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1. 发明申请

US20110112067A1 Inhibitors of the Human Aldosterone Sythase CYP11B2 有权
标题翻译：人醛固酮相关CYP11B2抑制剂
公开(公告)号：US20110112067A1
公开(公告)日：2011-05-12
申请号：US12938581
申请日：2010-11-03
申请人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
发明人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
IPC分类号： A61K31/4709 , C07D401/10 , C07D417/10 , C07D413/10 , C07D471/06 , A61K31/4439 , A61K31/4725 , A61K31/55 , A61K31/4745 , A61K31/553 , A61K31/554 , A61P9/12 , A61P9/04 , A61P9/10 , A61P9/00 , A61P29/00 , A61P3/04 , A61P7/00
CPC分类号： C07D401/10 , C07D413/10 , C07D417/10 , C07D471/06
摘要： The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11β-hydroxylase (CYP11B1) with these compounds.
摘要翻译：本发明提供了作为人醛固酮合酶抑制剂的通式（I）化合物，以及含有这些化合物的药物组合物，以及治疗醛固酮增多症和/或由11β-羟化酶介导的疾病或疾病的方法（ CYP11B1）与这些化合物。

2. 发明授权

US08541404B2 Inhibitors of the human aldosterone synthase CYP11B2 有权
标题翻译：人醛固酮合酶抑制剂CYP11B2
公开(公告)号：US08541404B2
公开(公告)日：2013-09-24
申请号：US12938581
申请日：2010-11-03
申请人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
发明人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
IPC分类号： C07D401/10 , C07D413/10 , A61K31/4745 , A61K31/4709
CPC分类号： C07D401/10 , C07D413/10 , C07D417/10 , C07D471/06
摘要： The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11β-hydroxylase (CYP11B1) with these compounds.
摘要翻译：本发明提供了作为人醛固酮合酶抑制剂的通式（I）化合物，以及含有这些化合物的药物组合物，以及治疗由11β-羟化酶（CYP11B1）介导的醛固酮增多症和/或病症或疾病的方法）与这些化合物。

3. 发明申请

US20110118241A1 6-Pyridin-3-YL-3,4-Dihydro-1H-Quinolin-2-One Derivatives and Related Compounds as Inhibitors of the Human Aldosterone Synthase CYP11B2 有权
标题翻译： 6-吡啶-3-基-L-3,4-二氢-1H-喹啉-2-酮衍生物和相关化合物作为人醛固酮合酶CYP11B2的抑制剂
公开(公告)号：US20110118241A1
公开(公告)日：2011-05-19
申请号：US12990909
申请日：2009-05-05
申请人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
发明人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
IPC分类号： A61K31/5415 , C07D401/10 , C07D471/06 , C07D417/10 , C07D413/10 , A61K31/4709 , A61K31/4439 , A61K31/4725 , A61K31/4745 , A61K31/506 , A61K31/538 , A61K31/498 , A61K31/536 , A61P9/12 , A61P5/40 , A61P9/04 , A61P13/12 , A61P9/10 , A61P9/00 , A61P3/04 , A61P29/00
CPC分类号： C07D401/04 , C07D215/227 , C07D221/06 , C07D401/14 , C07D471/04
摘要： The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1).
摘要翻译：本发明提供了作为人醛固酮合酶抑制剂的通式（I）化合物，以及含有这些化合物的药物组合物，以及这些化合物和其它杂芳基取代的喹啉酮衍生物用于治疗醛固酮增多症和/或病症或由11β-羟化酶（CYP11B1）介导的疾病。

4. 发明授权

US4839370A Novel derivatives of 3-aryl-3-cycloalkyl-piperidine-2,6-dione 失效
标题翻译： 3-芳基-3-环烷基 - 哌啶-2,6-二酮的新衍生物
公开(公告)号：US4839370A
公开(公告)日：1989-06-13
申请号：US79964
申请日：1987-07-31
申请人： Rolf W. Hartmann , Christine Batzl
发明人： Rolf W. Hartmann , Christine Batzl
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/451 , A61P3/00 , A61P35/00 , C07D211/26 , C07D211/88 , C07D401/04
CPC分类号： C07D401/04 , C07D211/88
摘要： Novel 3-aryl-3-cycloalkyl-piperidine-2,6-dione derivatives of the general formula I: ##STR1## in which A is a 4-aminophenyl radical or a pyridyl-(4)-radical and R.sub.1 is a saturated or unsaturated C.sub.3 -C.sub.10 -cycloalkyl radical or a C.sub.3 -C.sub.12 -alkenyl radical as well as physiologically acceptable salts thereof. The compounds are useful as inhibitors of estrogen biosynthesis. The compounds are made by a process which includes the step of heating a compound of the formula II ##STR2## wherein A and R.sub.1 have the meanings given above, and in addition A may also be a phenyl radical or a 4-nitrophenyl radical, X and Y are the same or different and repesent CN or COOC.sub.1 -C.sub.6 -alkyl and X or Y may also be COOH or a carboxylic acid ester group of the formula COOC.sub.1 -C.sub.6 -alkyl group, in a high boiling solvent at a temperature between 50.degree. and 200.degree. C. in particular between 80.degree. and 100.degree. C., optionally in the presence of condensation agents to form a piperidine dione ring.
摘要翻译：通式I的新型3-芳基-3-环烷基 - 哌啶-2,6-二酮衍生物：其中A是4-氨基苯基或吡啶基 - （4） - 衍生物，R 1是饱和的或不饱和C 3 -C 10 - 环烷基或C 3 -C 12 - 烯基以及其生理上可接受的盐。该化合物可用作雌激素生物合成的抑制剂。该化合物通过包括加热式II化合物II的步骤的方法制备，其中A和R 1具有上述含义，另外A也可以是苯基或4-硝基苯基， X和Y相同或不同，并且重复的CN或COOC 1 -C 6烷基，X或Y也可以是COOH或式COOC 1 -C 6 - 烷基的羧酸酯基，在高沸点溶剂中， 50℃和200℃，特别是80℃至100℃之间，任选在缩合剂存在下形成哌啶二酮环。

5. 发明授权

US4745233A Derivatives of 1,1,2,2-tetramethyl-1,2-bis-(2-fluoro-4-hydroxyphenyl)-ethane 失效
标题翻译： 1,1,2,2-四甲基-1,2-双 - （2-氟-4-羟基苯基） - 乙烷的衍生物
公开(公告)号：US4745233A
公开(公告)日：1988-05-17
申请号：US871892
申请日：1986-06-09
申请人： Helmut Schonenberger , Rolf W. Hartmann , Martin Schneider , Walter Schwarz , Jurgen Engel
发明人： Helmut Schonenberger , Rolf W. Hartmann , Martin Schneider , Walter Schwarz , Jurgen Engel
IPC分类号： C07F9/145 , A61K31/055 , A61K31/22 , A61K31/27 , A61K31/66 , A61P35/00 , C07C39/367 , C07C67/00 , C07C67/475 , C07C69/95 , C07C239/00 , C07C269/00 , C07F9/12 , F16J15/00 , C07C39/14 , C07C125/04 , C07C125/06
CPC分类号： C07C39/367 , C07F9/12
摘要： Antitumor compounds corresponding to the following formula: ##STR1## in which the substituents R.sub.1 and R.sub.2 may be the same or different and represent hydrogen, an aminocarbonyl group, a C.sub.1 -C.sub.6 alkylaminocarbonyl group, a di-C.sub.1 -C.sub.6 -alkylaminocarbonyl group, the group PO(OH).sub.2, a C.sub.2 -C.sub.8 alkanoyl group, a C.sub.2 -C.sub.8 halogen alkanoyl group or a C.sub.3 -C.sub.8 alkenoyl group, a process for their preparation, and their use in treating oestrogen-receptor-positive-tumors as well as the prostate carcinoma.
摘要翻译：对应于下式的抗肿瘤化合物：其中取代基R 1和R 2可以相同或不同并表示氢，氨基羰基，C 1 -C 6烷基氨基羰基，二-C 1 -C 6烷基氨基羰基，基团PO（OH）2，C 2 -C 8烷酰基，C 2 -C 8卤代烷酰基或C 3 -C 8烯酰基，其制备方法及其在治疗雌激素受体阳性肿瘤中的用途作为前列腺癌。

6. 发明申请

US20090221591A1 Selective Inhibitors of Human Corticosteroid Synthases 有权
标题翻译：人类皮质类固醇合成酶的选择性抑制剂
公开(公告)号：US20090221591A1
公开(公告)日：2009-09-03
申请号：US11885605
申请日：2006-03-02
申请人： Rolf W. Hartmann , Marieke Voets , Ursula Müller-Vieira
发明人： Rolf W. Hartmann , Marieke Voets , Ursula Müller-Vieira
IPC分类号： A61K31/498 , C07D401/04 , A61K31/497 , A61K31/4406 , C07D213/16 , A61P3/10
CPC分类号： A61K31/4164 , A61K31/4406 , A61K31/4709 , A61K31/505 , C07D213/16 , C07D213/30 , C07D213/55 , C07D213/56 , C07D213/57 , C07D233/54 , C07D233/56 , C07D233/64 , C07D239/26 , C07D239/30 , C07D239/34 , C07D263/32
摘要： The invention relates to compounds for selectively inhibiting human corticosteroid synthases CYP1 1 B1 and CYP1 1 B2, and to the production and use thereof for treating hypercortisolism, diabetes mellitus, hyperaldosteronism, cardiac insufficiency, myocardial fibrosis, depression, age-related cognitive decline and metabolic syndrome.
摘要翻译：本发明涉及用于选择性抑制人类皮质类固醇合酶CYP11B和CYP11B的化合物及其用于治疗高皮质醇血症，糖尿病，醛固酮增多症，心功能不全，心肌纤维化，抑郁症，年龄相关认知衰退和代谢的生产和用途综合征

7. 发明授权

US08685960B2 6-pyridin-3-yl-3,4-dihydro-1h-quinolin-2-one derivatives and related compounds as inhibitors of the human aldosterone synthase CYP11B2 有权
标题翻译： 6-吡啶-3-基-3,4-二氢-1h - 喹啉-2-酮衍生物和相关化合物作为人醛固酮合酶CYP11B2的抑制剂
公开(公告)号：US08685960B2
公开(公告)日：2014-04-01
申请号：US12990909
申请日：2009-05-05
申请人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
发明人： Rolf W. Hartmann , Ralf Heim , Simon Lucas
IPC分类号： C07D401/04 , A61K31/4745
CPC分类号： C07D401/04 , C07D215/227 , C07D221/06 , C07D401/14 , C07D471/04
摘要： The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 β-hydroxylase (CYP11 B1).
摘要翻译：本发明提供了作为人醛固酮合酶抑制剂的通式（I）化合物，以及含有这些化合物的药物组合物，以及这些化合物和其它杂芳基取代的喹啉酮衍生物用于治疗醛固酮增多症和/或病症或由11β-羟化酶（CYP11B1）介导的疾病。

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