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1. 发明授权

US08815213B2 RGD-(bacterio)chlorophyll conjugates for photodynamic therapy and Imaging of Necrotic tumors 有权
标题翻译： RGD-（细菌）叶绿素共轭物用于光动力学治疗和坏死肿瘤成像
公开(公告)号：US08815213B2
公开(公告)日：2014-08-26
申请号：US12920088
申请日：2009-03-01
申请人： Avigdor Scherz , Liat Goldshaid , Yoram Salomon
发明人： Avigdor Scherz , Liat Goldshaid , Yoram Salomon
IPC分类号： A61B5/055 , A61K51/04 , A61K41/00 , C07D257/04
CPC分类号： A61K51/0485 , A61K41/0057 , A61K41/0071 , A61K49/0036 , A61K49/0056 , A61K49/085 , A61K49/14 , A61K51/044 , A61K51/0446 , A61K51/0451 , A61K51/082 , A61K51/088 , C07D257/04
摘要： RGD-chlorophyll and RGD-bacteriochlorophyll conjugates that home and accumulate in necrotic tumor domains much longer than in tumor non-necrotic domains are provided for use in minimally invasive tumor-targeted imaging, tumor-targeted photodynamic therapy, and/or on-line prognosis of necrotic tumors.
摘要翻译：家庭和积累在坏死肿瘤域中的RGD-叶绿素和RGD-细菌叶绿素缀合物比在肿瘤非坏死区域中长得多的时间被提供用于微创肿瘤靶向成像，肿瘤靶向光动力学治疗和/或在线预后的坏死性肿瘤。

2. 发明授权

US08461142B2 Water-soluble anionic bacteriochlorophyll derivatives and their uses 有权
标题翻译：水溶性阴离子细菌叶绿素衍生物及其用途
公开(公告)号：US08461142B2
公开(公告)日：2013-06-11
申请号：US12942938
申请日：2010-11-09
申请人： Avigdor Scherz , Alexander Brandis , Ohad Mazor , Yoram Salomon , Hugo Scheer
发明人： Avigdor Scherz , Alexander Brandis , Ohad Mazor , Yoram Salomon , Hugo Scheer
IPC分类号： A01N55/02 , A61K31/40 , C07D487/02 , A61B5/00
CPC分类号： A61N5/062 , A61F9/0008 , A61K31/40 , A61K41/0071 , A61K41/0076 , A61K49/0036 , A61N5/0624 , C07F1/08 , C07F3/02 , C07F3/06 , C07F13/005 , C07F15/006 , C07F15/0066 , C07F15/045
摘要： The invention provides anionic water-soluble tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one, preferably two or three, negatively charged groups and/or acidic groups that are converted to negatively charged groups at the physiological pH, preferably Bchls having a group COO , COS , SO3 , PO3 , COOH, COSH, SO3H, and/or PO3H2 bound through an ester or amide bond to one or more of the positions 17 , 13 , and 3 of the tetracyclic or pentacyclic Bchl molecule, for photodynamic therapy and diagnosis.
摘要翻译：本发明提供阴离子水溶性四环和五环类细菌叶绿素衍生物（Bchls），其含有至少一个，优选两个或三个带负电荷的基团和/或酸性基团，其在生理pH下转化为带负电荷的基团，优选具有基团的Bchls CO 3，SO 3 - ，SO 3 - ，PO 3 2-，COOH，COSH，SO 3 H和/或PO 3 H 2，其通过酯或酰胺键与一个或多个位置17 3， 13 3和3 2的四环或五环Bchl分子，用于光动力学治疗和诊断。

3. 发明授权

US07169753B2 Chlorophyll and bacteriochlorophyll esters, their preparation and pharmaceutical compositions comprising them 失效
标题翻译：叶绿素和细菌叶绿素酯，它们的制备和包含它们的药物组合物
公开(公告)号：US07169753B2
公开(公告)日：2007-01-30
申请号：US10148552
申请日：2000-12-01
申请人： Hugo Scheer , Nina Kammhuber , Avigdor Scherz , Alexander Brandis , Yoram Salomon
发明人： Hugo Scheer , Nina Kammhuber , Avigdor Scherz , Alexander Brandis , Yoram Salomon
IPC分类号： A61K38/00
CPC分类号： C07D487/22 , A61K41/0019 , A61K41/0071 , C07H13/04 , C07H13/10
摘要： Novel C-132-COXR1, C-172-COXR2 and C-132-COXR1, C-172-COXR1 derivatives of chlorophyll and bacteriochlorophyll compounds are provided wherein X is O, S or N and R1 and R2, the same or different, may be an optionally substituted hydrocarbyl, amino acid, peptide, protein or saccharide radical. The compounds are for use in photodynamic therapy (PDT), for diagnosis of tumors, and for killing cells and infectious agents such as bacteria and virus, both in biological products and in living tissues.
摘要翻译：新型C-13 2 -COXR 1，C-17 2 -COXR 2和C-13 SUP 提供了叶绿素和细菌叶绿素化合物的2个-COXR 1，C-17 2 -XX 1 H 1 N衍生物，其中X是O ，S或N和R 1和R 2相同或不同，可以是任选取代的烃基，氨基酸，肽，蛋白质或糖基。该化合物用于光动力学治疗（PDT），用于诊断肿瘤，以及用于杀死生物制品和活组织中的细胞和感染因子如细菌和病毒。

4. 发明授权

US06569846B1 Palladium-substituted bacteriochlorophyll derivatives and use thereof 有权
标题翻译：钯取代的细菌叶绿素衍生物及其用途
公开(公告)号：US06569846B1
公开(公告)日：2003-05-27
申请号：US09857772
申请日：2001-09-18
申请人： Avigdor Scherz , Yoram Salomon , Alexander Brandis , Hugo Scheer
发明人： Avigdor Scherz , Yoram Salomon , Alexander Brandis , Hugo Scheer
IPC分类号： A61K31555
CPC分类号： C07D487/22 , A61K41/0071 , C07D491/22
摘要： Palladium-substituted Bacteriochlorophyll derivatives of formula (I), wherein A represents OH, OR1, —O—(CH2)n—Y, —S—(CH2)n—Y, —NH—(CH2)n—Y, —O—(CH2)2—NH2, —O—(CH2)2—OH, —NH—(CH2)n—+N o, X—, —NH0(CH2)2—NH═BOC or —N—(CH2—CH═CH2)2; wherein R1 represents Na+, K+, (Ca2+)0, 5, (Mg2+)0, 5, Li+, NH4+, NH3—C(CH2OH)3 +NH3—CH2—(CHOH)4—CH2OH, +NH2(CH3)—CH2—(CHOH)4—CH2OH or +N(CN′H2n′+1)4; R2 represents H, OH or COOR4, wherein R4 is C1-C12 alkyl or C3-C12 cycloalkl; R3 represents H, OH or C1-C12 alkyl or alkoxy; n is 1, 2, 3, 4, 5 or 6, Y is —NR′1R′2R′3, X-wherein R′1, R′2 and R′3 independently from each other represent —CH3 or —C2H5; X is F, Cl, Br or 1, n′ is 1, 2, 3 or 4 and their oxidized forms, are useful in the field of photodynamic therapy (PDT).
摘要翻译：式（I）的钯取代的细菌叶绿素衍生物，其中A表示OH，OR1，-O-（CH2）nY，-S-（CH2）nY，-NH-（CH2）nY，-O-（CH2）2- NH 2，-O-（CH 2）2 -OH，-NH-（CH 2）n + N o，X-，-NHO（CH 2）2 -NH = BOC或-N-（CH 2 -CH = CH 2）其中R1表示Na +，K +，（Ca2 +）0,5（Mg2 +）0,5，Li +，NH4 +，NH3-C（CH2OH）3 + NH3-CH2-（CHOH）4-CH2OH，+ NH2（CH3） CH2-（CHOH）4-CH2OH或+ N（CN'H2n'+ 1）4; R2代表H，OH或COOR4，其中R4是C1-C12烷基或C3-C12环烷基; R3表示H，OH或C1-C12烷基或烷氧基; n是1,2,3,4,5或6，Y是-NR'1R'2R'3，X-其中R'1，R'2和R'3彼此独立地表示-CH3或-C2H5; X是F，Cl，Br或1，n'是1,2,3或4，它们的氧化形式是用途

5. 发明授权

US5955585A Catalytic condensation method for the preparation of chlorophyll and bacteriochlorophyll derivatives 失效
标题翻译：用于制备叶绿素和细菌叶绿素衍生物的催化缩合方法
公开(公告)号：US5955585A
公开(公告)日：1999-09-21
申请号：US461243
申请日：1995-06-05
申请人： Avigdor Scherz , Yoram Salomon , Leszek Fiedor
发明人： Avigdor Scherz , Yoram Salomon , Leszek Fiedor
IPC分类号： A61K31/555 , A61K38/00 , A61K38/22 , A61K39/395 , A61K41/00 , A61K47/48 , A61K49/00 , A61N5/06 , A61P35/00 , A61P43/00 , C07D487/22 , C07K1/113 , C07K5/023 , C07K14/575 , C07K14/685 , C07K14/795 , C07K16/00 , C12N9/18 , C12P17/18 , G01N33/50 , G01N33/574 , C07K17/06
CPC分类号： A61K49/0036 , A61K41/0071 , A61K47/48246 , A61K47/48384 , A61K47/48569 , A61K49/00 , A61K49/0052 , A61K49/0056 , C07K14/685 , C07K14/795 , C12N9/18 , C12P17/182
摘要： Conjugates of chlorophyll (Chl) and bacteriochlorophyll (Bchl) derivatives with amino acids, peptides and proteins are provided by the invention. The amino acid, peptide or protein residue is linked to the 17-propionic acid group of a Chl or Bchl residue directly or through a chain. The conjugates are for use as photosensitizers in photodynamic therapy and in diagnostics of tumors. Conjugation with cell-specific ligands, such as hormones, growth factors or tumor-specific antibodies, will target the Chl or Bchl moiety to the tumor site. Thus, conjugates with melanocyte stimulating hormones are suitable for photodynamic therapy of melanoma tumors.
摘要翻译：本发明提供了具有氨基酸，肽和蛋白质的叶绿素（Chl）和细菌叶绿素（Bchl）衍生物的缀合物。氨基酸，肽或蛋白质残基直接或通过链连接到Chl或Bchl残基的17-丙酸基团。该缀合物用作光动力疗法和肿瘤诊断中的光敏剂。与细胞特异性配体如激素，生长因子或肿瘤特异性抗体的缀合将靶向Chl或Bchl部分到肿瘤部位。因此，与黑素细胞刺激激素的缀合物适用于黑素瘤肿瘤的光动力学治疗。

6. 发明授权

US5650292A Chlorophyll and bacteriochlorophyll derivatives, their preparation and pharmaceutical compositions comprising them 失效
标题翻译：叶绿素和细菌叶绿素衍生物，它们的制备和包含它们的药物组合物
公开(公告)号：US5650292A
公开(公告)日：1997-07-22
申请号：US463950
申请日：1995-07-31
申请人： Avigdor Scherz , Yoram Salomon , Leszek Fiedor
发明人： Avigdor Scherz , Yoram Salomon , Leszek Fiedor
IPC分类号： A61K31/555 , A61K38/00 , A61K38/22 , A61K39/395 , A61K41/00 , A61K47/48 , A61K49/00 , A61N5/06 , A61P35/00 , A61P43/00 , C07D487/22 , C07K1/113 , C07K5/023 , C07K14/575 , C07K14/685 , C07K14/795 , C07K16/00 , C12N9/18 , C12P17/18 , G01N33/50 , G01N33/574 , C12P21/00 , C12P13/04
CPC分类号： A61K49/0036 , A61K41/0071 , A61K47/48246 , A61K47/48384 , A61K47/48569 , A61K49/00 , A61K49/0052 , A61K49/0056 , C07K14/685 , C07K14/795 , C12N9/18 , C12P17/182
摘要： Conjugates of chlorophyll (Chl) and bacteriochlorophyll (Bchl) derivatives with amino acids, peptides and proteins are provided by the invention. The amino acid, peptide or protein residue is linked to the 17-propionic acid group of a Chl or Bchl residue directly or through a chain. The conjugates are for use as photosensitizers in photodynamic therapy and in diagnostics of tumors. Conjugation with cell-specific ligands, such as hormones, growth factors or tumor-specific antibodies, will target the Chl or Bchl moiety to the tumor site. Thus, conjugates with melanocyte stimulating hormones are suitable for photodynamic therapy of melanoma tumors.
摘要翻译：本发明提供了具有氨基酸，肽和蛋白质的叶绿素（Chl）和细菌叶绿素（Bchl）衍生物的缀合物。氨基酸，肽或蛋白质残基直接或通过链连接到Chl或Bchl残基的17-丙酸基团。该缀合物用作光动力疗法和肿瘤诊断中的光敏剂。与细胞特异性配体如激素，生长因子或肿瘤特异性抗体的缀合将靶向Chl或Bchl部分到肿瘤部位。因此，与黑素细胞刺激激素的缀合物适用于黑素瘤肿瘤的光动力学治疗。

7. 发明申请

US20120294801A1 CONJUGATES OF RGD PEPTIDES AND PORPHYRIN OR (BACTERIO)CHLOROPHYLL PHOTOSYNTHESIZERS AND THEIR USES 有权
标题翻译： RGD肽和PORPHYRIN或（BACTERIO）氯代乙酰基光合酶及其用途的结合
公开(公告)号：US20120294801A1
公开(公告)日：2012-11-22
申请号：US13447825
申请日：2012-04-16
申请人： Avigdor Scherz , Yoram Salomon , Efrat Rubinstein , Alexander Brandis , Doron Eren , Karin Neimann
发明人： Avigdor Scherz , Yoram Salomon , Efrat Rubinstein , Alexander Brandis , Doron Eren , Karin Neimann
IPC分类号： C07K4/00 , C07K7/64 , C07K7/06 , C07K14/47 , A61K38/03 , A61K38/12 , A61K38/08 , A61K38/17 , C07F15/00 , A61K31/555 , A61K49/00 , A61K51/08 , A61K49/14 , A61P35/00 , A61P35/04 , A61B5/055 , A61B6/00 , A61M37/00 , C07K2/00
CPC分类号： C07K5/123 , A61K41/00 , A61K41/0071 , A61K47/64 , A61K51/082 , A61K51/088 , C07K5/0817 , C07K5/10 , C07K5/126 , C07K7/06 , C07K7/64 , G01N33/57426 , G01N2333/96411
摘要： Conjugates of porphyrin, chlorophyll and bacteriochlorophyll photosensitizers with RGD-containing peptides or RGD peptidomimetics are provided that are useful for photodynamic therapy (PDT), particularly vascular-targeted PDT (VTP), of tumors and nonneoplastic vascular diseases such as age-related macular degeneration, and for diagnosis of tumors by different techniques.
摘要翻译：提供了含有RGD的肽或RGD肽模拟物的卟啉，叶绿素和细菌叶绿素光敏剂的缀合物，其可用于光动力学治疗（PDT），特别是血管靶向PDT（VTP），肿瘤和非肿瘤性血管疾病如年龄相关性黄斑变性，并通过不同的技术诊断肿瘤。

8. 发明申请

US20110064658A1 RGD-(bacterio)chlorophyll conjugates for photodynamic therapy and Imaging of Necrotic tumors 有权
标题翻译： RGD-（细菌）叶绿素共轭物用于光动力学治疗和坏死肿瘤成像
公开(公告)号：US20110064658A1
公开(公告)日：2011-03-17
申请号：US12920088
申请日：2009-03-01
申请人： Avigdor Scherz , Liat Goldshaid , Yoram Salomon
发明人： Avigdor Scherz , Liat Goldshaid , Yoram Salomon
IPC分类号： A61K51/08 , A61K49/00 , A61K49/14 , A61K38/00 , A61P35/00 , A61P43/00
CPC分类号： A61K51/0485 , A61K41/0057 , A61K41/0071 , A61K49/0036 , A61K49/0056 , A61K49/085 , A61K49/14 , A61K51/044 , A61K51/0446 , A61K51/0451 , A61K51/082 , A61K51/088 , C07D257/04
摘要： RGD-chlorophyll and RGD-bacteriochlorophyll conjugates that home and accumulate in necrotic tumor domains much longer than in tumor non-necrotic domains are provided for use in minimally invasive tumor-targeted imaging, tumor-targeted photodynamic therapy, and/or on-line prognosis of necrotic tumors.
摘要翻译：家庭和积累在坏死肿瘤域中的RGD-叶绿素和RGD-细菌叶绿素缀合物比在肿瘤非坏死区域中长得多的时间被提供用于微创肿瘤靶向成像，肿瘤靶向光动力学治疗和/或在线预后的坏死性肿瘤。

9. 发明授权

US07830702B2 Synthetic molecular spring device 失效
标题翻译：合成分子弹簧装置
公开(公告)号：US07830702B2
公开(公告)日：2010-11-09
申请号：US10468840
申请日：2002-03-12
申请人： Roie Yerushalmi , Avigdor Scherz
发明人： Roie Yerushalmi , Avigdor Scherz
IPC分类号： C07B47/00 , G11C13/00
CPC分类号： F16F1/3605 , F16F1/00 , F16F3/00
摘要： Synthetic molecular spring device featuring: (a) a synthetic molecular assembly, SMA, each scalable chemical module including: (i) at least one atom, M, (ii) at least one complexing group, CG, complexed to an atom, M, (iii) at least one axial ligand, AL, reversibly physicochemically paired with at least one atom, M, complexed to a complexing group, CG, (iv) at least one substantially elastic molecular linker, ML, having body and two ends with at least one chemically bonded to another component of SMA; (b) activating mechanism, AM, operatively directed to an atom-axial ligand pair, whereby following activating mechanism, AM, sending activating signal, AS/AS′, to an atom-axial ligand pair for physicochemically modifying the atom-axial ligand pair, there is activating at least one cycle of spring-type elastic reversible transitions between contracted and expanded linear conformational states of molecular linker, ML. Optionally includes (v) chemical connectors, CC, and/or, (vi) binding sites, BS.
摘要翻译：合成分子弹簧装置，其特征在于：（a）合成分子组装，SMA，每个可伸缩化学模块，包括：（i）至少一个原子，M，（ii）至少一个与原子复合的络合基团，（iii）至少一个轴向配体AL，与至少一个与络合基团复合的原子M可逆地物理化学配对，（iv）至少一个基本上弹性的分子接头ML，其具有体和两端，至少一个化学键合到SMA的另一个组分; （b）活化机制AM，可操作地导向原子 - 轴配体对，由此在激活机制AM之后，将激活信号AS / AS'发送到原子 - 轴配体对，用于物理化学修饰原子 - 轴配体对，激活了分子连接子的收缩和扩展的线性构象状态之间的弹簧型弹性可逆转换的至少一个循环。可选地包括（v）化学连接剂，CC和/或（vi）结合位点，BS。

10. 发明授权

US06740637B1 Chlorophyll and bacteriochlorophyll derivatives, their preparation and pharmaceutical compositions comprising them 失效
标题翻译：叶绿素和细菌叶绿素衍生物，它们的制备和包含它们的药物组合物
公开(公告)号：US06740637B1
公开(公告)日：2004-05-25
申请号：US09615310
申请日：2000-07-13
申请人： Avigdor Scherz , Yoram Salomon , Leszek Fiedor
发明人： Avigdor Scherz , Yoram Salomon , Leszek Fiedor
IPC分类号： A61K3800
CPC分类号： A61K49/00 , A61K41/0071 , A61K47/64 , A61K47/6803 , A61K47/6851 , A61K49/0036 , A61K49/0052 , A61K49/0056 , C07K14/685 , C07K14/795 , C12N9/18 , C12P17/182
摘要： Conjugates of chlorophyll (Chl) and bacteriochlorophyll (Bchl) derivatives with amino acids, peptides and proteins are provided by the invention. The amino acid, peptide or protein residue is linked to the 17-propionic acid group of a Chl or Bchl residue directly or through a chain. The conjugates are for use as photosensitizers in photodynamic therapy and in diagnostics of tumors. Conjugation with cell-specific ligands, such as hormones, growth factors or tumor-specific antibodies, will target the Chl or Bchl moiety to the tumor site. Thus, conjugates with melanocyte stimulating hormones are suitable for photodynamic therapy of melanoma tumors.
摘要翻译：本发明提供了具有氨基酸，肽和蛋白质的叶绿素（Chl）和细菌叶绿素（Bchl）衍生物的缀合物。氨基酸，肽或蛋白质残基直接或通过链连接到Chl或Bchl残基的17-丙酸基团。该缀合物用作光动力疗法和肿瘤诊断中的光敏剂。与细胞特异性配体如激素，生长因子或肿瘤特异性抗体的缀合将靶向Chl或Bchl部分到肿瘤部位。因此，与黑素细胞刺激激素的缀合物适用于黑素瘤肿瘤的光动力学治疗。

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