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1. 发明申请

WO0118032A2 DOLASTATIN PEPTIDES 审中-公开
公开(公告)号：WO0118032A2
公开(公告)日：2001-03-15
申请号：PCT/US0024658
申请日：2000-09-08
申请人： BASF AG , UNIV ARIZONA , PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
发明人： PETIT GEORGE R , SRIRANGAM JAYARAM K , WILLIAMS MICHAEL D , DURKIN KIERAN P M , BARLOZZARI TERESA , KLING ANDREAS , JANSSEN BERND , HAUPT ANDREAS
IPC分类号： C07K5/02 , C07K7/02 , C07K5/00
CPC分类号： C07K5/0202 , C07K5/0205 , C07K7/02
摘要： The present invention provides compounds of formula (I) where R1-R5 are each, independently, a hydrogen atom or a normal or branched C1-C6-alkyl group; A is a methionyl, phenylalanyl or phenylglycyl residue; n is 0 or 1; R6 is a hydrogen atom; and R7 is a carbocyclic group, an aromatic group, a C1-C4-alkyl group, a pyridylalkyl group or a heterocyclic group. In another embodiment, R6 is benzyl or -C(O)OR8, where R8 is a C1-C6-alkyl group, and R7 is a heteroaromatic group, such as a 2-thiazolyl group.
摘要翻译：本发明提供式（I）化合物，其中R 1 -R 5各自独立地为氢原子或正
或支链C 1 -C 6烷基; A是甲硫氨酰基，苯丙氨酰或苯基甘氨酰残基; n为0或1; R6是氢原子; 并且R 7是碳环基，芳基，C 1 -C 4 - 烷基，吡啶基烷基或杂环基。在另一个实施方案中，R 6为苄基或-C（O）OR 8，其中R 8为C 1 -C 6烷基，R 7为杂芳族基团，例如2-噻唑基。

2. 发明申请

WO9722621A3 ANTINEOPLASTIC PEPTIDES 审中-公开
标题翻译：抗生素PEPTIDES
公开(公告)号：WO9722621A3
公开(公告)日：1998-02-26
申请号：PCT/EP9605518
申请日：1996-12-11
申请人： BASF AG , AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
发明人： AMBERG WILHELM , BARLOZZARI TERESA , BERNARD HARALD , BUSCHMANN ERNST , HAUPT ANDREAS , HEGE HANS-GUENTHER , JANSSEN BERND , KLING ANDREAS , LIETZ HELMUT , RITTER KURT , ULLRICH MARTINA , WEYMANN JUERGEN , ZIERKE THOMAS
IPC分类号： A61K38/00 , A61K31/00 , A61K38/08 , A61P35/00 , A61P35/02 , C07K1/00 , C07K7/06
CPC分类号： A61K38/08
摘要： Novel peptides of the following formula (I): R1R2N-CHX-CO-A-B-D-E-(G)¿s?-K in which R?1, R2¿, A, B, D, E, G, K, X, and s have the meanings stated in the description, and the preparation thereof are described. The novel peptides have an antineoplastic effect.

3. 发明申请

WO9804278A3 TETRAPEPTIDE DERIVATIVES OF DOLASTATIN AS ANTITUMOR AGENTS 审中-公开
标题翻译： DOLASTATIN作为抗肿瘤药物的四肽衍生物
公开(公告)号：WO9804278A3
公开(公告)日：2003-04-17
申请号：PCT/EP9703898
申请日：1997-07-21
申请人： BASF AG , BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
发明人： BARLOZZARI TERESA , HAUPT ANDREAS , JANSSEN BERND , GRIESINGER CHRISTIAN , BELIK DANIEL , BORETZKY MICHAEL
IPC分类号： A61K38/00 , A61P35/00 , C07K4/00 , C07K5/02 , C07K5/027 , A61K38/04
CPC分类号： C07K5/0205 , A61K38/00
摘要： The present invention provides antitumor peptides of formula (I): A-B-NR -CHD-CH(OCH3)-CH2CO-E-K and the acid salts thereof. A is an amino acid residue selected from the group consisting of N-methyl-D-prolyl, N-methyl-D-homoprolyl and N, N-dimethyl-2 -ethylphenylglycyl, or an amino acid residue of the formula R R N-CHX-CO, wherein R is a methyl group or an ethyl group, R is a hydrogen atom, a methyl group or an ethyl group, and X is an alkyl group. B is an amino acid residue selected from the group consisting of valyl, isoleucyl, leucyl, and 2-t-butylglycyl. R is a hydrogen atom or a methyl group. D is a normal or branched C2-C5-alkyl group. E is an amino acid residue selected from the group consisting of prolyl, homoprolyl, 5-methylprolyl, and phenylalanyl, or E is a residue derived from an amino acid comprising a pyrrolidine group. K is an alkoxy group or an amino group. An additional embodiment of the present invention is a method for treating a malignancy in a mammal, such as a human, comprising administering to the mammal an effective amount of a compound or compounds of the formula (I) in a pharmaceutically acceptable composition.
摘要翻译：本发明提供式（I）的抗肿瘤肽：A-B-NR 3 -CHD-CH（OCH 3）-CH 2 CO-E-K及其酸式盐。 A是选自N-甲基-D-脯氨酰基，N-甲基-D-正戊基和N，N-二甲基-2-乙基苯基甘氨酰或式R 1的氨基酸残基的氨基酸残基。 R 2为N-CHX-CO，其中R 1为甲基或乙基，R 2为氢原子，甲基或乙基，X为烷基。 B是选自缬氨酰基，异亮氨酰基，亮氨酰基和2-叔丁基甘氨酰基的氨基酸残基。 R 3是氢原子或甲基。 D是正链或支链C 2 -C 5 - 烷基。 E是选自脯氨酰基，同环戊基，5-甲基脯氨酰基和苯丙氨酰基的氨基酸残基，或E是衍生自包含吡咯烷基的氨基酸的残基。 K是烷氧基或氨基。本发明的另一个实施方案是用于治疗哺乳动物（例如人）的恶性肿瘤的方法，其包括向所述哺乳动物施用有效量的药学上可接受的组合物中的式（I）化合物或化合物。

4. 发明专利

CA2009604A1 DIARYL-SUBSTITUTED HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND DRUGS AND COSMETICS OBTAINED THEREFROM 未知
公开(公告)号：CA2009604A1
公开(公告)日：1990-08-10
申请号：CA2009604
申请日：1990-02-08
申请人： WUEST HANS HEINER , JANSSEN BERND , MURRAY WILLIAM V , WACHTER MICHAEL P , BELL STANLEY , BASF AG
发明人： WUEST HANS-HEINER , JANSSEN BERND , MURRAY WILLIAM V , WACHTER MICHAEL P , BELL STANLEY
IPC分类号： A61K31/00 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/41 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/496 , A61K31/50 , A61K31/505 , A61P17/00 , A61P17/10 , A61P29/00 , A61P35/00 , C07D207/32 , C07D207/323 , C07D207/325 , C07D207/333 , C07D207/337 , C07D231/06 , C07D231/12 , C07D231/20 , C07D231/22 , C07D231/24 , C07D233/54 , C07D233/64 , C07D233/84 , C07D237/08 , C07D239/36 , C07D261/08 , C07D263/04 , C07D263/10 , C07D263/32 , C07D271/06 , C07D271/10 , C07D271/107 , C07D277/20 , C07D277/22 , C07D277/30 , C07D307/36 , C07D307/38 , C07D307/40 , C07D307/54 , C07D333/08 , C07D333/18 , C07D333/24 , C07D521/00 , C07D307/68
摘要： Compounds of formulae (I) and (Ia): (see above formulas I, II) where L is a saturated or unsaturated five-membered or six-membered heterocyclic structure. The novel compounds and their physiologically tolerated salts can be used in the topical and systemic therapy and prophylaxis of precancerous conditions and carcinomas of the skin, of the mucus membranes and of the internal organs and in the topical and systemic therapy of acne, psoriasis and other dermatological disorders accompanied by pathological changes in hornification, in particular ichthyosis, Darier's disease, lichen or leucoplakia, or even against eczema, vitiligo, dry eyes and other corneo-pathias, and for the treatment of rheumatic disorders, in particular those of an inflammatory or degenerative nature. As cosmetics, these compounds can be used for the therapy of injury to the skin by light (embrittlement, creases and wrinkles due to excessive exposure to UV light or sunlight and against warts.

5. 发明专利

CA2007933A1 PHENYLHYDRAZONES OF B-IONONE, THE PREPARATION THEREOF AND DRUGS AND COSMETICS PREPARED THEREFROM 未知
公开(公告)号：CA2007933A1
公开(公告)日：1990-08-10
申请号：CA2007933
申请日：1990-01-17
申请人： JANSSEN BERND , BASF AG
发明人： JANSSEN BERND , WUEST HANS-HEINER
IPC分类号： A61K31/15 , A61K20060101 , A61K8/00 , A61K8/30 , A61K31/165 , A61K31/19 , A61K31/195 , A61K31/235 , A61K31/255 , A61K31/275 , A61P17/00 , A61P27/02 , A61P29/00 , A61P31/04 , A61P35/00 , A61Q17/00 , C07C20060101 , C07C229/60 , C07C233/65 , C07C249/16 , C07C251/80 , C07C255/66 , C07C259/10 , C07C309/46 , C07C317/32 , C07C317/34 , C07C403/18 , A61K7/48
摘要： O.Z. 0050/40552 .beta.-ionone phenylhydrazones of the formula I I, where R has the meaning indicated in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.

6. 发明申请

WO02089749A3 ARYLSULFONAMIDE ETHERS, AND METHODS OF USE THEREOF 审中-公开
标题翻译：芳香酰胺类及其使用方法
公开(公告)号：WO02089749A3
公开(公告)日：2003-02-27
申请号：PCT/US0215002
申请日：2002-05-10
申请人： ABBOTT GMBH & CO KG , WARNER LAMBERT CO , KNOBELSDORF JAMES , HAYS SHERYL , STANKOVIC CHARLES J , PARA KIMBERLY S , CONNOLLY MICHAEL K , GALATSIS PAUL , HARTER WILLIAM , SHAHRIPOR AURASH B , PLUMMER MARK STEPHEN , LUNNEY BETH , JANSSEN BERND , FELL JAY BRADFORD
发明人： KNOBELSDORF JAMES , HAYS SHERYL , STANKOVIC CHARLES J , PARA KIMBERLY S , CONNOLLY MICHAEL K , GALATSIS PAUL , HARTER WILLIAM , SHAHRIPOR AURASH B , PLUMMER MARK STEPHEN , LUNNEY BETH , JANSSEN BERND , FELL JAY BRADFORD
IPC分类号： C07D295/08 , A61K31/197 , A61K31/416 , A61K31/437 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/5375 , A61P1/00 , A61P9/00 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/04 , A61P43/00 , C07C311/29 , C07C311/37 , C07C311/42 , C07C311/46 , C07C311/47 , C07C335/18 , C07D215/14 , C07D215/60 , C07D217/16 , C07D231/12 , C07D233/84 , C07D235/06 , C07D277/30 , C07D405/12 , C07D417/04 , C07D417/14 , C07D471/04 , C07D513/04 , A61K31/24 , A61K31/195 , A61K31/40 , A61K31/415 , A61K31/425 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/50 , A61K31/535 , C07C317/00 , C07C321/00 , C07D207/00 , C07D211/06 , C07D215/36 , C07D217/00 , C07D231/56 , C07D235/00 , C07D241/04 , C07D295/00 , C07D403/00 , C07D413/00 , C07D471/02 , C07D513/00
CPC分类号： C07D235/06 , C07C311/29 , C07C311/42 , C07C311/46 , C07C311/47 , C07C335/18 , C07C2603/74 , C07D217/16 , C07D405/12 , C07D417/04 , C07D417/14
摘要： Novel arylsulfonamide ether compounds and pharmaceutical compositions thereof are described. The use of the novel arylsulfonamide ether compounds and pharmaceutical compositions thereof as inhibitors of interleukin-1 beta converting enzyme and other cysteine proteases in the ICE family is also described. In addition, methods of treating stroke, inflammatory diseases, septic shock, repurfusion injury, Alzheimer's disease, and shigellosis using a compound of the invention or a pharmaceutical composition thereof are described.
摘要翻译：描述了新的芳基磺酰胺醚化合物及其药物组合物。还描述了使用新的芳基磺酰胺醚化合物及其药物组合物作为ICE家族中白细胞介素-1β转换酶和其他半胱氨酸蛋白酶的抑制剂。另外，还描述了使用本发明的化合物或其药物组合物治疗中风，炎性疾病，败血性休克，再灌注损伤，阿尔茨海默病和志贺氏菌病的方法。

7. 发明申请

WO2010076033A9 TOLUIDINE SULFONAMIDES AND THEIR USE 审中-公开
标题翻译：甲苯磺酰胺及其用途
公开(公告)号：WO2010076033A9
公开(公告)日：2010-08-26
申请号：PCT/EP2009009337
申请日：2009-12-30
申请人： EUROPEAN MOLECULAR BIOLOGY LAB EMBL , ELARA PHARMACEUTICALS GMBH , ALONSO JORGE , LOPEZ ARANTXA , MUELBAIER MARCEL , AMMENN JOCHEN , WENDT BERND , LEWIS JOE , SCHULTES CRISTOPH , JANSSEN BERND
发明人： ALONSO JORGE , LOPEZ ARANTXA , MUELBAIER MARCEL , AMMENN JOCHEN , WENDT BERND , LEWIS JOE , SCHULTES CRISTOPH , JANSSEN BERND
IPC分类号： C07C311/21 , A61K31/18 , A61K31/341 , A61K31/381 , A61K31/41 , A61P35/00 , C07D207/416 , C07D213/76 , C07D231/42 , C07D249/14 , C07D257/04 , C07D261/16 , C07D277/52 , C07D307/66 , C07D333/36
CPC分类号： C07C311/21 , C07C311/29 , C07C311/39 , C07D207/335 , C07D207/34 , C07D213/42 , C07D213/61 , C07D213/63 , C07D213/64 , C07D213/74 , C07D213/84 , C07D213/85 , C07D231/12 , C07D249/08 , C07D257/04 , C07D261/08 , C07D263/32 , C07D277/28 , C07D307/52 , C07D307/84 , C07D333/20 , C07D333/38
摘要： The present invention provides novel compounds that inhibit cell proliferation and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)-mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition comprising a compound of the invention and a second therapeutic agent or radiation useful for the treatment or prevention of the mentioned diseases or disorders. In a first aspect the present invention relates to a compound having a structure according to formula (I).
摘要翻译：本发明提供抑制细胞增殖和细胞分裂并抑制低氧条件下缺氧诱导因子（HIF）介导的转录和信号传导的活化的新化合物。一方面，本发明化合物可用于制备用于治疗或预防选自以下的疾病或病症的药物：炎性疾病，过度增殖性疾病或病症，缺氧相关病变和以过度血管化为特征的疾病。还提供了包含本发明化合物和用于治疗或预防所述疾病或病症的第二治疗剂或辐射的药物组合物。在第一方面，本发明涉及具有根据式（I）的结构的化合物。

8. 发明专利

JPS61229820A AZOLYLMETHYLOXIRANE FOR CONTROLLING VIRAL DISEASES 失效
公开(公告)号：JPS61229820A
公开(公告)日：1986-10-14
申请号：JP5843686
申请日：1986-03-18
申请人： BASF AG
发明人： JANSSEN BERND , KARBACH STEFAN , MEYER NORBERT , LAUER GERHARD
IPC分类号： C07D405/06 , A01N43/50 , A01N43/653 , A61K31/41 , A61K31/415 , A61P31/12 , C07D521/00

9. 发明专利

JPS61246179A AZOLYLMETHYLOXIRANE AND PLANT PROTECTOR 失效
公开(公告)号：JPS61246179A
公开(公告)日：1986-11-01
申请号：JP6888086
申请日：1986-03-28
申请人： BASF AG
发明人： KARBACH STEFAN , JANSSEN BERND , MEYER NORBERT , SAUTER HUBERT , AMMERMANN EBERHARD , POMMER ERNST-HEINRICH
IPC分类号： C07D405/06 , A01N43/50 , A01N43/653 , C07D521/00

10. 发明专利

CA2069691A1 ANTIMYCOTICS WHICH CONTAIN PHENYLACETIC ACID DERIVATIVES 未知
公开(公告)号：CA2069691A1
公开(公告)日：1992-11-29
申请号：CA2069691
申请日：1992-05-27
申请人： SAUTER HUBERT , LORENZ GISELA , STEINER GERD , JANSSEN BERND , ANKE TIMM , STEGLICH WOLFGANG
发明人： SAUTER HUBERT , LORENZ GISELA , STEINER GERD , JANSSEN BERND , ANKE TIMM , STEGLICH WOLFGANG
IPC分类号： A61K31/165 , A61K31/215 , A61K31/415 , A61K31/42 , A61K31/44 , A61K31/505 , A01N37/10 , A01N53/00 , A01N43/40 , A01N37/44 , A01N43/54 , A01N43/56 , A01N43/80
摘要： O.Z. 0050/42431 Antimycotics containing a compound of the formula 1 where =Y is =CH-OCH3, =CH-CH3, =CH-CH2-CH3, =CH-SCH3 or =N-OCH3, and X is oxygen, or X may also be NH if Y is =N-OCH3, Z is halogen, nitro, cyano, unsubstituted or substituted alkyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aralkyl, unsubstituted or substituted aryloxyalkyl, unsubstituted or substituted arylthioalkyl, unsubstituted or substituted hetarylalkyl, unsubstituted or substituted hetaxyloxyalkyl, unsubstituted or substituted hetarylthioalkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted aralkenyl, unsubstituted or substituted aryloxyalkenyl, unsubstituted or substituted arylthioalkenyl, unsubstituted or substituted hetarylalkenyl, unsubstituted or substituted hetaryloxyalkenyl, unsubstituted or substituted hetarylthioalkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted aryl, unsubstituted or substituted hetaryl, unsubstituted or substituted amino, unsubstituted or substituted arylazo, unsubstituted or substituted acylamino, OR12, SR13, SoR14, SO2R15, -COOR16, -CONR17R18, -COR19, -CR20=NR21, -N=CR22R23 -CR24=N-OR25, -CR25R26-O-N=CR27R28 and U, V, W can be hydrogen or one of the meanings given for Z, O.Z. 0050/42431 or where two of Z, U, V and W in adjacent positions on the phenyl ring can form an unsubstituted or substituted five- or six-membered, aromatic or aliphatic ring which may contain one to three hetero atoms (N, S, O), and R12 to R28 are identical or different and are hydrogen, unsubstituted or substituted C1-C8-alkyl, unsubstituted or substituted C2-C8-alkenyl, unsubstituted or substituted C2-C8-alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted cycloalkylalkyl, unsubstituted or substituted aryl, unsubstituted or substituted hetaryl, unsubstituted or substituted aralkyl, unsubstituted or substituted hetarylalkyl, unsubstituted or substituted aryloxyalkyl, unsubstituted or substituted arylthioalkyl, unsubstituted or substituted hetaryloxyalkyl or unsubstituted or substituted hetarylthioalkyl, are used for controlling mycoses.

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