JP2019500387A5 - - Google Patents
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- Publication number
- JP2019500387A5 JP2019500387A5 JP2018534101A JP2018534101A JP2019500387A5 JP 2019500387 A5 JP2019500387 A5 JP 2019500387A5 JP 2018534101 A JP2018534101 A JP 2018534101A JP 2018534101 A JP2018534101 A JP 2018534101A JP 2019500387 A5 JP2019500387 A5 JP 2019500387A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound according
- pharmaceutically acceptable
- compound
- acceptable salt
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 17
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 239000000651 prodrug Substances 0.000 claims 6
- 229940002612 prodrug Drugs 0.000 claims 6
- -1 2 - cyclopropyl Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 208000030507 AIDS Diseases 0.000 claims 3
- 208000015181 infectious disease Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- 125000006727 (C1-C6) alkenyl group Chemical group 0.000 claims 2
- 108010002459 HIV Integrase Proteins 0.000 claims 2
- KJHKTHWMRKYKJE-SUGCFTRWSA-N Kaletra Chemical compound N1([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=2C=CC=CC=2)NC(=O)COC=2C(=CC=CC=2C)C)CC=2C=CC=CC=2)CCCNC1=O KJHKTHWMRKYKJE-SUGCFTRWSA-N 0.000 claims 2
- NCDNCNXCDXHOMX-UHFFFAOYSA-N Ritonavir Natural products C=1C=CC=CC=1CC(NC(=O)OCC=1SC=NC=1)C(O)CC(CC=1C=CC=CC=1)NC(=O)C(C(C)C)NC(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-UHFFFAOYSA-N 0.000 claims 2
- 229960004748 abacavir Drugs 0.000 claims 2
- MCGSCOLBFJQGHM-SCZZXKLOSA-N abacavir Chemical compound C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 MCGSCOLBFJQGHM-SCZZXKLOSA-N 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 229960001627 lamivudine Drugs 0.000 claims 2
- JTEGQNOMFQHVDC-NKWVEPMBSA-N lamivudine Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims 2
- 229960004525 lopinavir Drugs 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 229960004742 raltegravir Drugs 0.000 claims 2
- CZFFBEXEKNGXKS-UHFFFAOYSA-N raltegravir Chemical compound O1C(C)=NN=C1C(=O)NC(C)(C)C1=NC(C(=O)NCC=2C=CC(F)=CC=2)=C(O)C(=O)N1C CZFFBEXEKNGXKS-UHFFFAOYSA-N 0.000 claims 2
- 229960000311 ritonavir Drugs 0.000 claims 2
- NCDNCNXCDXHOMX-XGKFQTDJSA-N ritonavir Chemical compound N([C@@H](C(C)C)C(=O)N[C@H](C[C@H](O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1SC=NC=1)CC=1C=CC=CC=1)C(=O)N(C)CC1=CSC(C(C)C)=N1 NCDNCNXCDXHOMX-XGKFQTDJSA-N 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- AXRYRYVKAWYZBR-UHFFFAOYSA-N Atazanavir Natural products C=1C=C(C=2N=CC=CC=2)C=CC=1CN(NC(=O)C(NC(=O)OC)C(C)(C)C)CC(O)C(NC(=O)C(NC(=O)OC)C(C)(C)C)CC1=CC=CC=C1 AXRYRYVKAWYZBR-UHFFFAOYSA-N 0.000 claims 1
- 108010019625 Atazanavir Sulfate Proteins 0.000 claims 1
- XQSPYNMVSIKCOC-NTSWFWBYSA-N Emtricitabine Chemical compound C1=C(F)C(N)=NC(=O)N1[C@H]1O[C@@H](CO)SC1 XQSPYNMVSIKCOC-NTSWFWBYSA-N 0.000 claims 1
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims 1
- 229960003277 atazanavir Drugs 0.000 claims 1
- AXRYRYVKAWYZBR-GASGPIRDSA-N atazanavir Chemical compound C([C@H](NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)[C@@H](O)CN(CC=1C=CC(=CC=1)C=1N=CC=CC=1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C1=CC=CC=C1 AXRYRYVKAWYZBR-GASGPIRDSA-N 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 229960002542 dolutegravir Drugs 0.000 claims 1
- RHWKPHLQXYSBKR-BMIGLBTASA-N dolutegravir Chemical compound C([C@@H]1OCC[C@H](N1C(=O)C1=C(O)C2=O)C)N1C=C2C(=O)NCC1=CC=C(F)C=C1F RHWKPHLQXYSBKR-BMIGLBTASA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960000366 emtricitabine Drugs 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- YIBOMRUWOWDFLG-ONEGZZNKSA-N rilpivirine Chemical compound CC1=CC(\C=C\C#N)=CC(C)=C1NC1=CC=NC(NC=2C=CC(=CC=2)C#N)=N1 YIBOMRUWOWDFLG-ONEGZZNKSA-N 0.000 claims 1
- 229960002814 rilpivirine Drugs 0.000 claims 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229960004556 tenofovir Drugs 0.000 claims 1
- VCMJCVGFSROFHV-WZGZYPNHSA-N tenofovir disoproxil fumarate Chemical compound OC(=O)\C=C\C(O)=O.N1=CN=C2N(C[C@@H](C)OCP(=O)(OCOC(=O)OC(C)C)OCOC(=O)OC(C)C)C=NC2=C1N VCMJCVGFSROFHV-WZGZYPNHSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 C*C1C=CC(F)=CC1 Chemical compound C*C1C=CC(F)=CC1 0.000 description 7
- LSLZKIFMRUZGQB-UHFFFAOYSA-N CC(C)c(ccc(F)c1)c1[F][F]c1cc(F)c(C(C)C)c(F)c1 Chemical compound CC(C)c(ccc(F)c1)c1[F][F]c1cc(F)c(C(C)C)c(F)c1 LSLZKIFMRUZGQB-UHFFFAOYSA-N 0.000 description 1
- LHPJOUKIBAEPMW-UHFFFAOYSA-N Cc(cccc1Cl)c1F Chemical compound Cc(cccc1Cl)c1F LHPJOUKIBAEPMW-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/CN2015/100106 WO2017113288A1 (en) | 2015-12-31 | 2015-12-31 | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
| CNPCT/CN2015/100106 | 2015-12-31 | ||
| PCT/US2016/068173 WO2017116928A1 (en) | 2015-12-31 | 2016-12-22 | Fused tricyclic heterocyclic compounds as hiv integrase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019500387A JP2019500387A (ja) | 2019-01-10 |
| JP2019500387A5 true JP2019500387A5 (enExample) | 2020-01-23 |
Family
ID=57799839
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018534101A Pending JP2019500387A (ja) | 2015-12-31 | 2016-12-22 | Ｈｉｖインテグラーゼ阻害剤としての縮合三環式複素環化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (4) | US20170190701A1 (enExample) |
| EP (1) | EP3397639B1 (enExample) |
| JP (1) | JP2019500387A (enExample) |
| KR (1) | KR20180095833A (enExample) |
| CN (1) | CN108473494A (enExample) |
| AR (1) | AR107170A1 (enExample) |
| AU (1) | AU2016381072B2 (enExample) |
| BR (1) | BR112018013251A2 (enExample) |
| CA (1) | CA3008018A1 (enExample) |
| JO (1) | JO3811B1 (enExample) |
| MA (1) | MA43528A (enExample) |
| MX (1) | MX2018008095A (enExample) |
| RU (1) | RU2740187C2 (enExample) |
| TW (1) | TW201726683A (enExample) |
| WO (2) | WO2017113288A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10081647B2 (en) * | 2015-03-26 | 2018-09-25 | Merck Sharp & Dohme Corp. | Phosphate substituted quinolizine derivatives useful as HIV integrase inhibitors |
| JOP20190130A1 (ar) | 2016-12-02 | 2019-06-02 | Merck Sharp & Dohme | مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv) |
| WO2018102634A1 (en) | 2016-12-02 | 2018-06-07 | Merck Sharp & Dohme Corp. | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
| WO2019209667A1 (en) * | 2018-04-27 | 2019-10-31 | Merck Sharp & Dohme Corp. | Tricyclic heterocycle compounds useful as hiv integrase inhibitors |
| EP3805221A4 (en) | 2018-05-31 | 2022-01-05 | Shionogi & Co., Ltd | POLYCYCLIC PYRIDONE DERIVATIVE |
| CR20230571A (es) | 2018-05-31 | 2024-01-22 | Shionogi & Co | DERIVADO POLICÍCLICO DE CARBAMOILPIRIDONA (divisional 2020-0644) |
| US11884683B2 (en) | 2018-06-05 | 2024-01-30 | Merck Sharp & Dohme Llc | Tricyclic heterocycle compounds useful as HIV integrase inhibitors |
| EP4751717A3 (en) * | 2018-10-22 | 2026-08-05 | Board of Regents of the University of Nebraska | Antiviral prodrugs and nanoformulations thereof |
| KR20240151256A (ko) | 2019-03-22 | 2024-10-17 | 길리애드 사이언시즈, 인코포레이티드 | 가교된 트리시클릭 카르바모일피리돈 화합물 및 그의 제약 용도 |
| US20200398978A1 (en) | 2019-06-20 | 2020-12-24 | Bell Helicopter Textron Inc. | Low-drag rotor blade extension |
| US12564595B2 (en) | 2019-11-28 | 2026-03-03 | Shionogi & Co., Ltd. | Prophylactic and therapeutic pharmaceutical agent for HIV infectious diseases characterized by comprising combination of integrase inhibitor and anti-HIV agent |
| WO2021107065A1 (ja) | 2019-11-28 | 2021-06-03 | 塩野義製薬株式会社 | 多環性ピリドピラジン誘導体 |
| EP4110783A1 (en) * | 2020-02-24 | 2023-01-04 | Gilead Sciences, Inc. | Tetracyclic compounds for treating hiv infection |
| CN116390924B (zh) | 2020-09-30 | 2025-11-07 | 吉利德科学公司 | 桥连三环氨基甲酰基吡啶酮化合物及其用途 |
| CR20260070A (es) | 2021-01-19 | 2026-04-24 | Gilead Sciences Inc | COMPUESTOS DE PIRIDOTRIAZINA SUSTITUIDOS Y USOS DE ESTOS (Divisional 2023-0315) |
| US11958864B2 (en) * | 2021-02-16 | 2024-04-16 | Merck Sharp & Dohme Llc | Tetracyclic heterocycle compounds useful as HIV integrase inhibitors |
| TWI856796B (zh) | 2022-04-06 | 2024-09-21 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
Family Cites Families (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE530520T1 (de) | 2001-08-10 | 2011-11-15 | Shionogi & Co | Antivirales mittel |
| DE122009000048I1 (de) | 2001-10-26 | 2010-04-08 | Angeletti P Ist Richerche Bio | N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase |
| CA2463975A1 (en) | 2001-10-26 | 2003-05-01 | Maria Emilia Di Francesco | Dihydroxypyrimidine carboxamide inhibitors of hiv integrase |
| EP1467970B1 (en) | 2002-01-17 | 2007-08-22 | Merck & Co., Inc. | Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors |
| WO2004058756A1 (en) | 2002-12-27 | 2004-07-15 | Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa | Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors |
| WO2004062613A2 (en) | 2003-01-13 | 2004-07-29 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7037908B2 (en) | 2003-04-24 | 2006-05-02 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| TW200510425A (en) | 2003-08-13 | 2005-03-16 | Japan Tobacco Inc | Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor |
| AR046938A1 (es) | 2003-12-12 | 2006-01-04 | Merck & Co Inc | Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares |
| TW200526635A (en) | 2003-12-22 | 2005-08-16 | Shionogi & Co | Hydroxypyrimidinone derivative having HIV integrase inhibitory activity |
| AU2005221864A1 (en) * | 2004-03-09 | 2005-09-22 | Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa | HIV integrase inhibitors |
| US7273859B2 (en) | 2004-05-12 | 2007-09-25 | Bristol-Myers Squibb Company | HIV integrase inhibitors: cyclic pyrimidinone compounds |
| US7115601B2 (en) | 2004-05-18 | 2006-10-03 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US7192948B2 (en) | 2004-05-28 | 2007-03-20 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7176196B2 (en) | 2004-05-28 | 2007-02-13 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7173022B2 (en) | 2004-05-28 | 2007-02-06 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| US7157447B2 (en) | 2004-05-28 | 2007-01-02 | Bristol-Myers Squibb Company | Bicyclic heterocycles as HIV integrase inhibitors |
| WO2006103399A1 (en) | 2005-03-31 | 2006-10-05 | Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa | Hiv integrase inhibitors |
| US7494984B2 (en) | 2005-08-31 | 2009-02-24 | Bristol-Myers Squibb Company | Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors |
| CN101346376A (zh) * | 2005-10-27 | 2009-01-14 | 盐野义制药株式会社 | 具有hiv整合酶抑制活性的多环性氨基甲酰基吡啶酮衍生物 |
| WO2007059125A2 (en) | 2005-11-15 | 2007-05-24 | Bristol-Myers Squibb Company | Hiv integrase inhibitors |
| US7902182B2 (en) | 2005-11-16 | 2011-03-08 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| US8039458B2 (en) | 2005-11-17 | 2011-10-18 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| WO2007143446A1 (en) | 2006-05-30 | 2007-12-13 | Bristol-Myers Squibb Company | Spiro-condensed heterotricyclic compounds as hiv integrase inhibitors |
| US7893055B2 (en) | 2006-06-28 | 2011-02-22 | Bristol-Myers Squibb Company | HIV integrase inhibitors |
| JP4833385B1 (ja) * | 2008-10-07 | 2011-12-07 | アクテリオン ファーマシューティカルズ リミテッド | 三環式オキサゾリジノン抗生物質化合物 |
| WO2011045330A1 (en) | 2009-10-13 | 2011-04-21 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| WO2011121105A1 (en) | 2010-04-02 | 2011-10-06 | Tibotec Pharmaceuticals | Macrocyclic integrase inhibitors |
| US9493479B2 (en) * | 2013-04-16 | 2016-11-15 | Merck Sharp & Dohme Corp. | Substituted pyrido[1,2-a]pyrazines as HIV integrase inhibitors |
| SI2997033T1 (en) * | 2013-05-17 | 2018-04-30 | Merck Sharp & Dohme Corp. | FUZYCLE TRICYCLE HETEROCYCLIC COMPOUNDS AS HIV INTEGRATED INHIBITORS |
-
2015
- 2015-12-31 WO PCT/CN2015/100106 patent/WO2017113288A1/en not_active Ceased
-
2016
- 2016-12-22 JP JP2018534101A patent/JP2019500387A/ja active Pending
- 2016-12-22 RU RU2018127728A patent/RU2740187C2/ru active
- 2016-12-22 AR ARP160103990A patent/AR107170A1/es unknown
- 2016-12-22 CN CN201680073126.9A patent/CN108473494A/zh active Pending
- 2016-12-22 KR KR1020187018217A patent/KR20180095833A/ko not_active Withdrawn
- 2016-12-22 WO PCT/US2016/068173 patent/WO2017116928A1/en not_active Ceased
- 2016-12-22 AU AU2016381072A patent/AU2016381072B2/en not_active Ceased
- 2016-12-22 TW TW105142826A patent/TW201726683A/zh unknown
- 2016-12-22 MX MX2018008095A patent/MX2018008095A/es unknown
- 2016-12-22 CA CA3008018A patent/CA3008018A1/en not_active Abandoned
- 2016-12-22 EP EP16826561.9A patent/EP3397639B1/en active Active
- 2016-12-22 JO JOP/2016/0271A patent/JO3811B1/ar active
- 2016-12-22 BR BR112018013251A patent/BR112018013251A2/pt not_active Application Discontinuation
- 2016-12-22 MA MA043528A patent/MA43528A/fr unknown
- 2016-12-22 US US15/387,732 patent/US20170190701A1/en not_active Abandoned
-
2017
- 2017-12-13 US US15/840,017 patent/US20180099967A1/en not_active Abandoned
-
2019
- 2019-06-27 US US16/454,857 patent/US20190322666A1/en not_active Abandoned
-
2020
- 2020-10-27 US US17/081,094 patent/US20210040096A1/en not_active Abandoned