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序号	专利名	申请号	申请日	公开（公告）号	公开（公告）日	发明人
1	杂交环状文库和其筛选	CN201180063026.5	2011-11-29	CN103282362A	2013-09-04	J·O·刘; J·王; M·达斯; S·布哈特; W·李; Z·郭
本发明提供新颖类型的杂交环状文库，其含有天然产物的已知蛋白质结合域。还提供制造所述文库的合成方法，和使用部分地分裂-合并的文库化合物对命中点进行去卷积的方法。所述方法适用于与整个人类蛋白质组一起用以筛选结合命中点的所述文库并且用于鉴别命中点。
2	杂交环状文库和其筛选	CN201610374535.4	2011-11-29	CN106084002A	2016-11-09	J·O·刘; J·王; M·达斯; S·布哈特; W·李; Z·郭
本发明提供新颖类型的杂交环状文库，其含有天然产物的已知蛋白质结合域。还提供制造所述文库的合成方法，和使用部分地分裂‑合并的文库化合物对命中点进行去卷积的方法。所述方法适用于与整个人类蛋白质组一起用以筛选结合命中点的所述文库并且用于鉴别命中点。
3	杂交环状文库和其筛选	CN201180063026.5	2011-11-29	CN103282362B	2016-06-29	J·O·刘; J·王; M·达斯; S·布哈特; W·李; Z·郭
本发明提供新颖类型的杂交环状文库，其含有天然产物的已知蛋白质结合域。还提供制造所述文库的合成方法，和使用部分地分裂-合并的文库化合物对命中点进行去卷积的方法。所述方法适用于与整个人类蛋白质组一起用以筛选结合命中点的所述文库并且用于鉴别命中点。
4	Hybrid cyclic libraries and screens thereof	US14987653	2016-01-04	US09783577B2	2017-10-10	Jun O. Liu; Jingxin Wang; Zufeng Guo; Wei Li; Shridhar Bhat; Manisha Das
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
5	Hybrid Cyclic Libraries and Screens Thereof	US13990396	2011-11-29	US20140073581A1	2014-03-13	Jun O. Liu; Jingxin Wang; Zufeng Guo; Wei Li; Shridhar Bhat; Manisha Das
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
6	Condensed pyridoindole derivatives	US10363528	2001-09-17	US06858620B2	2005-02-22	Mark W. Orme; Jason Scott Sawyer; Alain Claude-Marie Daugan; Romain Luc Marie Gosmini; Lisa M. Schultze
Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed
7	Method of preparing N-oxo-tetrahydro-.beta.-carbolines	US16675	1993-02-12	US5348949A	1994-09-20	Peter H. H. Hermkens; Jan H. Van Maarseveen; Johan W. Scheeren; Cornelis G. Kruse
The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## by an intramolecular ringclosure reaction of compounds of formula 2. ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.
8	Method of preparing n-oxo-tetrahydro-beta-carbolines	US533415	1990-06-05	US5106840A	1992-04-21	Peter H. H. Hermkens; Jan H. Van Maarseveen; Johan W. Scheeren; Cornelis G. Kruse
The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.1, andA together with the group --C--N--O--, forms a saturated heterocyclic ring systems consisting of 6-8 ring atoms, wherein, in addition to the already present oxygen atom and nitrogen atom, an extra hetero atom from the group, O, S and N may be present, which ring system may be substituted with one or more of the substituents alkyl, alkoxycarbonyl, alkanoyl, alkoxy, hydroxy, oxo, amino, mono- or dialkylamino, alkanoyl-or alkoxycarbonylamino, which ring system may be annelated with a saturated carbocyclic group of 5 or 6 ring atoms, by an intramolecular ring closure reaction of compounds of formula 2 ##STR2## wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a funciton during the ring closure reaction.The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumor activity.
9	HYBRID CYCLIC LIBRARIES AND SCREENS THEREOF	US15728282	2017-10-09	US20180222942A1	2018-08-09	Jun O. Liu; Jingxin Wang; Zufeng Guo; Wei Li; Shridhar Bhat; Manisha Das
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
10	Hybrid cyclic libraries and screens thereof	US13990396	2011-11-29	US09250237B2	2016-02-02	Jun O. Liu; Jingxin Wang; Zufeng Guo; Wei Li; Shridhar Bhat; Manisha Das
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
11	Di- and tetrahydroisoquinoline derivatives	US480755	1989-11-27	US5162335A	1992-11-10	Maurits E. A. Vandewalle; Johan T. A. Van der Eycken; Ineke van Wijngaarden; Roelof van Hes; Antonius Hulkenberg; Christophorus M. J. F. Keet
The invention relates to new di- and tetrahydroisoquinoline derivatives having interesting cytostatic properties, to the preparation of the said new compounds, and to compositions comprising such a compound as a cytostatically active substance.
12	BIARYL PYRAZOLES AS NRF2 REGULATORS	US15765354	2016-10-06	US20180282349A1	2018-10-04	James CALLAHAN; Jeffrey K. KERNS; Peng LI; Tindy LI; Brent W. McCLELAND; Hong NIE; Joseph E. PERO; Thomas Glanmor DAVIES; Maria GRAZIA CARR; Charlotte Mary GRIFFITHS-JONES; Thomas Daniel HEIGHTMAN; David NORTON; Marinus Leedert VERDONK; Alison Jo-Anne WOOLFORD; Hendrika Maria Gerarda WILLEMS
The present invention relates to biaryl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
13	NOSCAPINOID-PRODUCING MICROBES AND METHODS OF MAKING AND USING THE SAME	US15517761	2015-11-16	US20170253898A1	2017-09-07	Christina D. SMOLKE; Yanran LI
Engineered non-plant cells that produce a benzylisoquinoline alkaloid product that is a derivative of canadine along a metabolic pathway that converts canadine, or an analog of canadine, to a noscapinoid product are provided. Methods of culturing engineered non-plant cells that produce a noscapinoid product and pharmaceutical compositions are also provided.
14	HYBRID CYCLIC LIBRARIES AND SCREENS THEREOF	US14987653	2016-01-04	US20160115203A1	2016-04-28	Jun O. Liu; Jingxin Wang; Zufeng Guo; Wei Li; Shridhar Bhat; Manisha Das
Provided are novel types of hybrid cyclic libraries that contain a known protein binding domain of a natural product. Also provided are synthetic methods to make such libraries and methods for the deconvolution of hits using partially split-pooled library compounds. Such methods are applicable for use with the entire human proteome to screen such libraries that bind and for the identification of hits.
15	Chemical compounds	US10363528	2003-03-03	US20040082787A1	2004-04-29	Mark W Orme; Jason Scott Sawyer; Alain Claude-Marie Daugan; Romain Luc Marie Gosmini; Lisa M Schultze
Compounds of general structural formula (I), and use of the compounds or salts or solvates thereof as therapeutic agents, are disclosed. 1
16	Cytostatic beta-carbolines	US397859	1989-08-24	US5095020A	1992-03-10	Antonius Hulkenberg; Ineke Van Wijngaarden
The invention relates to a group of new .beta.-carbolines, their bio-isosteric benzofuran and benzothiophene analogues, and to the preparation of these compounds.The new compounds can be represented by the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are hydrogen, or R+R.sub.1 or R.sub.1 +R.sub.2 form a saturated heterocyclic ring having 5 or 6 ring atoms, which comprise 1 or 2 oxygen atoms;R.sub.3 is hydrogen, or hydroxy optionally derivatised with a sugar radical the 4,6-hydroxy groups of which are acetalised with an -ylidene group;R.sub.4 is a group of the formula --C(R.sub.11).sub.2 --X--R.sub.12, wherein the groups R.sub.11 are hydrogen, or both groups R.sub.11 together represent a double-bonded keto oxygen atom, X is oxygen or a group NR.sub.14, wherein R.sub.14 is hydrogen or alkyl having 1-4 C-atoms, and R.sub.12 is hydrogen, alkyl having 1-4 C-atoms, alkanoyl having 1-4 C-atoms, the carbamoyl group or mono- or dialkylcarbamoyl group having 1-4 C-atoms per alkyl group;R.sub.5 is hydrogen, alkanoyl or alkyl having 1-4 C-atoms, or R.sub.4 +R.sub.5 together form a group of the formula --C(R.sub.11).sub.2 --X--Z, wherein R.sub.11 and X have the above-mentioned meanings and Z is bound to the ring nitrogen atom and is a group ##STR2## R.sub.7 and R.sub.9 independently of each other are hydrogen or alkoxy having 1-4 C-atoms, trifluoromethyl or halogen;R.sub.8 is hydrogen, alkoxy or alkanoyloxy having 1-4 C-atoms, hydroxy, halogen, benzyloxy, or R.sub.8 and R.sub.9 together constitute a dioxyalkylidene bridge;A is oxygen, sulphur or a group ##STR3## and R.sub.6 and R.sub.13 independently of each other are hydrogen or methyl, or, when A is nitrogen, R.sub.6 and R.sub.13 together may form a ring having 5-7 C-atoms. The compounds have good cytostatic properies.
17	Antiviral eudistomins from a marine tunicate	US578443	1984-02-09	US4631149A	1986-12-23	Kenneth L. Rinehart, Jr.; Gary C. Harbour; Jun'ichi Kobayashi
The subject invention concerns novel and useful antiviral compounds referred to as eudistomins. These compounds are obtainable from well-known and available marine organisms. Their utility is as antiviral agents as well as antibacterial and antitumor agents in some cases.
18	N-oxotetrahydro-beta-carbolines	EP96200625.0	1990-06-05	EP0719777A3	1996-07-17	Hermkens, Peter Harold Han; van Maarseveen, Jan Herman; Scheeren, Johan Wilhelm; Kruse, Cornelis Gerrit
The invention relates to a method of preparing N-oxo-tetrahydro-β-carbolines having formula 1. wherein R₁ is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino, n has the value 0, 1 or 2, R₂ is hydrogen, lower alkyl or acyl, R₃ is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R₁, and A together with the group -C-N-O-, forms a saturated heterocyclic ring system consisting of 6-8 ring atoms, wherein, in addition to the already present oxygen atom and nitrogen atom, an extra hetero atom from the group O, S and N may be present, which ring system may he substituted with one or more of the substituents alkyl,alkoxycarbonyl, alkanoyl, alkoxy, hydroxy, oxo, amino, mono- or dialkylamino, alkanoyl-or alkoxycarbonylamino, which ring system may be annelated with a saturated carbocyclic group of 5 or 6 ring atoms, by an intramolecular ringclosure reaction of compounds of formula 2 wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction. The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.
19	Method of preparing N-oxotetrahydro- -carbolines	EP90201430.7	1990-06-05	EP0401929A2	1990-12-12	Hermkens, Peter Harold Han; van Maarseveen, Herman; Scheeren, Johan Wilhelm; Kruse, Cornelis Gerrit
The invention relates to a method of preparing N-oxo-tetrahydro-β-carbolines having formula 1. wherein - R₁ is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino, - n has the value 0, 1 or 2, - R₂ is hydrogen, lower alkyl or acyl, - R₃ is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R₁, and - A together with the group -C-N-O-, forms a saturated heterocyclic ring system consisting of 6-8 ring atoms, wherein, in addition to the already present oxygen atom and nitrogen atom, an extra hetero atom from the group O, S and N may be present, which ring system may be substituted with one or more of the substituents alkyl,alkoxycarbonyl, alkanoyl, alkoxy, hydroxy, oxo, amino, mono- or dialkylamino, alkanoyl- or alkoxycarbonylamino, which ring system may be annelated with a saturated carbocyclic group of 5 or 6 ring atoms, by an intramolecular ringclosure reaction of compounds of formula 2 wherein Z is an aldehyde function or acetal function, or is a functional group which can be converted into such a function during the ringclosure reaction. The eudistomin derivatives within the group of compounds having formula 1 have strong antiviral and antitumour activity.
20	Antibiotics	EP84304968.5	1984-07-20	EP0133000B1	1990-09-26	Rinehart, Kenneth Lloyd; HARBOUR, Gary C.; KOBAYASHI, Junichi

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