (zh) 2024-09-17
JP7500785B2 (ja) 2024-06-17
JP7209116B2 (ja) 2023-01-19

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