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1. 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。

2. 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。

3. 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

4. 发明授权

US09957293B2 Conjugates of RGD peptides and porphyrin or (bacterio)chlorophyll photosynthesizers and their uses 有权
公开(公告)号：US09957293B2
公开(公告)日：2018-05-01
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： C07K5/12 , C07K5/09 , C07K5/10 , C07K7/06 , C07K7/64 , A61K41/00 , A61K51/08 , G01N33/574 , A61K47/64 , A61K51/00 , A61M36/14
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.

5. 发明申请

US20140378888A1 (BACTERIO)CHLOROPHYLL PHOTOSENSITIZERS FOR TREATMENT OF EYE DISEASES AND DISORDERS 有权
标题翻译：（BACTERIO）氯仿荧光素治疗眼病和疾病
公开(公告)号：US20140378888A1
公开(公告)日：2014-12-25
申请号：US14240328
申请日：2012-08-23
申请人： Avigdor Scherz , Yoram Salomon , Arie Marcovich , Alexander Brandis , Daniel Wagner
发明人： Avigdor Scherz , Yoram Salomon , Arie Marcovich , Alexander Brandis , Daniel Wagner
IPC分类号： A61K31/555 , A61K41/00
CPC分类号： A61K41/0071 , A61K9/0048 , A61K31/407 , A61K31/519 , A61K31/555 , A61K47/186 , A61K47/36 , A61N5/062 , A61N2005/0659
摘要： An ophthalmic composition is provided, comprising chlorophyll or bacteriochlorophyll compounds for photodynamic treatment (PDT) of diseases, disorders and conditions associated with corneal or scleral anomalies such as corneal thinning and scleral stretching.
摘要翻译：提供了一种眼用组合物，其包含用于光动力治疗（PDT）的叶绿素或细菌叶绿素化合物与角膜或巩膜异常如角膜变薄和巩膜拉伸相关的疾病，病症和病症。

6. 发明授权

US08207154B2 Catatonic bacteriochlorophyll derivatives 有权
标题翻译：致命菌素叶绿素衍生物
公开(公告)号：US08207154B2
公开(公告)日：2012-06-26
申请号：US11628719
申请日：2005-06-07
申请人： Avigdor Scherz , Alexander Brandis , Yoram Salomon , Doron Eren , Avraham Cohen
发明人： Avigdor Scherz , Alexander Brandis , Yoram Salomon , Doron Eren , Avraham Cohen
IPC分类号： A01N55/02 , C07B47/00
CPC分类号： A61K31/409 , A61K41/0071 , Y02A50/406
摘要： The invention provides cationic tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one positively charged group and/or at least one basic group that is converted to a positively charged group under physiological conditions, preferably Bchls having an onium group derived from a N-containing aliphatic or heterocyclic radical such as ammonium, guanidinium, imidazolium, pyridinium, and the like or a phosphonium, arsonium, oxonium, sulfonium, selenonium, telluronium, stibonium, or bismuthonium group, or a basic group that is converted to such onium groups under physiological conditions, said groups being bound to one or more of the positions 17 , 13 and 3 of the Bchl molecule by ester or amide bond. The Bchls are useful for photodynamic therapy and diagnosis.
摘要翻译：本发明提供了含有至少一个带正电基团和/或至少一个碱性基团的阳离子四环和五环类细菌叶绿素衍生物（Bchls），其在生理条件下转化为带正电荷的基团，优选具有衍生自N- 含有脂族或杂环基团如铵，胍，咪唑鎓，吡啶鎓等，或鏻，ium，氧鎓，锍，硒鎓，碲鎓，锑或铋鎓基团，或转化为这种鎓基团的碱性基团生理条件，所述基团通过酯或酰胺键与Bchl分子的一个或多个位置17 3，13 3和3 2结合。 Bchls可用于光动力疗法和诊断。

7. 发明授权

US07947672B2 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：US07947672B2
公开(公告)日：2011-05-24
申请号：US10534692
申请日：2003-11-17
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： A61K31/555 , A01N55/02 , C07B47/00 , C07D487/22
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。

8. 发明申请

US20110117029A1 WATER-SOLUBLE ANIONIC BACTERIOCHLOROPHYLL DERIVATIVES AND THEIR USES 有权
标题翻译：水溶性阴离子聚合氯乙烯衍生物及其用途
公开(公告)号：US20110117029A1
公开(公告)日：2011-05-19
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： A61K31/555 , C07D487/22 , C07K17/02 , A61K49/00 , A01N55/02 , A61K39/44 , A61P35/00 , A61P27/02 , A01P1/00
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。

9. 发明申请

US20080076748A1 Catatonic Bacteriochlorophyll Derivatives 有权
标题翻译：紧致细菌叶绿素衍生物
公开(公告)号：US20080076748A1
公开(公告)日：2008-03-27
申请号：US11628719
申请日：2005-06-07
申请人： Avigdor Scherz , Alexander Brandis , Yoram Salomon , Doron Eren , Avraham Cohen
发明人： Avigdor Scherz , Alexander Brandis , Yoram Salomon , Doron Eren , Avraham Cohen
IPC分类号： A61K31/555 , C07D487/22 , A61K31/409 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/55
CPC分类号： A61K31/409 , A61K41/0071 , Y02A50/406
摘要： The invention provides cationic tetracyclic and pentacyclic bacteriochlorophyll derivatives (Bchls) containing at least one positively charged group and/or at least one basic group that is converted to a positively charged group under physiological conditions, preferably Bchls having an onium group derived from a N-containing aliphatic or heterocyclic radical such as ammonium, guanidinium, imidazolium, pyridinium, and the like or a phosphonium, arsonium, oxonium, sulfonium, selenonium, telluronium, stibonium, or bismuthonium group, or a basic group that is converted to such onium groups under physiological conditions, said groups being bound to one or more of the positions 17 , 13 and 3 of the Bchl molecule by ester or amide bond. The Bchls are useful for photodynamic therapy and diagnosis.
摘要翻译：本发明提供了含有至少一个带正电基团和/或至少一个碱性基团的阳离子四环和五环类细菌叶绿素衍生物（Bchls），其在生理条件下转化为带正电荷的基团，优选具有衍生自N- 含有脂族或杂环基团如铵，胍，咪唑鎓，吡啶鎓等，或鏻，ium，氧鎓，锍，硒鎓，碲鎓，锑或铋鎓基团，或转化为这种鎓基团的碱性基团生理条件，所述基团通过酯或酰胺键与Bchl分子的一个或多个位置17 3，13 3和3 2结合。 Bchls可用于光动力疗法和诊断。

10. 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。

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