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    DENDRIMER CONJUGATES
    1.
    发明申请
    DENDRIMER CONJUGATES 有权
    DENDRIMER联合

    公开(公告)号：US20120277376A1

    公开(公告)日：2012-11-01

    申请号：US13547929

    申请日：2012-07-12

    Applicant: James R. Baker, JR. ,  Xue-min Cheng ,  Thommey P. Thomas ,  Baohua Mark Huang

    Inventor： James R. Baker, JR. ,  Xue-min Cheng ,  Thommey P. Thomas ,  Baohua Mark Huang

    IPC: C08G69/48

    CPC classification number: C07D305/08

    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.

    Abstract translation: 本发明涉及新的治疗和诊断树枝状大分子。 特别地，本发明涉及树枝状大分子 - 连接体缀合物，其合成方法，包含缀合物的组合物，以及利用缀合物的系统和方法（例如，在诊断和/或治疗设置（例如，用于递送 治疗，成像和/或靶向剂（例如，在疾病（例如癌症）诊断和/或治疗，疼痛治疗等中））。因此，本发明的树枝状大分子 - 接头缀合物还可包含一种或多种 用于靶向，成像，感测和/或提供治疗或诊断材料和/或监测治疗反应的组分。

    DENDRIMER BASED MODULAR PLATFORMS
    2.
    发明申请
    DENDRIMER BASED MODULAR PLATFORMS 审中-公开
    基于DENDRIMER的模块化平台

    公开(公告)号：US20100158850A1

    公开(公告)日：2010-06-24

    申请号：US12645081

    申请日：2009-12-22

    Applicant: James R. Baker, JR. ,  Mark M. Banaszak Holl ,  Xue-min Cheng ,  Baohua Huang ,  Daniel McNemy ,  Douglas G. Mullen ,  Thommey Thomas

    Inventor： James R. Baker, JR. ,  Mark M. Banaszak Holl ,  Xue-min Cheng ,  Baohua Huang ,  Daniel McNemy ,  Douglas G. Mullen ,  Thommey Thomas

    IPC: A61K31/74 ,  C08G69/00

    CPC classification number: A61K31/74 ,  A61K31/00 ,  A61K45/06 ,  A61K47/551 ,  A61K47/59 ,  A61K47/595 ,  C08G73/0206 ,  C08G73/028 ,  C08G81/00 ,  C08G83/003 ,  C08L79/02 ,  C08L101/005 ,  A61K2300/00

    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimer based modular platforms (e.g., drug delivery platforms). In particular, the dendrimer based modular platforms are configured such that two or more dendrimers (e.g., PAMAM dendrimers) are coupled together (e.g., via a cycloaddition reaction) wherein each of the coupled dendrimers is functionalized (e.g., functionalized for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy). In some embodiments, the present invention provides dendrimer based modular platforms having coupled dendrimers (e.g., two or more coupled dendrimers) wherein each dendrimer is conjugated to one or more functional groups (e.g., therapeutic agent, imaging agent, targeting agent, triggering agent) (e.g., for specific targeting and/or therapeutic use of the dendrimer based modular platform). In some embodiments, the functional groups are conjugated to the dendrimers via a linker and/or a triggering agent. In addition, the present invention is directed to methods of synthesizing dendrimer based modular platforms, compositions comprising the dendrimer based modular platforms, as well as systems and methods utilizing the dendrimer based modular platforms (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, etc.)).

    Abstract translation: 本发明涉及新颖的基于树枝状大分子的模块化平台（例如药物递送平台）。 特别地，基于树枝状聚合物的模块化平台被配置为使得两个或更多个树枝状聚合物（例如，PAMAM树枝状聚合物）偶联在一起（例如，通过环加成反应），其中每个偶联的树枝状聚合物被官能化（例如，功能化用于靶向，成像， 感测和/或提供治疗或诊断材料和/或监测对治疗的响应）。 在一些实施方案中，本发明提供了具有结合的树枝状大分子（例如两个或更多个偶联的树枝状大分子）的树枝状大分子模块化平台，其中每个树枝状聚合物与一个或多个官能团（例如，治疗剂，成像剂，靶向剂，引发剂） （例如，用于基于树枝状聚合物的模块化平台的特异性靶向和/或治疗用途）。 在一些实施方案中，官能团通过接头和/或引发剂与树枝状聚合物缀合。 此外，本发明涉及基于树枝状聚合物的模块化平台的方法，包含基于树枝状聚合物的模块化平台的组合物以及利用基于树枝状聚合物的模块化平台的系统和方法（例如，在诊断和/或治疗设置（例如， 用于递送治疗剂，成像和/或靶向剂（例如，在疾病（例如癌症）诊断和/或治疗中等））。

    Nonpeptide endothelin antagonists with increased water solubility
    5.
    发明授权
    Nonpeptide endothelin antagonists with increased water solubility 失效
    具有增加的水溶性的非肽内皮素拮抗剂

    公开(公告)号：US06297274B1

    公开(公告)日：2001-10-02

    申请号：US09117667

    申请日：1998-08-04

    Applicant: Xue-Min Cheng ,  Annette Marian Doherty ,  William Chester Patt ,  Joseph Thomas Repine

    Inventor： Xue-Min Cheng ,  Annette Marian Doherty ,  William Chester Patt ,  Joseph Thomas Repine

    IPC: A61K3134

    CPC classification number: C07D407/04 ,  C07D307/60

    Abstract: Novel nonpeptide endothelin I antagonists of Formula are described wherein R1 is unsubstituted or substituted cycloalkyl, phenyl, naphthyl or heteroaryl, R2 is unsubstituted or substituted alkyl, aryl or heteroaryl, R3 is unsubstituted or substituted alkyl, cycloalkyl, aryl or heteroayl, and R1 and/or R2 and/or R3 are independently substituted by a total of from 1 to 4 substituents which enhance aqueous solubility with the proviso that when R2 is alkyl and is substituted, the substituent is not oxygen at the &agr;-position of the furanone ring. Further described are methods for the preparation and pharmaceutical compositions of compounds of Formula I, which are useful in treating atherosclerosis, restenosis, Raynaud's phenomenon, mild or severe congestive heart failure, cerebral ischemia, cerebral infarction, embolic stroke, cerebral vasospasm, glaucoma, subarachnoid hemorrhage, hemorrhagic stroke, diabetes, gastric ulceration and mucosal damage, ischemic bowel disease, Chrohn's disease, male penile erectile dysfunction, essential or malignant hypertension, pulmonary hypertension, pulmonary hypertension after bypass, cancer, especially malignant hemangioendothelioma or prostate cancer, myocardial infarction or ischemia, acute or chronic renal failure, renal ischemia, radiocontrast-induced nephrotoxcity, endotoxic, septic hemorrhagic shock, angina, preeclampsia, asthma, arrhythmias, benign prostatic hyperplasia, and elevated levels of endothelin.

    Abstract translation: 苯基，萘基或杂芳基，R2为未取代或取代的烷基，芳基或杂芳基，R3为未取代或取代的烷基，环烷基，芳基或杂芳基，R1和/ 或R 2和/或R 3独立地被总共1至4个增强水溶性的取代基取代，条件是当R 2是烷基且被取代时，该取代基不是在呋喃酮环的α-位上的氧。 进一步描述了用于制备治疗动脉粥样硬化，再狭窄，雷诺现象，轻度或重度充血性心力衰竭，脑缺血，脑梗死，栓塞性中风，脑血管痉挛，青光眼，蛛网膜下腔出血 出血性，出血性中风，糖尿病，胃溃疡和粘膜损伤，缺血性肠病，克罗恩病，男性阴茎勃起功能障碍，基本或恶性高血压，肺动脉高压，旁路后肺动脉高压，癌症，特别是恶性血管内皮瘤或前列腺癌，心肌梗塞或 缺血，急性或慢性肾衰竭，肾缺血，放射性对照诱导的肾毒性，内毒素性，败血性出血性休克，心绞痛，先兆子痫，哮喘，心律失常，良性前列腺增生和内皮素水平升高。

    Small molecule biaryl compounds as inhibitors of endothelin converting enzyme
    7.
    发明授权
    Small molecule biaryl compounds as inhibitors of endothelin converting enzyme 失效
    小分子联芳基化合物作为内皮素转化酶的抑制剂

    公开(公告)号：US5891892A

    公开(公告)日：1999-04-06

    申请号：US949632

    申请日：1997-10-14

    Applicant: Xue-Min Cheng ,  Mark Alan Massa ,  William Chester Patt

    Inventor： Xue-Min Cheng ,  Mark Alan Massa ,  William Chester Patt

    IPC: C07D417/04 ,  A61K31/44

    CPC classification number: C07D417/04

    Abstract: Novel small molecular biaryl compounds as inhibitors of endothelin converting enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in treating elevated levels of endothelin, acute and chronic renal failure, hypertension, myocardial infarction, myocardial ischemia, cerebral vasospasm, cerebral ischemia, cerebral infarction, cirrhosis, septic shock, congestive heart failure, endotoxic shock, subarachnoid hemorrhage, arrhythmias, asthma, preeclampsia, atherosclerotic disorders including Raynaud's disease and restenosis, angina, cancer, pulmonary hypertension, ischemic disease, gastric mucosal damage, hemorrhagic shock, ischemic bowel disease, stroke, benign prosthatic hyperplasia (BPH), and diabetes.

    Abstract translation: 描述了新型小分子联芳基化合物作为内皮素转化酶的抑制剂，以及其制备方法及其药物组合物，其可用于治疗高水平的内皮素，急性和慢性肾衰竭，高血压，心肌梗死，心肌 缺血，脑血管痉挛，脑缺血，脑梗塞，肝硬化，败血性休克，充血性心力衰竭，内毒素性休克，蛛网膜下腔出血，心律失常，哮喘，先兆子痫，动脉粥样硬化疾病包括雷诺氏病和再狭窄，心绞痛，癌症，肺动脉高压，缺血性疾病， 胃粘膜损伤，出血性休克，缺血性肠病，中风，良性前列腺增生（BPH）和糖尿病。

    Dendrimer conjugates
    10.
    发明授权
    Dendrimer conjugates 有权

    公开(公告)号：US08445528B2

    公开(公告)日：2013-05-21

    申请号：US13547929

    申请日：2012-07-12

    Applicant: James R. Baker, Jr. ,  Xue-min Cheng ,  Thommey P. Thomas ,  Baohua Mark Huang

    Inventor： James R. Baker, Jr. ,  Xue-min Cheng ,  Thommey P. Thomas ,  Baohua Mark Huang

    IPC: A61K31/403 ,  A61K31/485 ,  C07D209/12 ,  C07D471/04

    CPC classification number: C07D305/08

    Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer-linker conjugates, methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer-linker conjugates of the present invention may further comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy.

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