公开(公告)号：US20030216481A1

公开(公告)日：2003-11-20

申请号：US10427746

申请日：2003-04-30

Applicant: UNIGEN PHARMACEUTICALS, INC.

Inventor： Qi Jia

IPC: A61K031/05 ,  A01N031/08

CPC classification number: A61K36/539 ,  A61K31/35 ,  A61K31/353 ,  A61K31/7048 ,  A61K36/11 ,  A61K36/15 ,  A61K36/185 ,  A61K36/28 ,  A61K36/47 ,  A61K36/48 ,  A61K36/484 ,  A61K36/486 ,  A61K36/53 ,  A61K36/54 ,  A61K36/60 ,  A61K36/74 ,  A61K36/906 ,  A61K36/9062

Abstract: The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compoundsnullFree-B-ring flavonoids and flavansnullfor use in the prevention and treatment of diseases and conditions mediated by the COX-2 and 5-LO pathways. The present invention further provides a novel method for simultaneously inhibiting the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) enzymes, and reducing cox-2 mRNA production. Finally, the present invention includes a method for weight loss and blood glucose control. The methods of this invention are comprised of administering to a host in need thereof an effective amount of the composition of this invention together with a pharmaceutically acceptable carrier. This invention relates generally to the prevention and treatment of diseases and conditions mediated by the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) pathways, including but not limited to the relief joint discomfort and pain associated with conditions such as osteoarthritis, rheumatoid arthritis, and other injuries that result from overuse.

公开(公告)号：US20040186062A1

公开(公告)日：2004-09-23

申请号：US10785704

申请日：2004-02-24

Applicant: UNIGEN PHARMACEUTICALS, INC.

Inventor： Bruce P. Burnett ,  Qi Jia

IPC: A61K031/7048 ,  A61K031/353

CPC classification number: A61K36/906 ,  A61K31/352 ,  A61K31/366 ,  A61K36/11 ,  A61K36/15 ,  A61K36/185 ,  A61K36/28 ,  A61K36/47 ,  A61K36/48 ,  A61K36/484 ,  A61K36/486 ,  A61K36/53 ,  A61K36/539 ,  A61K36/54 ,  A61K36/60 ,  A61K36/9062 ,  A61K2300/00

Abstract: The present invention provides a novel method for inhibiting sugar-induced weight gain resulting from fructose and glucose driven lipogenesis. The method for inhibiting sugar-induced weight gain is comprised of administering a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the Scutellaria and Acacia genus of plants to a host in need thereof. The present also includes novel methods for the prevention and treatment of diseases and conditions resulting from high carbohydrate ingestion. The method for preventing and treating these sugar-induced diseases and conditions is comprised of administering to a host in need thereof a therapeutically effective amount of a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the Scutellaria and Acacia genus of plants and a pharmaceutically acceptable carrier.

Abstract translation: 本发明提供了抑制由果糖和葡萄糖驱动的脂肪生成引起的糖诱导的体重增加的新方法。 用于抑制糖诱导的体重增加的方法包括施用包含游离B环类黄酮和从单一植物或多种植物合成和/或分离的黄酮的混合物，优选在植物的黄芩和相思属中分离的组合物的组合物 需要的主机。 本发明还包括用于预防和治疗由高碳水化合物摄取引起的疾病和病症的新方法。 用于预防和治疗这些糖诱发的疾病和病症的方法包括向有需要的宿主施用治疗有效量的组合物，其包含游离B环类黄酮和从单一的合成和/或分离的黄烷的混合物 植物或多种植物，优选在植物的黄芩和相思属中以及药学上可接受的载体。

公开(公告)号：US20030165588A1

公开(公告)日：2003-09-04

申请号：US10091362

申请日：2002-03-01

Applicant: UNIGEN PHARMACEUTICALS, INC.

Inventor： Qi Jia ,  Timothy C. Nichols ,  Eric E. Rhoden ,  Scott Waite

IPC: A61K035/78

CPC classification number: A61K31/7048 ,  A61K31/353 ,  A61K36/18

Abstract: The present invention provides a novel method for inhibiting the cyclooxygenase COX-2. The method is comprised of administering a composition containing a Free-enzyme B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 mediated diseases and conditions. The method for preventing and treating COX-2 mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition containing a Free-B-Ring flavonoid or a composition containing a mixture of Free-B-Ring flavonoids and a pharmaceutically acceptable carrier.

Abstract translation: 本发明提供抑制环加氧酶COX-2的新方法。 该方法包括将含有游离酶B环类黄酮或含有游离B环类黄酮的混合物的组合物给予需要其的宿主的组合物。 本发明还包括预防和治疗COX-2介导的疾病和病症的新方法。 预防和治疗COX-2介导的疾病和病症的方法包括向有需要的宿主施用有效量的含有游离B环类黄酮或含有游离B环类黄酮混合物的组合物 和药学上可接受的载体。

公开(公告)号：US20040152787A1

公开(公告)日：2004-08-05

申请号：US10658881

申请日：2003-09-09

Applicant: UniGen Pharmaceuticals, Inc.

Inventor： Qi Jia ,  Ji-Fu Zhao

IPC: C07C039/16 ,  A61K031/045

CPC classification number: A61K31/045 ,  Y10S514/925 ,  A61K2300/00

Abstract: The present invention provides a novel method for the preparation of a unique profile of primary aliphatic alcohols having 24 to 30 carbon atoms, from the wax secreted by the insect Ericerus pela. Included in the present invention is the composition of matter, referred to herein as nullpolycosanolnull produced by the method of this invention. The polycosanol composition is comprised primarily of the four primary aliphatic alcohols, tetracosanol, hexacosanol, octacosanol and triacontanol. Further included in this invention is the use of said composition of matter for the prevention and treatment of obesity, syndrome X, diabetes, hypercholesterolemia, atherosclerotic complications, ischemia and thrombosis.

Abstract translation: 本发明提供一种制备由昆虫埃里克木虱分泌的蜡的具有24-30个碳原子的伯脂肪醇的独特分布的新方法。 本发明中包括由本发明的方法生产的物质组合物，这里称为“多可醇”。 多糖醇组合物主要由四种脂族醇，二十四烷醇，二十四烷醇，三十烷醇组成。 本发明还包括所述物质组合物用于预防和治疗肥胖症，综合征X，糖尿病，高胆固醇血症，动脉粥样硬化并发症，局部缺血和血栓形成的用途。

公开(公告)号：US20030232763A1

公开(公告)日：2003-12-18

申请号：US10462030

申请日：2003-06-13

Applicant: Unigen Pharmaceuticals, Inc.

Inventor： Qi Jia

IPC: A61K031/7048 ,  A61K031/353

CPC classification number: A61K36/539 ,  A61K31/35 ,  A61K31/353 ,  A61K31/7048 ,  A61K36/11 ,  A61K36/15 ,  A61K36/185 ,  A61K36/28 ,  A61K36/47 ,  A61K36/48 ,  A61K36/484 ,  A61K36/486 ,  A61K36/53 ,  A61K36/54 ,  A61K36/60 ,  A61K36/74 ,  A61K36/906 ,  A61K36/9062

Abstract: The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compoundsnullFree-B-ring flavonoids and flavansnullfor use in the prevention and treatment of diseases and conditions mediated by the COX-2 and 5-LO pathways. The present invention further provides a novel method for simultaneously inhibiting the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) enzymes, and reducing cox-2 mRNA production. Finally, the present invention includes a method for weight loss and blood glucose control. The methods of this invention are comprised of administering to a host in need thereof an effective amount of the composition of this invention together with a pharmaceutically acceptable carrier. This invention relates generally to the prevention and treatment of diseases and conditions mediated by the cyclooxygenase-2 (COX-2) and 5-lipoxygenase (5-LO) pathways, including but not limited to the relief joint discomfort and pain associated with conditions such as osteoarthritis, rheumatoid arthritis, and other injuries that result from overuse.

Abstract translation: 本发明提供由两种特定类别的化合物 - 游离B-环类黄酮和黄烷的混合物组成的新型组合物，用于预防和治疗由COX-2和5-LO介导的疾病和病症 途径。 本发明还提供了同时抑制环氧合酶-2（COX-2）和5-脂氧合酶（5-LO）酶，降低cox-2 mRNA产生的新方法。 最后，本发明包括减肥和血糖控制的方法。 本发明的方法包括向有需要的宿主施用有效量的本发明组合物和药学上可接受的载体。 本发明一般涉及由环氧合酶-2（COX-2）和5-脂氧合酶（5-LO）途径介导的疾病和病症的预防和治疗，包括但不限于与这样的病症有关的救济关节不适和疼痛 作为骨关节炎，类风湿性关节炎以及过度使用引起的其他损伤。

公开(公告)号：US20040220119A1

公开(公告)日：2004-11-04

申请号：US10817330

申请日：2004-04-02

Applicant: Unigen Pharmaceuticals, Inc.

Inventor： Qi Jia

IPC: A61K031/7048 ,  A61K031/353

CPC classification number: A61K8/97 ,  A61K8/498 ,  A61K8/67 ,  A61K31/352 ,  A61K31/353 ,  A61K31/7048 ,  A61K36/11 ,  A61K36/15 ,  A61K36/185 ,  A61K36/28 ,  A61K36/47 ,  A61K36/48 ,  A61K36/484 ,  A61K36/486 ,  A61K36/53 ,  A61K36/539 ,  A61K36/54 ,  A61K36/60 ,  A61K36/906 ,  A61K36/9062 ,  A61K45/06 ,  A61K2800/782 ,  A61Q19/00 ,  A61Q19/004 ,  A61Q19/08 ,  A61K2300/00

Abstract: The present invention provides a novel composition of matter comprised of a mixture of two specific classes of compoundsnullFree-B-Ring flavonoids and flavansnullfor use in the prevention and treatment of diseases and conditions associated with the skin. This composition of matter simultaneously inhibits cyclooxygenase (COX) and lipoxygenase (LOX) enzymatic activity in normal, aged and damaged dermal cells and tissues. This invention further provides a method for the prevention and treatment of diseases and conditions of the skin mediated by cyclooxygenase (COX) and lipoxygenase (LOX). The method for preventing and treating COX and LOX mediated diseases and conditions of the skin is comprised of topically administering to a host in need thereof a therapeutically effective amount of a composition comprising a mixture of Free-B-Ring flavonoids and flavans synthesized and/or isolated from a single plant or multiple plants, preferably in the Scutellaria and Acacia genus of plants and pharmaceutically and/or cosmetically acceptable carriers. Finally the present invention provides a method for the prevention and treatment of COX and LOX mediated diseases and conditions, including but not limited to sun burns, thermal burns, acne, topical wounds, minor inflammatory conditions caused by fungal, microbial and viral infections, vitilago, systemic lupus erythromatosus, psoriasis, carcinoma, melanoma, as well as other mammal skin cancers, skin damage resulting from exposure to ultraviolet (UV) radiation, chemicals, heat, wind and dry environments, wrinkles, saggy skin, lines and dark circles around the eyes, dermatitis and other allergy related conditions of the skin. Use of the composition described herein also affords the benefit of smooth and youthful skin with improved elasticity, reduced and delayed aging, enhanced youthful appearance and texture, and increased flexibility, firmness, smoothness and suppleness.

公开(公告)号：US20030180402A1

公开(公告)日：2003-09-25

申请号：US10104477

申请日：2002-03-22

Applicant: UNIGEN PHARMACEUTICALS, INC.

Inventor： Qi Jia ,  Timothy C. Nichols ,  Eric E. Rhoden ,  Scott Waite

IPC: A61K035/78 ,  A61K031/33

CPC classification number: A61K31/353 ,  A61K31/33 ,  A61K36/00 ,  A61K36/48

Abstract: The present invention provides a novel method for simultaneously inhibiting the cyclooxygenase COX-2 and 5-lipoxygenase (5-LO) enzymes. The method for the simultaneous dual inhibition of COX-2 and 5-LO is comprised of administering a composition containing an individual and/or a mixture of multiple flavans isolated from a single plant or multiple plants in the Acacia genus of plants to a host in need thereof. The present also includes novel methods for the prevention and treatment of COX-2 and 5-LO mediated diseases and conditions. The method for preventing and treating COX-2 and 5-LO mediated diseases and conditions is comprised of administering to a host in need thereof an effective amount of a composition comprising an individual and/or a mixture of multiple flavans isolated from a single plant or multiple plants in the Acacia genus of plants and a pharmaceutically acceptable carrier. The present invention includes a method for isolating and purifying a composition of flavans having dual specificity for COX-2 and 5-LO from the Acacia genus of plants.

Abstract translation: 本发明提供了同时抑制环氧合酶COX-2和5-脂氧合酶（5-LO）酶的新方法。 同时双重抑制COX-2和5-LO的方法包括将含有单个植物的多种黄烷和/或从植物相思树属中的多种植物分离的多种黄烷的混合物的组合物施用于宿主 需要。 本发明还包括预防和治疗COX-2和5-LO介导的疾病和病症的新方法。 预防和治疗COX-2和5-LO介导的疾病和病症的方法包括向有需要的宿主施用有效量的组合物，其包含从单一植物分离的个体和/或多种黄烷的混合物或 植物相思树属植物多种植物和药学上可接受的载体。 本发明包括分离和纯化来自植物相思树属的COX-2和5-LO双重特异性的黄烷组合物的方法。

公开(公告)号：US20030113797A1

公开(公告)日：2003-06-19

申请号：US10185758

申请日：2002-06-27

Applicant: UNIGEN PHARMACEUTICALS, INC.

Inventor： Qi Jia ,  Mei-Feng Hong

IPC: G01N033/53 ,  G01N033/543 ,  A61K035/78

CPC classification number: G01N30/88 ,  A61K36/00 ,  C12Q1/025 ,  C40B40/04 ,  G01N30/02 ,  G01N33/5097 ,  G01N33/6842 ,  G01N2030/8813 ,  G01N2500/00 ,  A61K2300/00 ,  B01D15/322 ,  B01D15/325 ,  G01N33/15

Abstract: The present invention relates generally to a technology platform, referred to as Phytologixnull for the discovery of novel bioactive pharmaceutical, nutraceutical and cosmetic agents. Specifically, this invention includes an integrated system for the collection of medicinal plants and creation of informatic databases related to these plants. This invention also relates to an improved standardized extraction and fractionation process, which provides significant advantages over the prior art in the terms of simplicity, efficiency of the separations, the quality of the library, low cost of the process and extraordinary throughput. This invention provides details to the structure dereplication process by utilizing the technology such as HPLC/PDA/MS coupled with high throughput bioassay data and an internal pure compound library. It has been proven to be much more efficient and accurate when compared to the prior art methods. Finally, the Phytologixnull platform has been approved as a realistic and efficient process by the demonstration of the whole process of discovery and development of natural COX-2 and tyrosinase inhibitors as novel nutraceutical and cosmetic products.

Abstract translation: 本发明一般涉及一种称为Phytologix TM的技术平台，用于发现新的生物活性药物，营养保健品和美容剂。 具体而言，本发明包括用于收集药用植物的综合系统和创建与这些植物有关的信息数据库。 本发明还涉及一种改进的标准化提取和分馏方法，其在简单性，分离效率，文库质量，低成本和非凡的生产量方面优于现有技术。 本发明通过利用与高通量生物测定数据耦合的HPLC / PDA / MS技术和内部纯化合物库来提供结构解除过程的细节。 与现有技术方法相比，已被证明是更有效和准确的。 最后，通过将天然COX-2和酪氨酸酶抑制剂的发现和开发的全过程展示为新型营养保健品和化妆品，Phytologix（TM）平台已经被批准为一个现实和有效的过程。