JP2018526399A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2018526399A5 JP2018526399A5 JP2018512339A JP2018512339A JP2018526399A5 JP 2018526399 A5 JP2018526399 A5 JP 2018526399A5 JP 2018512339 A JP2018512339 A JP 2018512339A JP 2018512339 A JP2018512339 A JP 2018512339A JP 2018526399 A5 JP2018526399 A5 JP 2018526399A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- aryl
- nhc
- heteroaryl
- nhs
- 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
Links
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 95
- 125000003118 aryl group Chemical group 0.000 claims 57
- 125000001072 heteroaryl group Chemical group 0.000 claims 41
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 40
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 16
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 14
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims 13
- 125000000217 alkyl group Chemical group 0.000 claims 11
- -1 -NC Chemical group 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 9
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 6
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 4
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000005358 mercaptoalkyl group Chemical group 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 3
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 125000002947 alkylene group Chemical group 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 3
- 125000001424 substituent group Chemical group 0.000 claims 3
- 230000002159 abnormal effect Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 102100037839 Acidic mammalian chitinase Human genes 0.000 claims 1
- 101710178876 Acidic mammalian chitinase Proteins 0.000 claims 1
- 208000030090 Acute Disease Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 102100037328 Chitotriosidase-1 Human genes 0.000 claims 1
- 208000018035 Dental disease Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000014151 Stomatognathic disease Diseases 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 125000000732 arylene group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
- 108010057052 chitotriosidase Proteins 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 208000037893 chronic inflammatory disorder Diseases 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000004430 oxygen atom Chemical group O* 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 claims 1
- 208000017520 skin disease Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021050972A JP2021100966A (ja) | 2015-09-04 | 2021-03-25 | ヒトキチナーゼ阻害剤として有用な置換アミノトリアゾール |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562214299P | 2015-09-04 | 2015-09-04 | |
| US62/214,299 | 2015-09-04 | ||
| PLP.415078 | 2015-12-04 | ||
| PL415078A PL415078A1 (pl) | 2015-09-04 | 2015-12-04 | Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków |
| PCT/IB2016/055269 WO2017037670A1 (en) | 2015-09-04 | 2016-09-02 | Substituted amino triazoles useful as human chitinase inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021050972A Division JP2021100966A (ja) | 2015-09-04 | 2021-03-25 | ヒトキチナーゼ阻害剤として有用な置換アミノトリアゾール |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018526399A JP2018526399A (ja) | 2018-09-13 |
| JP2018526399A5 true JP2018526399A5 (https=) | 2019-10-10 |
| JP6859325B2 JP6859325B2 (ja) | 2021-04-14 |
Family
ID=58190067
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018512339A Active JP6859325B2 (ja) | 2015-09-04 | 2016-09-02 | ヒトキチナーゼ阻害剤として有用な置換アミノトリアゾール |
| JP2021050972A Pending JP2021100966A (ja) | 2015-09-04 | 2021-03-25 | ヒトキチナーゼ阻害剤として有用な置換アミノトリアゾール |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021050972A Pending JP2021100966A (ja) | 2015-09-04 | 2021-03-25 | ヒトキチナーゼ阻害剤として有用な置換アミノトリアゾール |
Country Status (29)
| Country | Link |
|---|---|
| US (3) | US9944624B2 (https=) |
| EP (1) | EP3344616B1 (https=) |
| JP (2) | JP6859325B2 (https=) |
| KR (1) | KR102699408B1 (https=) |
| CN (1) | CN108290863B (https=) |
| AU (1) | AU2016314345B2 (https=) |
| CA (1) | CA2997382C (https=) |
| CL (1) | CL2018000564A1 (https=) |
| CO (1) | CO2018003484A2 (https=) |
| CY (1) | CY1121432T1 (https=) |
| DK (1) | DK3344616T3 (https=) |
| ES (1) | ES2717181T3 (https=) |
| HK (1) | HK1249510B (https=) |
| HR (1) | HRP20190223T1 (https=) |
| HU (1) | HUE042726T2 (https=) |
| IL (1) | IL257545B (https=) |
| LT (1) | LT3344616T (https=) |
| ME (1) | ME03308B (https=) |
| MX (1) | MX368674B (https=) |
| PE (1) | PE20181048A1 (https=) |
| PH (1) | PH12018500286A1 (https=) |
| PL (2) | PL415078A1 (https=) |
| PT (1) | PT3344616T (https=) |
| SA (1) | SA518391033B1 (https=) |
| SI (1) | SI3344616T1 (https=) |
| SM (1) | SMT201900172T1 (https=) |
| TR (1) | TR201903826T4 (https=) |
| WO (1) | WO2017037670A1 (https=) |
| ZA (1) | ZA201801978B (https=) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104364239B (zh) | 2012-06-13 | 2017-08-25 | 霍夫曼-拉罗奇有限公司 | 二氮杂螺环烷烃和氮杂螺环烷烃 |
| MX368615B (es) | 2012-09-25 | 2019-10-09 | Hoffmann La Roche | Derivados bicíclicos como inhibidores de la autotaxina (atx) que son inhibidores de la producción de ácido lisofosfatídico (lpa) y el uso de los mismos. |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| DK3074400T3 (en) | 2013-11-26 | 2018-01-15 | Hoffmann La Roche | Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors |
| EA032357B1 (ru) | 2014-03-26 | 2019-05-31 | Ф. Хоффманн-Ля Рош Аг | Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| CA2937616A1 (en) | 2014-03-26 | 2015-10-01 | F. Hoffmann-La Roche Ag | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| PL415078A1 (pl) | 2015-09-04 | 2017-03-13 | Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością | Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków |
| CA2992889A1 (en) | 2015-09-04 | 2017-03-09 | F. Hoffmann-La Roche Ag | Phenoxymethyl derivatives |
| AU2016328436B2 (en) | 2015-09-24 | 2020-05-14 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| WO2017050732A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | Bicyclic compounds as atx inhibitors |
| JP6876685B2 (ja) | 2015-09-24 | 2021-05-26 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ａｔｘ阻害剤としての二環式化合物 |
| BR112017026682A2 (pt) | 2015-09-24 | 2018-08-14 | Hoffmann La Roche | novos compostos bicíclicos como inibidores de dupla ação de atx/ca |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ．ホフマン－ラ ロシュ アーゲー | Ａｔｘインヒビターとしての新規二環式化合物 |
| CN109503449A (zh) * | 2018-12-17 | 2019-03-22 | 天津药明康德新药开发有限公司 | 一种3-硝基吖丁啶-1-甲酸叔丁酯的合成方法 |
| MX2022000306A (es) | 2019-07-15 | 2022-03-11 | Oncoarendi Therapeutics Sa | Amino triazoles sustituidos utiles como inhibidores de quitinasa. |
| MX2022002881A (es) * | 2019-09-25 | 2022-06-08 | Oncoarendi Therapeutics Sa | Proceso para la produccion de 5-(4-((2s,5s)-5-(4-clorobencil)-2-me tilmorfolino)piperidin-1-il)-1h-1,2,4-triazol-3-amina. |
| EP3854789A1 (en) | 2020-01-22 | 2021-07-28 | Cygnet Biosciences B.V. | Macrocyclic compounds useful as chitinase inhibitors |
| CN114057714B (zh) * | 2021-11-22 | 2023-07-14 | 苏州健雄职业技术学院 | 杂环基取代的氨基三唑的衍生物及其应用 |
| US12325701B2 (en) * | 2022-03-04 | 2025-06-10 | Molecure S.A. | YKL-40 inhibitors and their therapeutic |
| CN116924985B (zh) * | 2022-03-29 | 2026-03-17 | 山东新时代药业有限公司 | 一种法舒地尔的制备方法 |
| EP4269400B1 (en) * | 2022-04-29 | 2025-07-09 | Molecure SA | Ykl-40 inhibitors and their therapeutic applications |
| CN114957098B (zh) * | 2022-06-02 | 2024-03-29 | 和鼎（南京）医药技术有限公司 | 一种制备喷他佐辛中间体的方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP3507486B2 (ja) | 1991-03-15 | 2004-03-15 | アムジエン・インコーポレーテツド | 顆粒球コロニー刺激因子の肺内投与 |
| US5451569A (en) | 1994-04-19 | 1995-09-19 | Hong Kong University Of Science And Technology R & D Corporation Limited | Pulmonary drug delivery system |
| EP3082805B1 (en) * | 2013-12-20 | 2020-02-05 | Institute for Drug Discovery, LLC | Substituted amino triazoles, and methods using same |
| US9440953B2 (en) * | 2014-12-19 | 2016-09-13 | OncoArendi Therapeutics Sp. z o.o. | Substituted amino triazoles useful as acidic mammalian chitinase inhibitors |
| PL415078A1 (pl) | 2015-09-04 | 2017-03-13 | Oncoarendi Therapeutics Spółka Z Ograniczoną Odpowiedzialnością | Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków |
-
2015
- 2015-12-04 PL PL415078A patent/PL415078A1/pl unknown
-
2016
- 2016-09-02 DK DK16767368.0T patent/DK3344616T3/en active
- 2016-09-02 US US15/255,226 patent/US9944624B2/en active Active
- 2016-09-02 HU HUE16767368A patent/HUE042726T2/hu unknown
- 2016-09-02 KR KR1020187009490A patent/KR102699408B1/ko active Active
- 2016-09-02 CN CN201680062288.2A patent/CN108290863B/zh active Active
- 2016-09-02 WO PCT/IB2016/055269 patent/WO2017037670A1/en not_active Ceased
- 2016-09-02 ME MEP-2019-33A patent/ME03308B/me unknown
- 2016-09-02 PL PL16767368T patent/PL3344616T3/pl unknown
- 2016-09-02 SI SI201630168T patent/SI3344616T1/sl unknown
- 2016-09-02 SM SM20190172T patent/SMT201900172T1/it unknown
- 2016-09-02 EP EP16767368.0A patent/EP3344616B1/en active Active
- 2016-09-02 HK HK18109046.5A patent/HK1249510B/en unknown
- 2016-09-02 CA CA2997382A patent/CA2997382C/en active Active
- 2016-09-02 HR HRP20190223TT patent/HRP20190223T1/hr unknown
- 2016-09-02 AU AU2016314345A patent/AU2016314345B2/en active Active
- 2016-09-02 PT PT16767368T patent/PT3344616T/pt unknown
- 2016-09-02 JP JP2018512339A patent/JP6859325B2/ja active Active
- 2016-09-02 LT LTEP16767368.0T patent/LT3344616T/lt unknown
- 2016-09-02 TR TR2019/03826T patent/TR201903826T4/tr unknown
- 2016-09-02 MX MX2018002659A patent/MX368674B/es active IP Right Grant
- 2016-09-02 ES ES16767368T patent/ES2717181T3/es active Active
- 2016-09-02 PE PE2018000314A patent/PE20181048A1/es unknown
-
2018
- 2018-02-08 PH PH12018500286A patent/PH12018500286A1/en unknown
- 2018-02-15 IL IL257545A patent/IL257545B/en active IP Right Grant
- 2018-02-28 US US15/908,249 patent/US10208020B2/en active Active
- 2018-02-28 SA SA518391033A patent/SA518391033B1/ar unknown
- 2018-03-01 CL CL2018000564A patent/CL2018000564A1/es unknown
- 2018-03-26 ZA ZA2018/01978A patent/ZA201801978B/en unknown
- 2018-03-29 CO CONC2018/0003484A patent/CO2018003484A2/es unknown
-
2019
- 2019-02-15 US US16/277,321 patent/US10538508B2/en active Active
- 2019-03-15 CY CY20191100310T patent/CY1121432T1/el unknown
-
2021
- 2021-03-25 JP JP2021050972A patent/JP2021100966A/ja active Pending