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1. 发明申请

WO2010102212A3 NEUROTROPHIN MIMETICS AND USES THEREOF 审中-公开
标题翻译：神经营养因子及其用途
公开(公告)号：WO2010102212A3
公开(公告)日：2011-03-31
申请号：PCT/US2010026372
申请日：2010-03-05
申请人： UNIV NORTH CAROLINA , LONGO FRANK M
发明人： LONGO FRANK M
IPC分类号： C07D265/06 , C07D403/04 , C07D473/02
CPC分类号： C07D295/125 , C07D295/135 , C07D413/12 , C07D473/08
摘要： The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.
摘要翻译：本申请涉及新型神经营养因子模拟物的化合物。本申请还公开了通过施用有效量的这些化合物治疗与p75表达相关的紊乱，例如哺乳动物表达p75的细胞的降解或功能障碍。

2. 发明申请

WO2008140859A1 DEUTERATED VENLAFAXINES AND 0-DESMETYLVENLAFAXINES WITH SEROTONINERGIC AND / OR NOREPINEPHRINERGIC ACTIVITY 审中-公开
标题翻译：去饱和的维生素和0-DESMETYLVENLAFAXINES具有丝氨酸和/或肾上腺素活性
公开(公告)号：WO2008140859A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/056780
申请日：2008-03-13
申请人： AUSPEX PHARMACEUTICALS, INC. , GANT, Thomas, G. , SEPEHR, Sarshar , WOO, Soon, Hyung
发明人： GANT, Thomas, G. , SEPEHR, Sarshar , WOO, Soon, Hyung
IPC分类号： C07C217/74 , C07C215/64 , C07D265/06 , C07B59/00
CPC分类号： C07C211/64 , C07B59/00 , C07B2200/05 , C07B2200/07 , C07B2200/13 , C07C215/64 , C07C217/74 , C07C2601/14 , C07D265/16
摘要： Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described.
摘要翻译：用于治疗和/或治疗精神病症，焦虑障碍，广泛性焦虑症，抑郁症，创伤后应激障碍，强迫症的单胺神经递质及其药学上可接受的盐和前药的新型抑制剂的化学合成和医学用途，强迫症，恐慌症，热潮红，老年痴呆，偏头痛，肝肺综合征，慢性疼痛，伤害性疼痛，神经性疼痛，疼痛性糖尿病性视网膜病变，双相抑郁症，阻塞性睡眠呼吸暂停，精神疾病，经前焦虑症，社交恐惧症，社交焦虑症，尿失禁，厌食症，神经性贪食症，肥胖症，缺血，头部损伤，脑细胞中的钙超载，药物依赖，注意缺陷多动障碍，纤维肌痛，肠易激综合征和/或早泄。

3. 发明申请

WO2007092961A3 ANTIBACTERIAL AGENTS 审中-公开
标题翻译：抗菌剂
公开(公告)号：WO2007092961A3
公开(公告)日：2008-07-17
申请号：PCT/US2007061943
申请日：2007-02-09
申请人： UNIV NEW ORLEANS RES & TECHNOL , WANG GUIJUN
发明人： WANG GUIJUN
IPC分类号： C07D263/06 , A61K31/538 , C07D265/06 , C07D413/12
CPC分类号： C07D413/12 , C07D263/06 , C07D265/06
摘要： This invention provides compositions which are l,3-oxazinan-2-one compounds of formulae (I) and (II), and oxazolidinone compounds of formula (III): wherein R is a hydrocarbyl group, a heterocyclic group, a hydrocarbyl group having at least one substituent, or a heterocyclic group having at least one hydrocarbyl substituent, wherein the substituent on the hydrocarbyl group or heterocyclic group is selected from the group consisting of a heterocyclic group, an azo group, a cyano group, a nitro group, a fluoro group, a chloro group, abromo group, an alkoxy group having up to 15 carbon atoms, and a hydrocarbyl group having up to 15 carbon atoms; and R' and R" are each independently hydrogen, an alkyl group, an aryl group, a methylaryl group, a carbonyl group, a hydrocarbylamido group, a sulfonyl group, a sulfonamoyl group, a heterocyclic group, a heterocyclic group having at least one substituent, or an aryl group or methylaryl group having at least one substituent, where the substituent on the heterocyclic group, aryl group, or methylaryl group is selected from the group consisting of a heterocyclic group, an azo group, a cyano group, a nitro group, a fluoro group, a chloro group, a bromo group, an alkoxy group having up to 15 carbon atoms, and a hydrocarbyl group having up to 15 carbon atoms. For the oxazolidinone compound of formula (HI), there is a proviso that when one of R' or R" is a (3-fluoro)-(4-morpholinyl)- phenyl group, the other of R' or R" is not an acetamido group.
摘要翻译：本发明提供了式（I）和（II）的1,3-恶嗪烷-2-酮化合物和式（III）的恶唑烷酮化合物的组合物：其中R是烃基，杂环基，具有至少一个取代基或具有至少一个烃基取代基的杂环基，其中烃基或杂环基上的取代基选自杂环基，偶氮基，氰基，硝基，氟基，氯基，溴代基，具有至多15个碳原子的烷氧基和至多15个碳原子的烃基; R'和R“各自独立地为氢，烷基，芳基，甲基芳基，羰基，烃基酰氨基，磺酰基，氨磺酰基，杂环基，具有至少一个取代基或具有至少一个取代基的芳基或甲基芳基，其中杂环基，芳基或甲基芳基上的取代基选自杂环基，偶氮基，氰基，硝基基团，氟基团，氯基团，溴基团，具有至多15个碳原子的烷氧基和具有至多15个碳原子的烃基，对于式（III）的恶唑烷酮化合物，条件是当R'或R“中的一个为（3-氟） - （4-吗啉基） - 苯基时，R'或R”中的另一个不是乙酰氨基。

4. 发明申请

WO02100844A3 HIV PROTEASE INHIBITORS, COMPOSITIONS CONTAINING THE SAME, THEIR PHARMACEUTICAL USES AND MATERIALS FOR THEIR SYNTHESIS 审中-公开
标题翻译： HIV蛋白酶抑制剂，含有它们的组合物，它们的药物用途和材料合成
公开(公告)号：WO02100844A3
公开(公告)日：2003-03-06
申请号：PCT/US0218717
申请日：2002-06-11
申请人： AGOURON PHARMA
发明人： CANON-KOCH STACIE S , ALEXANDER THERESE N , BARVIAN MARK , BOLTON GARY , BOYER FREDRICK E , BURKE BENJAMIN J , HOLLER TOD , JEWELL TANYA M , PRASAD JOSYULA VARA , KUCERA DAVID J , LINTON MARIA A , MACHAK JEFF , MITCHELL LENNERT J , MURPHY SEAN T , REICH SIEGFRIED H , SKALITZKY DONALD J , TATLOCK JOHN H , VARNEY MICHAEL D , VIRGIL SCOTT C , WEBBER STEPHEN E , WORLAND STEPHEN T , MELNICK MICHAEL
IPC分类号： C07D277/04 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/421 , A61K31/422 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/472 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K38/04 , A61K45/00 , A61P31/00 , A61P31/12 , A61P31/18 , A61P37/02 , A61P43/00 , C07D207/09 , C07D207/16 , C07D207/24 , C07D209/52 , C07D213/38 , C07D217/26 , C07D231/12 , C07D263/04 , C07D263/06 , C07D277/00 , C07D277/06 , C07D277/20 , C07D277/28 , C07D277/32 , C07D277/38 , C07D277/60 , C07D295/13 , C07D307/52 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/08 , C07K5/04 , C07D211/60 , C07D265/06 , C07D401/12
CPC分类号： C07D231/12 , A61K31/426 , A61K31/427 , C07D207/09 , C07D207/16 , C07D213/38 , C07D217/26 , C07D277/06 , C07D277/60 , C07D295/13 , C07D307/52 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/08
摘要： Compounds of Formula (I), where the formula variables are as defined herein, are disclosed that advantageously inhibit or block the biological activity of the HIV protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with the HIV virus. Intermediates and synthetic methods for preparing such compounds are also described.
摘要翻译：公开了式（I）化合物，其中式变量如本文所定义，其有利地抑制或阻断HIV蛋白酶的生物活性。这些化合物以及含有这些化合物的药物组合物可用于治疗感染HIV病毒的患者或宿主。还描述了制备这些化合物的中间体和合成方法。

5. 发明申请

WO00049002A1 PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF 1,3-OXAZIN-6-ONES AND URACILS 审中-公开
标题翻译：制备1,3-氧化物-6-酮和尿素的方法和中间体
公开(公告)号：WO00049002A1
公开(公告)日：2000-08-24
申请号：PCT/US2000/003731
申请日：2000-02-14
IPC分类号： C07B61/00 , C07C273/18 , C07C275/20 , C07D239/54 , C07D261/20 , C07D265/06 , C07D275/04 , C07D295/215 , C07D413/04 , C07D417/04 , C07D207/02 , C07D263/44
CPC分类号： C07D239/54 , C07C275/20 , C07D265/06 , C07D295/215 , C07D413/04 , C07D417/04
摘要： An improved process and intermediate compounds (N) for the preparation of 2-(N,N-disubstituted)amino-4-(perfluoroalkyl)-1,3-oxazin-6-one compounds having structural formula (I) and an improved process for the preparation of 6-(perfluoroalkyl)uracil compounds having structural formula (V).
摘要翻译：用于制备具有结构式（I）的2-（N，N-二取代的）氨基-4-（全氟烷基）-1,3-恶嗪-6-酮化合物的改进方法和中间体化合物（N）用于制备具有结构式（V）的6-（全氟烷基）尿嘧啶化合物。

6. 发明申请

WO99007697A1 SUBSTITUTED 4-BENZOYL-PYRAZOLES 审中-公开
标题翻译：取代的4- Benzoylpyrazoles
公开(公告)号：WO99007697A1
公开(公告)日：1999-02-18
申请号：PCT/EP1998/004481
申请日：1998-07-20
IPC分类号： C07D231/20 , A01N43/08 , A01N43/40 , A01N43/56 , A01N43/74 , C07D213/30 , C07D261/08 , C07D263/32 , C07D265/06 , C07D307/42 , C07D307/58 , C07D401/10 , C07D405/10 , C07D413/10 , C07D417/10
CPC分类号： C07D213/30 , C07D261/08 , C07D307/42 , C07D307/58 , C07D401/10 , C07D405/10 , C07D413/10
摘要： The invention relates to 4-benzoyl-pyrazoles of formula (I), in which the substituents R , R and Q and the groups X and Het have the meaning as given in the description. The invention also relates to their salts suited for use in agriculture, the methods and intermediary products required for producing compounds of formula (I), the products containing such compounds and salts, as well as the use of compounds of formula (I) and products containing them for destroying adventive plants.
摘要翻译：式（I），4-苯甲酰基吡唑，其中所述取代基R <1>，R <2>，Q和基团X <1>和Het具有说明书中给出的含义，及其可农用盐，流程和式（I）的化合物的制备中间体，是指含有它们，并使用式（I）和组合物的化合物的包含它们的用于防治有害植物。

7. 发明申请

WO2022127704A1 羧基环内酸酐的制备方法审中-公开
公开(公告)号：WO2022127704A1
公开(公告)日：2022-06-23
申请号：PCT/CN2021/137111
申请日：2021-12-10
申请人：北京大学
发明人：吕华 , 田子由
IPC分类号： C07D265/06 , C07D263/44 , C07D273/00 , C07D317/36 , C08G69/10 , C08G69/04
摘要：本发明公开了羧基环内酸酐的制备方法及制备产物。式(II)化合物的制备方法，该方法包括将式(I)的化合物与环化试剂反应以生成式(II)化合物和酸，并且使用环氧化合物作为除酸剂的步骤。本发明是一个新的羧基环内酸酐合成方法，成本低廉，对实验所需试剂、场所及设备要求低，条件温和，底物适用范围广，官能团耐受度高，合成路线可回收部分溶剂与其他高附加值副产品，废液排放少，易放大，具有极高的工业及学术价值，可极大推动聚氨基酸、聚羟基酸(聚酯)、聚巯基酸(聚硫酯)等产品的迅速大规模生产及应用。

8. 发明申请

WO2016020732A1 MODULATORS OF CASPASE-6 审中-公开
标题翻译： CASPASE-6的调节剂
公开(公告)号：WO2016020732A1
公开(公告)日：2016-02-11
申请号：PCT/IB2015/000144
申请日：2015-02-14
申请人： THE UNIVERSITY OF BRITISH COLUMBIA , UNIVERSITÄT HAMBURG
发明人： KHANKISCHPUR, Medhi, Mike , PETINA, Olga , GEFFKEN, Detlef , ERNHOEFER, Dagmar , HAYDEN, Michael
IPC分类号： A61K31/535 , A61K31/165 , A61P25/14 , A61P25/28 , C07C251/28 , C07D265/06
CPC分类号： A61K31/165 , A61K31/535 , A61K45/06 , C07C251/28 , A61K2300/00
摘要： The current application relates to a pharmaceutical composition for the treatment or amelioration of a neurological disease, wherein the composition comprises a therapeutically effective amount of a caspase-6 inhibitor which is an arylpropynamide derivative. The composition can be formulated for oral or topical administration, subcutaneous, intravenous, or intramuscular injection, infusion, inhalation, or intrthecal injection.
摘要翻译：本申请涉及用于治疗或改善神经疾病的药物组合物，其中所述组合物包含治疗有效量的作为芳基丙酰胺衍生物的胱天蛋白酶-6抑制剂。组合物可以配制用于口服或局部给药，皮下，静脉内或肌内注射，输注，吸入或鞘内注射。

9. 发明申请

WO2010028051A3 SUBSTITUTED HETEROCYCLIC MERCAPTOSULFONAMIDE METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：取代的杂环羧甲基磺酰胺金属蛋白酶抑制剂
公开(公告)号：WO2010028051A3
公开(公告)日：2010-07-08
申请号：PCT/US2009055742
申请日：2009-09-02
申请人： UNIV FLORIDA STATE RES FOUND , SCHWARTZ MARTIN A , JIN YONGHAO , SANG QING-XIANG AMY
发明人： SCHWARTZ MARTIN A , JIN YONGHAO , SANG QING-XIANG AMY
IPC分类号： C07D207/327 , A61K31/415 , A61P35/00 , C07D207/16 , C07D237/02 , C07D237/12 , C07D265/06
CPC分类号： C07D207/14 , A61K31/415 , C07D403/12
摘要： The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions.
摘要翻译：本发明一般涉及取代的杂环巯基磺酰胺化合物，前体和衍生物，以及制备这些化合物和包含这些化合物的药物组合物的方法。这些化合物被设计为基质金属蛋白酶（MMP）的有效选择性抑制剂，包括例如明胶酶，胶原酶，基质溶素，金属弹性蛋白酶，溶基质素和膜型1基质金属蛋白酶。这些抑制剂可用于控制MMPs被认为起重要作用的生理和病理过程和疾病状态。

10. 发明申请

WO2010028051A2 SUBSTITUTED HETEROCYCLIC MERCAPTOSULFONAMIDE METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：取代的杂环磷酰胺金属蛋白酶抑制剂
公开(公告)号：WO2010028051A2
公开(公告)日：2010-03-11
申请号：PCT/US2009/055742
申请日：2009-09-02
申请人： FLORIDA STATE UNIVERSITY RESEARCH FOUNDATION, INC. , SCHWARTZ, Martin A. , JIN, Yonghao , SANG, Qing-Xiang (Amy)
发明人： SCHWARTZ, Martin A. , JIN, Yonghao , SANG, Qing-Xiang (Amy)
IPC分类号： C07D207/327 , C07D207/16 , C07D265/06 , C07D237/02 , C07D237/12 , A61K31/415 , A61P35/00
CPC分类号： C07D207/14 , A61K31/415 , C07D403/12
摘要： The present invention generally relates to substituted heterocyclic mercaptosulfonamide compounds, precursors, and derivatives as well as methods for the preparation of and pharmaceutical compositions comprising these compounds. These compounds are designed to be potent selective inhibitors of matrix metalloproteinases (MMPs), including, for example, gelatinases, collagenases, matrilysins, metalloelastase, stromelysin, and membrane-type 1 matrix metalloproteinase. These inhibitors may be used for the control of physiological and pathological processes and disease conditions in which MMPs are believed to play significant functions.
摘要翻译：本发明一般涉及取代的杂环巯基磺酰胺化合物，前体和衍生物以及制备包含这些化合物的药物组合物的方法。这些化合物被设计为基质金属蛋白酶（MMPs）的有效选择性抑制剂，包括例如明胶酶，胶原酶，母体溶胶蛋白，金属弹性蛋白酶，溶基质蛋白酶和膜型1基质金属蛋白酶。这些抑制剂可用于控制生理和病理过程以及MMP被认为具有重要功能的疾病状况。

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