公开(公告)号：US5908919A

公开(公告)日：1999-06-01

申请号：US476119

申请日：1995-06-07

Applicant: Lawrence M. Kauvar ,  Matthew H. Lyttle ,  Apparao Satyam

Inventor： Lawrence M. Kauvar ,  Matthew H. Lyttle ,  Apparao Satyam

IPC: A61K38/00 ,  A61K38/04 ,  A61P35/00 ,  C07K5/02 ,  C07K5/023 ,  C07K5/037 ,  C07K5/08 ,  A61K38/06

CPC classification number: C07K5/0215 ,  A61K38/00

Abstract: Compounds of the formula ##STR1## or of the formula ##STR2## or the amides, esters or salts thereof, wherein: S.sup.x is S.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.3 wherein R.sup.3 is alkyl (1-6C) or O--C.dbd.O or HN--C.dbd.O;each R of R.sup.1, and R.sup.2 is independently H or a noninterfering substituent;wherein (conj) represents a conjugated system capable of transmitting electrons;n is 0 or 1;YCO is selected from the group consisting of .gamma.-Glu, .gamma.-Glu-Gly, Glu, Glu-Gly, .beta.Asp, .beta.-Asp-Gly, Asp and Asp-Gly;AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of Formula 1; andN(Z) represents a reduced nitrogen-containing leaving group and L represents an electron-withdrawing leaving group,are useful as prodrugs and to generate active components released by the activity of glutathione S-transferase.

Abstract translation: 式或式的化合物或其酰胺，酯或盐，其中：Sx为S = O，O = S = O，S = NH，HN = S = O，Se = O，O = Se = O ，Se = NH，HN = Se = O，S + R3，其中R3是烷基（1-6C）或OC = O或HN-C = O; R 1的每个R和R 2独立地为H或非干扰取代基; 其中（conj）表示能够传输电子的共轭系统; n为0或1; YCO选自γ-Glu，γ-Glu-Gly，Glu，Glu-Gly，β-Asp，β-Asp-Gly，Asp和Asp-Gly; AAC是通过肽键与所述式1化合物的剩余部分连接的氨基酸; 并且N（Z）表示还原的含氮离去基团，L表示吸电子离去基团，可用作前药并产生通过谷胱甘肽S-转移酶活性释放的活性成分。

公开(公告)号：US5556942A

公开(公告)日：1996-09-17

申请号：US309005

申请日：1994-09-19

Applicant: Lawrence M. Kauvar ,  Matthew H. Lyttle ,  Apparao Satyam

Inventor： Lawrence M. Kauvar ,  Matthew H. Lyttle ,  Apparao Satyam

IPC: A61K38/00 ,  A61K38/06 ,  A61P31/12 ,  A61P35/00 ,  A61P43/00 ,  C07K5/02 ,  C07K5/037 ,  C12N9/10 ,  G01N30/02 ,  G01N33/573 ,  G01N33/574 ,  C07K5/083

CPC classification number: A61K38/06 ,  C07K5/0215 ,  C12N9/1088 ,  G01N33/573 ,  G01N33/57496 ,  G01N2333/91177 ,  G01N30/02

Abstract: Compounds of the formula: ##STR1## or the amides, esters or salts thereof, wherein: L is an electron withdrawing leaving group;S.sup.x is S.dbd.O, O.dbd.S.dbd.O, S.dbd.NH, HN.dbd.S.dbd.O, Se.dbd.O, O.dbd.Se.dbd.O, Se.dbd.NH, HN.dbd.Se.dbd.O, S.sup.+ R.sup.4 wherein R.sup.4 is alkyl (1-6C), or O--C.dbd.O or HN--C.dbd.O;each R of R.sup.1, R.sup.2 and R.sup.3 is independently H or a noninterfering substituent;n is 0, 1 or 2;Y is selected from the group consisting of ##STR2## wherein m is 1 or 2; and AA.sub.C is an amino acid linked through a peptide bond to the remainder of said compound of formula 1, are disclosed.These compounds are useful prodrugs for selective treatment of target tissues which contain compatible glutathione S-transferase (GST) isoenzymes, and simultaneously elevate the levels of GM progenitor cells in bone marrow.

Abstract translation: 下式的化合物：其中：L是吸电子离去基团; S x为S = O，O = S = O，S = NH，HN = S = O，Se = O，O = Se = O，Se = NH，HN = Se = O，S + 1-6C），或OC = O或HN-C = O; R 1，R 2和R 3的每个R独立地为H或非干扰取代基; n为0,1或2; Y选自 和，其中m为1或2; 并且AAC是通过肽键与所述式1化合物的其余部分连接的氨基酸。 这些化合物是用于选择性处理含有相容的谷胱甘肽S-转移酶（GST）同工酶的靶组织的有用的前药，并且同时提高骨髓中GM祖细胞的水平。

公开(公告)号：US08349901B2

公开(公告)日：2013-01-08

申请号：US12977838

申请日：2010-12-23

Applicant: Apparao Satyam

Inventor： Apparao Satyam

IPC: A61K31/105 ,  C07C323/12

CPC classification number: C07D305/14 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60 ,  A61K47/61 ,  C07C323/12 ,  C07C323/25 ,  C07C323/41 ,  C07C323/42 ,  C07C2601/14 ,  C07D207/26 ,  C07D211/22 ,  C07D211/90 ,  C07D213/82 ,  C07D233/91 ,  C07D253/075 ,  C07D261/08 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D411/14 ,  C07D413/12 ,  C07D495/04

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。 本发明还提供了制备方法和使用前药的方法，包括释放NO的前药，双前药和包含式I化合物的共价前药。

公开(公告)号：US20110269722A1

公开(公告)日：2011-11-03

申请号：US12977838

申请日：2010-12-23

Applicant: Apparao Satyam

Inventor： Apparao Satyam

IPC: A61K31/63 ,  A61K31/22 ,  C07C271/62 ,  A61K31/27 ,  C07C69/84 ,  A61K31/24 ,  C07D213/82 ,  A61K31/4406 ,  C07D209/26 ,  A61K31/405 ,  C07D253/075 ,  A61K31/53 ,  C07D207/16 ,  A61K31/40 ,  C07D237/34 ,  A61K31/502 ,  C07D261/08 ,  A61K31/42 ,  C07D231/12 ,  C07D317/70 ,  A61K31/58 ,  C07D211/94 ,  A61K31/45 ,  C07C309/70 ,  C07C321/14 ,  A61P13/00 ,  A61P13/10 ,  A61P25/28 ,  A61P27/02 ,  A61P27/16 ,  A61P9/00 ,  A61P19/00 ,  A61P37/08 ,  A61P17/00 ,  C07C69/22

CPC classification number: C07D305/14 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60 ,  A61K47/61 ,  C07C323/12 ,  C07C323/25 ,  C07C323/41 ,  C07C323/42 ,  C07C2601/14 ,  C07D207/26 ,  C07D211/22 ,  C07D211/90 ,  C07D213/82 ,  C07D233/91 ,  C07D253/075 ,  C07D261/08 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D411/14 ,  C07D413/12 ,  C07D495/04

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.

公开(公告)号：US20060046967A1

公开(公告)日：2006-03-02

申请号：US11213396

申请日：2005-08-26

Applicant: Apparao Satyam

Inventor： Apparao Satyam

IPC: A61K38/04 ,  A61K31/7072 ,  A61K31/455 ,  A61K31/53 ,  A61K31/4172 ,  A61K31/4178 ,  A61K31/337 ,  A61K31/21

CPC classification number: C07D305/14 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60 ,  A61K47/61 ,  C07C323/12 ,  C07C323/25 ,  C07C323/41 ,  C07C323/42 ,  C07C2601/14 ,  C07D207/26 ,  C07D211/22 ,  C07D211/90 ,  C07D213/82 ,  C07D233/91 ,  C07D253/075 ,  C07D261/08 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D411/14 ,  C07D413/12 ,  C07D495/04

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.

公开(公告)号：US06329431B1

公开(公告)日：2001-12-11

申请号：US08916088

申请日：1997-08-21

Applicant: Richard Sportsman ,  Hugo O. Villar ,  Lawrence M. Kauvar ,  Apparao Satyam

Inventor： Richard Sportsman ,  Hugo O. Villar ,  Lawrence M. Kauvar ,  Apparao Satyam

IPC: A01N4728

CPC classification number: C07C309/34 ,  C12Q1/34 ,  C12Q1/48 ,  G01N33/582 ,  G01N2333/62 ,  G01N2333/72 ,  G01N2333/9121 ,  G06F17/30905 ,  H04N21/2356 ,  H04N21/2541 ,  H04N21/25875 ,  H04N21/25891 ,  H04N21/4622 ,  H04N21/4782 ,  H04N21/4786

Abstract: Modulation of the activity of the insulin receptor, enhancement of glucose uptake by cells, and other effects significant in the control and management of diabetes are accomplished using compounds of the formula wherein each A is independently a proton-accepting substituent; each R is independently a noninterfering substituent; m is 0 or 1; n is 0, 1, or 2; and each linker is independently —NHCNHNH—, —NHCOO—, OCOO—,—CH═CH—, —CH═N—, —CH2CH2—, —NHCH2—, —OCO— or —COO—. Compounds in the genus of Formula (1) can also be used for structure activity studies to identify features responsible for the relevant activities.

Abstract translation: 胰岛素受体的活性调节，细胞葡萄糖摄取的增强以及糖尿病的控制和治疗中显着的其它作用是使用アルフラフラ座的化合物，每个A独立地是质子受体取代基;每个R独立地是非干扰的 取代基; m为0或1; n为0,1或2; 连接体独立为-NHCNHNH-，-NHCOO-，OCOO - ， - CH = CH - ， - CH = N - ， - CH2CH2 - ， - NHCH2-，-OCO-或-COO-。 式（1）属中的化合物也可用于结构活性研究，以鉴定负责相关活性的特征。

公开(公告)号：US5254664A

公开(公告)日：1993-10-19

申请号：US815227

申请日：1991-12-31

Applicant: Subhash C. Narang ,  Asutosh Nigam ,  Apparao Satyam ,  Susanna C. Ventura ,  Yoshihiro Arita

Inventor： Subhash C. Narang ,  Asutosh Nigam ,  Apparao Satyam ,  Susanna C. Ventura ,  Yoshihiro Arita

IPC: C08F226/06 ,  C08F26/00 ,  C08G8/28 ,  C08G69/44 ,  C08G73/02 ,  C08G73/04 ,  C08K5/00 ,  C08L101/00 ,  C08G69/00 ,  C08G8/04 ,  C08G14/02 ,  C08G14/04

CPC classification number: C08G8/28 ,  C08G69/44 ,  C08G73/0233 ,  Y10T428/31504

Abstract: A reaction of the compound (A) having at least two 2-oxazoline groups with the compound (B) having at least two functional groups of one or a plural kind selected from the group consisting of an aromatic hydroxyl group, an amino group and a thiol group proceeds in a short period of time to produce a cured resin with superior mechanical strength, heat resistance and adhesion properties.

Abstract translation: 具有至少两个2-恶唑啉基团的化合物（A）与具有至少两个选自芳族羟基，氨基和氨基的一种或多种官能团的化合物（B）的反应 硫醇基团在短时间内进行以产生具有优异的机械强度，耐热性和粘合性能的固化树脂。

公开(公告)号：US08354455B2

公开(公告)日：2013-01-15

申请号：US12977984

申请日：2010-12-23

Applicant: Apparao Satyam

Inventor： Apparao Satyam

IPC: A61K31/105 ,  C07C323/12

CPC classification number: C07D305/14 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60 ,  A61K47/61 ,  C07C323/12 ,  C07C323/25 ,  C07C323/41 ,  C07C323/42 ,  C07C2601/14 ,  C07D207/26 ,  C07D211/22 ,  C07D211/90 ,  C07D213/82 ,  C07D233/91 ,  C07D253/075 ,  C07D261/08 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D411/14 ,  C07D413/12 ,  C07D495/04

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.

公开(公告)号：US20110269709A1

公开(公告)日：2011-11-03

申请号：US12977929

申请日：2010-12-23

Applicant: Apparao Satyam

Inventor： Apparao Satyam

IPC: A61K31/7072 ,  A61K31/4406 ,  C07D213/82 ,  C07H19/06 ,  C07D241/04 ,  A61K31/495 ,  C07C69/712 ,  A61K31/27 ,  C07D207/27 ,  A61K31/4015 ,  C07D253/075 ,  A61K31/53 ,  C07D401/12 ,  C07D401/10 ,  A61K31/496 ,  C07C69/96 ,  C07C69/16 ,  C07D315/00 ,  C07C321/16 ,  C07C271/22 ,  C07C215/40 ,  C07C309/70 ,  A61P25/28 ,  A61P27/16 ,  A61P17/00 ,  A61P21/00 ,  A61P35/00 ,  A61P3/00 ,  A61P31/00 ,  A61P37/00 ,  A61P23/00 ,  C07D213/80

CPC classification number: C07D305/14 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60 ,  A61K47/61 ,  C07C323/12 ,  C07C323/25 ,  C07C323/41 ,  C07C323/42 ,  C07C2601/14 ,  C07D207/26 ,  C07D211/22 ,  C07D211/90 ,  C07D213/82 ,  C07D233/91 ,  C07D253/075 ,  C07D261/08 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D411/14 ,  C07D413/12 ,  C07D495/04

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.

公开(公告)号：US07932294B2

公开(公告)日：2011-04-26

申请号：US11213396

申请日：2005-08-26

Applicant: Apparao Satyam

Inventor： Apparao Satyam

IPC: A61K31/105 ,  C07C323/12

CPC classification number: C07D305/14 ,  A61K47/55 ,  A61K47/551 ,  A61K47/555 ,  A61K47/60 ,  A61K47/61 ,  C07C323/12 ,  C07C323/25 ,  C07C323/41 ,  C07C323/42 ,  C07C2601/14 ,  C07D207/26 ,  C07D211/22 ,  C07D211/90 ,  C07D213/82 ,  C07D233/91 ,  C07D253/075 ,  C07D261/08 ,  C07D295/088 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D411/14 ,  C07D413/12 ,  C07D495/04

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。 本发明还提供了制备方法和使用前药的方法，包括释放NO的前药，双前药和包含式I化合物的共价前药。