AU2021213758A1 - Inhibitors of APOL1 and methods of using same - Google Patents

Inhibitors of APOL1 and methods of using same Download PDF

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Publication number
AU2021213758A1
AU2021213758A1 AU2021213758A AU2021213758A AU2021213758A1 AU 2021213758 A1 AU2021213758 A1 AU 2021213758A1 AU 2021213758 A AU2021213758 A AU 2021213758A AU 2021213758 A AU2021213758 A AU 2021213758A AU 2021213758 A1 AU2021213758 A1 AU 2021213758A1
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Australia
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groups
linear
branched
optionally substituted
chosen
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AU2021213758A
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English (en)
Inventor
Jingrong Cao
Jon H. Come
Leslie A. DAKIN
Francois Denis
Warren A. DORSCH
Anne FORTIER
Martine Hamel
Elaine B. Krueger
Brian Ledford
Francois Maltais
Suganthini S. Nanthakumar
Olivier Nicolas
Camil E. SAYEGH
Timothy J. SENTER
Tiansheng Wang
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Application filed by Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of AU2021213758A1 publication Critical patent/AU2021213758A1/en
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/02—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 two hetero rings
    • C07D403/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D405/02—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 two hetero rings
    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D407/02—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 two hetero rings
    • C07D407/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • 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
    • C07D491/02—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 two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • 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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
AU2021213758A 2020-01-29 2021-01-28 Inhibitors of APOL1 and methods of using same Pending AU2021213758A1 (en)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202062967276P 2020-01-29 2020-01-29
US62/967,276 2020-01-29
US202063038278P 2020-06-12 2020-06-12
US63/038,278 2020-06-12
US202063040166P 2020-06-17 2020-06-17
US63/040,166 2020-06-17
PCT/US2021/015495 WO2021154997A1 (en) 2020-01-29 2021-01-28 Inhibitors of apol1 and methods of using same

Publications (1)

Publication Number Publication Date
AU2021213758A1 true AU2021213758A1 (en) 2022-09-01

Family

ID=74673393

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2021213758A Pending AU2021213758A1 (en) 2020-01-29 2021-01-28 Inhibitors of APOL1 and methods of using same

Country Status (7)

Country Link
US (1) US12116343B2 (https=)
EP (1) EP4097083A1 (https=)
JP (1) JP7668804B2 (https=)
CN (1) CN116348447A (https=)
AU (1) AU2021213758A1 (https=)
CA (1) CA3168909A1 (https=)
WO (1) WO2021154997A1 (https=)

Families Citing this family (16)

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Publication number Priority date Publication date Assignee Title
US11618746B2 (en) 2018-12-17 2023-04-04 Vertex Pharmaceuticals Incorporated Inhibitors of APOL1 and methods of using same
AU2020328598A1 (en) 2019-08-15 2022-03-03 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
WO2021154997A1 (en) 2020-01-29 2021-08-05 Vertex Pharmaceuticals Incorporated Inhibitors of apol1 and methods of using same
IL296035A (en) 2020-03-06 2022-10-01 Vertex Pharma Methods of treating apol-1 dependent focal segmental glomerulosclerosis
CN115867543A (zh) 2020-06-12 2023-03-28 弗特克斯药品有限公司 Apol1抑制剂的固体形式及其使用方法
CN115867532A (zh) * 2020-06-12 2023-03-28 弗特克斯药品有限公司 Apol1的抑制剂及其用途
CA3185604A1 (en) * 2020-06-12 2021-12-16 Vertex Pharmaceuticals Incorporated Inhibitors of apol1 and use of the same
CN116547287B (zh) 2020-08-26 2025-09-26 弗特克斯药品有限公司 Apol1的抑制剂及其使用方法
US20230119114A1 (en) * 2021-08-26 2023-04-20 Vertex Pharmaceuticals Incorporated Solid forms of apol1 inhibitors and methods of using same
US12612379B2 (en) * 2021-11-30 2026-04-28 Vertex Pharmaceuticals Incorporated Inhibitors of APOL1 and methods of using same
EP4440697A1 (en) * 2021-11-30 2024-10-09 Vertex Pharmaceuticals Incorporated Spirocyclic inhibitors of apol1 and methods of using same
MX2024008868A (es) * 2022-01-18 2024-09-23 Maze Therapeutics Inc Inhibidores de la apolipoproteína l1 (apol1) y métodos de uso.
EP4543870A1 (en) * 2022-06-24 2025-04-30 F. Hoffmann-La Roche AG New heterocyclic-carbonyl-cyclic compounds as magl inhibitors
WO2024242846A1 (en) * 2023-05-03 2024-11-28 Omniab, Inc. Heteroarylindole inhibitors of apol-1
GB202401326D0 (en) * 2024-02-01 2024-03-20 Podium Bio Ltd Novel compounds
WO2025231011A1 (en) * 2024-05-01 2025-11-06 Omniab, Inc. Heteroarylindole inhibitors of apol-1

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WO2021154997A1 (en) 2020-01-29 2021-08-05 Vertex Pharmaceuticals Incorporated Inhibitors of apol1 and methods of using same
US20210246121A1 (en) 2020-02-04 2021-08-12 Vertex Pharmaceuticals Incorporated Solid forms of apol1 inhibitor and methods of using same
IL296035A (en) 2020-03-06 2022-10-01 Vertex Pharma Methods of treating apol-1 dependent focal segmental glomerulosclerosis
JP2023524563A (ja) 2020-05-07 2023-06-12 ラムバム メド－テック リミテッド Ａｐｏｌ１－関連疾患の治療に使用するための組成物
CN115867532A (zh) 2020-06-12 2023-03-28 弗特克斯药品有限公司 Apol1的抑制剂及其用途
CN115867543A (zh) 2020-06-12 2023-03-28 弗特克斯药品有限公司 Apol1抑制剂的固体形式及其使用方法
CA3185604A1 (en) 2020-06-12 2021-12-16 Vertex Pharmaceuticals Incorporated Inhibitors of apol1 and use of the same
CN116547287B (zh) 2020-08-26 2025-09-26 弗特克斯药品有限公司 Apol1的抑制剂及其使用方法
US20230119114A1 (en) 2021-08-26 2023-04-20 Vertex Pharmaceuticals Incorporated Solid forms of apol1 inhibitors and methods of using same
US12612379B2 (en) 2021-11-30 2026-04-28 Vertex Pharmaceuticals Incorporated Inhibitors of APOL1 and methods of using same
EP4440697A1 (en) 2021-11-30 2024-10-09 Vertex Pharmaceuticals Incorporated Spirocyclic inhibitors of apol1 and methods of using same
AU2023219516A1 (en) 2022-02-08 2024-08-22 Vertex Pharmaceuticals Incorporated 2-methyl-4-phenylpiperidin-4-ol derivatives as inhibitors of apol1 and methods of using same
CN119212986A (zh) 2022-02-08 2024-12-27 弗特克斯药品有限公司 作为apol1的抑制剂的螺哌啶衍生物及其使用方法
EP4476228A1 (en) 2022-02-08 2024-12-18 Vertex Pharmaceuticals Incorporated 4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] derivatives as inhibitors of apol1 and methods of using same
CA3251050A1 (en) 2022-02-08 2023-08-17 Vertex Pharmaceuticals Incorporated 2-METHYL-4',5'-DIHYDROSPIRO[PIPERIDINE-4,7'-THIENO[2,3-C]PYRAN] DERIVATIVES USED AS APOL1 INHIBITORS AND THEIR METHODS OF USE

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Publication number Publication date
JP7668804B2 (ja) 2025-04-25
US20220340523A1 (en) 2022-10-27
CA3168909A1 (en) 2021-08-05
EP4097083A1 (en) 2022-12-07
CN116348447A (zh) 2023-06-27
JP2023512213A (ja) 2023-03-24
WO2021154997A1 (en) 2021-08-05
US12116343B2 (en) 2024-10-15

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