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1. 发明申请

WO2016050945A1 PHARMACEUTICAL COMBINATIONS COMPRISING ESTROGEN RECEPTOR-BETA AGONISTS WITH PLATINUM DRUGS OR PACLITAXEL FOR TREATING OVARIAN CANCER 审中-公开
标题翻译：包含雌激素受体-β激动剂的药物组合与铂药物或PACLITAXEL治疗OVARIAN癌症
公开(公告)号：WO2016050945A1
公开(公告)日：2016-04-07
申请号：PCT/EP2015/072763
申请日：2015-10-01
申请人： KARO BIO AB
发明人： NILSSON, Stefan , MORO, Laura , PINTON, Giulia
IPC分类号： A61K31/282 , A61K31/337 , A61K31/404 , A61P35/00
CPC分类号： A61K31/404 , A61K31/337 , A61K31/555 , A61K33/24 , A61K2300/00
摘要： The invention provides a treatment of ovarian cancer, particularly ovarian cancer that is resistant to platinum-containing anti-cancer drugs, using an estrogen receptor β subtype (ERβ) agonist, wherein the treatment comprises administering the ERβ agonist to the patient, and administering a platinum-containing anti-cancer drug to the patient, the administrations being simultaneous, sequential or separate. The invention also provides an ERβ agonist and a platinum- containing anti-cancer drug for use in the treatment of ovarian cancer in a patient, wherein the treatment comprises administering the ERβ agonist to the patient, and administering the platinum-containing anti-cancer drug to the patient, the administrations being simultaneous, sequential or separate; a kit comprising an ERβ agonist, a platinum-containing anti-cancer drug, and a further compound suitable for the treatment of ovarian cancer; and an ERβ agonist for use in the treatment of ovarian cancer in a patient, or an ERβ agonist and a taxane for use in the treatment of ovarian cancer in a patient, wherein the treatment comprises administering the ERβ agonist to the patient, and administering a taxane to the patient, the administrations being simultaneous, sequential or separate.
摘要翻译：本发明提供使用雌激素受体β亚型（ERβ）激动剂治疗卵巢癌，特别是耐铂性抗癌药物的卵巢癌，其中所述治疗包括向患者施用ERβ激动剂，并施用含铂的抗癌药物给患者，给药是同时，顺序或分开的。本发明还提供了用于治疗患者卵巢癌的ERβ激动剂和含铂的抗癌药物，其中所述治疗包括向患者施用ERβ激动剂，并施用含铂的抗癌药物对病人，主管部门同时，连续或分开; 包含ERβ激动剂，含铂的抗癌药物和适用于治疗卵巢癌的其它化合物的试剂盒; 和用于治疗患者的卵巢癌的ERβ激动剂，或用于治疗患者卵巢癌的ERβ激动剂和紫杉烷，其中所述治疗包括向患者施用ERβ激动剂，并施用紫杉烷对患者，主管部门同时，连续或分开。

2. 发明申请

WO2011042475A1 SUBSTITUTED PYRAZOLES AS ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：替代吡唑作为雌激素受体配体
公开(公告)号：WO2011042475A1
公开(公告)日：2011-04-14
申请号：PCT/EP2010/064941
申请日：2010-10-06
申请人： KARO BIO AB , LÖFSTEDT, Joakim , WU, Xiongyu , KRÜGER, Lars
发明人： LÖFSTEDT, Joakim , WU, Xiongyu , KRÜGER, Lars
IPC分类号： C07D231/14 , C07D231/38 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/4155 , A61P5/00 , A61P25/00 , A61P35/00 , A61P37/00
CPC分类号： C07D231/12 , C07D207/416 , C07D231/38 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14
摘要： The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R 4 , R 5 , R 6 and R 7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
摘要翻译：本发明提供式（I）化合物，其中G是说明书中定义的吡唑环，R4，R5，R6和R7如说明书中所定义; 或其药学上可接受的酯，酰胺，溶剂合物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物。本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。

3. 发明申请

WO2007039125A2 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2007039125A2
公开(公告)日：2007-04-12
申请号：PCT/EP2006/009184
申请日：2006-09-21
申请人： KARO BIO AB , SJOBLOM, Ase, Husman , LOFSTEDT, Anton, Joakim , GARCIA COLLAZO, Ana, Maria , GARG, Neeraj , RAHIMI-GHADIM, Mahmoud
发明人： SJOBLOM, Ase, Husman , LOFSTEDT, Anton, Joakim , GARCIA COLLAZO, Ana, Maria , GARG, Neeraj , RAHIMI-GHADIM, Mahmoud
IPC分类号： C07C59/56 , C07C217/76 , C07C311/08 , C07C205/34
CPC分类号： C07C59/56 , C07B2200/07 , C07C69/732 , C07C205/12 , C07C205/26 , C07C205/35 , C07C205/56 , C07C217/76 , C07C311/08 , C07C311/48
摘要： The invention provides an optically active form of the compound of formula (I), or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt; uses of the compound; and methods of preparation of the compound.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂合物或其盐的光学活性形式，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物 ; 化合物的用途; 和该化合物的制备方法。

4. 发明申请

WO2003082777A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2003082777A2
公开(公告)日：2003-10-09
申请号：PCT/EP2003/003362
申请日：2003-03-31
申请人： KARO BIO AB , KOEHLER, Konrad , LIU, Ye , PELCMAN, Benjamin , PALM, Rune , HOLM, Kjetil , NESET, Siren
发明人： KOEHLER, Konrad , LIU, Ye , PELCMAN, Benjamin , PALM, Rune , HOLM, Kjetil , NESET, Siren
IPC分类号： C07B41/00
CPC分类号： C07C255/57 , C07C233/36 , C07C233/37 , C07C233/40 , C07C233/62 , C07C233/78 , C07C271/20 , C07C271/34 , C07C271/52 , C07C275/24 , C07C275/26 , C07C275/40 , C07C311/08 , C07C311/18 , C07C2601/08 , C07D233/84 , C07D307/68 , C07D333/24 , C07D333/38
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as glucocorticoid receptor modulators. The compounds of the instant invention are ligands for glucocorticoid receptors and as such may be useful for treatment or prevention of a variety of conditions related to glucocorticoid functioning including rheumatoid arthritis, osteoarthritis, allery, asthma, pneumonia, dermatitis, eczema, psoriasis, lupus, colitis, inflammatory bowel disease, multiple sclerosis, congenital neutropenia, Wegener's granulomatosis, Addison's Disease, Crohn's disease Cushing Syndrome, or as immunosuppressants in organ transplantation.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为糖皮质激素受体调节剂的用途。本发明的化合物是糖皮质激素受体的配体，因此可用于治疗或预防与糖皮质激素功能相关的各种病症，包括类风湿性关节炎，骨关节炎，美容，哮喘，肺炎，皮炎，湿疹，牛皮癣，狼疮，结肠炎，炎性肠病，多发性硬化症，先天性中性粒细胞减少，韦格纳肉芽肿病，艾迪生病，克罗恩病库兴综合症，或作为器官移植中的免疫抑制剂。

5. 发明申请

WO2003059943A3 CONFORMATION-SPECIFIC, PROTEIN KINASE BINDING PEPTIDES AND RELATED METHODS AND PRODUCTS 审中-公开
公开(公告)号：WO2003059943A3
公开(公告)日：2003-07-24
申请号：PCT/EP2003/000343
申请日：2003-01-15
申请人： KARO BIO AB , ASHRAF, Syed, Salman , BALLAS, Lawrence, Michael , HAMILTON, Paul, T.
发明人： ASHRAF, Syed, Salman , BALLAS, Lawrence, Michael , HAMILTON, Paul, T.
IPC分类号： C07K11/00
摘要： A method is described of identifying peptides which bind to protein kinases, especially a protein kinase C, in (a) an active conformation-specific, (b) an inactive conformation- specific, or (c) an active conformation-independent manner. Peptides which specifically bind PKCα in an active conformation specific manner have been identified , and may be used diagnostically and in other ways.

6. 发明申请

WO2003018515A3 PRIME RING SUBSTITUTED THYROID RECEPTOR ANTAGONISTS FOR THE TREATMENT OF CARDIAC AND METABOLIC DISORDERS 审中-公开
公开(公告)号：WO2003018515A3
公开(公告)日：2003-03-06
申请号：PCT/EP2002/009120
申请日：2002-08-13
申请人： KARO BIO AB , MALM, Johan , BRANDT, Peter , EDVINSSON, Karin , KOEHLER, Konrad , SANIN, Andrei , GORDON, Sandra
发明人： MALM, Johan , BRANDT, Peter , EDVINSSON, Karin , KOEHLER, Konrad , SANIN, Andrei , GORDON, Sandra
IPC分类号： C07C59/68
摘要： This invention relates to novel compounds according to the general formula (I) or a pharmaceutically acceptable salt thereof, which are thyroid receptor ligands, preferably antagonists and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyroidism and liver diseases.

7. 发明申请

WO2013017654A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新颖的雌激素受体配体
公开(公告)号：WO2013017654A1
公开(公告)日：2013-02-07
申请号：PCT/EP2012/065134
申请日：2012-08-02
申请人： KARO BIO AB , CHENG, Aiping , GARG, Neeraj , KRÜGER, Lars , LÖFSTEDT, Joakim , KOCH, Eva , KOEHLER, Konrad , HAGBERG, Lars , NÖTEBERG, Daniel
发明人： CHENG, Aiping , GARG, Neeraj , KRÜGER, Lars , LÖFSTEDT, Joakim , KOCH, Eva , KOEHLER, Konrad , HAGBERG, Lars , NÖTEBERG, Daniel
IPC分类号： C07D213/58 , C07D215/12 , C07D217/14 , C07D231/12 , C07D233/64 , C07D235/16 , C07D261/08 , C07D277/30 , C07D277/34 , C07D307/54 , C07D307/68 , C07D307/87 , C07D317/60 , C07D333/20 , C07D409/10
CPC分类号： A61K31/472 , A61K31/155 , A61K31/165 , A61K31/277 , A61K31/341 , A61K31/343 , A61K31/365 , A61K31/381 , A61K31/402 , A61K31/404 , A61K31/415 , A61K31/416 , A61K31/4192 , A61K31/42 , A61K31/44 , A61K31/4418 , A61K31/47 , C07C209/68 , C07C251/48 , C07D207/327 , C07D213/58 , C07D215/12 , C07D215/14 , C07D217/14 , C07D217/16 , C07D231/12 , C07D233/64 , C07D235/16 , C07D261/08 , C07D277/30 , C07D277/34 , C07D295/155 , C07D307/54 , C07D307/68 , C07D307/87 , C07D317/60 , C07D333/20 , C07D333/24 , C07D409/10 , C07D413/10 , C07C211/65
摘要： Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R 1 to R 9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
摘要翻译：式（I）化合物或其药学上可接受的酯，酰胺，氨基甲酸酯或其盐，包括其中R 1至R 9具有如本说明书中所定义的含义的酯，酰胺或氨基甲酸酯的盐，可用作雌激素受体配体。

8. 发明申请

WO2011042477A1 SUBSTITUTED PYRROLES AND IMIDAZOLES AS ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：作为雌激素受体配体的替代吡咯和咪唑
公开(公告)号：WO2011042477A1
公开(公告)日：2011-04-14
申请号：PCT/EP2010/064944
申请日：2010-10-06
申请人： KARO BIO AB , WENNERSTÅL, Mattias , LÖFSTEDT, Joakim , WU, Xiongyu , KRÜGER, Lars , HAGBERG, Lars
发明人： WENNERSTÅL, Mattias , LÖFSTEDT, Joakim , WU, Xiongyu , KRÜGER, Lars , HAGBERG, Lars
IPC分类号： C07D207/416 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , A61K31/4178 , A61P5/00 , A61P25/00 , A61P35/00 , A61P37/00 , A61K31/4025
CPC分类号： C07D231/12 , C07D207/416 , C07D231/38 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14
摘要： The invention provides a compound of formula (I) wherein G is a pyrrole or imidazole moiety and R 4 , R 5 , R 6 , R 7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
摘要翻译：本发明提供式（I）化合物，其中G是吡咯或咪唑部分，R4，R5，R6，R7如说明书中所定义; 或其药学上可接受的酯，酰胺，溶剂合物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物。本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。

9. 发明申请

WO2009124968A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新颖的雌激素受体配体
公开(公告)号：WO2009124968A1
公开(公告)日：2009-10-15
申请号：PCT/EP2009/054220
申请日：2009-04-08
申请人： KARO BIO AB , NÖTEBERG, Daniel , KALLIN, Elisabet , WENNERSTÅL, Mattias
发明人： NÖTEBERG, Daniel , KALLIN, Elisabet , WENNERSTÅL, Mattias
IPC分类号： A61K31/343 , C07D307/80 , A61K31/381 , A61K31/4025 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/443 , A61K31/4709 , C07D405/04 , C07D407/04 , C07D409/04 , C07D417/04 , A61P35/00
CPC分类号： C07D307/80 , A61K31/343 , A61K31/381 , A61K31/4025 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/443 , A61K31/4709 , C07D405/04 , C07D407/04 , C07D409/04 , C07D409/14 , C07D417/04
摘要： The invention provides a pharmaceutical composition comprising a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt: wherein R 3 is selected from the group consisting of OR A ; -CHO; -C(O)C 1-4 alkyl; -C(O)phenyl; -O-C(O)R A ; and N(R B )2; R 6 is selected from certain cyclic groups defined in the specification; and the remaining groups are defined in the specification; together with a pharmaceutically acceptable carrier. Most of the compounds are novel. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
摘要翻译：本发明提供包含式（I）化合物或其药学上可接受的酯，酰胺，溶剂合物或其盐，包括这种酯或酰胺的盐以及这种酯，酰胺或盐的溶剂合物的药物组合物：其中 R3选自ORA; -CHO; -C（O）C 1-4烷基; -C（O）苯基; -O-C（O）R A; 和N（RB）2; R6选自说明书中定义的某些环状基团; 其余组在规范中定义; 以及药学上可接受的载体。大多数化合物是新的。本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。

10. 发明申请

WO2009080835A1 THYROMIMETRIC COMPOUNDS IN TREATMENT OF DISEASE RELATED TO SONIC HEDGEHOG SIGNALLING 审中-公开
标题翻译：治疗与SONIC HEDGEHOG信号相关的疾病的噻嗪化合物
公开(公告)号：WO2009080835A1
公开(公告)日：2009-07-02
申请号：PCT/EP2008/068274
申请日：2008-12-23
申请人： KARO BIO AB , CARLSSON, Bo
发明人： CARLSSON, Bo
IPC分类号： A61K31/195 , A61K31/196 , A61K31/4184 , A61K31/47 , A61P35/00
CPC分类号： A61K31/195 , A61K31/196 , A61K31/4184 , A61K31/47
摘要： This invention relates to compounds for the treatment of disease induced, caused or dependent on activation of the Sonic hedgehog pathway, wherein the compound is a thyromimetic lacking inner-ring iodines. Preferably the compound is of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, formula (I), wherein G is a group selected from: formula (II) (III) (IV) (IV) and the remaining groups/substituents are as defined herein.
摘要翻译：本发明涉及用于治疗诱发，引起或依赖于Sonic刺猬蛋白通路活化的疾病的化合物，其中该化合物是缺乏内环碘的甲状霉素。优选地，化合物是式（I）化合物或其药学上可接受的酯，酰胺，溶剂合物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物，式（I），其中 G是选自：式（II）（III）（IV）（IV）的基团，其余基团/取代基如本文所定义。

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