CN105121454A - 具有hiv成熟抑制活性的c-19经修饰的三萜类化合物 - Google Patents
具有hiv成熟抑制活性的c-19经修饰的三萜类化合物 Download PDFInfo
- Publication number
- CN105121454A CN105121454A CN201480019576.0A CN201480019576A CN105121454A CN 105121454 A CN105121454 A CN 105121454A CN 201480019576 A CN201480019576 A CN 201480019576A CN 105121454 A CN105121454 A CN 105121454A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- mmol
- pentamethyl
- substituted
- 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.)
- Pending
Links
- 0 CC1CN([*+])CCC1 Chemical compound CC1CN([*+])CCC1 0.000 description 19
- HVDQNXXOOFTKOW-OVWKCCRJSA-N CC(C)(C)OC(c(cc1)ccc1C(C(C)(C)[C@@H]1CC2)=CCC1(C)[C@@H](CC1)[C@]2(C)[C@](C)(CC2)[C@H]1[C@@H]([C@@H](CC1)C(CN(C)CCN(C)C)=C)[C@@]21C(NCCN(C)C)=O)=O Chemical compound CC(C)(C)OC(c(cc1)ccc1C(C(C)(C)[C@@H]1CC2)=CCC1(C)[C@@H](CC1)[C@]2(C)[C@](C)(CC2)[C@H]1[C@@H]([C@@H](CC1)C(CN(C)CCN(C)C)=C)[C@@]21C(NCCN(C)C)=O)=O HVDQNXXOOFTKOW-OVWKCCRJSA-N 0.000 description 1
- LZLNVZUACAOMHN-ZWOKJLCPSA-N CC(C)([C@@H]1CC2)C(c(cc3)ccc3C(O)=O)=CC[C@]1(C)[C@@H](CC1)[C@]2(C)[C@](C)(CC2)[C@H]1C([C@@H](CC1)C(CNCCO)=C)[C@@]21C(O)=O Chemical compound CC(C)([C@@H]1CC2)C(c(cc3)ccc3C(O)=O)=CC[C@]1(C)[C@@H](CC1)[C@]2(C)[C@](C)(CC2)[C@H]1C([C@@H](CC1)C(CNCCO)=C)[C@@]21C(O)=O LZLNVZUACAOMHN-ZWOKJLCPSA-N 0.000 description 1
- SYRMPFBAVYMHEP-WVNHYXHCSA-N CC(CCN(C)C)[C@@H](C)CNC(CC1)(C(CCC2)[C@]2(CC2)C(N)=O)C2C(C)(CC2)C1C(C)(CC1)C2C(C)(C)C1c1ccc(COC(C)(C)C)cc1 Chemical compound CC(CCN(C)C)[C@@H](C)CNC(CC1)(C(CCC2)[C@]2(CC2)C(N)=O)C2C(C)(CC2)C1C(C)(CC1)C2C(C)(C)C1c1ccc(COC(C)(C)C)cc1 SYRMPFBAVYMHEP-WVNHYXHCSA-N 0.000 description 1
- BLKHTSZVILYTKT-UHFFFAOYSA-N CC=S1CCNCC1 Chemical compound CC=S1CCNCC1 BLKHTSZVILYTKT-UHFFFAOYSA-N 0.000 description 1
- OCZSNIABVJCQDB-UHFFFAOYSA-N CCCN(C)CCN(C)C Chemical compound CCCN(C)CCN(C)C OCZSNIABVJCQDB-UHFFFAOYSA-N 0.000 description 1
- TYCSKWGBDSJVGH-HSDUUJJHSA-N CCN(C)C([C@@](C)(CC1)C([C@@H](C)[C@H](C)CCN(C)CCN(C)C)C(CC2)C1C(C)(CC1)C2C2(C)C1C(C)(C)C(C1C=CC(C(N)OC(C)C)=CC1)=CC2)I Chemical compound CCN(C)C([C@@](C)(CC1)C([C@@H](C)[C@H](C)CCN(C)CCN(C)C)C(CC2)C1C(C)(CC1)C2C2(C)C1C(C)(C)C(C1C=CC(C(N)OC(C)C)=CC1)=CC2)I TYCSKWGBDSJVGH-HSDUUJJHSA-N 0.000 description 1
- LHIJANUOQQMGNT-UHFFFAOYSA-N NCCNCCO Chemical compound NCCNCCO LHIJANUOQQMGNT-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J63/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton has been modified by expansion of only one ring by one or two atoms
- C07J63/008—Expansion of ring D by one atom, e.g. D homo steroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361761403P | 2013-02-06 | 2013-02-06 | |
| US61/761403 | 2013-02-06 | ||
| PCT/US2014/014647 WO2014123889A1 (en) | 2013-02-06 | 2014-02-04 | C-19 modified triterpenoids with hiv maturation inhibitory activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105121454A true CN105121454A (zh) | 2015-12-02 |
Family
ID=50150818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480019576.0A Pending CN105121454A (zh) | 2013-02-06 | 2014-02-04 | 具有hiv成熟抑制活性的c-19经修饰的三萜类化合物 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US20140221361A1 (https=) |
| EP (1) | EP2953960A1 (https=) |
| JP (1) | JP6186010B2 (https=) |
| KR (1) | KR20150115881A (https=) |
| CN (1) | CN105121454A (https=) |
| AR (1) | AR094684A1 (https=) |
| AU (1) | AU2014215468B2 (https=) |
| BR (1) | BR112015018491A2 (https=) |
| CA (1) | CA2900124A1 (https=) |
| EA (1) | EA027371B1 (https=) |
| IL (1) | IL240289A0 (https=) |
| MX (1) | MX2015010003A (https=) |
| SG (1) | SG11201505639SA (https=) |
| TW (1) | TW201443073A (https=) |
| WO (1) | WO2014123889A1 (https=) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109153700A (zh) * | 2016-02-04 | 2019-01-04 | Viiv保健英国第五有限公司 | 作为hiv-1抑制剂的c-3和c-17修饰的三萜类化合物 |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8906889B2 (en) * | 2012-02-15 | 2014-12-09 | Bristol-Myers Squibb Company | C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity |
| RU2018105352A (ru) | 2015-07-28 | 2019-08-29 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Производные бетулина для предупреждения или лечения ВИЧ-инфекций |
| WO2017017609A1 (en) | 2015-07-28 | 2017-02-02 | Glaxosmithkline Intellectual Property (No.2) Limited | Betuin derivatives for preventing or treating hiv infections |
| WO2017025901A1 (en) * | 2015-08-11 | 2017-02-16 | Hetero Research Foundation | Novel c28-analogues with c3-modifications of triterpene derivatives as hiv inhibitors |
| RU2018112958A (ru) | 2015-09-24 | 2019-10-28 | ГлаксоСмитКлайн Интеллекчуал Проперти (N2) Лимитед | Соединения с ингибирующей созревание ВИЧ активностью |
| WO2017125870A1 (en) | 2016-01-20 | 2017-07-27 | Glaxosmithkline Intellectual Property (No.2) Limited | Amine derivatives of lupanes with hiv maturation inhibitory activity |
| WO2017149518A1 (en) * | 2016-03-04 | 2017-09-08 | Hetero Labs Limited | C-3 novel triterpene with c-17 amine derivatives as hiv inhibitors |
| WO2018002848A1 (en) * | 2016-06-30 | 2018-01-04 | VIIV Healthcare UK (No.5) Limited | Azadecalin derivatives as inhibitors of human immunodeficiency virus replication |
| EP3506902A4 (en) * | 2016-08-31 | 2020-04-22 | VIIV Healthcare Company | COMBINATIONS AND USES AND TREATMENTS THEREOF |
| WO2018044853A1 (en) * | 2016-08-31 | 2018-03-08 | Viiv Healthcare Conpany | Combinations and uses and treatments thereof |
| ES2970042T3 (es) | 2018-04-24 | 2024-05-24 | Viiv Healthcare Uk No 5 Ltd | Compuestos con actividad inhibidora de la maduración del VIH |
| CA3101643C (en) | 2018-06-29 | 2023-02-21 | Dfh Therapeutics | Triterpene amine derivatives |
| SI3924361T1 (sl) | 2019-02-11 | 2024-02-29 | Hetero Labs Limited | Novi derivati triterpena kot zaviralci virusa hiv |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5468888A (en) * | 1991-11-13 | 1995-11-21 | Rhone-Poulenc Rorer S.A. | Lupane derivatives, their preparation and the pharmaceutical compositions which contain them |
| WO2011153319A1 (en) * | 2010-06-04 | 2011-12-08 | Bristol-Myers Squibb Company | C-28 amides of modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
| WO2011153315A1 (en) * | 2010-06-04 | 2011-12-08 | Bristol-Myers Squibb Company | Modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
| WO2012106190A1 (en) * | 2011-01-31 | 2012-08-09 | Bristol-Myers Squibb Company | C-17 and c-3 modified triterpenoids with hiv maturation inhibitory activity |
| WO2012106188A1 (en) * | 2011-01-31 | 2012-08-09 | Bristol-Myers Squibb Company | C-28 amines of c-3 modified betulinic acid derivatives as hiv maturation inhibitors |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2694048B2 (ja) * | 1991-05-09 | 1997-12-24 | 日立建機株式会社 | 建設機械の油圧駆動装置 |
| US5413999A (en) | 1991-11-08 | 1995-05-09 | Merck & Co., Inc. | HIV protease inhibitors useful for the treatment of AIDS |
| US5679828A (en) | 1995-06-05 | 1997-10-21 | Biotech Research Labs, Inc. | Betulinic acid and dihydrobetulinic acid derivatives and uses therefor |
| US20020137755A1 (en) | 2000-12-04 | 2002-09-26 | Bilodeau Mark T. | Tyrosine kinase inhibitors |
| 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 |
| US7745625B2 (en) | 2004-03-15 | 2010-06-29 | Bristol-Myers Squibb Company | Prodrugs of piperazine and substituted piperidine antiviral agents |
| EP1730163A4 (en) | 2004-03-17 | 2009-12-30 | Panacos Pharmaceuticals Inc | Pharmaceutical salts of 3-O- (3,3-dimethylsuccinyl) betulinic acid |
| TW200628161A (en) | 2004-11-12 | 2006-08-16 | Panacos Pharmaceuticals Inc | Novel betulin derivatives, preparation thereof and use thereof |
| WO2008115281A2 (en) | 2006-10-16 | 2008-09-25 | Myriad Genetics, Inc. | Compounds for treating viral infections |
| 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 |
| CN103270736B (zh) | 2010-06-29 | 2016-08-10 | 华为技术有限公司 | 一种网络设备 |
| US8906889B2 (en) | 2012-02-15 | 2014-12-09 | Bristol-Myers Squibb Company | C-3 cycloalkenyl triterpenoids with HIV maturation inhibitory activity |
| WO2013160810A2 (en) * | 2012-04-24 | 2013-10-31 | Hetero Research Foundation | Novel betulinic acid derivatives as hiv inhibitors |
| US8889854B2 (en) | 2012-05-07 | 2014-11-18 | Bristol-Myers Squibb Company | C-17 bicyclic amines of triterpenoids with HIV maturation inhibitory activity |
-
2014
- 2014-02-04 SG SG11201505639SA patent/SG11201505639SA/en unknown
- 2014-02-04 US US14/172,389 patent/US20140221361A1/en not_active Abandoned
- 2014-02-04 WO PCT/US2014/014647 patent/WO2014123889A1/en not_active Ceased
- 2014-02-04 JP JP2015556998A patent/JP6186010B2/ja not_active Expired - Fee Related
- 2014-02-04 CA CA2900124A patent/CA2900124A1/en not_active Abandoned
- 2014-02-04 KR KR1020157023907A patent/KR20150115881A/ko not_active Withdrawn
- 2014-02-04 MX MX2015010003A patent/MX2015010003A/es unknown
- 2014-02-04 EP EP14705662.6A patent/EP2953960A1/en not_active Withdrawn
- 2014-02-04 EA EA201591406A patent/EA027371B1/ru not_active IP Right Cessation
- 2014-02-04 BR BR112015018491A patent/BR112015018491A2/pt not_active Application Discontinuation
- 2014-02-04 CN CN201480019576.0A patent/CN105121454A/zh active Pending
- 2014-02-04 AU AU2014215468A patent/AU2014215468B2/en not_active Ceased
- 2014-02-05 TW TW103103839A patent/TW201443073A/zh unknown
- 2014-02-06 AR ARP140100400A patent/AR094684A1/es unknown
-
2015
- 2015-08-02 IL IL240289A patent/IL240289A0/en unknown
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5468888A (en) * | 1991-11-13 | 1995-11-21 | Rhone-Poulenc Rorer S.A. | Lupane derivatives, their preparation and the pharmaceutical compositions which contain them |
| WO2011153319A1 (en) * | 2010-06-04 | 2011-12-08 | Bristol-Myers Squibb Company | C-28 amides of modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
| WO2011153315A1 (en) * | 2010-06-04 | 2011-12-08 | Bristol-Myers Squibb Company | Modified c-3 betulinic acid derivatives as hiv maturation inhibitors |
| WO2012106190A1 (en) * | 2011-01-31 | 2012-08-09 | Bristol-Myers Squibb Company | C-17 and c-3 modified triterpenoids with hiv maturation inhibitory activity |
| WO2012106188A1 (en) * | 2011-01-31 | 2012-08-09 | Bristol-Myers Squibb Company | C-28 amines of c-3 modified betulinic acid derivatives as hiv maturation inhibitors |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109153700A (zh) * | 2016-02-04 | 2019-01-04 | Viiv保健英国第五有限公司 | 作为hiv-1抑制剂的c-3和c-17修饰的三萜类化合物 |
| CN109153700B (zh) * | 2016-02-04 | 2021-03-09 | Viiv保健英国第五有限公司 | 作为hiv-1抑制剂的c-3和c-17修饰的三萜类化合物 |
Also Published As
| Publication number | Publication date |
|---|---|
| BR112015018491A2 (pt) | 2017-07-18 |
| JP2016507558A (ja) | 2016-03-10 |
| US20140221361A1 (en) | 2014-08-07 |
| TW201443073A (zh) | 2014-11-16 |
| WO2014123889A1 (en) | 2014-08-14 |
| EA201591406A1 (ru) | 2015-12-30 |
| EA027371B1 (ru) | 2017-07-31 |
| AR094684A1 (es) | 2015-08-19 |
| CA2900124A1 (en) | 2014-08-14 |
| MX2015010003A (es) | 2015-10-30 |
| EP2953960A1 (en) | 2015-12-16 |
| AU2014215468B2 (en) | 2017-05-18 |
| IL240289A0 (en) | 2015-09-24 |
| KR20150115881A (ko) | 2015-10-14 |
| JP6186010B2 (ja) | 2017-08-23 |
| SG11201505639SA (en) | 2015-08-28 |
| AU2014215468A1 (en) | 2015-09-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| RJ01 | Rejection of invention patent application after publication |
Application publication date: 20151202 |
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| RJ01 | Rejection of invention patent application after publication |