AU2015247983B2 - Compounds as modulators of ROR gamma - Google Patents

Compounds as modulators of ROR gamma Download PDF

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Publication number
AU2015247983B2
AU2015247983B2 AU2015247983A AU2015247983A AU2015247983B2 AU 2015247983 B2 AU2015247983 B2 AU 2015247983B2 AU 2015247983 A AU2015247983 A AU 2015247983A AU 2015247983 A AU2015247983 A AU 2015247983A AU 2015247983 B2 AU2015247983 B2 AU 2015247983B2
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cycloalkyl
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halo
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AU2015247983A1 (en
Inventor
Johanna Bakonyi
Steven Richard Brunette
Delphine Collin
Robert Owen Hughes
Xiang Li
Shuang Liang
Robert Sibley
Michael Robert Turner
Lifen Wu
Qiang Zhang
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
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    • 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
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
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    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
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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
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
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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
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    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Cardiology (AREA)
  • Otolaryngology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
AU2015247983A 2014-04-14 2015-04-10 Compounds as modulators of ROR gamma Ceased AU2015247983B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2019203027A AU2019203027B2 (en) 2014-04-14 2019-04-30 Compounds as modulators of ROR gamma

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461979231P 2014-04-14 2014-04-14
US61/979,231 2014-04-14
PCT/US2015/025328 WO2015160654A1 (en) 2014-04-14 2015-04-10 Compounds as modulators of ror gamma

Related Child Applications (1)

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AU2019203027A Division AU2019203027B2 (en) 2014-04-14 2019-04-30 Compounds as modulators of ROR gamma

Publications (2)

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AU2015247983A1 AU2015247983A1 (en) 2016-09-08
AU2015247983B2 true AU2015247983B2 (en) 2019-05-16

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AU2019203027A Ceased AU2019203027B2 (en) 2014-04-14 2019-04-30 Compounds as modulators of ROR gamma

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EP (2) EP3418280B1 (enExample)
JP (2) JP6282759B2 (enExample)
KR (2) KR102410069B1 (enExample)
CN (3) CN106132965B (enExample)
AP (1) AP2016009403A0 (enExample)
AR (2) AR100058A1 (enExample)
AU (2) AU2015247983B2 (enExample)
BR (2) BR112016021962A2 (enExample)
CA (1) CA2944787C (enExample)
CL (1) CL2016002421A1 (enExample)
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WO2015160654A1 (en) 2014-04-14 2015-10-22 Boehringer Ingelheim International Gmbh Compounds as modulators of 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)
MX394388B (es) 2015-05-15 2025-03-21 Aurigene Discovery Tech Ltd Compuestos de tetrahidroquinolinona sustituidos como moduladores de ror gamma
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
CN109071516B (zh) 2015-12-15 2021-08-31 阿斯利康(瑞典)有限公司 新颖的化合物
EP3405470B1 (en) * 2016-01-20 2020-07-15 Boehringer Ingelheim International GmbH Pyrazinedihydropyrimidinone or pyridazinedihydropyrimidinone compounds as modulators of ror gamma
AR110481A1 (es) 2016-12-05 2019-04-03 Lead Pharma Holding Bv MODULADORES DE ROR g (RORg)
US20200031753A1 (en) 2017-04-06 2020-01-30 Boehringer Ingelheim International Gmbh Cyclopropyl alkyl amines and process for their preparation
WO2018229155A1 (en) 2017-06-14 2018-12-20 Astrazeneca Ab 2,3-dihydroisoindole-1-carboxamides useful as ror-gamma modulators
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
AU2019262169B2 (en) 2018-05-03 2024-05-02 Jiangsu Hengrui Medicine Co., Ltd. Benzimidazole derivatives as modulators of retinoid-related orphan receptor gamma (RORy) and pharmaceutical uses thereof
US20210395185A1 (en) 2018-10-18 2021-12-23 Boehringer Ingelheim International Gmbh Scalable synthesis of optically active 1-cyclopropylalkyl-1-amines
US20230014730A1 (en) 2019-09-23 2023-01-19 Nanjing Zhengxiang Pharmaceuticals Co., Ltd. Phosphodiesterase inhibitors and use
US20220411380A1 (en) 2019-10-31 2022-12-29 Jiangsu Hengrui Medicine Co., Ltd. ACID ADDITION SALT OF RORy REGULATOR
WO2022106548A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Solid forms of a ror gamma inhibitor
WO2022106549A1 (en) 2020-11-19 2022-05-27 Boehringer Ingelheim International Gmbh Crystalline salts 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
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
WO2023216910A1 (zh) * 2022-05-07 2023-11-16 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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WO2003024966A1 (en) * 2001-08-14 2003-03-27 Astrazeneca Ab Pteridinone derivatives as modulators of chemokine receptor activity
WO2009022185A2 (en) * 2007-08-16 2009-02-19 Astrazeneca Ab 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use

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WO2011049917A1 (en) 2009-10-21 2011-04-28 Boehringer Ingelheim International Gmbh Indazole and pyrazolopyridine compounds as ccr1 receptor antagonists
CN103717070A (zh) * 2011-06-01 2014-04-09 贾纳斯生物治疗有限公司 新型免疫系统调节剂
DE112013002484B4 (de) * 2012-05-14 2023-05-04 Shanghai Yidian Pharmaceutical Technology Development Co., Ltd. Pteridinketon-Derivat und Anwendungen desselben als EGFR-, BLK- und FLT3-Inhibitor
WO2015160654A1 (en) * 2014-04-14 2015-10-22 Boehringer Ingelheim International Gmbh Compounds as modulators of ror gamma
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

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2003024966A1 (en) * 2001-08-14 2003-03-27 Astrazeneca Ab Pteridinone derivatives as modulators of chemokine receptor activity
WO2009022185A2 (en) * 2007-08-16 2009-02-19 Astrazeneca Ab 6, 6-fused heterocycles, their pharmaceutical compositions and methos of use

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NZ723530A (en) 2023-05-26
TWI652268B (zh) 2019-03-01
AU2019203027A1 (en) 2019-05-23
HRP20191579T1 (hr) 2019-11-29
LT3131902T (lt) 2019-09-25
US20160075706A1 (en) 2016-03-17
JP6282759B2 (ja) 2018-02-21
MA46373A (fr) 2019-08-07
UA121255C2 (uk) 2020-04-27
CN106132965B (zh) 2020-02-07
EP3418280B1 (en) 2023-07-12
CY1122012T1 (el) 2020-10-14
KR20160142396A (ko) 2016-12-12
CA2944787C (en) 2023-03-14
AU2015247983A1 (en) 2016-09-08
JP2018065874A (ja) 2018-04-26
UY36077A (es) 2015-10-30
PL3131902T3 (pl) 2019-11-29
MX370780B (es) 2020-01-03
IL247419B (en) 2019-03-31
IL263878A (en) 2019-01-31
TW201625622A (zh) 2016-07-16
EA201890329A1 (ru) 2018-07-31
JP2017511357A (ja) 2017-04-20
HUE045847T2 (hu) 2020-01-28
IL263878B (en) 2019-11-28
US20150291607A1 (en) 2015-10-15
EP3131902B1 (en) 2019-06-12
AU2019203027B2 (en) 2020-07-09
PH12016502019A1 (en) 2017-01-09
KR102410069B1 (ko) 2022-06-20
CN107266450A (zh) 2017-10-20
MX2016013342A (es) 2017-01-26
PE20161572A1 (es) 2017-02-01
WO2015160654A1 (en) 2015-10-22
EA035063B1 (ru) 2020-04-23
PT3131902T (pt) 2019-09-17
PH12016502019B1 (en) 2020-10-23
KR20200040917A (ko) 2020-04-20
ES2744299T3 (es) 2020-02-24
CN107266450B (zh) 2020-07-24
CN107266454A (zh) 2017-10-20
UA120094C2 (uk) 2019-10-10
AR119454A2 (es) 2021-12-22
MY182834A (en) 2021-02-05
BR112016021962A2 (pt) 2023-01-20
ME03513B (me) 2020-04-20
US9242989B2 (en) 2016-01-26
US20180022749A1 (en) 2018-01-25
TW201841915A (zh) 2018-12-01
PE20211002A1 (es) 2021-06-01
EA201691978A1 (ru) 2017-02-28
US20170008894A1 (en) 2017-01-12
AR100058A1 (es) 2016-09-07
HK1244800A1 (zh) 2018-08-17
PH12020500252A1 (en) 2021-07-26
HK1244801A1 (zh) 2018-08-17
EA031351B1 (ru) 2018-12-28
US20190002465A1 (en) 2019-01-03
TWI655192B (zh) 2019-04-01
CA2944787A1 (en) 2015-10-22
SI3131902T1 (sl) 2019-10-30
CN107266454B (zh) 2019-08-09
DK3131902T3 (da) 2019-09-02
JP6463855B2 (ja) 2019-02-06
EP3131902A1 (en) 2017-02-22
BR112016021962B1 (pt) 2022-12-13
AP2016009403A0 (en) 2016-08-31
BR122020020657B1 (pt) 2022-12-20
RS59170B1 (sr) 2019-10-31
US9598415B2 (en) 2017-03-21
SG11201608537SA (en) 2016-11-29
KR102410076B1 (ko) 2022-06-22
CN106132965A (zh) 2016-11-16
CL2016002421A1 (es) 2017-03-24
EP3418280A1 (en) 2018-12-26

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