公开(公告)号：US06649654B1

公开(公告)日：2003-11-18

申请号：US09721380

申请日：2000-11-22

申请人： Michael Karin ,  Pankaj Kapahi

发明人： Michael Karin ,  Pankaj Kapahi

IPC分类号： A01N3708

CPC分类号： A61K31/557 ,  A61K31/00 ,  A61K31/5575 ,  C12Q1/485 ,  G01N2500/04

摘要： The present invention provides methods and compositions for inhibiting IKK, as well as methods and compositions for identifying compounds with activity as inhibitors of IKK, and methods and compositions for the treatment of diseases and/or conditions wherein IKK is implicated and inhibition of its activity is desired. In addition, the present invention provides methods and compositions for the improving the therapeutic activity of COX2 inhibitors, comprising administering the COX2 to a subject in combination with a compound that inhibits IKK activity. The present invention further provides compositions that comprise compounds that inhibit IKK and COX2.

公开(公告)号：US06566396B2

公开(公告)日：2003-05-20

申请号：US09727042

申请日：2000-11-30

申请人： Ronald J. Leflein ,  Alexander D. D'Addio

发明人： Ronald J. Leflein ,  Alexander D. D'Addio

IPC分类号： A01N3708

CPC分类号： A61K9/0095 ,  A61K9/2009 ,  A61K9/205 ,  A61K9/2054 ,  A61K31/7028 ,  A61K45/06 ,  Y10S514/85

摘要： Tannate compositions consisting essentially of carbetapentane tannate and chlorpheniramine tannate which are effective when administered orally for the symptomatic relief of coryza associated with the common cold, sinusitis, allergic rhinitis, unproductive cough and upper respiratory tract conditions are disclosed.

公开(公告)号：US06410591B1

公开(公告)日：2002-06-25

申请号：US09851296

申请日：2001-05-08

申请人： Robert M. Burk ,  Mark Holoboski ,  Mari F. Posner

发明人： Robert M. Burk ,  Mark Holoboski ,  Mari F. Posner

IPC分类号： A01N3708

CPC分类号： C07C405/0033 ,  A61K31/5575

摘要： The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma a therapeutically effective amount of a 3, 7 or 3 and 7 thia or oxa prostanoic acid derivative.

摘要翻译： 本发明提供一种治疗眼高血压或青光眼的方法，其包括向具有高眼压症或青光眼的动物施用治疗有效量的3,7或3和7和硫代前列腺酸衍生物。

公开(公告)号：US06569900B1

公开(公告)日：2003-05-27

申请号：US09807004

申请日：2001-07-09

申请人： Johannes Dekker ,  Constance Elizabeth Medlen

发明人： Johannes Dekker ,  Constance Elizabeth Medlen

IPC分类号： A01N3708

CPC分类号： A61K31/352 ,  Y02A50/473

摘要： Fulvic acid salts, esters or derivatives thereof in pharmaceutical preparations are effective for treating inflammation, acne, exzema or bacterial or fungal or viral infections. These pharmaceutical preparations may be given either orally or topically in the form of a solution, paste, ointment, powder to humans or animals.

摘要翻译： 药物制剂中的呋喃酸盐，酯或其衍生物对于治疗炎症，痤疮，湿疹或细菌或真菌或病毒感染是有效的。 这些药物制剂可以口服或局部给予溶液，糊剂，软膏，粉末给人或动物的形式。

公开(公告)号：US06395786B1

公开(公告)日：2002-05-28

申请号：US09701332

申请日：2000-11-27

申请人： Fumie Sato ,  Tohru Tanami ,  Kazuya Kameo ,  Kenji Yamada ,  Shigeru Okuyama ,  Naoya Ono

发明人： Fumie Sato ,  Tohru Tanami ,  Kazuya Kameo ,  Kenji Yamada ,  Shigeru Okuyama ,  Naoya Ono

IPC分类号： A01N3708

CPC分类号： A61K31/5575 ,  A61K31/557 ,  C07C405/00 ,  Y10S514/923

摘要： A sleep-inducing preparation which comprises as an effective ingredient a prostaglandin derivative represented by the formula: wherein X is a halogen atom, Y is a group represented by (CH2)m, a cis-vinylene group or a phenylene group, Z is an ethylene group, a trans-vinylene group, OCH2 or S(O)nCH2, R1 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C4-13 cycloalkylalkyl group, a C5-10 alkyl group, a C5-10 alkenyl group, a C5-10 alkynyl group or a bridged cyclic hydrocarbon group, R2 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 1 to 3, and n is 0, 1 or 2, a pharmaceutically acceptable salt thereof or a hydrate thereof.

摘要翻译： 一种睡眠诱导制剂，其包含作为有效成分的由下式表示的前列腺素衍生物：其中X是卤素原子，Y是由（CH 2）m表示的基团，顺式亚乙烯基或亚苯基，Z是 亚乙基，反亚乙烯基，OCH 2或S（O）n CH 2，R 1是C 3-10环烷基，被C 1-4烷基取代的C 3-10环烷基，C 4-13环烷基烷基， C5-10烷基，C5-10烯基，C5-10炔基或桥连环烃基，R2是氢原子，C1-10烷基或C3-10环烷基，m是 1〜3的整数，n为0,1或2，其药学上可接受的盐或其水合物。

公开(公告)号：US06316389B1

公开(公告)日：2001-11-13

申请号：US09202887

申请日：1997-06-16

申请人： Henry Szczepanski ,  Martin Zeller ,  Ottmar Franz Hüter

发明人： Henry Szczepanski ,  Martin Zeller ,  Ottmar Franz Hüter

IPC分类号： A01N3708

CPC分类号： C07D213/30 ,  A01N37/38 ,  A01N37/50 ,  A01N43/40 ,  A01N43/80 ,  C07C69/736 ,  C07C251/42 ,  C07C251/54 ,  C07C255/62 ,  C07C323/60 ,  C07C2601/10 ,  C07D213/61 ,  C07D213/69 ,  C07D239/26 ,  C07D241/12 ,  C07D261/08 ,  C07D263/32 ,  C07D277/24 ,  C07D317/22 ,  C07D333/16

摘要： Compounds of the formula I in which: where: X is CH or N; Y is O; S, S═O or NR5; Z is OR2, SR2, N(R3)R4; or Y and Z together form 5- to 7-membered ring which contains, 2 or 3 hetero atoms O and/or N and which is unsubstituted or substituted by C1-C4alkyl, halo-C1-C4alkyl, halogen, ═O or cyclopropyl; V is a direct bond or C1-C6alkylene, which is unsubstituted or substituted by C1-C3alkyl, C2-C3alkylidene or C3-C6cycloalkylidene; U is O, S, NR7, SO or SO2; W is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; R1 is cyclopropyl, C1C6alkyl or halo-C1-C6alkyl; R2 and R3 independently of one another are C1-C6alkyl or halo-C1-C6alkyl; R4 and R5 independently of one another are hydrogen, C1-C6alkyl or C1-C6alkoxy; R7 is hydrogen, C1-C6alkyl, benzyl, C1-C6alkylcarbonyl, halo-C1-C6alkylcarbonyl, halo-C2-C6alkenylcarbonyl; R21 and R22 independently of one another are hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy or C1-C8alkylthio; R23, R24, R25, R26 independently of one another are hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy; are pesticidally active. They can be used for pest control, in particular as fungicides, acaricides and insecticides in crop protection.

摘要翻译： 式Iin的化合物，其中：其中：X为CH或N; Y为O; S，S = O或NR5; Z是OR2，SR2，N（R3）R4; 或Y和Z一起形成5-至7-元环，其含有2或3个杂原子O和/或N，并且其未被取代或被C 1 -C 4烷基，卤代-C 1 -C 4烷基，卤素，O或环丙基取代; V C 1 -C 3亚烷基或C 3 -C 6亚烷基; U是O，S，NR 7，SO或SO 2; W是取代或未取代的芳基或取代或未取代的杂芳基 R 1和R 2各自独立地为C 1 -C 6烷基或卤代-C 1 -C 6烷基; R 4和R 5彼此独立地为氢，C 1 -C 6烷基或C 1 -C 6烷氧基; R 7为 R 2和R 22彼此独立地是氢，卤素，C 1 -C 8烷基或C 1 -C 8烷氧基或C 1 -C 8烷硫基; R 23是氢，C 1 -C 6烷基，苄基，C 1 -C 6烷基羰基，卤代C 1 -C 6烷基羰基 R 24，R 25，R 26彼此独立地是氢，卤素，C 1 -C 8烷基或C 1 -C 8烷氧基; 具有杀虫活性，可用于防治害虫，特别是杀虫剂，杀螨剂和作物保护中的杀虫剂。

公开(公告)号：US06642274B1

公开(公告)日：2003-11-04

申请号：US09658180

申请日：2000-09-08

申请人： Gary W. Neal

发明人： Gary W. Neal

IPC分类号： A01N3708

CPC分类号： A61K38/21 ,  A61K31/557 ,  A61K31/5575 ,  A61K2300/00

摘要： The present invention relates to methods, compositions, devices and kits for the prevention and treatment of prostate disorders in mammals, including, but not limited to, benign prostatic hypertrophy, carcinoma of the prostate, prostadynia, prostatitis, and chronic prostatitis. The present invention provides methods for preventing and treating prostate disorders in mammals by administration of a therapeutic compound to mucosal membranes in the lower urinary tract of the mammal. The present invention also provides devices for administering a therapeutic compound to mucosal membranes in the lower urinary tract of the mammal.

摘要翻译： 本发明涉及用于预防和治疗哺乳动物前列腺疾病的方法，组合物，装置和试剂盒，包括但不限于良性前列腺肥大，前列腺癌，前列腺炎，前列腺炎和慢性前列腺炎。 本发明提供了通过向哺乳动物的下尿路的粘膜施用治疗化合物来预防和治疗哺乳动物前列腺疾病的方法。 本发明还提供了用于向哺乳动物下泌尿道中的粘膜施用治疗化合物的装置。

公开(公告)号：US06476074B1

公开(公告)日：2002-11-05

申请号：US09462450

申请日：2000-04-10

申请人： Johan Stjernschantz ,  Bahram Resul

发明人： Johan Stjernschantz ,  Bahram Resul

IPC分类号： A01N3708

CPC分类号： A61K31/557

摘要： Compositions and methods for treatment of impotence or erectile dysfunction employ prostaglandins that are selective EP2 or EP4 prostanoid receptor agonists. The compositions can be formulated for intracavernous injection, or for transurethral or transdermal application.

摘要翻译： 用于治疗阳ence或勃起功能障碍的组合物和方法使用作为选择性EP2或EP4前列腺素受体激动剂的前列腺素。 组合物可以配制用于海绵体内注射，或用于经尿道或经皮施用。

公开(公告)号：US06414028B1

公开(公告)日：2002-07-02

申请号：US09542668

申请日：2000-04-04

申请人： Servet Büyüktimkin ,  Nadir Büyüktimkin ,  James L. Yeager

发明人： Servet Büyüktimkin ,  Nadir Büyüktimkin ,  James L. Yeager

IPC分类号： A01N3708

CPC分类号： A61K9/0034 ,  A61K9/0014 ,  A61K31/557 ,  A61K31/5575 ,  A61K47/14 ,  A61K47/18 ,  A61K47/183 ,  A61K47/36 ,  Y10S514/946 ,  Y10S514/947

摘要： A topical composition of a semi-solid consistency suitable is provided for transdermal application of prostaglandin E1. The composition comprises prostaglandin E1, a penetration enhancer, a polysaccharide gum, a lipophilic compound, and an acidic buffer system. The penetration enhancer is an acid addition salt of an alkyl-2-(substituted amino)-alkanoate ester, of a (substituted amino)-alkanol alkanoate, or of a mixture thereof. The lipophilic compound may be an aliphatic C1 to C8 alcohol, an aliphatic C8 to C30 ester, or a mixture of these. The composition includes a buffer system capable of providing a buffered pH value for said composition in the range of about 3 to about 7.4.

摘要翻译： 提供适用于半固体稠度的局部组合物用于经皮施用前列腺素E1。 组合物包含前列腺素E1，渗透促进剂，多糖胶，亲脂性化合物和酸性缓冲体系。 渗透促进剂是烷基-2-（取代的氨基） - 烷酸酯，（取代的氨基） - 链烷酸烷基酯或它们的混合物的酸加成盐。 亲脂性化合物可以是脂肪族C 1〜C 8醇，脂肪族C 8〜C 30酯，或它们的混合物。 该组合物包括能够提供约3至约7.4范围内所述组合物的缓冲pH值的缓冲系统。

公开(公告)号：US06359001B1

公开(公告)日：2002-03-19

申请号：US09403524

申请日：2000-01-21

申请人： Filippo Drago

发明人： Filippo Drago

IPC分类号： A01N3708

CPC分类号： A61K31/198 ,  Y10S514/912 ,  Y10S514/913

摘要： The use of agents for blocking the synthesis of tyrosinase to prevent permanent pigmentation of the iris caused by melanin deposit induced by pharmacological treatments or by metabolic imbalance is described.

摘要翻译： 描述了用于阻断酪氨酸酶合成以阻止由药物治疗或代谢不平衡引起的黑色素沉积引起的虹膜永久性色素沉着的试剂的用途。