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1. 发明申请

WO2013132317A1 PEPTIDOMIMETIC COMPOUNDS AS IMMUNOMODULATORS 审中-公开
标题翻译：作为免疫调节剂的肽化合物
公开(公告)号：WO2013132317A1
公开(公告)日：2013-09-12
申请号：PCT/IB2013/000493
申请日：2013-03-04
申请人： AURIGENE DISCOVERY TECHNOLOGIES LIMITED
发明人： POTTAYIL GOVINDAN NAIR, Sasikumar , RAMACHANDRA, Muralidhara , NAREMADDEPALLI SEETHARAMAIAH SETTY, Sudarshan
IPC分类号： C07K5/02
CPC分类号： A61K31/197 , A61K31/16 , A61K31/222 , A61K31/405 , A61K45/06 , C07C243/34 , C07C275/16 , C07C327/56 , C07C335/08 , C07D209/18 , C07D209/20 , C07K5/0217 , Y02A50/411
摘要： The present invention relates to novel peptidomimetic compounds as therapeutic agents capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The invention also relates to derivatives of the therapeutic agents. The invention also encompasses the use of the said therapeutic agents and derivatives for treatment of disorders via immunopotentiation comprising inhibition of immunosuppressive signal induced due to PD-1, PD-L1, or PD-L2 and therapies using them.
摘要翻译：本发明涉及新颖的拟肽化合物作为能够抑制程序性细胞死亡1（PD1）信号通路的治疗剂。本发明还涉及治疗剂的衍生物。本发明还包括所述治疗剂和衍生物用于通过免疫激活治疗疾病的用途，包括抑制由于PD-1，PD-L1或PD-L2引起的免疫抑制信号和使用它们的疗法。

2. 发明申请

WO2009102997A2 ACETYL MIMIC COMPOUNDS FOR THE INHIBITION OF ISOPRENYL-S-CYSTEINYL METHYLTRANSFERASE 审中-公开
标题翻译：用于抑制异丙肾上腺素甲基衍生物的乙炔化合物
公开(公告)号：WO2009102997A2
公开(公告)日：2009-08-20
申请号：PCT/US2009034120
申请日：2009-02-13
申请人： SIGNUM BIOSCIENCES INC , LEE SEUNG-YUB , VORONKOV MICHAEL , WOLANIN PETER
发明人： LEE SEUNG-YUB , VORONKOV MICHAEL , WOLANIN PETER
IPC分类号： A61K31/5377
CPC分类号： C07D233/88 , C07C323/57 , C07C323/58 , C07C323/59 , C07C323/60 , C07C327/42 , C07C335/08 , C07D207/22 , C07D207/34 , C07D213/74 , C07D233/70 , C07D235/14 , C07D239/42 , C07D249/04 , C07D257/04 , C07D263/48 , C07D265/30 , C07D277/42 , C07D295/215 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： Among other things, the present invention provides novel compounds capable of effectively inhibiting inflammatory responses that are mediated by G-proteins or GPCRs in neutrophils, macrophages and platelets. In particular, compounds of the present invention act as inhibitors of edema, inhibitors of erythema and inhibitors of MPO (myeloperoxidase), pharmaceutical compositions containing the same compounds and the use thereof for the treatment of diseases that may benefit from edema, erythema and MPO inhibition, such as inflammation (acute or chronic), asthma, autoimmune diseases, and chronic obstructive pulmonary disease (COPD) (e.g., emphysema, chronic bronchitis and small airways disease, etc.), inflammatory responses of the immune system, skin diseases (e.g., reducing acute skin irritation for patients suffering from rosacea, atopic dermatitis, seborrheic dermatitis, psoriasis), irritable bowel syndrome (e.g., Chron's disease and ulcerative colitis, etc.), and central nervous system disorders (e.g., Parkinson's disease).
摘要翻译：除此之外，本发明提供能够有效抑制嗜中性粒细胞，巨噬细胞和血小板中G蛋白或GPCR介导的炎症反应的新型化合物。特别地，本发明的化合物作为水肿抑制剂，红斑抑制剂和MPO抑制剂（髓过氧化物酶），含有相同化合物的药物组合物及其用于治疗可能受益于水肿，红斑和MPO抑制的疾病的用途例如炎症（急性或慢性），哮喘，自身免疫疾病和慢性阻塞性肺病（COPD）（例如肺气肿，慢性支气管炎和小气道疾病等），免疫系统的炎症反应，皮肤疾病（例如对于患有酒渣鼻，特应性皮炎，脂溢性皮炎，牛皮癣的患者，肠易激综合征（例如，Chron氏病和溃疡性结肠炎等）以及中枢神经系统疾病（例如帕金森氏病））减少急性皮肤刺激。

3. 发明申请

WO02083627A3 LIGANDS DES INTEGRINS AVSS6 审中-公开
标题翻译：整ALPHA-V的配位体BETA-6
公开(公告)号：WO02083627A3
公开(公告)日：2003-10-09
申请号：PCT/EP0202728
申请日：2002-03-13
申请人： MERCK PATENT GMBH , SCHADT OLIVER , JONCZYK ALFRED , STAEHLE WOLFGANG , GOODMAN SIMON
发明人： SCHADT OLIVER , JONCZYK ALFRED , STAEHLE WOLFGANG , GOODMAN SIMON
IPC分类号： A61P1/04 , A61K31/19 , A61K31/197 , A61K31/27 , A61P1/16 , A61P3/10 , A61P3/14 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P11/00 , A61P13/00 , A61P13/02 , A61P13/12 , A61P15/00 , A61P15/08 , A61P17/00 , A61P17/02 , A61P17/06 , A61P19/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P27/00 , A61P27/02 , A61P27/06 , A61P27/10 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P33/00 , A61P35/00 , A61P35/02 , A61P37/04 , A61P43/00 , C07C269/06 , C07C271/22 , C07C273/18 , C07C275/16 , C07C275/18 , C07C275/20 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C275/42 , C07C335/08 , C07C335/12 , C07K5/023 , A61K31/17
CPC分类号： C07C275/20 , C07B2200/07 , C07C271/22 , C07C275/16 , C07C275/18 , C07C275/24 , C07C275/26 , C07C275/28 , C07C275/30 , C07C275/34 , C07C335/08 , C07C335/12 , C07C2601/14 , C07C2603/18
摘要： The invention relates to the novel biphenyl derivatives of the general formula (I), wherein R , R ', R '', R and n are defined as in claim 1. The invention also relates to the stereoisomers and the physiologically acceptable salts or solvates thereof which represent novel integrin ligands, especially of the alphavbeta6 integrin receptor. The novel compounds are suitable for use as medicaments.
摘要翻译：（I）通式的新的联苯衍生物，其中R <1>，R <1> 'R <1>'，R <2>和n具有权利要求1中给出的含义，它们的立体异构体及其生理学可接受的盐或溶剂化物是新的整合，尤其是alphavbeta6整合。新的化合物可以用作药物。

4. 发明申请

WO2003000643A1 NITRATE ESTER DERIVATIVES USEFUL FOR PREPARING DRUGS FOR EPILEPSY 审中-公开
标题翻译：用于制备药物的硝酸酯衍生物有用
公开(公告)号：WO2003000643A1
公开(公告)日：2003-01-03
申请号：PCT/EP2002/006389
申请日：2002-06-11
申请人： NICOX S.A. , ONGINI, Ennio , DEL SOLDATO, Piero
发明人： ONGINI, Ennio , DEL SOLDATO, Piero
IPC分类号： C07C203/04
CPC分类号： C07D213/30 , C07C203/04 , C07C229/08 , C07C229/28 , C07C279/12 , C07C279/14 , C07C327/34 , C07C335/08 , C07C2601/14
摘要： Nitrooxyderivative compounds or salts thereof having the following general formula (I): A-(B) b0 -(C) co -NO 2 (I) wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A = R-T 1 -, wherein R is the radical of formula (II) as defined in the application; B is such that its precursor is selected from aminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid acid function, C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.
摘要翻译：具有以下通式（I）的硝基氧化还原化合物或其盐：A-（B）b0-（C）co-NO2（I）其中：c0为整数，为0或1，b0为整数，为0或 1，A = R-T1-，其中R是如申请中定义的式（II）的基团; B的前体选自氨基酸，羟基酸，多元醇，含有至少一个酸性官能团的化合物，C是含有脂族，杂环或芳族基团的二价基团。

5. 发明申请

WO2002068384A2 (2-HYDROXY)ETHYL-THIOUREAS USEFUL AS MODULATORS OF ALPHA2B ADRENERGIC RECEPTORS 审中-公开
标题翻译：（2-羟基）乙二醇作为ALPHA2B ADRENERGIC受体的调节剂有用
公开(公告)号：WO2002068384A2
公开(公告)日：2002-09-06
申请号：PCT/US2002/005021
申请日：2002-02-19
申请人： ALLERGAN SALES, INC.
发明人： CHOW, Ken , GIL, Daniel, W. , FANG, Wenkui, Ken , GARST, Michael, E.
IPC分类号： C07C335/08
CPC分类号： C07C335/10 , C07C335/08 , C07C335/14 , C07C2601/08 , C07C2601/10 , C07C2601/14 , C07C2601/16 , C07C2601/18
摘要： Compounds of formula (i) and of formula (ii), wherein the symbols have the meaning disclosed in the specification, specifically or selectively modulate α 2B and/or α 2C adrenergic receptors in preference over α 2A adrenergic receptors, and as such are useful for alleviating chronic pain and allodynia and have no or only minimal cardivascular and/or sedatory activity.
摘要翻译：式（ⅰ）和式（ⅱ）的化合物，其中符号具有权利要求中公开的含义，具体地或选择性调节α2A肾上腺素能受体，因此可用于缓解慢性疼痛和异常性疼痛，并且没有或仅有最小的心血管和/或镇静活性。本发明还涉及通过施用具有α2B或α2C肾上腺素能受体活性并且没有显着的α2A激动剂活性的化合物来激活哺乳动物中α2B或α2C肾上腺素能受体的方法。

6. 发明申请

WO2002068383A2 THIOL-MODIFIED HYALURONAN 审中-公开
标题翻译： THIOL改性HYALURONONAN
公开(公告)号：WO2002068383A2
公开(公告)日：2002-09-06
申请号：PCT/US2002/005081
申请日：2002-02-21
申请人： ANIKA THERAPEUTICS, INC.
发明人： BULPITT, Paul, C., A. , SHERWOOD, Charles, H. , SADOZAI, Khalid, K.
IPC分类号： C07C323/25
CPC分类号： C07C323/25 , C07C323/32 , C07C323/37 , C07C323/44 , C07C335/08 , C07C335/16 , C08B37/0072
摘要： The present invention relates to biscarbodiimides, thiourea derivatives, urea derivatives, and cross-linked hyaluronan derivatives having at least one intramolecular disulfide bond, and methods of preparation thereof. The invention also includes thiolated hyaluronan derivatives and salts thereof having at least one pendant thiol group or a modified pendant thiol group, and methods of preparation thereof. An example of a modified pendant thiol group is a sulfhydryl group linked to a small molecule such as a bioactive agent, for example a drug or pharmaceutically active moiety. A hyaluronan derivative having a sulfhydryl group linked to a pharmaceutically active moiety is useful as a sustained or controlled release drug delivery vehicle. Compositions containing the hyaluronan derivatives of the invention can reversibly viscosify in vivo or in vitro , in response to mild changes in condition, and are thus useful in ophthalmic surgery and in tissue engineering.
摘要翻译：本发明涉及双碳二亚胺，硫脲衍生物，脲衍生物和具有至少一个分子内二硫键的交联透明质酸衍生物及其制备方法。本发明还包括硫醇化透明质酸衍生物及其盐，其具有至少一个硫醇基侧基或修饰侧链巯基，及其制备方法。修饰的侧链硫醇基团的实例是与小分子连接的巯基，例如生物活性剂，例如药物或药学活性部分。具有与药学活性部分连接的巯基的透明质酸衍生物可用作持续或控释药物递送载体。包含本发明的透明质酸衍生物的组合物可以在体内或体外可逆地粘稠，以响应于条件的轻微变化，因此可用于眼科手术和组织工程。

7. 发明申请

WO0064911A9 LIGANDS FOR METABOTROPIC GLUTAMATE RECEPTORS 审中-公开
标题翻译：代谢谷氨酸受体的配体
公开(公告)号：WO0064911A9
公开(公告)日：2002-07-11
申请号：PCT/US0011262
申请日：2000-04-27
申请人： UNIV GEORGETOWN
发明人： KOZIKOWSKI ALAN P , WROBLEWSKI JARDA T , NAN FAJUN
IPC分类号： A61K31/662 , A61K31/194 , A61K31/197 , A61K31/198 , A61K31/22 , A61K31/225 , A61P3/00 , A61P9/00 , A61P9/10 , A61P25/00 , A61P25/02 , A61P25/08 , A61P25/16 , A61P25/28 , A61P31/04 , A61P39/00 , A61P41/00 , A61P43/00 , C07C59/347 , C07C69/716 , C07C275/16 , C07C335/08 , C07F9/30 , C07F9/32 , C07C273/16
CPC分类号： C07C335/08 , C07C59/347 , C07C69/716 , C07F9/301
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

8. 发明申请

WO01058855A1 USE OF ANDROGEN RECEPTOR SUPPRESSORS 审中-公开
标题翻译：治疗中的安哥拉受体抑制剂和前列腺癌，ALOPECIA和其他高发病综合征的诊断
公开(公告)号：WO01058855A1
公开(公告)日：2001-08-16
申请号：PCT/US2001/004290
申请日：2001-02-09
申请人： BIOPHYSICA, INC
发明人： SOVAK, Milos , SELIGSON, Allen , DOUGLASS, James, Gordon, III , BROWN, Jason, W. , CAMPION, Brian
IPC分类号： C07C237/22
CPC分类号： C07C237/04 , A61K31/165 , C07C237/22 , C07C255/56 , C07C255/60 , C07C275/30 , C07C317/46 , C07C323/60 , C07C335/08 , C07C335/16 , C07C335/22 , C07C2601/14 , C07D207/408 , C07D233/86 , C07D233/88
摘要： Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in indications associated with the androgen receptor, such as cell hyperplasia dependent on androgens, hirsutism, acne and androgenetic alopecia.
摘要翻译：提供了取代的苯丙氨酸，其包括乙内酰脲，脲或2-羟基，2-甲基丙酰基，其二聚体和其烷基，聚氟代氨基和卤代芳基氨基衍生物，以及其放射性标记的衍生物。这些化合物特异性结合雄激素受体，可用于与雄激素受体有关的适应症，如依赖雄激素，多毛症，痤疮和雄激素性脱发的细胞增生。

9. 发明申请

WO99063940A3 INHIBITORS OF H<+>K<+>-ATPase 审中-公开
标题翻译： H + ATP酶抑制剂
公开(公告)号：WO99063940A3
公开(公告)日：2001-06-07
申请号：PCT/US1999/012925
申请日：1999-06-08
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
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 , Y02A50/401 , Y02A50/57 , 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”）。

10. 发明申请

WO9964033A9 PHOSPHODIESTERASE-V MODULATOR DRUGS AND THEIR USES 审中-公开
标题翻译：磷酸二酯酶-V调节剂药物及其用途
公开(公告)号：WO9964033A9
公开(公告)日：2000-07-27
申请号：PCT/US9911800
申请日：1999-06-07
申请人： ADVANCED MEDICINE INC , KLEIN UWE , ZHU YAN , GRIFFIN JOHN H
发明人： KLEIN UWE , ZHU YAN , GRIFFIN JOHN H
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
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： This invention relates to novel multibinding compounds that bind to the enzyme phosphodiesterase V (PDE V) and modulate its activity. The compounds of this invention comprise 2-10 PDE V modulator (particularly inhibitor) ligands covalently connected by a linker or linkers, wherein the ligands in their monovalent (i.e., unlinked) state bind to a PDE V enzyme. The manner of linking the ligands together is such that the multibinding agents thus formed demonstrate an increased biologic and/or therapeutic effect as compared to the same number of unlinked ligands made available for binding to PDE V. The invention also relates to methods of using such compounds and to methods of preparing them. The compounds of this invention are particularly useful for treating diseases and conditions of mammals that are mediated by PDE V. Accordingly, this invention also relates to pharmaceutical compositions comprising a pharmaceutically acceptable excipient and an effective amount of a compound of this invention.
摘要翻译：本发明涉及结合酶磷酸二酯酶V（PDE V）并调节其活性的新型多结合化合物。本发明的化合物包含通过接头或接头共价连接的2-10个PDE V调节剂（特别是抑制剂）配体，其中其单价（即未连接）状态的配体与PDE V酶结合。将配体连接在一起的方式使得如此形成的多结合剂与可用于与PDE V结合的相同数目的未连接的配体相比，显示增加的生物学和/或治疗效果。本发明还涉及使用这些化合物及其制备方法。本发明的化合物特别可用于治疗由PDE V介导的哺乳动物的疾病和病症。因此，本发明还涉及包含药学上可接受的赋形剂和有效量的本发明化合物的药物组合物。

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