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1. 发明申请

WO2009063364A3 MODULATORS OF UROTENSIN RECEPTOR AND METHODS OF USE THEREOF 审中-公开
标题翻译： UROTENSIN受体的调节剂及其使用方法
公开(公告)号：WO2009063364A3
公开(公告)日：2009-07-02
申请号：PCT/IB2008054633
申请日：2008-11-06
申请人： ENCYSIVE PHARMACEUTICALS INC , GAO DAXIN , WU CHENGDE
发明人： GAO DAXIN , WU CHENGDE
IPC分类号： C07D487/08 , A61K31/4995 , A61P1/12 , A61P3/10 , A61P9/00 , A61P25/00
CPC分类号： C07D487/08
摘要： Provided are compounds that are modulators of urotensin-II receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of urotensin-II receptor activity wherein the disease is a cardiovascular disorder, atherosclerosis, renal failure, nephrotoxicity and diarrhea caused by antineoplastic agents, post-myocardial infarction, pulmonary hypertension, diabetes or a CNS related disease.
摘要翻译：提供的是作为泌尿生长素-2受体活性调节剂的化合物，含有化合物的组合物和使用该化合物和组合物的方法。在某些实施方案中，提供了用于治疗或改善与调节泌尿生长因素-II受体活性相关的疾病的方法，其中所述疾病是由抗肿瘤剂引起的心血管疾病，动脉粥样硬化，肾衰竭，肾毒性和腹泻，心肌梗塞后，肺动脉高压，糖尿病或CNS相关疾病。

2. 发明申请

WO0149685A3 SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN 审中-公开
标题翻译：调节内皮素活性的磺酰胺及其衍生物
公开(公告)号：WO0149685A3
公开(公告)日：2002-02-14
申请号：PCT/US0035599
申请日：2000-12-29
申请人： TEXAS BIOTECHNOLOGY CORP , WU CHENGDE , HOLLAND GEORGE W , BLOK NATALIE
发明人： WU CHENGDE , HOLLAND GEORGE W , BLOK NATALIE
IPC分类号： A61K9/19 , A61K9/20 , A61K9/48 , A61K31/422 , A61K47/12 , A61K47/14 , A61K47/34 , A61K47/38 , A61K47/44 , A61P1/00 , A61P7/00 , A61P9/00 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/02 , A61P13/12 , A61P15/00 , A61P15/06 , A61P15/10 , A61P15/12 , A61P17/00 , A61P19/10 , A61P27/02 , A61P27/06 , A61P29/00 , A61P37/00 , A61P37/02 , C07D413/12 , C07D413/14 , A61K31/42 , C07D261/16
CPC分类号： C07D413/12 , C07D413/14
摘要： Thienyl-, furyl-, pyrrolyl- and phenylsulfonamides, formulations of pharmaceutically-acceptable derivatives thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides, N-(isoxazolyl)pyrrolylsulfonamides and N-(isoxazoly)phenylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or pharmaceutically acceptable derivatives thereof that inhibit the activity of endothelin are also provided.
摘要翻译：提供噻吩基，呋喃基，吡咯基和苯基磺酰胺，其药学上可接受的衍生物的制剂和调节或改变肽内皮素家族的活性的方法。特别地，N-（异恶唑基）噻吩基磺酰胺，N-（异恶唑基） - 呋喃基磺酰胺，N-（异恶唑基）吡咯烷基磺酰胺和N-（异恶唑基）苯基磺酰胺，其制剂及使用这些磺酰胺抑制内皮肽与内皮素结合的方法提供了通过使受体与磺酰胺接触的受体。还提供了通过施用有效量的一种或多种这些抑制内皮素活性的磺酰胺或其药学上可接受的衍生物来治疗内皮素介导的病症的方法。

3. 发明申请

WO2013029338A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2013029338A1
公开(公告)日：2013-03-07
申请号：PCT/CN2012/001221
申请日：2012-08-30
申请人： GLAXO GROUP LIMITED , WANG, Yonghui , CAI, Wei , LIU, Qian , MENG, Qinghua , CHENG, Yaobang , YANG, Ting , ZHANG, Guifeng , XIANG, Jianing , WU, Chengde
发明人： WANG, Yonghui , CAI, Wei , LIU, Qian , MENG, Qinghua , CHENG, Yaobang , YANG, Ting , ZHANG, Guifeng , XIANG, Jianing , WU, Chengde
IPC分类号： C07C317/14 , C07D209/08 , C07D211/84 , C07D231/12 , C07D235/02 , C07D237/08 , C07D237/10 , C07D249/06 , A61K31/10 , A61K31/33 , A61P19/02 , A61P25/28 , A61P29/00 , A61P37/00
CPC分类号： C07D211/70 , C07C311/16 , C07C311/29 , C07C311/51 , C07C317/44 , C07C317/46 , C07C2601/02 , C07C2601/08 , C07D205/04 , C07D207/325 , C07D207/34 , C07D209/08 , C07D209/30 , C07D211/26 , C07D211/46 , C07D213/40 , C07D213/64 , C07D213/71 , C07D213/75 , C07D213/84 , C07D231/12 , C07D231/18 , C07D231/56 , C07D233/61 , C07D237/08 , C07D237/20 , C07D239/26 , C07D239/34 , C07D239/38 , C07D239/42 , C07D241/20 , C07D249/06 , C07D261/08 , C07D263/32 , C07D295/135 , C07D295/185 , C07D309/12 , C07D319/18 , C07D403/04 , C07D471/04
摘要： Disclosed are novel retinoid-related orphan receptor gamma (RORy) modulators and their use in the treatment of diseases mediated by RORy.
摘要翻译：公开了新型维甲酸相关孤儿受体γ（RORY）调节剂及其在治疗由RORy介导的疾病中的用途。

4. 发明申请

WO2004073634A2 PHENYLENEDIAMINE UROTENSIN-II RECEPTOR ANTAGONISTS AND CCR-9 ANTAGONISTS 审中-公开
标题翻译：苯二甲酸尿激酶Ⅱ受体拮抗剂和CCR-9拮抗剂
公开(公告)号：WO2004073634A2
公开(公告)日：2004-09-02
申请号：PCT/US2004/004645
申请日：2004-02-18
申请人： ENCYSIVE PHARMACEUTICALS INC. , WU, Chengde , ANDERSON, Eric, C. , BUI, Huong , GAO, Daxin , KASSIR, Jamal , LI, Wen , WANG, Junmei , MARKET, Robert, V.
发明人： WU, Chengde , ANDERSON, Eric, C. , BUI, Huong , GAO, Daxin , KASSIR, Jamal , LI, Wen , WANG, Junmei , MARKET, Robert, V.
IPC分类号： A61K
CPC分类号： C07D333/38 , C07D207/16 , C07D209/08 , C07D209/44 , C07D213/74 , C07D237/08 , C07D239/26 , C07D241/42 , C07D295/135 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
摘要翻译：本发明涉及尿素调节素II受体拮抗剂，CCR-9拮抗剂，含有它们的药物组合物及其应用。

5. 发明申请

WO0067746A8 CARBOXYLIC ACID DERIVATIVES THAT INHIBIT THE BINDING OF INTEGRINS TO THEIR RECEPTORS 审中-公开
标题翻译：阻止整合素与其受体结合的羧酸衍生物
公开(公告)号：WO0067746A8
公开(公告)日：2002-02-28
申请号：PCT/US0012303
申请日：2000-05-05
申请人： TEXAS BIOTECHNOLOGY CORP , BIEDIGER RONALD J , CHEN QI , HOLLAND GEORGE W , KASSIR JAMAL M , LI WEN , MARKET ROBERT V , SCOTT IAN L , WU CHENGDE
发明人： BIEDIGER RONALD J , CHEN QI , HOLLAND GEORGE W , KASSIR JAMAL M , LI WEN , MARKET ROBERT V , SCOTT IAN L , WU CHENGDE
IPC分类号： C07D239/36 , A61K31/215 , A61K31/216 , A61K31/335 , A61K31/357 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/4015 , A61K31/4025 , A61K31/44 , A61K31/4409 , A61K31/4412 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/47 , A61K31/506 , A61K31/55 , A61P1/00 , A61P3/10 , A61P9/10 , A61P11/06 , A61P17/00 , A61P19/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07C69/66 , C07C275/32 , C07C275/34 , C07D207/04 , C07D207/18 , C07D207/416 , C07D211/68 , C07D211/72 , C07D213/02 , C07D213/64 , C07D213/69 , C07D213/73 , C07D213/74 , C07D213/75 , C07D215/00 , C07D215/38 , C07D221/04 , C07D233/96 , C07D239/46 , C07D239/47 , C07D317/58 , C07D333/20 , C07D401/06 , C07D405/12 , C07D409/12 , C07D409/14 , C07D471/04 , C07D487/04
CPC分类号： C07D213/75 , C07D239/47 , C07D405/12 , C07D409/14
摘要： A method for the inhibition of the binding of alpha 4 beta 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and to the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which alpha 4 beta 1 is involved.
摘要翻译：抑制α4β1整联蛋白与其受体结合的方法，例如VCAM-1（血管细胞粘附分子-1）和纤连蛋白; 抑制这种结合的化合物; 包含这些化合物的药物活性组合物; 以及如上所述的这种化合物的使用，或用于控制或预防涉及α4β1的疾病状态的制剂中。

6. 发明申请

WO2009053895A3 QUINOLINE UROTENSIN-II RECEPTOR ANTAGONISTS 审中-公开
标题翻译：喹诺酮尿毒素Ⅱ受体拮抗剂
公开(公告)号：WO2009053895A3
公开(公告)日：2009-06-11
申请号：PCT/IB2008054311
申请日：2008-10-20
申请人： ENCYSIVE PHARMACEUTICALS INC , KESSLER RAYMOND J , WU CHENGDE
发明人： KESSLER RAYMOND J , WU CHENGDE
IPC分类号： C07D215/42 , A61K31/4706 , A61P9/00
CPC分类号： C07D215/44
摘要： Provided are compounds that are modulators of urotensin-II receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of urotensin-II receptor activity.
摘要翻译：提供的是作为泌尿生长素-2受体活性调节剂的化合物，含有化合物的组合物和使用该化合物和组合物的方法。在某些实施方案中，提供了用于治疗或改善与调节泌尿生长素受体活性相关的疾病的方法。

7. 发明申请

WO2004073634A3 PHENYLENEDIAMINE UROTENSIN-II RECEPTOR ANTAGONISTS AND CCR-9 ANTAGONISTS 审中-公开
标题翻译：苯二甲酸尿激酶Ⅱ受体拮抗剂和CCR-9拮抗剂
公开(公告)号：WO2004073634A3
公开(公告)日：2006-09-14
申请号：PCT/US2004004645
申请日：2004-02-18
申请人： ENCYSIVE PHARMACEUTICALS INC , WU CHENGDE , ANDERSON ERIC C , BUI HUONG , GAO DAXIN , KASSIR JAMAL , LI WEN , WANG JUNMEI , MARKET ROBERT V
发明人： WU CHENGDE , ANDERSON ERIC C , BUI HUONG , GAO DAXIN , KASSIR JAMAL , LI WEN , WANG JUNMEI , MARKET ROBERT V
IPC分类号： C07D211/26 , A61K20060101 , A61K31/18 , A61K31/40 , A61K31/402 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/537 , A61K31/5375 , A61K31/55 , C07C311/29 , C07D207/08 , C07D207/09 , C07D207/16 , C07D209/08 , C07D209/44 , C07D211/14 , C07D213/74 , C07D237/08 , C07D239/26 , C07D241/42 , C07D265/30 , C07D295/135 , C07D333/38 , C07D401/12 , C07D403/12 , C07D409/12
CPC分类号： C07D333/38 , C07D207/16 , C07D209/08 , C07D209/44 , C07D213/74 , C07D237/08 , C07D239/26 , C07D241/42 , C07D295/135 , C07D401/12 , C07D403/12 , C07D409/12
摘要： The present invention relates to urotensin II receptor antagonists, CCR-9 antagonists, pharmaceutical compositions containing them and their use.
摘要翻译：本发明涉及尿素调节素II受体拮抗剂，CCR-9拮抗剂，含有它们的药物组合物及其应用。

8. 发明申请

WO0068188A9 PROPANOIC ACID DERIVATIVES THAT INHIBIT THE BINDING OF INTEGRINS TO THEIR RECEPTORS 审中-公开
标题翻译：禁止将它们结合到其受体的丙酸衍生物
公开(公告)号：WO0068188A9
公开(公告)日：2002-08-29
申请号：PCT/US0012464
申请日：2000-05-05
申请人： TEXAS BIOTECHNOLOGY CORP , BIEDIGER RONALD J , HOLLAND GEORGE W , KASSIR JAMAL M , LI WEN , MARKET ROBERT V , SCOTT IAN L , WU CHENGDE
发明人： BIEDIGER RONALD J , HOLLAND GEORGE W , KASSIR JAMAL M , LI WEN , MARKET ROBERT V , SCOTT IAN L , WU CHENGDE
IPC分类号： C07D229/00 , A61K31/192 , A61K31/33 , A61K31/4166 , A61K31/4184 , A61K31/4412 , A61K31/443 , A61K31/465 , A61K31/497 , A61K31/498 , A61K31/501 , A61K31/505 , A61K31/517 , A61P1/04 , A61P3/10 , A61P7/00 , A61P9/10 , A61P11/06 , A61P17/00 , A61P19/02 , A61P25/00 , A61P29/00 , A61P37/06 , C07C229/00 , C07C233/00 , C07D213/30 , C07D213/64 , C07D215/02 , C07D235/04 , C07D239/36 , C07D317/60 , C07D405/12 , C07D409/14 , C07C315/00 , C07C205/00 , C07C321/00
CPC分类号： C07D213/64 , C07D317/60 , C07D405/12 , C07D409/14
摘要： A method for the inhibition of the binding of alpha 4 beta 1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which alpha 4 beta 1 is involved.
摘要翻译：抑制α4β1整联蛋白与其受体结合的方法，例如VCAM-1（血管细胞粘附分子-1）和纤连蛋白; 抑制这种结合的化合物; 包含这些化合物的药物活性组合物; 以及如上所述或在用于控制或预防涉及α4β1的疾病状态的制剂中的这些化合物的使用。

9. 发明申请

WO1994027979A1 SULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN 审中-公开
标题翻译：调节内皮素活性的磺酰胺及其衍生物
公开(公告)号：WO1994027979A1
公开(公告)日：1994-12-08
申请号：PCT/US1994005755
申请日：1994-05-20
申请人： IMMUNOPHARMACEUTICS, INC. , CHAN, Ming, Fai , RAJU, Bore, Gowda , KOIS, Adam , VERNER, Erik, Joel , WU, Chengde , CASTILLO, Rosario, Silvestre , YALAMOORI, Venkatachalapathi , BALAJI, Vitukudi, Narayanaiyengar , RAMNARAYAN, Kalyanaraman
发明人： IMMUNOPHARMACEUTICS, INC.
IPC分类号： C07D261/14
CPC分类号： C07D413/12 , C07D261/14 , C07D261/16 , C07D261/20 , C07D413/14 , C07D417/12
摘要： Sulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided. The sulfonamides have formula (I) in which Ar is a 3- or 5-isoxazolyl and Ar is selected from among alkyl, including straight and branched chains, aromatic rings, fused aromatic rings and heterocyclic rings, including 5-membered heterocycles with one, two or more heteroatoms and fused ring analogs thereof and 6-membered rings with one, two or more heteroatoms and fused ring analogs thereof. Ar is preferably thiophenyl, furyl, pyrrolyl, naphthyl, and phenyl. Compounds in which Ar is a 4-halo-substituted isoxazole are more active than the corresponding alkyl-substituted compound and compounds in which Ar is substituted at this position with a higher alkyl tend to exhibit greater affinity for ETB receptors than the corresponding lower alkyl-substituted compound.
摘要翻译：提供磺酰胺和使用这些磺酰胺通过使受体与磺酰胺接触来抑制内皮素肽与内皮素受体结合的方法。还提供了通过施用有效量的一种或多种这些抑制或增加内皮素活性的磺酰胺或其前体来治疗内皮素介导的病症的方法。磺酰胺具有式（I），其中Ar 1是3-或5-异恶唑基，Ar 2选自烷基，包括直链和支链，芳环，稠合芳环和杂环，包括5 具有一个，两个或更多个杂原子及其稠环类似物和与其一个，两个或更多个杂原子和稠合环类似物的6-元环的杂环。 Ar 2优选为噻吩基，呋喃基，吡咯基，萘基和苯基。其中Ar 1是4-卤代 - 取代的异恶唑的化合物比相应的烷基取代的化合物更有活性，其中Ar 1在该位置被高级烷基取代的化合物往往表现出对ETB受体的更大的亲和力比相应的低级烷基取代的化合物。

10. 发明申请

WO2015102929A1 TRICYCLIC SULFONAMIDE DERIVATIVES 审中-公开
标题翻译：三聚磺胺衍生物
公开(公告)号：WO2015102929A1
公开(公告)日：2015-07-09
申请号：PCT/US2014/071174
申请日：2014-12-18
申请人： NOVARTIS AG , CHEN, Shuhui , HE, Haiying , LAGU, Bharat , QIN, Hua , WU, Chengde , XIAO, Yisong
发明人： CHEN, Shuhui , HE, Haiying , LAGU, Bharat , QIN, Hua , WU, Chengde , XIAO, Yisong
IPC分类号： C07D413/04 , C07D498/04 , C07D498/10 , A61K31/4439 , A61K31/42 , A61K31/5386 , A61K31/5365 , A61P29/00
CPC分类号： C07D498/10 , A61K31/424 , A61K31/4439 , A61K31/4745 , A61K31/519 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D413/04 , C07D498/04
摘要： The invention relates to derivatives of formula (I), wherein the substituents are as defined in the specification; to processes for the preparation of such derivatives; pharmaceutical compositions comprising such derivatives; such derivatives as a medicament; such derivatives for the treatment of pain.
摘要翻译：本发明涉及式（I）的衍生物，其中取代基如说明书中所定义; 制备此类衍生物的方法; 包含这些衍生物的药物组合物; 这种衍生物作为药物; 这类衍生物用于治疗疼痛。

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