公开(公告)号：US09822136B2

公开(公告)日：2017-11-21

申请号：US14998864

申请日：2016-02-23

申请人： Edward T. Wei ,  Seong J. Kim

发明人： Edward T. Wei ,  Seong J. Kim

IPC分类号： A61Q19/00 ,  A61K8/55 ,  A61K31/683 ,  C07F9/53 ,  A61K9/00

CPC分类号： C07F9/5304 ,  A61K8/55 ,  A61K9/0014 ,  A61K9/12 ,  A61K31/683 ,  A61K2800/244 ,  A61Q19/00 ,  A61Q19/008

摘要： The present discovery pertains to the discovery of certain amphiphilic compounds that may be useful for the management of sebum secretion in subjects with acne, oily skin, or seborrheic dermatitis. These compounds are 1-dialkylphosphorylalkanes with the longest alkyl group being seven or more carbons. Preferably, a compound is dissolved in a dermatologically acceptable vehicle, and delivered to the skin in a solution, gel, lotion, cream, or ointment. The method of application may be with the surface of the finger, or via an applicator. The decrease is sebum secretion in certain subjects may result in skin conditions that enhance cosmetic appearance and ameliorate skin disorders.

公开(公告)号：US20170240575A1

公开(公告)日：2017-08-24

申请号：US14998864

申请日：2016-02-23

申请人： Edward T. Wei ,  Seong J. Kim

发明人： Edward T. Wei ,  Seong J. Kim

IPC分类号： C07F9/53 ,  A61Q19/00 ,  A61K8/55 ,  A61K9/00 ,  A61K31/662

CPC分类号： C07F9/5304 ,  A61K8/55 ,  A61K9/0014 ,  A61K9/12 ,  A61K31/683 ,  A61K2800/244 ,  A61Q19/00 ,  A61Q19/008

摘要： The present discovery pertains to the discovery of certain amphiphilic compounds that may be useful for the management of sebum secretion in subjects with acne, oily skin, or seborrheic dermatitis. These compounds are 1-dialkylphosphorylalkanes with the longest alkyl group being seven or more carbons. Preferably, a compound is dissolved in a dermatologically acceptable vehicle, and delivered to the skin in a solution, gel, lotion, cream, or ointment. The method of application may be with the surface of the finger, or via an applicator. The decrease is sebum secretion in certain subjects may result in skin conditions that enhance cosmetic appearance and ameliorate skin disorders.

公开(公告)号：US09895382B2

公开(公告)日：2018-02-20

申请号：US15330573

申请日：2016-10-13

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A61K31/662 ,  A61K31/66 ,  A61K49/00 ,  A61K9/00 ,  C07F9/53 ,  A61K9/70 ,  G01N33/68

CPC分类号： A61K31/662 ,  A61K9/0014 ,  A61K9/7023 ,  A61K31/66 ,  A61K49/00 ,  C07F9/5304 ,  C07F9/532 ,  G01N33/6872 ,  G01N33/6896 ,  G01N2333/705 ,  G01N2800/2842

摘要： The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to certain di-isopropyl-phosphinoyl-alkanes as described herein, DIPA-1-5, DIPA-1-6, DIPA-1-7, DIPA-1-8, and DIPA-1-9, collectively referred to herein as “DIPA compounds”, that are useful, for example, in the treatment of disorders (e.g., diseases) including: sensory discomfort (e.g., caused by irritation, itch, or pain); a skin dysesthesia; dermatitis; ocular pain and discomfort; heat discomfort; heat stress; flushing and/or night sweats (vasomotor symptoms); post-operative hypothermia; post-anaesthetic shivering; nasal congestion and nasal obstruction; pharyngeal and esophageal discomfort; fatigue; tiredness; depression; cognitive dysfunction; and to enhance cognitive function. The applicant has found that localized delivery of DIPA compounds to the upper eyelid and/or facial skin has an alerting and enhancement effect on behavior and can be used to give a cosmetic refreshing look, to mental alertness, to reduce fatigue, and to improve work output. The present discovery also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy, in diagnosis of neuropathic pain, and in study of TRPM8 function.

公开(公告)号：US20150105349A1

公开(公告)日：2015-04-16

申请号：US13987657

申请日：2013-08-19

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A61K31/662 ,  A61K31/047 ,  A61K31/045 ,  A61K31/22 ,  A61K31/166

CPC分类号： A61K31/662 ,  A61K31/045 ,  A61K31/047 ,  A61K31/166 ,  A61K31/22

摘要： Short-chain 2- to 3-carbon alcohols are used as solvents for cooling agents in the preparation of topical therapeutic and cosmetic formulations. Some of these alcohols, especially ethanol, inhibit the ability of the cooling agent to activate its target receptor. In one embodiment of this invention, (R)-1,2-propanediol is used as an alcoholic solvent for the topical delivery of cooling agents to biological surfaces. This (R)-1,2-propanediol enantiomer has a minimum inhibitory effect on cooling with respect to standard 2- to 3-carbon alcoholic solvents, and functions to substantially protect the agents cooling activity from inhibition when in the presence of a short-chain alcohol such as ethanol.

摘要翻译： 短链2-至3-碳醇用作制备局部治疗和化妆品制剂中的冷却剂的溶剂。 这些醇，特别是乙醇中的一些，抑制冷却剂活化其目标受体的能力。 在本发明的一个实施方案中，（R）-1,2-丙二醇用作用于将冷却剂局部递送到生物表面的醇溶剂。 该（R）-1,2-丙二醇对映异构体对于标准2-至3-碳醇溶剂的冷却具有最小的抑制作用，并且在短时间存在下基本保护试剂冷却活性不受抑制， 链醇如乙醇。

公开(公告)号：US5306710A

公开(公告)日：1994-04-26

申请号：US876487

申请日：1992-04-30

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A01D1/02 ,  A01N1/02 ,  A61K38/22 ,  A61P3/00 ,  C07K14/575 ,  A61K37/40

CPC分类号： A61K38/2228 ,  A01N1/021 ,  A01N1/0226

摘要： Administration of a Corticotropin-Releasing Factor (or a salt or analog thereof) decreases the leakage of blood components into brain tissue produced by various adverse medical conditions and reduces bleeding when muscle tissues are cut and handled, such as in plastic and reconstructive surgery. A method of treating a patient for injury to or disease of the brain, central nervous system, or musculature in which edema is a factor comprises administering to the patient a Corticotropin-Releasing Factor (or a salt or analog) in an amount effective to decrease vascular permeability in the injured or diseased brain, nervous system tissue or musculature, and thereby to reduce edema. Administration in accordance with the method can be about two hours before surgery, or can be up to three days after injury.

摘要翻译： 促肾上腺皮质激素释放因子（或其盐或类似物）的施用减少了由各种不利的医学条件产生的血液成分渗透到脑组织中，并且在肌肉组织被切割和处理时减少出血，例如在塑性和重建手术中。 治疗患者对水肿是水肿的脑，中枢神经系统或肌肉组织的损伤或疾病的方法包括向患者施用有效降低的量的促肾上腺皮质激素释放因子（或盐或类似物） 损伤或患病的脑，神经系统组织或肌肉组织中的血管通透性，从而减少水肿。 按照方法管理可以在手术前约两个小时，否则可能在伤后三天内。

公开(公告)号：US5177060A

公开(公告)日：1993-01-05

申请号：US462578

申请日：1990-01-09

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A61K38/00 ,  A61P29/00 ,  C07K7/06 ,  C07K14/575

CPC分类号： C07K14/57509 ,  A61K38/00

摘要： Relatively small, synthetic anti-inflammatory peptides are provided having the primary sequenceT.sub.N --A.sub.1 --A.sub.2This invention was made with Government support under Grant No. DA-00091 awarded by the National Institutes of Health. The Government has certain rights in this invention.

摘要翻译： 提供了相对较小的合成抗炎肽，其具有其中TN是氨基酸部分的一级序列TN-A1-A2-A3-A4-A5-A6-TC，A1至A6各自为合成或天然氨基酸 D-或L-构型，TC是酰胺化羧基末端部分的一部分或包含酰胺化的羧基末端部分。 A1，A2和A5中的每一个是极性氨基酸，而A3，A4和A6中的每一个是非极性氨基酸。 这些相对小的合成肽抑制血管渗漏，并且有用地施用于哺乳动物用于诸如治疗与脑，皮肤，粘膜和肌肉组织损伤相关的水肿的应用。

公开(公告)号：US4481191A

公开(公告)日：1984-11-06

申请号：US480691

申请日：1983-03-30

申请人： Edward T. Wei ,  Nancy M. Lee ,  Jaw-Kang Chang

发明人： Edward T. Wei ,  Nancy M. Lee ,  Jaw-Kang Chang

IPC分类号： A61K38/00 ,  A61P9/06 ,  A61P9/12 ,  C07K14/665 ,  A61K37/00 ,  C07C103/52

CPC分类号： C07K14/665 ,  A61K38/00

摘要： A method is provided for treating high blood pressure and disturbances of cardiac function by administering a therapeutically effective dosage of dynorphin-related opioid peptides, such as dynorphin(1-13) and dynorphin(1-10) amide, having at least ten amino acids linked sequentially by peptide bonds and with the five amino acids from the N-terminal end being the same as, or mimicking, Leu-enkephalin. Administration may be over a period of time, as for individuals with chronic high blood pressure, and may be by dispensing the medicament in aerosol form.

摘要翻译： 提供了一种治疗高血压和心脏功能紊乱的方法，其通过施用治疗有效剂量的强啡肽相关阿片肽，例如具有至少十个氨基酸的强啡肽（1-13）和强啡肽（1-10）酰胺） 通过肽键顺序连接，并且来自N-末端的五个氨基酸与Leu-脑啡肽相同或模仿。 对于具有慢性高血压的个体，给药可以是一段时间，并且可以通过以气溶胶形式分配药物。

公开(公告)号：US20220265687A1

公开(公告)日：2022-08-25

申请号：US17803311

申请日：2022-05-03

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A61K31/662 ,  A61K9/00 ,  A61P17/04

摘要： The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to certain di-isopropyl-phosphinoyl-alkanes as described herein, DIPA-1-7, DIPA-1-8, and DIPA-1-9, collectively referred to herein as “DIPA compounds”, that are useful, for example, in the treatment of the discomforts of dermatological disorders (e.g., diseases) The treatment is for the dysesthesia (e.g., caused by irritation, itch, or pain) due to dermatitis, urticaria; scalp itch; vulvar itch; lichen sclerosus; cholestatic itch; psoriasis; sebhorrheic dermatitis; allergic conjunctivitis; blepharitis; and pruritus of the elderly. The applicant has found that topical delivery of DIPA compounds to the skin alleviates the dysesthesia of these conditions in human subjects. The present discovery pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in the treatment of the dysesthesia of these dermatological disorders.

公开(公告)号：US20200261477A1

公开(公告)日：2020-08-20

申请号：US16602539

申请日：2019-10-25

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A61K31/662 ,  A61K9/00 ,  A61P11/00

摘要： The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to a particular 1-di-alkyl-phosphinoyl-alkane, 1-(Diisopropyl-phosphinoyl)-nonane, referred to herein as “DIPA-1-9”. DIPA-1-9, is able to selectively treat (e.g., suppress) sensory discomfort arising from the airways without side effects. Compared to structurally similar compounds, DIPA-1-9 did not have the problems of excessive cold, stinging, or irritancy, or of adverse taste. To deliver the DIPA-1-9 to the upper airway it is formulated as a solution of DIPA-1-9 in water, a water-based solution, or syrup, at a concentration of 2 to 10 mg/mL and a delivery volume of less than 0.5 mL per unit dose. The drops of DIPA-1-9 are administered into the nasal cavity or onto the base of the tongue, next to the pillars of fauces. The DIPA-1-9 then reaches the nerve endings at the base of the epithelia and transduces signals of coolness and cold. Cooling of the upper airways relieves discomfort and is useful for conditions such as throat irritation, cough, pharyngitis, and lower airway blockage disorders. The elicitation of cooling in the upper airways can be used to control cough, to treat dyspnea, and to enhance mucus clearance in lower airway disorders such as chronic obstructive pulmonary diseases (which includes bronchitis and bronchiectasis), asthma, interstitial lung diseases, cystic fibrosis, lung fibrosis, pneumonia, and other lung disorders. The efficacy of DIPA-1-9 in treating chronic obstructive pulmonary disease is especially attractive because the four primary signs of chronic obstructive pulmonary disease, cough, excessive sputum production, dyspnea, and psychic distress from the lack of control of airway discomfort, are favorably ameliorated by topical application of DIPA-1-9 to the upper airways. This method of treating chronic obstructive pulmonary disease with a cooling agent to the upper airways has not been previously described.

公开(公告)号：US20150265752A1

公开(公告)日：2015-09-24

申请号：US14545014

申请日：2015-03-16

申请人： Edward T. Wei

发明人： Edward T. Wei

IPC分类号： A61L31/16 ,  A61K31/66 ,  A61K9/00 ,  A61L31/14

CPC分类号： A61K31/66 ,  A61K9/0031 ,  A61K9/0043 ,  A61K9/0053 ,  A61K47/02 ,  A61M35/006 ,  A61M2210/0618

摘要： The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to certain di-alkyl-phosphinoyl-alkanes as described herein, DIPA-1-8 and DIPA-1-9, and 2-6 and 2-7 that are collectively referred to herein as “DAPA compounds”, that are useful in the treatment of disorders (e.g., diseases) including: sensory discomfort (e.g., caused by inflammation, irritation, itch, or pain) in the nasal cavity. The applicant has found that localized delivery of DAPA compounds with a swab to the Kiesselbach's area of the human nose will relieve the discomforts of rhinitis and other nasal cavity discomforts.

摘要翻译： 本发明一般涉及治疗化合物领域。 更具体地，本发明涉及本文所述的某些二烷基 - 膦酰基烷烃，DIPA-1-8和DIPA-1-9以及2-6和2-7，其在本文中统称为“DAPA化合物” ，其可用于治疗包括鼻腔中的感觉不适（例如，由炎症，刺激，瘙痒或疼痛引起）的疾病（例如疾病）。 申请人已经发现，使用棉签将DAPA化合物局部递送到Kiesselbach的人鼻区域可缓解鼻炎和其他鼻腔不适的不适。