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1. 发明申请

WO1991016078A1 CONJUGATE COMPOUNDS CONTAINING AZA-MACROCYCLES, AND PROCESSES FOR THEIR PREPARATION 审中-公开
标题翻译：含有AZA-MACROCYCLES的共轭化合物及其制备方法
公开(公告)号：WO1991016078A1
公开(公告)日：1991-10-31
申请号：PCT/GB1991000613
申请日：1991-04-18
申请人： CELLTECH LIMITED , PARKER, David , BEELEY, Nigel, Robert, Arnold , MILLICAN, Thomas, Andrew
发明人： CELLTECH LIMITED
IPC分类号： A61K47/48
CPC分类号： C07D257/02 , A61K49/06 , C07F9/6524
摘要： Conjugate compounds are described comprising a compound of formula (1), wherein A is a group -Alk3- or -Alk?3N(R4)Alk4-; Alk1, Alk2, Alk3¿ and Alk4 which may be the same or different is each a C¿1-4?alkylene chain optionally substituted by one or more C1-6alkyl groups; and R?1, R2, R3 and R4¿, which may be the same or different, is each a hydrogen atom or a group-AlkR5 where Alk is an optionally substituted straight or branched C¿1-6? alkyl group and R?5¿ is a hydrogen atom or a -CO¿2?H, -CONR?6R7¿ (where R?6 and R7¿, which may be the same or different is each a hydrogen atom or an alkyl group) or -P(X1)(X2R8)L group where X?1 and X2¿ is each an oxygen or sulphur atom, R8 is a hydrogen atom or an alkyl group and L is an aliphatic, aromatic, or heteroaromatic group or a linker group with the proviso that at least one of R?1, R2, R3 and R4¿ is a group AlkP(X1)(X2R8)L where L is a linker group; and a metal complexes and/or salts thereof, coupled to a protein, peptide or carbohydrate. The conjugates are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours.

2. 发明申请

WO2016209619A1 12H-BENZO[A]XANTHEN-12-ONES, COMPOSITIONS CONTAINING, AND USES OF, SAME 审中-公开
标题翻译： 12H-BENZO [A] XANTHEN-12-ONES，组合物及其用途
公开(公告)号：WO2016209619A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/036337
申请日：2016-06-08
申请人： THESAN PHARMACEUTICALS, INC. , BEELEY, Nigel Robert, Arnold , WELGUS, Howard, Glenn , BIRNBAUM, Jay, Edward , FOULKES, J., Gordon , JENKINSON, Celia, Patricia , SAURAT, Jean, Hilaire
发明人： BEELEY, Nigel Robert, Arnold , WELGUS, Howard, Glenn , BIRNBAUM, Jay, Edward , FOULKES, J., Gordon , JENKINSON, Celia, Patricia , SAURAT, Jean, Hilaire
IPC分类号： A61K47/14 , A61K47/06 , A61K31/5575
CPC分类号： A61K31/352 , A61K9/0014 , A61K31/357 , A61K31/36 , A61K2300/00 , A61P17/08 , A61P17/10 , A61P27/02 , A61P35/00
摘要： The present invention provides compounds of the following structure, (I), methods of using such compounds, and pharmaceutical compositions containing such compounds. In addition, this invention provides methods for the treatment and/or prevention of disease states mediated by Aryl Hydrocarbon receptor pathways.
摘要翻译：本发明提供以下结构的化合物，（I），使用这些化合物的方法，以及含有这些化合物的药物组合物。此外，本发明提供了治疗和/或预防由芳基烃受体途径介导的疾病状态的方法。

3. 发明申请

WO2003028641A3 MCH RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2003028641A3
公开(公告)日：2003-04-10
申请号：PCT/US2002/031059
申请日：2002-09-30
申请人： TAISHO PHARMACEUTICAL CO., LTD. , SEKIGUCHI, Yoshinori , KANUMA, Kosuke , OMODERA, Katsunori , TRAN, Thuy-Anh , KRAMER, Bryan, Aubrey , BEELEY, Nigel, Robert, Arnold
发明人： SEKIGUCHI, Yoshinori , KANUMA, Kosuke , OMODERA, Katsunori , TRAN, Thuy-Anh , KRAMER, Bryan, Aubrey , BEELEY, Nigel, Robert, Arnold
IPC分类号： C07D239/95
摘要： The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.

4. 发明申请

WO03028641A2 MCH RECEPTOR ANTAGONISTS 审中-公开
标题翻译： MCH受体拮抗剂
公开(公告)号：WO03028641A2
公开(公告)日：2003-04-10
申请号：PCT/US0231059
申请日：2002-09-30
申请人： TAISHO PHARMA CO LTD , SEKIGUCHI YOSHINORI , KANUMA KOSUKE , OMODERA KATSUNORI , TRAN THUY-ANH , KRAMER BRYAN AUBREY , BEELEY NIGEL ROBERT ARNOLD
发明人： SEKIGUCHI YOSHINORI , KANUMA KOSUKE , OMODERA KATSUNORI , TRAN THUY-ANH , KRAMER BRYAN AUBREY , BEELEY NIGEL ROBERT ARNOLD
IPC分类号： A61K31/18 , A61K31/381 , A61K31/517 , A61K31/5377 , A61K31/538 , A61P3/04 , A61P25/22 , A61P25/24 , A61P43/00 , C07C311/18 , C07C311/29 , C07C311/41 , C07D239/95 , C07D333/34 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D513/04 , A61K
CPC分类号： C07D239/95 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to novel compounds of the formula (I) which act as MCH receptor antagonists. These compositions are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of obesity, obesity related disorders, anxiety, or depression.
摘要翻译：本发明涉及作为MCH受体拮抗剂的新的式（I）化合物。这些组合物可用于其用途包括预防或治疗肥胖症，肥胖症相关病症，焦虑症或抑郁症的药物组合物中。

5. 发明申请

WO1998005351A1 METHODS FOR REGULATING GASTROINTESTINAL MOTILITY 审中-公开
标题翻译：调节胃肠动力学的方法
公开(公告)号：WO1998005351A1
公开(公告)日：1998-02-12
申请号：PCT/US1997014199
申请日：1997-08-08
申请人： AMYLIN PHARMACEUTICALS, INC. , YOUNG, Andrew, A. , GEDULIN, Bronislava , BEELEY, Nigel, Robert, Arnold , PRICKETT, Kathryn, S.
发明人： AMYLIN PHARMACEUTICALS, INC.
IPC分类号： A61K38/00
CPC分类号： C07K14/605 , A61K38/00 , A61K38/22 , A61K38/26 , C07K14/57563 , A61K2300/00
摘要： Methods for reducing gastric motility and delaying gastric emptying for therapeutic and diagnostic purposes are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist. Methods for treating conditions associated with elevated, inapropriate, or undesired post-prandial blood glucose levels are disclosed which comprise administration of an effective amount of an exendin or an exendin agonist alone or in conjunction with other anti-gastric emptying agents.
摘要翻译：公开了减少胃动力和延迟胃排空用于治疗和诊断目的的方法，其包括施用有效量的毒蜥外泌肽或毒蜥外泌肽激动剂。公开了用于治疗与升高，不适当或不期望的餐后血糖水平相关的病症的方法，其包括单独施用有效量的毒蜥外泌肽或毒蜥外泌肽激素或与其他抗胃排空剂联合施用。

6. 发明申请

WO1993024449A1 PEPTIDYL DERIVATIVES AND THEIR USE AS METALLOPROTEINASES INHIBITORS 审中-公开
标题翻译：肽衍生物及其作为金属蛋白酶抑制剂的用途
公开(公告)号：WO1993024449A1
公开(公告)日：1993-12-09
申请号：PCT/GB1993001186
申请日：1993-06-03
申请人： CELLTECH LIMITED , PORTER, John, Robert , MORPHY, John, Richard , MILLICAN, Thomas, Andrew , BEELEY, Nigel, Robert, Arnold
发明人： CELLTECH LIMITED
IPC分类号： C07C237/22
CPC分类号： C07C259/06 , C07C237/22 , C07C2601/14 , C07D213/56
摘要： Compounds of formula (1) are described wherein R represents a -CONHOH, carboxyl (-CO2H), esterified carboxyl or -P(O)(X R )X R group, where X and X , which may be the same or different is each an oxygen or a sulphur atom, and R and R , which may be the same or different each represents a hydrogen atom or an optionally substituted alkyl, aryl or aralkyl group; R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R represents an optionally substituted aryloxy, arylthio, aryloxyalkyl, arylthioalkyl, heteroaryl, heteroaralkyl, heteroaryloxy, heteroarylthio, heteroaryloxyalkyl or heteroarylthioalkyl group; R represents a hydrogen atom or an alkyl group; R represents a hydrogen atom or an alkyl group; R represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R ) groups, [where R is a hydrogen atom or a C1-6 alkyl group] or a group -[Alk]nR where Alk is an alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R ) groups, n is zero or an integer 1 and R is an optionally substituted cycloalkyl or cycloalkenyl group; X represents an amino (-NH2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular are selective inhibitors of the action of gelatinase, and may be of use in the treatment of cancer to control the development of tumour metastases.
摘要翻译：描述式（1）化合物，其中R表示-CONHOH，羧基（-CO 2 H），酯化羧基或-P（O）（X 1 R 8）X 2 R 9基团，其中 X 1和X 2可以相同或不同，各自为氧或硫原子，R 8和R 9可以相同或不同，表示氢原子或任选取代的烷基，芳基或芳烷基; R 1表示氢原子或任选取代的烷基，烯基，芳基，芳烷基，杂芳烷基或杂芳硫基烷基; R 2表示任选取代的芳氧基，芳硫基，芳氧基烷基，芳硫基烷基，杂芳基，杂芳烷基，杂芳氧基，杂芳硫基，杂芳氧基烷基或杂芳硫基烷基; R 3表示氢原子或烷基; R 4表示氢原子或烷基; R 5表示任选被一个或多个-O-或-S-或-N（R 7）基团间隔的任选取代的烷基或烯基，其中R 7是氢原子或C1 -6烷基]或基团 - [Alk] nR 6，其中Alk是任选地被一个或多个-O-或-S-或-N（R 7）基团间隔的烷基或烯基，n 为零或整数1，R 6为任选取代的环烷基或环烯基; X表示氨基（-NH 2）或取代的氨基，羟基或取代的羟基; 及其盐，溶剂化物和水合物。化合物是金属蛋白酶抑制剂，特别是明胶酶作用的选择性抑制剂，并且可用于治疗癌症以控制肿瘤转移的发展。

7. 发明申请

WO2016209596A1 12H-BENZO[B]XANTHEN-12-ONES, COMPOSITIONS CONTAINING, AND USES OF, SAME 审中-公开
标题翻译： 12H-BENZO [B] XANTHEN-12-ONES，组合物及其用途
公开(公告)号：WO2016209596A1
公开(公告)日：2016-12-29
申请号：PCT/US2016/035978
申请日：2016-06-06
申请人： THESAN PHARMACEUTICALS, INC. , BEELEY, Nigel Robert Arnold , WELGUS, Howard Glenn , BIRNBAUM, Jay Edward , FOULKES, J. Gordon , JENKINSON, Celia Patricia , SAURAT, Jean Hilaire
发明人： BEELEY, Nigel Robert Arnold , WELGUS, Howard Glenn , BIRNBAUM, Jay Edward , FOULKES, J. Gordon , JENKINSON, Celia Patricia , SAURAT, Jean Hilaire
IPC分类号： A61K47/14 , A61K47/06 , A61K31/5575
CPC分类号： C07D311/78 , A61K9/0014 , A61K31/352 , A61K31/357 , A61K31/366 , A61K48/00 , A61P17/08 , C07B2200/07 , C07B2200/09 , C07D493/04 , C07D493/14
摘要： The present invention provides compounds of structure (I), methods of using such compounds, and pharmaceutical compositions containing such compounds. In addition, this invention provides methods for the treatment and/or prevention of disease states mediated by Aryl Hydrocarbon receptor pathways.
摘要翻译：本发明提供结构（I）的化合物，使用这些化合物的方法和含有这些化合物的药物组合物。此外，本发明提供了治疗和/或预防由芳基烃受体途径介导的疾病状态的方法。

8. 发明申请

WO1990004605A1 CALCITONIN GENE RELATED PEPTIDE ANALOGUES 审中-公开
标题翻译： CALCITONIN基因相关肽类似物
公开(公告)号：WO1990004605A1
公开(公告)日：1990-05-03
申请号：PCT/GB1989001249
申请日：1989-10-20
申请人： CELLTECH LIMITED , EATON, Michael, Anthony, William , BEELEY, Nigel, Robert, Arnold , BOSE, Christopher, Cyril
发明人： CELLTECH LIMITED
IPC分类号： C07K07/10
CPC分类号： C07K14/57527 , A61K38/00
摘要： Novel analogues of calcitonin gene related peptide comprise analogues of natural CGRPs modified at at least two of positions 3, 22 and 25. These compounds are of general formula NH2-Ala-Cys-A-aaα-B-C-Lys-D-aa?β-CONH¿2, wherein A is a carboxylate or amide substituted amino acid or amino acid analogue; aaα is substantially the amino acid sequence of a CGRP from position 4 to position 21; B is a hydrocarbyl or thio substituted amino acid or amino acid analogue; C is valine or glycine; D is an amine or hydroxyl substituted amino acid or amino acid analogue. The novel analogues may comprise natural amino acid residues. Preferably A is aspartate or asparagine, B is valine or methionine, C is valine and D is asparagine or serine. The analogues exhibit desirable cardiovascular properties and are potentially useful in therapy, e.g. for treatment of deficiencies in cerebral blood supply.

9. 发明申请

WO2016200817A1 BETA-NAPHTHOISOFLAVONES, COMPOSITIONS CONTAINING, AND USES OF, SAME 审中-公开
标题翻译： β-萘酚，其组合物及其用途
公开(公告)号：WO2016200817A1
公开(公告)日：2016-12-15
申请号：PCT/US2016/036226
申请日：2016-06-07
申请人： THESAN PHARMACEUTICALS, INC. , BEELEY, Nigel, Robert, Arnold , WELGUS, Howard, Glenn , BIRNBAUM, Jay, Edward , FOULKES, J., Gordon , JENKINSON, Celia, Patricia , SAURAT, Jean, Hilaire
发明人： BEELEY, Nigel, Robert, Arnold , WELGUS, Howard, Glenn , BIRNBAUM, Jay, Edward , FOULKES, J., Gordon , JENKINSON, Celia, Patricia , SAURAT, Jean, Hilaire
IPC分类号： A61K47/14 , A61K47/06 , A61K31/5575
CPC分类号： C07D311/80 , A61K9/0014 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/4355 , A61K31/436 , A61K31/4433 , A61P1/04 , A61P3/00 , A61P3/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P17/08 , A61P17/10 , A61P19/02 , A61P19/04 , A61P23/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P37/06 , C07B2200/07 , C07B2200/09 , C07D405/04 , C07D407/04 , C07D491/056 , C07D493/04
摘要： The present Invention provides compounds of the following structure, (I), methods of using such compounds, and pharmaceutical compositions containing such compounds. In addition, this invention provides methods for the treatment and/or prevention of disease states mediated by Ary! Hydrocarbon receptor pathways.
摘要翻译：本发明提供以下结构的化合物，（I），使用这些化合物的方法，以及含有这些化合物的药物组合物。此外，本发明提供了治疗和/或预防由Ary介导的疾病状态的方法！烃受体途径。

10. 发明申请

WO1992009564A1 PEPTIDYL DERIVATIVES 审中-公开
标题翻译： PEPTIDYL衍生物
公开(公告)号：WO1992009564A1
公开(公告)日：1992-06-11
申请号：PCT/GB1991002142
申请日：1991-12-03
申请人： CELLTECH LIMITED , PORTER, John, Robert , MORPHY, John, Richard , MILLICAN, Thomas, Andrew , BEELEY, Nigel, Robert, Arnold
发明人： CELLTECH LIMITED
IPC分类号： C07C259/06
CPC分类号： C07C55/02 , A61K38/00 , C07C237/22 , C07C259/06 , C07C311/46 , C07C2601/14 , C07D209/20 , C07K5/06052 , C07K5/06113
摘要： Compounds of formula (I) are described wherein R represents a -CONHOH, carboxyl (-CO2H) or esterified carboxyl group; R1 represents an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R3 represents a hydrogen atom or an alkyl group; R4 represents a hydrogen atom or an alkyl group; R5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more -O- or -S- atoms or -N(R7)-groups [where R7 is a hydrogen atom or a C¿1-6?alkyl group]; X represents an amino (-NH2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases.

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