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1. 发明授权

US08450341B2 Substituted indolin-2-one derivatives and their use as P38 mitogen-activated kinase inhibitors 失效
标题翻译：取代的二氢吲哚-2-酮衍生物及其作为P38丝裂原活化激酶抑制剂的用途
公开(公告)号：US08450341B2
公开(公告)日：2013-05-28
申请号：US12989696
申请日：2009-04-16
申请人： Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Victor Giulio Matassa
发明人： Paul Robert Eastwood , Jacob Gonzalez Rodriguez , Victor Giulio Matassa
IPC分类号： A01N43/42 , A01N43/82 , A01N43/38 , A61K31/44 , A61K31/41 , A61K31/40 , A61K31/405 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02 , C07D515/02 , C07D271/06 , C07D271/12 , C07D413/00 , C07D498/00 , C07D261/20 , C07D249/00 , C07D487/02 , C07D495/02 , C07D497/02 , C07D405/00 , C07D409/00 , C07D411/00 , C07D209/36
CPC分类号： C07D413/04 , C07D491/107 , C07D491/20
摘要： The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：本公开涉及具有通式（I）的p38丝裂原活化蛋白激酶的新抑制剂，其制备方法，其药物组合物及其使用方法。

2. 发明申请

US20210284655A1 LIBRARIES OF HETEROARYL-CONTAINING MACROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING THE SAME 有权
公开(公告)号：US20210284655A1
公开(公告)日：2021-09-16
申请号：US17173153
申请日：2021-02-10
申请人： CYCLENIUM PHARMA INC.
发明人： Amal WAHHAB , Helmut THOMAS , Luc RICHARD , Mark L. PETERSON , Dwight MACDONALD , Daniel DUBÉ
IPC分类号： C07D498/00 , C07D497/00 , C07D497/02 , C07D498/08 , C40B40/04 , C07D498/02 , G01N33/50
摘要： The present disclosure relates to novel macrocyclic compounds and libraries thereof containing heteroaryl moieties that are useful as research tools for drug discovery efforts. The present disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.

3. 发明授权

US08273269B2 Red colour filter composition 有权
标题翻译：红色滤色片组成
公开(公告)号：US08273269B2
公开(公告)日：2012-09-25
申请号：US12993095
申请日：2009-05-05
申请人： Roman Lenz , Gerardus De Keyzer , Mathias Duggeli , Patrick Christopher Holzhuter
发明人： Roman Lenz , Gerardus De Keyzer , Mathias Duggeli , Patrick Christopher Holzhuter
IPC分类号： G02B5/23 , C07D487/02 , C07D491/02 , C07D495/02 , C07D497/02
CPC分类号： C09B57/004 , C09B67/0033 , C09B67/0039 , C09B69/00 , G02B5/223
摘要： A composition, for producing dispersions, thermoplastic masses and/or color filters, comprising (a) a colorant of formula (1) wherein 20-100 mol % R1 are Br and 80-100 mol % R3 are H, especially of formula (Ib) and/or (Ic); (b) from 0 to 150% by weight, based on (a), of C. I. Pigment Red 144, 188, 190, 224, 242 or 2,4,6-trimethylphenylperylene diimide; (c) from 3 to 25% by weight, based on (a), of a di- or tri-azacyclopentylmethyl-substituted colorant (formulae given); (d) from 0 to 10% by weight, preferably from 0.01 to 8% by weight, based on the sum of (a) and (b), of an additionally sulfonated colorant of the same kernels as in (c); and (e) from 0 to 30% by weight, preferably from 3 to 25% by weight, especially from 5 to 20% by weight, based on (a), of a diketopyrrolopyrrole colorant substituted by at least one chain containing a plurality of nitrogen atoms (cf. formula (V)).
摘要翻译：一种用于生产分散体，热塑性物质和/或滤色剂的组合物，其包含（a）式（1）的着色剂，其中20-100摩尔％的R 1是Br，80-100摩尔％的R 3是H，特别是式）和/或（Ic）; （b）基于（a）0-150重量％的C.I.颜料红144,188,190,224,242或2,4,6-三甲基苯基亚苯基二酰亚胺; （c）基于（a）3至25重量％的二 - 或三 - 氮杂环戊基甲基取代的着色剂（给出公式）; （d）相对于（c）中相同核的另外的磺化着色剂，基于（a）和（b）的总和为0至10重量％，优选为0.01至8重量％和（e）基于（a）0至30重量％，优选3至25重量％，特别是5至20重量％的由至少一个链取代的二酮吡咯并吡咯着色剂，所述链含有多个氮原子（参见式（Ⅴ））。

4. 发明授权

US08013170B2 Substituted pyrrolo[1,2-d][1,4]-diazonines and treatment of brain damage 有权
标题翻译：取代的吡咯并[1,2-d] [1,4] - 二氮嗪并治疗脑损伤
公开(公告)号：US08013170B2
公开(公告)日：2011-09-06
申请号：US12002178
申请日：2007-12-14
申请人： Paul William Richard Harris , Margaret Anne Brimble
发明人： Paul William Richard Harris , Margaret Anne Brimble
IPC分类号： C07D487/02 , C07D491/02 , C07D495/02 , C07D497/02
CPC分类号： C07D487/04 , C07D471/04 , C07K5/06139 , C07K5/0821
摘要： Embodiments of this invention provide novel peptidomimetics that contain a macrocycle, an embodiment of which is 2S,9′S,12′S)-2-{[(1′,4′-Diaza-2′-oxobicyclo[7.3.0]dodecyl)-12′-carbonyl]amino}-1,5-pentanedioic acid trifluoroacetate. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterized by neuronal degeneration and/or neuronal cell death caused by in embodiments, toxicity or hypoxia. Compounds are also useful for manufacture of medicaments useful for treatment of such conditions.
摘要翻译：本发明的实施方案提供了含有大环的新型肽模拟物，其实施方案为2S，9'S，12'S）-2 - {[（1'，4'-二氮杂-2'-氧代双环[7.3.0] 十二烷基）-12'-羰基]氨基} -1,5-戊二酸三氟乙酸盐。这些化合物是神经保护性的，并且具有用作治疗由实施方案，毒性或缺氧引起的疾病，损伤和特征在于神经元变性和/或神经元细胞死亡的其它病症的治疗剂。化合物也可用于制备可用于治疗这些病症的药物。

5. 发明授权

US4666904A Aminoacyllabdanes, pharmacuetical compositions and use 失效
标题翻译：氨基酰氨基胆碱，药物组合物和用途
公开(公告)号：US4666904A
公开(公告)日：1987-05-19
申请号：US920547
申请日：1986-10-20
申请人： Raymond W. Kosley, Jr. , Robert J. Cherill
发明人： Raymond W. Kosley, Jr. , Robert J. Cherill
IPC分类号： C07D311/92 , C07D405/12 , C07D493/04 , C07D497/04 , A61K31/36 , A61K31/54 , C07D493/02 , C07D497/02
CPC分类号： C07D405/12 , C07D311/92 , C07D493/04 , C07D497/04
摘要： Novel aminoacyllabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
摘要翻译：公开了新型氨基酰氨基乙烷，其中间体及其制备方法，以及利用化合物或其组合物降低眼内压的方法。

6. 发明授权

US07714018B2 Heterocyclic antiviral compounds 失效
标题翻译：杂环抗病毒化合物
公开(公告)号：US07714018B2
公开(公告)日：2010-05-11
申请号：US11637423
申请日：2006-12-11
申请人： Eun Kyung Lee , Chris Richard Melville , David Mark Rotstein
发明人： Eun Kyung Lee , Chris Richard Melville , David Mark Rotstein
IPC分类号： A61K31/40 , C07D487/02 , C07D491/02 , C07D495/02 , C07D497/02 , C07D209/44 , C07D209/52
CPC分类号： C07D487/04
摘要： Chemokine receptor antagonists, in particular, 3,7-diazabicyclo[3.3.0]octane compounds according to formula (I) are antagonists of chemokine CCR5 receptors which are useful for treating or preventing an human immunodeficiency virus (HIV) infection, or treating AIDS or ARC. The invention further provides methods for treating diseases that are alleviated with CCR5 antagonists. The invention includes pharmaceutical compositions and methods of using the compounds for the treatment of these diseases. The invention further includes processes for the preparation of compounds according to formula I.
摘要翻译：趋化因子受体拮抗剂，特别是根据式（I）的3,7-二氮杂双环[3.3.0]辛烷化合物是可用于治疗或预防人类免疫缺陷病毒（HIV）感染或治疗AIDS的趋化因子CCR5受体的拮抗剂或ARC。本发明还提供了用于治疗被CCR5拮抗剂缓解的疾病的方法。本发明包括药物组合物和使用该化合物治疗这些疾病的方法。本发明还包括制备式I化合物的方法。

7. 发明申请

US20100098630A1 Phenazine and Quinoxaline Substituted Amino Acids and Polypeptides 审中-公开
标题翻译：吩嗪和喹喔啉取代的氨基酸和多肽
公开(公告)号：US20100098630A1
公开(公告)日：2010-04-22
申请号：US12520979
申请日：2007-12-28
申请人： Zhenwei Miao
发明人： Zhenwei Miao
IPC分类号： A61K31/498 , C07D241/36 , C07D241/46 , C07D497/02 , C07D265/34 , C07K14/475 , C12P21/02 , A61K31/5383 , A61K51/04 , A61K38/18 , A61K38/21 , A61K38/28
CPC分类号： C07K1/1075 , C07D241/40 , C07D401/14 , C07D487/12 , C07K14/615
摘要： Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a phenazine or quinoxaline substituent. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides.
摘要翻译：本文公开了包含至少一种非天然氨基酸的非天然氨基酸和多肽，以及制备这种非天然氨基酸和多肽的方法。非天然氨基酸本身或作为多肽的一部分可以包括吩嗪或喹喔啉取代基。本文还公开了在翻译后进一步修饰的非天然氨基酸多肽，用于实现这种修饰的方法，以及纯化这些多肽的方法。

8. 发明申请

US20050272938A1 Process and intermediates for the preparation of thienopyrrole derivatives 失效
标题翻译：制备噻吩并吡咯衍生物的方法和中间体
公开(公告)号：US20050272938A1
公开(公告)日：2005-12-08
申请号：US10528612
申请日：2003-09-29
申请人： Michael Butters , Paul Schofield , Andrew Stocker
发明人： Michael Butters , Paul Schofield , Andrew Stocker
IPC分类号： C07D333/36 , C07D495/04 , C07D497/02
CPC分类号： C07D495/04 , C07D333/36 , Y02P20/55
摘要： Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed.
摘要翻译：新工艺和中间体。制备其中R 4和R 5的式（I）化合物的方法如说明书中所定义; 和R 6是氢或保护基，该方法包括式（II）化合物的环化，其中R 4和R 5和R 5和 R 6如关于式（I）所定义，R 7为氮保护基，除去基团R 7，和此后如果需要，除去任何保护基团R 6。还描述和要求保护新型中间体及其在药物化合物形成中的用途。

9. 发明申请

US20020006921A1 Pyrrolo {2,1-b}{1,3}benzothiazepines with atypical antipsychotic activity 失效
标题翻译：具有非典型抗精神病活性的吡咯并{2,1-b} {1,3}苯并硫氮杂
公开(公告)号：US20020006921A1
公开(公告)日：2002-01-17
申请号：US09769740
申请日：2001-01-26
发明人： Giuseppe Campiani , Vito Nacci , Patrizia Minetti , Maria Assunta Di Cesare
IPC分类号： A61K031/554 , C07D497/02
CPC分类号： C07D513/04
摘要： Polycondensated heterocycles with a pyrrolenull2,1-bnullnull1,3nullbenzothiazepine structure of the following formula (I) 1 where the groups are defined as in the description are disclosed. As compared to known antipsychotic agents, these compounds present substantial activity associated with a simultaneous reduction in unwanted extrapyramidal symptoms. These compounds can be formulated in pharmaceutical compositions for the treatment of psychoses such as, for example, schizophrenia.
摘要翻译：公开了具有如描述中定义的基团的下式（I）的吡咯[2,1-b] [1,3]苯并硫氮杂结构的缩聚杂环。与已知的抗精神病药相比，这些化合物具有与同时减少不需要的锥体外系症状相关的显着活性。这些化合物可以配制在用于治疗精神病例如精神分裂症的药物组合物中。

10. 发明授权

US4127667A Substituted thiopyrano(4,3-b)pyrans 失效
标题翻译：取代的噻喃（4,3-b）吡喃
公开(公告)号：US4127667A
公开(公告)日：1978-11-28
申请号：US893722
申请日：1978-04-05
申请人： George C. Rovnyak
发明人： George C. Rovnyak
IPC分类号： C07D495/04 , A61K31/335 , A61K31/38 , C07D493/02 , C07D497/02
CPC分类号： C07D495/04 , Y10S514/825
摘要： 3,4,7,8-Tetahydro-2H,5H-thiopyrano[4,3-b]pyrans of the structure ##STR1## are provided wherein X is O, S or SO.sub.2, R is hydrogen, halogen, lower alkyl, lower alkoxy, cyano or trifluoromethyl, and R' is carbethoxy, carboxy, alkali metal carboxylate and cyano. These compounds are useful as antiinflammatory agents and anti-hypertensive agents.
摘要翻译：提供结构为“IMAGE”的3,4,7,8-二氢-2H，5H-噻喃并[4,3-b]吡喃，其中X为O，S或SO 2，R为氢，卤素，低级烷基，低级烷氧基，氰基或三氟甲基，R'是乙酯基，羧基，碱金属羧酸盐和氰基。这些化合物可用作抗炎剂和抗高血压药。

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