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1. 发明授权

US5240957A Oxysalicylamido derivatives 失效
标题翻译：氧代水杨酰胺衍生物
公开(公告)号：US5240957A
公开(公告)日：1993-08-31
申请号：US607746
申请日：1990-10-29
申请人： Karl S. Bengtsson , Thomas Hogberg , Lars G. Johansson , Tomas DePaulis , Hans E. P. Strom , Marianne E. Widman , Sven O. gren
发明人： Karl S. Bengtsson , Thomas Hogberg , Lars G. Johansson , Tomas DePaulis , Hans E. P. Strom , Marianne E. Widman , Sven O. gren
IPC分类号： C07C65/21 , C07D207/08
CPC分类号： C07D207/08 , C07C65/21
摘要： Novel therapeutically active compounds of the formula ##STR1## wherein Z.sup.i, being Z.sup.1, Z.sup.2 or Z.sup.3, is the same or different and selected among OH, OR.sup.1, NH.sub.2, NR.sub.2.sup.4, NHR.sup.4, SH, SR.sup.4 and OR.sup.4 wherein R.sup.1 is a formyl group, an acyl group, an alkoxycarbonyl group or a mono- or dialkylcarbamoyl group and R.sup.4 is a lower alkyl group,R.sup.2 is a hydrogen, a halogen, a lower alkyl or a lower trifluoroalkyl group,R.sup.3 is a hydrogen atom, a lower alkyl group, an alkenyl group, an alkynyl group or a phenyl group, which phenyl group could optionally be substituted by one or more of fluoro, chloro, bromo, trifluoromethyl, methyl, ethyl, methoxy or ethoxy in the ortho, meta or para positions, or optionally substituted by methylenedioxy, provided that at least one of Z.sup.1, Z.sup.2 and Z.sup.3 is a group OR.sup.4 and further provided that when Z.sup.2 is OH or NH.sub.2, Z.sup.1 is NR.sub.2.sup.4, NHR.sup.4, SH, SR.sup.4 or OR.sup.4 or a physiologically acceptable salt or optical isomer thereof, intermediates and methods for their preparation, pharmaceutical preparations containing the compounds and methods for their therapeutical use.
摘要翻译：其中Z 1，Z 1，Z 2或Z 3相同或不同并且选自OH，OR 1，NH 2，NR 24，NHR 4，SH，SR 4和OR 4中的新颖的治疗活性化合物，其中R 1是甲酰基，酰基，烷氧基羰基或单烷基氨基甲酰基，R4为低级烷基，R2为氢，卤素，低级烷基或低级三氟烷基，R3为氢原子，低级烷基，链烯基，炔基或苯基，该苯基可以任选被邻位，间位或对位中的一个或多个氟，氯，溴，三氟甲基，甲基，乙基，甲氧基或乙氧基取代，或任选地被亚甲二氧基取代，条件是Z 1，Z 2和Z 3中的至少一个是OR 4基团，并且进一步规定当Z 2是OH或NH 2时，Z 1是NR 24，NHR 4，SH，SR 4或OR 4或生理上可接受的盐或旋光异构体中间体及其制备方法，药物制剂c 保持其治疗用途的化合物和方法。

2. 发明授权

US5300660A Efficient stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines and intermediates thereto 失效
标题翻译： 1-取代（S） - 和（R）-2-氨基甲基吡咯烷的有效立体保守合成及其中间体
公开(公告)号：US5300660A
公开(公告)日：1994-04-05
申请号：US974683
申请日：1992-11-12
申请人： Hans-Jurgen Federsel , Thomas Hogberg , Sten I. Ramsby , Hans E. P. Strom
发明人： Hans-Jurgen Federsel , Thomas Hogberg , Sten I. Ramsby , Hans E. P. Strom
IPC分类号： C07D207/08 , C07D207/09 , C07D207/16
CPC分类号： C07D207/08 , C07D207/09 , C07D207/16
摘要： Stereoconservative method for preparation of an (R)- or (S)-isomer of the compound of the formula I with at least 95% optical purity ##STR1## wherein R.sup.1 is a hydrogen atom, a saturated or unsaturated lower alkyl group, a cycloalkyl group, or a group (CH.sub.2).sub.m Ph wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group including1) O,N-dialkylation, directly or stepwise of (R)- or (S)-proline2) aminolysis3) reduction to formation of the (R)- or (S)-isomer of the compound of the formula I, and new intermediates II and III in optical active form obtained by the reaction steps above and wherein R.sup.2 is defined as R.sup.1 above. ##STR2##
摘要翻译：用于制备具有至少95％光学纯度（*化学结构*）（I）的式I化合物的（R） - 或（S） - 异构体的立体保真剂方法，其中R 1是氢原子，饱和或不饱和的低级烷基，环烷基或基团（CH 2）m Ph，其中m为0-3，Ph为取代或未取代的苯基，包括1）O，N-二烷基化，直接或分步的（R） - 或（ S） - 脯氨酸2）氨解3）还原形成式I化合物的（R） - 或（S） - 异构体，以及通过上述反应步骤获得的光学活性形式的新中间体II和III，其中 R2定义为R1。（*化学结构*）（II）（*化学结构*）（III）

3. 发明授权

US6140308A Colon or ileum-specific glucocorticosteroid derivatives 有权
标题翻译：结肠或回肠特异性糖皮质激素衍生物
公开(公告)号：US6140308A
公开(公告)日：2000-10-31
申请号：US261247
申请日：1999-03-03
申请人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
发明人： Ralph Lennart Brattsand , Peter Edman , Thomas Hogberg , Stinabritt Nilsson , Bror Arne Thalen , Jan Erik Ulmius
IPC分类号： A61K31/58 , A61P1/00 , A61P29/00 , C07J20060101 , C07J71/00 , A61K31/70
CPC分类号： C07J71/0031
摘要： Novel compounds which are a glucocorticosteroid (GCS) chemically bound to a sugar, having the general formulaGCS.sup.1 --O--Sugar.sup.1for colon- or ileum-specific delivery of the GCS to inflamed bowel mucosa, as well as processes for their preparation, pharmaceutical preparations containing the compounds and the use of said compounds in therapy.
摘要翻译：化学结合糖的糖皮质激素（GCS）的新型化合物，具有通式GCS1-O-糖1用于结肠或回肠特异性递送GCS至发炎肠粘膜，以及其制备方法，药物制剂含有化合物和所述化合物在治疗中的用途。

4. 发明授权

US4418065A Halophenyl-pyridyl-allylamine derivatives and use 失效
标题翻译：卤代苯基 - 吡啶基 - 烯丙胺衍生物和用途
公开(公告)号：US4418065A
公开(公告)日：1983-11-29
申请号：US232043
申请日：1981-07-16
申请人： Thomas Hogberg , Tomas de Paulis , Svante B. Ross , Carl B. J. Ulff
发明人： Thomas Hogberg , Tomas de Paulis , Svante B. Ross , Carl B. J. Ulff
IPC分类号： C07C225/16 , A61K31/4402 , A61K31/4406 , A61P25/24 , C07D213/00 , C07D213/26 , C07D213/30 , C07D213/38 , C07D213/48 , A61K31/44
CPC分类号： C07D213/30 , C07D213/26 , C07D213/38 , C07D213/48
摘要： Compounds of the formula ##STR1## wherein R is H or CH.sub.3, n is 1 or 2 and X is F, Cl, Br, I bound in an optional position to the phenyl group, provided that when X is Br it is bound in a position other than the 4 position, processes for their preparation and phrmaceutical preparations, methods of treatment employing such compounds. The compounds are useful for therapeutic treatment of various kinds of depressive conditions.
摘要翻译： PCT No.PCT / SE80 / 00286 Sec。 371日期1981年7月16日 102（e）日期1981年1月13日PCT申请日1980年11月14日PCT公布。公开号WO81 / 01407 日期：1981年5月28日。式中，R为H或CH 3，n为1或2，X为F，Cl，Br，I的化合物与苯基的任意位置相结合，条件是当X为其结合在除4位以外的位置，其制备方法和制剂制剂，使用这些化合物的治疗方法。该化合物可用于治疗各种抑郁症状。

5. 发明申请

US20060111357A1 Quinoline compounds for use in mch receptor related disorders 审中-公开
标题翻译：用于mch受体相关疾病的喹啉化合物
公开(公告)号：US20060111357A1
公开(公告)日：2006-05-25
申请号：US10538455
申请日：2003-12-11
申请人： Thomas Frimurer , Trond Ulven , Thomas Hogberg , Pia Norregaard , Paul Little , Jean-Marie Receveur
发明人： Thomas Frimurer , Trond Ulven , Thomas Hogberg , Pia Norregaard , Paul Little , Jean-Marie Receveur
IPC分类号： A61K31/519 , A61K31/517 , A61K31/498 , A61K31/4745 , A61K31/525 , A61K31/4709
CPC分类号： C07D401/04 , A61K31/435 , A61K31/4375 , A61K31/4985 , A61K31/5025 , A61K31/506 , A61K31/519
摘要： The present invention relates to the use of quinoline compounds for the preparation of a pharmaceutical and/or a cosmetic composition for the treatment, prophylaxis and/or diagnosis of a condition caused by or involving a melanin-concentrating hormone. The invention also relates to novel quinoline compounds per se. The quinoline compounds have been found to interact with a melanin-concentrating hormone receptor, a MCH receptor. The compounds have modulating activity on the MCH receptor such as e.g. antagonistic, agonistic or allosteric activity and are useful for medicinal or cosmetic purposes such as, e.g. in the treatment or prevention of feeding disorders like obesity, metabolic syndrome, Type II diabetes, bulimia, etc. or in the treatment or prevention of depression.
摘要翻译：本发明涉及喹啉化合物在制备药物和/或化妆品组合物中的用途，用于治疗，预防和/或诊断由黑色素浓缩激素引起或涉及的病症。本发明还涉及新的喹啉化合物本身。已发现喹啉化合物与黑色素浓缩激素受体MCH受体相互作用。这些化合物对MCH受体具有调节活性，例如。拮抗，激动或变构活性，并且可用于药物或化妆品目的，例如。治疗或预防肥胖症，代谢综合征，II型糖尿病，食欲过盛等进食障碍，或治疗或预防抑郁症。

6. 发明授权

US4990534A Aralkyl esters and processes for their preparation 失效
标题翻译：芳烷基酯及其制备方法
公开(公告)号：US4990534A
公开(公告)日：1991-02-05
申请号：US305728
申请日：1989-01-24
申请人： Gerd M. Hallnemo , Thomas Hogberg , Ulf H. Lindberg , Bengt C. J. Ulff , Sven Ove gren
发明人： Gerd M. Hallnemo , Thomas Hogberg , Ulf H. Lindberg , Bengt C. J. Ulff , Sven Ove gren
IPC分类号： A61K31/22 , A61K31/215 , A61P25/18 , A61P43/00 , C07B61/00 , C07C227/04 , C07C229/08 , C08L71/02
CPC分类号： A61K31/215
摘要： Aralkyl esters are used to provide a potentiating effect on cholinergic responses.

7. 发明申请

US20130303525A1 KAPPA OPIOID RECEPTOR AGONISTS 有权
公开(公告)号：US20130303525A1
公开(公告)日：2013-11-14
申请号：US13811020
申请日：2011-07-19
申请人： Pradip Kumar Sasmal , Vamsee Krishna Chintakunta , Vijay Potluri , Ish Kumar Khanna , Ashok Tehim , Mahaboobi Jaleel , Thomas Hogberg , Oystein Rist , Lisbeth Elster , Thomas Michael Frimurer , Lars-Ole Gerlach
发明人： Pradip Kumar Sasmal , Vamsee Krishna Chintakunta , Vijay Potluri , Ish Kumar Khanna , Ashok Tehim , Mahaboobi Jaleel , Thomas Hogberg , Oystein Rist , Lisbeth Elster , Thomas Michael Frimurer , Lars-Ole Gerlach
IPC分类号： C07D419/12 , C07D401/12 , C07D413/14 , C07D403/12 , C07D207/09 , C07D417/12 , C07D413/12
CPC分类号： C07D419/12 , C07D207/09 , C07D207/12 , C07D209/34 , C07D213/76 , C07D215/12 , C07D215/227 , C07D231/56 , C07D249/18 , C07D261/20 , C07D263/56 , C07D263/58 , C07D275/06 , C07D277/30 , C07D279/02 , C07D295/13 , C07D401/12 , C07D403/12 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
摘要翻译：本发明涉及一系列具有通式（I）的取代的化合物，包括其立体异构体和/或其药学上可接受的盐。（I）其中A，m，R 1，R 2，R 3，R 4如本文所定义。本发明还涉及制备这些化合物包括中间体的方法。本发明的化合物在κ（κ）阿片样物质受体（KOR）位点是有效的。因此，本发明的化合物可用作药物，特别是用于治疗和/或预防各种中枢神经系统疾病（CNS），包括但不限于急性和慢性疼痛以及相关疾病，特别是周边功能在CNS。

8. 发明申请

US20090099189A1 CRTH2 Receptor Ligands For Medicinal Uses 失效
标题翻译： CRTH2受体配体用于药用
公开(公告)号：US20090099189A1
公开(公告)日：2009-04-16
申请号：US11597873
申请日：2005-05-30
申请人： Trond Ulven , Thomas Frimurer , Oystein Rist , Evi Kostenis , Thomas Hogberg , Jean-Marie Receveur , Marie Grimstrup
发明人： Trond Ulven , Thomas Frimurer , Oystein Rist , Evi Kostenis , Thomas Hogberg , Jean-Marie Receveur , Marie Grimstrup
IPC分类号： A61K31/53 , C07D263/32 , A61K31/421 , C07D403/02 , C07D231/12 , A61K31/415
CPC分类号： A61K31/415 , A61K31/454 , C07D231/12 , C07D261/08 , C07D263/32 , C07D271/06 , C07D277/24 , C07D277/34
摘要： Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis, wherein A represents a carboxyl group —COON, or a carboxyl bioisostere; A1, is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Are2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.
摘要翻译：式（I）化合物可用于治疗对CRTH2受体活性调节作用的疾病，例如哮喘，鼻炎，过敏性气道综合征和过敏性鼻炎支原体，其中A表示羧基-COON或羧基生物电子等排体; A1，是氢或甲基; 环Ar1是任选取代的苯环5-或6-元单环杂芳基环，其中AA1CHO-和L2与相邻的环原子连接; 环A 2，Ar 3各自独立地表示苯基或5-或6-元单环杂芳基环，或由5-或6-元碳环或杂环组成的双环系统，其被苯并稠合或稠合至5-或 6元单环杂芳基环，所述环或环系统任选被取代; t为0或1; L2和L3是如说明书中定义的连接基团。

9. 发明申请

US20070156342A1 Pseudo-sequence method for comparing 7tm receptors with respect to the physico-chemical properties of their binding sites 审中-公开
标题翻译：比较7tm受体相对于其结合位点的物理化学性质的伪序列方法
公开(公告)号：US20070156342A1
公开(公告)日：2007-07-05
申请号：US10547944
申请日：2004-03-05
申请人： Thomas Frimurer , Trond Ulven , Thomas Hogberg , Christian Elling
发明人： Thomas Frimurer , Trond Ulven , Thomas Hogberg , Christian Elling
IPC分类号： G06F19/00 , G06G7/48
CPC分类号： G16B20/00 , G16B15/00
摘要： A pseudo-sequence method for comparing 7TM receptors with respect to the physicochemical properties of their binding sites, the method comprising the steps of: (i) optionally, aligning part of or all of the amino acid sequence of the first 7TM receptor with part of or all or the amino acid sequence of the one or more further 7TM receptors, (ii) selecting, in a sequential or non-sequential order, at the most 12 amino acid residues per helix and/or extracellular loops, which are involved in one or more binding sites of each 7TM receptor. (iii) forming a pseudo-sequence comprising at the most 50 amino acid residues from the selected sequential or non-sequential amino acid residues, (iv) for each 7TM receptor assigning one or more physicochemical descriptors to the amino acid residues of the selected amino acid pseudo-sequence involved in one or more binding sites, (v) optionally, for each 7TM receptor mathematically manipulating the physicochemical descriptors of step (iv) to obtain a simplified measure of the physicochemical properties of the binding site. (vi) for each 7TM receptor generating a similarity score as defined herein by comparing the physicochemical descriptor or, if relevant, the simplified measure for the first 7TM receptor with the physicochemical descriptors or, if relevant, the simplified measures for the one or further 7TM receptors, (vii) optionally, ranking the 7TM receptors with respect to the physicochemical properties of their binding sites according to the similarity scores obtained in step vi)
摘要翻译：一种用于比较7TM受体相对于其结合位点的物理化学性质的伪序列方法，所述方法包括以下步骤：（i）任选地使第一7TM受体的部分或全部氨基酸序列与或全部或一个或多个其它7TM受体的氨基酸序列，（ii）以顺序或非顺序的顺序选择每个螺旋和/或细胞外环最多12个氨基酸残基，其参与一个或更多的每个7TM受体的结合位点。（iii）形成包含来自所选序列或非连续氨基酸残基的至多50个氨基酸残基的伪序列，（iv）对于每个7TM受体，将一个或多个物理化学描述符分配给所选氨基酸的氨基酸残基参与一个或多个结合位点的酸性伪序列，（v）任选地，对于每个7TM受体，在数学上操纵步骤（iv）的物理化学描述符以获得结合位点的物理化学性质的简化测量。（vi）对于每个7TM受体，通过将物理化学描述符或如果相关的第一7TM受体的简化测量与物理化学描述符相比较，或者如果相关的话，通过将一个或另外7个TM的简化测量受体，（vii）任选地，根据步骤vi）中获得的相似性得分，相对于其结合位点的物理化学性质对7TM受体进行排序，

10. 发明申请

US20060235035A1 Novel methoxybenzamibe compounds for use in mch receptor related disorders 审中-公开
公开(公告)号：US20060235035A1
公开(公告)日：2006-10-19
申请号：US10510907
申请日：2003-04-08
申请人： Thomas Hogberg , Emelie Bjurling , Jean-Marie Receveur , Trond Ulven , Paul Little , Christian Elling , Pia Norregaard
发明人： Thomas Hogberg , Emelie Bjurling , Jean-Marie Receveur , Trond Ulven , Paul Little , Christian Elling , Pia Norregaard
IPC分类号： A61K31/513 , A61K31/4747 , A61K31/4745 , A61K31/4035 , A61K31/4709 , A61K31/381 , A61K31/35 , A61K31/34
CPC分类号： C07D213/643 , C07C237/42 , C07C237/44 , C07C275/42 , C07C323/44 , C07C2601/14 , C07D207/09 , C07D207/14 , C07D211/26 , C07D211/58 , C07D213/75 , C07D233/32 , C07D295/13 , C07D317/58
摘要： Novel compounds of Formula (I) which modulate MCH activity are disclosed, in which A is a linker; Ar1 is an aryl or heteroaryl group; R1 is a lower alkoxy group; R2 is an R1 group or hydrogen, an OH or an NH2 group, Q together with the carbonyl forms an amide group, which is further substituted with an amine group; R5 is selected from hydrogen, halogen atoms, alkoxy groups, hydroxy, alkylamino groups, dialkylamino groups, hydroxylalkyl groups, carboxamido groups, acylamido groups, acyl groups, —CHO, nitrile, alkyl, alkenyl or alkynyl groups, —SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups such as —CH2CF3, —CF2CF3, —CF3, —OCF3, —SCF3; —SO2NH2, —SO2NHAlk, —SO2NAlk2, —SO2Alk; X is H, F, Cl, Br, I, —SCH3, —CF3, —OCF3, —SCF3, OCH3, or lower alkyl or alkenyl group; R8 is halogen atoms, alkyl, alkenyl or alkynyl groups, cycloalkyl groups, aryl groups, heteroaryl groups, heterocyclyl groups, alkylcycloalkyl groups, alkylaryl groups, alkylheterocyclyl groups, alkylheteroaryl groups, arylalkoxy groups, aryloxy groups, alkoxy groups, dialkylamino groups, —CONHAlk, —CONHAr, —CONAlk2, —NHCO-Alk, —NHCO—Ar, —CO-Alk, —CO—Ar, —SCH3, partially or fully fluorinated alkyl, alkoxy or thioalkoxy groups; or R8 is R6-Ar2—B—, in which B is a single bond or a connecting moiety; Ar2 is an Ar1 group; R6 is an R5 group; and which are useful in the treatment or prevention of e.g. obesity, depression, diabetes, bulimia etc.

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