EA201990604A1 - Aryl, heteroaryl and heterocyclic compounds for the treatment of complement-mediated disorders - Google Patents

Aryl, heteroaryl and heterocyclic compounds for the treatment of complement-mediated disorders

Info

Publication number
EA201990604A1
EA201990604A1 EA201990604A EA201990604A EA201990604A1 EA 201990604 A1 EA201990604 A1 EA 201990604A1 EA 201990604 A EA201990604 A EA 201990604A EA 201990604 A EA201990604 A EA 201990604A EA 201990604 A1 EA201990604 A1 EA 201990604A1
Authority
EA
Eurasian Patent Office
Prior art keywords
complement
factor
heteroaryl
aryl
treatment
Prior art date
Application number
EA201990604A
Other languages
Russian (ru)
Other versions
EA038607B1 (en
Inventor
Венкат Рао Гадхачанда
Цюпин Ван
Годвин Пэйс
Акихиро Хашимото
Давей Чэнь
Сянчжу Ван
Атул Агарвал
Милинд Дешпанде
Авинаш С. Фадке
Джейсон Аллан Вайлс
Original Assignee
Ачиллион Фармасьютикалс, Инк.
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 Ачиллион Фармасьютикалс, Инк. filed Critical Ачиллион Фармасьютикалс, Инк.
Publication of EA201990604A1 publication Critical patent/EA201990604A1/en
Publication of EA038607B1 publication Critical patent/EA038607B1/en

Links

Classifications

    • 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
    • A61K31/40Heterocyclic 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
    • A61K31/401Proline; Derivatives thereof, e.g. captopril
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders

Abstract

Заявлены соединения, способы применения и способы получения ингибиторов фактора D комплемента, включающих формулу I, или их фармацевтически приемлемая соль, или их композиция, где Rили Rна группе A представляет собой арил, гетероарил или гетероцикл (R). Описанные в настоящем документе ингибиторы воздействуют на фактор D и ингибируют или регулируют каскад комплемента в ранней и существенной точке альтернативного пути комплемента, и снижают способность фактора D модулировать классический и лектиновый пути комплемента. Описанные в настоящем документе ингибиторы фактора D способны снижать чрезмерную активацию комплемента, которая связана с определенными аутоиммунными, воспалительными и нейродегенеративными заболеваниями, а также ишемически-реперфузионными повреждениями и раком.The claimed compounds, methods of use and methods for the preparation of inhibitors of factor D complement, including formula I, or a pharmaceutically acceptable salt, or a composition thereof, where R or R on group A is aryl, heteroaryl or heterocycle (R). The inhibitors described herein act on factor D and inhibit or regulate the complement cascade at an early and significant point in the alternative complement pathway and reduce the ability of factor D to modulate the classical and lectin complement pathways. The factor D inhibitors described herein are capable of reducing excessive complement activation, which is associated with certain autoimmune, inflammatory and neurodegenerative diseases, as well as ischemia-reperfusion injury and cancer.

EA201990604A 2014-09-05 2015-02-25 Aryl, heteroaryl and heterocyclic compounds for treating complement-mediated disorders EA038607B1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462046783P 2014-09-05 2014-09-05

Publications (2)

Publication Number Publication Date
EA201990604A1 true EA201990604A1 (en) 2020-01-09
EA038607B1 EA038607B1 (en) 2021-09-22

Family

ID=69374504

Family Applications (2)

Application Number Title Priority Date Filing Date
EA202191781A EA202191781A1 (en) 2014-09-05 2015-02-25 ARYL, HETEROARYL AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF DISORDERS MEDIED BY THE COMPLETE
EA201990604A EA038607B1 (en) 2014-09-05 2015-02-25 Aryl, heteroaryl and heterocyclic compounds for treating complement-mediated disorders

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA202191781A EA202191781A1 (en) 2014-09-05 2015-02-25 ARYL, HETEROARYL AND HETEROCYCLIC COMPOUNDS FOR TREATMENT OF DISORDERS MEDIED BY THE COMPLETE

Country Status (1)

Country Link
EA (2) EA202191781A1 (en)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK2119703T3 (en) * 2007-01-15 2013-01-14 Santen Pharmaceutical Co Ltd New indole derivative with inhibitory effect on I-B kinase.
SG191844A1 (en) * 2011-01-04 2013-08-30 Novartis Ag Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)
US9056874B2 (en) * 2012-05-04 2015-06-16 Novartis Ag Complement pathway modulators and uses thereof

Also Published As

Publication number Publication date
EA038607B1 (en) 2021-09-22
EA202191781A1 (en) 2021-09-03

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