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11. 发明授权

US06933298B2 Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides and the use thereof for selectively inhibiting collagenases 有权
标题翻译：吡啶-2,4-二羧酸二酰胺和嘧啶-4,6-二羧酸二酰胺及其用于选择性抑制胶原酶的用途
公开(公告)号：US06933298B2
公开(公告)日：2005-08-23
申请号：US10065994
申请日：2002-12-09
申请人： Klaus-Ulrich Weithmann , Jörg Habermann , Herbert Kogler , Reinhard Kirsch , Volkmar Wehner
发明人： Klaus-Ulrich Weithmann , Jörg Habermann , Herbert Kogler , Reinhard Kirsch , Volkmar Wehner
IPC分类号： C07D213/81 , C07D239/28 , C07D405/12 , C07D405/14 , C07D239/26 , A61K31/506 , A61P35/00 , C07D403/12 , C07D403/14
CPC分类号： C07D213/81 , C07D239/28 , C07D405/12 , C07D405/14
摘要： Pyridine-2,4-dicarboxylic acid diamides and pyrimidine-4,6-dicarboxylic acid diamides of formula I. These compounds are found to possess the property of selectively inhibiting collagenase (MMP). They may therefore be useful in prophylaxis and therapy of diseases whose course involves an increased activity of matrix metalloproteinase 13.
摘要翻译：吡啶-2,4-二羧酸二酰胺和式I的嘧啶-4,6-二羧酸二酰胺。发现这些化合物具有选择性抑制胶原酶（MMP）的性质。因此，它们可用于预防和治疗其课程涉及基质金属蛋白酶13活性增加的疾病。

12. 发明授权

US6022851A Lantibiotic related to actagardine, and processes for the preparation and use thereof 有权
标题翻译：与阿达加丁有关的蓝霉素，以及其制备和使用的方法
公开(公告)号：US6022851A
公开(公告)日：2000-02-08
申请号：US172042
申请日：1998-10-14
申请人： Laszlo Vertesy , Herbert Kogler , Matthias Schiell , Joachim Wink
发明人： Laszlo Vertesy , Herbert Kogler , Matthias Schiell , Joachim Wink
IPC分类号： C12P21/02 , A61K31/00 , A61K38/00 , A61P31/00 , A61P31/04 , C07K7/08 , C07K14/365 , C12R1/045 , A61K38/04 , A61K38/12 , C07K1/107 , C07K4/04
CPC分类号： C07K7/08 , A61K38/00
摘要： The present invention relates to a novel lantibiotic having the formula NH.sub.2 --R-actagardine, where NH.sub.2 --R is the radical of the amino acid alanine, which is formed by the microorganism Actinoplanes liguriae, DSM 11797 or Actinoplanes garbadiensis, DSM 11796 during fermentation, chemical derivatives of the lantibiotic, a process for its preparation and the use of the lantibiotics as pharmaceuticals.
摘要翻译：本发明涉及一种新型的具有式NH2-R-卡那加丁的羊毛硫抗生素，其中NH2-R是氨基酸丙氨酸的基团，其由微生物活性荧光素，DSM 11797或Actinoplanes garbadiensis，DSM 11796在发酵过程中形成，羊毛硫抗生素的化学衍生物，其制备方法以及作为药物使用的羊毛硫抗生素。

13. 发明授权

US07019028B2 Endiandric acid H and its derivatives, process for their preparation and use thereof 失效
标题翻译：内切酸H及其衍生物，其制备及使用方法
公开(公告)号：US07019028B2
公开(公告)日：2006-03-28
申请号：US10627850
申请日：2003-07-25
申请人： Claudia Eder , Herbert Kogler , Sabine Haag-Richter
发明人： Claudia Eder , Herbert Kogler , Sabine Haag-Richter
IPC分类号： A61K31/36 , C07D317/44
CPC分类号： C07D317/60
摘要： The invention relates to compounds of the formula (I) process for their preparation starting from the plant Beilschmiedia fulva, PLA 101037, and the use thereof for producing a medicament, in particular for the treatment of allergic disorders, of asthmatic disorders, of inflammatory concomitant symptoms of asthma and/or of diseases which can be treated by inhibiting c-maf and NFAT.
摘要翻译：本发明涉及从植物Beilschmiedia fulva，PLA 101037开始制备的式（I）化合物及其用于制备药物，特别是用于治疗过敏性疾病的哮喘性疾病，炎性伴随症的药物可以通过抑制c-maf和NFAT治疗的哮喘和/或疾病的症状。

14. 发明授权

US06297043B1 Mumbaistatin, a process for it's production and its use as a pharmaceutical 失效
标题翻译：孟买斯他汀（Mumbaistatin），它是生产和作为药物使用的过程
公开(公告)号：US06297043B1
公开(公告)日：2001-10-02
申请号：US09338601
申请日：1999-06-23
申请人： Nirogi Venkata Satya Ramakrishna , Keshavapura Hosamane Sreedhara Swamy , Erra Koteswara Satya Vijaya Kumar , Manoj Maniram Singh Kushwaha , Sridevi Kota , Mythili Raman , Swati Dhananjay Tare , Sunil Kumar Deshmukh , Dietmar Schummer , Michael Kurz , Herbert Kogler
发明人： Nirogi Venkata Satya Ramakrishna , Keshavapura Hosamane Sreedhara Swamy , Erra Koteswara Satya Vijaya Kumar , Manoj Maniram Singh Kushwaha , Sridevi Kota , Mythili Raman , Swati Dhananjay Tare , Sunil Kumar Deshmukh , Dietmar Schummer , Michael Kurz , Herbert Kogler
IPC分类号： C12N100
CPC分类号： C12R1/465 , C12P1/04 , Y10S435/822 , Y10S435/886
摘要： The present invention relates to a compound named Mumbaistatin, its pharmaceutically acceptable salts and derivatives, a process for its production, and its use as a pharmaceutical. Mumbaistatin is obtainable by cultivation of the microorganism HIL-008003 (DSM 11641). Mumbaistatin is a glucose-6-phosphate translocase inhibitor and can be used in the treatment of diabetes mellitus. The present invention further relates to a process for the production of Mumbaistatin, to the microorganism HIL-008003 (DSM 11641), to the use of Mumbaistatin and its pharmaceutically acceptable salts and derivatives as pharmaceuticals, in particular to their use in the treatment of diabetes mellitus, and to pharmaceutical compositions comprising Mumbaistatin or a pharmaceutically acceptable salt or derivative thereof.
摘要翻译：本发明涉及一种名为孟巴斯丁（Mumbaistatin）的化合物及其药学上可接受的盐和衍生物，其生产方法及其作为药物的用途。孟巴斯汀可通过培养微生物HIL-008003（DSM 11641）获得。孟巴司他是一种葡萄糖-6-磷酸转位酶抑制剂，可用于治疗糖尿病。本发明还涉及生产孟鲁司他汀对微生物HIL-008003（DSM11641）的使用，以使用孟巴斯妥及其药学上可接受的盐和衍生物作为药物，特别是其用于治疗糖尿病以及包含孟巴斯妥坦或其药学上可接受的盐或衍生物的药物组合物。

15. 发明授权

US06579903B2 Klainetins and their derivatives, method for their preparation and use thereof 失效
标题翻译：蛇毒素及其衍生物，其制备方法和用途
公开(公告)号：US06579903B2
公开(公告)日：2003-06-17
申请号：US10000450
申请日：2001-12-04
申请人： Sabine Haag , Herbert Kogler , Ziyu Li , Laszlo Vertésy
发明人： Sabine Haag , Herbert Kogler , Ziyu Li , Laszlo Vertésy
IPC分类号： A61K3135
CPC分类号： C07D311/32 , C07C45/78 , C07C49/84
摘要： The invention relates to compounds of formula I and of formula II in which R1, R2, R3, R4, R5, X1, X2, X3, X4, X5 and Y are defined in the specification. The compounds of formulae I and II inhibit cyclin-dependent kinases (CDKS) and other kinases (KDR), have cytostatic actions, and are suitable for treating tumors. The compounds of formulae I and II are obtainable by extracting the plant Uvaria klaineri, PLA 100484, by cell cultures of the plant Uvaria klaineri, or by chemical synthesis. The invention relates to a method for preparing the compounds of formulae I and II, to the use of the compounds for producing a pharmaceutical for the treatment of malignant disorders and of diseases which may be treated by inhibition of CDKs and KDR, and also to pharmaceutical compositions comprising at least one compound of the formula I or II.
摘要翻译：本发明涉及式I和式IIin化合物，其中R1，R2，R3，R4，R5，X1，X2，X3，X4，X5和Y在本说明书中定义。式I和II的化合物抑制细胞周期蛋白依赖性激酶（CDKS）和其他激酶（KDR），具有细胞抑制作用，并且适用于治疗肿瘤。式I和II的化合物可以通过植物Uvaria klaineri的细胞培养物提取植物Uvaria klaineri，PLA 100484或通过化学合成获得。本发明涉及一种制备式I和II化合物的方法，该化合物用于制备用于治疗恶性疾病的药物和可通过抑制CDK和KDR治疗的疾病，以及药物组合物，其包含至少一种式I或II的化合物。

16. 发明授权

US06818667B2 Eurotinones, and derivatives thereof, processes for preparing them, and their use 有权
标题翻译：欧卡因及其衍生物，其制备方法及其应用
公开(公告)号：US06818667B2
公开(公告)日：2004-11-16
申请号：US10180003
申请日：2002-06-26
申请人： Claudia Eder , Herbert Kogler , Luigi Toti
发明人： Claudia Eder , Herbert Kogler , Luigi Toti
IPC分类号： A61K31335
CPC分类号： C07D313/12
摘要： The present invention relates to novel compounds of the formula I in which R(1), R(2), R(3) and R(4) are, independently of each other, hydrogen or an alkyl radical. The compounds of the formula I are inhibitors of KDR kinase and, due to their antiangiogenic effect, are suitable for preventing and/or treating malignant diseases. The compounds of the formula I can be obtained by fermenting the microorganism Eurotium echinulatum Delacroix (DSM 13872) or by chemically derivatizing the compounds which are obtained after fermenting said microorganism. The invention consequently also relates to a process for preparing the compounds of the formula I, to the use of the compounds of the formula I for preparing a pharmaceutical for treating malignant diseases and diseases which can be treated by inhibiting KDR kinase, and also to pharmaceutical preparations which have a content of at least one compound of the formula I.
摘要翻译：本发明涉及式Iin的新化合物，其中R（1），R（2），R（3）和R（4）彼此独立地为氢或烷基。式I的化合物是KDR激酶的抑制剂，并且由于其抗血管生成作用，适用于预防和/或治疗恶性疾病。式I的化合物可以通过发酵微生物欧氏螺旋体（DSM 13872）或通过化学衍生在发酵所述微生物后获得的化合物而获得。因此，本发明还涉及制备式I化合物的方法，使用式I化合物来制备治疗可通过抑制KDR激酶治疗的恶性疾病和疾病的药物，还涉及药物具有至少一种式I化合物含量的制剂。

17. 发明授权

US06627604B2 Memno peptides, process for their preparation and use thereof 有权
标题翻译： Memno肽，其制备方法和用途
公开(公告)号：US06627604B2
公开(公告)日：2003-09-30
申请号：US09794346
申请日：2001-02-28
申请人： Laszlo Vertesy , Herbert Kogler , Astrid Markus , Matthias Schiell
发明人： Laszlo Vertesy , Herbert Kogler , Astrid Markus , Matthias Schiell
IPC分类号： A61K3808
CPC分类号： C07K7/06 , A61K38/00
摘要： The invention relates to novel peptide derivatives, called memno peptides, of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7, R8 and (A)n have the meaning herein, obtainable by cultivation of Memnoniella echinata FH2272, DSM 13195 or mutants and variants of this, a process for their preparation and the use of the compounds as pharmaceuticals, for example against cardiac insufficiency.
摘要翻译：本发明涉及式（I）所示的新型肽衍生物（称为memno肽）：其中R1，R2，R3，R4，R5，R6，R7，R8和（A）n具有本文的含义，可通过培养Memnoniella echinata FH2272，DSM 13195或其突变体和变体，其制备方法和化合物用作药物的方法，例如针对心脏功能不全。

18. 发明授权

US06221844B1 Antifungal peptides from scleroderma texense 失效
标题翻译：来自硬皮病texense的抗真菌肽
公开(公告)号：US06221844B1
公开(公告)日：2001-04-24
申请号：US09155603
申请日：1999-05-18
申请人： Heike Stump , Wilhelm Stahl , Joachim Wink , Astrid Markus , Herbert Kogler , Jürgen Backhaus
发明人： Heike Stump , Wilhelm Stahl , Joachim Wink , Astrid Markus , Herbert Kogler , Jürgen Backhaus
IPC分类号： A61K3800
CPC分类号： C07K7/02 , A61K38/00
摘要： The invention relates to novel peptides, namely texenomycins, from Scleroderma texense, a process for their preparation and their use as pharmaceuticals, in particular as antimycotics. The texenomycins according to the present invention are distinguished in particular by the amino acid sequence I in which FS is an oxo fatty acid radical, Aib is aminoisobutyric acid and Arg-ol=argininol.
摘要翻译：本发明涉及来自硬皮病texense的新型肽，即泰克星菌素，其制备方法及其作为药物，特别是抗真菌剂的用途。根据本发明的泰克星霉素特别是由以下的氨基酸序列Iin区分：其中FS是氧代脂肪酸基，Aib是氨基异丁酸，Ar-ol =精氨醇。

19. 发明授权

US08268775B2 Macrolactone derivatives 有权
标题翻译：麦芽糖内酯衍生物
公开(公告)号：US08268775B2
公开(公告)日：2012-09-18
申请号：US12640273
申请日：2009-12-17
申请人： Holger Hoffmann , Christine Klemke-Jahn , Dietmar Schummer , Herbert Kogler
发明人： Holger Hoffmann , Christine Klemke-Jahn , Dietmar Schummer , Herbert Kogler
IPC分类号： A61K38/00 , C09F1/00
CPC分类号： C07D273/00 , C07K5/0808 , C12P17/00 , C12R1/01
摘要： The disclosure relates to compounds of the formula (I): wherein R1, R2, R3, and R4 are as defined in the disclosure, or a pharmaceutically acceptable salt thereof; which is formed by the microorganism ST 201196 (DSM 18870); the use thereof for the treatment and/or prophylaxis of fungal disorders; medicaments containing a compound of formula (I); processes for production thereof; and the microorganism ST 201196 (DSM 18870).
摘要翻译：本公开涉及式（I）的化合物：其中R 1，R 2，R 3和R 4如本公开内容所定义，或其药学上可接受的盐; 其由微生物ST 201196（DSM 18870）形成; 其用于治疗和/或预防真菌病症的用途; 含有式（I）化合物的药物; 生产过程; 和微生物ST 201196（DSM 18870）。

20. 发明申请

US20110306563A1 MACROLACTONE DERIVATIVES, METHOD FOR THE PRODUCTION THEREOF AND USE THEREOF FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：麦角酮衍生物，其生产方法及其用于治疗癌症的方法
公开(公告)号：US20110306563A1
公开(公告)日：2011-12-15
申请号：US13139458
申请日：2009-12-10
申请人： Holger Hoffmann , Michael Caspers , Dietmar Schummer , Herbert Kogler , Christine Klemke-Jahn
发明人： Holger Hoffmann , Michael Caspers , Dietmar Schummer , Herbert Kogler , Christine Klemke-Jahn
IPC分类号： A61K38/12 , C12P21/04 , A61P35/00 , C07K5/12
CPC分类号： A61K31/395 , C07K5/0808
摘要： The present invention relates to the use of a compound of the formula (I), wherein X and Y independently of one another are OH, O—(C1-C6)-alkyl, NH2 or NH—(C1-C6)-alkyl, or X and Y together form a group —O— or wherein X and Y together form a further bond between the C atoms to which they are attached; R1 and R2 independently of one another are H, Cl or Br; R3 is H,(C1-C6)alkyl, C(═O)—(C1-C6)-alkyl or (C1-C6)-alkylene-NH—(C1-C6)-alkyl; R4 is H, (C1-C6)-alkyl or C(═O)—(C1-C6)-alkyl, and R5 is methyl or ethyl; or a physiologically tolerable salt of a compound of the formula (I), for the treatment and/or prophylaxis of cancer diseases, a pharmaceutical composition for the treatment and/or prophylaxis of cancer diseases comprising a compound of the formula (I), a compound of the formula (I) and a process for the preparation of the compound (I).
摘要翻译：本发明涉及式（I）化合物的用途，其中X和Y彼此独立地为OH，O-（C 1 -C 6） - 烷基，NH 2或NH-（C 1 -C 6） - 烷基，或X和Y一起形成基团-O-或其中X和Y一起在它们所连接的C原子之间形成另外的键; R1和R2彼此独立地是H，Cl或Br; R3是H，（C1-C6）烷基，C（= O） - （C1-C6） - 烷基或（C1-C6） - 亚烷基-NH-（C1-C6） - 烷基; R4是H，（C1-C6） - 烷基或C（= O） - （C1-C6） - 烷基，R5是甲基或乙基; 或式（I）化合物的生理上可耐受的盐，用于治疗和/或预防癌症疾病，用于治疗和/或预防癌症疾病的药物组合物，其包含式（I）化合物，式（I）的化合物和化合物（I）的制备方法。

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