公开(公告)号：US09850183B2

公开(公告)日：2017-12-26

申请号：US14746349

申请日：2015-06-22

Applicant: Reiley Pharmaceuticals, Inc.

Inventor： Mark A. Reiley ,  B. Michael Silber ,  Julio Medina ,  Frank Kayser ,  William D. Shrader

IPC: A61M36/00 ,  A61K51/00 ,  C07B59/00 ,  C07F13/00 ,  A61K51/04

CPC classification number: C07B59/004 ,  A61K51/0402 ,  A61K51/0478 ,  A61K51/0487 ,  A61K51/0497 ,  C07F13/00 ,  C07F13/005

Abstract: Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

公开(公告)号：US20040166058A1

公开(公告)日：2004-08-26

申请号：US10703405

申请日：2003-11-07

Applicant: Board of Regents, The University of Texas System ,  Cell>Point LLC

Inventor： David J. Yang ,  Dong-Fang Yu ,  Chang-Sok Oh ,  Jerry L. Bryant JR.

IPC: A61K051/00 ,  C07K016/46 ,  C07F005/00

CPC classification number: C07F13/005 ,  A61K51/04 ,  A61K51/0402 ,  A61K51/0453 ,  A61K51/0455 ,  A61K51/0459 ,  A61K51/0487 ,  A61K51/0491 ,  A61K51/08 ,  A61K51/081 ,  A61K51/088 ,  A61K51/1027 ,  A61K51/1093

Abstract: The invention provides, in a general sense, a new labeling strategy employing compounds that are are N2S2 chelates conjugated to a targeting ligand, wherein the targeting ligand is a disease cell cycle targeting compound, a tumor angiogenesis targeting ligand, a tumor apoptosis targeting ligand, a disease receptor targeting ligand, amifostine, angiostatin, monoclonal antibody C225, monoclonal antibody CD31, monoclonal antibody CD40, capecitabine, COX-2, deoxycytidine, fullerene, herceptin, human serum albumin, lactose, leuteinizing hormone, pyridoxal, quinazoline, thalidomide, transferrin, or trimethyl lysine. The present invention also pertains to kits employing the compounds of interest, and methods of assessing the pharmacology of an agent of interest using the present compounds.

Abstract translation: 本发明在一般意义上提供了使用与靶向配体缀合的N 2 S 2螯合物的化合物的新标记策略，其中靶向配体是疾病细胞周期靶向化合物，肿瘤血管生成靶向配体，肿瘤凋亡靶向配体， 疾病受体靶向配体，氨磷汀，血管抑素，单克隆抗体C225，单克隆抗体CD31，单克隆抗体CD40，卡培他滨，COX-2，脱氧胞苷，富勒烯，赫赛汀，人血清白蛋白，乳糖，促黄体激素，吡哆醛，喹唑啉，沙利度胺， ，或三甲基赖氨酸。 本发明还涉及使用目的化合物的试剂盒，以及使用本发明化合物评价感兴趣剂的药理学的方法。

公开(公告)号：US20170216436A1

公开(公告)日：2017-08-03

申请号：US15329116

申请日：2014-07-29

Applicant: Beijing Fullcan Bio-technology Co., Ltd.

Inventor： Chunru Wang ,  Mingming Zhen ,  Chunying Shu ,  Taishan Wang ,  Jie Li ,  Guoqiang Zhang

IPC: A61K41/00 ,  A61K51/12 ,  A61K51/04 ,  A61K9/00

CPC classification number: A61K41/0028 ,  A61K9/0019 ,  A61K41/00 ,  A61K51/0487 ,  A61K51/1251

Abstract: Metallofullerene monocrystalline nanoparticles are used as tumor vascular disrupting agents. The monocrystalline nanoparticles are water-soluble metallofullerene nanoparticles with negative charges on their surfaces. The particle sizes range from 50 to 250 nanometers. The nanomaterials are able to absorb outside radiation energy, and transform it into heat energy. The volumes rapidly expand when temperature reaches a phase transformation point. For treatment, metallofullerene monocrystalline nanoparticles are administrated to a tumor-bearing organism via injection. The metallofullerene monocrystalline nanoparticles reach tumor sites via blood circulation, and are retained at the tumor sites. The monocrystalline nanoparticles of metallofullerene accumulate heat and the temperature increases under outside radiation energy. The volumes sharply expand when the temperature exceeds a critical point of phase transition thereof, thereby causing changes in the morphologies, structures or functions of endothelium cells of tumor vessels.

公开(公告)号：US20150374858A1

公开(公告)日：2015-12-31

申请号：US14746349

申请日：2015-06-22

Applicant: Reiley Pharmaceuticals, Inc.

Inventor： Mark A. REILEY ,  B. Michael SILBER ,  Julio MEDINA ,  Frank KAYSER ,  William D. SHRADER

IPC: A61K51/04 ,  C07F17/00 ,  C07B59/00 ,  C07F13/00 ,  A61K51/08

CPC classification number: C07B59/004 ,  A61K51/0402 ,  A61K51/0478 ,  A61K51/0487 ,  A61K51/0497 ,  C07F13/00 ,  C07F13/005

Abstract: Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

Abstract translation: 公开了衍生自非甾体抗炎药（NSAID）的缀合物及其使用方法，用于特别是鉴定和定位病人和/或炎症部位，该部位负责患者的疼痛感觉; 用于鉴定原发性，继发性，良性或恶性肿瘤的部位; 并用于诊断感染或确认或排除疑似感染。 基于NSAID的缀合物含有成像部分。 缀合物集中在增加的环加氧酶表达的位点，从而揭示了与疼痛和炎症相关的前列腺素产生增加的位点，并且与肿瘤存在和/或位置相关。 识别增加的COX表达的区域也可以帮助筛查感染。

公开(公告)号：US08623326B2

公开(公告)日：2014-01-07

申请号：US12994259

申请日：2009-05-22

Applicant: Leonard G. Luyt ,  Dina Rosita

Inventor： Leonard G. Luyt ,  Dina Rosita

IPC: A61K51/08 ,  A61K38/03 ,  G01N33/567

CPC classification number: C07K14/575 ,  A61K47/64 ,  A61K49/0002 ,  A61K49/0056 ,  A61K51/0487 ,  A61K51/088

Abstract: Ghrelin analogues having high affinity for a target receptor in diseased cells are provided, as well as methods of diagnosis and treatment utilizing such analogues.

Abstract translation: 提供了在患病细胞中对靶受体具有高亲和力的生长素释放肽类似物，以及利用这些类似物的诊断和治疗方法。

公开(公告)号：US07544715B2

公开(公告)日：2009-06-09

申请号：US10507221

申请日：2003-04-24

Applicant: Mark M. Goodman ,  Jonathan McConathy

Inventor： Mark M. Goodman ,  Jonathan McConathy

IPC: A61K31/195 ,  A61K31/19 ,  C07C229/00

CPC classification number: C07F13/005 ,  A61K51/04 ,  A61K51/0478 ,  A61K51/0487 ,  C07B2200/05 ,  C07C229/20 ,  C07C229/22

Abstract: The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of α-aminoisobutyric acid (AIB) analogs namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. In addition the compounds can be labeled with technetium and rhenium isotopes using known chelation complexes. The amino acid compounds disclosed herein have a high specificity for target sites when administered to a subject in vivo. The labeled amino acid compounds are useful as imaging agents in detecting and/or monitoring tumors in a subject by Positron Emission Tomography (PET) and Single Photon Emission Computer Tomography (SPECT).

Abstract translation: 本发明提供了用于检测和评价脑和体肿瘤的新型氨基酸化合物。 这些化合物结合了α-氨基异丁酸（AIB）类似物的有利性质，即它们在肿瘤中的快速摄取和延长的保留性，其具有卤素取代基的性质，包括某些有用的卤素同位素如氟-18，碘-123，碘-124 ，碘-125，碘-131，溴-75，溴-76，溴-77，溴-82，ast ine -21，ast ine -211和其他ast同位素。 此外，化合物可以使用已知的螯合络合物用锝和铼同位素标记。 当在体内施用于受试者时，本文公开的氨基酸化合物对靶位点具有高特异性。 标记的氨基酸化合物可用作通过正电子发射断层扫描（PET）和单光子发射计算机断层扫描（SPECT）检测和/或监测受试者的肿瘤的成像剂。

公开(公告)号：US5808146A

公开(公告)日：1998-09-15

申请号：US554906

申请日：1995-11-09

Applicant: Mark M. Goodman ,  Timothy Shoup

Inventor： Mark M. Goodman ,  Timothy Shoup

IPC: A61K51/00 ,  A61K51/04 ,  C07B59/00 ,  C07C45/30 ,  C07C45/59 ,  C07C229/20 ,  C07C229/30 ,  C07C229/48 ,  C07F13/00 ,  C07F17/00 ,  C07C61/06

CPC classification number: A61K51/0487 ,  A61K51/0478 ,  C07B59/001 ,  C07C229/20 ,  C07C229/30 ,  C07C229/48 ,  C07C45/30 ,  C07C45/59 ,  C07F13/005 ,  A61K2123/00 ,  C07C2101/04 ,  C07C2101/08 ,  C07C2101/10 ,  C07C2101/14 ,  C07C2101/16

Abstract: The invention provides novel amino acid compounds of use in detecting and evaluating brain and body tumors. These compounds combine the advantageous properties of 1-amino-cycloalkyl-1-carboxylic acids, namely, their rapid uptake and prolonged retention in tumors with the properties of halogen substituents, including certain useful halogen isotopes including fluorine-18, iodine-123, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77 and bromine-82. In one aspect, the invention features amino acid compounds that have a high specificity for target sites when administered to a subject in vivo. Preferred amino acid compounds show a target to non-target ratio of at least 5:1, are stable in vivo and substantially localized to target within 1 hour after administration. An especially preferred amino acid compound is �.sup.18 F!-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC). In another aspect, the invention features pharmaceutical compositions comprised of an .alpha.-amino acid moiety attached to either a four, five, or a six member carbon-chain ring. In addition, the invention features analogs of .alpha.-aminoisobutyric acid.

Abstract translation: 本发明提供了用于检测和评价脑和体肿瘤的新型氨基酸化合物。 这些化合物结合了1-氨基 - 环烷基-1-羧酸的有利特性，即它们在肿瘤中的快速吸收和延长的保留性，其具有卤素取代基的性质，包括某些有用的卤素同位素，包括氟-18，碘-123，碘 -125，碘-131，溴-75，溴-76，溴-77和溴-82。 在一个方面，本发明的特征在于在体内施用于受试者时对靶位点具有高特异性的氨基酸化合物。 优选的氨基酸化合物显示至少5:1的目标与非目标比例，在给药后1小时内体内稳定并基本上定位于靶。 特别优选的氨基酸化合物是[18 F] -1-氨基-3-氟环丁烷-1-羧酸（FACBC）。 在另一方面，本发明的特征在于由连接到四个，五个或六个碳链环上的α-氨基酸部分组成的药物组合物。 此外，本发明具有α-氨基异丁酸的类似物。

公开(公告)号：US4933055A

公开(公告)日：1990-06-12

申请号：US63567

申请日：1987-06-17

Applicant: Dennis W. Wester

Inventor： Dennis W. Wester

IPC: A61K51/04 ,  B01J19/10 ,  C07F13/00

CPC classification number: C07F13/00 ,  A61K51/0487 ,  B01J19/10 ,  A61K2123/00

Abstract: A novel method for the production of bis(arene) technetium radiodiagnostic imaging agents is herein disclosed. The method consists of employing Fischer synthesis reactants in an ultrasonic bath. The products are virtually pure, thus lacking the severe degree of disproportionation which routinely occurs when partially alkylated bis(arene)technetium compounds are produced by thermally driven reactions.

Abstract translation: 本文公开了生产双（芳烃）锝放射性诊断显像剂的新方法。 该方法包括在超声波浴中使用费雪合成反应物。 产物几乎是纯的，因此缺乏通过热驱动反应产生部分烷基化双（芳烃）锝化合物时常常发生的严重程度的歧化。

公开(公告)号：US20240190790A1

公开(公告)日：2024-06-13

申请号：US18207628

申请日：2023-06-08

Applicant: Reiley Pharmaceuticals, Inc.

Inventor： Mark A. REILEY ,  B. Michael SILBER ,  Julio MEDINA ,  Frank KAYSER ,  William D. SHRADER

IPC: C07B59/00 ,  A61K51/04 ,  C07F13/00

CPC classification number: C07B59/004 ,  A61K51/0402 ,  A61K51/0478 ,  A61K51/0487 ,  A61K51/0497 ,  C07F13/00 ,  C07F13/005

Abstract: Conjugates derived from non-steroidal anti-inflammatory drugs (NSAIDs) and methods of use thereof are disclosed, useful for, inter alia, identifying and localizing the site of pathology and/or inflammation responsible for the sensation of pain in a patient; for identifying the sites of primary, secondary, benign, or malignant tumors; and for diagnosing infection or confirming or ruling out suspected infection. The NSAID-based conjugates contain an imaging moiety. The conjugates concentrate at sites of increased cyclooxygenase expression, thus revealing the sites of increased prostaglandin production, which is correlated with pain and inflammation, and correlated with tumor presence and/or location. Identifying areas of increased COX expressing can also aid in screening for infections.

公开(公告)号：US11931431B2

公开(公告)日：2024-03-19

申请号：US16981432

申请日：2019-03-29

Applicant: FUTURECHEM CO., LTD

Inventor： Dae Yoon Chi ,  Byoung Se Lee ,  So Young Chu ,  Hyeon Jin Jeong ,  Min Hwan Kim ,  Kyo Chul Lee ,  Yong Jin Lee

IPC: A61K51/04 ,  A61P35/00 ,  C07F5/00

CPC classification number: A61K51/0487 ,  A61P35/00 ,  C07F5/003

Abstract: The present invention relates to a pharmaceutical composition for diagnosing and treating prostate cancer, capable of targeting PSMA, and a compound provided by one aspect of the present invention has a glutamine-urea-lysine compound to which a radioactive metal-coupled chelator is structurally coupled and to which an aryl group that can additionally bind to PSMA protein is coupled. Coupling between the glutamine-urea-lysine compound and the chelator includes a polar spacer so as to serve the role of reducing in vivo nonspecific coupling and exhibit an effect of being rapidly removed from vital organs, but not from prostate cancer. These characteristics lower the radiation exposure, which is caused by a therapeutic radioisotope-coupled compound, to normal tissue and organs, and thus reduce side effects. In addition, a compound that contains a phenyl group having a coupling force with albumin has an increased residence time in the blood, thereby becoming more accumulated in prostate cancer.