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1. 发明申请

WO2020156571A1 一种哒嗪衍生物及其制备方法和医药用途审中-公开
公开(公告)号：WO2020156571A1
公开(公告)日：2020-08-06
申请号：PCT/CN2020/074212
申请日：2020-02-03
申请人：杭州华东医药集团新药研究院有限公司 , 殷建明
发明人：殷建明 , 吕裕斌 , 李邦良
IPC分类号： C07D237/02 , C07D401/04 , C07D403/04 , C07C235/60 , A61K31/50 , A61P9/00
摘要：提供一种式(I)所示的哒嗪衍生物，及在制备预防和/或治疗与HIF调节有关的适应症的药物中的用途。所述哒嗪衍生物是理想的高效HIF-PHD抑制剂，可用于治疗或预防与HIF调节有关的病症或疾病，例如贫血和缺血。

2. 发明申请

WO0183458A3 ASYMMETRIC SYNTHESIS OF PIPERAZIC ACID AND DERIVATIVES THEREOF 审中-公开
标题翻译：不对称合成其酸及其衍生物
公开(公告)号：WO0183458A3
公开(公告)日：2002-05-23
申请号：PCT/US0113330
申请日：2001-04-25
申请人： VERTEX PHARMA , ROBIDOUX ANDREA , SERAFINI SIRO , DIETERICH PETRA , LEONARDI STEPHANIA , STIBBARD JOHN
发明人： ROBIDOUX ANDREA , SERAFINI SIRO , DIETERICH PETRA , LEONARDI STEPHANIA , STIBBARD JOHN
IPC分类号： C07D237/02 , C07D237/04 , C07D487/04
CPC分类号： C07D487/04 , C07D237/04
摘要： This invention provides a short, asymmetric synthesis of piperazic acid and derivatives thereof, whereby either the (3S)- or (3R)-enantiomeric form may be obtained with high optical purity. (3S)-piperazic acid is derived from D-glutamic acid through an (R)-2, 5-dihydroxyvalerate ester intermediate. After the hydroxy groups are converted to suitable leaving groups,such as mesylates, the ester is treated with a bis-protected hydrazine to provide the desired (3S)-piperazic acid derivative. The (3R) enantiomer of piperazic acid may be similarly obtained starting with L-glutamic acid. The method may also be used to obtain piperazic acid derivatives that have moderate optical purity or are racemic. By this method, piperazic acid derivatives may be obtained that are useful as intermediates for pharmacologically active compounds. For example, certain intermediates of this invention are useful for preparing caspase inhibitors, particularly inhibitors of ICE, through additional steps known in the art.
摘要翻译：本发明提供哌嗪酸及其衍生物的短的不对称合成，由此可以以高光学纯度获得（3S） - 或（3R） - 对映体形式。（3S） - 哌嗪酸通过（R）-2,5-二羟基戊酸酯中间体衍生自D-谷氨酸。将羟基转化为合适的离去基团（如甲磺酸酯）后，用双 - 保护的肼处理酯，得到所需的（3S） - 哌嗪酸衍生物。哌嗪酸的（3R）对映异构体可以从L-谷氨酸开始类似地获得。该方法也可用于获得具有中等光学纯度或外消旋的哌嗪酸衍生物。通过该方法，可以得到可用作药理活性化合物的中间体的哌嗪酸衍生物。例如，通过本领域已知的其它步骤，本发明的某些中间体可用于制备胱天蛋白酶抑制剂，特别是ICE的抑制剂。

3. 发明申请

WO0068190A3 1-ALKOXY AND 1-ACYLOXY SUBSTITUTED CYCLOHEX-1-ENE COMPOUNDS AND SULFUR AND 1-ALKOXYCARBONYL ANALOGS HAVING RETINOID-LIKE BIOLOGICAL ACTIVITY 审中-公开
标题翻译： 1-烷氧基和1-乙酰氧基取代的环己基-1-环己酮化合物和具有类似生物活性的硫酸和1-烷氧羰基类似物
公开(公告)号：WO0068190A3
公开(公告)日：2001-01-18
申请号：PCT/US0011975
申请日：2000-05-03
申请人： ALLERGAN SALES INC
发明人： BEARD RICHARD L , COLON DIANA F , CHANDRARATNA ROSHANTHA A
IPC分类号： C07C69/76 , C07C69/78 , C07C327/36 , C07C327/48 , C07C403/00 , C07D213/00 , C07D237/02 , C07D333/10 , C07F7/08 , C07F7/18 , C07C403/20 , C07C403/18 , C07C403/22
CPC分类号： C07C403/02 , C07C69/76 , C07C2601/16 , C07F7/0812 , C07F7/0818 , C07F7/1852 , C07F7/1856
摘要： Compounds of Formula (1) and Formula (2) where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.
摘要翻译：符号具有本说明书中定义的含义的式（1）和式（2）的化合物具有类视黄醇，维生素A拮抗剂或类视黄醇负性激素，如生物活性。

4. 发明申请

WO99041230A1 PROCESSES AND INTERMEDIATES USEFUL TO MAKE ANTIFOLATES 审中-公开
标题翻译：使用过程和中间体有助于制备抗体
公开(公告)号：WO99041230A1
公开(公告)日：1999-08-19
申请号：PCT/US1999/001689
申请日：1999-01-27
IPC分类号： C07D333/40 , A61K31/519 , A61P35/00 , C07D275/02 , C07D307/68 , C07D333/38 , C07D471/04 , C07C255/00 , C07D207/02 , C07D211/04 , C07D213/02 , C07D231/02 , C07D231/04 , C07D231/06 , C07D231/10 , C07D233/02 , C07D233/04 , C07D233/54 , C07D237/02 , C07D237/04 , C07D237/06 , C07D239/02 , C07D239/04 , C07D239/06 , C07D239/20 , C07D239/24 , C07D241/02 , C07D241/06 , C07D241/10 , C07D261/02 , C07D263/02 , C07D265/02 , C07D265/04 , C07D265/28 , C07D277/02 , C07D279/02 , C07D279/04 , C07D279/10 , C07D307/02 , C07D333/02 , C07D405/14 , C07D409/14 , C07D413/02 , C07D417/02 , C07D471/02
CPC分类号： C07D471/04 , C07D333/38 , Y02P20/55
摘要： The present invention concerns intermediates, and processes directed to and from those intermediates, to a series of pyrimidine derivatives of formula (V), which are intermediates to useful antifolate compounds or are themselves useful antifolate compounds.
摘要翻译：本发明涉及涉及中间体和从这些中间体引入的一系列式（Ⅴ）嘧啶衍生物的方法，它们是有用的抗叶酸化合物的中间体，或本身是有用的抗叶酸化合物。

5. 发明申请

WO98048799A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO98048799A1
公开(公告)日：1998-11-05
申请号：PCT/US1998/008740
申请日：1998-04-29
IPC分类号： C12N9/50 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/4375 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/4725 , A61K31/5377 , A61K38/00 , A61P1/02 , A61P19/00 , A61P19/02 , A61P43/00 , C07D233/90 , C07D263/34 , C07D277/20 , C07D277/56 , C07D401/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07K5/078 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/495 , A61K31/50 , A61K31/505 , A61K31/53 , A61K31/555 , C07D231/04 , C07D231/06 , C07D231/10 , C07D233/02 , C07D233/04 , C07D233/54 , C07D233/96 , C07D237/00 , C07D237/02 , C07D239/02 , C07D241/02 , C07D249/08 , C07D251/00 , C07D253/00 , C07D257/08 , C07D257/12 , C07D261/04 , C07D261/08 , C07D263/04 , C07D263/08 , C07D263/30 , C07D271/06 , C07D271/10 , C07D273/01 , C07D275/02 , C07D277/04 , C07D277/08 , C07D285/00 , C07D285/08 , C07D285/12 , C07D291/04 , C07D403/02 , C07D403/04 , C07D403/14 , C07D405/02 , C07D405/14 , C07D407/02 , C07D407/14 , C07D409/02 , C07D409/14 , C07D411/02 , C07D411/14 , C07D413/02 , C07D417/02 , C07D419/02 , C07D419/14
CPC分类号： C07D417/12 , C07D277/56 , C07D417/14 , C07D471/04 , C07K5/06139
摘要： The present invention provides compounds of formula (I) which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia or malignancy; and metabolic bone disease therewith.
摘要翻译：本发明提供抑制蛋白酶（包括组织蛋白酶K），这种化合物的药物组合物的式（I）化合物，以及用于治疗过度骨丢失或软骨或基质降解（包括骨质疏松症）的疾病的方法。牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特病高钙血症或恶性肿瘤; 和代谢性骨病。

6. 发明申请

WO2022150756A1 PROCESS FOR THE PREPARATION OF HIGH PURITY LEVOSIMENDAN 审中-公开
公开(公告)号：WO2022150756A1
公开(公告)日：2022-07-14
申请号：PCT/US2022/011965
申请日：2022-01-11
申请人： NAVINTA, LLC
发明人： BHATT, Chiragkumar Anilkumar , PANDYA, Keyurkumar Amrutla , PARMAR, Pankaj Vasudev , JEYAKUMAR, John Muthiah Raja
IPC分类号： A61K31/495 , A61K31/50 , C07D237/02 , C07D237/04 , C07D237/06
摘要： An improved process for the preparation of high purity Levosimendan includes treatment of Levosimendan crude with an organic acid, adding an organic acid to precipitate Levosimendan and isolating pure Levosimendan from the precipitate. Levosimendan obtained by the improved process is pharmaceutically acceptable with no impurity higher than 0.2 percent.

7. 发明申请

WO2022121868A1 含酰胺基和杂环烷基的TYK2抑制剂化合物审中-公开
公开(公告)号：WO2022121868A1
公开(公告)日：2022-06-16
申请号：PCT/CN2021/135912
申请日：2021-12-07
申请人：正大天晴药业集团股份有限公司 CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD. [CN]/[CN]
发明人：刘飞 LIU, Fei , 张健青 ZHANG, Jianqing , 施伟 SHI, Wei , 王宇冰 WANG, Yubing , 杨列超 YANG, Liechao
IPC分类号： C07D405/12 , C07D403/12 , C07D413/12 , C07D401/12 , C07D237/02 , A61P29/00 , A61P37/06 , A61K31/501
摘要：一种含酰胺基和杂环烷基的TYK2抑制剂化合物及其制备方法，并涉及其在制备治疗或预防TYK2相关疾病的药物中的用途。

8. 发明申请

WO2014158943A1 TYROSINASE INHIBITORS 审中-公开
公开(公告)号：WO2014158943A1
公开(公告)日：2014-10-02
申请号：PCT/US2014/021020
申请日：2014-03-06
申请人： AVON PRODUCTS, INC
发明人： HU, Hong , YIM, Sunghan , SANTHANAM, Uma , LYGA, John W.
IPC分类号： A61K31/50 , A61K31/535 , C07D237/02
CPC分类号： C07D513/04 , A61K8/49 , A61K8/494 , A61K8/4946 , A61K8/496 , A61K8/4966 , A61K31/4196 , A61K31/4245 , A61K31/429 , A61K31/501 , A61K31/53 , A61K2800/75 , A61K2800/782 , A61Q19/00 , A61Q19/007 , A61Q19/02 , A61Q19/08 , C07D249/12 , C07D403/04 , C07D409/04 , C07D413/04 , C07D487/04
摘要： The compositions and methods of described herein comprise novel ingredients effective to reduce unwanted pigmentation, such as skin discoloration, freckles, age spots, liver spots, sun damage, tans, pigmented acne marks, scars, pigmented birthmarks, hyperpigmentation, post-inflammatory hyperpigmentation, post-injury hyperpigmentation, melasma, cholasma, after-burn scar, nail stain, yellowing of skin, dark circles under eyes, and the like. The composition may include additional ingredients accordingly for a colored cosmetic, moisturizer, cleanser, toner, and the like.

9. 发明申请

WO2014150114A1 SUBSTITUTED PYRIDIZINONE DERIVATIVES AS PDE10 INHIBITORS 审中-公开
标题翻译：取代的吡啶酮衍生物作为PDE10抑制剂
公开(公告)号：WO2014150114A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/022266
申请日：2014-03-11
申请人： MERCK SHARP & DOHME CORP. , KUDUK, Scott, D. , MCCOMAS, Casey, C. , REGER, Thoma, S. , QI, Changhe
发明人： KUDUK, Scott, D. , MCCOMAS, Casey, C. , REGER, Thoma, S. , QI, Changhe
IPC分类号： A61K31/501 , C07D237/02
CPC分类号： C07D417/14 , A61K31/50 , A61K31/501 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D471/04 , A61K2300/00
摘要： The present invention is directed to substituted pyridizinone compounds of formula I which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译：本发明涉及可用作治疗与磷酸二酯酶10（PDE10）相关的中枢神经系统疾病的治疗剂的式I的取代吡啶嗪酮化合物。本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿氏病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。

10. 发明申请

WO2004003102A3 POLYMERIZABLE, LUMINESCENT COMPOUNDS AND MIXTURES, LUMINESCENT POLYMER MATERIALS AND THEIR USE 审中-公开
标题翻译：可聚合，发光化合物和混合物，发光聚合物材料及其用途
公开(公告)号：WO2004003102A3
公开(公告)日：2004-08-26
申请号：PCT/EP0306450
申请日：2003-06-18
申请人： MERCK PATENT GMBH , POETSCH EIKE , JACOB THOMAS , SERRANO JOSE , PINOL MILAGROS , GIMENEZ RAQUEL , STUMPE JOACHIM , FISCHER THOMAS , ROSENHAUER REGINA , SCHULZ BURKHARD
发明人： POETSCH EIKE , JACOB THOMAS , SERRANO JOSE , PINOL MILAGROS , GIMENEZ RAQUEL , STUMPE JOACHIM , FISCHER THOMAS , ROSENHAUER REGINA , SCHULZ BURKHARD
IPC分类号： H01L51/50 , C07C43/23 , C07C69/54 , C07C69/734 , C07C69/92 , C07C219/08 , C07C235/56 , C07C255/54 , C07C255/65 , C07D213/06 , C07D271/10 , C07D271/107 , C07D305/06 , C07D405/12 , C08F20/30 , C08G65/04 , C08G73/06 , C08G73/08 , C09K11/06 , C09K19/04 , H01L51/00 , H01L51/30 , H05B33/14 , C07C15/28 , C07D237/02 , C07D271/06 , C08F38/02 , C08G61/02 , C09K19/00 , H01L51/20
CPC分类号： H01L51/004 , C07D213/06 , C07D271/107 , C08G73/0616 , C08G73/08 , C09K11/06 , C09K19/0403 , C09K2019/0444 , C09K2211/1007 , C09K2211/1044 , C09K2211/1048 , C09K2211/1408 , C09K2211/1416 , C09K2211/1425 , C09K2211/1466 , C09K2211/1475 , H01L51/0035 , H01L51/0038 , H01L51/0052 , H01L51/007 , H01L51/5012 , H05B33/14
摘要： The invention relates to new polymerizable, luminescent compounds of formula I wherein R , R , Q and L have the meanings given in claim 1. Furthermore the invention relates to polymerizable mixtures containing compounds according to the invention and preferably at least one polymerizable mesogenic compound. Polymer materials obtainable by polymerizing such mixtures are also described. These compounds, mixtures and materials show advantageous photoluminescent and/or electroluminescent properties and may be used in light emitting devices and optical- or electrooptical display elements.
摘要翻译：本发明涉及式I的新型可聚合的发光化合物，其中R 1，R 2，Q和L 1具有权利要求1中给出的含义。此外，本发明涉及含有根据本发明的化合物并且优选至少一种可聚合介晶化合物。还描述了通过聚合这种混合物可获得的聚合物材料。这些化合物，混合物和材料显示出有利的光致发光和/或电致发光性质，并且可以用于发光装置和光学或电光学显示元件中。

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