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1. 发明授权

US4851406A Heterocyclic-substituted indoles and pharmaceutical compositions containing them 失效
标题翻译：杂环取代的吲哚和含有它们的药物组合物
公开(公告)号：US4851406A
公开(公告)日：1989-07-25
申请号：US904092
申请日：1986-09-04
申请人： Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Alfred Mertens , Wolfgang von der Saal , Walter-Gunar Friebe , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： C07D409/14 , A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/50 , A61K31/53 , A61K31/535 , A61P9/00 , C07D237/00 , C07D333/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14 , C07D417/14
CPC分类号： C07D401/14
摘要： The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.2 is ##STR2## the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them.Furthermore, the present invention provides intermediates of the general formula: ##STR3## in which R.sub.1, R.sub.2, A and X have the same meanings as above, and processes for the preparation of these intermediates.
摘要翻译：本发明提供以下通式的吲哚衍生物：其中R 1是氢原子或烷基，烯基，环烷基，环烯基，羧基，氰基，烷基羰基，烷氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基或芳基， R2是氢原子或烷基，三卤代甲基，羟基，环烷基，氰基，羧基，烷氧基羰基，烷基羰基，氨基羰基，烷基氨基羰基或二烷基氨基羰基; R2是含有1至4个杂原子的杂环五元环或含有1至5个杂原子的杂环六元环，五元和六元环的杂原子相同或不同，为氮，氧或硫，一个或多个氮原子任选地带有氧原子，所述五元和六元环任选被一个或多个烷基，烷氧基，烷硫基，氧代，羟基，硝基，氨基，卤素或氰基取代; 或者R2是其互变异构体及其与无机和有机酸的生理上可接受的盐。本发明还提供了制备这些化合物的方法和含有它们的药物组合物。此外，本发明提供通式如下的中间体：其中R1，R2，A和X具有与上述相同的含义，以及制备这些中间体的方法。

2. 发明授权

US4835167A Tricyclic benzotriazoles, processes for the preparation thereof and pharmaceutical compositions containing them 失效
标题翻译：三环苯并三唑，其制备方法和含有它们的药物组合物
公开(公告)号：US4835167A
公开(公告)日：1989-05-30
申请号：US80658
申请日：1987-08-03
申请人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Gisbert Sponer
发明人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Gisbert Sponer
IPC分类号： C07D487/04 , C07D487/10 , C07D498/04 , C07D513/04
CPC分类号： C07D487/04 , C07D487/10 , C07D513/04
摘要： The present invention provides new tricyclic benzotriazoles of the general formula: ##STR1## wherein Z is a hydrogen atom or an acyl radical, Y is an oxygen or sulphur atom or two hydrogen atoms and X is an oxygen or sulphur atom or a >CR.sub.1 R.sub.2 or >NR.sub.3 group, R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, alkenyl or cyano group or a carbonyl group substituted by a hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino group or R.sub.2, together with R.sub.1, represents a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical and R.sub.3 is a hydrogen atom or an alkyl radical; the tautomers thereof and the physiologically acceptable acid-addition salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these tricyclic benzotriazoles and pharmaceutical compositions containing them for the treatment of heart and circulatory diseases.
摘要翻译：本发明提供了新的具有以下通式的三环苯并三唑：其中Z是氢原子或酰基，Y是氧或硫原子或两个氢原子，X是氧或硫原子或 > CR1R2或> NR3基团，R1是氢原子或烷基，烯基或环烷基，R2是氢原子或烷基，烯基或氰基或被羟基，烷基，烷氧基，氨基，烷基氨基取代的羰基，二烷基氨基或肼基或R 2与R 1一起代表亚环烷基或R 1和R 2一起形成亚烷基或亚环烷基，R 3为氢原子或烷基; 其互变异构体及其与无机和有机酸的生理上可接受的酸加成盐。本发明还提供了制备这些三环苯并三唑的方法和含有它们用于治疗心脏和循环系统疾病的药物组合物。

3. 发明授权

US4870077A Heterocyclic substituted indolinones 失效
标题翻译：杂环取代的二氢吲哚酮
公开(公告)号：US4870077A
公开(公告)日：1989-09-26
申请号：US94871
申请日：1987-09-10
申请人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Lothar Kling
发明人： Wolfgang Von Der Saal , Walter-Gunar Friebe , Alfred Mertens , Bernd Muller-Beckmann , Lothar Kling
IPC分类号： A61K31/50 , A61K31/535 , A61K31/54 , A61P9/00 , C07D209/34 , C07D209/46 , C07D403/04 , C07D413/04 , C07D417/04
CPC分类号： C07D403/04 , C07D209/34 , C07D413/04 , C07D417/04
摘要： Heterocyclic substituted indolinones of the formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a carboxyl group or an alkoxy-carbonyl, hydroxyalkyl or alkylcarbonyloxyalkyl radical or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a lactone having 4, 5 or 6 ring atoms, A-B is --CH.sub.2 --CH(R.sub.3)--, --CH.dbd.CR.sub.3 --, --CH.sub.2 --NH--, --NH--CH.sub.2 --, --CH.sub.2 --O--, --O--CH.sub.2 --, --CH.sub.2 --S-- or --S--CH.sub.2 -- radical, R.sub.3 being a hydrogen atom or an alkyl or hydroxyalkyl radical, or A is a valency bond and B is a methylene radical ##STR2## or an imino group ##STR3## R.sub.4, R.sub.5, and R.sub.6 independently being hydrogen atoms or alkyl radicals wherein the alkyl groups independently contain 1 to 6 carbon atoms; as well as the tautomers thereof and the physiologically acceptable salt thereof and the physiologically acceptable salts thereof with inorganic and organic acids, are disclosed, such as, for instance, the compound 5-(2,3,4,5-tetrahydro-3-oxopyridazin-6-yl)-3-ethoxycarbonyl-3-methyl-1H-indol n-2-one. The compounds of the invention are useful in the treatment of heart and circulatory diseases, for example, by producing a positive inotropic action in a patient to whom the compounds are administered.
摘要翻译：式（I）的杂环取代的二氢吲哚酮：其中R 1是氢原子或烷基或羟烷基，R 2是羧基或烷氧羰基，羟基烷基或烷基羰基氧基烷基或R 1和R 2与碳它们连接的原子形成具有4,5或6个环原子的内酯，AB是-CH 2 -CH（R 3） - ， - CH = CR 3 - ， - CH 2 -NH-，-NH-CH 2 - ， - CH 2 -O-，-O-CH 2 - ， - CH 2 -S-或-S-CH 2 - 基，R 3是氢原子或烷基或羟烷基，或A是价键，B是亚甲基。或亚氨基基团R4，R5和R6独立地为氢原子或烷基，其中烷基独立地含有1至6个碳原子; 以及其与无机和有机酸的互变异构体及其生理上可接受的盐及其生理上可接受的盐，例如化合物5-（2,3,4,5-四氢-3- 氧基哒嗪-6-基）-3-乙氧基羰基-3-甲基-1H-吲哚-2-酮。本发明的化合物可用于治疗心脏和循环系统疾病，例如通过在施用化合物的患者中产生正性肌力作用。

4. 发明授权

US4146630A Blood pressure lowering and adrenergic .beta.-receptor inhibiting 3-(4-phenoxymethylpiperidino)-propyl-phenyl ethers 失效
标题翻译：血压降低和ADRENERGIC“ - 抑制3-（4-苯甲酰氨基哌啶）丙基苯基醚
公开(公告)号：US4146630A
公开(公告)日：1979-03-27
申请号：US846057
申请日：1977-10-27
申请人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
发明人： Wolfgang Kampe , Walter-Gunar Friebe , Fritz Wiedemann , Gisbert Sponer , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07D401/12 , A61K31/403 , A61K31/4184 , A61K31/44 , A61K31/4427 , A61K31/445 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/02 , C07D209/90 , C07D211/22 , C07D231/56
CPC分类号： C07D211/22 , C07D231/56
摘要： A 3-(4-phenoxymethylpiperidino)-propyl-phenyl-ether of the formula ##STR1## wherein R.sub.1 and R.sub.2 each independently is hydrogen, lower alkyl, hydroxyalkyl, lower alkanoyloxyalkyl or --CO--Z,Z is hydroxy, lower alkyloxy or ##STR2## R.sub.6 and R.sub.7 each independently is hydrogen, lower alkyl or hydroxyalkyl,R.sub.3 is hydrogen or --O--R.sub.8,R.sub.8 is hydrogen, lower alkanoyl or aroyl optionally substituted by halogen, lower alkyl, lower alkoxy, alkoxycarbonyl, hydroxyl, alkylthio, nitrile, nitro or trifluoromethyl,R.sub.4 and R.sub.5 each independently is hydrogen, halogen, hydroxy, benzyloxy, lower alkyl, lower alkoxy, lower alkylthio, carboxy, benzyloxycarbonyl or lower alkoxycarbonyl,X and Y each independently is nitrogen or ##STR3## R.sub.9 is hydrogen, lower allkyl optionally substituted by --O--R.sub.8, or --CO--Z,or a pharmacologically acceptable salt thereof. The compounds lower blood pressure and inhibit adrenergic .beta.-receptors.

5. 发明授权

US4086347A 9-[3-(4-Phenoxymethylpiperidino)-propyl]-adenines 失效
标题翻译： 9- {8- 3-（4-苯氧基甲基哌啶子基） - 丙基{9-腺嘌呤
公开(公告)号：US4086347A
公开(公告)日：1978-04-25
申请号：US737507
申请日：1976-11-02
申请人： Walter-Gunar Friebe , Max Thiel , Kurt Stach, deceased , by Werner Plattner, administrator , Otto-Henning Wilhelms , Erika VON Mullendorff , Gisbert Sponer
发明人： Walter-Gunar Friebe , Max Thiel , Kurt Stach, deceased , by Werner Plattner, administrator , Otto-Henning Wilhelms , Erika VON Mullendorff , Gisbert Sponer
IPC分类号： A61K31/52 , A61P3/00 , A61P9/12 , A61P29/00 , A61P37/08 , C07D401/06 , C07D401/14 , C07D473/34
CPC分类号： C07D473/34 , Y10S514/826 , Y10S514/87
摘要： 9-[3-(4-Phenoxymethylpiperidino)-propyl]-adenines of the formula ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl radical,R.sub.2 is a hydrogen atom, a ower alkyl radical optionally substituted by hydroxyl, or a cycloalkyl radical, orR.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a heterocyclic ring, andR.sub.3 is a hydrogen atom, a halogen atom, a lower alkyl radical or a lower alkoxy radical,In the form of the free base or a salt thereof, exhibit anti-allergic, anti-inflammatory, anti-oedematous and anti-hypertensive activity.
摘要翻译：式[IMAGE]的9- [3-（4-苯氧基甲基哌啶子基） - 丙基] - 腺嘌呤，其中R 1为氢原子或低级烷基，R 2为氢原子，任选被羟基取代的烷基，或环烷基或R 1和R 2与它们所连接的氮原子一起形成杂环，并且R 3是氢原子，卤素原子，低级烷基或低级烷氧基，在自由基的形式或其盐，展示抗过敏，抗炎，抗氧化和抗高血压活性。

6. 发明授权

US4288442A Inhibiting adrenergic .beta.-receptors with piperidinopropyl derivatives 失效
标题翻译：用哌啶丙基衍生物抑制肾上腺素β受体
公开(公告)号：US4288442A
公开(公告)日：1981-09-08
申请号：US117172
申请日：1980-01-31
申请人： Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Gisbert Sponer , Wolfgang Schaumann
发明人： Walter-Gunar Friebe , Helmut Michel , Carl H. Ross , Fritz Wiedemann , Gisbert Sponer , Wolfgang Schaumann
IPC分类号： C07D401/12 , A61K31/44 , A61K31/4427 , A61K31/4523 , A61K31/505 , A61P9/08 , A61P9/12 , A61P25/02 , C07C205/56 , C07D209/04 , C07D209/08 , C07D209/82 , C07D211/14 , C07D211/22 , C07D235/04 , C07D401/14 , A61K31/445
CPC分类号： C07D211/22 , C07C205/56
摘要： A piperidinopropyl derivative of the formula ##STR1## in which R.sub.1 and R.sub.2 each independently is hydrogen or a lower alkyl radical, or together are an alkylene radical,R.sub.3 is hydrogen, hydroxy, or acyloxy,R.sub.4 is hydrogen or formyl,A together with the adjacent benzene ring and N-R.sub.4 forms a benzimidazolin-2-one, benzimidazoline-2-thione, oxindole, indazole carbazole, benztriazole, benzimidazole, indoline or indole moiety, andB is a heterocyclic radical or, under certain circumstances, a phenyl radical, either of which is optionally substituted by halogen, hydroxy, lower alkyl, hydroxy-lower alkyl, carboxamido-lower alkyl, lower alkoxy, amino, carboxamido, lower alkyl-carbonylamino, acyl or lower alkylsulphonylamino,or a pharmacologically acceptable salt thereof. The compounds inhibit adrenergic .beta.-receptors and lower blood pressure.
摘要翻译：其中R 1和R 2各自独立地是氢或低级烷基，或者一起是亚烷基，R 3是氢，羟基或酰氧基，R 4是氢或甲酰基，A和相邻的苯环和N-R4形成苯并咪唑啉-2-酮，苯并咪唑啉-2-硫酮，羟吲哚，吲唑咔唑，苯并三唑，苯并咪唑，二氢吲哚或吲哚部分，B为杂环基团，或在某些情况下为苯基羟基，低级烷基，羟基 - 低级烷基，甲酰胺基 - 低级烷基，低级烷氧基，氨基，甲酰氨基，低级烷基 - 羰基氨基，酰基或低级烷基磺酰基氨基，或其药理学上可接受的盐。这些化合物抑制肾上腺素能β受体和降低血压。

7. 发明授权

US4378363A Certain heterocyclic-carboxamido-phenoxy-aminopropanols, compositions containing same and methods of using same 失效
标题翻译：某些杂环 - 甲酰胺基 - 苯氧基 - 氨基丙醇，含有它们的组合物及其使用方法
公开(公告)号：US4378363A
公开(公告)日：1983-03-29
申请号：US207527
申请日：1980-11-17
申请人： Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Karl Dietmann
发明人： Walter-Gunar Friebe , Wolfgang Kampe , Wolfgang Bartsch , Gisbert Sponer , Karl Dietmann
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/4406 , A61K31/4418 , A61K31/455 , A61P9/00 , A61P25/02 , C07D207/26 , C07D207/27 , C07D207/34 , C07D209/18 , C07D209/42 , C07D209/43 , C07D213/81 , C07D213/82 , C07D215/48 , C07D235/24 , C07D307/85
CPC分类号： C07D207/27 , C07D207/34 , C07D209/18 , C07D209/42 , C07D213/81 , C07D213/82 , C07D215/48 , C07D235/24 , C07D307/85 , Y10S514/821
摘要： This invention relates to new aminopropanol compounds having beta-adrenergic activity. In addition, the invention is directed to pharmaceutical compositions containing such compounds for the treatment of cardiac and circulatory infirmities and to methods for treating such infirmities.More particularly, the invention relates to new aminopropanol compound of the formula ##STR1## wherein R.sub.1 is a low alkyl moiety, which can be substituted, if desired, by a group Z-R.sub.5 ;R.sub.2 is hydrogen or a low alkanoyl group;R.sub.3 is a mono- or bicyclic heterocyclic compound having 1 to 2 hetero atoms, which can be mono- or polysubstituted, if desired, by halogen, amino, hydroxyl, low alkoxyl, low alkyl;R.sub.4 is hydrogen, a low alkanoyl group or an aroyl group;R.sub.5 is hydrogen or a carbocyclic or heterocyclic aryl moiety, which can be mono- or polysubstituted, if desired, by hydroxyl, low alkyl, low alkenyl, low alkoxyl or low alkenyloxyl;X is a valence bond or a methylene group; andZ is a valence bond, an oxygen atom, or a sulfur atom, and their pharmacologically compatible salts.
摘要翻译：本发明涉及具有β-肾上腺素能活性的新的氨基丙醇化合物。此外，本发明涉及含有用于治疗心脏和循环系统疾病的化合物的药物组合物以及用于治疗这些病症的方法。更具体地，本发明涉及式（I）的新的氨基丙醇化合物，其中R 1是低级烷基部分，如果需要，可以被Z-R5基团取代; R2是氢或低烷酰基; R3是具有1至2个杂原子的单环或双环杂环化合物，如果需要，可以被卤素，氨基，羟基，低烷氧基，低级烷基单取代或多取代; R4是氢，低级烷酰基或芳酰基; R5是氢或碳环或杂环芳基部分，如果需要，可以被羟基，低级烷基，低级链烯基，低烷氧基或低链烯氧基单取代或多取代; X是价键或亚甲基; Z是价键，氧原子或硫原子，以及它们的药理学上相容的盐。

8. 发明授权

US4863945A Pyrrolobenzimidazoles and pharmaceutical compositions containing them 失效
标题翻译：吡咯并苯并咪唑和含有它们的药物组合物
公开(公告)号：US4863945A
公开(公告)日：1989-09-05
申请号：US131367
申请日：1987-12-10
申请人： Walter-Gunar Friebe , Alfred Mertens , Klaus Strein , Erwin Boehm
发明人： Walter-Gunar Friebe , Alfred Mertens , Klaus Strein , Erwin Boehm
IPC分类号： A61K31/40 , A61P7/02 , A61P9/04 , A61P9/12 , C07D487/04
CPC分类号： C07D487/04
摘要： Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.
摘要翻译：下式的吡咯并苯并咪唑：可用于治疗心脏和循环系统疾病。 R1是取代的苯基; 或任选取代的萘基或可与苯环缩合形成双环基团的五元或六元杂环基。 R2是氢，烷基，烯基或环烯基; R3是烷基，烯基或羟基烷基或与R2一起形成亚环烷基; 或者R 2和R 3一起形成亚烷基或亚环烷基。 R4是氢或低级烷酰基。 X是价键，亚烷基，亚乙烯基，亚氨基或羰基氨基。 T代表两个氢原子。当X是价键时，R 1也可以是氢，也可以含有氧，氨基，硫，羰基和磺酰基的烃基。当X是亚氨基或羰基氨基时，或当R1是双环基时，T也可以是氧。化合物还包括与无机和有机酸形成的互变异构体和生理上可接受的盐。

9. 发明授权

US07432291B2 Ether derivatives 失效
标题翻译：醚衍生物
公开(公告)号：US07432291B2
公开(公告)日：2008-10-07
申请号：US11083176
申请日：2005-03-17
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Ulrike Reiff , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Thomas Friess , Ulrike Reiff , Edgar Voss
IPC分类号： A61K31/41 , C07D249/04
CPC分类号： C07D417/12 , C07D413/12 , C07D413/14
摘要： The present invention provides the compounds of formula (I) their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明提供式（I）化合物的药学上可接受的盐或酯，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的组合物及其制备方法，以及上述用途，提及的化合物在控制或预防诸如癌症的疾病中。

10. 发明授权

US07247649B2 Oxazoles, their manufacture and use as pharmaceutical agents 失效
标题翻译：恶唑，其制造和用作药剂
公开(公告)号：US07247649B2
公开(公告)日：2007-07-24
申请号：US10910765
申请日：2004-08-03
申请人： Birgit Bossenmaier , Walter-Gunar Friebe , Ulrike Reiff , Matthias Rueth , Edgar Voss
发明人： Birgit Bossenmaier , Walter-Gunar Friebe , Ulrike Reiff , Matthias Rueth , Edgar Voss
IPC分类号： A61K31/422 , C07D263/30 , C07D413/12
CPC分类号： C07D413/12
摘要： The present invention relates to novel oxazoles of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
摘要翻译：本发明涉及式（I）的新颖恶唑，其药学上可接受的盐，对映体形式，非对映异构体和外消旋体，上述化合物的制备，含有它们的药物及其制备，以及上述用途控制或预防疾病如癌症的化合物。

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