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公开(公告)号：US09096642B2
公开(公告)日：2015-08-04
申请号：US14124370
申请日：2011-12-21
申请人： Pottayil G. N. Sasikumar , Muralidhara Ramachandra , Suresh Kumar Vadlamani , K. Rajeev Shrimali , Krishnaprasad Subbarao
发明人： Pottayil G. N. Sasikumar , Muralidhara Ramachandra , Suresh Kumar Vadlamani , K. Rajeev Shrimali , Krishnaprasad Subbarao
CPC分类号： C07K7/02 , A61K38/00 , A61K38/08 , C07K5/0227 , Y02A50/385 , Y02A50/401 , Y02A50/402 , Y02A50/406 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/463 , Y02A50/465 , Y02A50/467 , Y02A50/469 , Y02A50/471 , Y02A50/473 , Y02A50/478 , Y02A50/481 , Y02A50/491
摘要： The present invention provides Immunosuppressive compounds capable of inhibiting the programmed cell death 1 (PD1) signalling pathway. The present invention further provides peptide based compositions for treatment of cancer or treatment of infections via immunopotentiation caused by inhibition of immunosuppressive signalling induced by PD-1, PD-L1, or PD-L2 and therapies using them, immunopotentiative substrates included as the active ingredient. Further, the invention provides pharmaceutical compositions comprising the Immunosuppressive peptide compounds or modified peptide moieties for preventive and/or therapeutic agents for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.
摘要翻译： 本发明提供能够抑制程序性细胞死亡1（PD1）信号传导途径的免疫抑制化合物。 本发明还提供了用于治疗癌症或通过由PD-1，PD-L1或PD-L2诱导的免疫抑制性信号传导引起的免疫增强治疗的感染治疗和使用它们的疗法，作为活性成分的免疫增强底物 。 此外，本发明提供了包含用于癌症，癌症转移，免疫缺陷，感染性疾病等的预防和/或治疗剂的免疫抑制肽化合物或修饰肽部分的药物组合物，以及PD-1或PD-L1作为 测试或诊断剂或这种疾病的研究药物。
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公开(公告)号：US6130315A
公开(公告)日：2000-10-10
申请号：US139009
申请日：1998-08-24
申请人： H. Michael Kolb , Joseph P. Burkhart , Michael J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
发明人： H. Michael Kolb , Joseph P. Burkhart , Michael J. Jung , Fritz E. Gerhart, deceased , Eugene L. Giroux , Bernhard Neises , Daniel G. Schirlin
IPC分类号： A61K38/00 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07D498/10 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/08 , C07K5/083 , C07K5/097 , C07K7/00 , C07K1/02 , C07K1/107 , C07K5/10
CPC分类号： C07K5/0227 , C07C271/22 , C07C279/18 , C07D207/16 , C07D209/42 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/06026 , C07K5/06078 , C07K5/06147 , C07K5/06191 , C07K5/0806 , C07K5/0823 , C07K5/0827 , A61K38/00
摘要： This invention relates to analogs of peptidase substrates in which the amide group containing the scissile amide bond of the substrate peptide has been replaced by an activated electrophilic ketone moiety. These analogs of the peptidase substrates provide specific enzyme inhibitors for a variety of proteases, the inhibition of which will have useful physiological consequences in a variety of disease states.
摘要翻译： 本发明涉及肽酶底物的类似物，其中含有底物肽的染色体酰胺键的酰胺基已被活化的亲电子酮部分代替。 肽酶底物的这些类似物为各种蛋白酶提供特异性酶抑制剂，其抑制将在各种疾病状态下具有有用的生理后果。
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公开(公告)号：US5643879A
公开(公告)日：1997-07-01
申请号：US440585
申请日：1995-05-15
申请人： Cleo Connolly , Annette Marion Doherty , Harriet Wall Hamilton , William Chester Patt , Ila Sircar
发明人： Cleo Connolly , Annette Marion Doherty , Harriet Wall Hamilton , William Chester Patt , Ila Sircar
IPC分类号： C07D233/88 , A61K31/00 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K38/00 , A61K38/55 , A61P5/38 , A61P9/00 , A61P9/12 , A61P27/02 , A61P31/12 , A61P43/00 , C07D263/48 , C07D277/20 , C07D277/40 , C07D277/46 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/065 , C07K14/81 , A61K38/05
CPC分类号： C07K5/06191 , C07K5/0205 , C07K5/0207 , C07K5/0227 , C07K5/06078 , A61K38/00
摘要： The invention concerns novel renin-inhibitory compounds which contain an amino-substituted heterocycle at the P.sub.2 position. These are useful for treating renin-associated hypertension, congestive heart failure, glaucoma, hyperaldosteronism, and diseases caused by retroviruses including HTLV-I and -III. Processes for preparing the compounds, compositions containing them, and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension, or hyperaldosteronism.
摘要翻译： 本发明涉及在P2位置含有氨基取代的杂环的新型肾素抑制化合物。 这些可用于治疗肾素相关性高血压，充血性心力衰竭，青光眼，醛固酮增多症和由逆转录病毒（包括HTLV-I和-III）引起的疾病。 包括制备化合物的方法，含有它们的组合物和使用它们的方法。 还包括使用该化合物来确定肾素相关性高血压或醛固酮增多症的存在的诊断方法。
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公开(公告)号：US5378691A
公开(公告)日：1995-01-03
申请号：US213365
申请日：1994-08-15
CPC分类号： C07K5/0227 , C07K5/0202 , C07K5/0205 , C07K5/0207
摘要： New amino acid derivatives of the formula IR.sup.1 --C.sub.p H.sub.2p --(NH).sub.y --CO--NH--CHR.sup.2 --CO--Z--C.sub.m H.sub.2m --CO--NH--CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--Q--Y Iin which R.sup.1 to R.sup.5, p, y, Z, m, n, E, Q and Y have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.
摘要翻译： 式I R1-CpH2p-（NH）y-CO-NH-CHR2-CO-Z-CmH2m-CO-NH-CHR3-CR4-（CHR5）n-CO-EQ-YI的新氨基酸衍生物，其中R1 至R5，p，y，Z，m，n，E，Q和Y具有本文定义的含义，其盐抑制人血浆肾素的活性。
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公开(公告)号：US5126451A
公开(公告)日：1992-06-30
申请号：US677007
申请日：1991-03-28
IPC分类号： C07C233/51 , C07C237/22 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C335/08 , C07D295/26 , C07K5/02
CPC分类号： C07D295/26 , C07C233/51 , C07C237/22 , C07C271/22 , C07C317/50 , C07C323/59 , C07C323/60 , C07C335/08 , C07K5/0205 , C07K5/0227
摘要： The invention concerns novel renin-inhibitory peptides which contain novel amino acids having an .alpha.-heteroatom attached to the backbone of the amino acid. ##STR1## These novel amino acids are positioned at the P.sub.2 position of the peptide. These are useful for treating renin-associated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Novel intermediates are also disclosed. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
摘要翻译： 本发明涉及含有新氨基酸的新型肾素抑制肽，其具有连接于氨基酸主链的α-杂原子。 这些新的氨基酸位于肽的P2位置。 这些可用于治疗肾素相关性高血压，醛固酮增多症和充血性心力衰竭。 包括肽的制备方法，含有它们的组合物以及使用它们的方法。 还公开了新的中间体。 还包括使用该化合物来确定肾素相关性高血压或醛固酮增多症的存在的诊断方法。
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公开(公告)号：US5126326A
公开(公告)日：1992-06-30
申请号：US361895
申请日：1989-06-06
IPC分类号： C12N9/99 , A61K38/55 , A61P9/00 , A61P9/12 , A61P43/00 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227
摘要： Disclosed herein are peptide derivatives which inhibit the activities of human immunodeficiency virus (HIV) protease and renin. The peptide derivatives can be represented by general formula R.sup.1 --R.sup.2 --Y--R.sup.3 --R.sup.4 wherein R.sup.1 is a derived amino acid based on an O.sup.4 -(carboxymethyl)-tyrosyl residue, R.sup.2 and are amino acid or analogous amino acid residues (R.sup.3 may optionally be absent), Y is a non-peptide linking unit, e.g. statyl, and R.sup.4 is [--NR.sup.17 CHR.sup.18 --C(O)].sub.p --Z wherein R.sup.17 is hydrogen or lower alkyl, R.sup.18 is an amino acid or analogous amino acid side chain, p is zero or one and Z is a terminal group (e.g. hydroxy or amino), or R.sup.4 is --NR.sup.17 CR.sup.18 (R.sup.21)CH.sub.2 OH wherein R.sup.17 and R.sup.18 are as noted hereinabove and R.sup.21 is hydrogen, lower alkyl or hydroxy(lower)alkyl. The derivatives are useful as agents for combatting HIV infections and for treating renin-associated hypertension and congestive heart failure.
摘要翻译： 本文公开了抑制人免疫缺陷病毒（HIV）蛋白酶和肾素的活性的肽衍生物。 肽衍生物可以由通式R 1 -R 2 -Y-R 3 -R 4表示，其中R 1是基于O 4 - （羧甲基） - 酪氨酰残基R2的衍生氨基酸，并且是氨基酸或类似氨基酸残基（R3可以 任选地不存在），Y是非肽连接单元，例如 辛基，R4是[-NR17CHR18-C（O）] pZ，其中R17是氢或低级烷基，R18是氨基酸或类似的氨基酸侧链，p是0或1，Z是末端基团（例如羟基或 氨基），或R 4是-NR 17 CR 18（R 21）CH 2 OH，其中R 17和R 18如上所述，R 21是氢，低级烷基或羟基（低级）烷基。 该衍生物可用作抗艾滋病毒感染和治疗肾素相关性高血压和充血性心力衰竭的药剂。
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公开(公告)号：US5122610A
公开(公告)日：1992-06-16
申请号：US467719
申请日：1990-01-19
IPC分类号： A61K38/55 , A61P5/38 , A61P9/00 , A61P9/12 , C07C323/65 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K7/02 , C07K14/81
CPC分类号： C07K5/0227 , C07K5/0205 , C07K7/02 , Y02P20/55
摘要： Renin-inhibiting aminomethyl peptides of the formula ##STR1## in which A is H, an alkyl radical, a sulphony radical or an amino-protecting group,B, D, E and F each independently is a direct bond or an amino-organo-carbonyl group,R.sup.1 is an optionally substituted alkyl or aryl radical,R.sup.2 is H, alyl or acyl,R.sup.3 is H, alkyl, aryl or acyl, andR.sup.4 is alkyl, alkoxy, aryl or amino, and physiologically acceptable salts thereof.
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公开(公告)号：US5034376A
公开(公告)日：1991-07-23
申请号：US497041
申请日：1990-03-21
IPC分类号： A61K38/00 , C07D265/32 , C07D295/145 , C07D295/205 , C07K5/02 , C07K5/065 , C07K5/078
CPC分类号： C07D295/205 , C07D265/32 , C07D295/145 , C07K5/0202 , C07K5/0227 , C07K5/06078 , C07K5/06139 , A61K38/00
摘要： Polypeptides and derivatives thereof containing nor-statine and nor-cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
摘要翻译： 含有诺斯汀和nor-cyclostatine的多肽及其衍生物可用于抑制肾素的血管紧张素原切割作用。
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公开(公告)号：US5024994A
公开(公告)日：1991-06-18
申请号：US233320
申请日：1988-08-17
申请人： Annette M. Doherty , James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , William H. Roark , Ila Sircar , Francis J. Tinney
发明人： Annette M. Doherty , James P. Hudspeth , James S. Kaltenbronn , Joseph T. Repine , William H. Roark , Ila Sircar , Francis J. Tinney
IPC分类号： C07K5/02
CPC分类号： C07K5/0227 , C07K5/0205
摘要： The invention concerns novel renin-inhibitory peptides which are useful for treating renin-assocated hypertension, hyperaldosteronism, and congestive heart failure. Processes for preparing the peptides, compositions containing them and methods of using them are included. Also included is a diagnostic method which uses the compounds to determine the presence of renin-associated hypertension or hyperaldosteronism.
摘要翻译： 本发明涉及可用于治疗肾素合成的高血压，醛固酮增多症和充血性心力衰竭的新型肾素抑制肽。 包括肽的制备方法，含有它们的组合物和使用它们的方法。 还包括使用该化合物来确定肾素相关性高血压或醛固酮增多症的存在的诊断方法。
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10.发明授权Dipeptide compounds, processes for their preparation and compositions containing them 失效二肽化合物，其制备方法和含有它们的组合物
公开(公告)号：US4985407A
公开(公告)日：1991-01-15
申请号：US280330
申请日：1988-12-06
IPC分类号： C12N9/99 , A61K38/55 , A61P5/38 , A61P9/00 , A61P9/10 , A61P9/12 , A61P27/02 , A61P27/06 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227 , C07K5/0207 , Y10S530/86
摘要： There are described new compounds of formula (1) ##STR1## wherein R.sup.1 represents an acyl group;X.sup.1 represents phenylalanine or p-methoxyphenylalanine bonded N-terminally to R.sup.1 and C-terminally to X.sup.2 ;X.sup.2 represents histidine or N-methylhistidine bonded N-terminally to X.sup.1 and C-terminally to the group --NH--;R.sup.2 represents a C.sub.4-6 cycloalkyl group;R.sup.3 represents a group CHR.sup.6 R.sup.7 is a hydrogen atom and R.sup.7 is a phenyl group, or R.sup.6 is a methyl group and R.sup.7 is a hydrogen atom or a methyl or ethyl group;X.sup.3 represents a C.sub.2-6 alkylene chain optionally substituted by one or more C.sub.1-4 alkyl groups;R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-4 alkyl group, or NR.sup.4 R.sup.5 may form a 5- or 6- membered polymethylenimine ring;and salts and solvates thereof.The new compounds have been found to exhibit activity as renin inhibitors, combining good duration of action with significant oral potency.Compositions containing the compounds of formula (1) and processes for preparing the compounds are also described.
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