JP2015510515A5 - - Google Patents
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- Publication number
- JP2015510515A5 JP2015510515A5 JP2014557739A JP2014557739A JP2015510515A5 JP 2015510515 A5 JP2015510515 A5 JP 2015510515A5 JP 2014557739 A JP2014557739 A JP 2014557739A JP 2014557739 A JP2014557739 A JP 2014557739A JP 2015510515 A5 JP2015510515 A5 JP 2015510515A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- group
- substituted
- cycloalkyl
- coor
- 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 28
- 150000001875 compounds Chemical class 0.000 claims 24
- 125000001072 heteroaryl group Chemical group 0.000 claims 15
- 125000000547 substituted alkyl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 8
- 230000000840 anti-viral effect Effects 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 239000003085 diluting agent Substances 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 125000000555 isopropenyl group Chemical group [H]\C([H])=C(\*)C([H])([H])[H] 0.000 claims 2
- 125000003107 substituted aryl group Chemical group 0.000 claims 2
- 125000006564 (C4-C8) cycloalkyl group Chemical group 0.000 claims 1
- 229940126154 HIV entry inhibitor Drugs 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 229960005475 antiinfective agent Drugs 0.000 claims 1
- 239000004599 antimicrobial Substances 0.000 claims 1
- 239000003443 antiviral agent Substances 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001475 halogen functional group Chemical group 0.000 claims 1
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 230000002584 immunomodulator Effects 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- -1 —COOR 3 Chemical group 0.000 claims 1
- 0 C*1CI*(C)CC1 Chemical compound C*1CI*(C)CC1 0.000 description 5
- FFWAQFXCJUHCDZ-UHFFFAOYSA-N C(C1)C11COCC1 Chemical compound C(C1)C11COCC1 FFWAQFXCJUHCDZ-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261599040P | 2012-02-15 | 2012-02-15 | |
| US61/599,040 | 2012-02-15 | ||
| US13/760,726 US8906889B2 (en) | 2012-02-15 | 2013-02-06 | C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity |
| US13/760,726 | 2013-02-06 | ||
| PCT/US2013/025897 WO2013123019A1 (en) | 2012-02-15 | 2013-02-13 | C-3 cycloalkenyl triterpenoids with hiv maturation inhibitory activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015510515A JP2015510515A (ja) | 2015-04-09 |
| JP2015510515A5 true JP2015510515A5 (enExample) | 2016-03-17 |
| JP6155285B2 JP6155285B2 (ja) | 2017-06-28 |
Family
ID=48946098
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014557739A Active JP6155285B2 (ja) | 2012-02-15 | 2013-02-13 | Ｈｉｖ成熟阻害活性のあるｃ−３シクロアルケニルトリテルペノイド |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US8906889B2 (enExample) |
| EP (1) | EP2814834B1 (enExample) |
| JP (1) | JP6155285B2 (enExample) |
| KR (1) | KR20140123584A (enExample) |
| CN (2) | CN106046106A (enExample) |
| AR (1) | AR089996A1 (enExample) |
| AU (1) | AU2013221725B2 (enExample) |
| BR (1) | BR112014019672A8 (enExample) |
| CA (1) | CA2864656A1 (enExample) |
| CL (1) | CL2014002141A1 (enExample) |
| CO (1) | CO7061077A2 (enExample) |
| EA (1) | EA024361B1 (enExample) |
| ES (1) | ES2656984T3 (enExample) |
| HK (1) | HK1204608A1 (enExample) |
| IL (1) | IL234077A (enExample) |
| MX (1) | MX2014009235A (enExample) |
| MY (1) | MY166793A (enExample) |
| NZ (1) | NZ631408A (enExample) |
| PE (1) | PE20142315A1 (enExample) |
| PH (1) | PH12014501816A1 (enExample) |
| PT (1) | PT2814834T (enExample) |
| SG (1) | SG11201404748XA (enExample) |
| TW (1) | TW201336863A (enExample) |
| UY (1) | UY34627A (enExample) |
| WO (1) | WO2013123019A1 (enExample) |
| ZA (1) | ZA201406724B (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8889854B2 (en) | 2012-05-07 | 2014-11-18 | Bristol-Myers Squibb Company | C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity |
| JP6186010B2 (ja) | 2013-02-06 | 2017-08-23 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｈｉｖ成熟阻害活性を有するｃ−１９修飾トリテルペノイド類 |
| MA39374A1 (fr) | 2014-04-11 | 2018-06-29 | Viiv Healthcare Uk No 4 Ltd | Triterpénoïdes présentant une activité d'inhibition de la maturation du vih, substitués en 3ème position par un cycle non aromatique portant un substituant halogénoalkyle |
| WO2015195776A1 (en) | 2014-06-19 | 2015-12-23 | Bristol-Myers Squibb Company | Betulinic acid derivatives with hiv maturation inhibitory activity |
| RU2017118576A (ru) | 2014-11-14 | 2018-12-14 | ВАЙВ ХЕЛТКЕР ЮКей (N5) ЛИМИТЕД | C-17-арил-замещённые аналоги бетулиновой кислоты |
| WO2016077572A1 (en) * | 2014-11-14 | 2016-05-19 | Bristol-Myers Squibb Company | Extended betulinic acid analogs |
| BR112017009850A2 (pt) * | 2014-11-14 | 2018-01-16 | Viiv Healthcare Uk No 5 Ltd | composto, composição, e, uso de uma quantidade melhoradora de hiv de um composto |
| KR20170135970A (ko) * | 2015-04-14 | 2017-12-08 | 비브 헬스케어 유케이 (넘버4) 리미티드 | Hiv 성숙화 억제제를 생산하는 방법 |
| KR20180028534A (ko) | 2015-07-28 | 2018-03-16 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | Hiv 감염을 예방하거나 치료하기 위한 베투인 유도체 |
| RU2018105352A (ru) | 2015-07-28 | 2019-08-29 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Производные бетулина для предупреждения или лечения ВИЧ-инфекций |
| CN108368071A (zh) | 2015-09-24 | 2018-08-03 | 葛兰素史克知识产权第二有限公司 | 具有hiv成熟抑制活性的化合物 |
| CN108699103A (zh) * | 2016-01-20 | 2018-10-23 | 葛兰素史克知识产权第二有限公司 | 具有hiv成熟抑制活性的羽扇烷类的胺衍生物 |
| AR107512A1 (es) * | 2016-02-04 | 2018-05-09 | VIIV HEALTHCARE UK Nº 5 LTD | Triterpenoides modificados en c-3 y c-17 como inhibidores del vih-1 |
| CN106905264B (zh) * | 2017-04-12 | 2019-06-07 | 连云港杰瑞药业有限公司 | 一种合成阿扎拉韦中间体的方法 |
| JP7670482B2 (ja) * | 2017-09-13 | 2025-04-30 | エミオン インコーポレイテッド | ウルソール酸モルホリン塩及びジエタノールアミン塩 |
| WO2019207460A1 (en) | 2018-04-24 | 2019-10-31 | VIIV Healthcare UK (No.5) Limited | Compounds with hiv maturation inhibitory activity |
| CN109705189B (zh) * | 2018-12-29 | 2020-06-05 | 中国医学科学院药用植物研究所 | 具有式i所示结构的三萜衍生物及其制备方法和应用 |
| MX2021009584A (es) | 2019-02-11 | 2021-09-23 | Hetero Labs Ltd | Nuevos derivados de triterpeno como inhibidores del virus de la inmunodeficiencia humana (vih). |
| WO2020229398A1 (de) | 2019-05-14 | 2020-11-19 | Bayer Aktiengesellschaft | (1-alkenyl)-substituierte pyrazole und triazole als schädlingsbekämpfungsmittel |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5413999A (en) | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| US5962527A (en) | 1995-03-21 | 1999-10-05 | The Board Of Trustees Of The University Of Illinois | Method and composition for treating cancers |
| US5869535A (en) | 1995-03-21 | 1999-02-09 | The Board Of Trustees Of The University Of Illinois | Method and composition for selectively inhibiting melanoma |
| US5679828A (en) | 1995-06-05 | 1997-10-21 | Biotech Research Labs, Inc. | Betulinic acid and dihydrobetulinic acid derivatives and uses therefor |
| US20040110785A1 (en) | 2001-02-02 | 2004-06-10 | Tao Wang | Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives |
| US7365221B2 (en) | 2002-09-26 | 2008-04-29 | Panacos Pharmaceuticals, Inc. | Monoacylated betulin and dihydrobetulin derivatives, preparation thereof and use thereof |
| WO2004089357A2 (en) | 2003-04-02 | 2004-10-21 | Regents Of The University Of Minnesota | Anti-fungal formulation of triterpene and essential oil |
| US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| JP2007529544A (ja) | 2004-03-17 | 2007-10-25 | パナコス ファーマシューティカルズ， インコーポレイテッド | ３−ｏ−（３’，３’−ジメチルスクシニル）ベツリン酸の製薬的な塩 |
| TW200628161A (en) | 2004-11-12 | 2006-08-16 | Panacos Pharmaceuticals Inc | Novel betulin derivatives, preparation thereof and use thereof |
| WO2008127364A2 (en) | 2006-10-13 | 2008-10-23 | Myriad Genetics, Inc. | Antiviral compounds and use thereof |
| US20110144069A1 (en) | 2006-10-16 | 2011-06-16 | Myriad Genetics, Incorporated | Compounds for treating viral infections |
| US20090062243A1 (en) | 2007-08-03 | 2009-03-05 | Advanced Life Sciences, Inc. | Lupane-Type Triterpenoids Modified at 30-Position and Analogues Thereof |
| MX2010007375A (es) * | 2008-01-03 | 2010-09-30 | Virochem Pharma Inc | Nuevos derivados de lupano. |
| CA2714049A1 (en) | 2008-02-14 | 2009-08-20 | Virochem Pharma Inc. | Novel 17.beta. lupane derivatives |
| US9067966B2 (en) | 2009-07-14 | 2015-06-30 | Hetero Research Foundation, Hetero Drugs Ltd. | Lupeol-type triterpene derivatives as antivirals |
| MX2012007154A (es) | 2009-12-17 | 2012-08-01 | Merck Sharp & Dohme | Aminopirimidinas como inhibidores de syk. |
| ES2612452T3 (es) * | 2010-06-04 | 2017-05-17 | VIIV Healthcare UK (No.5) Limited | Derivados de ácido betulínico C-3 modificados como inhibidores de la maduración del VIH |
| EP2576586B1 (en) * | 2010-06-04 | 2015-08-12 | Bristol-Myers Squibb Company | C-28 amides of modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
| US9102614B2 (en) | 2010-07-02 | 2015-08-11 | Gilead Sciences, Inc. | Naphth-2-ylacetic acid derivatives to treat AIDS |
| ES2653847T3 (es) * | 2011-01-31 | 2018-02-09 | Viiv Healthcare Uk (No. 4) Limited | Triterpenoides C-17 y C-3 modificados con actividad inhibitoria contra maduración del VIH |
| CN103339141B (zh) | 2011-01-31 | 2016-08-24 | 百时美施贵宝公司 | 作为hiv成熟抑制剂的c-3修饰的桦木酸衍生物的c-28胺 |
| ES2611727T3 (es) | 2011-09-21 | 2017-05-10 | VIIV Healthcare UK (No.5) Limited | Derivados de ácido betulínico novedosos con actividad antivírica |
| US8889854B2 (en) | 2012-05-07 | 2014-11-18 | Bristol-Myers Squibb Company | C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity |
| JP6186010B2 (ja) * | 2013-02-06 | 2017-08-23 | ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ | Ｈｉｖ成熟阻害活性を有するｃ−１９修飾トリテルペノイド類 |
-
2013
- 2013-02-06 US US13/760,726 patent/US8906889B2/en active Active
- 2013-02-08 TW TW102105203A patent/TW201336863A/zh unknown
- 2013-02-13 CN CN201610397768.6A patent/CN106046106A/zh active Pending
- 2013-02-13 KR KR1020147025339A patent/KR20140123584A/ko not_active Ceased
- 2013-02-13 CN CN201380019696.6A patent/CN104220451B/zh not_active Expired - Fee Related
- 2013-02-13 EA EA201491531A patent/EA024361B1/ru not_active IP Right Cessation
- 2013-02-13 PT PT137074936T patent/PT2814834T/pt unknown
- 2013-02-13 BR BR112014019672A patent/BR112014019672A8/pt not_active Application Discontinuation
- 2013-02-13 WO PCT/US2013/025897 patent/WO2013123019A1/en not_active Ceased
- 2013-02-13 ES ES13707493.6T patent/ES2656984T3/es active Active
- 2013-02-13 EP EP13707493.6A patent/EP2814834B1/en active Active
- 2013-02-13 CA CA2864656A patent/CA2864656A1/en not_active Abandoned
- 2013-02-13 SG SG11201404748XA patent/SG11201404748XA/en unknown
- 2013-02-13 NZ NZ631408A patent/NZ631408A/en not_active IP Right Cessation
- 2013-02-13 JP JP2014557739A patent/JP6155285B2/ja active Active
- 2013-02-13 PE PE2014001279A patent/PE20142315A1/es not_active Application Discontinuation
- 2013-02-13 MX MX2014009235A patent/MX2014009235A/es unknown
- 2013-02-13 MY MYPI2014702277A patent/MY166793A/en unknown
- 2013-02-13 HK HK15105069.8A patent/HK1204608A1/xx unknown
- 2013-02-13 AU AU2013221725A patent/AU2013221725B2/en not_active Ceased
- 2013-02-14 UY UY0001034627A patent/UY34627A/es not_active Application Discontinuation
- 2013-02-14 AR ARP130100466A patent/AR089996A1/es unknown
-
2014
- 2014-08-12 IL IL234077A patent/IL234077A/en not_active IP Right Cessation
- 2014-08-12 PH PH12014501816A patent/PH12014501816A1/en unknown
- 2014-08-13 CL CL2014002141A patent/CL2014002141A1/es unknown
- 2014-08-28 CO CO14189685A patent/CO7061077A2/es unknown
- 2014-09-12 ZA ZA2014/06724A patent/ZA201406724B/en unknown