JP2020521775A5 - - Google Patents
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- Publication number
- JP2020521775A5 JP2020521775A5 JP2019565535A JP2019565535A JP2020521775A5 JP 2020521775 A5 JP2020521775 A5 JP 2020521775A5 JP 2019565535 A JP2019565535 A JP 2019565535A JP 2019565535 A JP2019565535 A JP 2019565535A JP 2020521775 A5 JP2020521775 A5 JP 2020521775A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently selected
- pharmaceutically acceptable
- unsubstituted
- substituted
- 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
- 125000000217 alkyl group Chemical group 0.000 claims description 47
- 150000001875 compounds Chemical class 0.000 claims description 42
- 125000001424 substituent group Chemical group 0.000 claims description 35
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 33
- 150000003839 salts Chemical class 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 28
- 125000006413 ring segment Chemical group 0.000 claims description 28
- 150000002367 halogens Chemical class 0.000 claims description 27
- 125000003545 alkoxy group Chemical group 0.000 claims description 21
- 125000005842 heteroatom Chemical group 0.000 claims description 21
- 229910052760 oxygen Inorganic materials 0.000 claims description 20
- 229910052717 sulfur Inorganic materials 0.000 claims description 20
- 229910052739 hydrogen Inorganic materials 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 18
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 16
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims description 12
- -1 cyano, hydroxyl Chemical group 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 10
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 8
- 150000002431 hydrogen Chemical class 0.000 claims description 8
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 6
- 125000002393 azetidinyl group Chemical group 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 206010001935 American trypanosomiasis Diseases 0.000 claims description 5
- 208000024699 Chagas disease Diseases 0.000 claims description 5
- 241000223109 Trypanosoma cruzi Species 0.000 claims description 5
- 125000003003 spiro group Chemical group 0.000 claims description 5
- 229930183010 Amphotericin Natural products 0.000 claims description 4
- QGGFZZLFKABGNL-UHFFFAOYSA-N Amphotericin A Natural products OC1C(N)C(O)C(C)OC1OC1C=CC=CC=CC=CCCC=CC=CC(C)C(O)C(C)C(C)OC(=O)CC(O)CC(O)CCC(O)C(O)CC(O)CC(O)(CC(O)C2C(O)=O)OC2C1 QGGFZZLFKABGNL-UHFFFAOYSA-N 0.000 claims description 4
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 claims description 4
- 208000004554 Leishmaniasis Diseases 0.000 claims description 4
- ARFHIAQFJWUCFH-IZZDOVSWSA-N Nifurtimox Chemical compound CC1CS(=O)(=O)CCN1\N=C\C1=CC=C([N+]([O-])=O)O1 ARFHIAQFJWUCFH-IZZDOVSWSA-N 0.000 claims description 4
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 4
- 229940009444 amphotericin Drugs 0.000 claims description 4
- APKFDSVGJQXUKY-INPOYWNPSA-N amphotericin B Chemical compound O[C@H]1[C@@H](N)[C@H](O)[C@@H](C)O[C@H]1O[C@H]1/C=C/C=C/C=C/C=C/C=C/C=C/C=C/[C@H](C)[C@@H](O)[C@@H](C)[C@H](C)OC(=O)C[C@H](O)C[C@H](O)CC[C@@H](O)[C@H](O)C[C@H](O)C[C@](O)(C[C@H](O)[C@H]2C(O)=O)O[C@H]2C1 APKFDSVGJQXUKY-INPOYWNPSA-N 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 208000029080 human African trypanosomiasis Diseases 0.000 claims description 4
- 229960002644 nifurtimox Drugs 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims description 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 2
- CULUWZNBISUWAS-UHFFFAOYSA-N Benznidazole Chemical group [O-][N+](=O)C1=NC=CN1CC(=O)NCC1=CC=CC=C1 CULUWZNBISUWAS-UHFFFAOYSA-N 0.000 claims description 2
- 206010011668 Cutaneous leishmaniasis Diseases 0.000 claims description 2
- UOZODPSAJZTQNH-UHFFFAOYSA-N Paromomycin II Natural products NC1C(O)C(O)C(CN)OC1OC1C(O)C(OC2C(C(N)CC(N)C2O)OC2C(C(O)C(O)C(CO)O2)N)OC1CO UOZODPSAJZTQNH-UHFFFAOYSA-N 0.000 claims description 2
- 206010047505 Visceral leishmaniasis Diseases 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 229960004001 benznidazole Drugs 0.000 claims description 2
- 208000035475 disorder Diseases 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- VLCYCQAOQCDTCN-UHFFFAOYSA-N eflornithine Chemical compound NCCCC(N)(C(F)F)C(O)=O VLCYCQAOQCDTCN-UHFFFAOYSA-N 0.000 claims description 2
- 229960002759 eflornithine Drugs 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000001188 haloalkyl group Chemical group 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- XOGYVDXPYVPAAQ-SESJOKTNSA-M meglumine antimoniate Chemical compound O[Sb](=O)=O.CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO XOGYVDXPYVPAAQ-SESJOKTNSA-M 0.000 claims description 2
- 229940005559 meglumine antimoniate Drugs 0.000 claims description 2
- PQLXHQMOHUQAKB-UHFFFAOYSA-N miltefosine Chemical compound CCCCCCCCCCCCCCCCOP([O-])(=O)OCC[N+](C)(C)C PQLXHQMOHUQAKB-UHFFFAOYSA-N 0.000 claims description 2
- 229960003775 miltefosine Drugs 0.000 claims description 2
- UOZODPSAJZTQNH-LSWIJEOBSA-N paromomycin Chemical compound N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)N)O[C@@H]1CO UOZODPSAJZTQNH-LSWIJEOBSA-N 0.000 claims description 2
- 229960001914 paromomycin Drugs 0.000 claims description 2
- XDRYMKDFEDOLFX-UHFFFAOYSA-N pentamidine Chemical group C1=CC(C(=N)N)=CC=C1OCCCCCOC1=CC=C(C(N)=N)C=C1 XDRYMKDFEDOLFX-UHFFFAOYSA-N 0.000 claims description 2
- 229960004448 pentamidine Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- FIAFUQMPZJWCLV-UHFFFAOYSA-N suramin Chemical compound OS(=O)(=O)C1=CC(S(O)(=O)=O)=C2C(NC(=O)C3=CC=C(C(=C3)NC(=O)C=3C=C(NC(=O)NC=4C=C(C=CC=4)C(=O)NC=4C(=CC=C(C=4)C(=O)NC=4C5=C(C=C(C=C5C(=CC=4)S(O)(=O)=O)S(O)(=O)=O)S(O)(=O)=O)C)C=CC=3)C)=CC=C(S(O)(=O)=O)C2=C1 FIAFUQMPZJWCLV-UHFFFAOYSA-N 0.000 claims description 2
- 229960005314 suramin Drugs 0.000 claims description 2
- 229940124597 therapeutic agent Drugs 0.000 claims description 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- PFOYFBYIHCVQGB-XCCFGPONSA-N (4r,5s,6r)-2-[[(4r,5s,6r)-4-carboxy-6-[(1r)-1,2-dihydroxyethyl]-5-hydroxy-2-oxo-1,3,2$l^{5}-dioxastibinan-2-yl]oxy]-6-[(1r)-1,2-dihydroxyethyl]-5-hydroxy-2-oxo-1,3,2$l^{5}-dioxastibinane-4-carboxylic acid Chemical compound O1[C@@H](C(O)=O)[C@@H](O)[C@@H]([C@H](O)CO)O[Sb]1(=O)O[Sb]1(=O)O[C@@H](C(O)=O)[C@@H](O)[C@@H]([C@H](O)CO)O1 PFOYFBYIHCVQGB-XCCFGPONSA-N 0.000 claims 1
- 125000004398 2-methyl-2-butyl group Chemical group CC(C)(CC)* 0.000 claims 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
- VTWFEEHAKPSYJM-UHFFFAOYSA-N BrC1=CC=2C(N=C1)=NN(C=2)C1=NC=CC(=C1)NC(N(C)C)=O Chemical compound BrC1=CC=2C(N=C1)=NN(C=2)C1=NC=CC(=C1)NC(N(C)C)=O VTWFEEHAKPSYJM-UHFFFAOYSA-N 0.000 claims 1
- DVGYRMPAMWBQQG-UHFFFAOYSA-N N-[3-(5-bromopyrazolo[3,4-b]pyridin-2-yl)-4-fluorophenyl]-3-fluoroazetidine-1-carboxamide Chemical compound BrC1=CC2=CN(N=C2N=C1)C1=C(F)C=CC(NC(=O)N2CC(C2)F)=C1 DVGYRMPAMWBQQG-UHFFFAOYSA-N 0.000 claims 1
- LNIYYDWUTGZHJT-UHFFFAOYSA-N N-[3-(5-bromopyrazolo[3,4-b]pyridin-2-yl)-4-fluorophenyl]azetidine-1-carboxamide Chemical compound BrC1=CC=2C(N=C1)=NN(C=2)C=1C=C(C=CC=1F)NC(=O)N1CCC1 LNIYYDWUTGZHJT-UHFFFAOYSA-N 0.000 claims 1
- PVXOUGHWLCBJOW-UHFFFAOYSA-N azetidine-1-carboxamide Chemical compound NC(=O)N1CCC1 PVXOUGHWLCBJOW-UHFFFAOYSA-N 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 238000000034 method Methods 0.000 description 4
- 0 *N(C1)CC1F Chemical compound *N(C1)CC1F 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- JCYZMTMYPZHVBF-UHFFFAOYSA-N Melarsoprol Chemical compound NC1=NC(N)=NC(NC=2C=CC(=CC=2)[As]2SC(CO)CS2)=N1 JCYZMTMYPZHVBF-UHFFFAOYSA-N 0.000 description 1
- 238000004132 cross linking Methods 0.000 description 1
- 125000000000 cycloalkoxy group Chemical group 0.000 description 1
- 229960001728 melarsoprol Drugs 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762513211P | 2017-05-31 | 2017-05-31 | |
| US62/513,211 | 2017-05-31 | ||
| US201762581919P | 2017-11-06 | 2017-11-06 | |
| US62/581,919 | 2017-11-06 | ||
| PCT/IB2018/053818 WO2018220531A1 (en) | 2017-05-31 | 2018-05-29 | 5,6-fused-bicyclic compounds and compositions for the treatment of parasitic diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020521775A JP2020521775A (ja) | 2020-07-27 |
| JP2020521775A5 true JP2020521775A5 (https=) | 2021-07-26 |
| JP7187490B2 JP7187490B2 (ja) | 2022-12-12 |
Family
ID=62749123
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019565535A Active JP7187490B2 (ja) | 2017-05-31 | 2018-05-29 | 寄生虫症の治療のための５，６－縮合二環式化合物及び組成物 |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US11384078B2 (https=) |
| EP (1) | EP3630771B1 (https=) |
| JP (1) | JP7187490B2 (https=) |
| KR (1) | KR20200010275A (https=) |
| CN (1) | CN110678468B (https=) |
| AR (1) | AR111826A1 (https=) |
| AU (1) | AU2018276190B2 (https=) |
| BR (1) | BR112019024804A2 (https=) |
| CA (1) | CA3060990A1 (https=) |
| CL (1) | CL2019003467A1 (https=) |
| CO (1) | CO2019013254A2 (https=) |
| CR (1) | CR20190545A (https=) |
| CU (1) | CU24543B1 (https=) |
| DO (1) | DOP2019000299A (https=) |
| EC (1) | ECSP19084722A (https=) |
| ES (1) | ES2927207T3 (https=) |
| IL (1) | IL270927B (https=) |
| JO (1) | JOP20190278A1 (https=) |
| MA (1) | MA50495A (https=) |
| MX (1) | MX389106B (https=) |
| PE (1) | PE20201148A1 (https=) |
| PH (1) | PH12019502652A1 (https=) |
| RU (1) | RU2738647C1 (https=) |
| TW (1) | TW201902894A (https=) |
| UY (1) | UY37745A (https=) |
| WO (1) | WO2018220531A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JOP20190278A1 (ar) * | 2017-05-31 | 2019-11-28 | Novartis Ag | مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية |
| CN115397807B (zh) * | 2020-04-17 | 2024-08-13 | 帝斯曼知识产权资产管理有限公司 | 用于制备取代的烯胺化合物的方法 |
| EP4155302A4 (en) * | 2020-06-23 | 2023-11-22 | Shanghai Meiyue Biotech Development Co., Ltd. | METHOD FOR PRODUCING A CONDENSED PYRAZOLE COMPOUND |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10053275A1 (de) | 2000-10-27 | 2002-05-02 | Dresden Arzneimittel | Neue 7-Azaindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
| US7468376B2 (en) | 2003-02-27 | 2008-12-23 | Palau Pharma, S.A. | Pyrazolopyridine derivates |
| US20120220453A1 (en) | 2011-02-25 | 2012-08-30 | Dow Agrosciences Llc | Pesticidal compostions and processes related thereto |
| WO2013067302A1 (en) * | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
| WO2013106254A1 (en) * | 2012-01-11 | 2013-07-18 | Dow Agrosciences Llc | Pesticidal compositions and processes related thereto |
| LT2925757T (lt) | 2012-11-19 | 2017-12-27 | Novartis Ag | Junginiai ir kompozicijos, skirti parazitinių ligų gydymui |
| WO2014151729A1 (en) * | 2013-03-15 | 2014-09-25 | Irm Llc | Compounds and compositions for the treatment of parasitic diseases |
| UY35400A (es) * | 2013-03-15 | 2014-10-31 | Novartis Ag | Compuestos y composiciones para el tratamiento de enfermedades parasitarias |
| BR112016014004B1 (pt) * | 2013-12-19 | 2022-11-01 | Novartis Ag | Compostos para tratamento de doenças parasíticas, seus usos, e composições farmacêuticas |
| US20170260183A1 (en) | 2014-12-02 | 2017-09-14 | Bayer Cropscience Aktiengesellschaft | Bicyclic compounds as pest control agents |
| CN112679467B (zh) | 2015-03-11 | 2024-11-01 | Fmc公司 | 杂环取代的二环唑杀有害生物剂 |
| CA2987329A1 (en) | 2015-05-29 | 2016-12-08 | Glaxosmithkline Intellectual Property Development Limited | Imidazo[1,2-b][1,2,4]triazine derivatives as antiparasitic agents |
| RS61434B1 (sr) | 2015-08-07 | 2021-03-31 | Glaxosmithkline Ip Dev Ltd | Jedinjenja |
| PL3458443T3 (pl) * | 2016-05-03 | 2021-03-08 | Bayer Pharma Aktiengesellschaft | Aromatyczne pochodne sulfonamidowe |
| JOP20190278A1 (ar) * | 2017-05-31 | 2019-11-28 | Novartis Ag | مركبات 5، 6-ثنائية الحلقة مندمجة وتركيبات لعلاج الأمراض الطفيلية |
-
2017
- 2017-06-16 JO JOP/2019/0278A patent/JOP20190278A1/ar unknown
-
2018
- 2018-05-23 UY UY0001037745A patent/UY37745A/es not_active Application Discontinuation
- 2018-05-24 AR ARP180101377A patent/AR111826A1/es unknown
- 2018-05-29 CN CN201880034658.0A patent/CN110678468B/zh active Active
- 2018-05-29 ES ES18734297T patent/ES2927207T3/es active Active
- 2018-05-29 KR KR1020197034689A patent/KR20200010275A/ko not_active Withdrawn
- 2018-05-29 RU RU2019138326A patent/RU2738647C1/ru active
- 2018-05-29 PE PE2019002477A patent/PE20201148A1/es unknown
- 2018-05-29 EP EP18734297.7A patent/EP3630771B1/en active Active
- 2018-05-29 US US16/615,749 patent/US11384078B2/en active Active
- 2018-05-29 AU AU2018276190A patent/AU2018276190B2/en not_active Ceased
- 2018-05-29 CR CR20190545A patent/CR20190545A/es unknown
- 2018-05-29 JP JP2019565535A patent/JP7187490B2/ja active Active
- 2018-05-29 MX MX2019014321A patent/MX389106B/es unknown
- 2018-05-29 TW TW107118305A patent/TW201902894A/zh unknown
- 2018-05-29 CU CU2019000095A patent/CU24543B1/es unknown
- 2018-05-29 CA CA3060990A patent/CA3060990A1/en active Pending
- 2018-05-29 BR BR112019024804A patent/BR112019024804A2/pt not_active Application Discontinuation
- 2018-05-29 WO PCT/IB2018/053818 patent/WO2018220531A1/en not_active Ceased
- 2018-05-29 MA MA050495A patent/MA50495A/fr unknown
-
2019
- 2019-11-25 PH PH12019502652A patent/PH12019502652A1/en unknown
- 2019-11-26 IL IL270927A patent/IL270927B/en unknown
- 2019-11-26 CO CONC2019/0013254A patent/CO2019013254A2/es unknown
- 2019-11-27 EC ECSENADI201984722A patent/ECSP19084722A/es unknown
- 2019-11-27 CL CL2019003467A patent/CL2019003467A1/es unknown
- 2019-11-27 DO DO2019000299A patent/DOP2019000299A/es unknown
-
2022
- 2022-05-13 US US17/744,432 patent/US20220324863A1/en not_active Abandoned