CN101903371B - N-(叔-丁氧基羰基)-3-甲基-l-缬氨酰-(4r)-4-((7-氯-4-甲氧基-1-异喹啉基)氧基)-n-((1r,2s)-1-((环丙基磺酰基)氨甲酰基)-2-乙烯基环丙基)-l-脯氨酰胺的晶型 - Google Patents
N-(叔-丁氧基羰基)-3-甲基-l-缬氨酰-(4r)-4-((7-氯-4-甲氧基-1-异喹啉基)氧基)-n-((1r,2s)-1-((环丙基磺酰基)氨甲酰基)-2-乙烯基环丙基)-l-脯氨酰胺的晶型 Download PDFInfo
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- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
- C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Abstract
Description
商品名 | 生理学种类 | 抑制剂或靶点的类型 | 来源公司 |
NIM811 | 亲环蛋白(Cyclophilin)抑制剂 | Novartis | |
Zadaxin | 免疫调节剂 | Sciclone | |
Suvus | 亚甲蓝 | Bioenvision | |
Actilon(CPG10101) | TLR9激动剂 | Coley | |
Batabulin(T67) | 抗癌 | β-微管蛋白抑制剂 | Tularik Inc.,South SanFrancisco,CA |
ISIS 14803 | 抗病毒 | 反义 | ISIS PharmaceuticalsInc,Carlsbad,CA/ElanPhamaceuticals Inc.,NewYork,NY |
Summetrel | 抗病毒 | 抗病毒 | Endo PharmaceuticalsHoldings Inc.,ChaddsFord,PA |
GS-9132(ACH-806) | 抗病毒 | HCV抑制剂 | Achillion/Gilead |
吡唑并嘧啶化合物和盐,得自2005年5月26日的WO-2005047288 | 抗病毒 | HCV抑制剂 | Arrow TherapeuticsLtd. |
Levovirin | 抗病毒 | IMPDH抑制剂 | Ribapharm Inc.,CostaMesa,CA |
Merimepodib(VX-497) | 抗病毒 | IMPDH抑制剂 | VertexPharmaceuticals Inc.,Cambridge,MA |
商品名 | 生理学种类 | 抑制剂或靶点的类型 | 来源公司 |
XTL-6865(XTL-002) | 抗病毒 | 单克隆抗体 | XTLBiopharmaceuticalsLtd.,Rehovot,Isreal |
Telaprevir(VX-950,LY-570310) | 抗病毒 | NS3丝氨酸蛋白酶抑制剂 | VertexPharmaceuticals Inc.,Cambridge,MA/EliLilly and Co.Inc.,Indianapolis,IN |
HCV-796 | 抗病毒 | NS5B复制酶抑制剂 | Wyeth/Viropharma |
NM-283 | 抗病毒 | NS5B复制酶抑制剂 | Idenix/Novartis |
GL-59728 | 抗病毒 | NS5B复制酶抑制剂 | Genne Labs/Novartis |
GL-60667 | 抗病毒 | NS5B复制酶抑制剂 | Gene Labs/Novartis |
2’C MeA | 抗病毒 | NS5B复制酶抑制剂 | Gilead |
PSI 6130 | 抗病毒 | NS5B复制酶抑制剂 | Roche |
R1626 | 抗病毒 | NS5B复制酶抑制剂 | Roche |
2’C甲基腺苷 | 抗病毒 | NS5B复制酶抑制剂 | Merek |
JTK-003 | 抗病毒 | RdRp抑制剂 | Japan Tobacco Inc.,Tokyo,Japann |
Levovirin | 抗病毒 | 利巴韦林 | ICN Pharmaceuticals,Costa Mesa,CA |
Ribavirin | 抗病毒 | 利巴韦林 | Schering-PloughCorporation,Kenilworth,NJ |
Viramidine | 抗病毒 | 利巴韦林前药 | Ribapharm Inc.,CostaMesa,CA |
Heptazyme | 抗病毒 | 核酶 | RibozymePharmaceuticals Inc.,Boulder,CO |
BILN-2061 | 抗病毒 | 丝氨酸蛋白酶抑制剂 | Boehringer IngelheimPharma KG,Ingelheim,Germany |
SCH 503034 | 抗病毒 | 丝氨酸蛋白酶抑制剂 | Schering Plough |
Zadazim | 免疫调节剂 | 免疫调节剂 | SciClonePharmaceuticals Inc.,San Mateo,CA |
Ceplene | 免疫调节剂 | 免疫调节剂 | MaximPharmaceuticals Inc.,San Diego,CA |
CellCept | 免疫抑制剂 | HCV IgG免疫抑制剂 | F.Hoffmann-LaRoche LTD,Basel,Switzerland |
Civacir | 免疫抑制剂 | HCV IgG免疫抑制剂 | NabiBiopharmaceuticalsInc.,Boca Raton,FL |
Albuferon-α | 干扰素 | 白蛋白IFN-α2b | Human GenomeSciences Inc.,Rockville,MD |
Infergen A | 干扰素 | IFN alfacon-1 | InterMunePharmaceuticals Inc.,Brisbane,CA |
商品名 | 生理学种类 | 抑制剂或靶点的类型 | 来源公司 |
Omega IFN | 干扰素 | IFN-ω | Intarcia Therapeutics |
IFN-β和EMZ701 | 干扰素 | IFN-β和EMZ70l | TransitionTherapeutics Inc.,Ontario,Canada |
Rebif | 干扰素 | IFN-βla | Serono,Geneva,Switzerland |
RoferonA | 干扰素 | IFN-α2a | F.Hoffmann-LaRoche LTD,Basel,SwitzerlaInd |
Intron A | 干扰素 | IFN-α2b | Schering-PloughCorporation,Kenilworth,NJ |
Intron A和Zadaxin | 干扰素 | IFN-α2b/α1-胸腺素 | RegeneRxBiopharmiceuticalsInc.,Bethesda,MD/SciClonePharmaceuticals Inc,San Mateo,CA |
Rebetron | 干扰素 | IFN-α2b/利巴韦林 | Schering-PloughCorporation,Kenilworth,NJ |
Actimmune | 干扰素 | INF-γ | InterMune Inc.,Brisbane,CA |
Interferon-β | 干扰素 | 干扰素-β-la | Serono |
Multiferon | 干扰素 | 长效IFN | Viragen/Valentis |
Wellferon | 干扰素 | 类淋巴母细胞IFN-αn1 | GlaxoSmithKline plc,Uxbridge,UK |
Omniferon | 干扰素 | 天然IFN-α | Viragen Inc.,Plantation,FL |
Pegasys | 干扰素 | PEG基化的IFN-α2a | F.Hoffmann-LaRoehe LTD,Basel,Switzerland |
Pegasys和Ceplene | 干扰素 | PEG 基化的IFN-α2a/免疫调节剂 | MaximPharmaceuticals Inc.,SanDiego,CA |
Pegasys和Ribavirin | 干扰素 | PEG 基化的IFN-α2a/利巴韦林 | F.Hoffmann-LaRoche LTD,Basel,Switzerland |
PEG-Intron | 干扰素 | PEG基化的IFN-α2b | Schering-PloughCorporation,Kenilworth,NJ |
PEG-Intron/Ribavirin | 干扰素 | PEG 基化的IFN-α2b/利巴韦林 | Schering-PloughCorporation,Kenilworth,NJ |
IP-501 | 肝保护 | 抗纤维化(antifibrotic) | IndevusPharmaceutieals Inc.,Lexington,MA |
IDN-6556 | 肝保护 | 半胱天冬酶抑制剂 | Idun PharmaceuticalsInc.,San Diego,CA |
ITMN-191(R-7227) | 抗病毒 | 丝氨酸蛋白酶抑制剂 | InterMunePharmaceuticals Inc.,Brisbane,CA |
商品名 | 生理学种类 | 抑制剂或靶点的类型 | 来源公司 |
GL-59728 | 抗病毒 | NS5B复制酶抑制剂 | Genelabs |
ANA-971 | 抗病毒 | TLR-7激动剂 | Anadys |
TMC-465350 | 抗病毒 | 丝氨酸蛋白酶抑制剂 | Medivir/Tibotec |
原子 | X | Y | Z | 原子 | X | Y | Z |
S(1) | 4633(2) | 1649(1) | 6093(1) | O(8) | 2101(3) | 6221(2) | 4962(2) |
N(1) | 4351(5) | 2223(2) | 5569(2) | C(1) | 2870(11 | 464(5) | 5759(4) |
N(2) | 3770(4) | 3280(2) | 4728(1) | C(2) | 4303(8) | 668(3) | 5873(3) |
N(3) | 3590(4) | 4937(2) | 5607(2) | C(3) | 3535(11 | 137(4) | 6251(3) |
N(4) | 2677(6) | 4277(4) | 6916(2) | C(4) | 5005(5) | 2093(3) | 5089(2) |
O(1) | 3677(8) | 1898(3) | 6465(2) | C(5) | 4463(4) | 2547(3) | 4620(2) |
O(2) | 5997(7) | 1682(4) | 6230(3) | C(6) | 5213(6) | 2451(3) | 4100(2) |
O(3) | 5891(4) | 1613(2) | 5053(2) | C(7) | 3892(6) | 2041(3) | 4159(2) |
O(4) | 5570(3) | 3910(2) | 5093(2) | C(8) | 3733(7) | 1146(4) | 4208(2) |
O(5) | 3215(3) | 3701(2) | 5941(1) | C(9) | 4597(9) | 621(4) | 4048(5) |
O(6) | 1838(7) | 5342(6) | 7297(3) | C(10) | 4385(4) | 3907(2) | 4968(2) |
O(7) | 965(8) | 4111(6) | 7476(3) | C(11) | 3500(4) | 4639(2) | 5061(2) |
C(12) | 3970(6) | 5355(3) | 4730(2) | C(30) | 304(8) | 6707(3) | 4469(3) |
C(13) | 3495(5) | 6077(3) | 5045(2) | C(31) | -584(7) | 6494(3) | 4875(3) |
C(14) | 3637(6) | 5819(3) | 5640(2) | C(32) | -1848(7) | 6620(4) | 4807(5) |
C(15) | 3451(5) | 4424(3) | 6021(2) | C(33) | -2325(15) | 6965(6) | 4310(7) |
C(16) | 3606(6) | 4702(3) | 6603(2) | C(34) | -1576(17) | 7197(5) | 3918(5) |
C(17) | 5104(7) | 4618(4) | 6797(3) | C1(1) | -2988(2) | 6335(2) | 5319(2) |
C(18) | 5991(7) | 5136(5) | 6512(3) | C(4′) | -530(14) | 5479(13) | 7544(9) |
C(19) | 5075(13 | 4835(6) | 7407(3) | C(3′) | 1250(30) | 6541(9) | 7751(10) |
C(20) | 5573(8) | 3749(5) | 6748(4) | C(2′) | 1088(19) | 5236(10) | 8267(5) |
C(21) | 1764(11 | 4565(8) | 7247(3) | C(1′) | 921(17) | 5659(9) | 7735(6) |
C(26) | 1723(7) | 6568(3) | 4504(2) | O(28) | 253(10) | 7631(5) | 3159(3) |
N(5) | 2626(8) | 6756(3) | 4152(2) | C(281 | 1165(18) | 7762(10) | 2753(6) |
C(27) | 2129(14) | 7105(5) | 3682(3) | OW | 1760(70) | 6690(30) | 6150(30) |
C(28) | 820(19) | 7272(4) | 3590(3) | ||||
C(29) | -131(13) | 7075(3) | 3984(3) |
晶型H-1 | 晶型T1F-1/2 |
6.3 | 7.3 |
7.1 | 9.1 |
9.4 | 10.0 |
10.3 | 10.6 |
12.7 | 11.1 |
13.8 | 12.3 |
17.5 | 15.6 |
18.7 | 20.1 |
20.6 | 20.9 |
22.5 | 27.8 |
Claims (8)
Priority Applications (2)
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CN201410043331.3A CN103755784B (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
CN201610420780.4A CN106146613A (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
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US61/015795 | 2007-12-21 | ||
PCT/US2008/086587 WO2009085659A1 (en) | 2007-12-21 | 2008-12-12 | Crystalline forms of n-(tert-butoxycarbonyl)-3-methyl-l-valyl-(4r)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-n-((1r,2s)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-l-prolinamide |
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CN201610420780.4A Division CN106146613A (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
CN201410043331.3A Division CN103755784B (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
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CN201610420780.4A Pending CN106146613A (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
CN201410043331.3A Expired - Fee Related CN103755784B (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
CN200880121915.0A Expired - Fee Related CN101903371B (zh) | 2007-12-21 | 2008-12-12 | N-(叔-丁氧基羰基)-3-甲基-l-缬氨酰-(4r)-4-((7-氯-4-甲氧基-1-异喹啉基)氧基)-n-((1r,2s)-1-((环丙基磺酰基)氨甲酰基)-2-乙烯基环丙基)-l-脯氨酰胺的晶型 |
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CN201610420780.4A Pending CN106146613A (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
CN201410043331.3A Expired - Fee Related CN103755784B (zh) | 2007-12-21 | 2008-12-12 | N‑(叔‑丁氧基羰基)‑3‑甲基‑l‑缬氨酰‑(4r)‑4‑((7‑氯‑4‑甲氧基‑1‑异喹啉基)氧基)‑n‑((1r,2s)‑1‑((环丙基磺酰基)氨甲酰基)‑2‑乙烯基环丙基)‑l‑脯氨酰胺的晶型 |
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KR101560428B1 (ko) | 2015-10-15 |
DK2231639T3 (en) | 2015-07-06 |
AR069886A1 (es) | 2010-02-24 |
MX2010006489A (es) | 2010-07-05 |
HRP20150458T1 (hr) | 2015-06-05 |
US20090202476A1 (en) | 2009-08-13 |
CN101903371A (zh) | 2010-12-01 |
PE20091217A1 (es) | 2009-08-14 |
US8338606B2 (en) | 2012-12-25 |
KR20100099703A (ko) | 2010-09-13 |
MX336329B (es) | 2016-01-15 |
CL2008003849A1 (es) | 2009-05-29 |
AR106338A2 (es) | 2018-01-03 |
WO2009085659A1 (en) | 2009-07-09 |
CN106146613A (zh) | 2016-11-23 |
ES2536409T3 (es) | 2015-05-25 |
CN103755784A (zh) | 2014-04-30 |
US8202996B2 (en) | 2012-06-19 |
TW200932214A (en) | 2009-08-01 |
PE20170534A1 (es) | 2017-05-11 |
JP2011507869A (ja) | 2011-03-10 |
EP2231639A1 (en) | 2010-09-29 |
TWI496573B (zh) | 2015-08-21 |
SI2231639T1 (sl) | 2015-11-30 |
JP5566907B2 (ja) | 2014-08-06 |
US20120230949A1 (en) | 2012-09-13 |
PE20131130A1 (es) | 2013-10-05 |
CN103755784B (zh) | 2017-04-12 |
EP2231639B1 (en) | 2015-04-01 |
PT2231639E (pt) | 2015-06-03 |
AU2008343423A1 (en) | 2009-07-09 |
AU2008343423B2 (en) | 2013-10-10 |
PL2231639T3 (pl) | 2015-09-30 |
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