公开(公告)号：US20020037254A1

公开(公告)日：2002-03-28

申请号：US09463474

申请日：2000-08-04

Inventor： HANNSJORG SINN ,  HANS-HERMANN SCHRENK ,  ANDREAS WUNDER ,  GERD STEHLE

IPC: A61B005/055 ,  C07D219/08 ,  A61B005/00 ,  C07K001/00 ,  A61K038/00 ,  C07K014/00 ,  C07K017/00 ,  C09H001/00 ,  C07K016/00 ,  A61K038/17 ,  A61K031/35 ,  A01N043/16

CPC classification number: A61K49/0026 ,  A61K49/0036 ,  A61K49/0039 ,  A61K49/0056 ,  C07K14/765 ,  C07K2319/00 ,  G01N21/64 ,  G01N33/54353 ,  G01N33/582

Abstract: The invention relates to conjugates, comprising a fluorescent compound and a carrier, wherein the compound and the carrier are connected via an acidic ester or an acidic amide bond and the compound has an excitation wavelength of 630 nm or more and/or 450 nm or less. The invention also relates to the production of said conjugates and to the use thereof.

Abstract translation: 本发明涉及包含荧光化合物和载体的缀合物，其中化合物和载体通过酸性酯或酸性酰胺键连接，该化合物具有630nm以上和/或450nm以下的激发波长 。 本发明还涉及所述缀合物的生产及其用途。

公开(公告)号：US06183727B2

公开(公告)日：2001-02-06

申请号：US09282610

申请日：1999-04-01

Applicant: John Devens Gust, Jr. ,  Ana L. Moore ,  Thomas A. Moore ,  William H. Ralston

Inventor： John Devens Gust, Jr. ,  Ana L. Moore ,  Thomas A. Moore ,  William H. Ralston

IPC: A61B1000

CPC classification number: A61K49/0052 ,  A61K41/0071 ,  A61K49/0021 ,  A61K49/0036 ,  C07D487/22

Abstract: A process of pathology or target tissue identification comprising administering an imaging material to a pathology or target tissue bearing mammalian host and irradiating the mammalian host with electromagnetic radiation having a wavelength between about 600 and 1100 nm, and especially in the region of 700 nm and longer wavelengths, whereupon the imaging material, which has been preferentially taken up by the pathology or target tissue, emits light and permits precise identification of the location, size and/or shape of the pathology or target tissue.

公开(公告)号：US5759563A

公开(公告)日：1998-06-02

申请号：US486262

申请日：1995-06-07

Applicant: Gerald L. Yewey ,  Nancy L. Krinick ,  Richard L. Dunn ,  Michael L. Radomsky ,  Gerbrand Brouwer ,  Arthur J. Tipton

Inventor： Gerald L. Yewey ,  Nancy L. Krinick ,  Richard L. Dunn ,  Michael L. Radomsky ,  Gerbrand Brouwer ,  Arthur J. Tipton

IPC: A61K9/00 ,  A61K9/08 ,  A61K9/20 ,  A61K9/22 ,  A61K9/70 ,  A61K47/48 ,  A61K49/00 ,  A61L15/44 ,  A61K9/127 ,  A61F13/00

CPC classification number: A61K9/0024 ,  A61K31/4439 ,  A61K31/485 ,  A61K31/704 ,  A61K38/09 ,  A61K38/27 ,  A61K47/34 ,  A61K47/48176 ,  A61K47/48192 ,  A61K47/482 ,  A61K47/48784 ,  A61K47/48853 ,  A61K49/0017 ,  A61K49/0036 ,  A61K49/0054 ,  A61K49/0063 ,  A61K49/0091 ,  A61K9/10 ,  A61K9/146 ,  A61K9/5026 ,  A61K9/5047 ,  A61L26/0019 ,  A61L26/0066 ,  A61L26/0085 ,  A61L27/18 ,  A61L27/56 ,  A61L31/06 ,  A61L31/146 ,  A61L31/16 ,  A61K47/42 ,  A61L2300/604 ,  A61L2300/62 ,  A61L2400/06 ,  Y10S514/90 ,  Y10S525/937 ,  Y10S977/774 ,  Y10S977/783 ,  Y10S977/906 ,  Y10S977/907 ,  Y10S977/915 ,  Y10S977/918

Abstract: Improved biocompatible liquid delivery compositions, which are useful for the formation of sustained release delivery systems for active agents, are provided. The compositions include liquid formulations of a biocompatible polymer or prepolymer in combination with a controlled release component. The controlled release component includes an active agent. These compositions may be introduced into the body of a subject in liquid form which then solidify or cure in situ to form a controlled release implant or a film dressing. The liquid delivery compositions may also be employed ex situ to produce a controlled release implant. Methods of forming a controlled release implant and employing the liquid formulations in the treatment of a subject are also provided.

Abstract translation: 提供改进的生物相容性液体递送组合物，其可用于形成活性剂的缓释递送系统。 组合物包括与受控释放组分组合的生物相容性聚合物或预聚物的液体制剂。 受控释放组分包括活性剂。 这些组合物可以以液体形式引入受试者的身体，其然后在现场固化或固化以形成控释植入物或膜敷料。 液体递送组合物也可以非原位地用于产生控释植入物。 还提供了形成受控释放植入物并使用液体制剂治疗受试者的方法。

公开(公告)号：US5726169A

公开(公告)日：1998-03-10

申请号：US097384

申请日：1993-07-26

Applicant: Avigdor Scherz ,  Yoram Salomon ,  Leszek Fiedor

Inventor： Avigdor Scherz ,  Yoram Salomon ,  Leszek Fiedor

IPC: 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 ,  A61K31/40

CPC classification number: A61K49/0036 ,  A61K41/0071 ,  A61K47/48246 ,  A61K47/48384 ,  A61K47/48569 ,  A61K49/00 ,  A61K49/0052 ,  A61K49/0056 ,  C07K14/685 ,  C07K14/795 ,  C12N9/18 ,  C12P17/182

Abstract: 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.

公开(公告)号：US5559207A

公开(公告)日：1996-09-24

申请号：US227370

申请日：1994-04-14

Applicant: Jonathan L. Sessler ,  Daniel A. Smith ,  Richard A. Miller ,  Kevin L. Ross ,  Meredith Wright ,  William C. Dow ,  Vladimir A. Kr al ,  Brent Iverson ,  Darren Magda

Inventor： Jonathan L. Sessler ,  Daniel A. Smith ,  Richard A. Miller ,  Kevin L. Ross ,  Meredith Wright ,  William C. Dow ,  Vladimir A. Kr al ,  Brent Iverson ,  Darren Magda

IPC: A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/04 ,  A61L2/00 ,  B01J31/06 ,  B01J31/16 ,  B01J31/18 ,  C07B61/00 ,  C07D487/22 ,  C07F9/06 ,  C07F9/6558 ,  C07F9/6561 ,  C07H21/00 ,  C07K2/00 ,  C07F5/00 ,  C07H3/00 ,  C07K16/00

CPC classification number: A61K47/48069 ,  A61K41/0038 ,  A61K41/0076 ,  A61K49/0021 ,  A61K49/0036 ,  A61K49/085 ,  A61K49/106 ,  A61K49/126 ,  A61K51/0485 ,  A61L2/0011 ,  B01J31/1658 ,  B01J31/1815 ,  C07D487/22 ,  C07H21/00 ,  B01J2531/025 ,  B01J2531/23 ,  B01J2531/26 ,  B01J2531/27 ,  B01J2531/28 ,  B01J2531/38 ,  B01J2531/72 ,  B01J2531/842 ,  B01J2531/845 ,  B01J2531/847 ,  B01J2531/96 ,  B01J31/061

Abstract: A method of phosphate ester hydrolysis including incubating a solution of an aqueous phosphate ester with a texaphyrin metal complex. The metal is a metal cation having catalytic activity for ester bond hydrolysis in aqueous solution, in particular, a lanthanide metal cation, preferably Eu(III) or Dy(III). A preferred substrate is RNA and a preferred texaphyrin is a derivatized texaphyrin having binding specificity, in particular, a texaphyrin covalently coupled to a site-directed molecule, preferably an oligonucleotide.

Abstract translation: 磷酸酯水解的方法，包括将磷酸酯水溶液与泰克萨菲金属络合物的溶液孵育。 金属是具有催化活性的金属阳离子，用于在水溶液中酯键水解，特别是镧系元素金属阳离子，优选Eu（III）或Dy（III）。 优选的底物是RNA，优选的泰克萨菲瑞是具有结合特异性的衍生的泰克萨菲林，特别是共价偶联到定点分子，优选寡核苷酸的泰克萨菲林。

公开(公告)号：US5492924A

公开(公告)日：1996-02-20

申请号：US126361

申请日：1993-09-24

Applicant: Shimon Gatt ,  Arie Dagan ,  Rene Santus ,  Jean-Claude Maziere ,  J. Donald Chapman ,  Edward L. Engelhardt

Inventor： Shimon Gatt ,  Arie Dagan ,  Rene Santus ,  Jean-Claude Maziere ,  J. Donald Chapman ,  Edward L. Engelhardt

IPC: A61K31/40 ,  A61K41/00 ,  A61K49/00 ,  A61K51/04 ,  C07D487/22

CPC classification number: A61K51/0485 ,  A61K31/40 ,  A61K41/0071 ,  A61K49/0036 ,  C07D487/22 ,  A61K2123/00

Abstract: Phorbine derivatives having high potency and light absorptivity in the 650 to 780 nanometer range are useful in cancer diagnosis and therapy, especially photodynamic therapy.

Abstract translation: 在650至780纳米范围内具有高效能和光吸收性的菲啡宾衍生物可用于癌症诊断和治疗，特别是光动力疗法。

公开(公告)号：US5451576A

公开(公告)日：1995-09-19

申请号：US112872

申请日：1993-08-25

Applicant: Jonathan L. Sessler ,  Gregory W. Hemmi ,  Tarak D. Mody

Inventor： Jonathan L. Sessler ,  Gregory W. Hemmi ,  Tarak D. Mody

IPC: A61K31/40 ,  A61K41/00 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/04 ,  A61L2/00 ,  A61P35/00 ,  A61P43/00 ,  C07D487/22 ,  C07H17/02 ,  C07H21/00 ,  A61K31/555

CPC classification number: A61K51/0485 ,  A61K41/0009 ,  A61K41/0038 ,  A61K41/0076 ,  A61K47/48069 ,  A61K49/0021 ,  A61K49/0036 ,  A61K49/0058 ,  A61K49/04 ,  A61K49/106 ,  A61K51/1093 ,  A61L2/0011 ,  C07D487/22 ,  C07H17/02 ,  C07H21/00

Abstract: The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.

Abstract translation: 本发明涉及保持亲油性的水溶性羟基取代的泰克萨菲瑞，合成这些化合物及其用途。 这些膨胀的卟啉大环是二价和三价金属离子的有效螯合剂。 本发明的羟基取代的泰克萨菲瑞衍生物的各种金属（例如，转变，主要和镧系元素）络合物具有不寻常的水溶性和稳定性。 它们在生理上重要的区域（即690-880nm）中强烈吸收光。 它们具有增强的放松性，因此在磁共振成像中是有用的。 它们以高产率形成长寿命的三重态，并且作为产生单线态氧的光敏剂。 因此，它们可用于灭活或破坏感染了这种病毒以及肿瘤细胞的人类免疫缺陷病毒（HIV-1），单核细胞或其他细胞。 它们是水溶性的，但它们保持足够的亲脂性，以便对富含脂质的区域如动脉粥样化和肿瘤具有更大的亲和力。 它们可用于磁共振成像，随后光动力学肿瘤治疗治疗动脉粥样化和肿瘤。 这些性质加上其高的化学稳定性和在水中的明显的溶解度，增加了它们的用途。

公开(公告)号：US5403928A

公开(公告)日：1995-04-04

申请号：US701449

申请日：1991-05-15

Applicant: Peter O. G. Arrhenuis

Inventor： Peter O. G. Arrhenuis

IPC: A61K31/695 ,  A61K41/00 ,  A61K47/48 ,  A61K49/00 ,  A61P35/00 ,  C07D487/22 ,  C07F7/10 ,  C07H15/26 ,  C07H17/00 ,  C07H23/00 ,  C07J43/00 ,  C07J51/00 ,  C09B47/00 ,  C09B47/073 ,  C09B47/08 ,  C09B47/24 ,  C09K11/06 ,  G01N33/533 ,  G01N33/58 ,  C09B47/30

CPC classification number: A61K49/0036 ,  A61K41/0071 ,  A61K47/48215 ,  A61K49/0015 ,  A61K49/0054 ,  C07J43/003 ,  C07J51/00 ,  C09B47/00 ,  C09B47/073 ,  C09B47/08 ,  C09B47/24 ,  G01N33/533 ,  G01N33/582 ,  G01N2333/19

Abstract: Marker components are provided which are compatible with aqueous solutions, exhibit favorable fluorescence properties and exhibit decreased non-specific binding to macromolecules in solution. These marker components are useful in applications such as fluorescence immunoassays, in vivo imaging and in vivo tumor therapy.

Abstract translation: 提供与水溶液相容的标记组分，显示出有利的荧光性质，并且在溶液中表现出降低的非特异性结合大分子。 这些标记组分可用于荧光免疫测定，体内成像和体内肿瘤治疗等应用。

公开(公告)号：US5286474A

公开(公告)日：1994-02-15

申请号：US966136

申请日：1992-10-22

Applicant: John D. Gust, Jr. ,  Ana L. Moore ,  Thomas A. Moore ,  Giulio Jori ,  Elena Reddi

Inventor： John D. Gust, Jr. ,  Ana L. Moore ,  Thomas A. Moore ,  Giulio Jori ,  Elena Reddi

IPC: A61K31/40 ,  A61K49/00 ,  C07D487/22 ,  A61B5/00 ,  A61K31/555 ,  C07B47/00

CPC classification number: A61K49/0036 ,  A61K31/40 ,  A61K49/0052 ,  C07D487/22 ,  Y10S436/80

Abstract: A process of tumor identification comprising administering a carotenoporphyrin to a tumor-bearing mammalian host and irradiating the mammalian host with light whereupon the carotenoporphyrin, which has been preferentially taken up by the tumor tissue, fluoresces and permits precise identification of the location, size and shape of the tumor tissue. An improved process of synthesizing carotenoporphyrins 1-5 is also provided.

Abstract translation: 一种肿瘤鉴定过程，包括向含荷瘤的哺乳动物宿主施用胡萝卜素卟啉并用光照射哺乳动物宿主，其中优先被肿瘤组织吸收的胡萝卜素卟啉发亮并允许精确鉴定位置，大小和形状 的肿瘤组织。 还提供了合成胡萝卜素卟啉1-5的改进方法。

公开(公告)号：US5252720A

公开(公告)日：1993-10-12

申请号：US822964

申请日：1992-01-21

Applicant: Jonathan L. Sessler ,  Gregory W. Hemmi ,  Tarak D. Mody

Inventor： Jonathan L. Sessler ,  Gregory W. Hemmi ,  Tarak D. Mody

IPC: A61K31/40 ,  A61K41/00 ,  A61K49/00 ,  A61K49/06 ,  A61K49/08 ,  A61K51/04 ,  A61L2/00 ,  A61P35/00 ,  A61P43/00 ,  C07D487/22 ,  C07H17/02 ,  C07H21/00 ,  C07F19/00 ,  C07H23/00

CPC classification number: A61K51/0485 ,  A61K41/0009 ,  A61K41/0038 ,  A61K41/0076 ,  A61K47/48069 ,  A61K49/0021 ,  A61K49/0036 ,  A61K49/0058 ,  A61K49/04 ,  A61K49/106 ,  A61K51/1093 ,  A61L2/0011 ,  C07D487/22 ,  C07H17/02 ,  C07H21/00

Abstract: The present invention involves water soluble hydroxy-substituted texaphyrins retaining lipophilicity, the synthesis of such compounds and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Various metal (e.g., transition, main group, and lanthanide) complexes of the hydroxy-substituted texaphyrin derivatives of the present invention have unusual water solubility and stability. They absorb light strongly in a physiologically important region (i.e. 690-880 nm). They have enhanced relaxivity and therefore are useful in magnetic resonance imaging. They form long-lived triplet states in high yield and act as photosensitizers for the generation of singlet oxygen. Thus, they are useful for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus as well as tumor cells. They are water soluble, yet they retain sufficient lipophilicity so as to have greater affinity for lipid rich areas such as atheroma and tumors. They may be used for magnetic resonance imaging followed by photodynamic tumor therapy in the treatment of atheroma and tumors. These properties, coupled with their high chemical stability and appreciable solubility in water, add to their usefulness.

Abstract translation: 本发明涉及保持亲油性的水溶性羟基取代的泰克萨菲瑞，合成这些化合物及其用途。 这些膨胀的卟啉大环是二价和三价金属离子的有效螯合剂。 本发明的羟基取代的泰克萨菲瑞衍生物的各种金属（例如，转变，主要和镧系元素）络合物具有不寻常的水溶性和稳定性。 它们在生理上重要的区域（即690-880nm）中强烈吸收光。 它们具有增强的放松性，因此在磁共振成像中是有用的。 它们以高产率形成长寿命的三重态，并且作为产生单线态氧的光敏剂。 因此，它们可用于灭活或破坏感染了这种病毒以及肿瘤细胞的人类免疫缺陷病毒（HIV-1），单核细胞或其他细胞。 它们是水溶性的，但它们保持足够的亲脂性，以便对富含脂质的区域如动脉粥样化和肿瘤具有更大的亲和力。 它们可用于磁共振成像，随后光动力学肿瘤治疗治疗动脉粥样化和肿瘤。 这些性质加上其高的化学稳定性和在水中的明显的溶解度，增加了它们的用途。