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1. 发明公开

EP3381925A1 DEUTERIUM-MODIFIED BRIGATINIB DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND USE THEREOF 有权转让
公开(公告)号：EP3381925A1
公开(公告)日：2018-10-03
申请号：EP16868007.2
申请日：2016-11-24
申请人： Chai Tai Tianqing Pharmaceutical Group Co., Ltd.
发明人： ZHANG, Yinsheng , LIU, Baomin , YANG, Beibei
IPC分类号： C07F9/6558 , A61K31/675 , A61P35/00
CPC分类号： C07F9/65583 , A61K31/675 , A61P35/00 , C07B59/004 , C07F9/6558
摘要： The present invention relates to the field of pharmaceutical chemistry, and relates to a deuterium-modified Brigatinib derivative, preparation method thereof, pharmaceutical composition containing the same and the uses of the deuterium-modified Brigatinib derivative and the pharmaceutical composition thereof in preparing a medicament for treating the disease mediated by anaplastic lymphoma kinase. The deuterium-modified Brigatinib derivative of the present invention has an excellent inhibitory activity on anaplastic lymphoma kinase and has better pharmacodynamic or pharmacokinetic properties relative to Brigatinib.

2. 发明公开

EP1813620A1 PHOSPHONIC ACID DERIVATIVE AND THERAPEUTIC AGENT FOR DISEASE IN WHICH HIGH PHOSPHATE LEVEL IN BLOOD PARTICIPATES 审中-公开
标题翻译：膦和治疗剂对抗疾病与血液中高磷水平有关
公开(公告)号：EP1813620A1
公开(公告)日：2007-08-01
申请号：EP05793817.7
申请日：2005-10-05
申请人： Kotobuki Pharmaceutical Co., Ltd.
发明人： TOMIYAMA, Hiroshi , YOKOTA, Masayuki , TOKUZAKI, Kazuo , TOMITA, Ryoko
IPC分类号： C07F9/38 , C07F9/6539 , C07F9/6553 , A61K31/662 , A61K31/665 , A61K31/67 , A61K31/675 , A61P43/00
CPC分类号： C07F9/6541 , C07F9/3834 , C07F9/3882 , C07F9/3891 , C07F9/591 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/6558 , C07F9/65586
摘要： This invention related to a series of new phosphonic acid derivatives having anti- hyperphosphatemia activity. (I)
[wherein: A is selected from -(CH 2 ) n -, -CO-, -(CH 2 ) n -CO-(CH 2 ) m -, -(CH 2 ) n -CS-(CH 2 ) m - or branched alkylene group. B ring and C ring are selected from benzene ring, naphthalene ring, azulene ring or, heterocycle or fused heterocycle. D is -(CH 2 ) (n+1) -, -(CH2)-O-(CH 2 ) m -, -(CH 2 )-S(O) o -(CH 2 ) m -, -CF 3 or -(CH 2 ) n -NR 10 -(CH 2 ) m - (wherein: D ring is connected with the carbon atom composing C ring.). E is selected from oxygen atom or sufur atom. P is phosphine atom. R 1 ~ R 7 (wherein R 1 and R 2 , R 4 and R 5 are joined together with neighbored carbon atom to form 5 ~ 7 membered saturated or unsaturated hydrocarbon ring, or 5 ~ 6 membered fused hetrocycle. R 1 , R 2 and R 3 are not hydrogen atom if B ring is benzene ring.) may be the same or different and are substituents. R 8 and R 9 are may be the same or different and are substituents. R 10 is alkyl group. n and m are 0-10. o is 0-2.
摘要翻译：本发明涉及一系列具有抗高磷血症活性的新的膦酸衍生物。（I）[其中：A选自 - （CH 2）N - ， - CO - ， - （CH 2）n的-CO-（CH 2）M - ， - （CH 2）（N - CS- CH 2 ）米 - 或支链亚烷基。 B环和C环都是由苯环，萘环，薁环，或杂环或稠合杂环选择。 D是 - （CH 2）（N + 1） - ， - （CH 2）-O-（CH 2）米 - ， - （CH 2）-S（O）O - （CH 2）米 - ，-CF 3 或 - （CH 2）n的-NR 10 - （CH 2）米 - （worin：D环与构成C环的碳原子连接）。 E选自氧原子或Sufur原子。 P是膦原子。的R 1〜，R 7（worin R 1和R 2，R 4和R 5与邻居碳原子连接在一起以形成5〜7元饱和或不饱和烃环，或5〜6元稠hetrocycle。R1，R2 和R 3不如果B环是苯环氢原子。）可以相同或不同，并且是取代基。 R8和R9可以相同或不同，并且是取代基。 R 10为烷基。 n和m是0-10。 o为0-2。

3. 发明公开

EP3383879A1 ANTI-BACTERIAL COMPOUNDS BASED ON AMINO-GOLD PHOSPHINE COMPLEXES 审中-公开
公开(公告)号：EP3383879A1
公开(公告)日：2018-10-10
申请号：EP16805820.4
申请日：2016-12-02
申请人： Auspherix Limited
发明人： HOLMES, Ian , NAYLOR, Alan , ALBER, Dagmar , POWELL, Jonathan Raymond , MAJOR, Meriel Ruth , NEGOITA-GIRAS, Gabriel , ALLEN, Daniel Rees , GUETZOYAN, Lucie Juliette , KING, Nigel Paul , CHAPMAN, Nicholas Andrew
IPC分类号： C07F9/50 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6503 , C07F9/6506 , C07F9/6518 , C07F9/6524 , C07F9/653 , C07F9/6533 , C07F9/6539 , C07F9/6544 , C07F9/6558 , C07F9/6568 , C07F9/6571 , A61K33/24 , A61L29/00
CPC分类号： C07F9/6571 , A61K31/675 , A61K45/06 , A61L27/54 , A61L29/16 , A61L31/16 , A61L2300/102 , A61L2300/404 , C07F9/5004 , C07F9/5728 , C07F9/58 , C07F9/59 , C07F9/65031 , C07F9/6506 , C07F9/65068 , C07F9/6518 , C07F9/6524 , C07F9/653 , C07F9/6533 , C07F9/65335 , C07F9/6539 , C07F9/6544 , C07F9/6558 , C07F9/65583 , C07F9/65686 , A61K2300/00
摘要： A compound of formula (I) for use in the prevention or treatment of a bacterial infection wherein: PX is selected from the group consisting of (P1), (P2) and (P3).

4. 发明公开

EP2791394A2 PROCESS AND CATALYST FOR THE ELECTROCHEMICAL REDUCTION OF CARBON DIOXIDE 审中-公开
标题翻译：工艺及催化剂的电化学还原二氧化碳
公开(公告)号：EP2791394A2
公开(公告)日：2014-10-22
申请号：EP12799584.3
申请日：2012-12-13
申请人： Solvay SA
发明人： MAZUR, Adam Wieslaw , NEDELEC, Jean-Yves , CACHET-VIVIER, Christine , PADMANILAYAM, Maniyan , LIEBENS, Armin T.
IPC分类号： C25B11/04 , C25B1/00 , C07F9/58 , C07F9/6503 , C07F9/6506 , C07F9/6524 , C07F9/6539 , C07F9/6558 , C07F9/6561 , C07F9/38 , C07F15/04 , C07F1/08
CPC分类号： C25B11/04 , C07F1/08 , C07F9/386 , C07F9/485 , C07F9/581 , C07F9/582 , C07F9/65032 , C07F9/65033 , C07F9/65062 , C07F9/650958 , C07F9/65121 , C07F9/6524 , C07F9/6539 , C07F9/6558 , C07F9/6561 , C07F15/045 , C25B1/00 , C25B11/0447
摘要： A process for the catalyzed electrochemical reduction of carbon dioxide wherein a metal organic framework comprising metal ions and an organic ligand is used as a catalyst and novel metal organic frameworks based on bisphosphonic acids.

5. 发明公开

EP1813620A4 PHOSPHONIC ACID DERIVATIVE AND THERAPEUTIC AGENT FOR DISEASE IN WHICH HIGH PHOSPHATE LEVEL IN BLOOD PARTICIPATES 审中-公开
标题翻译：膦和治疗剂对抗疾病与血液中高磷水平有关
公开(公告)号：EP1813620A4
公开(公告)日：2009-12-30
申请号：EP05793817
申请日：2005-10-05
申请人： KOTOBUKI PHARMACEUTICAL CO LTD
发明人： TOMIYAMA HIROSHI , YOKOTA MASAYUKI , TOKUZAKI KAZUO , TOMITA RYOKO
IPC分类号： C07F9/38 , A61K31/662 , A61K31/665 , A61K31/67 , A61K31/675 , A61P43/00 , C07F9/6539 , C07F9/6553
CPC分类号： C07F9/6541 , C07F9/3834 , C07F9/3882 , C07F9/3891 , C07F9/591 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/6558 , C07F9/65586

6. 发明公开

EP2049200A2 NOVEL INHIBITORS OF BETA-LACTAMASE 有权
标题翻译： β-内酰胺酶的新抑制剂
公开(公告)号：EP2049200A2
公开(公告)日：2009-04-22
申请号：EP07870696.7
申请日：2007-05-21
申请人： MethylGene Inc.
发明人： DININNO, Frank , HAMMOND, Milton L. , DYKSTRA, Kevin , KIM, Seongkon , TAN, Qiang , YOUNG, Katherine , HERMES, Jeffrey Donald , CHEN, Helen , RAEPPEL, Stephane , MANNION, Michael , GAUDETTE, Frederic , VAISBURG, Arkadii , RAHIL, Jubrail , GEORGOPAPADAKOU, Nafsika , ZHOU, Nancy Z.
IPC分类号： A61P31/04 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561 , A61K31/67 , A61K31/675
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel β-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.

7. 发明公开

EP1541564A1 FIVE-MEMBERED HETEROCYCLIC COMPOUNDS 审中-公开
标题翻译： F NFGLIEDRIGE HETEROCYCLISCHE VERBINDUNGEN
公开(公告)号：EP1541564A1
公开(公告)日：2005-06-15
申请号：EP03795338.7
申请日：2003-09-09
申请人： Takeda Pharmaceutical Company Limited
发明人： MOMOSE, Yu , TAKAKURA, Nobuyuki , MAEKAWA, Tsuyoshi , ODAKA, Hiroyuki , KIMURA, Hiroyuki
IPC分类号： C07D263/32 , C07D413/12 , C07D413/14 , C07D417/14 , C07D417/12 , C07D401/14 , C07D403/12 , C07F7/18 , C07F9/6558 , A61K31/422 , A61K31/4439 , A61K31/427 , A61K31/4245 , A61K31/454 , A61K31/5377 , A61K31/675 , A61K31/695 , A61K31/662 , A61P3/06 , A61P3/04 , A61P3/10
CPC分类号： C07D263/32 , C07F9/6558 , C07F9/65583
摘要： The present invention provides a compound represented by the formula:
wherein R 1 is an optionally substituted 5-membered heterocyclic group; X, Y and V are the same or different and each is a bond, an oxygen atom, a sulfur atom and the like; Q is a divalent hydrocarbon group having 1 to 20 carbon atoms; ring A is an aromatic ring optionally further having 1 to 3 substituents; Z is -(CH 2 ) n -Z 1 - or -Z 1 -(CH 2 ) n - (n is an integer of 0 to 8, Z 1 is a bond, an oxygen atom, a sulfur atom and the like); ring B is a nitrogen-containing heterocycle optionally further having 1 to 3 substituents; W is a bond or a divalent hydrocarbon group having 1 to 20 carbon atoms; R 2 is a hydrogen atom, a cyano group, -PO(OR 9 )(OR 10 ) (R 9 and R 10 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, and R 9 and R 10 are optionally bonded to form an optionally substituted ring) and the like, or a salt thereof, which has a superior adipose tissue weight decreasing action, a hypoglycemic action and a hypolipidemic action, and which is useful as an agent for the prophylaxis or treatment of obesity, diabetes mellitus, hyperlipidemia, impaired glucose tolerance, hypertension and the like.
摘要翻译：本发明提供由下式表示的化合物：其中R 1为任选取代的5元杂环基; X，Y和V相同或不同，各自为键，氧原子，硫原子等; Q为碳原子数为1〜20的二价烃基; 环A是任选进一步具有1至3个取代基的芳环; Z是 - （CH 2）n Z 1 - 或-Z 1 - （CH 2）n - （n是0至8的整数，Z 1是键，氧原子，硫原子和喜欢）; 环B是任选还含有1至3个取代基的含氮杂环; W是碳原子数为1〜20的键或二价烃基; R 2是氢原子，氰基，-PO（OR 9）（OR 10）（R 9和R 10）相同或不同，各自为氢原子或任选取代的烃基，R 9和R 10任选地键合以形成任选取代的环）等，或其盐具有优异的脂肪组织重量减轻作用，降血糖作用和降血脂症作为预防或治疗肥胖症，糖尿病，高脂血症，葡萄糖耐量降低，高血压等的作用剂。

8. 发明公开

EP0524439A1 Novel cyclohexane and tetrahydropyran derivatives and antifungal compositions containing these derivatives 失效
标题翻译：环己烷 - 四氢吡喃衍生物衍生物enthaltende，抗真菌Zusammensetzungen。
公开(公告)号：EP0524439A1
公开(公告)日：1993-01-27
申请号：EP92110497.2
申请日：1992-06-22
申请人： F.HOFFMANN-LA ROCHE & CO. AKTIENGESELLSCHAFT
发明人： Aoki,Yuhko , Kotaki, Hiromichi , Masubuchi, Kazunao , Okuda, Toru , Shimma, Nobuo , Tsukuda, Takuo , Umeda, Isao, Imperial Higashihakuraku Gardenhouse
IPC分类号： C07D309/10 , C07D405/12 , C07D495/10 , C07D493/10 , C07D309/14 , C07C237/02 , C07F9/655 , C07D233/64 , C07D249/08 , A61K31/35 , A61K31/41 , C07D309/04
CPC分类号： C07D231/12 , A01N37/44 , A01N43/16 , A01N43/50 , A01N43/653 , A01N43/90 , A01N49/00 , C07C43/188 , C07C43/196 , C07C45/30 , C07C45/40 , C07C45/513 , C07C217/52 , C07C225/20 , C07C237/04 , C07C2601/14 , C07D233/56 , C07D249/08 , C07D309/10 , C07D309/14 , C07D493/10 , C07D495/10 , C07F9/6558 , C07C49/753 , C07C49/577 , C07C47/47
摘要： Compounds of the formula

wherein the symbols have the meaning given in the specification have antifungal activity
摘要翻译：式CHEM的化合物其中符号具有本说明书中给出的含义具有抗真菌活性

9. 发明授权

EP0094687B1 Phosphinylalkanoyl substituted imino acids 失效
标题翻译：磷酰基取代的氨基酸
公开(公告)号：EP0094687B1
公开(公告)日：1986-09-10
申请号：EP83104912.7
申请日：1983-05-18
申请人： E.R. Squibb & Sons, Inc.
发明人： Karanewsky, Donald S. , Petrillo, Edward W., Jr.
IPC分类号： C07F9/65 , A61K31/675
CPC分类号： C07F9/6558 , C07D217/26 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/5728 , C07F9/62

10. 发明公开

EP3309151A1 HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF NEUROLOGICAL AND PSYCHOLOGICAL DISORDERS 审中-实审
标题翻译：杂环化合物用于治疗神经和心理疾病
公开(公告)号：EP3309151A1
公开(公告)日：2018-04-18
申请号：EP17176623.1
申请日：2010-06-24
申请人： Alkermes Pharma Ireland Limited
发明人： REMENAR, Julius F. , BLUMBERG, Laura Cook , ZEIDAN, Tarek A.
IPC分类号： C07D263/58 , C07D401/12 , C07D417/12 , C07D471/04 , C07F9/6558 , C07D215/227 , A61K31/497
CPC分类号： C07D215/227 , A61K31/496 , A61K31/497 , C07D215/22 , C07D241/04 , C07D263/58 , C07D401/12 , C07D401/14 , C07D413/10 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07F9/6558 , C07F9/65583
摘要： Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.
摘要翻译：公开了式I的内酰胺化合物及其用于治疗包括精神分裂症，双相型障碍，焦虑症和失眠的神经和精神障碍的用途。

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