JP2018525379A5 - - Google Patents
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- Publication number
- JP2018525379A5 JP2018525379A5 JP2018506144A JP2018506144A JP2018525379A5 JP 2018525379 A5 JP2018525379 A5 JP 2018525379A5 JP 2018506144 A JP2018506144 A JP 2018506144A JP 2018506144 A JP2018506144 A JP 2018506144A JP 2018525379 A5 JP2018525379 A5 JP 2018525379A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- heterocyclyl
- aryl
- independently
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 90
- 125000000623 heterocyclic group Chemical group 0.000 claims 78
- 125000003118 aryl group Chemical group 0.000 claims 73
- -1 -OH Chemical group 0.000 claims 53
- 125000000217 alkyl group Chemical group 0.000 claims 45
- 229910052799 carbon Inorganic materials 0.000 claims 23
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 22
- 125000003545 alkoxy group Chemical group 0.000 claims 19
- 125000002950 monocyclic group Chemical group 0.000 claims 19
- 125000005843 halogen group Chemical group 0.000 claims 17
- 125000002757 morpholinyl group Chemical group 0.000 claims 14
- 125000004452 carbocyclyl group Chemical group 0.000 claims 11
- 125000001424 substituent group Chemical group 0.000 claims 11
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 10
- 125000004076 pyridyl group Chemical group 0.000 claims 9
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 8
- 125000003226 pyrazolyl group Chemical group 0.000 claims 8
- 150000001721 carbon Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000006620 amino-(C1-C6) alkyl group Chemical group 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000003373 pyrazinyl group Chemical group 0.000 claims 6
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 125000000304 alkynyl group Chemical group 0.000 claims 5
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 4
- 125000003386 piperidinyl group Chemical group 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 3
- 125000002433 cyclopentenyl group Chemical group C1(=CCCC1)* 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 2
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 201000005569 Gout Diseases 0.000 claims 2
- 206010059176 Juvenile idiopathic arthritis Diseases 0.000 claims 2
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000005110 aryl thio group Chemical group 0.000 claims 2
- 125000004104 aryloxy group Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 125000004655 dihydropyridinyl group Chemical group N1(CC=CC=C1)* 0.000 claims 2
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 2
- 125000005113 hydroxyalkoxy group Chemical group 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 201000002215 juvenile rheumatoid arthritis Diseases 0.000 claims 2
- 125000006405 methylpyridazinyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 230000000737 periodic effect Effects 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 125000002098 pyridazinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 125000004853 tetrahydropyridinyl group Chemical group N1(CCCC=C1)* 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010016207 Familial Mediterranean fever Diseases 0.000 claims 1
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000003456 Juvenile Arthritis Diseases 0.000 claims 1
- 208000005777 Lupus Nephritis Diseases 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000000068 chlorophenyl group Chemical group 0.000 claims 1
- 208000004921 cutaneous lupus erythematosus Diseases 0.000 claims 1
- 125000004802 cyanophenyl group Chemical group 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 208000024908 graft versus host disease Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000003944 tolyl group Chemical group 0.000 claims 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562200424P | 2015-08-03 | 2015-08-03 | |
| US62/200,424 | 2015-08-03 | ||
| PCT/US2016/045110 WO2017023905A1 (en) | 2015-08-03 | 2016-08-02 | Heterocyclic compounds useful as modulators of tnf alpha |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018525379A JP2018525379A (ja) | 2018-09-06 |
| JP2018525379A5 true JP2018525379A5 (https=) | 2019-08-15 |
| JP6955482B2 JP6955482B2 (ja) | 2021-10-27 |
Family
ID=56618285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018506144A Active JP6955482B2 (ja) | 2015-08-03 | 2016-08-02 | Ｔｎｆアルファの修飾因子として有用なヘテロ環化合物 |
Country Status (22)
| Country | Link |
|---|---|
| US (1) | US10865191B2 (https=) |
| EP (1) | EP3331871A1 (https=) |
| JP (1) | JP6955482B2 (https=) |
| KR (1) | KR102697810B1 (https=) |
| CN (1) | CN108137547B (https=) |
| AR (1) | AR105575A1 (https=) |
| AU (1) | AU2016302144B2 (https=) |
| BR (1) | BR112018001960A2 (https=) |
| CA (1) | CA2994717A1 (https=) |
| CL (1) | CL2018000293A1 (https=) |
| CO (1) | CO2018002061A2 (https=) |
| EA (1) | EA033686B1 (https=) |
| HK (1) | HK1252623A1 (https=) |
| IL (1) | IL257154A (https=) |
| MA (1) | MA43512A (https=) |
| MX (1) | MX375341B (https=) |
| PE (1) | PE20181366A1 (https=) |
| SG (1) | SG10201911831RA (https=) |
| TW (1) | TW201718536A (https=) |
| UY (1) | UY36838A (https=) |
| WO (1) | WO2017023905A1 (https=) |
| ZA (1) | ZA201800716B (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016168633A1 (en) | 2015-04-17 | 2016-10-20 | Abbvie Inc. | Indazolones as modulators of tnf signaling |
| US9879016B2 (en) | 2015-04-17 | 2018-01-30 | Abbvie Inc. | Indazolones as modulators of TNF signaling |
| EP3288939A1 (en) | 2015-04-17 | 2018-03-07 | AbbVie Inc. | Tricyclic modulators of tnf signaling |
| GB201510758D0 (en) | 2015-06-18 | 2015-08-05 | Ucb Biopharma Sprl | Novel TNFa structure for use in therapy |
| GB201513742D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| CN108026050B (zh) | 2015-08-03 | 2021-04-30 | 格兰马克药品股份有限公司 | 作为RORγ调节剂的新型化合物 |
| GB201621907D0 (en) | 2016-12-21 | 2017-02-01 | Ucb Biopharma Sprl And Sanofi | Antibody epitope |
| JOP20190257A1 (ar) | 2017-04-28 | 2019-10-28 | Novartis Ag | مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats |
| JP2021512898A (ja) * | 2018-02-09 | 2021-05-20 | アメリカ合衆国 | 複素環ｐ２ｙ１４受容体拮抗薬 |
| CN108658977A (zh) * | 2018-04-12 | 2018-10-16 | 苏州康润医药有限公司 | 一种7-溴-1,5-萘啶-3-甲酸的合成方法 |
| CN115803317B (zh) | 2020-05-19 | 2025-07-15 | 拜耳作物科学股份公司 | 作为杀真菌化合物的氮杂双环(硫代)酰胺 |
| WO2021249995A1 (en) | 2020-06-10 | 2021-12-16 | Bayer Aktiengesellschaft | Azabicyclyl-substituted heterocycles as fungicides |
| US11926632B2 (en) | 2020-06-22 | 2024-03-12 | Pmv Pharmaceuticals, Inc. | Methods and compounds for restoring mutant p53 function |
| JP2023532888A (ja) | 2020-06-27 | 2023-08-01 | クレセンタ バイオサイエンシズ | 細胞代謝を調節する化合物の組成及び使用方法 |
| JP2023550830A (ja) * | 2020-11-27 | 2023-12-05 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | Ｐ２ｘ３阻害剤としての（アザ）キノリン４－アミン誘導体 |
| WO2022140456A1 (en) * | 2020-12-22 | 2022-06-30 | Mekanistic Therapeutics Llc | Substituted aminobenzyl heteroaryl compounds as egfr and/or pi3k inhibitors |
| CN117999263A (zh) * | 2021-09-29 | 2024-05-07 | 上海海和药物研究开发股份有限公司 | 一类具有吡啶并六元环结构的sos1抑制剂 |
| US20240425501A1 (en) * | 2021-10-21 | 2024-12-26 | Sanjita Sasmal | Novel bicyclic heteroaryl derivatives as sos1:kras proteinprotein interaction inhibitors |
| US12138243B2 (en) | 2021-12-31 | 2024-11-12 | Crescenta Biosciences | Antiviral use of FABP4 modulating compounds |
| CN114605409B (zh) * | 2022-04-01 | 2024-04-02 | 苏州睿尔思科技有限公司 | 一种4-羟基-1,5-萘啶类配体的生产制备方法 |
| CN114751858B (zh) * | 2022-04-20 | 2023-09-12 | 沈阳药科大学 | 含有喹啉基的氨甲环酸衍生物及其制备与应用 |
| CN117024404A (zh) * | 2022-05-10 | 2023-11-10 | 四川汇宇制药股份有限公司 | 苯并吡啶衍生物及其用途 |
| US20250084063A1 (en) * | 2023-08-18 | 2025-03-13 | Incyte Corporation | Bicyclic heterocycles as mrgprx2 antagonists |
| TW202542130A (zh) * | 2024-01-05 | 2025-11-01 | 美商露點治療股份有限公司 | 胺基喹啉化合物及其用途 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US856095A (en) * | 1906-09-01 | 1907-06-04 | Railway Safety Signal Company | Electric semaphore. |
| PH25124A (en) | 1987-03-17 | 1991-02-19 | Hoechst Roussel Pharma | Substituted 9-amino-tetrahydro acridines and related compounds |
| DE3917232A1 (de) * | 1989-05-26 | 1990-11-29 | Basf Ag | 4-arylmethamino-2,3-dialkyl-chinoline, ihre verwendung und daraus hergestellte arzneimittel |
| KR100745307B1 (ko) | 2001-05-31 | 2007-08-01 | 사노피-아벤티스 | 아미노퀴놀린 유도체 및 아데노신 ａ３ 리간드로서의 이의 용도 |
| AU2002341715A1 (en) * | 2001-09-17 | 2003-04-01 | Bristol-Myers Squibb Company | Cyclic hydroxamic acids as inhibitors of matrix metalloproteinases and/or tnf-alpha converting enzyme (tace) |
| AU2002357312A1 (en) * | 2001-12-20 | 2003-07-09 | Bristol-Myers Squibb Company | Barbituric acid derivatives as inhibitors of tnf-alpha converting enzyme (tace) and/or matrix metalloproteinases |
| HUP0105406A3 (en) | 2001-12-21 | 2003-12-29 | Sanofi Aventis | Imidazo[1,2-a]quinolin derivatives, process for their preparation, pharmaceutical compositions thereof and intermediates |
| EP1663982B1 (en) | 2003-07-31 | 2007-11-21 | Sanofi-Aventis | Aminoquinoline derivatives and their use as adenosine a3 ligands |
| TW200815447A (en) | 2006-06-14 | 2008-04-01 | Astrazeneca Ab | Novel compounds IV |
| JP5599783B2 (ja) * | 2008-05-30 | 2014-10-01 | アムジエン・インコーポレーテツド | Ｐｉ３キナーゼの阻害薬 |
| ES2565627T3 (es) * | 2010-07-30 | 2016-04-06 | Oncotherapy Science, Inc. | Derivados de quinolina e inhibidores de MELK que contienen los mismos |
| US9550737B2 (en) | 2012-06-11 | 2017-01-24 | Ucb Biopharma Sprl | TNF -α modulating benzimidazoles |
| GB201212513D0 (en) | 2012-07-13 | 2012-08-29 | Ucb Pharma Sa | Therapeutic agents |
| CN104619709B (zh) * | 2012-07-13 | 2016-11-09 | Ucb生物制药私人有限公司 | 作为tnf活性调节剂的咪唑并吡啶衍生物 |
| EP2914296B2 (en) | 2012-11-01 | 2021-09-29 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| JP6464139B2 (ja) | 2013-03-14 | 2019-02-06 | コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ | ブロモドメイン含有タンパク質の阻害のための方法および組成物 |
| AR105556A1 (es) | 2015-08-03 | 2017-10-18 | Hoffmann La Roche | Derivados de etinilo |
| CN108026050B (zh) | 2015-08-03 | 2021-04-30 | 格兰马克药品股份有限公司 | 作为RORγ调节剂的新型化合物 |
| GB201513742D0 (en) | 2015-08-03 | 2015-09-16 | Heptares Therapeutics Ltd | Muscarinic agonists |
| EA201892153A1 (ru) | 2016-04-01 | 2019-04-30 | Юсб Байофарма Спрл | Конденсированные пентациклические производные имидазола в качестве модуляторов активности tnf |
-
2016
- 2016-08-02 PE PE2018000172A patent/PE20181366A1/es unknown
- 2016-08-02 MX MX2018001054A patent/MX375341B/es active IP Right Grant
- 2016-08-02 BR BR112018001960A patent/BR112018001960A2/pt not_active IP Right Cessation
- 2016-08-02 EA EA201890165A patent/EA033686B1/ru not_active IP Right Cessation
- 2016-08-02 HK HK18111924.8A patent/HK1252623A1/zh unknown
- 2016-08-02 CA CA2994717A patent/CA2994717A1/en not_active Abandoned
- 2016-08-02 AR ARP160102357A patent/AR105575A1/es unknown
- 2016-08-02 TW TW105124501A patent/TW201718536A/zh unknown
- 2016-08-02 WO PCT/US2016/045110 patent/WO2017023905A1/en not_active Ceased
- 2016-08-02 EP EP16750343.2A patent/EP3331871A1/en not_active Withdrawn
- 2016-08-02 SG SG10201911831RA patent/SG10201911831RA/en unknown
- 2016-08-02 CN CN201680057509.7A patent/CN108137547B/zh active Active
- 2016-08-02 UY UY0001036838A patent/UY36838A/es unknown
- 2016-08-02 AU AU2016302144A patent/AU2016302144B2/en not_active Ceased
- 2016-08-02 MA MA043512A patent/MA43512A/fr unknown
- 2016-08-02 JP JP2018506144A patent/JP6955482B2/ja active Active
- 2016-08-02 KR KR1020187005707A patent/KR102697810B1/ko active Active
- 2016-08-02 US US15/887,214 patent/US10865191B2/en active Active
-
2018
- 2018-01-25 IL IL257154A patent/IL257154A/en unknown
- 2018-02-01 CL CL2018000293A patent/CL2018000293A1/es unknown
- 2018-02-02 ZA ZA2018/00716A patent/ZA201800716B/en unknown
- 2018-02-26 CO CONC2018/0002061A patent/CO2018002061A2/es unknown
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