公开(公告)号：US5241107A

公开(公告)日：1993-08-31

申请号：US798125

申请日：1985-11-14

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07C215/10 ,  C07C217/58 ,  C07C217/74

CPC分类号： C07C215/10 ,  C07C217/58 ,  C07C217/74 ,  C07C2103/24 ,  C07C2103/26 ,  C07C2103/40 ,  C07C2103/42 ,  C07C2103/48 ,  C07C2103/50

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carboxylic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）化合物，其中ArCH 2 R 1（I）或其单甲醚或单乙醚（包括这些醚的式（I）化合物总共可含不多于30个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是含有3或4个芳环的C 15-18稠合四环环体系或含有4或5个芳环的C 17-22稠合五碳环体系或其取代衍生物; 环系统Ar应该是平面的或仅偏离平面度。 因此，环系统最多含有两个非芳族碳原子，它们可以在相同的环中，在这种情况下它们相邻或在不同的环中; Ar不是苝，荧蒽，芘，芘或三亚苯; R1含有不多于8个碳原子，并且是一个基团，其中m是0或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-5烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; 五元或六元饱和羧酸环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。

公开(公告)号：US5075455A

公开(公告)日：1991-12-24

申请号：US401643

申请日：1989-08-29

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07D219/14 ,  C07D307/77 ,  C07D333/50

CPC分类号： C07D307/77 ,  C07D219/14 ,  C07D333/50

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tricyclic aromatic ring system containing a maximum of 14 ring atoms and at least one heteroatom or a fused pentacyclic ring system with at least 4 aromatic rings containing a maximum of 22 ring atoms and at least one heteroatom; or a substituted derivative thereof; for either the tricyclic or pentacyclic ring system there is a maximum of one heteroatom for each ring present but preferably only one or two of the rings contain a heteroatom; the rings forming the tricyclic or the pentacyclic ring system contain five or six atoms; the heteroatoms are conveniently nitrogen, phosphorus, oxygen, sulfur or selenium; suitably the heteroatom is oxygen, sulfur or nitrogen; the tricyclic or the pentacyclic ring system should be planar or deviate only slightly from planarity; suitably the ring system is aromatic or contains one non-aromatic ring; preferably the ring system is aromatic; nitrogen atoms contained in five-membered rings are substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

公开(公告)号：US4918101A

公开(公告)日：1990-04-17

申请号：US234252

申请日：1988-08-19

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07D209/80 ,  C07D307/77 ,  C07D333/50

CPC分类号： C07D209/80 ,  C07D307/77 ,  C07D333/50 ,  Y10S514/908

摘要： The present invention relates to antitumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is O or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）的抗肿瘤化合物，其中ArCH2R1（Ⅰ）或其单甲醚或单乙醚（包括这些醚的式（I）化合物总共可含不多于29个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是由5元和6元环组成并且含有至少一个杂原子和3个芳环和总共不超过18个环原子的稠合四环芳族环系统或其取代的衍生物; 杂原子优选为氧，硫或氮; 当它是氮时，它被氢，甲基或乙基取代; R1含有不多于8个碳原子，并且是基团，其中m是O或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-5烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; -C-C-是五或六元饱和碳环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。

公开(公告)号：US4910218A

公开(公告)日：1990-03-20

申请号：US49282

申请日：1987-05-12

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07D221/18 ,  C07D307/77 ,  C07D333/50

CPC分类号： C07D307/77 ,  C07D221/18 ,  C07D333/50 ,  Y10S514/908

摘要： The present invention relates to anti tumor compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tetracyclic aromatic ring system comprised of 5-membered and 6-membered rings and contains at least one heteroatom and 3 aromatic rings and a total of no more than 18 ring atoms, or a substituted derivative thereof; the heteroatom is preferably oxygen, sulfur or nitrogen; when it is nitrogen this is substituted by hydrogen, methyl or ethyl; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）的抗肿瘤化合物，其中ArCH2R1（Ⅰ）或其单甲醚或单乙醚（包括这些醚的式（Ⅰ）化合物总共不超过29个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是由5元和6元环组成并且含有至少一个杂原子和3个芳环和总共不超过18个环原子的稠合四环芳族环系统或其取代的衍生物; 杂原子优选为氧，硫或氮; 当它是氮时，它被氢，甲基或乙基取代; R1含有不多于8个碳原子，并且是一个基团，其中m是0或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-5烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; 是一个五或六元饱和碳环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。

公开(公告)号：US4866070A

公开(公告)日：1989-09-12

申请号：US132724

申请日：1987-12-11

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07D219/14 ,  C07D307/77 ,  C07D333/50

CPC分类号： C07D307/77 ,  C07D219/14 ,  C07D333/50

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 29 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fused tricyclic aromatic ring system containing a maximum of 14 ring atoms and at least one heteroatom or a fused pentacyclic ring system with at least 4 aromatic rings containing a maximum of 22 ring atoms and at least one heteroatom; or a substituted derivative thereof; for either the tricyclic or pentacyclic ring system there is a maximum of one heteroatom for each ring present but preferably only one or two of the rings contain a heteroatom; the rings forming the tricyclic or the pentacyclic ring system contain five or six atoms; the heteroatoms are conveniently nitrogen, phosphorus, oxygen, sulfur or selenium; suitably the heteroatom is oxygen, sulfur or nitrogen; the tricyclic or the pentacyclic ring system should be planar or deviate only slightly from planarity; suitably the ring system is aromatic or contains one non-aromatic ring; preferably the ring system is aromatic; nitrogen atoms contained in five-membered rings are substituted by hydrogen, methyl or ethyl.

摘要翻译： 本发明涉及式（I）化合物，其中ArCH 2 R 1（I）或其单甲醚或单乙醚（包括这些醚的式（I）化合物总共可以不超过29个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是含有最多14个环原子和至少一个杂原子或稠合五环体系的稠合三环芳环体系，其具有至少4个含有最多22个环原子和至少一个杂原子的芳环; 或其取代的衍生物; 对于三环或五环系统，存在每个环最多有一个杂原子，但优选只有一个或两个环含有杂原子; 形成三环或五环系的环含有五个或六个原子; 杂原子方便地是氮，磷，氧，硫或硒; 适当地，杂原子是氧，硫或氮; 三环或五环系统应平面或偏离平面度; 适当地，环系是芳族的或含有一个非芳香环; 优选环系是芳族的; 五元环中含有的氮原子被氢，甲基或乙基取代。

公开(公告)号：US4810823A

公开(公告)日：1989-03-07

申请号：US136094

申请日：1987-12-21

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07C87/28

CPC分类号： Y10S514/908

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

公开(公告)号：US4810727A

公开(公告)日：1989-03-07

申请号：US83238

申请日：1987-08-06

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： A61K31/135 ,  C07C93/00

CPC分类号： A61K31/135 ,  C07C2103/48

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a chrysene or substituted chrysene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）化合物，其中ArCH 2 R 1（I）或其单甲醚或单乙醚（包括这些醚的式（I）化合物总共可含有不超过30个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是一个或多个取代的环烯系; R1含有不多于8个碳原子，并且是一个基团，其中m是0或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-3烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; -C-C-是五或六元饱和碳环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。

公开(公告)号：US4808753A

公开(公告)日：1989-02-28

申请号：US146221

申请日：1988-01-20

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07C87/28

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters, thereof; acid addition salts thereof; wherein Ar is a C.sub.15-18 fused tetracarbocyclic ring system containing 3 or 4 aromatic rings or a C.sub.17-22 fused pentacarbocyclic ring system containing 4, or 5 aromatic rings, or a substituted derivative thereof; the ring system Ar should be planar or deviate only slightly from planarity. Thus, the ring system contains a maximum of two non-aromatic carbon atoms which may be in the same ring, in which case they are adjacent, or in different rings;Ar is not perylene, fluoranthene, chrysene, pyrene, or triphenylene;R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1;R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-5 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl;--C--C-- is a five- or six-membered saturated carbocyclic ring;R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）化合物，其中ArCH 2 R 1（I）或其单甲醚或单乙醚（包括这些醚的式（I）化合物总共可含不多于30个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是含有3或4个芳环的C 15-18稠合四环环体系或含有4或5个芳环的C 17-22稠合五碳环体系或其取代衍生物; 环系统Ar应该是平面的或仅偏离平面度。 因此，环系统最多含有两个非芳族碳原子，它们可以在相同的环中，在这种情况下它们相邻或在不同的环中; Ar不是苝，荧蒽，芘，芘或三亚苯; R1含有不多于8个碳原子，并且是一个基团，其中m是0或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-5烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; -C-C-是五或六元饱和碳环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。

公开(公告)号：US4808632A

公开(公告)日：1989-02-28

申请号：US79352

申请日：1987-07-30

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07C215/10

CPC分类号： C07C215/10 ,  C07C2103/14 ,  C07C2103/24 ,  C07C2103/26 ,  C07C2103/40 ,  C07C2103/48 ,  C07C2103/50 ,  Y10S514/908

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monomethyl or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a fluoranthene or substituted fluoranthene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five- or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）化合物，其中ArCH 2 R 1（I）或其单甲醚或单乙醚（包括这些醚的式（I）化合物总共可含有不超过30个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是荧蒽或取代的荧蒽环体系; R1含有不多于8个碳原子，并且是一个基团，其中m是0或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-3烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; 一个五元或六元饱和碳环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。

公开(公告)号：US4808625A

公开(公告)日：1989-02-28

申请号：US090578

申请日：1987-08-28

申请人： Kenneth W. Bair

发明人： Kenneth W. Bair

IPC分类号： C07C205/15 ,  C07D263/52 ,  C07D263/62 ,  C07D263/64 ,  C07D309/12 ,  C07D319/06 ,  C07D498/04 ,  C07D521/00 ,  A61K31/135 ,  C07C87/64 ,  C07C93/00

CPC分类号： C07D263/52 ,  C07C205/15 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D263/64 ,  C07D309/12 ,  C07D319/06 ,  C07C2103/24 ,  C07C2103/26 ,  C07C2103/48 ,  C07C2103/50

摘要： The present invention relates to compounds of formula (I)ArCH.sub.2 R.sup.1 (I)or a monoethyl ether thereof (the compound of formula (I) including these ethers may contain no more than 30 carbon atoms in total); ethers, esters thereof; acid addition salts thereof; wherein Ar is a phenanthrene or substituted phenanthrene ring system; R.sup.1 contains not more than eight carbon atoms and is a group ##STR1## wherein m is 0 or 1; R.sup.5 is hydrogen;R.sup.6 and R.sup.7 are the same or different and each is hydrogen or C.sub.1-3 alkyl optionally substituted by hydroxy;R.sup.8 and R.sup.9 are the same or different and each is hydrogen or C.sub.1-3 alkyl; ##STR2## is a five-or six-membered saturated carbocyclic ring; R.sup.10 is hydrogen, methyl or hydroxymethyl;R.sup.11, R.sup.12 and R.sup.13 are the same or different and each is hydrogen or methyl;R.sup.14 is hydrogen, methyl, hydroxy, or hydroxymethyl.

摘要翻译： 本发明涉及式（I）化合物，其中ArCH 2 R 1（I）或其单乙醚（包括这些醚的式（I）化合物总共可含有不超过30个碳原子）; 醚，酯; 其酸加成盐; 其中Ar是菲或取代的菲环体系; R1含有不多于8个碳原子，并且是一个基团，其中m是0或1; R5是氢; R6和R7相同或不同，各自为氢或任选被羟基取代的C 1-3烷基; R 8和R 9相同或不同，各自为氢或C 1-3烷基; 是一个五元或六元饱和碳环; R 10是氢，甲基或羟甲基; R11，R12和R13相同或不同，各自为氢或甲基; R14是氢，甲基，羟基或羟甲基。