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1. 发明授权

US4689432A Chelators whose affinity for calcium is decreased by illumination 失效
标题翻译：通过照明降低钙对钙的亲和力的螯合剂
公开(公告)号：US4689432A
公开(公告)日：1987-08-25
申请号：US648536
申请日：1984-09-07
申请人： Roger Y. Tsien , Grzegorz Grynkiewicz , Akwasi Minta
发明人： Roger Y. Tsien , Grzegorz Grynkiewicz , Akwasi Minta
IPC分类号： C07F9/09 , C07C67/00 , C07C201/00 , C07C205/37 , C07C227/00 , C07C227/16 , C07C229/16 , C07C229/18 , C07C301/00 , C07C309/66 , C07D215/40 , C07D317/62 , C07D319/18 , C07F9/60 , C09K3/00 , G01N33/84 , C07C101/26 , C07D215/38
CPC分类号： G01N33/84 , C07D317/62 , Y10S424/06
摘要： The present invention discloses a group of calcium chelating compounds which have a descreased affinity for calcium following illumination. These new compounds contain a photolabile nitrobenzyl derivative coupled to a tetracarboxylate Ca.sup.2+ chelating parent compound having the octacoordinate chelating groups characteristic of EGTA or BAPTA. In a first form, the new compounds are comprised of a BAPTA-like chelator coupled to a single 2-nitrobenzyl derivative, which in turn is a photochemical precursor of a 2-nitrosobenzophenone. In a second form, the new compounds are comprised of a BAPTA-like chelator coupled to two 2-nitrobenzyl derivatives, themselves photochemical prcursors of the related 2-nitrosobenzophenones.The present invention also discloses a novel method for preparing 1-hydroxy- or 1-alkoxy-1-(2-nitroaryl)-1-aryl methanes. Methanes of this type are critical to the preparation of, or actually constitute, the photolabile Ca.sup.2+ chelating compounds disclosed and claimed herein.
摘要翻译：本发明公开了一种钙照射后对钙的亲和力降低的钙螯合化合物。这些新化合物含有偶联到具有EGTA或BAPTA特征的八配位螯合基团的四羧酸盐Ca 2+螯合母体化合物的光不稳定的硝基苄基衍生物。在第一种形式中，新化合物由与单一2-硝基苄基衍生物偶联的BAPTA样螯合剂组成，其又是2-亚硝基二苯甲酮的光化学前体。在第二种形式中，新化合物由与两个2-硝基苄基衍生物偶联的BAPTA样螯合剂组成，它们本身是相关的2-亚硝基二苯甲酮的光化学原子。本发明还公开了一种制备1-羟基 - 或1-烷氧基-1-（2-硝基芳基）-1-芳基甲烷的新方法。这种类型的甲烷对于制备或实际构成本文公开和要求保护的光不稳定的Ca 2+螯合化合物至关重要。

2. 发明授权

US4603209A Fluorescent indicator dyes for calcium ions 失效
标题翻译：用于钙离子的荧光指示剂染料
公开(公告)号：US4603209A
公开(公告)日：1986-07-29
申请号：US648649
申请日：1984-09-07
申请人： Roger Y. Tsien , Grzegorz Grynkiewicz
发明人： Roger Y. Tsien , Grzegorz Grynkiewicz
IPC分类号： A61K38/00 , A61K38/22 , A61P5/00 , C07C229/18 , C07C229/52 , C07C237/30 , C07C255/59 , C07C309/49 , C07C311/39 , C07C317/32 , C07D209/08 , C07D209/14 , C07D215/40 , C07D307/79 , C07D307/82 , C07D413/04 , C07K7/23 , G01N21/78 , G01N33/84 , C07C101/447 , C07D307/87
CPC分类号： C07D307/79 , C07D209/08 , C07D215/40 , C07D413/04 , Y10S436/80
摘要： The present invention discloses a new class of highly fluorescent indicator dyes that are specific for calcium ions. The new fluorescent indicator dyes combine a stilbene-type fluorophore with a tetracarboxylate parent Ca.sup.2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of EGTA and BAPTA. Preferred forms contain extra heterocyclic bridges to reinforce the ethylenic bond of the stilbene and to reduce hydrophobicity. Compared to their widely used predecessor, "quin2", the new dyes offer up to thirty-fold brighter fluorescence, major changes in wavelength (not just intensity) upon Ca.sup.2+ binding, slightly lower affinities for Ca.sup.2+, slightly longer wavelengths of excitation, and considerably improved selectivity for Ca.sup.2+ over other divalent cations. These properties, particularly the wavelength sensitivity to Ca.sup.2+, make the dyes useful indicators for many intracellular applications, especially in single cells, adherent cell layers, or bulk tissues.The present invention also discloses an improved method for synthesizing alpha-acyloxyalkyl bromides wherein the bromides so synthesized are free of contaminating bis(1-bromoalkyl)ether. The improved method is exemplified herein in the synthesis of acetoxymethyl bromide, a compound useful in preparing the acetoxymethyl esters disclosed herein as novel Ca.sup.2+ specific fluorescent indicators.
摘要翻译：本发明公开了一类对钙离子具有特异性的高荧光指示剂染料。新的荧光指示剂染料将二苯乙烯型荧光团与具有EGTA和BAPTA特征的连接组的八配位图案的四羧酸母体Ca 2+螯合化合物结合。优选的形式包含额外的杂环桥，以加强1,2-二苯乙烯的烯键并降低疏水性。与其广泛使用的前身“quin2”相比，新型染料提供高达三十倍的荧光，Ca2 +结合时的波长（不仅仅是强度）的主要变化，Ca2 +的亲和力略低，激发波长稍长，提高Ca2 +对其他二价阳离子的选择性。这些性质，特别是对Ca2 +的波长敏感性，使得染料对于许多细胞内应用尤其是在单细胞，贴壁细胞层或体组织中是有用的指标。本发明还公开了一种合成α-酰氧基烷基溴化物的改进方法，其中如此合成的溴化物没有污染的双（1-溴烷基）醚。改进的方法在本文中示例性地合成乙酰氧甲基溴，其是可用于制备本文公开的乙酰氧基甲酯作为新型Ca 2+特异性荧光指示剂的化合物。

3. 发明授权

US08623910B2 Isoflavones for treating mucopolysaccharidoses 失效
标题翻译：用于治疗粘多糖症的异黄酮
公开(公告)号：US08623910B2
公开(公告)日：2014-01-07
申请号：US13433492
申请日：2012-03-29
申请人： Grzegorz Grynkiewicz , Grzegorz Wegrzyn , Barbara Szechner , Wieslaw Szeja , Anna Tylki-Szymanska , Alicja Wegrzyn , Joanna Jakobkiewicz-Banecka , Sylwia Baranska , Barbara Czartoryska , Ewa Piotrowska
发明人： Grzegorz Grynkiewicz , Grzegorz Wegrzyn , Barbara Szechner , Wieslaw Szeja , Anna Tylki-Szymanska , Alicja Wegrzyn , Joanna Jakobkiewicz-Banecka , Sylwia Baranska , Barbara Czartoryska , Ewa Piotrowska
IPC分类号： A61K47/32
CPC分类号： A61K31/352
摘要： A method of treatment of mucopolysaccharidosis, the method including administering to a patient in the need of such treatment—a therapeutically effective amount of a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition including a pharmaceutically acceptable excipient; and a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof, the natural isoflavone, the derivative thereof, or the pharmaceutically acceptable salt thereof being in a therapeutically effective amount for the treatment of mucopolysaccharidosis.
摘要翻译：一种治疗粘多糖贮积症的方法，所述方法包括对需要这种治疗的患者施用治疗有效量的式（I）的天然异黄酮，其衍生物或其药学上可接受的盐。包含药学上可接受的赋形剂的药物组合物; 和式（I）的天然异黄酮，其衍生物或其药学上可接受的盐，其用于治疗粘多糖贮积病的治疗有效量的天然异黄酮，其衍生物或其药学上可接受的盐。

4. 发明授权

US07109177B2 Methods and compositions for the manufacture of C-3′ and C-4′ anthracycline antibiotics 有权
公开(公告)号：US07109177B2
公开(公告)日：2006-09-19
申请号：US10752426
申请日：2004-01-06
申请人： Waldeman Priebe , Izabella Fokt , Teresa Przewloka , Marta Krawczyk , Piotr Skibicki , Grzegorz Grynkiewicz , Roman Perez-Soler
发明人： Waldeman Priebe , Izabella Fokt , Teresa Przewloka , Marta Krawczyk , Piotr Skibicki , Grzegorz Grynkiewicz , Roman Perez-Soler
IPC分类号： A61K31/70 , C07H15/24
CPC分类号： C07H15/252 , A61K31/704
摘要： The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4′ of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.

5. 发明授权

US08178609B2 Isoflavones for treating mucopolysaccharidoses 有权
标题翻译：用于治疗粘多糖症的异黄酮
公开(公告)号：US08178609B2
公开(公告)日：2012-05-15
申请号：US12067289
申请日：2006-09-21
申请人： Grzegorz Grynkiewicz , Grzegorz Wegrzyn , Barbara Szechner , Wieslaw Szeja , Anna Tylki-Szymańska , Alicja Wegrzyn , Joanna Jakobkiewicz-Banecka , Sylwia Barańska , Barbara Czartoryska , Ewa Piotrowska
发明人： Grzegorz Grynkiewicz , Grzegorz Wegrzyn , Barbara Szechner , Wieslaw Szeja , Anna Tylki-Szymańska , Alicja Wegrzyn , Joanna Jakobkiewicz-Banecka , Sylwia Barańska , Barbara Czartoryska , Ewa Piotrowska
IPC分类号： A61K47/32
CPC分类号： A61K31/352
摘要： A method of treatment of mucopolysaccharidosis, the method including administering to a patient in the need of such treatment-a therapeutically effective amount of a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition including a pharmaceutically acceptable excipient; and a natural isoflavone of formula (I), a derivative thereof, or a pharmaceutically acceptable salt thereof, the natural isoflavone, the derivative thereof, or the pharmaceutically acceptable salt threof being in a therapeutically effective amount for the treatment of mucopolysaccharidosis.
摘要翻译：一种治疗粘多糖贮积症的方法，所述方法包括对需要这种治疗的患者施用治疗有效量的式（I）的天然异黄酮，其衍生物或其药学上可接受的盐。包含药学上可接受的赋形剂的药物组合物; 和式（I）的天然异黄酮，其衍生物或其药学上可接受的盐，其用于治疗粘多糖贮积症的治疗有效量的天然异黄酮，其衍生物或药学上可接受的盐。

6. 发明申请

US20050004048A1 Methods and compositions for the manufacture of C-3' and C-4' anthracycline antibiotics 有权
标题翻译：用于制造C-3'和C-4'蒽环类抗生素的方法和组合物
公开(公告)号：US20050004048A1
公开(公告)日：2005-01-06
申请号：US10752426
申请日：2004-01-06
申请人： Waldeman Priebe , Izabella Fokt , Teresa Przewloka , Marta Krawczyk , Piotr Skibicki , Grzegorz Grynkiewicz , Roman Perez-Soler
发明人： Waldeman Priebe , Izabella Fokt , Teresa Przewloka , Marta Krawczyk , Piotr Skibicki , Grzegorz Grynkiewicz , Roman Perez-Soler
IPC分类号： C07H15/252 , A61K31/704 , C07H15/24
CPC分类号： C07H15/252 , A61K31/704
摘要： The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4′ of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracyline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.
摘要翻译：本发明公开了在糖部分的C-3'上具有改性的烷基 - 芳环取代的新的和新的取代的蒽环类，或在糖部分的C-4'被修饰或未修饰的烷基 - 芳环取代。它还公开了制备糖底物的新方法和制备蒽环类抗生素的方法。这些蒽环霉素类似物在体外对几种肿瘤细胞系显示高细胞毒性。

7. 发明授权

US06673907B2 Methods and compositions for the manufacture of C-3′ and C-4′ anthracycline antibiotics 有权
标题翻译：用于制造C-3'和C-4'蒽环类抗生素的方法和组合物
公开(公告)号：US06673907B2
公开(公告)日：2004-01-06
申请号：US09956588
申请日：2001-09-19
申请人： Waldemar Priebe , Izabella Fokt , Teresa Przewloka , Marta Krawczyk , Piotr Skibicki , Grzegorz Grynkiewicz , Roman Perez-Soler
发明人： Waldemar Priebe , Izabella Fokt , Teresa Przewloka , Marta Krawczyk , Piotr Skibicki , Grzegorz Grynkiewicz , Roman Perez-Soler
IPC分类号： C07H100
CPC分类号： C07H15/252 , A61K31/704
摘要： The present invention discloses new and novel substituted anthracyclines with modified alkyl-aromatic ring substitutions on the C-3′ of the sugar moiety or modified or unmodified alkyl-aromatic ring substitutions at the C-4′ of the sugar moiety. It also discloses novel methods for the preparation of sugar substrates and methods for the preparation of anthracycline antibiotics. These anthracycline analogs show high cytotoxicity in vitro against several tumor cell lines.
摘要翻译：本发明公开了在糖部分的C-3'上具有改性的烷基 - 芳环取代的新的和新的取代的蒽环类，或在糖部分的C-4'被修饰或未修饰的烷基 - 芳环取代。它还公开了制备糖底物的新方法和制备蒽环类抗生素的方法。这些蒽环霉素类似物在体外对几种肿瘤细胞系显示高细胞毒性。

8. 发明申请

US20180244714A1 PROTOESCIGENIN DERIVATIVE, PROCESS OF ITS PREPARATION, USE OF SAID COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THAT COMPOUND 审中-公开
公开(公告)号：US20180244714A1
公开(公告)日：2018-08-30
申请号：US15553301
申请日：2016-02-26
申请人： Katarzyna KOZIAK , Krzysztof BOJAKOWSKI , Magdalena KOWALEWSKA , Dorota MACIEJKO , Oliwia ZEGROCKA-STENDEL , Iwona GRABOWSKA , Grzegorz GRYNKIEWICZ , Mariusz Marek GRUZA , Kamil JATCZAK , Katarzyna FILIP , Piotr CMOCH , Marta LASZCZ , Instytut Farmaceutyczny
发明人： Katarzyna Koziak , Krzysztof Bojakowski , Magdalena Kowalewska , Dorota Maciejko , Oliwia Zegrocka-Stendel , Iwona Grabowska , Grzegorz Grynkiewicz , Mariusz Marek Gruza , Kamil Jatczak , Katarzyna Filip , Piotr Cmoch , Marta Laszcz
IPC分类号： C07J63/00 , A61K31/58
CPC分类号： C07J63/008 , A61K31/58
摘要： Described herein is compound including a protoescigenin derivative having pharmacological properties. Also described are a process of its preparation, and the use of such a compound as a medicament, especially for treating vascular disorders. A pharmaceutical composition comprising such compound is further described.

9. 发明授权

US06355784B1 Methods and compositions for the manufacture of halogenated anthracyclines with increased antitumor activity, other anthracyclines, halogenated sugars, and glycosyl donors 失效
标题翻译：用于制备具有增加的抗肿瘤活性的卤代蒽环类抗生素的方法和组合物，其它蒽环类，卤代糖和糖基供体
公开(公告)号：US06355784B1
公开(公告)日：2002-03-12
申请号：US09330226
申请日：1999-06-10
申请人： Waldemar Priebe , Marta Krawczyk , Piotr Skibicki , Izabela Fokt , Krzysztof Dziewiszek , Grzegorz Grynkiewicz , Roman Perez-Soler
发明人： Waldemar Priebe , Marta Krawczyk , Piotr Skibicki , Izabela Fokt , Krzysztof Dziewiszek , Grzegorz Grynkiewicz , Roman Perez-Soler
IPC分类号： C07H1524
CPC分类号： C07H15/252
摘要： The present invention discloses new and novel halogenated anthracyclines linked through the saccharide portions. These congeners show high activity in vitro against several tumor cell lines. In doxorubicin (DOX) sensitive cell lines, they are at least as cytotoxic as DOX and in some cases more so. Many of these 4′- and 6′-fluorinated anthracyclines are more effective against multidrug-resistant tumors than was DOX, and/or have greater effectiveness than DOX against DOX sensitive cells. The compounds of this invention also have anti-amyloidogenic effects and the use of these compounds in the treatment of Alzheimer's disease is contemplated.
摘要翻译：本发明公开了通过糖部分连接的新型和新型卤代蒽环类。这些同系物在体外对几种肿瘤细胞系显示出高活性。在多柔比星（DOX）敏感细胞系中，它们至少与DOX一样具有细胞毒性，在某些情况下更为如此。这些4'-和6'-氟化蒽环类药物中的许多对抗多药耐药肿瘤比DOX更有效，和/或比DOX对DOX敏感细胞具有更大的效力。本发明的化合物还具有抗淀粉样变性作用，并且考虑这些化合物在治疗阿尔茨海默氏病中的用途。

10. 发明授权

US4908464A Process for the production of 1,3,2-oxazaphosphorinanes 失效
标题翻译：生产1,3,2-oxazaphosphorinanes的方法
公开(公告)号：US4908464A
公开(公告)日：1990-03-13
申请号：US204582
申请日：1988-06-09
申请人： Wojciech J. Stec , Czeslaw Radzikowski , Wieslaw Szelejewski , Ryszard Kinas , Konrad Misiura , Grzegorz Grynkiewicz , Jacek Grodner , Halina Kusnierczyk , Andrzej Kutner , Slawomira Pilichowska
发明人： Wojciech J. Stec , Czeslaw Radzikowski , Wieslaw Szelejewski , Ryszard Kinas , Konrad Misiura , Grzegorz Grynkiewicz , Jacek Grodner , Halina Kusnierczyk , Andrzej Kutner , Slawomira Pilichowska
IPC分类号： C07F9/6584
CPC分类号： C07F9/65846
摘要： Process for production of derivatives of 1,3,2-oxazaphosphorinane of general formula 1, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atom or 2-halogenoalkyl group, and R.sub.1 and R.sub.2 are not at the same time hydrogen atoms, and X represents halogen atom is based, according to the invention, on the reduction of the respective 3-halogenoacyl derivatives of 1,3,2-oxazaphosphorinane of general formula 2, ##STR2## wherein the substituents have the above given meaning. The reduction is accomplished with the use of sodium borohydride in the presence of boron trifluoride etherate.Derivatives that are prepared by the procedure described here demonstrate antitumor activity.

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