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1. 发明申请

WO2008094507A2 NOVEL FUSION COMPOUNDS 审中-公开
标题翻译：新型融合化合物
公开(公告)号：WO2008094507A2
公开(公告)日：2008-08-07
申请号：PCT/US2008/001092
申请日：2008-01-25
申请人： CELLICON BIOTECHNOLOGIES, INC. , LAZAROVA, Tsvetelina , THORMANN, Michael , ALMSTETTER, Michael , COTTAREL, Guillaume , RIESINGER, Steven, Wayne
发明人： LAZAROVA, Tsvetelina , THORMANN, Michael , ALMSTETTER, Michael , COTTAREL, Guillaume , RIESINGER, Steven, Wayne
CPC分类号： C07D471/04 , C07D405/12 , C07D499/46 , C07H17/00
摘要： The present invention relates to novel compounds derived from compounds having antibiotic activities. The invention further provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by anti-infective agents, particularly those relating to the management of bacterial infection.
摘要翻译：本发明涉及衍生自具有抗生素活性的化合物的新化合物。本发明进一步提供了包含本发明化合物的组合物以及这些组合物在治疗由抗感染剂，特别是与细菌感染的治疗有关的疾病和病症治疗的疾病和病症的方法中的用途。

2. 发明申请

WO2003033010A1 CYCLOSPORIN ANALOGS FOR THE TREATMENT OF AUTOIMMUNE DISEASES 审中-公开
标题翻译：用于治疗自身免疫性疾病的环磷酰胺类似物
公开(公告)号：WO2003033010A1
公开(公告)日：2003-04-24
申请号：PCT/US2002/032118
申请日：2002-10-11
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina , HAMANN, Blake , CHEN, Jason
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina , HAMANN, Blake , CHEN, Jason
IPC分类号： A61K38/00
CPC分类号： C07K7/645 , Y10S514/828
摘要： The present invention relates to a cyclosporin analog of the following , formula (I) or a pro-drug or pharmaceutically acceptable salt thereof: Formula (I). In particular, residue A maybe represented by either formula A1 or A2 as illustrated below: Formulas (A1) or (A2) where X is absent, -C1-C6-alkyl- or -C3-C6-cycloalkyl-; Y is selected from the groups: aryl, substituted aryl, heteroaryl, and substituted heteroaryl; residue B is - aAbu-, -Val-, -Thr- or -Nva-; and residue U is -(D)Ala-, -(D)Ser-, -[0-(2- hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- or -[0-(2-acyloxyethyl)(D)Ser]-. In a second embodiment, the present invention relates to the use of the cyclosporin analogs of the present invention or a pro-drug or pharmaceutically acceptable salt 20 thereof in pharmaceutical compositions for the treatment of autoimmune diseases or for the prevention of organ transplantation rejection in a subject. In a third embodiment, the present invention relates to processes for the production of novel cyclosporin analogs of the present invention. The present invention also contemplates method(s) of treatment of autoimmune diseases or prevention of 25 organ transplant rejection in a subject by administering to the subject therapeutically effective amounts of the cyclosporin analogs of the present invention with or without the concurrent use of other drugs or pharmaceutically acceptable carriers or excipients.
摘要翻译：本发明涉及以下的式（I）的环孢菌素类似物或其前药或其药学上可接受的盐：式（I）。特别地，残基A可以由式A1或A2表示，如下所示：式（A1）或（A2）其中X不存在，-C 1 -C 6 - 烷基 - 或-C 3 -C 6 - 环烷基 - ; Y选自芳基，取代的芳基，杂芳基和取代的杂芳基; 残基B是-aAbu-，-Val-，-Thr-或-Nva-; 并且残基U是 - （D）Ala-， - （D）Ser-， - [O-（2-羟乙基）（D）Ser] - ， - [O-酰基（D）Ser] - 或 - （2-酰氧基乙基）（D）丝氨酸] - 。在第二个实施方案中，本发明涉及本发明的环孢菌素类似物或其前药或其药学上可接受的盐20在药物组合物中用于治疗自身免疫疾病或用于预防器官移植排斥反应的用途学科。在第三个实施方案中，本发明涉及用于生产本发明的新型环孢菌素类似物的方法。本发明还考虑了通过给予本发明治疗有效量的本发明的环孢菌素类似物来治疗自身免疫疾病或预防受试者的器官移植排斥反应的方法，所述方法在或不同时使用其它药物或药学上可接受的载体或赋形剂。

3. 发明申请

WO2006108039A2 SUBSTITUTED AZETIDINONES 审中-公开
标题翻译：取代的AZETIDINONES
公开(公告)号：WO2006108039A2
公开(公告)日：2006-10-12
申请号：PCT/US2006/012665
申请日：2006-04-04
申请人： DAIAMED, INC. , BANNISTER, Thomas , CELATKA, Cassandra , CHANDRAKUMAR, Nizal, S , DENG, Hongfeng , GUO, Zihong , JIN, Lei , LAZAROVA, Tsvetelina , LIN, Jian , MOE, Scott, T. , NAGAFUJI, Pamela , NAVIA, Manuel , RIPKA, Amy , RYNKIEWICZ, Michael, J , SPEAR, Kerry, L , STRICKLER, James, E , XIE, Roger
发明人： BANNISTER, Thomas , CELATKA, Cassandra , CHANDRAKUMAR, Nizal, S , DENG, Hongfeng , GUO, Zihong , JIN, Lei , LAZAROVA, Tsvetelina , LIN, Jian , MOE, Scott, T. , NAGAFUJI, Pamela , NAVIA, Manuel , RIPKA, Amy , RYNKIEWICZ, Michael, J , SPEAR, Kerry, L , STRICKLER, James, E , XIE, Roger
IPC分类号： A61K31/397 , C07D403/02
CPC分类号： C07D405/06 , C07D205/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/14
摘要： Compounds are provided which have the structure of formula (1), wherein A, B, C, D, m, Y, Ra, Rc, Rd, and Rd' are as described herein, and which are useful as inhibitors of tryptase, thrombin, trypsin, Factor Xa, Factor Vila, Factor XIa, and urokinase-type plasminogen activator and may be employed in preventing and/or treating asthma, chronic asthma, allergic rhinitis, and thrombotic disorders.
摘要翻译：提供具有式（1）结构的化合物，其中A，B，C，D，m，Y，Ra，Rc，Rd和Rd'如本文所述，并且其可用作类胰蛋白酶，凝血酶的抑制剂，胰蛋白酶，因子Xa，因子VIIa，因子XIa和尿激酶型纤溶酶原激活剂，可用于预防和/或治疗哮喘，慢性哮喘，过敏性鼻炎和血栓形成障碍。

4. 发明申请

WO2004072108A1 CYCLOSPORINS FOR THE TREATMENT OF IMMUNE DISORDERS 审中-公开
标题翻译：用于治疗免疫障碍的环磷酰胺
公开(公告)号：WO2004072108A1
公开(公告)日：2004-08-26
申请号：PCT/US2004/003582
申请日：2004-02-06
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina , CHEN, Jason
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina , CHEN, Jason
IPC分类号： C07K7/64
CPC分类号： C07K7/645 , A61K38/00 , Y02P20/55
摘要： The present invention provides a cyclosporin of the following Formula (I), A compound of Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof: wherein: A is (A) X is selected from the group consisting of : -(CH 2 ) n - and -CH 2 -CH=CH-(CH 2 ) m -, where n is an integer of from 2 to 8 and m is an integer of from 2 to 5; Y is selected form the group consisting of: deuterium; halogen SCN; NCO; NCS; NO 2 ; OR 1 , where R 1 is selected from the group consisting of: C 1 -C 6 alkyl optionally substituted with aryl, substituted aryl, heteroaryl, substituted heteroaryl, halogen, C 3 -C 6 alkenyl optionally substituted with aryl, substituted aryl, heteroaryl, substituted heteroaryl, halogen, C 3 -C 6 alkynyl optionally substituted with aryl, substituted aryl, heteroaryl, substituted heteroaryl, halogen, aryl, substituted aryl, heteroaryl, and substituted heteroaryl; OC(O)-W-R 1 , wherein W is absent, -O-, or -NH-, and R 1 is as previously defined; OCH 2 SR 2 , wherein R 2 is C 1 -C 6 alkyl optionally substituted with aryl, substituted aryl, heteroaryl, substituted heteroaryl; SR 3 , wherein R 3 is selected from the group consisting of: hydrogen, thiol protecting group, and R 1 as previously defined; and S(O) n R 1 , where n in an integer 1 or 2 and R 1 is as previously defined; R is selected from the group consisting of: hydrogen and a hydroxyl protecting group; B is selected from the group consisting of : -αAbu-, -Val-, Thr- and -Nva-; and U is selected from the group consisting of: -(D)Ala-, -(D)Ser- -[O-(2 hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- and -[O-(2-acyloxyethyl)(D)Ser]-.
摘要翻译：本发明提供下述式（I）的环孢菌素，式（I）的化合物或其药学上可接受的盐，酯或前药：其中：A为（A）X选自：（CH 2）n - 和-CH 2 -CH = CH-（CH 2）m - ，其中n为2至8的整数，m为2至5的整数; Y选自：氘; 卤素SCN; NCO; NCS; NO2; OR 1，其中R 1选自：任选被芳基取代的芳基，杂芳基，取代的杂芳基，卤素，任选被芳基取代的C 3 -C 6烯基，取代的芳基，杂芳基，取代的杂芳基，卤素，任选被芳基，取代的芳基，杂芳基，取代的杂芳基，卤素，芳基，取代的芳基，杂芳基和取代的杂芳基取代的C 3 -C 6炔基; OC（O）-W-R 1，其中W不存在，-O-或-NH-，并且R 1如前所定义; OCH 2 S R 2，其中R 2是任选被芳基取代的芳基，杂芳基，取代的杂芳基的C 1 -C 6烷基; SR3，其中R3选自：如前所定义的氢，硫醇保护基和R1; 和S（O）nR1，其中整数1或2中的n和R 1如前所定义; R选自：氢和羟基保护基; B选自：-alphaAbu-，-Val-，Thr-和-Nva-; 并且U选自： - （D）Ala-， - （D）Ser- [O-（2-羟乙基）（D）Ser] - ， - [O-酰基（D）Ser] - 和 - [O-（2-酰氧基乙基）（D）丝氨酸] - 。

5. 发明申请

WO2003030834A2 CYCLOSPORIN ANALOGS FOR THE TREATMENT OF LUNG DISEASES 审中-公开
标题翻译：用于治疗肺疾病的环磷酰胺类似物
公开(公告)号：WO2003030834A2
公开(公告)日：2003-04-17
申请号：PCT/US2002/032646
申请日：2002-10-11
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina
IPC分类号： A61K
CPC分类号： C07K7/645 , A61K38/00
摘要： The present invention relates to a cyclosporin analog of the following formula (I) or a pro-drug or pharmaceutically acceptable salt thereof. In formula (I), the formula for residue A is formula (II), where X is absent, -C1-C6 alkyl-, or -C3-C6 cycloalkyl-; Y is selected from the groups: -C(O)-O-R1; -C(O)-S-R1; -C(O)-OCH 2 -OC(O)R2; -C(S)-O-R1; and -C(S)- S-R1; where R1 is hydrogen, C1-C6 alkyl optionally substituted with halogen, 15 heterocyclics, aryl, C1-C6 alkoxy or C1-C6 alkylthio or halogen substituted C1-C6 alkoxy, halogen substituted C1-C6 alkylthio and where R2 is C1-C6 alkyl optionally substituted with halogen, C1-C6 alkoxy, C1-C6 alkylthio heterocyclics or aryl; B is -αAbu-, -Val-, -Thr- or -Nva-; and U is -(D)Ala-, -(D)Ser- or -[O-(2-hydroxyethyl)(D)Ser]-, or -[O-acyl(D)Ser]- or -[O-(2-acyloxyethyl)(D)Ser]-. In a second embodiment, the present invention relates to the use of the cyclosporin analogs of the present invention or a pro-drug or pharmaceutically acceptable salt thereof in pharmaceutical compositions for the treatment of asthma and other diseases characterized by airflow obstruction in a subject. In a third embodiment, the present invention relates to processes for the production of novel cyclosporin analogs of the present invention. The present invention also contemplates method(s) of treatment of asthma and other diseases characterized by airflow obstruction in a subject by administering to the subject therapeutically effective amounts of the cyclosporin analogs of the present invention with or without the concurrent use of other drugs or pharmaceutically acceptable carriers or excipients.
摘要翻译：本发明涉及下式（I）的环孢菌素类似物或其前药或其药学上可接受的盐。在式（I）中，残基A的式为式（II），其中X不存在，-C 1 -C 6烷基 - 或-C 3 -C 6环烷基 - ; Y选自-C（O）-O-R 1; -C（O）-S-R 1; -C（O）-OCH 2-OC（O）R2; -C（S）-O-R1; 和-C（S）-S-R 1; 其中R 1是氢，任选被卤素取代的C 1 -C 6烷基，15个杂环基，芳基，C 1 -C 6烷氧基或C 1 -C 6烷硫基或卤素取代的C 1 -C 6烷氧基，卤素取代的C 1 -C 6烷硫基，其中R 2是C 1 -C 6烷基任选被卤素，C 1 -C 6烷氧基，C 1 -C 6烷硫基杂环或芳基取代; B为 - 阿布鲁，-Val-，-Thr-或-Nva-; 并且U是 - （D）Ala-， - （D）Ser-或 - [O-（2-羟乙基）（D）Ser] - 或 - [O-酰基（D）Ser] - 或 - （2-酰氧基乙基）（D）丝氨酸] - 。在第二个实施方案中，本发明涉及本发明的环孢菌素类似物或其前药或其药学上可接受的盐在药物组合物中用于治疗特征为受试者气道阻塞的哮喘和其它疾病的用途。在第三个实施方案中，本发明涉及用于生产本发明的新型环孢菌素类似物的方法。本发明还考虑了治疗哮喘和其它疾病的方法，其特征在于受试者的气流阻塞，其通过向受试者施用治疗有效量的本发明的环孢菌素类似物，同时使用或不同时使用其它药物或药学上可接受的载体或赋形剂。

6. 发明申请

WO2003030834A3 CYCLOSPORIN ANALOGS FOR THE TREATMENT OF LUNG DISEASES 审中-公开
公开(公告)号：WO2003030834A3
公开(公告)日：2003-04-17
申请号：PCT/US2002/032646
申请日：2002-10-11
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina
IPC分类号： A61K38/00
摘要： The present invention relates to a cyclosporin analog of the following formula (I) or a pro-drug or pharmaceutically acceptable salt thereof. In formula (I), the formula for residue A is formula (II), where X is absent, -C1-C6 alkyl-, or -C3-C6 cycloalkyl-; Y is selected from the groups: -C(O)-O-R1; -C(O)-S-R1; -C(O)-OCH 2 -OC(O)R2; -C(S)-O-R1; and -C(S)- S-R1; where R1 is hydrogen, C1-C6 alkyl optionally substituted with halogen, 15 heterocyclics, aryl, C1-C6 alkoxy or C1-C6 alkylthio or halogen substituted C1-C6 alkoxy, halogen substituted C1-C6 alkylthio and where R2 is C1-C6 alkyl optionally substituted with halogen, C1-C6 alkoxy, C1-C6 alkylthio heterocyclics or aryl; B is -αAbu-, -Val-, -Thr- or -Nva-; and U is -(D)Ala-, -(D)Ser- or -[O-(2-hydroxyethyl)(D)Ser]-, or -[O-acyl(D)Ser]- or -[O-(2-acyloxyethyl)(D)Ser]-. In a second embodiment, the present invention relates to the use of the cyclosporin analogs of the present invention or a pro-drug or pharmaceutically acceptable salt thereof in pharmaceutical compositions for the treatment of asthma and other diseases characterized by airflow obstruction in a subject. In a third embodiment, the present invention relates to processes for the production of novel cyclosporin analogs of the present invention. The present invention also contemplates method(s) of treatment of asthma and other diseases characterized by airflow obstruction in a subject by administering to the subject therapeutically effective amounts of the cyclosporin analogs of the present invention with or without the concurrent use of other drugs or pharmaceutically acceptable carriers or excipients.

7. 发明申请

WO2002069902A3 CYCLOSPORINS FOR THE TREATMENT OF RESPIRATORY DISEASES 审中-公开
公开(公告)号：WO2002069902A3
公开(公告)日：2002-09-12
申请号：PCT/US2002/006541
申请日：2002-03-05
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina , HAMANN, Blake, Christopher
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina , HAMANN, Blake, Christopher
IPC分类号： A61K38/13
摘要： The present invention relates to novel semisynthetic cyclosporin analogs of formula (I), wherein A is (II), X is absent, -C1-C6 alkyl-, or -C3-C6 cycloalkyl- Y is selected from the group consisting of: (i) C(O)-O-R1, where R1 is hydrogen, C1-C6-alkyl, optionally substituted with halogen, heterocyclic, aryl, C1-C6-alkoxy, C1-C6-alkylthio, halogen-substituted C1-C6-alkoxy, or halogen-substituted C1-C6-alkylthio; (ii) C(O)-S-R1 , where R1 is as previously defined; (iii) C(O)-OCH 2 -OC(O)R2, where R2 is C1-C6-alkyl, optionally substituted with halogen, C1-C6-alkoxy; C1-C6-alkylthio, heterocyclic or aryl; (iv) C(S)-O-R1 , where R1 is as previously defined; and (v) C(S)-S-R1 , where R1 is as previously defined; B is -αAbu-, -Val-, -Thr- or -Nva- ;U and is -(D)Ala-, -(D)Ser-, -[O-(2 -hydroxyethyl)(D)Ser]-, -[O-acyl(D)Ser]- or -[O-(2-acyloxyethyl) (D )Ser]-.

8. 发明申请

WO2002060912A1 14-MEMBERED MACROLIDES DERIVED FROM LEUCOMYCINS 审中-公开
标题翻译：来自卵巢癌的14种成纤维细胞
公开(公告)号：WO2002060912A1
公开(公告)日：2002-08-08
申请号：PCT/US2001/051041
申请日：2001-12-21
申请人： ENANTA PHARMACEUTICALS, INC. , OR, Yat, Sun , LAZAROVA, Tsvetelina , BINET, Sophie , WANG, Jianchao
发明人： OR, Yat, Sun , LAZAROVA, Tsvetelina , BINET, Sophie , WANG, Jianchao
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Novel 14-Membered Macrolides derived from Leucomycins comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, a method for treating bacterial infections by administering to a mammal a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.
摘要翻译：衍生自Leucomycins的新型14-成员的大环内酯类包括治疗有效量的本发明化合物与药学上可接受的载体的组合，通过向哺乳动物施用药物组合物来治疗细菌感染的方法，所述药物组合物包含治疗有效量的本发明及其制备方法。

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