CN101479275B - 2-(取代的-氨基)-苯并噻唑磺酰胺hiv蛋白酶抑制剂 - Google Patents
2-(取代的-氨基)-苯并噻唑磺酰胺hiv蛋白酶抑制剂 Download PDFInfo
- Publication number
- CN101479275B CN101479275B CN2007800236807A CN200780023680A CN101479275B CN 101479275 B CN101479275 B CN 101479275B CN 2007800236807 A CN2007800236807 A CN 2007800236807A CN 200780023680 A CN200780023680 A CN 200780023680A CN 101479275 B CN101479275 B CN 101479275B
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- compound
- amino
- alkyl
- hiv
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- 0 CC(C)CN(C[C@]([C@](Cc1ccccc1)NC(O[C@@]1[C@](CCO2)[C@]2OC1)=O)O)S(c(cc1)cc2c1nc(N*)[s]2)(=O)=O Chemical compound CC(C)CN(C[C@]([C@](Cc1ccccc1)NC(O[C@@]1[C@](CCO2)[C@]2OC1)=O)O)S(c(cc1)cc2c1nc(N*)[s]2)(=O)=O 0.000 description 2
- XNNYFIMWBZGFIW-UHFFFAOYSA-N CC(C)(C)OC(NC(CC1)CCN1C1CCCC1)=O Chemical compound CC(C)(C)OC(NC(CC1)CCN1C1CCCC1)=O XNNYFIMWBZGFIW-UHFFFAOYSA-N 0.000 description 1
- CKXZPVPIDOJLLM-UHFFFAOYSA-N CC(C)(C)OC(NC1CCNCC1)=O Chemical compound CC(C)(C)OC(NC1CCNCC1)=O CKXZPVPIDOJLLM-UHFFFAOYSA-N 0.000 description 1
- LRQCYZRSYDIQDV-LSFRQUOKSA-N CC(C)CN(C[C@H]([C@H](Cc1ccccc1)NC(OC1[C@H](CCO)COC1)=O)O)S(c(cc1)cc2c1nc(NC(CC1)CCN1C1CCCC1)[s]2)(=O)=O Chemical compound CC(C)CN(C[C@H]([C@H](Cc1ccccc1)NC(OC1[C@H](CCO)COC1)=O)O)S(c(cc1)cc2c1nc(NC(CC1)CCN1C1CCCC1)[s]2)(=O)=O LRQCYZRSYDIQDV-LSFRQUOKSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
-
- 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
-
- 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
-
- 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
Abstract
Description
A | V003I,L010I,V032T,L033M,E035D,S037Y,M046I,R057R/K,Q058E,L063P,K070T,A071V,I072V,I084V,L089V |
B | V003I,V032I,L035D,M036I,S037N,K043T,M046I,I047V,I050V,K055R,I057K,I062V,L063P,A071L,V082I,I085V,L090M,I093L |
D | V003I L010I I013V G016A/G L019I L033F S037N M046I I050V F053LI054V K055R L063P A071V G073C V077I/V V082A L090M |
C | V003I L010F I013V V032T S037N M046I I047V I050V L063P A071VI084V L089V T091A Q092R |
化合物编号 | WT-IIIB-2-001pEC50 | ApEC50 | BpEC50 | CpEC50 | DpEC50 |
5 | 7.72 | 7.89 | 7.57 | 5.38 | 7.86 |
6 | 8.31 | 7.84 | 7.58 | 5.46 | 7.86 |
7 | 7.88 | 7.93 | 7.70 | 5.54 | 7.87 |
8 | 7.44 | 6.65 | 7.00 | 5.25 | NA |
9 | 6.56 | 6.99 | 6.59 | 5.00 | 6.99 |
10 | 6.53 | 6.84 | 6.52 | 5.11 | 6.62 |
11 | 8.60 | 7.65 | 7.47 | 5.24 | 7.73 |
12 | 8.34 | 8.26 | 7.71 | 5.19 | 8.27 |
13 | 8.18 | 8.06 | 7.94 | 6.04 | 7.98 |
14 | 7.85 | 7.85 | 7.78 | 5.90 | 7.84 |
15 | 8.24 | 8.38 | 7.71 | 5.46 | 8.24 |
16 | 6.82 | 5.93 | 5.89 | 5.90 | NA |
17 | 7.73 | 7.88 | 7.77 | 5.47 | NA |
18 | 7.76 | 7.61 | 7.24 | 5.32 | NA |
19 | 8.42 | 7.84 | 7.33 | 5.35 | 7.75 |
20 | 8.27 | 8.23 | 7.84 | 5.59 | 8.12 |
21 | 7.95 | 8.31 | 7.84 | 5.74 | 8.15 |
22 | 7.71 | NA | 7.77 | 6.19 | NA |
23 | 7.97 | 8.56 | 7.56 | 5.36 | 8.27 |
24 | 8.22 | 7.91 | 7.70 | 5.08 | 7.89 |
25 | 5.77 | 5.59 | 5.04 | <4.49 | 5.41 |
化合物 | 剂量(mg/kg) | AUC(ng.h/ml) | 红斑/水肿 |
具有式(II)的化合物+RTV* | 204080 | 7747**23016**23016** | 否否否 |
具有式(III)的参照化合物 | 104080120 | 47-2383319-50887366-1599810204-27507 | 否否是是 |
Claims (11)
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP06116003.2 | 2006-06-23 | ||
EP06116003 | 2006-06-23 | ||
PCT/EP2007/056235 WO2007147884A1 (en) | 2006-06-23 | 2007-06-22 | 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors |
Publications (2)
Publication Number | Publication Date |
---|---|
CN101479275A CN101479275A (zh) | 2009-07-08 |
CN101479275B true CN101479275B (zh) | 2012-03-07 |
Family
ID=37596252
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CN2007800236807A Active CN101479275B (zh) | 2006-06-23 | 2007-06-22 | 2-(取代的-氨基)-苯并噻唑磺酰胺hiv蛋白酶抑制剂 |
Country Status (31)
Country | Link |
---|---|
US (1) | US8202887B2 (zh) |
EP (1) | EP2035432B1 (zh) |
JP (1) | JP5232776B2 (zh) |
KR (1) | KR101419320B1 (zh) |
CN (1) | CN101479275B (zh) |
AP (1) | AP2069A (zh) |
AR (1) | AR061619A1 (zh) |
AT (1) | ATE544769T1 (zh) |
AU (1) | AU2007262943B2 (zh) |
BR (1) | BRPI0713487B1 (zh) |
CA (1) | CA2653233C (zh) |
CL (1) | CL2007001826A1 (zh) |
CY (1) | CY1112971T1 (zh) |
DK (1) | DK2035432T3 (zh) |
EA (1) | EA016387B1 (zh) |
ES (1) | ES2381129T3 (zh) |
HK (1) | HK1125633A1 (zh) |
IL (1) | IL195381A (zh) |
JO (1) | JO2841B1 (zh) |
MX (1) | MX2009000160A (zh) |
MY (1) | MY146805A (zh) |
NZ (1) | NZ573286A (zh) |
PE (1) | PE20080342A1 (zh) |
PL (1) | PL2035432T3 (zh) |
PT (1) | PT2035432E (zh) |
SI (1) | SI2035432T1 (zh) |
TW (1) | TWI415851B (zh) |
UA (1) | UA96445C2 (zh) |
UY (1) | UY30416A1 (zh) |
WO (1) | WO2007147884A1 (zh) |
ZA (1) | ZA200810350B (zh) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JO3090B1 (ar) * | 2009-12-11 | 2017-03-15 | Janssen Sciences Ireland Uc | 5- امينو-4- هيدروكسي-بنتويل اميدات |
US9102614B2 (en) | 2010-07-02 | 2015-08-11 | Gilead Sciences, Inc. | Naphth-2-ylacetic acid derivatives to treat AIDS |
AU2011274323B2 (en) | 2010-07-02 | 2015-08-06 | Gilead Sciences, Inc. | 2 -quinolinyl- acetic acid derivatives as HIV antiviral compounds |
US9024038B2 (en) * | 2010-12-27 | 2015-05-05 | Purdue Research Foundation | Compunds and methods for treating HIV |
AP2015008931A0 (en) | 2011-04-21 | 2015-12-31 | Gilead Sciences Inc | Benzothiazole compounds and their pharmaceutical use |
WO2013103738A1 (en) | 2012-01-04 | 2013-07-11 | Gilead Sciences, Inc. | Napthalene acetic acid derivatives against hiv infection |
WO2013103724A1 (en) | 2012-01-04 | 2013-07-11 | Gilead Sciences, Inc. | 2- (tert - butoxy) -2- (7 -methylquinolin- 6 - yl) acetic acid derivatives for treating aids |
CA2850881C (en) | 2012-04-20 | 2021-02-16 | Gilead Sciences, Inc. | Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection |
WO2021209563A1 (en) | 2020-04-16 | 2021-10-21 | Som Innovation Biotech, S.A. | Compounds for use in the treatment of viral infections by respiratory syndrome-related coronavirus |
Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1525962A (zh) * | 2001-02-14 | 2004-09-01 | ̩���ؿ�ҩƷ����˾ | 广谱的2-(取代-氨基)-苯并噻唑磺酰胺hiv蛋白酶抑制剂 |
CN1604803A (zh) * | 2001-12-12 | 2005-04-06 | 泰博特克药品有限公司 | 细胞色素p450依赖性蛋白酶抑制剂的组合物 |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ538488A (en) * | 2002-08-02 | 2007-10-26 | Tibotec Pharm Ltd | Broadspectrum 2-amino-benzothiazole sulfonamide HIV protease inhibitors |
JP2007507469A (ja) * | 2003-09-30 | 2007-03-29 | テイボテク・フアーマシユーチカルズ・リミテツド | Hcv阻害性スルホンアミド |
-
2007
- 2007-06-04 JO JO2007212A patent/JO2841B1/en active
- 2007-06-15 UY UY30416A patent/UY30416A1/es not_active Application Discontinuation
- 2007-06-21 CL CL2007001826A patent/CL2007001826A1/es unknown
- 2007-06-22 PE PE2007000802A patent/PE20080342A1/es active IP Right Grant
- 2007-06-22 PL PL07765554T patent/PL2035432T3/pl unknown
- 2007-06-22 TW TW096122406A patent/TWI415851B/zh active
- 2007-06-22 KR KR1020097000754A patent/KR101419320B1/ko active IP Right Grant
- 2007-06-22 DK DK07765554.6T patent/DK2035432T3/da active
- 2007-06-22 JP JP2009515891A patent/JP5232776B2/ja active Active
- 2007-06-22 SI SI200730904T patent/SI2035432T1/sl unknown
- 2007-06-22 AP AP2008004679A patent/AP2069A/en active
- 2007-06-22 CN CN2007800236807A patent/CN101479275B/zh active Active
- 2007-06-22 ES ES07765554T patent/ES2381129T3/es active Active
- 2007-06-22 BR BRPI0713487-8A patent/BRPI0713487B1/pt not_active IP Right Cessation
- 2007-06-22 EA EA200970052A patent/EA016387B1/ru not_active IP Right Cessation
- 2007-06-22 MY MYPI20085209A patent/MY146805A/en unknown
- 2007-06-22 PT PT07765554T patent/PT2035432E/pt unknown
- 2007-06-22 AR ARP070102776A patent/AR061619A1/es active IP Right Grant
- 2007-06-22 WO PCT/EP2007/056235 patent/WO2007147884A1/en active Application Filing
- 2007-06-22 MX MX2009000160A patent/MX2009000160A/es active IP Right Grant
- 2007-06-22 NZ NZ573286A patent/NZ573286A/en not_active IP Right Cessation
- 2007-06-22 AU AU2007262943A patent/AU2007262943B2/en not_active Ceased
- 2007-06-22 EP EP07765554A patent/EP2035432B1/en active Active
- 2007-06-22 AT AT07765554T patent/ATE544769T1/de active
- 2007-06-22 US US12/304,990 patent/US8202887B2/en active Active
- 2007-06-22 UA UAA200813950A patent/UA96445C2/ru unknown
- 2007-06-22 CA CA2653233A patent/CA2653233C/en active Active
-
2008
- 2008-11-19 IL IL195381A patent/IL195381A/en active IP Right Grant
- 2008-12-05 ZA ZA200810350A patent/ZA200810350B/xx unknown
-
2009
- 2009-04-30 HK HK09104046.7A patent/HK1125633A1/xx not_active IP Right Cessation
-
2012
- 2012-05-08 CY CY20121100429T patent/CY1112971T1/el unknown
Patent Citations (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1525962A (zh) * | 2001-02-14 | 2004-09-01 | ̩���ؿ�ҩƷ����˾ | 广谱的2-(取代-氨基)-苯并噻唑磺酰胺hiv蛋白酶抑制剂 |
CN1604803A (zh) * | 2001-12-12 | 2005-04-06 | 泰博特克药品有限公司 | 细胞色素p450依赖性蛋白酶抑制剂的组合物 |
Non-Patent Citations (1)
Title |
---|
Dominique L.N.G. Surleraux et al..Design of Hiv-1 Protease Inhibitors Active on Multidrug-Resistant Virus.《J.Med.Chem.》.2005,第48卷(第6期),1965-1973. * |
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C14 | Grant of patent or utility model | ||
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Owner name: IRELAND JANSSEN R + D COMPANY Free format text: FORMER OWNER: JANSSEN R + D IRELAND Effective date: 20150724 |
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C41 | Transfer of patent application or patent right or utility model | ||
C56 | Change in the name or address of the patentee |
Owner name: TIBOTEC PHARM LTD. Free format text: FORMER NAME: TIBOTEC NV Owner name: JANSSEN R + D IRELAND Free format text: FORMER NAME: TIBOTEC PHARM LTD. |
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CP01 | Change in the name or title of a patent holder |
Address after: The Irish Village Patentee after: JANSSEN R&D IRELAND Address before: The Irish Village Patentee before: TIBOTEC PHARMACEUTICALS Address after: The Irish Village Patentee after: TIBOTEC PHARMACEUTICALS Address before: The Irish Village Patentee before: TIBOTEC PHARMACEUTICALS Ltd. |
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Effective date of registration: 20150724 Address after: The Irish Village Patentee after: JANSSEN R&D IRELAND Address before: The Irish Village Patentee before: JANSSEN R&D IRELAND |