EA035063B1 - Соединения в качестве модуляторов ror гамма - Google Patents

Соединения в качестве модуляторов ror гамма Download PDF

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Publication number
EA035063B1
EA035063B1 EA201890329A EA201890329A EA035063B1 EA 035063 B1 EA035063 B1 EA 035063B1 EA 201890329 A EA201890329 A EA 201890329A EA 201890329 A EA201890329 A EA 201890329A EA 035063 B1 EA035063 B1 EA 035063B1
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mmol
compound
mixture
stirred
solution
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EA201890329A
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Russian (ru)
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EA201890329A1 (ru
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Джоанна Баконий
Стивен Ричард Брунетте
Делфин Коллин
Роберт Оуэн Хьюз
Сян Ли
Шуан Лян
Роберт Сибли
Майкл Роберт Тёрнер
Лифэнь Ву
Цян Чжан
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Бёрингер Ингельхайм Интернациональ Гмбх
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Publication of EA035063B1 publication Critical patent/EA035063B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
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    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
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    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • General Chemical & Material Sciences (AREA)
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  • Rheumatology (AREA)
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  • Diabetes (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Cardiology (AREA)
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  • Obesity (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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 EA201890329A1 (ru) 2018-07-31
EA035063B1 true EA035063B1 (ru) 2020-04-23

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

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EA201691978A EA031351B1 (ru) 2014-04-14 2015-04-10 СОЕДИНЕНИЯ В КАЧЕСТВЕ МОДУЛЯТОРОВ RORγ

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US (5) US9242989B2 (OSRAM)
EP (2) EP3418280B1 (OSRAM)
JP (2) JP6282759B2 (OSRAM)
KR (2) KR102410076B1 (OSRAM)
CN (3) CN106132965B (OSRAM)
AP (1) AP2016009403A0 (OSRAM)
AR (2) AR100058A1 (OSRAM)
AU (2) AU2015247983B2 (OSRAM)
BR (2) BR122020020657B1 (OSRAM)
CA (1) CA2944787C (OSRAM)
CL (1) CL2016002421A1 (OSRAM)
CY (1) CY1122012T1 (OSRAM)
DK (1) DK3131902T3 (OSRAM)
EA (2) EA031351B1 (OSRAM)
ES (1) ES2744299T3 (OSRAM)
HR (1) HRP20191579T1 (OSRAM)
HU (1) HUE045847T2 (OSRAM)
IL (2) IL247419B (OSRAM)
LT (1) LT3131902T (OSRAM)
MA (1) MA46373A (OSRAM)
ME (1) ME03513B (OSRAM)
MX (1) MX370780B (OSRAM)
MY (1) MY182834A (OSRAM)
NZ (1) NZ723530A (OSRAM)
PE (2) PE20161572A1 (OSRAM)
PH (2) PH12016502019B1 (OSRAM)
PL (1) PL3131902T3 (OSRAM)
PT (1) PT3131902T (OSRAM)
RS (1) RS59170B1 (OSRAM)
SG (1) SG11201608537SA (OSRAM)
SI (1) SI3131902T1 (OSRAM)
TW (2) TWI652268B (OSRAM)
UA (2) UA121255C2 (OSRAM)
UY (1) UY36077A (OSRAM)
WO (1) WO2015160654A1 (OSRAM)

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PE20161572A1 (es) 2014-04-14 2017-02-01 Boehringer Ingelheim Int Compuestos como moduladores de ror gamma
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)
JP6684516B2 (ja) 2015-05-15 2020-04-22 オーリジーン ディスカバリー テクノロジーズ リミテッドAurigene Discovery Technologies Limited Rorガンマ調節物質としての置換型テトラヒドロキノリン化合物
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
JP6448867B2 (ja) 2015-12-15 2019-01-09 アストラゼネカ・アクチエボラーグAstrazeneca Aktiebolag イソインドール化合物
WO2017127375A1 (en) * 2016-01-20 2017-07-27 Boehringer Ingelheim International Gmbh Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma
UY37507A (es) 2016-12-05 2018-06-29 Lead Pharma Holding Bv Moduladores de ror gamma (ror¿)
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HRP20230643T1 (hr) 2018-05-03 2023-09-29 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Derivati benzimidazola kao modulatori receptora siroče gama (rory) povezanih s retinoidima i njihova farmaceutska upotreba
CN112930336A (zh) 2018-10-18 2021-06-08 勃林格殷格翰国际有限公司 光学活性的1-环丙基烷基-1-胺的可放大合成
CA3154475A1 (en) 2019-09-23 2021-04-01 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
US20230014730A1 (en) 2019-09-23 2023-01-19 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
EP4053109A4 (en) 2019-10-31 2022-12-21 Jiangsu Hengrui Medicine Co., Ltd. ACID ADDITION SALT OF RORy REGULATOR
WO2022106547A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Process for synthesising a ror gamma inhibitor
WO2022106551A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Co-crystals of a ror gamma inhibitor
WO2022106550A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline polymorphic form of a ror gamma inhibitor
WO2022106549A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline salts of a ror gamma inhibitor
WO2022106548A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Solid forms of a ror gamma inhibitor
CN117003757A (zh) * 2022-05-07 2023-11-07 苏州浦合医药科技有限公司 取代的双环杂芳基化合物作为usp1抑制剂
WO2023232870A1 (en) 2022-05-31 2023-12-07 Immunic Ag Rorg/rorgt modulators for the treatment of virus infections like covid-19
CN116178279A (zh) * 2023-03-15 2023-05-30 上海药坦药物研究开发有限公司 一种5-溴-4-环丙基-6-甲氧基嘧啶及其中间体的制备方法
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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
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KR20160142396A (ko) 2016-12-12
UY36077A (es) 2015-10-30
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
US20150291607A1 (en) 2015-10-15
CY1122012T1 (el) 2020-10-14
AR100058A1 (es) 2016-09-07
JP6282759B2 (ja) 2018-02-21
KR20200040917A (ko) 2020-04-20
RS59170B1 (sr) 2019-10-31
JP6463855B2 (ja) 2019-02-06
EP3131902A1 (en) 2017-02-22
EA031351B1 (ru) 2018-12-28
AU2015247983A1 (en) 2016-09-08
MY182834A (en) 2021-02-05
PT3131902T (pt) 2019-09-17
AU2019203027A1 (en) 2019-05-23
TW201841915A (zh) 2018-12-01
KR102410076B1 (ko) 2022-06-22
TWI652268B (zh) 2019-03-01
PE20161572A1 (es) 2017-02-01
DK3131902T3 (da) 2019-09-02
AU2019203027B2 (en) 2020-07-09
ES2744299T3 (es) 2020-02-24
US20170008894A1 (en) 2017-01-12
UA120094C2 (uk) 2019-10-10
CA2944787A1 (en) 2015-10-22
CN107266454B (zh) 2019-08-09
TW201625622A (zh) 2016-07-16
EP3418280A1 (en) 2018-12-26
CN107266450B (zh) 2020-07-24
EA201691978A1 (ru) 2017-02-28
MX2016013342A (es) 2017-01-26
IL263878B (en) 2019-11-28
PE20211002A1 (es) 2021-06-01
NZ723530A (en) 2023-05-26
CN107266454A (zh) 2017-10-20
CN106132965A (zh) 2016-11-16
BR122020020657B1 (pt) 2022-12-20
US9242989B2 (en) 2016-01-26
BR112016021962B1 (pt) 2022-12-13
BR112016021962A2 (pt) 2023-01-20
JP2017511357A (ja) 2017-04-20
ME03513B (me) 2020-04-20
AP2016009403A0 (en) 2016-08-31
MX370780B (es) 2020-01-03
MA46373A (fr) 2019-08-07
SG11201608537SA (en) 2016-11-29
HUE045847T2 (hu) 2020-01-28
PH12020500252A1 (en) 2021-07-26
AR119454A2 (es) 2021-12-22
CN106132965B (zh) 2020-02-07
WO2015160654A1 (en) 2015-10-22
EP3418280B1 (en) 2023-07-12
HK1244801A1 (zh) 2018-08-17
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CN107266450A (zh) 2017-10-20
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US9598415B2 (en) 2017-03-21
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PL3131902T3 (pl) 2019-11-29
US20180022749A1 (en) 2018-01-25
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JP2018065874A (ja) 2018-04-26

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