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61. 发明申请

WO00066571A1 CYCLOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 审中-公开
标题翻译： CYCOCARBAMATE衍生物作为孕激素受体调节剂
公开(公告)号：WO00066571A1
公开(公告)日：2000-11-09
申请号：PCT/US2000/011822
申请日：2000-05-01
IPC分类号： C07D265/12 , A61K31/536 , A61K31/537 , A61P15/00 , A61P15/18 , A61P35/00 , A61P43/00 , C07D265/18 , C07D413/04 , C07D413/10 , C07D417/04 , C07F9/6533
CPC分类号： C07D265/18 , C07D413/04 , C07D413/10 , C07D417/04
摘要： This invention provides compounds of Formula (I) wherein R and R may be single substituents or fused to form spirocyclic or heterospirocyclic rings; R is H, OH, NH2, C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C6 alkenyl, substituted C1 to C6 alkenyl, alkynyl, or substituted alkynyl, COR ; R is H, C1 to C3 alkyl, substituted C1 to C3 alkyl, aryl, substituted aryl, C1 to C3 alkoxy , substituted C1 to C3 alkoxy, C1 to C3 aminoalkyl, or substituted C1 to C3 aminoalkyl; R is H, halogen, CN, NO2, C1 to C6 alkyl, substituted C1 to C6 alkyl, alkynyl, or substituted alkynyl, C1 to C6 alkoxy, substituted C1 to C6 alkoxy, substituted C1 to C6 alkoxy, amino, C1 to C6 aminoalkyl, or substituted C1 to C6 aminoalkyl; and R is selected from a trisubstituted benzene ring of a five or six membered ring with 1, 2, or 3 heteroatoms from the group including O, S, SO, SO2 or NR and containing one or two independent substituents from the group including H, halogen, CN, NO2, amino, and C1 to C3 alkyl, C1 to C3 alkoxy, C1 to C3 aminoalkyl, COR , or NR COR ; or pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods using the compounds as antagonists of the progesterone receptor.
摘要翻译：本发明提供式（I）化合物，其中R 1和R 2可以是单取代基或稠合形成螺环或杂环环; R 3是H，OH，NH 2，C 1至C 6烷基，取代的C 1 -C 6烷基，C 3至C 6烯基，取代的C 1至C 6烯基，炔基或取代的炔基。 R C是H，C 1至C 3烷基，取代的C 1至C 3烷基，芳基，取代的芳基，C 1至C 3的烷氧基，取代的C 1至C 3的烷氧基，C 1至C 3的氨基烷基或取代的C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2，C 1至C 6烷基，取代的C 1 -C 6烷基，炔基或取代的炔基，C 1至C 6烷氧基，取代的C 1至C 6烷氧基，取代的C 1至C 6烷氧基，至C6氨基烷基或取代的C1至C6氨基烷基; R 5选自具有1,2或3个杂原子的五元或六元环的三取代苯环，所述杂原子包括O，S，SO，SO 2或NR 6，并含有一个或两个独立的取代基包括H，卤素，CN，NO 2，氨基和C 1至C 3烷基，C 1至C 3烷氧基，C 1至C 3氨基烷基，COR F或NR G COR F; 或其药学上可接受的盐，以及使用该化合物作为孕酮受体的拮抗剂的药物组合物和方法。

62. 发明申请

WO0032584A3 NONSTEROIDAL ANTIINFLAMMATORIES 审中-公开
标题翻译：的NSAIDs
公开(公告)号：WO0032584A3
公开(公告)日：2000-11-09
申请号：PCT/EP9909754
申请日：1999-11-29
申请人： SCHERING AG , LEHMANN MANFRED , KROLIKIEWICZ KONRAD , SKUBALLA WERNER , STREHLKE PETER , KALKBRENNER FRANK , EKERDT ROLAND , GIESEN CLAUDIA
发明人： LEHMANN MANFRED , KROLIKIEWICZ KONRAD , SKUBALLA WERNER , STREHLKE PETER , KALKBRENNER FRANK , EKERDT ROLAND , GIESEN CLAUDIA
IPC分类号： C07D237/32 , A61K31/343 , A61K31/381 , A61K31/502 , A61K31/536 , A61K31/5365 , A61P1/00 , A61P1/08 , A61P1/16 , A61P7/00 , A61P9/00 , A61P11/00 , A61P17/00 , A61P19/02 , A61P23/00 , A61P25/00 , A61P27/02 , A61P27/16 , A61P29/00 , A61P35/00 , A61P37/00 , C07D265/02 , C07D307/88 , C07D333/72 , A61K31/16 , A61K31/165 , A61K31/365 , A61K31/38 , A61K31/50 , A61K31/535
CPC分类号： C07D265/02 , A61K31/502 , A61K31/5365 , C07D307/88
摘要： The invention relates to the use of compounds of general formula (I), wherein A, B, A, Ar, R , R and R have the meanings detailed more closely in the description, for producing medicaments with an antiinflammatory action. The compounds of general formula (I) show a clear dissociation between antiinflammatory and metabolic effects.
摘要翻译：本发明描述了使用通式（I），其中A，B，A中，Ar，R <1>，R <2>和R <3>是如在说明书中给出更详细定义的，用于与产生药物抗炎活性。通式（I）的化合物显示出抗炎和代谢作用之间有明显的解离。

63. 发明申请

WO00035429A1 UTILIZATION OF INHIBITORS OF THE KQT1 CHANNEL IN ORDER TO PRODUCE A MEDICAMENT FOR TREATING DISEASES WHICH ARE CAUSED BY PARASITIC HELMINTHS AND ECTOPARASITES 审中-公开
标题翻译： KQT1 CHANNEL抑制剂用于制造药物疾病的治疗中，BY THEN希勒米和体外寄生虫，OUT所产生USE
公开(公告)号：WO00035429A1
公开(公告)日：2000-06-22
申请号：PCT/EP1999/009547
申请日：1999-12-07
IPC分类号： C07D311/70 , A01N41/06 , A01N43/16 , A61K31/00 , A61K31/015 , A61K31/145 , A61K31/18 , A61K31/352 , A61K31/353 , A61K31/435 , A61K31/4433 , A61K31/4965 , A61K31/498 , A61K31/536 , A61K31/5415 , A61K45/00 , A61P33/00 , A61P33/10 , A61P33/14
CPC分类号： A61K31/4433 , A61K31/00 , A61K31/18 , A61K31/352 , A61K31/353
摘要： The invention relates to the utilization of inhibitors of the KQT1 channel in order produce a medicament for treating diseases which are caused by parasitic helminths and ectoparasites. According to the invention, inhibitors of the KQT1 channel depict a novel lethal fundamental constituent for parasitic helminths and ectoparasites. Blockers of the cellular KQT1 channel, said channel occurring in the parasitic helminths and ectoparasites, are therefore used to produce a medicament for treating vertebrates and humans which are afflicted with the parasitic helminths or ectoparasites. These KQT1 blockers are used alone as medicaments or in combination with other medicaments and therapeutic measures. Inhibitors of the KQT1 channel also depict a novel working mechanism for plant pests such as insects, spiders, mollusks and nematoda, and are consequently used in order to produce a plant protective agent.
摘要翻译：所述KQT1通道的抑制剂代表一种新颖的致死原则蠕虫和体外寄生虫，因此，蜂窝KQT1信道，发生在寄生虫和体外寄生虫，用于制备所述药物用于脊椎动物及人的治疗，蠕虫或体外寄生虫的阻断剂受到影响。这KQT1阻滞剂作为单独或与其他药物和治疗措施的组合药物。所述KQT1通道的抑制剂也代表Planzenschädlinge动作，例如昆虫，蜘蛛，软体动物和线虫的新机制，并因此可用于植物保护剂的制备。

64. 发明申请

WO9963940A2 INHIBITORS OF H<+>K<+>-ATPase 审中-公开
标题翻译： H + ATP酶抑制剂
公开(公告)号：WO9963940A2
公开(公告)日：1999-12-16
申请号：PCT/US9912925
申请日：1999-06-08
申请人： ADVANCED MEDICINE INC , MEIER DAVIS SUSAN , GRIFFIN JOHN H , CHOI SEOK KI
发明人： MEIER-DAVIS SUSAN , GRIFFIN JOHN H , CHOI SEOK-KI
IPC分类号： C07D499/44 , A01N57/34 , A61K31/00 , A61K31/357 , A61K31/397 , A61K31/407 , A61K31/421 , A61K31/424 , A61K31/431 , A61K31/439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/522 , A61K31/536 , A61K31/5377 , A61K31/546 , A61K31/551 , A61K31/65 , A61K31/7028 , A61K31/7034 , A61K31/7036 , A61K31/7042 , A61K31/7048 , A61K31/7052 , A61K31/7056 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K38/00 , A61K39/00 , A61K39/395 , A61K39/44 , A61K47/48 , A61K51/00 , A61P31/04 , A61P31/18 , A61P43/00 , C07B61/00 , C07C233/36 , C07C233/78 , C07C237/24 , C07C237/26 , C07C271/20 , C07C275/42 , C07C321/04 , C07C323/12 , C07C335/08 , C07C335/32 , C07D207/32 , C07D207/333 , C07D211/58 , C07D215/56 , C07D233/90 , C07D235/30 , C07D263/28 , C07D265/18 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D413/14 , C07D453/02 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/34 , C07D475/04 , C07D475/08 , C07D477/00 , C07D487/04 , C07D487/06 , C07D493/04 , C07D493/06 , C07D495/04 , C07D498/04 , C07D498/18 , C07D501/20 , C07D519/00 , C07H15/236 , C07H15/238 , C07H15/26 , C07H17/08 , C07H19/06 , C07H19/20 , C07K2/00 , C07K4/00 , C12N9/99 , C12P19/38 , C12Q1/26 , C12Q1/44 , C12Q1/48 , C12Q1/533 , C40B30/04 , C40B40/04 , G01N33/15 , G01N33/50 , G01N33/53 , G01N33/543 , G01N33/566 , G01N33/573 , G01N33/68 , G01N33/92 , G01N37/00 , A61K
CPC分类号： C40B30/04 , A61K31/00 , A61K47/54 , A61K47/55 , A61K47/552 , A61K47/60 , C07C233/36 , C07C233/78 , C07C237/24 , C07C271/20 , C07C321/04 , C07C323/12 , C07C335/08 , C07C335/32 , C07C2603/18 , C07D207/333 , C07D211/58 , C07D215/56 , C07D233/90 , C07D235/30 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D413/14 , C07D471/04 , C07D471/14 , C07D473/00 , C07D473/34 , C07D475/04 , C07D475/08 , C07D487/04 , C07D487/06 , C07D493/04 , C07D493/06 , C07H19/20 , C12Q1/26 , C12Q1/44 , C12Q1/48 , C12Q1/533 , C40B40/04 , G01N33/573 , G01N33/6842 , G01N33/6845 , G01N33/92 , G01N2500/00 , G01N2500/04 , G01N2800/044 , Y10S530/807
摘要： Disclosed are multibinding compounds which inhibit H /K -ATPase, an enzyme which is involved in the control of acid secretion in the stomach. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is an inhibitor of H /K -ATPase. The multibinding compounds of this invention are useful in the treatment gastroesophageal reflux disease ("GERD").
摘要翻译：公开了抑制H + / K + -ATP酶的多相结合化合物，其是参与控制胃中酸分泌的酶。含有2-10个配体的本发明的多相结合化合物共价连接到一个或多个接头上。每个配体是H + / K + - ATP酶的抑制剂。本发明的多重联结化合物可用于治疗胃食管反流病（“GERD”）。

65. 发明申请

WO99051239A1 FORMULATION OF FAST-DISSOLVING EFAVIRENZ CAPSULES OR TABLETS USING SUPER-DISINTEGRANTS 审中-公开
标题翻译：快速溶解EFAVIRENZ胶囊或使用超级消毒剂的片剂的配方
公开(公告)号：WO99051239A1
公开(公告)日：1999-10-14
申请号：PCT/US1999/007228
申请日：1999-04-01
IPC分类号： A61K9/16 , A61K9/20 , A61K9/48 , A61K31/535 , A61K31/536 , A61K47/36 , A61P31/18
CPC分类号： A61K31/536 , A61K9/1652 , A61K9/2054 , A61K9/2059 , Y10S514/885
摘要： The present invention provides improved oral dosage form formulations of efavirenz that are useful in the inhibition of human immunodeficiency virus (HIV), the prevention or treatment of infection by HIV, and in the treatment of the resulting acquired immune deficiency syndrome (AIDS). In particular, the present invention relates to compressed tablets or capsules comprising efavirenz that contain one or more disintegrants that enhance the dissolution rate of the efavirenz in the gastrointestinal tract thereby improving the rate and extent of absorption of efavirenz in the body. The present invention also relates to the process of making such tablets or capsules.
摘要翻译：本发明提供了可用于抑制人类免疫缺陷病毒（HIV），预防或治疗HIV感染和治疗所得到的获得性免疫缺陷综合征（AIDS）的依法韦仑的改进的口服剂型制剂。特别地，本发明涉及包含依法韦仑的压片或胶囊，其包含一种或多种增强依法韦仑在胃肠道中的溶解速率的崩解剂，从而改善依法韦仑在体内的吸收速率和程度。本发明还涉及制备这种片剂或胶囊剂的方法。

66. 发明申请

WO9942456A3 NOVEL COMPOUNDS AND THEIR USE AS POSITIVE AMPA RECEPTOR MODULATORS 审中-公开
标题翻译：新型化合物及其作为阳性AMPA受体调节剂的应用
公开(公告)号：WO9942456A3
公开(公告)日：1999-10-07
申请号：PCT/DK9900070
申请日：1999-02-18
申请人： NEUROSEARCH AS , GOULIAEV ALEX HAAHR , LARSEN MOGENS , VARMING THOMAS , MATHIESEN CLAUS , JOHANSEN TINA HOLM , SCHEEL KRUEGER JOERGEN , OLSEN GUNNAR M , NIELSEN ELSEBET OESTERGAARD
发明人： GOULIAEV ALEX HAAHR , LARSEN MOGENS , VARMING THOMAS , MATHIESEN CLAUS , JOHANSEN TINA HOLM , SCHEEL-KRUEGER JOERGEN , OLSEN GUNNAR M , NIELSEN ELSEBET OESTERGAARD
IPC分类号： C07D239/74 , A61K31/18 , A61K31/517 , A61K31/535 , A61K31/536 , A61K31/5415 , A61K31/549 , A61K31/554 , A61P9/10 , A61P25/00 , A61P25/08 , A61P25/14 , A61P25/18 , A61P25/24 , A61P25/28 , A61P25/30 , A61P25/32 , A61P25/36 , A61P43/00 , C07C311/37 , C07C311/39 , C07D239/88 , C07D239/90 , C07D239/91 , C07D265/22 , C07D285/24 , C07D285/28 , C07D285/32 , C07D285/36 , C07D417/04 , C07D417/10 , C07D417/12 , C07D513/04 , A61K31/505 , A61K31/54 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04
CPC分类号： C07D417/04 , C07D239/90 , C07D285/24 , C07D285/28 , C07D513/04
摘要： The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R ; X represents SO2 or C=O of CH2; Y represents -CH(R )-, -N(R )- or -N(R )-CH2-, O; and the meaning of R , R , R , R , R , R , and R are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.
摘要翻译：本发明提供了由通式（I）表示的新化合物，其中由虚线表示的键可以是单键，双键或不存在; 如果该键不存在，则该氮被氢和R 2取代; X代表CH 2的SO 2或C = O; Y代表-CH（R 4） - ， - N（R 4） - 或-N（R 4）-CH 2 - ，O; 并且R 2，R 3，R 4，R 5，R 6，R 7和R 8的含义如本申请中所定义。该化合物可用作AMPA受体的正调节剂。

67. 发明申请

WO9940944A2 HYDROXYLATION ACTIVATED DRUG RELEASE 审中-公开
标题翻译：羟基化活性药物释放
公开(公告)号：WO9940944A2
公开(公告)日：1999-08-19
申请号：PCT/GB9900416
申请日：1999-02-10
申请人： UNIV MONTFORT , POTTER GERARD ANDREW , PATTERSON LAWRENCE HYLTON , BURKE MICHAEL DANNY
发明人： POTTER GERARD ANDREW , PATTERSON LAWRENCE HYLTON , BURKE MICHAEL DANNY
IPC分类号： A61K47/48 , A46B9/04 , A61K31/27 , A61K31/337 , A61K31/37 , A61K31/505 , A61K31/513 , A61K31/535 , A61K31/536 , A61K31/565 , A61K31/70 , A61K31/704 , A61P35/00 , A61P43/00 , G07F17/30
CPC分类号： A61K47/555 , A61K47/554
摘要： The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.
摘要翻译：本发明涉及其芳香族氧化，尤其是其酶促芳香族羟基化，通过释放药物部分而导致其活化的前药。它特别涉及抗肿瘤前体药物和那些由P-450酶CYP1B1的羟基化活性特异性激活的前体药物。还提供了检测芳族氧化活性的方法。

68. 发明申请

WO99040920A1 ORAL LIQUID FORMULATIONS OF BENZOXAZINONES HIV REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：苯甲酸的口服液体制剂HIV逆转录酶抑制剂
公开(公告)号：WO99040920A1
公开(公告)日：1999-08-19
申请号：PCT/US1999/003316
申请日：1999-02-17
IPC分类号： A61K9/00 , A61K9/48 , A61K9/64 , A61K31/536 , A61K47/44 , A61K31/535
CPC分类号： A61K31/536 , A61K9/0095 , A61K9/4858 , A61K47/44
摘要： A palatable oral liquid pharmaceutical composition of benzoxazinone compounds useful as HIV reverse transcriptase inhibitors comprising the benzoxazinone active ingredient in a liquid vehicle comprising a vegetable oil selected from olive oil, peanut oil, soybean oil, corn oil, safflower oil, sunflower oil, canola oil or walnut oil. Other formulating agents such as sweetening agents, lecithin suspending agents, etc. may be optionally added.
摘要翻译：一种可用作HIV逆转录酶抑制剂的苯并恶嗪酮化合物的可口的口服液体药物组合物，其包含在液体载体中的苯并恶嗪酮活性成分，其包含选自橄榄油，花生油，大豆油，玉米油，红花油，向日葵油，菜刀油或核桃油。可以任选地加入其它配制剂如甜味剂，卵磷脂悬浮剂等。

69. 发明申请

WO2023058987A1 에파비렌즈 및 플루옥세틴을 유효성분으로 함유하는 바이러스 감염 질환 예방 또는 치료용 약학적 조성물 审中-公开
公开(公告)号：WO2023058987A1
公开(公告)日：2023-04-13
申请号：PCT/KR2022/014517
申请日：2022-09-28
申请人： (주)프론트바이오
发明人： 박수현 , 김샛별 , 김정훈 , 모영원
IPC分类号： A61K31/536 , A61K31/138 , A61K45/06 , A61P31/12 , A61P25/24
摘要： 본 발명은 에파비렌즈(efavirenz) 및 플루옥세틴(fluoxetine)을 유효성분으로 함유하는 바이러스 감염 질환의 예방 또는 치료용 약학적 조성물에 관한 것으로서, 에파비렌즈 및 플루옥세틴을 복합, 혼합 또는 병용 투여하거나, 에파비렌즈 및 플루옥세틴에 바이구아나이드(biguanide) 계열 화합물인 메트포르민을 추가하여 복합, 혼합, 또는 병용 투여하는 경우 각각을 단독 투여하였을 때에 비하여 SARS-CoV-2을 포함하는 다양한 인수공통감염 바이러스에 대해 현저히 높은 항바이러스 효능을 나타내는 것을 확인하였으므로, 상기 에파비렌즈 및 플루옥세틴, 추가적으로 바이구아나이드 계열 화합물은 바이러스 감염 질환 예방 또는 치료용 조성물의 유효성분으로 유용하게 사용될 수 있다.

70. 发明申请

WO2023008921A1 항바이러스제 및 항우울제를 유효성분으로 함유하는 암 예방 또는 치료용 약학적 조성물 审中-公开
公开(公告)号：WO2023008921A1
公开(公告)日：2023-02-02
申请号：PCT/KR2022/011112
申请日：2022-07-28
申请人： (주)프론트바이오
发明人： 박수현 , 김샛별 , 김정훈 , 모영원
IPC分类号： A61K31/536 , A61K31/138 , A61K31/4525 , A61K31/135 , A61K31/505 , A61K31/137 , A61K31/55 , A61K31/155 , A61K45/06 , A61P35/00
摘要： 본 발명은 항바이러스제 및 항우울제를 유효성분으로 함유하고, 바이구아나이드 계열 화합물을 추가할 수 있는 암 예방 또는 치료용 약학적 조성물에 관한 것으로서, 보다 구체적으로는 항바이러스제로 항바이러스제로 에파비렌즈, 에트라비린, 릴피비린, 로피나비르, 아타자나비르, 다루나비르 및 리토나비르, 및 항우울제로 플루옥세틴, 플루복사민, 파록세틴, 설트랄린, 둘록세틴, 아미트리프틸린, 클로미프라민, 노르트립틸린, 데시프라민, 아목사핀, 마프로틸린, 트라이미프라민, 프로트립틸린 및 멜리트라센을 복합, 혼합 또는 병용 투여하거나 에파비렌즈 및 플루옥세틴에 바이구아나이드 계열 화합물인 메트포르민을 추가하여 복합, 혼합 또는 병용 투여하는 경우 각각을 단독 투여하였을 때에 비하여 현저히 높은 상승적 항암 활성을 나타내는 것을 확인하였으므로, 본 발명에 따른 항바이러스제 및 항우울제는 암 예방 또는 치료용 조성물의 유효성분으로 유용하게 사용될 수 있다.

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