公开(公告)号：US20030212078A1

公开(公告)日：2003-11-13

申请号：US10276508

申请日：2003-03-26

发明人： Gerald L. Klein

IPC分类号： A61K031/542 ,  A61K031/495 ,  A61K031/453

CPC分类号： A61K31/453 ,  A61K31/495 ,  A61K31/542

摘要： A pharmacological composition includes an anti-histaminic in spray formulation that reduces symptomatic skin itching of skin without substantially eliciting weight gain or sedation in the patient when the composition is sprayed onto the area of skin at a dosage of at least 10 mg/ml over a period of at least 10 applications. Particularly contemplated anti-histaminic include hydroxyzine and ketotifen.

摘要翻译： 药物组合物包括喷雾制剂中的抗组胺剂，当将组合物以至少10mg / ml的剂量喷洒到皮肤区域上时，其可以减少皮肤的症状性皮肤瘙痒，而不会在患者体内基本上引起体重增加或镇静 期限至少10个申请。 特别考虑的抗组胺包括羟嗪和酮替芬。

公开(公告)号：US20030212061A1

公开(公告)日：2003-11-13

申请号：US10096420

申请日：2002-03-12

发明人： Simon N. Haydar

IPC分类号： A61K031/542 ,  A61K031/541 ,  A61K031/538 ,  A61K031/5377 ,  A61K031/519 ,  A61K031/4743 ,  A61K031/453 ,  A61K031/403 ,  A61K031/382

CPC分类号： C07D495/04 ,  C07D335/16

摘要： The present invention relates to a group of aza-thioxanthenone compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-thioxanthenone compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.

摘要翻译： 本发明涉及一组具有抗肿瘤活性的氮杂 - 噻吨酮化合物及其制备方法。 还公开了含有氮杂 - 噻吨酮化合物的组合物和用本发明化合物治疗哺乳动物肿瘤和癌症的方法。

公开(公告)号：US20030203897A1

公开(公告)日：2003-10-30

申请号：US10220350

申请日：2002-08-29

发明人： Christopher Love ,  Jean Pierre Frans Van Wauwe ,  Marc De Brabander ,  Ludwig Cooymans ,  Nele Vandermaesen ,  Ludo Edmond Josephine Kennis

IPC分类号： A61K031/542 ,  A61K031/538 ,  A61K031/498 ,  A61K031/4709 ,  A61K031/427

CPC分类号： C07D417/04 ,  C07D277/42 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： This invention concerns the use of a compound of formula (Inull) 1 a N-oxide, pharmaceutically acceptable addition salt, quaternary amine and stereochemically isomeric form thereof, wherein Q is optionally substituted C3-6cycloalkyl, phenyl, naphthyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl; or Q is a radical of formula 2 wherein X and Y each independently are O, NR3, CH2 or S, with R3 being hydrogen or C1-4alkyl; q is 1 to 4; Z is O or NR4 with R4 being hydrogen or C1-4alkyl; r is 1 to 3; L is optionally substituted phenyl or L is Het with Het being an optionally substituted five- or six-membered heterocyclic ring or an optionally substituted bicyclic heterocyclic ring; for the manufacture of a medicament for the prevention or the treatment of diseases mediated through cytokines.

摘要翻译： 本发明涉及式（I'）化合物的N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式的用途，其中Q是任选取代的C 3-6环烷基，苯基，萘基，吡啶基，嘧啶基，吡嗪基 ，哒嗪基，苯并噻唑基，苯并恶唑基，苯并咪唑基，吲唑基或咪唑并吡啶基; 或Q是下式的基团，其中X和Y各自独立地是O，NR 3，CH 2或S，R 3是氢或C 1-4烷基; q为1〜4; Z是O或NR 4，其中R 4是氢或C 1-4烷基; r为1〜3; L是任选取代的苯基或L是Het，Het是任选取代的五元或六元杂环或任选取代的双环杂环; 用于制备用于预防或治疗通过细胞因子介导的疾病的药物。

公开(公告)号：US20030195200A1

公开(公告)日：2003-10-16

申请号：US10370856

申请日：2003-02-20

发明人： John Patrick Mogensen ,  Per Sauerberg ,  Paul Stanley Bury ,  Lone Jeppesen ,  Ingrid Pettersson

IPC分类号： A61K031/542 ,  A61K031/538 ,  A61K031/498 ,  A61K031/4745 ,  A61K031/473 ,  C07D417/02 ,  C07D413/02 ,  C07D43/02

CPC分类号： C07D213/30 ,  A61K31/34 ,  A61K31/357 ,  A61K31/435 ,  A61K45/06 ,  C07C59/68 ,  C07C59/72 ,  C07C59/90 ,  C07C69/65 ,  C07C69/734 ,  C07C2603/18 ,  C07C2603/26 ,  C07D215/14 ,  C07D307/42 ,  C07D307/79 ,  C07D307/80 ,  C07D317/54 ,  A61K2300/00

摘要： The present invention relates to compounds of the general formula (I) 1 The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

摘要翻译： 本发明涉及通式（I）的化合物。该化合物可用于治疗和/或预防由核受体介导的病症，特别是过氧化物酶体增殖物激活受体（PPAR）。

公开(公告)号：US20030166928A1

公开(公告)日：2003-09-04

申请号：US10329719

申请日：2002-12-23

发明人： Nathalie Schlienger

IPC分类号： C07D498/12 ,  C07D491/12 ,  C07D487/12 ,  A61K031/542 ,  A61K031/538 ,  A61K031/519

CPC分类号： C07D471/10 ,  C07D491/10 ,  C07D498/10

摘要： The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

摘要翻译： 本发明涉及作为单胺受体调节剂的螺环环化合物; 包含它们的组合物; 用所述化合物抑制单胺受体的活性的方法; 使用所述化合物治疗与单胺受体相关的疾病状况的方法; 以及用于鉴定适于使用所述化合物治疗的受试者的方法。

公开(公告)号：US20030158182A1

公开(公告)日：2003-08-21

申请号：US10342719

申请日：2003-01-15

申请人： Wyeth

发明人： Mark A. Collins ,  Valerie A. Mackner ,  Jay E. Wrobel ,  Lin Zhi ,  Todd K. Jones ,  James P. Edwards ,  Christopher M. Tegley

IPC分类号： A61K031/542 ,  C07D417/02

CPC分类号： C07D403/04 ,  A61K31/405 ,  A61K31/5415 ,  C07D413/04

摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure 1 wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain nullCH2(CH2)nCH2null, nullCH2CH2CMe2CH2CH2null, nullO(CH2)pCH2null, nullO(CH2)qOnull, nullCH2CH2OCH2CH2null, or nullCH2CH2NR7CH2CH2null; nnull1-5; pnull1-4; qnull1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof.

摘要翻译： 本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体拮抗剂; R 1和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，并且一起含有-CH 2（CH 2）n CH 2 - ， - CH 2 CH 2 CH 2 CH 2 CH 2 - ， - O（CH 2）p CH 2 - ， - O（CH 2）q O - ， - CH 2 CH 2 OCH 2 CH 2 - 或-CH 2 CH 2 NR 7 CH 2 CH 2 - n = 1-5; p = 1-4; q = 1-4; R3是氢，OH，NH2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或CORA; RA是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R4是氢，卤素，CN，NH2，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R5是氢，烷基或取代的烷基; R6是氢，烷基，取代的烷基或CORB; RB是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R7是氢或烷基，或其药学上可接受的盐。

公开(公告)号：US20030055050A1

公开(公告)日：2003-03-20

申请号：US10123076

申请日：2002-04-11

申请人： Neurocrine Biosciences, Inc.

发明人： Mustapha Haddach ,  John Patrick Williams ,  Dragan Marinkovic ,  Jane Han Bu

IPC分类号： A61K031/542 ,  A61K031/5383 ,  A61K031/519 ,  A61K031/498

CPC分类号： C07D491/16 ,  C07D498/16 ,  C07D513/16

摘要： CRF receptor antagonists are disclosed which have utility in the treatment of a variety of disorders, including the treatment of disorders manifesting hypersecretion of CRF in a warm-blooded animals, such as stroke. The CRF receptor antagonists of this invention have the following structure: 1 including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein m, R, R1, R2, X, Y, A, B and C are as defined herein. Compositions containing a CRF receptor antagonist in combination with a pharmaceutically acceptable carrier are also disclosed, as well as methods for use of the same.

摘要翻译： 公开了CRF受体拮抗剂，其可用于治疗各种疾病，包括治疗在温血动物（例如中风）中表现出CRF过度分泌的病症。 本发明的CRF受体拮抗剂具有以下结构：包括其立体异构体，前药和药学上可接受的盐，其中m，R，R 1，R 2，X，Y，A，B和C如本文所定义。 还公开了含有CRF受体拮抗剂与药学上可接受的载体的组合物，以及其用途的方法。

公开(公告)号：US20030050300A1

公开(公告)日：2003-03-13

申请号：US10211879

申请日：2002-08-02

发明人： William W. McWhorter JR.

IPC分类号： A61K031/553 ,  A61K031/554 ,  A61K031/551 ,  A61K031/542 ,  A61K031/538 ,  C07D498/14 ,  C07D487/22

CPC分类号： C07D498/16 ,  C07D513/16

摘要： The present invention provides compounds of Formula (I): 1 wherein R1, R2, R3, R4, R5, R6, R7, and R8 have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of Formula (I). The compounds are 5-HT ligands, and are useful for treating diseases whereas modulation of 5-HT activity is desired.

摘要翻译： 本发明提供式（I）化合物：其中R1，R2，R3，R4，R5，R6，R7和R8具有说明书中定义的任何值，以及包含该化合物的药物组合物。 本发明还提供治疗方法以及可用于制备式（I）化合物的方法和中间体。 该化合物是5-HT配体，并且可用于治疗疾病，而期望5-HT活性的调节。

公开(公告)号：US20030049308A1

公开(公告)日：2003-03-13

申请号：US10257564

申请日：2002-10-15

发明人： Frank Theobald ,  Ulrich Frick

IPC分类号： A61K031/542 ,  A61K031/4439 ,  A61K009/70

CPC分类号： A61K45/06 ,  A61K9/006 ,  A61K9/7023 ,  A61K31/465 ,  A61K31/00 ,  A61K2300/00

摘要： A transdermal or transmucosal pharmaceutical administration form for treating nicotine dependency or for disaccustoming smokers, comprising nicotine, a nicotine salt, a nicotine derivative or a nicotinergic substance in combination with at least one further active substance is characterized in that as additional active substance(s) it comprises at least one substance which acts on the central nervous system.

摘要翻译： 用于治疗尼古丁依赖性或不适合吸烟者的经皮或经粘膜药物施用形式，其包含与至少一种其它活性物质组合的尼古丁，尼古丁盐，尼古丁衍生物或烟碱能物质，其特征在于作为另外的活性物质， 它包含作用于中枢神经系统的至少一种物质。

公开(公告)号：US20020042415A1

公开(公告)日：2002-04-11

申请号：US09822095

申请日：2001-03-30

发明人： Philip Albert Carpino ,  David Andrew Griffith ,  Bruce Allen Lefker

IPC分类号： A61K031/4985 ,  A61K031/542

CPC分类号： C07D487/04 ,  A61K38/00 ,  C07D471/04 ,  C07D491/04 ,  C07D513/04 ,  C07K5/0202 ,  C07K5/0205 ,  C07K5/0207 ,  C07K5/021 ,  C07K5/06026

摘要： This invention is directed to compounds of the formula 1 and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中取代基如本说明书中所定义，其为生长激素分泌因子并且增加内源性生长激素的水平。 本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱，充血性心力衰竭，与衰老相关的脆弱性，肥胖症; 加速骨折修复，减轻主要手术后的蛋白质分解代谢反应，减少慢性疾病引起的恶病质和蛋白质损失，加速伤口愈合，或加速烧伤患者或经历大手术的患者的恢复; 改善肌肉力量，移动性，维持皮肤厚度，代谢体内平衡或肾脏体内平衡。 当与以下物质组合使用时，本发明的化合物还可用于治疗骨质疏松症和/或虚弱：双膦酸盐化合物如阿仑膦酸盐; 雌激素，雌激素和可选的孕酮; 雌激素激动剂或拮抗剂; 或降钙素，以及对此有用的药物组合物。 此外，本发明涉及可用于增加人或其他动物中生长激素的内源性产生或释放的药物组合物，其包含有效量的本发明化合物和选自GHRP-6的生长激素促分泌素， Hexarelin，GHRP-1，生长激素释放因子（GRF），IGF-1，IGF-2或B-HT920。 本发明还涉及可用于制备式I化合物的中间体。