公开(公告)号：US20060142361A1

公开(公告)日：2006-06-29

申请号：US11289348

申请日：2005-11-29

Applicant: Keykavous Parang ,  Soroush Sardari ,  Nguyen Nam

Inventor： Keykavous Parang ,  Soroush Sardari ,  Nguyen Nam

IPC: A61K31/4196 ,  C07D403/02

CPC classification number: C07D249/08 ,  C07D403/06 ,  C07F9/6518 ,  C07F9/65586

Abstract: The present invention is broadly directed to azole derivatives that exhibit antifungal activity and methods for making the same. In one aspect, the invention includes carboxylic acid and phosphate ester derivatives of fluconazole that exhibit antifungal activity. In addition, the invention comprises methods for synthesizing the derivatives and pharmaceutical compositions containing the derivatives.

Abstract translation: 本发明广泛涉及显示抗真菌活性的唑衍生物及其制备方法。 一方面，本发明包括具有抗真菌活性的氟康唑的羧酸和磷酸酯衍生物。 此外，本发明包括合成衍生物的方法和含有衍生物的药物组合物。

公开(公告)号：US07045617B2

公开(公告)日：2006-05-16

申请号：US09811870

申请日：2001-03-21

Applicant: Philip A. Cole ,  Keykavous Parang ,  Ararat Abloogu ,  Ronald A. Kohanski ,  Aliya Courtney

Inventor： Philip A. Cole ,  Keykavous Parang ,  Ararat Abloogu ,  Ronald A. Kohanski ,  Aliya Courtney

IPC: C07H19/20 ,  A61K38/28 ,  A61K38/00 ,  A61K38/04

CPC classification number: A61K47/62

Abstract: Protein kinase inhibitors have applications as anti-cancer therapeutic agents and biological tools in cell signalling. Potent and selective bisubstrate inhibitors for the insulin receptor tyrosine kinase are based on a phosphoryl transfer mechanism involving a dissociative transition state. One such inhibitor is synthesized by linking ATPγS to a peptide substrate analog via a two-carbon spacer. The compound is a high-affinity competitive inhibitor against both nucleotide and peptide substrate and shows a slow off-rate. A crystal structure of this inhibitor bound to the tyrosine kinase domain of the insulin receptor confirms the key design features inspired by a dissociative transition state, and reveal that the linker takes part in the octahedral coordination of an active site Mg2+ ion.

Abstract translation: 蛋白激酶抑制剂可用作细胞信号传导中的抗癌治疗剂和生物工具。 用于胰岛素受体酪氨酸激酶的强效选择性双底物抑制剂是基于涉及离解过渡态的磷酰转移机制。 一种这样的抑制剂通过经由二碳间隔基连接ATPgammaS到肽底物类似物来合成。 该化合物是针对核苷酸和肽底物的高亲和力竞争性抑制剂，显示出缓慢的脱离率。 结合胰岛素受体的酪氨酸激酶结构域的这种抑制剂的晶体结构证实了由解离过渡状态启发的关键设计特征，并且揭示了连接体参与活性位点Mg 2+的八面体配位， / SUP>离子。

公开(公告)号：US20230000999A1

公开(公告)日：2023-01-05

申请号：US17788954

申请日：2020-12-24

Applicant: Keykavous PARANG ,  Hamidreza MONTAZERI ALIABADI ,  Dindyal MANDAL ,  Eman MOHAMMED ,  Saghar MOZAFFARI ,  Sandeep LOHAN ,  Rakesh TIWARI ,  Ryley HALL ,  AJK BIOPHARMACEUTICAL, LLC

Inventor： Keykavous PARANG ,  Hamidreza MONTAZERI ALIABADI ,  Dindyal MANDAL ,  Eman MOHAMMED ,  Saghar MOZAFFARI ,  Sandeep LOHAN ,  Rakesh TIWARI ,  Ryley HALL

IPC: A61K47/64 ,  C07K7/08 ,  C07K7/06 ,  C07K7/64 ,  A61K48/00 ,  A61K47/69 ,  C12N15/113 ,  C12N15/11 ,  A61P35/00 ,  A61K8/64 ,  A61Q19/00 ,  A61K8/60 ,  A61K47/60

Abstract: Peptide-based systems containing hydrophobic amino acids (e.g., tryptophan), charged amino acids (e.g., arginine), and/or sulfur-containing amino acids (e.g., cysteine), which can be used either alone or in combination with nanoparticles (e.g., gold or silver nanoparticles) for siRNA delivery into living cells are disclosed.

公开(公告)号：US20070173437A1

公开(公告)日：2007-07-26

申请号：US11565914

申请日：2006-12-01

Applicant: Keykavous Parang ,  Gonqqin Sun ,  Anil Kumar ,  Nguyen Nam ,  Yue-Hao Wang ,  Guofeng Ye

Inventor： Keykavous Parang ,  Gonqqin Sun ,  Anil Kumar ,  Nguyen Nam ,  Yue-Hao Wang ,  Guofeng Ye

IPC: A61K38/16

CPC classification number: A61K31/70 ,  A61K47/549 ,  A61K47/62

Abstract: A bisubstrate inhibitor of Src kinases, having a nucleotide or N-heteroaromatic moiety; and a peptide/phosphopeptide, peptidomimetic, or phosphopeptide mimic moiety. The moieties are linked by a rigid or a flexible linker. The nucleotide or N-heteroaromatic moiety is ATP, ATP-mimics, N-heteroaromatics including purine-based derivatives, pyrimidine-based derivatives such as 2,4-diamino-5-substituted pyrimidine derivatives, pyrazole[3,4-d]pyrimidine derivatives, pyrrolo[2,3-d]pyrimidine derivatives, pyrido[2,3-d]pyrimidine derivatives, amino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives, thieno- and furo-substituted derivatives, quinazoline derivatives, and quinoline derivatives, and several natural products such as aminogenistein. The phosphopeptide mimics comprise phosphonate-based phosphotyrosine mimetics such as phosphonomethylphenylalanine (Pmp) and its analogues, carboxylic acid-based phosphotyrosine mimetics such as malonyltyrosine or phenylalanine analogues and their derivatives such as carboxymethyl phenylalanine, uncharged pTyr mimetics, and confonnationally constrained peptides. The phosphopeptide or phosphopeptide mimics inhibits the Src kinases SH2 domain.

Abstract translation: 具有核苷酸或N-杂芳族部分的Src激酶的双底物抑制剂; 和肽/磷酸肽，拟肽或磷酸肽模拟部分。 这些部分通过刚性或柔性接头连接。 核苷酸或N-杂芳族部分是ATP，ATP-模拟物，包括嘌呤类衍生物的N-杂芳族化合物，嘧啶类衍生物如2,4-二氨基-5-取代的嘧啶衍生物，吡唑[3,4-d]嘧啶 衍生物，吡咯并[2,3-d]嘧啶衍生物，吡啶并[2,3-d]嘧啶衍生物，氨基取代的二氢嘧啶并[4,5-d]嘧啶酮衍生物，噻吩并呋喃基取代的衍生物，喹唑啉衍生物和 喹啉衍生物和几种天然产物如氨基前列腺素。 磷酸肽类似物包括基于膦酸酯的磷酸酪氨酸模拟物，例如膦酰基甲基苯丙氨酸（Pmp）及其类似物，羧酸基磷酸酪氨酸模拟物如丙二酰基酪氨酸或苯丙氨酸类似物及其衍生物如羧甲基苯丙氨酸，不带电荷的pTyr模拟物和配对限制肽。 磷酸肽或磷酸肽模拟物抑制Src激酶SH2结构域。

公开(公告)号：US09296776B2

公开(公告)日：2016-03-29

申请号：US12668262

申请日：2008-07-09

Applicant: Gustavo F. Doncel ,  Keykavous Parang ,  Hitesh Kumar Agarwal

Inventor： Gustavo F. Doncel ,  Keykavous Parang ,  Hitesh Kumar Agarwal

IPC: C07H19/06 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

CPC classification number: C07H19/06 ,  C07D411/04 ,  C07H19/10 ,  C07H19/16 ,  C07H19/20

Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.

Abstract translation: 本发明涉及脂肪酸和脂肪醇取代的核苷衍生物以及在多价支架（例如，聚合物，肽，多羧酸取代的化合物，含有多环维生素基团的化合物）上取代的核苷和核苷衍生物，其显示有效的抗HIV活性。 此外，它们显示增强的抗多药耐药性，R5和细胞相关病毒的活性。 其中一些还显示针对其他性传播病原体和精子的活动。 本发明提供了它们的合成方法，物质组成和使用方法。 强调其作为局部杀微生物剂的应用，以治疗或预防疾病，特别是艾滋病毒/艾滋病的性传播。

公开(公告)号：US07799753B2

公开(公告)日：2010-09-21

申请号：US11565914

申请日：2006-12-01

Applicant: Keykavous Parang ,  Gongqin Sun ,  Anil Kumar ,  Nguyen H. Nam ,  Yue-Hao Wang ,  Guofeng Ye

Inventor： Keykavous Parang ,  Gongqin Sun ,  Anil Kumar ,  Nguyen H. Nam ,  Yue-Hao Wang ,  Guofeng Ye

IPC: A61K38/00

CPC classification number: A61K31/70 ,  A61K47/549 ,  A61K47/62

Abstract: A bisubstrate inhibitor of Src kinases, having a nucleotide or N-heteroaromatic moiety; and a peptide/phosphopeptide, peptidomimetic, or phosphopeptide mimic moiety. The moieties are linked by a rigid or a flexible linker. The nucleotide or N-heteroaromatic moiety is ATP, ATP-mimics, N-heteroaromatics including purine-based derivatives, pyrimidine-based derivatives such as 2,4-diamino-5-substituted pyrimidine derivatives, pyrazole[3,4-d]pyrimidine derivatives, pyrrolo[2,3-d]pyrimidine derivatives, pyrido[2,3-d]pyrimidine derivatives, amino-substituted dihydropyrimido[4,5-d]pyrimidinone derivatives, thieno- and furo-substituted derivatives, quinazoline derivatives, and quinoline derivatives, and several natural products such as aminogenistein. The phosphopeptide mimics comprise phosphonate-based phosphotyrosine mimetics such as phosphonomethylphenylalanine (Pmp) and its analogues, carboxylic acid-based phosphotyrosine mimetics such as malonyltyrosine or phenylalanine analogues and their derivatives such as carboxymethyl phenylalanine, uncharged pTyr mimetics, and conformationally constrained peptides. The phosphopeptide or phosphopeptide mimics inhibits the Src kinases SH2 domain.

Abstract translation: 具有核苷酸或N-杂芳族部分的Src激酶的双底物抑制剂; 和肽/磷酸肽，拟肽或磷酸肽模拟部分。 这些部分通过刚性或柔性接头连接。 核苷酸或N-杂芳族部分是ATP，ATP-模拟物，包括嘌呤类衍生物的N-杂芳族化合物，嘧啶类衍生物如2,4-二氨基-5-取代的嘧啶衍生物，吡唑[3,4-d]嘧啶 衍生物，吡咯并[2,3-d]嘧啶衍生物，吡啶并[2,3-d]嘧啶衍生物，氨基取代的二氢嘧啶并[4,5-d]嘧啶酮衍生物，噻吩并呋喃基取代的衍生物，喹唑啉衍生物和 喹啉衍生物和几种天然产物如氨基前列腺素。 磷酸肽类似物包括基于磷酸酯的磷酸酪氨酸模拟物，例如膦酰基甲基苯丙氨酸（Pmp）及其类似物，羧酸基磷酸酪氨酸模拟物如丙二酰基酪氨酸或苯丙氨酸类似物及其衍生物如羧甲基苯丙氨酸，不带电的pTyr模拟物和构象约束肽。 磷酸肽或磷酸肽模拟物抑制Src激酶SH2结构域。

公开(公告)号：US20080207551A1

公开(公告)日：2008-08-28

申请号：US11972254

申请日：2008-01-10

Applicant: Keykavous Parang ,  Yousef Ahamdibeni

Inventor： Keykavous Parang ,  Yousef Ahamdibeni

IPC: A61K31/70 ,  C07H21/04

CPC classification number: C07H21/02

Abstract: The synthesis and biochemical utility of modified oligonucleotides containing diphosphodiester internucleotide linkages. The synthesis of these compounds was carried out using diphosphitylating reagents. Oligonucleotides containing diphosphate diester bridges wherein said oligonucleotides are synthesized via a solid-phase synthesis strategy to form modified oligonucleotides. Diphosphitylating, triphosphitylating, tetraphosphitylating, β-triphosphitylating, bifunctional diphosphitylating, bifunctional triphosphitylating, and bifunctional tetraphosphitylating reagents wherein, the phosphorus atoms are linked together through oxygen, sulfur, amino, or methylene groups and/or are substituted with chlorine, diisopropylamine and cyanoethoxy groups.

Abstract translation: 含有二磷酸二酯核苷酸键的修饰寡核苷酸的合成和生物化学实用性。 这些化合物的合成使用二磷酸化试剂进行。 含有二磷酸二酯桥的寡核苷酸，其中所述寡核苷酸通过固相合成策略合成以形成修饰的寡核苷酸。 双磷化，三磷酸化，四磷酸化，β-三磷酸化，双功能二磷酸化，双功能三磷酸化，双功能四磷酸化试剂，其中磷原子通过氧，硫，氨基或亚甲基连接在一起，和/或被氯，二异丙胺和氰基乙氧基取代 。

公开(公告)号：US07351731B2

公开(公告)日：2008-04-01

申请号：US11289348

申请日：2005-11-29

Applicant: Keykavous Parang ,  Soroush Sardari ,  Nguyen Hai Nam

Inventor： Keykavous Parang ,  Soroush Sardari ,  Nguyen Hai Nam

IPC: A61K31/4196 ,  C07D249/08

CPC classification number: C07D249/08 ,  C07D403/06 ,  C07F9/6518 ,  C07F9/65586

Abstract: The present invention is broadly directed to azole derivatives that exhibit antifungal activity and methods for making the same. In one aspect, the invention includes carboxylic acid and phosphate ester derivatives of fluconazole that exhibit antifungal activity. In addition, the invention comprises methods for synthesizing the derivatives and pharmaceutical compositions containing the derivatives.

Abstract translation: 本发明广泛涉及显示抗真菌活性的唑衍生物及其制备方法。 一方面，本发明包括具有抗真菌活性的氟康唑的羧酸和磷酸酯衍生物。 此外，本发明包括合成衍生物的方法和含有衍生物的药物组合物。

公开(公告)号：US20150038671A1

公开(公告)日：2015-02-05

申请号：US14292745

申请日：2014-05-30

Applicant: Keykavous Parang ,  Rakesh Tiwari

Inventor： Keykavous Parang ,  Rakesh Tiwari

IPC: C07K7/56

CPC classification number: C07K7/56 ,  C07K7/06

Abstract: Synthesized macrocyclic ligand, CN2097 and analogs, optimized with systemic structure modifications to develop the compounds with lower molecular weights and less peptidic characters.

Abstract translation: 合成的大环配体CN2097和类似物，用系统结构修饰进行优化，以开发具有较低分子量和较少肽性质的化合物。

公开(公告)号：US20140336259A1

公开(公告)日：2014-11-13

申请号：US14125237

申请日：2012-06-11

Applicant: Navindra Seeram ,  Julie Barbeau ,  Genevieve BeLand ,  Keykavous Parang

Inventor： Navindra Seeram ,  Julie Barbeau ,  Genevieve BeLand ,  Keykavous Parang

IPC: C07C67/343 ,  C07C39/15 ,  C07C41/30 ,  C07C41/22 ,  C07C41/26 ,  C07C59/68 ,  C07C43/205

CPC classification number: C07C67/343 ,  A61K31/05 ,  A61K31/085 ,  A61K31/216 ,  C07C39/15 ,  C07C41/22 ,  C07C41/26 ,  C07C41/30 ,  C07C43/2055 ,  C07C43/23 ,  C07C59/68 ,  C07C69/734

Abstract: The present document describes a phytochemical isolated from maple syrup and composition comprising the same. More specifically, the document describes an antioxidant phytochemical compound, derivates thereof, and composition comprising the same. The document also describes a process of synthesizing the antioxidant phytochemical compound.

Abstract translation: 本文件描述了从枫糖浆中分离的植物化学物质和包含其的组合物。 更具体地，该文献描述了抗氧化植物化学化合物，其衍生物和包含其的组合物。 该文献还描述了合成抗氧化植物化学化合物的方法。