EA201890329A1 - СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ RORγ - Google Patents

СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ RORγ

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Publication number
EA201890329A1
EA201890329A1 EA201890329A EA201890329A EA201890329A1 EA 201890329 A1 EA201890329 A1 EA 201890329A1 EA 201890329 A EA201890329 A EA 201890329A EA 201890329 A EA201890329 A EA 201890329A EA 201890329 A1 EA201890329 A1 EA 201890329A1
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EA
Eurasian Patent Office
Prior art keywords
connections
rorγ
rorγ modulators
formula
present
Prior art date
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EA201890329A
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English (en)
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EA035063B1 (ru
Inventor
Джоанна Баконий
Стивен Ричард Брунетте
Делфин Коллин
Роберт Оуэн Хьюз
Сян Ли
Шуан Лян
Роберт Сибли
Майкл Роберт Тёрнер
Лифэнь Ву
Цян Чжан
Original Assignee
Бёрингер Ингельхайм Интернациональ Гмбх
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Publication of EA201890329A1 publication Critical patent/EA201890329A1/ru
Publication of EA035063B1 publication Critical patent/EA035063B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D475/00Heterocyclic compounds containing pteridine ring 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
    • 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
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
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    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/06Antiasthmatics
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    • A61P13/00Drugs for disorders of the urinary system
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    • AHUMAN NECESSITIES
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    • AHUMAN NECESSITIES
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    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
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    • A61P9/00Drugs for disorders of the cardiovascular system
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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
    • C07D475/00Heterocyclic compounds containing pteridine ring systems
    • C07D475/06Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/10Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with an aromatic or hetero-aromatic ring directly attached in position 2
    • CCHEMISTRY; METALLURGY
    • 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

Abstract

Настоящее изобретение охватывает соединения формулы (I)где переменные, определенные здесь, пригодны для модуляции RORγ и лечения заболеваний, связанных с модуляцией RORγ. Настоящее изобретение также охватывает способы получения соединений формулы (I) и содержащие их фармацевтические препараты.
EA201890329A 2014-04-14 2015-04-10 Соединения в качестве модуляторов ror гамма EA035063B1 (ru)

Applications Claiming Priority (1)

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US201461979231P 2014-04-14 2014-04-14

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EA201890329A1 true EA201890329A1 (ru) 2018-07-31
EA035063B1 EA035063B1 (ru) 2020-04-23

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EA201890329A EA035063B1 (ru) 2014-04-14 2015-04-10 Соединения в качестве модуляторов ror гамма
EA201691978A EA031351B1 (ru) 2014-04-14 2015-04-10 СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ RORγ

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US (5) US9242989B2 (ru)
EP (2) EP3131902B1 (ru)
JP (2) JP6282759B2 (ru)
KR (2) KR102410076B1 (ru)
CN (3) CN106132965B (ru)
AP (1) AP2016009403A0 (ru)
AR (2) AR100058A1 (ru)
AU (2) AU2015247983B2 (ru)
BR (2) BR122020020657B1 (ru)
CA (1) CA2944787C (ru)
CL (1) CL2016002421A1 (ru)
CY (1) CY1122012T1 (ru)
DK (1) DK3131902T3 (ru)
EA (2) EA035063B1 (ru)
ES (1) ES2744299T3 (ru)
HK (2) HK1244801A1 (ru)
HR (1) HRP20191579T1 (ru)
HU (1) HUE045847T2 (ru)
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LT (1) LT3131902T (ru)
MA (1) MA46373A (ru)
ME (1) ME03513B (ru)
MX (1) MX370780B (ru)
MY (1) MY182834A (ru)
NZ (1) NZ723530A (ru)
PE (2) PE20161572A1 (ru)
PH (2) PH12016502019B1 (ru)
PL (1) PL3131902T3 (ru)
PT (1) PT3131902T (ru)
RS (1) RS59170B1 (ru)
SG (1) SG11201608537SA (ru)
SI (1) SI3131902T1 (ru)
TW (2) TWI652268B (ru)
UA (2) UA120094C2 (ru)
UY (1) UY36077A (ru)
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CN106132965B (zh) * 2014-04-14 2020-02-07 勃林格殷格翰国际有限公司 作为RORγ调节剂的化合物
FR3030518B1 (fr) * 2014-12-19 2018-03-23 Galderma Research & Development Derives sulfonamides en tant qu'agonistes inverses du recepteur gamma orphelin associe aux retinoides ror gamma (t)
RS62016B1 (sr) 2015-05-15 2021-07-30 Aurigene Discovery Tech Ltd Supstituisana jedinjenja tetrahidrohinolina kao modulatori ror gama receptora
JP6778259B2 (ja) * 2015-10-01 2020-10-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Rorガンマのモジュレーターとしてのプテリジン誘導体
TN2018000188A1 (en) 2015-12-15 2019-10-04 Astrazeneca Ab Isoindole compounds
EP3405470B1 (en) * 2016-01-20 2020-07-15 Boehringer Ingelheim International GmbH Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma
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US20200031753A1 (en) 2017-04-06 2020-01-30 Boehringer Ingelheim International Gmbh Cyclopropyl alkyl amines and process for their preparation
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CN109206346A (zh) * 2017-07-01 2019-01-15 复旦大学 叔胺类衍生物或其盐及其制备方法和用途
CN107903263B (zh) * 2017-12-28 2019-11-12 山东铂源药业有限公司 一种帕布昔利布中间体的合成方法
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BR112022008293A2 (pt) 2019-10-31 2022-07-26 Jiangsu Hengrui Medicine Co Sal de adição de ácido de regulador de ror?, composições farmacêuticas, uso dos mesmos e métodos para preparar forma cristalina e composição farmacêutica
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JP6778259B2 (ja) * 2015-10-01 2020-10-28 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Rorガンマのモジュレーターとしてのプテリジン誘導体
EP3405470B1 (en) * 2016-01-20 2020-07-15 Boehringer Ingelheim International GmbH Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma

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CN106132965A (zh) 2016-11-16
US20170008894A1 (en) 2017-01-12
MY182834A (en) 2021-02-05
CN107266450A (zh) 2017-10-20
UA121255C2 (uk) 2020-04-27
EA031351B1 (ru) 2018-12-28
ES2744299T3 (es) 2020-02-24
CL2016002421A1 (es) 2017-03-24
JP2018065874A (ja) 2018-04-26
US9598415B2 (en) 2017-03-21
KR20200040917A (ko) 2020-04-20
NZ723530A (en) 2023-05-26
TW201625622A (zh) 2016-07-16
KR102410076B1 (ko) 2022-06-22
BR122020020657B1 (pt) 2022-12-20
UY36077A (es) 2015-10-30
PE20211002A1 (es) 2021-06-01
MA46373A (fr) 2019-08-07
UA120094C2 (uk) 2019-10-10
EP3131902B1 (en) 2019-06-12
EA201691978A1 (ru) 2017-02-28
HUE045847T2 (hu) 2020-01-28
KR102410069B1 (ko) 2022-06-20
DK3131902T3 (da) 2019-09-02
AR100058A1 (es) 2016-09-07
CN107266454B (zh) 2019-08-09
EP3131902A1 (en) 2017-02-22
US20180022749A1 (en) 2018-01-25
AU2019203027A1 (en) 2019-05-23
MX2016013342A (es) 2017-01-26
CA2944787C (en) 2023-03-14
AR119454A2 (es) 2021-12-22
PH12016502019A1 (en) 2017-01-09
AP2016009403A0 (en) 2016-08-31
AU2015247983A1 (en) 2016-09-08
TWI655192B (zh) 2019-04-01
CN106132965B (zh) 2020-02-07
BR112016021962B1 (pt) 2022-12-13
PL3131902T3 (pl) 2019-11-29
SI3131902T1 (sl) 2019-10-30
US20160075706A1 (en) 2016-03-17
HK1244801A1 (zh) 2018-08-17
HK1244800A1 (zh) 2018-08-17
US20150291607A1 (en) 2015-10-15
WO2015160654A1 (en) 2015-10-22
JP2017511357A (ja) 2017-04-20
AU2019203027B2 (en) 2020-07-09
PE20161572A1 (es) 2017-02-01
US20190002465A1 (en) 2019-01-03
ME03513B (me) 2020-04-20
CY1122012T1 (el) 2020-10-14
PT3131902T (pt) 2019-09-17
SG11201608537SA (en) 2016-11-29
CA2944787A1 (en) 2015-10-22
JP6463855B2 (ja) 2019-02-06
BR112016021962A2 (pt) 2023-01-20
PH12020500252A1 (en) 2021-07-26
PH12016502019B1 (en) 2017-01-09
TW201841915A (zh) 2018-12-01
EP3418280B1 (en) 2023-07-12
US9242989B2 (en) 2016-01-26
AU2015247983B2 (en) 2019-05-16
CN107266450B (zh) 2020-07-24
MX370780B (es) 2020-01-03
JP6282759B2 (ja) 2018-02-21
LT3131902T (lt) 2019-09-25
KR20160142396A (ko) 2016-12-12
EP3418280A1 (en) 2018-12-26
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
HRP20191579T1 (hr) 2019-11-29
CN107266454A (zh) 2017-10-20
IL263878B (en) 2019-11-28
RS59170B1 (sr) 2019-10-31
EA035063B1 (ru) 2020-04-23
TWI652268B (zh) 2019-03-01

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