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1. 发明申请

US20210094943A1 HETEROCYCLIC COMPOUNDS 有权
公开(公告)号：US20210094943A1
公开(公告)日：2021-04-01
申请号：US17017200
申请日：2020-09-10
申请人： Hoffmann-La Roche Inc.
发明人： Joerg BENZ , Luca GOBBI , Uwe GRETHER , Katrin GROEBKE ZBINDEN , Benoit HORNSPERGER , Carsten KROLL , Bernd KUHN , Rainer E. MARTIN , Fionn O`HARA , Bernd PUELLMANN , Hans RICHTER , Martin RITTER
IPC分类号： C07D413/12 , A61K9/20 , A61K9/48 , C07D265/28
摘要： The invention provides new heterocyclic compounds having the general formula (I) wherein A, B, L1, X, m, n, and RI to R7 are as described herein, compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds.

2. 发明申请

US20200089070A1 ELECTROCHROMIC COMPOUND, ELECTROCHROMIC COMPOSITION, AND ELECTROCHROMIC DISPLAY ELEMENT 审中-公开
公开(公告)号：US20200089070A1
公开(公告)日：2020-03-19
申请号：US16692002
申请日：2019-11-22
申请人： Satoshi YAMAMOTO , Daisuke GOTO , Toshiya SAGISAKA , Masato SHINODA , Mamiko INOUE , Fuminari KANEKO , Tohru YASHIRO
发明人： Satoshi YAMAMOTO , Daisuke GOTO , Toshiya SAGISAKA , Masato SHINODA , Mamiko INOUE , Fuminari KANEKO , Tohru YASHIRO
IPC分类号： G02F1/15 , C07D265/38 , G02F1/1516 , C07D265/28 , G09F9/30 , C09K9/02 , C08F20/36
摘要： Provided is an electrochromic compound represented by the following general formula (I) or (II) where R1 to R13 are each independently a hydrogen atom, a halogen atom, a monovalent organic group, or a polymerizable functional group, and at least one of the R1 to the R13 is a polymerizable functional group.

3. 发明授权

US08822459B2 Compound containing basic group and use thereof 有权
标题翻译：含有碱性基团的化合物及其用途
公开(公告)号：US08822459B2
公开(公告)日：2014-09-02
申请号：US13027957
申请日：2011-02-15
申请人： Masaya Kokubo , Yoshikazu Takaoka , Shiro Shibayama
发明人： Masaya Kokubo , Yoshikazu Takaoka , Shiro Shibayama
IPC分类号： A61K31/535 , C07D265/28 , C07D471/10 , C07D233/90 , C07D401/14 , C07D487/10 , C07D233/16 , C07D233/84 , C07D403/12 , C07D403/14
CPC分类号： C07D471/10 , C07D233/16 , C07D233/84 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D487/10
摘要： The present invention relates to a compound represented by formula (I-0): wherein symbols in formula have the same meanings as described in the present specification, a salt thereof, an N-oxide thereof or a solvate thereof or a prodrug thereof, and medical use thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
摘要翻译：本发明涉及由式（I-0）表示的化合物：其中式中的符号与本说明书中所述的相同含义，其盐，其N-氧化物或其溶剂合物或其前药，以及医疗用途。本发明的化合物对CXCR4具有拮抗作用，因此可用作CXCR4介导的疾病的预防和/或治疗剂，例如炎性和免疫疾病（例如类风湿性关节炎，关节炎，视网膜病变，肺纤维化，移植器官排斥反应等），过敏性疾病，感染（例如人类免疫缺陷病毒感染，获得性免疫缺陷综合征等），精神神经病，脑疾病，心血管疾病，代谢疾病和癌性疾病（例如癌症，癌转移等）或再生治疗剂。

4. 发明授权

US08399459B2 1,4 oxazines as BACE1 and/or BACE2 inhibitors 失效
标题翻译： 1,4个恶嗪作为BACE1和/或BACE2抑制剂
公开(公告)号：US08399459B2
公开(公告)日：2013-03-19
申请号：US13357640
申请日：2012-01-25
申请人： Matteo Andreini , Emanuele Gabellieri , Robert Narquizian , Massimiliano Travagli , Wolfgang Wostl
发明人： Matteo Andreini , Emanuele Gabellieri , Robert Narquizian , Massimiliano Travagli , Wolfgang Wostl
IPC分类号： A61K31/535 , C07D265/28
CPC分类号： C07D413/10 , C07D265/30
摘要： The present invention provides 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
摘要翻译：本发明提供了具有BACE1和/或BACE2抑制活性的1,4型恶唑酸，其制备方法，含有它们的药物组合物及其作为治疗活性物质的用途。本发明的活性化合物可用于例如治疗和/或预防性治疗。阿尔茨海默病和2型糖尿病。

5. 发明授权

US08299065B2 Antibacterial condensed thiazoles 有权
标题翻译：抗菌缩合噻唑
公开(公告)号：US08299065B2
公开(公告)日：2012-10-30
申请号：US12747811
申请日：2008-12-12
申请人： David John Haydon , Lloyd George Czaplewski
发明人： David John Haydon , Lloyd George Czaplewski
IPC分类号： A61K31/5365 , A61K31/4427 , A61K31/4196 , A61K31/497 , A61K31/428 , A61K31/47 , A61K31/5377 , A61K31/506 , C07D417/14 , C07D417/02 , C07D265/28 , C07D241/10 , C07D277/62 , C07D401/14 , C07D265/30 , C07D241/04 , C07D239/20
CPC分类号： C07D417/04 , C07D277/82 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
摘要： Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, or —C(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N═ or —CH═Z2 is —N═ or —C(R1)═; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 5 or 6 ring atoms or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 9 or 10 ring atoms; Q1 is hydrogen, an optional substituent, or an optionally substituted carbocyclic or heterocyclic radical having 3-7 ring atoms.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C 1 -C 6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - 或-C（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基; Z1是-N =或-CH = Z2是-N =或-C（R1）=; R 1是氢，甲基，乙基，乙烯基，乙炔基，甲氧基，巯基，巯基甲基，卤素，完全或部分氟化的（C1-C2）烷基，（C1-C2-烷氧基或（C1-C2）烷硫基，硝基或腈）; R2是Q1- [Alk1] q-Q2-，其中q是0或1; Alk1是任选取代的，二价的，直链或支链的C 1 -C 6亚烷基或C 2 -C 6亚烯基或C 2 -C 6亚炔基可以含有或终止于醚（-O-），硫醚（-S-）或氨基（-NR））连接基团的基团; Q 2是具有5或6个环原子的任选取代的二价单环碳环或杂环基团，具有9或10个环原子的取代的二价双环碳环或杂环基; Q 1是氢，任选的取代基或具有3-7个环原子的任选取代的碳环或杂环基。

6. 发明授权

US08202999B2 Compounds for inflammation and immune-related uses 失效
标题翻译：用于炎症和免疫相关用途的化合物
公开(公告)号：US08202999B2
公开(公告)日：2012-06-19
申请号：US11326872
申请日：2006-01-06
申请人： Lijun Sun , Shoujun Chen , Zhi-Qiang Xia , Jun Jiang , Yu Xie , Junyi Zhang
发明人： Lijun Sun , Shoujun Chen , Zhi-Qiang Xia , Jun Jiang , Yu Xie , Junyi Zhang
IPC分类号： C07D213/02 , C07D263/02 , C07D265/28 , A61K31/415 , A61K31/433 , A61K31/455 , A61K31/537
CPC分类号： A61K31/426 , A61K31/24 , A61K31/41 , A61K31/421 , A61K31/433 , A61K31/44 , A61K31/4439 , A61K31/444 , A61K45/06 , C07C233/81 , C07D207/335 , C07D213/40 , C07D213/64 , C07D213/81 , C07D231/12 , C07D249/10 , C07D249/12 , C07D257/04 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D277/22 , C07D277/28 , C07D285/12 , C07D295/135 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
摘要翻译：本发明涉及结构式（I），（VII）和（XI）的化合物或其药学上可接受的盐，溶剂合物，包合物或前药，其中X1，X2，X3，Y，Z，L，R1，R2 ，R 3，R 18和n如本文所定义。这些化合物可用作免疫抑制剂并用于治疗和预防炎性病症，过敏性疾病和免疫疾病。

7. 发明授权

US07829702B2 Racemic separation of 2,6-trans-dimethymorpholine 有权
标题翻译：外消旋分离2,6-反式二甲基吗啉
公开(公告)号：US07829702B2
公开(公告)日：2010-11-09
申请号：US12159504
申请日：2006-12-18
申请人： Klaus Ditrich , Frank Haese
发明人： Klaus Ditrich , Frank Haese
IPC分类号： C07D265/28
CPC分类号： C07D295/027
摘要： A process for preparing optically active trans-2,6-dimethylmorpholine by (i) reacting racemic trans-2,6-dimethylmorpholine with D-mandelic acid, (ii) removing the salt formed from D-mandelic acid and one enantiomer of trans-2,6-dimethylmorpholine from the other enantiomer of trans-2,6-dimethylmorpholine and (iii) isolating the desired optically active trans-2,6-dimethylmorpholine.
摘要翻译：（i）使外消旋反式-2,6-二甲基吗啉与D-扁桃酸反应制备光学活性的反式-2,6-二甲基吗啉的方法，（ii）除去由D-扁桃酸形成的盐和反式-2,6-二甲基吗啉的一种对映异构体，由2,6-二甲基吗啉的另一个对映异构体制备2,6-二甲基吗啉，（iii）分离所需的光学活性反式-2,6-二甲基吗啉。

8. 发明申请

US20090291945A1 CYSTEINE PROTEASE INHIBITORS 审中-公开
标题翻译： CYSTEINE PROTEASE抑制剂
公开(公告)号：US20090291945A1
公开(公告)日：2009-11-26
申请号：US12419722
申请日：2009-04-07
申请人： Gen Unoki , Takashi Hayamizu , Hiroshi Eguchi , Yumiko Muroga , Toshiyuki Kaneko , Naoki Yajima
发明人： Gen Unoki , Takashi Hayamizu , Hiroshi Eguchi , Yumiko Muroga , Toshiyuki Kaneko , Naoki Yajima
IPC分类号： A61K31/54 , A61K31/535 , A61K31/445 , A61K31/165 , C07D279/12 , C07D265/28 , C07D211/60 , C07C237/02
CPC分类号： C07C255/16 , C07C237/10 , C07C237/14 , C07C237/20 , C07C237/24 , C07C259/06 , C07C317/18 , C07C317/28 , C07C317/32 , C07C323/12 , C07C323/41 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/34 , C07D211/60 , C07D211/62 , C07D213/26 , C07D213/40 , C07D231/12 , C07D231/14 , C07D233/61 , C07D265/30 , C07D295/155 , C07D295/185 , C07D317/50 , C07D401/12
摘要： To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.
摘要翻译：提供具有优异的半胱氨酸蛋白酶抑制作用的化合物，提供治疗或预防选自骨质疏松症，骨关节炎，慢性类风湿性关节炎，骨关节炎，高钙血症，癌症骨转移的疾病的药物，和骨痛。由式（1）表示的化合物或其药学上可接受的盐，或其含有与有效成分相同的药物或药物组合物。

9. 发明授权

US07507817B2 Prostaglandin prodrugs 有权
标题翻译：前列腺素前药
公开(公告)号：US07507817B2
公开(公告)日：2009-03-24
申请号：US11938902
申请日：2007-11-13
申请人： David W. Old , Vinh X. Ngo , Wha-Bin Im
发明人： David W. Old , Vinh X. Ngo , Wha-Bin Im
IPC分类号： C07D265/30 , C07D333/02 , C07D321/00 , C07D333/32 , C07D307/00 , C07D213/04 , C07D265/28 , A61K31/535 , A61K31/335 , C07C61/00 , C07C63/36
CPC分类号： C07D295/088
摘要： Novel compounds, and therapeutic methods, compositions and medicament related thereto are disclosed herein.
摘要翻译：本文公开了新颖的化合物及其相关的治疗方法，组合物和药物。

10. 发明申请

US20080139540A1 Antibacterial Agents 失效
标题翻译：抗菌剂
公开(公告)号：US20080139540A1
公开(公告)日：2008-06-12
申请号：US11814614
申请日：2006-01-24
申请人： William Henry Miller , Meagan B. Rouse , Mark Andrew Seefeld
发明人： William Henry Miller , Meagan B. Rouse , Mark Andrew Seefeld
IPC分类号： A61K31/542 , C07D279/16 , C07D265/28 , A61P31/04 , A61K31/5365
CPC分类号： C07D471/04
摘要： Naphthyridine and related derivatives useful in the treatment of bacterial infections, particularly humans, are disclosed herein.
摘要翻译：本文公开了用于治疗细菌感染，特别是人的萘吡啶和相关衍生物。

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