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1. 发明授权

US4721776A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US4721776A
公开(公告)日：1988-01-26
申请号：US930483
申请日：1986-11-14
申请人： Peter Raddatz , Gunter Holzemann , Claus J. Schmitges , Klaus O. Minck
发明人： Peter Raddatz , Gunter Holzemann , Claus J. Schmitges , Klaus O. Minck
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D235/14 , C07D403/12 , C07D471/04 , C07K1/113 , C07K5/00 , C07K5/02 , C07K5/06 , C07K5/08 , A61K37/64 , C07C103/52 , C12Q1/36
CPC分类号： C07D403/12 , C07D235/14 , C07D471/04 , C07K5/0205 , C07K5/0227 , Y10S530/86
摘要： New amino acid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CHR.sup.4 --(CHR.sup.5).sub.n CO--B--D Iin which X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, B, D and n have the meanings defined herein, and their salts inhibit the activity of human plasma renin.
摘要翻译：其中X，Z，R2，R3，R4，R5，B，D和n具有本文定义的含义的式I XZ-NR2-CHR3-CHR4-（CHR5）nCO-BDI的新氨基酸衍生物，盐抑制人血浆肾素的活性。

2. 发明授权

US4709010A Peptides useful for inhibition of renin 失效
标题翻译：可用于抑制肾素的肽
公开(公告)号：US4709010A
公开(公告)日：1987-11-24
申请号：US789286
申请日：1985-10-18
申请人： Gunter Holzemann , Peter Raddatz , Alfred Jonczyk , Claus J. Schmitges
发明人： Gunter Holzemann , Peter Raddatz , Alfred Jonczyk , Claus J. Schmitges
IPC分类号： C07K14/81 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07K1/113 , C07K5/00 , C07K5/02 , C07C103/52 , A61K37/02 , A61K49/00
CPC分类号： C07K5/0227 , C07K5/0205 , Y10S530/86
摘要： New peptides of the formula IX--Z--NH--CHR--CHOH--CH.sub.2 --CO--NH--CHR.sup.1 --CH.sub.2 --NH--CHY--C.sub.n H.sub.2n --R.sup.2 Iin whichX is H, R.sup.3 --O--CH.sub.2 --CO--, R.sup.3 --O--CO--, R.sup.3 --CH.sub.2 --O--CO-- or R.sup.3 --C.sub.m H.sub.2m --CO--,Z is 1 to 4 aminoacid residues which are bonded together in the manner of peptides and are selected from the group comprising Abu, Ala, Arg, Asn, Dab, Gln, Gly, His, Ile, Leu, Lys, Met, NLeu, Orn, Phe, Pro, Trp, Tyr and Val,is A, Ar-alkyl (in which the group -alkyl contains 1-4 C atoms) or cycloalkyl-alkyl having 4-11 C atoms,R.sup.1 is H or A,Y is H, A, --C.sub.p H.sub.2p --OR.sup.4, --C.sub.p H.sub.2p --NHR.sup.4, --COOR.sup.4, --CONHR.sup.4 or --CONA.sub.2,R.sup.2 is A, cycloalkyl having 3-7 C atoms, Ar, pyridyl, indolyl, imidazolyl, piperidyl, N-benzylpiperidyl or piperazinyl,R.sup.3 is A, cycloalkyl having 3-7 C atoms or Ar,R.sup.4 is H, A or cycloalkyl having 3-7 C atoms,A is alkyl having 1-6 C atoms,Ar is phenyl which is unsubstituted or substituted once or several times by A, AO, F, Cl, Br, I, CF.sub.3 and/or NH.sub.2, or is unsubstituted naphthyl, andm, n and p each are 0, 1, 2, 3, 4 or 5, and their salts inhibit the activity of the renin in human plasma.
摘要翻译：式I XZ-NH-CHR-CHOH-CH2-CO-NH-CHR1-CH2-NH-CHY-CnH2n-R2Ⅰ的新肽，其中X是H，R3-O-CH2-CO-，R3-O -CO-，R3-CH2-O-CO-或R3-CmH2m-CO-，Z是1-4个氨基酸残基，其以肽的方式结合在一起，并且选自Abu，Ala，Arg，Asn ，Dab，Gln，Gly，His，Ile，Leu，Lys，Met，NLeu，Orn，Phe，Pro，Trp，Tyr和Val是A，Ar-烷基（其中烷基含有1-4个C原子）或具有4-11个碳原子的环烷基 - 烷基，R1是H或A，Y是H，A，-CpH2p-OR4，-CpH2p-NHR4，-COOR4，-CONHR4或-CONA2，R2是A，具有3 -7个C原子，Ar，吡啶基，吲哚基，咪唑基，哌啶基，N-苄基哌啶基或哌嗪基，R3是A，具有3-7个C原子的环烷基或Ar，R4是H，A或具有3-7个C原子的环烷基，A 是具有1-6个C原子的烷基，Ar是未取代或被A，AO，F，Cl，Br，I，CF 3和/或NH 2取代或被取代一次或几次的苯基，或未取代的萘基，m，n和 p分别为0,1,2,3,4或5及其s 抑制人血浆中肾素的活性。

3. 发明申请

US20090247584A1 PHENOXY-PIPERIDINES FOR THE TREATMENT OF DISEASES SUCH AS SCHIZOPHRENIA AND DEPRESSION 审中-公开
标题翻译：用于治疗疾病的苯氧基苯丙胺，如抗抑郁药和抑郁症
公开(公告)号：US20090247584A1
公开(公告)日：2009-10-01
申请号：US12393480
申请日：2009-02-26
申请人： Gunter HOLZEMANN , Helmut Prucher , Kai Schiemann , Joachim Leibrock , Hartmut Greiner , Christa Burger , Laurie von Melchner
发明人： Gunter HOLZEMANN , Helmut Prucher , Kai Schiemann , Joachim Leibrock , Hartmut Greiner , Christa Burger , Laurie von Melchner
IPC分类号： A61K31/445 , A61P25/28 , A61P25/18
CPC分类号： C07D211/46 , A61K31/445 , A61K2300/00
摘要： Compounds of the formula (I), in which R1, R2′, R2″, R2′″, R3 and n are as defined in Claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receptor and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, Parkinson's disease, Huntington's disease, Tourette's syndrome, learning and memory impairments, age-related memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds.
摘要翻译：式（I）化合物，其中R 1，R 2'，R 2“，R 2”'，R 3和n如权利要求1所定义，是烟碱和/或毒蕈碱性乙酰胆碱受体的作用剂，并且适用于预防或治疗精神分裂症，抑郁症，焦虑状态，痴呆，阿尔茨海默病，路易体痴呆，神经退行性疾病，帕金森病，亨廷顿氏病，杜氏综合征，学习记忆障碍，年龄相关记忆障碍，尼古丁依赖戒断症状改善，中风或脑损伤的有毒化合物。

4. 发明授权

US6001961A Cyclic adhesion inhibitors 失效
标题翻译：环状粘连抑制剂
公开(公告)号：US6001961A
公开(公告)日：1999-12-14
申请号：US694387
申请日：1996-09-16
申请人： Alfred Jonczyk , Simon Goodman , Beate Diefenbach , Arne Sutter , Gunter Holzemann , Horst Kessler , Michael Dechantsreiter
发明人： Alfred Jonczyk , Simon Goodman , Beate Diefenbach , Arne Sutter , Gunter Holzemann , Horst Kessler , Michael Dechantsreiter
IPC分类号： A61K38/00 , A61K38/04 , A61K38/12 , A61P9/00 , A61P31/04 , A61P35/00 , A61P35/04 , A61P39/00 , A61P43/00 , C07K1/113 , C07K7/64 , C07K7/00
CPC分类号： C07K7/64 , A61K38/00
摘要： The invention relates to novel cyclopeptides of the formula Icyclo-(nArg-nGly-nAsp-nD-nE) I,in whichD and E in each case independently of one another are Gly, Ala, .beta.-Ala, Asn, Asp, Asp(OR), Arg, Cha, Cys, Gln, Glu, His, Ile, Leu, Lys, Lys(Ac), Lys(AcNH.sub.2), Lys(AcSH), Met, Nal, Nle, Orn, Phe, 4-Hal-Phe, homo-Phe, Phg, Pro, Pya, Ser, Thr, Tia, Tic, Trp, Tyr or Val, which amino acid residues can also be derivatized,R is alkyl having 1-18 carbon atoms,Hal is F, Cl, Br, I,Ac is alkanoyl having 1-10 carbon atoms, aroyl having 7-11 carbon atoms or aralkanoyl having 8-12 carbon atoms,n denotes no substituent or an alkyl radical R, benzyl or an aralkyl radical having 7-18 carbon atoms on the alpha-amino function of the relevant amino acid residue,with the proviso that at least one amino acid residue has a substituent n and that, where residues of optically active amino acids and amino acid derivatives are involved, both the D and the L forms are included, and also their physiologically acceptable salts.These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, angiogenic disorders, microbial infections and in tumor therapy.
摘要翻译：本发明涉及式I环 - （nArg-nGly-nAsp-nD-nE）I的新型环肽，其中D和E各自独立地为Gly，Ala，β-Ala，Asn，Asp，Asp （OR），Arg，Cha，Cys，Gln，Glu，His，Ile，Leu，Lys，Lys（Ac），Lys（AcNH 2），Lys（AcSH），Met，Nal，Nle，Orn， -Phe，Phe-Phe，Phg，Pro，Pya，Ser，Thr，Tia，Tic，Trp，Tyr或Val，该氨基酸残基也可被衍生化，R是具有1-18个碳原子的烷基，Hal是F， Cl，Br，I，Ac是具有1-10个碳原子的烷酰基，具有7-11个碳原子的芳酰基或具有8-12个碳原子的芳烷酰基，n表示没有取代基或烷基R，苄基或具有7- 相关氨基酸残基的α-氨基官能团上的18个碳原子，条件是至少一个氨基酸残基具有取代基n，并且当涉及光学活性氨基酸和氨基酸衍生物的残基时，D 并且包括L形式，也包括它们的生理学可接受的盐。这些化合物用作整联蛋白抑制剂，特别可用于预防和治疗循环障碍，血管生成障碍，微生物感染和肿瘤治疗。

5. 发明授权

US4829053A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US4829053A
公开(公告)日：1989-05-09
申请号：US80265
申请日：1987-07-31
申请人： Peter Raddatz , Joachim Gante , Claus J. Schmitges , Klaus Otto Minck , Johannes Sombroek , Gunter Holzemann
发明人： Peter Raddatz , Joachim Gante , Claus J. Schmitges , Klaus Otto Minck , Johannes Sombroek , Gunter Holzemann
IPC分类号： A61K38/00 , A61K31/41 , A61K31/425 , A61K31/426 , A61P5/38 , A61P9/00 , A61P9/12 , C07D257/04 , C07D257/06 , C07D277/20 , C07D277/40 , C07D277/46 , C07D417/12 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81
CPC分类号： C07K5/0227 , Y10S530/86
摘要： New aminoacid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--NR.sup.6 --(CHR.sup.7).sub.s --D Iwherein X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E, R.sup.6, R.sup.7, D, n and s have the meanings defined herein and their salts, inhibit the activity of human plasma renin.
摘要翻译：式I XZ-NR2-CHR3-CR4-（CHR5）n-CO-E-NR6-（CHR7）sD I的新的氨基酸衍生物其中X，Z，R2，R3，R4，R5，E，R6，R7， D，n和s具有本文定义的含义及其盐，抑制人血浆肾素的活性。

6. 发明申请

US20060122191A1 N-(indolethyl-)cycloamine compounds 审中-公开
标题翻译： N-（吲哚基）环胺化合物
公开(公告)号：US20060122191A1
公开(公告)日：2006-06-08
申请号：US10539516
申请日：2003-11-27
申请人： Timo Heinrich , Henning Bottcher , Kali Schiemann , Gunter Holzemann , Christoph Van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
发明人： Timo Heinrich , Henning Bottcher , Kali Schiemann , Gunter Holzemann , Christoph Van Amsterdam , Gerd Bartoszyk , Joachim Leibrock , Christoph Seyfried
IPC分类号： A61K31/496 , C07D417/14 , C07D405/14
CPC分类号： C07D405/12 , C07D209/14 , C07D209/18 , C07D209/42 , C07D417/12
摘要： N-(indolethyl-)cycloamine compounds of the formula (I): in which R1′, R1″ X, Ar, and n have a meaning indicated in Claim 1, are serotonin reuptake inhibitors (SSRIs) and effectors of the serotonergic receptors 5-HT1A and 5-HT2A. They are therefore suitable for the prophylaxis or treatment of various diseases of the central nervous system, such as depression, dyskinesia, Parkinson's disease, dementia, strokes, schizophrenia, Alzheimer's disease, Lewy bodies dementia, Huntington's disease, Tourette's syndrome, anxiety, learning and memory impairment, pain, sleeping disorders and neurodegenerative diseases.
摘要翻译：式（I）的N-（吲哚基 - ）环胺化合物：其中R 1，R 1，X，Ar和n具有以下含义：权利要求1是5-羟色胺再摄取抑制剂（SSRI）和5-羟色胺受体5-HT 1A和5-HT 2A 2A的作用剂。因此，它们适合于预防或治疗中枢神经系统的各种疾病，例如抑郁症，运动障碍，帕金森病，痴呆，中风，精神分裂症，阿尔茨海默病，路易体痴呆，亨廷顿病，图雷特综合征，焦虑症，学习和记忆障碍，疼痛，睡眠障碍和神经退行性疾病。

7. 发明授权

US06333308B1 Cyclic peptide derivatives 失效
标题翻译：环肽衍生物
公开(公告)号：US06333308B1
公开(公告)日：2001-12-25
申请号：US09341552
申请日：1999-10-07
申请人： Gunter Holzemann , Claus Fittschen , Simon Goodman
发明人： Gunter Holzemann , Claus Fittschen , Simon Goodman
IPC分类号： A61K3812
CPC分类号： C07K7/56 , A61K38/00
摘要： Compounds of the formula I cyclo-(Arg-X-Asp-R1) I in which X is Gly, Ala or NH—NH—CO, R1 is a radical of the formula II and R2,R3 and R4 have the meanings indicated in claim 1, and their salts, can be used as integrin inhibitors, in particular for the prophylaxis and treatment of disorders of the circulation, in thrombosis, cardiac infarct, coronary heart disorders, arteriosclerosis, in pathological processes which are supported or propagated by angiogenesis and in tumour therapy.
摘要翻译：式Iin的化合物，其中X是Gly，Ala或NH-NH-CO，R1是式II的基团，R2，R3和R4具有权利要求1所示的含义，它们的盐可以用作整联蛋白抑制剂，特别是用于预防和治疗通过血管生成和肿瘤治疗支持或繁殖的病理过程中的血液循环障碍，血栓形成，心肌梗塞，冠心病，动脉硬化。

8. 发明授权

US5866540A Cyclic adhesion inhibitors 失效
标题翻译：环状粘连抑制剂
公开(公告)号：US5866540A
公开(公告)日：1999-02-02
申请号：US368760
申请日：1995-01-04
申请人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Guido Melzer , Beate Diefenbach , David A. Cheresh , Horst Kessler , Marion Gurrath , Gerhard Muller
发明人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Guido Melzer , Beate Diefenbach , David A. Cheresh , Horst Kessler , Marion Gurrath , Gerhard Muller
IPC分类号： A61K38/00 , A61K38/12 , A61P7/02 , A61P9/00 , A61P9/10 , A61P17/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07K7/64 , C07K14/75 , C07K14/78 , C07K7/54
CPC分类号： C07K14/75 , C07K14/78 , A61K38/00
摘要： The present invention relates to pharmaceutical compositions which contain at least one cyclopeptide of formula I (a)-(r):(a) cyclo(-Arg-Gly-Asp-D-Phe-Val-Ala);(b) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Ala);(c) cyclo(-Arg-Gly-Asp-Phe-Val-D-Ala);(d) cyclo(-Arg-Gly-Asp-Phe-Leu-D-Ala);(e) cyclo(-Arg-Gly-Asp-D-Phe-Val-Gly);(f) cyclo(-Arg-Gly-Asp-D-Phe-Leu-Gly);(g) cyclo(-D-Arg-Gly-Asp-Phe-Val-Ala);(h) cyclo(-D-Arg-Gly-Asp-Phe-Val-Gly);(i) cyclo(-Arg-Gly-Asp-Phe-Pro-Gly);(j) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Gly);(k) cyclo(-Arg-Gly-Asp-Phe-Pro-Ala);(l) cyclo(-Arg-Gly-Asp-Phe-D-Pro-Ala);(m) cyclo(-D-Arg-Gly-Asp-Phe-Val);(n) cyclo(-Arg-D-Ala-Asp-Phe-Val);(o) cyclo(-Arg-Gly-Asp-D-Phe-Val);(p) cyclo(-Arg-Ala-Asp-D-Phe-Val);(q) cyclo(-Arg-Gly-Asp-Phe-D-Val);(r) cyclo(-Arg-Gly-D-Asp-Phe-Val);or a salt thereof. The pharmaceutical compositions can be used as cell adhesion inhibitors, e.g., in the treatment of thrombosis, myocardial infarct, apoplexy, arteriosclerosis, inflammations, angina pectoris, and/or tumors.
摘要翻译：本发明涉及含有至少一种式I（a） - （r）的环肽的药物组合物：（a）环（-Arg-Gly-Asp-D-Phe-Val-Ala）; （b）环（-Arg-Gly-Asp-D-Phe-Leu-Ala）; （c）环（-Arg-Gly-Asp-Phe-Val-D-Ala）; （d）环（-Arg-Gly-Asp-Phe-Leu-D-Ala）; （e）环（-Arg-Gly-Asp-D-Phe-Val-Gly）; （f）环（-Arg-Gly-Asp-D-Phe-Leu-Gly）; （g）环（-D-Arg-Gly-Asp-Phe-Val-Ala）; （h）环（-D-Arg-Gly-Asp-Phe-Val-Gly）; （i）环（-Arg-Gly-Asp-Phe-Pro-Gly）; （j）环（-Arg-Gly-Asp-Phe-D-Pro-Gly）; （k）环（-Arg-Gly-Asp-Phe-Pro-Ala）; （1）环（-Arg-Gly-Asp-Phe-D-Pro-Ala）; （m）环（-D-Arg-Gly-Asp-Phe-Val）; （n）环（-Arg-D-Ala-Asp-Phe-Val）; （o）环（-Arg-Gly-Asp-D-Phe-Val）; （p）环（-Arg-Ala-Asp-D-Phe-Val）; （q）环（-Arg-Gly-Asp-Phe-D-Val）; （r）环（-Arg-Gly-D-Asp-Phe-Val）; 或其盐。药物组合物可用作细胞粘附抑制剂，例如用于治疗血栓形成，心肌梗塞，中风，动脉硬化，炎症，心绞痛和/或肿瘤。

9. 发明授权

US5705481A Cyclopeptides 失效
标题翻译：环肽
公开(公告)号：US5705481A
公开(公告)日：1998-01-06
申请号：US436601
申请日：1995-05-08
申请人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Guido Melzer , Beate Diefenbach
发明人： Alfred Jonczyk , Gunter Holzemann , Brunhilde Felding-Habermann , Friedrich Rippmann , Guido Melzer , Beate Diefenbach
IPC分类号： A61K38/00 , C07K7/64 , C07K14/75 , A61K38/08 , A61K38/12
CPC分类号： C07K14/75 , C07K7/64 , A61K38/00
摘要： The invention relates to novel cyclopeptides of the formula I cyclo-(A-B-C-D-Arg) I in which A and B are each independently of one another Ala, Asn, Asp, Arg, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr or Val; C is Asp or Asp(O--C.sub.1-4 -alkyl); and D is Gly or Ala; at least two of the amino acid radicals stated being present in the D-form;and their salts. These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation and in tumor therapy.
摘要翻译：本发明涉及式I环 - （ABCD-Arg）Iin的新型环肽，其中A和B各自独立地为Ala，Asn，Asp，Arg，Cys，Gln，Glu，Gly，His，Ile，Leu，Lys ，Met，Phe，Pro，Ser，Thr，Trp，Tyr或Val; C是Asp或Asp（O-C 1-4 - 烷基）; D为Gly或Ala; 所述至少两个所述氨基酸基团以D-形式存在; 和它们的盐。这些化合物用作整联蛋白抑制剂，特别可用于预防和治疗循环障碍和肿瘤治疗。

10. 发明授权

US4812555A Peptides possessing renin inhibitory activity 失效
标题翻译：具有肾素抑制活性的肽
公开(公告)号：US4812555A
公开(公告)日：1989-03-14
申请号：US171973
申请日：1988-03-22
申请人： Peter Raddatz , Gunter Holzemann , Alfred Jonczyk , Claus J. Schmitges , Klaus O. Minck
发明人： Peter Raddatz , Gunter Holzemann , Alfred Jonczyk , Claus J. Schmitges , Klaus O. Minck
IPC分类号： C07K7/06 , A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07C67/00 , C07C231/00 , C07C237/12 , C07C237/22 , C07C239/00 , C07C269/00 , C07C301/00 , C07C303/40 , C07C309/18 , C07C313/00 , C07D233/54 , C07K1/113 , C07K5/00 , C07K5/02 , C07K5/06 , C07K5/08 , C07K5/10 , C07K14/81 , A61K37/02
CPC分类号： C07D233/64 , C07K5/00 , C07K5/0227 , Y10S530/86
摘要： New peptides of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CHOH--(CHR.sup.4).sub.n --CO--Ewherein X, Z, R.sup.2, R.sup.3, R.sup.4, E and n are as defined herein and their salts inhibit the activity of human plasma renin.
摘要翻译：式XZ-NR2-CHR3-CHOH-（CHR4）n-CO-E的新肽，其中X，Z，R2，R3，R4，E和n如本文所定义，并且它们的盐抑制人血浆肾素的活性。

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