CN107266454B - 作为RORγ调节剂的化合物 - Google Patents

作为RORγ调节剂的化合物 Download PDF

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Publication number
CN107266454B
CN107266454B CN201710445005.9A CN201710445005A CN107266454B CN 107266454 B CN107266454 B CN 107266454B CN 201710445005 A CN201710445005 A CN 201710445005A CN 107266454 B CN107266454 B CN 107266454B
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compound
mixture
solution
generate
stirred
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CN107266454A (zh
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J·巴科尼
S·R·布鲁内特
D·科林
R·O·休斯
X·李
梁爽
R·西布莉
M·R·特纳
L·吴
Q·张
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Boehringer Ingelheim International GmbH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
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    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D475/00—Heterocyclic compounds containing pteridine ring systems
    • C07D475/06—Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4
    • C07D475/10—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
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  • Ophthalmology & Optometry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Transplantation (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201710445005.9A 2014-04-14 2015-04-10 作为RORγ调节剂的化合物 Active CN107266454B (zh)

Applications Claiming Priority (3)

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US201461979231P 2014-04-14 2014-04-14
US61/979,231 2014-04-14
CN201580016630.0A CN106132965B (zh) 2014-04-14 2015-04-10 作为RORγ调节剂的化合物

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CN107266454B true CN107266454B (zh) 2019-08-09

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CN201580016630.0A Active CN106132965B (zh) 2014-04-14 2015-04-10 作为RORγ调节剂的化合物
CN201710445827.7A Active CN107266450B (zh) 2014-04-14 2015-04-10 作为RORγ调节剂的化合物

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CN201710445827.7A Active CN107266450B (zh) 2014-04-14 2015-04-10 作为RORγ调节剂的化合物

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EP (2) EP3418280B1 (enExample)
JP (2) JP6282759B2 (enExample)
KR (2) KR102410076B1 (enExample)
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HRP20191579T1 (hr) 2014-04-14 2019-11-29 Boehringer Ingelheim Int Spojevi kao modulatori za ror gama
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)
BR112017024517A2 (pt) 2015-05-15 2018-07-24 Aurigene Discovery Technologies Limited compostos de tetraidroquinolinona como moduladores ror gama
US10450314B2 (en) 2015-10-01 2019-10-22 Boehringer Ingelheim International Gmbh Pteridine derivatives as modulators of ROR gamma
ES2927631T3 (es) 2015-12-15 2022-11-08 Astrazeneca Ab Compuestos de isoindol
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TWI705958B (zh) 2016-12-05 2020-10-01 荷蘭商領導醫藥控股責任有限公司 ＲＯＲγ調節子
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JP2020524660A (ja) 2017-06-14 2020-08-20 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ Ｒｏｒ−ガンマモジュレーターとして有用な２，３−ジヒドロイソインドール−１−カルボキサミド
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
MX2020011405A (es) 2018-05-03 2021-01-08 Jiangsu Hengrui Medicine Co Derivados de bencimidazol como moduladores del receptor gamma huerfano (rory) relacionado con retinoide y usos farmaceuticos de los mismos.
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
EP4034094A4 (en) 2019-09-23 2024-01-24 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
KR20220093340A (ko) 2019-10-31 2022-07-05 지앙수 헨그루이 메디슨 컴퍼니 리미티드 RORγ 조절제의 산부가염
WO2022106551A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Co-crystals of a ror gamma inhibitor
WO2022106547A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Process for synthesising 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
AU2024267864A1 (en) * 2023-05-09 2025-11-06 11949098 Canada Inc. Inverse agonists of rar related orphan receptors (rors)

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HRP20191579T1 (hr) * 2014-04-14 2019-11-29 Boehringer Ingelheim Int Spojevi kao modulatori za ror gama
US10450314B2 (en) * 2015-10-01 2019-10-22 Boehringer Ingelheim International Gmbh Pteridine derivatives as modulators of ROR gamma
JP6899391B2 (ja) * 2016-01-20 2021-07-07 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 ガンマのモジュレータとしての化合物

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WO2013170671A1 (zh) * 2012-05-14 2013-11-21 华东理工大学 蝶啶酮衍生物及其作为egfr、blk、flt3抑制剂的应用

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LT3131902T (lt) 2019-09-25
BR112016021962B1 (pt) 2022-12-13
MX2016013342A (es) 2017-01-26
PH12016502019B1 (en) 2020-10-23
HK1244800A1 (zh) 2018-08-17
HUE045847T2 (hu) 2020-01-28
EP3418280A1 (en) 2018-12-26
PT3131902T (pt) 2019-09-17
US20160075706A1 (en) 2016-03-17
MX370780B (es) 2020-01-03
AP2016009403A0 (en) 2016-08-31
TW201841915A (zh) 2018-12-01
CN107266454A (zh) 2017-10-20
BR122020020657B1 (pt) 2022-12-20
EP3131902A1 (en) 2017-02-22
HRP20191579T1 (hr) 2019-11-29
EA201691978A1 (ru) 2017-02-28
TW201625622A (zh) 2016-07-16
AU2019203027A1 (en) 2019-05-23
EP3131902B1 (en) 2019-06-12
RS59170B1 (sr) 2019-10-31
CN106132965B (zh) 2020-02-07
PH12020500252A1 (en) 2021-07-26
US9598415B2 (en) 2017-03-21
CA2944787A1 (en) 2015-10-22
EA035063B1 (ru) 2020-04-23
JP2017511357A (ja) 2017-04-20
UA120094C2 (uk) 2019-10-10
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CA2944787C (en) 2023-03-14
IL263878B (en) 2019-11-28
US20190002465A1 (en) 2019-01-03
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BR112016021962A2 (pt) 2023-01-20
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TWI655192B (zh) 2019-04-01
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US20180022749A1 (en) 2018-01-25
PE20211002A1 (es) 2021-06-01
AU2019203027B2 (en) 2020-07-09
DK3131902T3 (da) 2019-09-02
EA201890329A1 (ru) 2018-07-31
CN107266450B (zh) 2020-07-24
CL2016002421A1 (es) 2017-03-24
HK1244801A1 (zh) 2018-08-17
UA121255C2 (uk) 2020-04-27
AU2015247983A1 (en) 2016-09-08
JP6463855B2 (ja) 2019-02-06
KR20160142396A (ko) 2016-12-12
KR20200040917A (ko) 2020-04-20
CN107266450A (zh) 2017-10-20
SI3131902T1 (sl) 2019-10-30
US20150291607A1 (en) 2015-10-15
MY182834A (en) 2021-02-05
ES2744299T3 (es) 2020-02-24
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
TWI652268B (zh) 2019-03-01
PH12016502019A1 (en) 2017-01-09
AR119454A2 (es) 2021-12-22
US20170008894A1 (en) 2017-01-12
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PE20161572A1 (es) 2017-02-01
MA46373A (fr) 2019-08-07
JP2018065874A (ja) 2018-04-26
KR102410076B1 (ko) 2022-06-22
JP6282759B2 (ja) 2018-02-21
KR102410069B1 (ko) 2022-06-20
PL3131902T3 (pl) 2019-11-29
WO2015160654A1 (en) 2015-10-22
NZ723530A (en) 2023-05-26

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