PE20230601A1 - Pirrolopirimidinaminas como inhibidores del sistema del complemento - Google Patents

Pirrolopirimidinaminas como inhibidores del sistema del complemento

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Publication number
PE20230601A1
PE20230601A1 PE2022002121A PE2022002121A PE20230601A1 PE 20230601 A1 PE20230601 A1 PE 20230601A1 PE 2022002121 A PE2022002121 A PE 2022002121A PE 2022002121 A PE2022002121 A PE 2022002121A PE 20230601 A1 PE20230601 A1 PE 20230601A1
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Peru
Prior art keywords
alkyl
complement system
independently
inhibitors
union
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Application number
PE2022002121A
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English (en)
Inventor
Pravin L Kotian
Yarlagadda S Babu
Minwan Wu
zhao Dang
Trung Xuan Nguyen
Krishnan Raman
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Biocryst Pharm Inc
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Publication date
Application filed by Biocryst Pharm Inc filed Critical Biocryst Pharm Inc
Publication of PE20230601A1 publication Critical patent/PE20230601A1/es

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    • 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
    • C07D487/04Ortho-condensed systems
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • 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
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
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    • 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
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
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    • C07D473/32Nitrogen atom
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    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
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    • 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
    • C07D498/14Ortho-condensed systems
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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Saccharide Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Refiere a compuestos de formula (I), o sales farmaceuticamente aceptables de los mismos, que son inhibidores del sistema del complemento, en donde X es una union o C(RX)2; Y es una union, C(RY )2, o -N(Rb) -; G es S o C(R3)2; Ra y Rb son independientemente H o (C1-C6)alquilo; R1 se sustituye opcionalmente con alquenilo, cicloalquenilo entre otros; R2 representa heteroarilo biciclico o triciclico opcionalmente sustituido; R3 es independientemente (C1- C6)alcoxi, (C1-C6)alquilo, entre otros, o dos instancias vecinales, geminales y hominales junto con un atomo de carbono, forman un (C3-C7)cicloalquilo; RX y RY son H, (C1-C6)alquilo, o (C3-C7)cicloalquilo; R13 y R14 representan independientemente haloalquilo, heteroarilo, entre otros. Asimismo, refiere a composiciones farmaceuticas que comprenden el compuesto, o una sal de este, y un vehiculo farmaceuticamente aceptable, para tratar o prevenir una enfermedad o condicion caracterizada por la actividad aberrante del sistema del complemento, seleccionados del grupo que consiste en vasculitis asociada a anticuerpos contra el citoplasma de neutrofilos (ANCA) (AAV), sindrome de Guillain-Barre, enfermedad de Crohn, entre otros.
PE2022002121A 2020-04-03 2021-04-02 Pirrolopirimidinaminas como inhibidores del sistema del complemento PE20230601A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202063004799P 2020-04-03 2020-04-03
PCT/US2021/025547 WO2021202977A1 (en) 2020-04-03 2021-04-02 Pyrrolopyrimidine amines as complement inhibitors

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PE20230601A1 true PE20230601A1 (es) 2023-04-10

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US (1) US20230159536A1 (es)
EP (1) EP4125914A1 (es)
JP (1) JP2023519824A (es)
KR (1) KR20220163955A (es)
CN (1) CN115427044A (es)
AR (1) AR121715A1 (es)
AU (1) AU2021246098A1 (es)
BR (1) BR112022018067A2 (es)
CA (1) CA3176808A1 (es)
CL (1) CL2022002649A1 (es)
CO (1) CO2022015630A2 (es)
CR (1) CR20220553A (es)
CU (1) CU20220060A7 (es)
DO (1) DOP2022000211A (es)
EC (1) ECSP22085221A (es)
IL (1) IL296978A (es)
JO (1) JOP20220227A1 (es)
MX (1) MX2022012056A (es)
PE (1) PE20230601A1 (es)
TW (1) TW202204358A (es)
UY (1) UY39150A (es)
WO (1) WO2021202977A1 (es)

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CA3234428A1 (en) * 2021-10-18 2023-04-27 Nader Najafian Use of complement factor d inhibitor for treatment of lupus nephritis and immunoglobulin a nephropathy
WO2024008121A1 (zh) * 2022-07-06 2024-01-11 南京明德新药研发有限公司 二氟取代的氮杂双环化合物及其应用
WO2024047078A1 (en) * 2022-09-01 2024-03-07 F. Hoffmann-La Roche Ag Dosage regimen of vicasinabin
US11945818B1 (en) 2023-09-06 2024-04-02 King Faisal University Pyrrolo[3,2-c]quinoline compounds as CK2 inhibitors
US11964981B1 (en) 2023-09-18 2024-04-23 King Faisal University Substituted pyrimido[4,5-b]indoles as CK2 inhibitors

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EA023259B1 (ru) * 2011-01-04 2016-05-31 Новартис Аг Индольные соединения или их аналоги, полезные для лечения возрастной макулярной дегенерации (amd)

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CR20220553A (es) 2023-02-03
CN115427044A (zh) 2022-12-02
WO2021202977A1 (en) 2021-10-07
KR20220163955A (ko) 2022-12-12
TW202204358A (zh) 2022-02-01
AR121715A1 (es) 2022-06-29
US20230159536A1 (en) 2023-05-25
IL296978A (en) 2022-12-01
CU20220060A7 (es) 2023-05-11
CO2022015630A2 (es) 2022-11-29
UY39150A (es) 2021-10-29
JOP20220227A1 (ar) 2023-01-30
JP2023519824A (ja) 2023-05-15
CA3176808A1 (en) 2021-10-07
BR112022018067A2 (pt) 2022-10-25
CL2022002649A1 (es) 2023-05-26
AU2021246098A1 (en) 2022-10-20
MX2022012056A (es) 2022-10-13
DOP2022000211A (es) 2022-11-15
ECSP22085221A (es) 2022-12-30
EP4125914A1 (en) 2023-02-08

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