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公开(公告)号：US20100222380A1
公开(公告)日：2010-09-02
申请号：US12777212
申请日：2010-05-10
申请人： Seth D. Rose , Rosemarie F. Hartman
发明人： Seth D. Rose , Rosemarie F. Hartman
IPC分类号： A61K31/47 , C07C69/587 , A61K31/265 , C12N5/02 , A61P35/00 , A61P35/02 , C07D307/42 , A61K31/341 , C07D333/22 , A61K31/381 , C07D213/50 , A61K31/4409 , C07D215/14
CPC分类号： C07C69/653 , C07C327/32 , C07D209/12 , C07D213/50 , C07D231/12 , C07D307/46 , C07D311/28
摘要： Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN-COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.
摘要翻译： 公开了包含改性查耳酮或改性查耳酮衍生物的抗微生物剂。 改性查耳酮或改性查耳酮衍生物化合物具有通式CHAL-LIN-COV，其中CHAL是查耳酮或查耳酮衍生物部分，LIN是任选的接头部分，COV是共价结合部分（例如，α，bgr ; - 不饱和巯基酯基）。 改性查耳酮或改性查耳酮衍生物化合物提供了一种改进的干扰微管蛋白聚合的方法，例如通过微管蛋白与共价结合部分之间的共价（且基本上不可逆）的结合，潜在地导致肿瘤大小和/或消失的降低 癌症，有利于癌症患者。
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2.发明申请公开(公告)号：US20080113919A1
公开(公告)日：2008-05-15
申请号：US11941914
申请日：2007-11-16
IPC分类号： A61K38/06 , A61K38/05 , A61K38/04 , A61K31/165 , A61K31/24
CPC分类号： C07C311/46 , C07C45/30 , C07C45/62 , C07C205/03 , C07C205/04 , C07C205/14 , C07C205/40 , C07C211/52 , C07C47/21
摘要： Conjugated nitro alkene compounds hamper or prevent proliferation of cancer cells in cell culture and in cancer patients, which can result in a decrease in tumor size and/or disappearance of the cancer. The compounds may act by interference with cancer cell biochemistry, in which isoprenoid groups such as farnesyl and geranylgeranyl become bonded to various oncogenic proteins such as Ras, RhoA, RhoB, or some other growth-related cellular protein(s).
摘要翻译： 共轭硝基烯化合物妨碍或预防细胞培养和癌症患者中癌细胞的增殖，这可能导致肿瘤大小和/或癌症消失。 这些化合物可以通过干扰癌细胞生物化学而起作用，其中类异戊二烯基如法呢基和香叶基香叶基结合成各种致癌蛋白如Ras，RhoA，RhoB或一些其它生长相关的细胞蛋白。
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公开(公告)号：US07344851B2
公开(公告)日：2008-03-18
申请号：US11246259
申请日：2005-10-11
申请人： Seth D. Rose , Steven R. Ottersberg , Karl J. Okolotowicz , Dale E. Robinson , Rosemarie F. Hartman , Scott Lefler
发明人： Seth D. Rose , Steven R. Ottersberg , Karl J. Okolotowicz , Dale E. Robinson , Rosemarie F. Hartman , Scott Lefler
IPC分类号： C12Q1/48
CPC分类号： C12Q1/48 , A61K31/12 , A61K31/121 , A61K31/195 , C12N9/1085 , C12N9/99 , C12Y205/01029 , G01N2500/04
摘要： Prenylating enzymes are involved in modifying oncoproteins, such as RAS, so that growth of neoplastic cells becomes uncontrolled. Inactivation of such enzymes can prevent uncontrolled growth. α-Dicarbonyl compounds can be used to covalently modify and thereby inactivate prenylating enzymes such as protein farnesyltransferase and protein geranylgeranyltransferase. The compounds can be designed to enhance affinity and/or specificity for a particular protein substrate.
摘要翻译： 过氧化酶参与修饰癌蛋白，如RAS，使肿瘤细胞的生长变得不受控制。 这种酶的失活可以防止不受控制的生长。 α-二羰基化合物可用于共价修饰，从而使预活化酶失活，如蛋白法呢基转移酶和蛋白质香叶基香叶基转移酶。 化合物可被设计成增强特定蛋白质底物的亲和性和/或特异性。
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4.发明授权公开(公告)号：US07312191B2
公开(公告)日：2007-12-25
申请号：US10901082
申请日：2004-07-29
IPC分类号： A61K38/00 , C07C201/00 , C07D207/08
CPC分类号： C07C311/46 , C07C45/30 , C07C45/62 , C07C205/03 , C07C205/04 , C07C205/14 , C07C205/40 , C07C211/52 , C07C47/21
摘要： Conjugated nitro alkene compounds hamper or prevent proliferation of cancer cells in cell culture and in cancer patients, which can result in a decrease in tumor size and/or disappearance of the cancer. The compounds may act by interference with cancer cell biochemistry, in which isoprenoid groups such as farnesyl and geranylgeranyl become bonded to various oncogenic proteins such as Ras, RhoA, RhoB, or some other growth-related cellular protein(s).
摘要翻译： 共轭硝基烯化合物妨碍或预防细胞培养和癌症患者中癌细胞的增殖，这可能导致肿瘤大小和/或癌症消失。 这些化合物可以通过干扰癌细胞生物化学而起作用，其中类异戊二烯基如法呢基和香叶基香叶基结合成各种致癌蛋白如Ras，RhoA，RhoB或一些其它生长相关的细胞蛋白。
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公开(公告)号：US20070265317A1
公开(公告)日：2007-11-15
申请号：US11744027
申请日：2007-05-03
申请人： Seth D. ROSE , Rosemarie F. HARTMAN
发明人： Seth D. ROSE , Rosemarie F. HARTMAN
IPC分类号： A61K31/44 , A61K31/405 , C07D307/02 , C07D209/42 , A61K31/34
CPC分类号： C07C69/653 , C07C327/32 , C07D209/12 , C07D213/50 , C07D231/12 , C07D307/46 , C07D311/28
摘要： Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.
摘要翻译： 公开了包含改性查耳酮或改性查耳酮衍生物的抗微生物剂。 改性查耳酮或改性查耳酮衍生物化合物具有通式CHAL-LIN-COV，其中CHAL是查耳酮或查耳酮衍生物部分，LIN是任选的接头部分，COV是共价结合部分（例如α，β - 不饱和巯基酯基）。 改性查耳酮或改性查耳酮衍生物化合物提供了一种改进的干扰微管蛋白聚合的方法，例如通过微管蛋白与共价结合部分之间的共价（且基本上不可逆）的结合，潜在地导致肿瘤大小和/或消失的降低 癌症，有利于癌症患者。
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公开(公告)号：US07714025B2
公开(公告)日：2010-05-11
申请号：US11744027
申请日：2007-05-03
申请人： Seth D. Rose , Rosemarie F. Hartman
发明人： Seth D. Rose , Rosemarie F. Hartman
IPC分类号： A61K31/16 , C07D231/10 , C07C49/00
CPC分类号： C07C69/653 , C07C327/32 , C07D209/12 , C07D213/50 , C07D231/12 , C07D307/46 , C07D311/28
摘要： Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN—COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.
摘要翻译： 公开了包含改性查耳酮或改性查耳酮衍生物的抗微生物剂。 改性查耳酮或改性查耳酮衍生物化合物具有通式CHAL-LIN-COV，其中CHAL是查耳酮或查耳酮衍生物部分，LIN是任选的接头部分，COV是共价结合部分（例如，α，bgr ; - 不饱和巯基酯基）。 改性查耳酮或改性查耳酮衍生物化合物提供了一种改进的干扰微管蛋白聚合的方法，例如通过微管蛋白与共价结合部分之间的共价（且基本上不可逆）的结合，潜在地导致肿瘤大小和/或消失的降低 癌症，有利于癌症患者。
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公开(公告)号：US07423170B2
公开(公告)日：2008-09-09
申请号：US11275662
申请日：2006-01-23
申请人： Seth D. Rose , Scott R. Lefler , Steven R. Ottersberg , Ann Y. Kim , Karl J. Okolotowicz , Rosemarie F. Hartman
发明人： Seth D. Rose , Scott R. Lefler , Steven R. Ottersberg , Ann Y. Kim , Karl J. Okolotowicz , Rosemarie F. Hartman
IPC分类号： C07C69/007 , C07C69/017 , A01N57/14 , A01N41/04 , A01N41/10
CPC分类号： A61K31/66 , A61K31/20 , C07C69/63 , C07C217/46 , C07C219/20 , C07D303/32 , C07D303/48 , C07F9/091
摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.
摘要翻译： 已知当诸如Ras和RhoB的癌蛋白定位在癌细胞膜的内表面时，诸如Ras和RhoB的癌蛋白以无限制的方式诱导细胞分裂。 定位通过异戊烯化反应进行，由此在酶（例如法呢基蛋白转移酶）的存在下将疏水基团（例如法呢基）连接到蛋白质上。 因此，通过共价修饰来停用异戊烯基化酶可最终导致癌细胞生长的缓解和/或停止。 具有与异戊烯基化酶共价或基本上不可逆地键合的必需结构基团的各种异戊二烯基化抑制剂包括与疏水性底物模拟基团键合的羰基或硫代羰基化合物（或这些化合物的掩蔽型）和α氧代环氧化物。 羰基或硫代羰基化合物还含有核原子或基团以增强形成共价键的倾向。
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8.发明授权公开(公告)号：US07977315B2
公开(公告)日：2011-07-12
申请号：US11941914
申请日：2007-11-16
CPC分类号： C07C311/46 , C07C45/30 , C07C45/62 , C07C205/03 , C07C205/04 , C07C205/14 , C07C205/40 , C07C211/52 , C07C47/21
摘要： Conjugated nitro alkene compounds hamper or prevent proliferation of cancer cells in cell culture and in cancer patients, which can result in a decrease in tumor size and/or disappearance of the cancer. The compounds may act by interference with cancer cell biochemistry, in which isoprenoid groups such as farnesyl and geranylgeranyl become bonded to various oncogenic proteins such as Ras, RhoA, RhoB, or some other growth-related cellular protein(s).
摘要翻译： 共轭硝基烯化合物妨碍或预防细胞培养和癌症患者中癌细胞的增殖，这可能导致肿瘤大小和/或癌症消失。 这些化合物可以通过干扰癌细胞生物化学而起作用，其中类异戊二烯基如法呢基和香叶基香叶基结合成各种致癌蛋白如Ras，RhoA，RhoB或一些其它生长相关的细胞蛋白。
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公开(公告)号：US07019031B2
公开(公告)日：2006-03-28
申请号：US09983232
申请日：2001-10-23
申请人： Seth D. Rose , Scott R. Lefler , Steven R. Ottersberg , Ann Y. Kim , Karl J. Okolotowicz , Rosemarie F. Hartman
发明人： Seth D. Rose , Scott R. Lefler , Steven R. Ottersberg , Ann Y. Kim , Karl J. Okolotowicz , Rosemarie F. Hartman
CPC分类号： A61K31/66 , A61K31/20 , C07C69/63 , C07C217/46 , C07C219/20 , C07D303/32 , C07D303/48 , C07F9/091
摘要： Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. a farnesyl group) is attached to the protein in the presence of an enzyme (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.
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公开(公告)号：US08552066B2
公开(公告)日：2013-10-08
申请号：US12777212
申请日：2010-05-10
申请人： Seth D. Rose , Rosemarie F. Hartman
发明人： Seth D. Rose , Rosemarie F. Hartman
IPC分类号： A61K31/16 , C07D233/70 , C07D319/00
CPC分类号： C07C69/653 , C07C327/32 , C07D209/12 , C07D213/50 , C07D231/12 , C07D307/46 , C07D311/28
摘要： Antimitotic agents comprising a modified chalcone or modified chalcone derivative are disclosed. The modified chalcone or modified chalcone derivative compounds are of the general formula CHAL-LIN-COV, wherein CHAL is a chalcone or chalcone derivative portion, LIN is an optional linker portion, and COV is a covalent bonding portion (e.g., an α,β-unsaturated thiol ester group). The modified chalcone or modified chalcone derivative compounds provide an improved method of interference with tubulin polymerization, for example by covalent (and essentially irreversible) bonding between tubulin and the covalent bonding portion, potentially resulting in a decrease in tumor size and/or disappearance of the cancer, to the benefit of cancer patients.
摘要翻译： 公开了包含改性查耳酮或改性查耳酮衍生物的抗微生物剂。 改性查耳酮或改性查耳酮衍生物化合物具有通式CHAL-LIN-COV，其中CHAL是查耳酮或查耳酮衍生物部分，LIN是任选的接头部分，COV是共价结合部分（例如α，β - 不饱和巯基酯基）。 改性查耳酮或改性查耳酮衍生物化合物提供了一种改进的干扰微管蛋白聚合的方法，例如通过微管蛋白与共价结合部分之间的共价（且基本上不可逆）的结合，潜在地导致肿瘤大小和/或消失的降低 癌症，有利于癌症患者。
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