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1. 发明申请

WO1995007901A1 SUBSTITUTED TETRONIC ACIDS USEFUL FOR TREATING HIV AND OTHER RETROVIRUSES 审中-公开
标题翻译：用于治疗艾滋病毒和其他复发性紫癜的替代疗法
公开(公告)号：WO1995007901A1
公开(公告)日：1995-03-23
申请号：PCT/US1994009533
申请日：1994-09-07
申请人： THE UPJOHN COMPANY , CHRUSCIEL, Robert, A. , MAGGIORA, Linda, L. , THAISRIVONGS, Suvit , TUSTIN, James, M. , SMITH, Clark, W. , TOMMASI, Rubin, A. , ARISTOFF, Paul, A. , SKULNICK, Harvey, I. , HOWE, W., Jeffrey , BUNDY, Gordon, L.
发明人： THE UPJOHN COMPANY
IPC分类号： C07D307/60
CPC分类号： C07D405/06 , C07D307/60 , C07D307/94 , C07D405/12 , C07D417/12 , C07D473/00 , C07D491/10
摘要： The invention comprises novel substituted tetronic acid type compounds, 2,4-(3H,5H)-furandiones, that are useful for the inhibition of the HIV protease enzyme. The compounds may be useful for the treatment of a person with AIDS or AIDS related diseases. The compounds may be used in the attempt to retard the further replication of any retrovirus containing the aspartyl protease enzyme. Compounds are represented by formula (1), wherein 3 tautomers of the same structure are shown, R1, R2 and R3 are replaced with various substituents.
摘要翻译：本发明包括可用于抑制HIV蛋白酶的新型取代的tetronic酸型化合物2,4-（3H，5H） - 呋喃二酮。该化合物可用于治疗患有AIDS或AIDS相关疾病的人。可以使用这些化合物来试图阻止含有天冬氨酰蛋白酶的任何逆转录病毒的进一步复制。化合物由式（1）表示，其中示出了相同结构的3个互变异构体，R1，R2和R3被各种取代基取代。

2. 发明申请

WO1992003472A1 PEPTIDES CONTAINING AMINO-POLYOLS AS TRANSITION-STATE MIMICS 审中-公开
标题翻译：含有氨基多元醇作为过渡态MIMIC的肽
公开(公告)号：WO1992003472A1
公开(公告)日：1992-03-05
申请号：PCT/US1991005727
申请日：1991-08-19
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/06
CPC分类号： C07D233/64 , A61K38/00 , C07K5/0202 , C07K5/06078 , C07K9/005
摘要： The present invention provides novel peptides. These peptides have a novel non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen) of formula (XL8). These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodeficiency disease syndrome (AIDS).
摘要翻译：本发明提供新的肽。这些肽具有对应于式（XL8）的肾素底物（血管紧张素原）的10,11位的新型不可切割过渡态插入物。这些肽可用作肾素抑制剂和作为逆转录病毒蛋白酶的抑制剂。肾素抑制剂可用于诊断和控制肾素依赖性高血压，充血性心力衰竭，肾素依赖性醛固酮增多症，其他肾素依赖性心血管疾病和眼部疾病。逆转录病毒蛋白酶如HIV-1蛋白酶的抑制剂可用于治疗由逆转录病毒引起的疾病，例如人类获得性免疫缺陷综合症（AIDS）。

3. 发明申请

WO1991007430A1 PEPTIDES CONTAINING CYCLIC TRIPEPTIDES 审中-公开
标题翻译：含有环孢霉素的肽
公开(公告)号：WO1991007430A1
公开(公告)日：1991-05-30
申请号：PCT/US1990005744
申请日：1990-10-12
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/02
CPC分类号： C07K7/54 , A61K38/00 , C07K5/0215
摘要： The present invention provides novel peptides. These peptides are useful as renin inhibitors and have a novel cyclic tripeptide of formula (I) at the N-terminus. Some of these peptides also have a non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen). Renin inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. These peptides are also useful as inhibitors of HIV-I protease. Inhibitors of HIV-I protease are useful for treating humain acquired immunodeficiency disease syndrome (AIDS).
摘要翻译：本发明提供新的肽。这些肽可用作肾素抑制剂，并且在N-末端具有新的式（I）的环状三肽。这些肽中的一些还具有对应于肾素底物（血管紧张素原）的10,11位的不可切割的过渡态插入物。肾素抑制剂可用于诊断和控制肾素依赖性高血压，充血性心力衰竭，肾素依赖性醛固酮增多症，其他肾素依赖型心血管疾病和眼部疾病。这些肽也可用作HIV-1蛋白酶的抑制剂。 HIV-1蛋白酶抑制剂可用于治疗人类获得性免疫缺陷综合征（AIDS）。

4. 发明申请

WO1990002137A1 RENIN INHIBITORY PEPTIDES CONTAINING SULEPTANIC ACID OR DERIVATIVES THEREOF 审中-公开
标题翻译：含有亚油酸或其衍生物的RENIN抑制肽
公开(公告)号：WO1990002137A1
公开(公告)日：1990-03-08
申请号：PCT/US1989003093
申请日：1989-07-20
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/02
CPC分类号： C07K5/0227
摘要： The present invention provides novel renin-inhibiting peptides having a non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen) and having a suleptanic acid moiety or derivatives thereof of formula L1 at the N-terminus of the peptide. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin dependent hyperaldosterism, other renin dependent cardiovascular disorders and ocular disorders.

5. 发明申请

WO1989000161A1 MALIC ACID DERIVATIVE CONTAINING RENIN INHIBITING PEPTIDES 审中-公开
标题翻译：含有酸性衍生物的含烯酸抑制肽
公开(公告)号：WO1989000161A1
公开(公告)日：1989-01-12
申请号：PCT/US1988001535
申请日：1988-05-13
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07D401/12
CPC分类号： C07D233/64 , C07D401/12
摘要： The present invention provides novel renin-inhibiting peptides of the formula Z-C(O)-CH(OH)-CH(CH2R1)-C(O)-N(R2)-CH(CH2R3)-C(O)-NH-CH(CH2R4)-X-C(R5) (R2)-C(O)-Y-Z containing malic acid derivatives. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension and other related diseases.
摘要翻译：本发明提供了式ZC（O）-CH（OH）-CH（CH 2 R 1）-C（O）-N（R 2）-CH（CH 2 R 3）-C（O）-NH-CH的新的肾素抑制肽（CH2R4）-XC（R5）（R2）-C（O）-YZ含苹果酸衍生物。这种抑制剂可用于诊断和控制肾素依赖性高血压和其他相关疾病。

6. 发明申请

WO1987005909A2 RENIN INHIBITORS HAVING A LACTAM PSEUDO DIPEPTIDE 审中-公开
标题翻译： RENIN抑制剂具有LACTAM PSEUDO DIPEPTIDE
公开(公告)号：WO1987005909A2
公开(公告)日：1987-10-08
申请号：PCT/US1987000507
申请日：1987-03-13
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/06
CPC分类号： C07D401/12 , A61K38/00 , C07K5/0227 , C07K5/06139 , Y10S530/86
摘要： Novel renin-inhibiting peptides of the formula X-A6-B7-C8-D9-E10-F11-G12-H13-I14-Z, having a lactam pseudo dipeptide at C8-D9 positions, X and Z are terminal groups, and the remaining variables are absent or are amino acid residues. Such inhibitors are useful for the diagnosis and control of renin-dependent hypertension.
摘要翻译：在C8-D9位具有内酰胺假二肽的X-A6-B7-C8-D9-E10-F11-G12-H13-I14-Z的新型肾素抑制肽，X和Z是末端基团，剩余的变量不存在或是氨基酸残基。这种抑制剂可用于诊断和控制肾素依赖性高血压。

7. 发明申请

WO1994011361A1 PYRAN-2-ONES AND 5,6-DIHYDROPYRAN-2-ONES USEFUL FOR TREATING HIV AND OTHER RETROVIRUSES 审中-公开
标题翻译： PYRAN-2-ONES和5,6-DIHYDROPYRAN-2-ONES用于治疗艾滋病毒和其他肝炎病毒
公开(公告)号：WO1994011361A1
公开(公告)日：1994-05-26
申请号：PCT/US1993010645
申请日：1993-11-09
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit , YANG, Chih-Ping , STROHBACH, Joseph, Walter , TURNER, Steven, Ronald , ROMERO, Donna, Lee , SKALETZKI, Louis, L, , ARISTOFF, Paul, Adrian , GAMMILL, Ronald, B, , JOHNSON, Paul, D. , SKULNICK, Harvey, Irving , PIPER, Richard, C, , TOMMASI, Ruben, A. , ZHANG, Qingwei
发明人： THE UPJOHN COMPANY
IPC分类号： C07D309/38
CPC分类号： C07D405/06 , C07D309/32 , C07D309/38 , C07D311/96 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/14 , C07D413/06 , C07D413/12 , C07D417/06 , C07D417/12
摘要： The present invention relates to compounds of formula (I) which are pyran-2-ones and 5,6-dihydropyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus.
摘要翻译：本发明涉及可用于在感染该逆转录病毒的哺乳动物细胞中抑制逆转录病毒的吡喃-2-酮和5,6-二氢吡喃-2-酮的式（I）化合物。

8. 发明申请

WO1991001327A1 PEPTIDES CONTAINING DIAMINO-GLYCOLS AS TRANSITION-STATE MIMICS 审中-公开
标题翻译：含有DIAMINO-GLYCOLS作为过渡态MIMICS的肽
公开(公告)号：WO1991001327A1
公开(公告)日：1991-02-07
申请号：PCT/US1990003754
申请日：1990-07-09
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/02
CPC分类号： C07K9/005 , A61K38/00 , C07K5/021 , C07K5/0227 , C07K5/06078 , C07K5/0812 , C07K5/1016
摘要： The present invention provides novel peptides. These peptides have a novel non-cleavable transition state insert corresponding to the 10,11-position of the renin substrate (angiotensinogen) of the formula XL8. These peptides are useful as renin inhibitors and as inhibitors of retroviral proteases. Renin inhibitors are useful for the diagnosis and control of renin-dependent hypertension, congestive heart failure, renin-dependent hyperaldosterism, other renin-dependent cardiovascular disorders and ocular disorders. Inhibitors of retroviral proteases, such as the HIV-I protease, are useful for treating diseases caused by retroviruses, such as human acquired immunodificiency disease syndrome (AIDS).
摘要翻译：本发明提供新的肽。这些肽具有对应于式XL8的肾素底物（血管紧张素原）的10,11位的新型不可切割过渡态插入物。这些肽可用作肾素抑制剂和作为逆转录病毒蛋白酶的抑制剂。肾素抑制剂可用于诊断和控制肾素依赖性高血压，充血性心力衰竭，肾素依赖性醛固酮增多症，其他肾素依赖型心血管疾病和眼部疾病。逆转录病毒蛋白酶如HIV-1蛋白酶的抑制剂可用于治疗由逆转录病毒引起的疾病，例如人类获得性免疫性疾病综合征（AIDS）。

9. 发明申请

WO1987005302A2 NOVEL RENIN-INHIBITING PEPTIDES HAVING A DIHYDROXYETHYLENE ISOSTERE TRANSITION STATE INSERT 审中-公开
标题翻译：具有二羟基乙烯基异构体转移状态插入剂的新型烯醇抑制肽
公开(公告)号：WO1987005302A2
公开(公告)日：1987-09-11
申请号：PCT/US1987000291
申请日：1987-02-13
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/02
CPC分类号： C07D233/64 , C07K5/0227
摘要： Novel renin-inhibiting peptides of the formula X-A6-B7-C8-D9-E10-F11-G12-H13-I14-Z, wherein the E10-F11 moiety is a dihydroxyethylene isostere, X and Z are terminal groups, and the remaining variables are absent or are amino acid residues. Such inhibitors are useful for the control of hypertension.
摘要翻译：式X-A6-B7-C8-D9-E10-F11-G12-H13-I14-Z的新型肾素抑制肽，其中E10-F11部分是二羟基亚乙基异构体，X和Z是末端基团，剩余的变数不存在或是氨基酸残基。这种抑制剂可用于控制高血压。

10. 发明申请

WO1986006379A1 DIHALO-STATINE SUBSTITUTED RENIN INHIBITORS 审中-公开
标题翻译： DIHALO-STATINE替代RENIN抑制剂
公开(公告)号：WO1986006379A1
公开(公告)日：1986-11-06
申请号：PCT/US1986000713
申请日：1986-04-07
申请人： THE UPJOHN COMPANY , THAISRIVONGS, Suvit
发明人： THE UPJOHN COMPANY
IPC分类号： C07K05/00
CPC分类号： C07D213/40 , C07K5/0227 , C07K5/1024
摘要： Novel renin inhibitory peptides of the formula X-A-B-C-D-E-F-G-H-Z wherein E-F is a dihalo-substituted statine group, X and Z are terminal groups, and the remaining variables are absent or amino acid residues. These compounds are useful for administration to humans to treat hypertension.
摘要翻译：式X-A-B-C-D-E-F-G-H-Z的新型肾素抑制肽其中E-F是二卤代替的他汀类，X和Z是末端基团，其余的变量不存在或氨基酸残基。这些化合物可用于给予人治疗高血压。

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