公开(公告)号：WO2006012527A1

公开(公告)日：2006-02-02

申请号：PCT/US2005/026068

申请日：2005-07-22

Applicant: ENDOCYTE, INC. ,  VLAHOV, Iontcho, Radoslavov ,  LEAMON, Christopher, Paul ,  SATYAM, Apparao ,  HOWARD, Stephen, J.

Inventor： VLAHOV, Iontcho, Radoslavov ,  LEAMON, Christopher, Paul ,  SATYAM, Apparao ,  HOWARD, Stephen, J.

IPC: C07D213/71

CPC classification number: C07D213/71 ,  A61K47/551 ,  A61K47/6803 ,  A61K49/0002 ,  C07D401/12 ,  C07D475/04

Abstract: Bivalent linkers derived from compounds of formulae (V), (VI) and (VII), where X 1 and X 2 are leaving groups and the other variables are as defined in the claims, to be included in or for preparing vitamin, drug, diagnostic agent, and/or imaging agent conjugates are described.

Abstract translation: 衍生自式（V），（VI）和（VII）的化合物的二价连接体，其中L是离去基团，其它变量如权利要求中所定义，被包括在维生素，药物，诊断剂， 和/或成像剂缀合物。

公开(公告)号：EP2560634A1

公开(公告)日：2013-02-27

申请号：EP11725808.7

申请日：2011-04-21

Applicant: Piramal Enterprises Limited ,  Satyam, Apparao

Inventor： SATYAM, Apparao

IPC: A61K31/21 ,  A61P9/00 ,  A61P29/00 ,  C07C203/04 ,  C07C229/42 ,  C07C233/25 ,  C07C233/63 ,  C07C317/18 ,  C07C323/12 ,  C07D207/34 ,  C07D209/28 ,  C07D209/52 ,  C07D211/90 ,  C07D213/80 ,  C07D223/22

CPC classification number: C07C203/04 ,  C07C229/42 ,  C07C233/25 ,  C07C233/63 ,  C07C317/18 ,  C07C323/12 ,  C07C2601/14 ,  C07D207/27 ,  C07D207/34 ,  C07D209/28 ,  C07D209/52 ,  C07D213/30 ,  C07D213/80 ,  C07D223/26 ,  C07D223/28 ,  C07D233/91 ,  C07D295/088 ,  C07D305/14 ,  C07D307/20 ,  C07D401/12 ,  C07D403/10 ,  C07D493/04 ,  C07J41/005 ,  C07J71/0031

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them. The present invention also relates to use of the compounds of formula (I) for the treatment of diseases or disorders for which the known drugs or therapeutic agents are used. The present invention also relates to method of treatment of diseases or disorders in humans or mammals by administering therapeutically effective amount of the compounds of formula (I) to said humans or mammals.

Abstract translation: 本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在本文中表示为式（I）化合物，其中药物或治疗剂含有一个或多个独立地选自羧酸，氨基，羟基的官能团 和巯基。 本发明还涉及制备一氧化氮释放前体药物（式（I）化合物）的方法，含有它们的药物组合物和使用前药的方法。

公开(公告)号：WO2014111957A1

公开(公告)日：2014-07-24

申请号：PCT/IN2014/000033

申请日：2014-01-17

Applicant: SATYAM, Apparao

Inventor： SATYAM, Apparao

IPC: C07C203/04 ,  A61K31/216 ,  A61K31/621 ,  A61P35/00 ,  A61P29/00 ,  A61P29/02 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P1/04 ,  A61P25/24 ,  A61P25/08 ,  A61P31/04 ,  A61P33/06 ,  A61P39/06

CPC classification number: A61K47/542 ,  A61K31/21 ,  A61K31/216 ,  A61K31/60 ,  A61K47/55 ,  C07C201/04 ,  C07C203/04 ,  C07C227/18 ,  C07C229/42

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents wherein the drug or therapeutic agents contain at least one carboxylic acid group. The invention also relates to processes for the preparation of these nitric oxide releasing prodrugs, to pharmaceutical compositions containing them and to methods of using these prodrugs.

Abstract translation: 本发明涉及已知药物或治疗剂的一氧化氮释放前药，其中药物或治疗剂含有至少一个羧酸基团。 本发明还涉及制备这些一氧化氮释放前药的方法，含有它们的药物组合物和使用这些前药的方法。

公开(公告)号：WO2006027711A2

公开(公告)日：2006-03-16

申请号：PCT/IB2005/052797

申请日：2005-08-26

Applicant: NICHOLAS PIRAMAL INDIA LIMITED ,  SATYAM, Apparao

Inventor： SATYAM, Apparao

IPC: A61K47/48

CPC classification number: A61K47/61 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60

Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula (I) or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula (I).

Abstract translation: 本发明提供式（I）化合物或其药学上可接受的盐。 本发明还提供包含一种或多种式（I）化合物或其中间体和另外一种药学上可接受的载体，载体或稀释剂的药物组合物。 本发明进一步提供了制备方法和前药的使用方法，包括释放NO的前药，双前药和包含式（I）化合物的联合前药。

公开(公告)号：WO2011132171A1

公开(公告)日：2011-10-27

申请号：PCT/IB2011/051751

申请日：2011-04-21

Applicant: PIRAMAL LIFE SCIENCES LIMITED ,  SATYAM, Apparao

Inventor： SATYAM, Apparao

IPC: A61K31/21 ,  A61P9/00 ,  A61P29/00 ,  C07C203/04 ,  C07C229/42 ,  C07C233/25 ,  C07C233/63 ,  C07C317/18 ,  C07C323/12 ,  C07D207/34 ,  C07D209/28 ,  C07D209/52 ,  C07D211/90 ,  C07D213/80 ,  C07D223/22

CPC classification number: C07C203/04 ,  C07C229/42 ,  C07C233/25 ,  C07C233/63 ,  C07C317/18 ,  C07C323/12 ,  C07C2601/14 ,  C07D207/27 ,  C07D207/34 ,  C07D209/28 ,  C07D209/52 ,  C07D213/30 ,  C07D213/80 ,  C07D223/26 ,  C07D223/28 ,  C07D233/91 ,  C07D295/088 ,  C07D305/14 ,  C07D307/20 ,  C07D401/12 ,  C07D403/10 ,  C07D493/04 ,  C07J41/005 ,  C07J71/0031

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them. The present invention also relates to use of the compounds of formula (I) for the treatment of diseases or disorders for which the known drugs or therapeutic agents are used. The present invention also relates to method of treatment of diseases or disorders in humans or mammals by administering therapeutically effective amount of the compounds of formula (I) to said humans or mammals.

Abstract translation: 本发明涉及已知药物或治疗剂的一氧化氮释放前药，其在本文中表示为式（I）化合物，其中药物或治疗剂含有一个或多个独立地选自羧酸，氨基，羟基的官能团 和巯基。 本发明还涉及制备一氧化氮释放前体药物（式（I）化合物）的方法，含有它们的药物组合物。 本发明还涉及式（I）化合物用于治疗已知药物或治疗剂的疾病或病症的用途。 本发明还涉及通过向所述人或哺乳动物施用治疗有效量的式（I）化合物来治疗人或哺乳动物疾病或病症的方法。

公开(公告)号：WO2004069159A2

公开(公告)日：2004-08-19

申请号：PCT/US2004/002070

申请日：2004-01-27

Applicant: ENDOCYTE, INC. ,  VLAHOV, Iontcho, Radoslavov ,  LEAMON, Christopher, Paul ,  PARKER, Matthew, A. ,  HOWARD, Stephen, J. ,  SANTHAPURAM, Hari, Krishna ,  SATYAM, Apparao ,  REDDY, Joseph, Anand

Inventor： VLAHOV, Iontcho, Radoslavov ,  LEAMON, Christopher, Paul ,  PARKER, Matthew, A. ,  HOWARD, Stephen, J. ,  SANTHAPURAM, Hari, Krishna ,  SATYAM, Apparao ,  REDDY, Joseph, Anand

IPC: A61K

CPC classification number: A61K47/48569 ,  A61K47/48384 ,  A61K47/484 ,  A61K47/48715 ,  A61K47/551 ,  A61K47/65 ,  A61K47/6803 ,  A61K47/6807 ,  A61K47/6851 ,  A61K47/6889 ,  C07K16/30 ,  C07K2317/55

Abstract: The invention describes a vitamin receptor binding drug delivery conjugate, and preparations therefor. The drug delivery conjugate consists of a vitamin receptor binding moiety, a bivalent linker (L), and a drug. The vitamin receptor binding moiety is a vitamin, or a vitamin receptor binding analog or a derivative thereof, and the drug includes analogs or derivatives thereof. The vitamin receptor binding moiety is covalently linked to the bivalent linker, and the drug, or the analog or the derivative thereof, is covalently linked to the bivalent linker, wherein the bivalent linker (L) comprises one or more spacer linkers, releasable linkers, and heteroatom linkers. Methods and pharmaceutical compositions for eliminating pathogenic cell populations using the drug delivery conjugate are also described.

Abstract translation: 本发明描述了维生素受体结合药物递送缀合物及其制备方法。 药物递送缀合物由维生素受体结合部分，二价连接体（L）和药物组成。 维生素受体结合部分是维生素或维生素受体结合类似物或其衍生物，并且该药物包括其类似物或衍生物。 维生素受体结合部分与二价连接体共价连接，并且药物或其类似物或衍生物与二价连接体共价连接，其中二价连接体（L）包含一个或多个间隔基连接体，可释放接头， 和杂原子接头。 还描述了使用药物递送缀合物消除致病细胞群的方法和药物组合物。