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1. 发明申请

US20080221140A1 1-[2',3' -Dideoxy-3' C-(Hydroxymethyl) - Beta-D-Erythro-Pentofuranosyl] Cytosine Derivatives as Hiv 失效
标题翻译： 1- [2'，3'-二脱氧-3'C-（羟甲基）-β-D-红 - 戊呋喃糖基]胞嘧啶衍生物
公开(公告)号：US20080221140A1
公开(公告)日：2008-09-11
申请号：US11994633
申请日：2006-07-05
申请人： Xiao-Xiong Zhou , Christer Sahlberg
发明人： Xiao-Xiong Zhou , Christer Sahlberg
IPC分类号： A61K31/513 , C07D493/04 , A61P31/18
CPC分类号： C07D493/04
摘要： Compounds of the formula (I) wherein: R1 is independently H1—OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is —OR3, that R2 may also be —C(═O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1, 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.
摘要翻译：式（I）的化合物其中：R 1独立地是H 1 - ， - 3，NHR 4， ; C 1 -C 4烷基; 或者当n为2时，相邻的R 1一起限定烯键; R 2是H; 或者当R 1是C 1 -C 4烷基时，R 2也可以是C 1 -C 4烷基， C 1 -C 4烷基; 或当R 1为-OR 3时，R 2还可以是-C（ - ） - OH或其药学上可接受的酯的; R 3独立地为H或其药学上可接受的酯; R 4独立地是H或其药学上可接受的酰胺; R 5和R 6是H或胺前体药物部分n是1,2或3; 及其药学上可接受的盐; 可用于治疗或预防艾滋病毒，特别是逆转录酶突变体，其允许通过ATP-或焦磷酸盐介导的切除从新生DNA链中切除专一性链终止核苷或磷酸核苷酸。

2. 发明申请

US20080070951A1 Non-Nucleotide Reverse Transcriptase Inhibitors 有权
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：US20080070951A1
公开(公告)日：2008-03-20
申请号：US10584933
申请日：2004-12-30
申请人： Christian Sund , Nathalie Roue , Stefan Lindstrom , Dmitry Antonov , Christer Sahlberg , Katarina Jansson
发明人： Christian Sund , Nathalie Roue , Stefan Lindstrom , Dmitry Antonov , Christer Sahlberg , Katarina Jansson
IPC分类号： A61K31/44 , A61P31/18 , C07D211/00
CPC分类号： C07D409/12 , C07D405/12 , C07D405/14 , C07D409/14
摘要： Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(═O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(═O)ORx, —NRxOH; —C(═O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(═O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(═O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(═O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is —O —, —S(═O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8′)n-D-(CR8R8′)m-; D is a bond, —NR9—, —O—, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
摘要翻译：式Z的化合物：其中; A是CH或N; R 1是含有选自-S（-O）n R a的A的环中的碳原子的取代基，其中R a是-C 1 - -O - ， - NR x R x，-NHNR x R x，-NHNHC（-O）OR x，-NR x OH; -C（-O）-R b，其中R b是-C 1 -C 4烷基，OR x，-NR x R x，-NHNR x R x，-NHC 1 -C 3 - 烷基 - C（-O）OR x -NR x R c，其中R c是H，C 1 -C 4烷基，-NR x R x; -C（= O）R d，-CN，S（-O）p R x，其中Rd是Rd是C 1 -C 4 - 烷基，-OR x，-NR x R x C 1 -C 3 - / - 烷基-O-C 1 -C 3 - 烷基C（O）OR x，-C 1 -C 3 - 烷基-COOR x; -C 1 -C 3烷基-OH或C 1 -C 4烷基醚或其酯（OC 烷基）qO-Rx，具有1-3个杂原子的5或6元芳环p为1或2; R x独立地选自H，C 1 -C 4烷基或乙酰基; 或一对Rx可与相邻的N原子一起形成环; L是-O - ， - S（-O） - 或-CH 2 - ，其中r是0,1或2; R 3 -R 7是说明书中定义的取代基; X是 - （CR 8 R 8 8）n-D-（CR 8 R 8）m - ; D是键，-NR 9 - ， - O - ， - S - ， - S（= O） - 或-S（= O）2 - 其药学上可接受的盐和前药具有作为HIV抗病毒剂的效用。

3. 发明申请

US20050240035A1 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US20050240035A1
公开(公告)日：2005-10-27
申请号：US11071675
申请日：2005-03-02
申请人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Oden , Lotta Naeslund
发明人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Oden , Lotta Naeslund
IPC分类号： C07D335/06 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P31/18 , A61P37/04 , A61P43/00 , C07C43/23 , C07C245/18 , C07D307/93 , C07D311/78 , C07D311/94 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
摘要翻译：本发明涉及对HIV-1有活性且具有改善的抗药性和药代动力学特征的非核苷逆转录酶抑制剂。本发明还涉及合成这些化合物的新型中间体以及该化合物在抗病毒方法和组合物中的用途。

4. 发明授权

US06458772B1 Prodrugs 失效
标题翻译：前药
公开(公告)号：US06458772B1
公开(公告)日：2002-10-01
申请号：US09249317
申请日：1999-02-12
申请人： Xiao-Xiong Zhou , Nils Gunnar Johansson , Horst Wahling , Christian Sund , Hans Wallberg , Lourdes Salvador , Stefan Lindstrom , Christer Sahlberg
发明人： Xiao-Xiong Zhou , Nils Gunnar Johansson , Horst Wahling , Christian Sund , Hans Wallberg , Lourdes Salvador , Stefan Lindstrom , Christer Sahlberg
IPC分类号： A61K3170
CPC分类号： C07D213/80 , C07C271/22 , C07D213/85 , C07D307/68 , C07D473/32 , C07D513/04 , C07F9/4006 , C07F9/404 , C07F9/4075 , C07F9/572 , C07H17/08 , C07H19/00 , C07H19/16 , C40B40/00
摘要： Compounds of the formula I or corresponding monohydroxynucleoside derivatives wherein: R1 is hydroxy, amino or carboxy: optionally having esterified/amide bonded thereon; a C4-C22 saturated or unsaturated, optionally substituted fatty acid or alcohol, or an aliphatic L-amino acid; R2 is the residue of an aliphatic L-amino acid; L1 is a trifunctional linker group; L2 is absent or a difunctional linker group; and pharmaceutically acceptable salts thereof have favorable pharmacological properties and are antivirally active.
摘要翻译：式I或相应的单羟基核苷衍生物的化合物，其中：R 1是羟基，氨基或羧基：任选地在其上键合有酯化/酰胺; C 4 -C 22饱和或不饱和，任选取代的脂肪酸或醇或脂族L-氨基酸; R 2 是脂族L-氨基酸的残基; L1是三官能连接基团; L2不存在或双官能连接基团;其药学上可接受的盐具有有利的药理学性质并具有抗病毒活性。

5. 发明授权

US08143396B2 1-[2′, 3′ -dideoxy-3′ C- (hydroxymethyl)—beta-D-erythro-pentofuranosyl] cytosine derivatives as HIV inhibitors 失效
标题翻译： 1- [2'，3'-二脱氧-3'C-（羟甲基）-β-D-赤 - 戊呋喃糖基]胞嘧啶衍生物作为HIV抑制剂
公开(公告)号：US08143396B2
公开(公告)日：2012-03-27
申请号：US12982667
申请日：2010-12-30
申请人： Xiao-Xiong Zhou , Christer Sahlberg
发明人： Xiao-Xiong Zhou , Christer Sahlberg
IPC分类号： C07D239/22
CPC分类号： C07D493/04
摘要： Novel bicyclic tetrahydrofuran compounds and derivatives, and pharmaceutically acceptable salts thereof, according to the formula: These compounds have utility in the treatment of retroviruses such as HIV, especially reverse transcriptase mutant which allow an obligate chain terminating nucleoside- or nucleotide-phosphate to be excised from the nascent DNA strand by ATP or pyrophosphate-mediated excision.
摘要翻译：根据下式的新型双环四氢呋喃化合物及其衍生物及其药学上可接受的盐：这些化合物可用于治疗逆转录病毒如HIV，特别是逆转录酶突变体，其允许切断专一性链终止核苷或磷酸核苷酸从新生的DNA链通过ATP或焦磷酸盐介导的切除。

6. 发明授权

US07888367B2 1-[2′,3′ -dideoxy-3′ C-(hydroxymethyl)—beta-D-erythro-pentofuranosyl] cytosine derivatives as HIV 失效
标题翻译： 1- [2'，3'-二脱氧-3'C-（羟甲基）-β-D-赤 - 戊呋喃糖基]胞嘧啶衍生物作为HIV
公开(公告)号：US07888367B2
公开(公告)日：2011-02-15
申请号：US11994633
申请日：2006-07-05
申请人： Xiao-Xiong Zhou , Christer Sahlberg
发明人： Xiao-Xiong Zhou , Christer Sahlberg
IPC分类号： C07D493/04 , A61K31/513
CPC分类号： C07D493/04
摘要： Compounds of the formula (I) wherein: R1 is independently H1—OR3, —NHR4; C1-C4 alkyl; or, when n is 2, adjacent R1 together define an olefinic bond; R2 is H; or when the gem R1 is C1-C4 alkyl, that R2 may also be C1-C4 alkyl; or when the gem R1 is —OR3, that R2 may also be —C(═O)OH or a pharmaceutically acceptable ester thereof; R3 is independently H, or a pharmaceutically acceptable ester thereof; R4 is independently H or a pharmaceutically acceptable amide thereof; R5 and R6 are H or an amine prodrug moiety n is 1, 2 or 3; and pharmaceutically acceptable salts thereof; have utility in the treatment or prophylaxis of HIV, especially reverse transcriptase mutants which allow an obligate chain terminating nucleoside- or nucleotide phosphate to be excised from the nascent DNA strand by ATP- or pyrophosphate-mediated excision.
摘要翻译：式（I）的化合物，其中：R 1独立地为H 1 -OR 3，-NHR 4; C 1 -C 4烷基; 或者当n为2时，相邻的R1一起限定烯键; R2为H; 或者当R 1为C 1 -C 4烷基时，R 2也可以是C 1 -C 4烷基; 或者当R 1为-OR 3时，该R2也可为-C（= O）OH或其药学上可接受的酯; R3独立地为H，或其药学上可接受的酯; R4独立地为H或其药学上可接受的酰胺; R5和R6是H或胺前体药物部分n是1,2或3; 及其药学上可接受的盐; 可用于治疗或预防艾滋病毒，特别是逆转录酶突变体，其允许通过ATP-或焦磷酸盐介导的切除从新生DNA链中切除专一性链终止核苷或磷酸核苷酸。

7. 发明申请

US20060167055A1 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US20060167055A1
公开(公告)日：2006-07-27
申请号：US10526598
申请日：2003-09-05
申请人： Dmitry Antonov , Christian Sund , Stefan Lindstrom , Christer Sahlberg
发明人： Dmitry Antonov , Christian Sund , Stefan Lindstrom , Christer Sahlberg
IPC分类号： A61K31/4433 , A61K31/4436 , C07D409/02
CPC分类号： C07D213/73 , C07D213/65 , C07D307/93 , C07D311/94 , C07D333/78 , C07D335/06 , C07D405/12 , Y02P20/582
摘要： A compound of the formula (Y): where; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(C8R8)n-D-(C8C8′)m—; D is a bond, —NR9—, —O—, —S—, —S(═O)— or —S(═O)2; n and m are independently 0, 1 or 2, R8 and R8′ are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8′ together with their adjacent C atom is —C(═O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(═O)—, —NR9—, —O—, —S—, —S(═O)2—; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q≦2; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, hydroxy; have utility as HIV antivirals.
摘要翻译：式（Y）的化合物：其中; R 1是O，S; R 2是含氮杂环; R 3是H，C 1 -C 3烷基; X是 - （C 8 R 8） - - - - （C 8 C 8） / SUB>'） D是键，-NR 9 - ， - O - ， - S - ， - S（-O） - 或-S（-O）2。 n和m独立地为0,1或2，R 8和R 8独立地为H，C 1 -C 3 烷基，卤代C 1 -C 3烷基，羟基或R 8和R 8' 与它们相邻的C原子一起是-C（-O） - ; R 9独立地是H，C 1 -C 3烷基; E是CH 2 - ， - CHOH - ， - C（-O） - ， - NR 9 - ， - O - ， - S - ， - S（-O ）＆lt; 2＆gt; - ; n和m独立地为0,1或2; p和q独立地为0,1或2，其中p + q <= 2; R 10是任选取代的碳环或杂环; R 11独立地是H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基， 3烷基，羟基; 具有艾滋病毒抗病毒药物的作用。

8. 发明授权

US5576429A 5-substituted pyrimidine nucleosides and nucleotides 失效
标题翻译： 5-取代的嘧啶核苷和核苷酸
公开(公告)号：US5576429A
公开(公告)日：1996-11-19
申请号：US395877
申请日：1995-02-28
申请人： Karl N. G. Johansson , Hans C. G. Malmberg , Rolf Noreen , S. Christer Sahlberg , Daniel D. Sohn , Sal o Gronowitz
发明人： Karl N. G. Johansson , Hans C. G. Malmberg , Rolf Noreen , S. Christer Sahlberg , Daniel D. Sohn , Sal o Gronowitz
IPC分类号： A61K31/505 , A61K31/53 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61P31/12 , C07D239/36 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D421/14 , C07D493/04 , C07D495/04 , C07F9/6558 , C07H19/06 , C07H19/10 , C07H19/00
CPC分类号： C07D239/36 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D417/04 , C07D495/04 , C07H19/06 , C07H19/10
摘要： The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections.
摘要翻译：本发明涉及式（I）的化合物，其中R 1是OH，NH 2; R2是杂芳族或芳族取代基; R3是H，OH，F，OCH3; R4是H，F，OH或其醚或酯残基，OCH3，CN，C = CH，N3; R5是OH或其醚或酯残基，包括单，二和三磷酸酯（α），其中n为0或1，M为氢或药学上可接受的抗衡离子如钠，钾，铵或烷基铵; 及其药学上可接受的盐; 并且包含所述化合物的药物组合物可用于病毒感染的治疗性治疗。

9. 发明授权

US07517992B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US07517992B2
公开(公告)日：2009-04-14
申请号：US10526598
申请日：2003-09-05
申请人： Dmitry Antonov , Christian Sund , Stefan Lindström , Christer Sahlberg
发明人： Dmitry Antonov , Christian Sund , Stefan Lindström , Christer Sahlberg
IPC分类号： C07D401/12 , A61K31/444
CPC分类号： C07D213/73 , C07D213/65 , C07D307/93 , C07D311/94 , C07D333/78 , C07D335/06 , C07D405/12 , Y02P20/582
摘要： A compound of the formula (Y): where; R1 is O, S; R2 is a nitrogen-containing heterocycle; R3 is H, C1-C3 alkyl; X is —(CR8R8′)n-D-(CR8R8′)m—; D is a bond, —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; n and m are independently 0, 1 or 2, R8 and R8′ are independently H, C1-C3 alkyl, haloC1-C3alkyl, hydroxy, or R8 and R8′ together with their adjacent C atom is —C(═O)—; R9 is independently H, C1-C3 alkyl; E is CH2—, —CHOH—, —C(═O)—, —NR9—, —O—, —S—, —S(═O)2—; n and m are independently 0, 1 or 2; p and q are independently 0, 1 or 2, where p+q≦2; R10 is an optionally substituted carbocycle or heterocycle; R11 is independently H, C1-C3 alkyl, halo substituted C1-C3alkyl, hydroxy; have utility as HIV antivirals.
摘要翻译：式（Y）的化合物：其中; R1为O，S; R2是含氮杂环; R3是H，C1-C3烷基; X是 - （CR8R8'）n-D-（CR8R8'）m-; D是键，-NR 9 - ， - O - ， - S - ， - S（-O） - 或-S（-O） n和m独立地是0,1或2，R 8和R 8'独立地是H，C 1 -C 3烷基，卤代C 1 -C 3烷基，羟基或R 8和R 8'连同它们相邻的C原子是-C（ - ） - 。 R9独立地为H，C1-C3烷基; E是CH 2 - ， - CHOH - ， - C（-O） - ， - NR 9 - ， - O - ， - S - ， - S（-O） n和m独立地为0,1或2; p和q独立地为0,1或2，其中p + q <= 2; R 10是任选取代的碳环或杂环; R 11独立地为H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基，羟基; 具有艾滋病毒抗病毒药物的作用。

10. 发明授权

US06894177B2 Intermediate compounds of non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂的中间体化合物
公开(公告)号：US06894177B2
公开(公告)日：2005-05-17
申请号：US10377057
申请日：2003-02-28
申请人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
发明人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
IPC分类号： C07D335/06 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P31/18 , A61P37/04 , A61P43/00 , C07C43/23 , C07C245/18 , C07D307/93 , C07D311/78 , C07D311/94 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D311/02
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CH2)n−—D—(CH2)m—; D is —O—, —S—; n and m are independently 0 or 1; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式I化合物：其中; R 1是O，S; R 2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3是H，C 1 -C 3烷基，R 4 -R 7，独立地选自H，C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，卤代C 1 -C 6烷基，C 1 -C 12烷基，C 1 -C 6烷基，C 1〜 C 6 -C 6烷酰基，C 1 -C 6烷酰基，C 1 -C 6烷酰基，烷氧基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基-C

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