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1. 发明申请

WO2021113690A1 MASP-2 INHIBITORS AND METHODS OF USE 审中-公开
公开(公告)号：WO2021113690A1
公开(公告)日：2021-06-10
申请号：PCT/US2020/063383
申请日：2020-12-04
申请人： OMEROS CORPORATION
发明人： CUTSHALL, Neil S. , GAGE, Jennifer Lynn , GOLDSTEIN, Sara Rebecca , KESHIPEDDY, Santosh Kumar , KWON, Do Yeon , LEMUS, Robert Huerta , LITTLE, Thomas L. , METZ, Markus , NOLLERT VON SPECHT, Peter Kurt , PRICE, Loren Michael , TSOUNG, Jennifer
IPC分类号： C07D211/60 , C07D403/14 , C07D413/12 , C07F9/38 , A61P3/00 , A61P7/00 , A61P7/02 , A61P9/00 , A61P11/00 , A61P13/00 , A61P27/02 , A61P29/00 , A61P37/00 , A61K31/662 , A61K31/4418 , A61K31/4439 , A61K31/4436 , C07D401/06 , C07D401/14 , C07D409/12 , C07F9/59 , C07F9/65583 , C07F9/6561
摘要： The present disclosure provides, inter alia, compounds with MASP-2 inhibitory activity, compositions of such compounds, and methods of making and using such compounds.

2. 发明申请

WO2021070200A2 STABLE COMPOSITIONS OF (7AS,2'S)-2-OXOCLOPIDOGREL AND ITS PHARMACEUTICAL SALTS 审中-公开
公开(公告)号：WO2021070200A2
公开(公告)日：2021-04-15
申请号：PCT/IN2020/050865
申请日：2020-10-08
申请人： IPCA LABORATORIES LIMITED
发明人： KUMAR, Ashok , SINGH, Dharmendra , BYJU, Thankachen , GUPTA, Mukesh , MATHUR, Arpana , BHADRA, Dinesh
IPC分类号： A61K31/4365 , A61P7/02 , C07D495/04 , C07F9/59 , A61K31/44
摘要： The present invention discloses stable oral pharmaceutical composition containing therapeutically effective amount of (7aS,2'S)-2-oxoclopidogrel and/or its salts or derivatives, in combination with pharmaceutically acceptable adjuvants or carriers. More particularly, the present invention discloses highly pure (7aS,2'S)-2-oxoclopidogrel and/or its salts, processes for manufacturing pure and stable (7aS,2'S)-2-oxoclopidogrel and stable compositions having a shelf-life of at least one year or more.

3. 发明申请

WO2018107131A1 METHYLPHENIDATE-PRODRUGS, PROCESSES OF MAKING AND USING THE SAME 审中-公开
公开(公告)号：WO2018107131A1
公开(公告)日：2018-06-14
申请号：PCT/US2017/065481
申请日：2017-12-09
申请人： KEMPHARM, INC.
发明人： MICKLE, Travis , GUENTHER, Sven M. , CHI, Gouchen
IPC分类号： C07D401/12 , C07F9/59
CPC分类号： C07D401/12
摘要： The present technology is directed to d-threo-methylphenidate conjugates and a composition comprising d-threo-methylphenidate conjugated to nicotinoyl-L-serine, or salt thereof. The present technology also relates to a composition comprising at least one conjugate of d-methylphenidate having at least two or more chiral centers. The composition is optically active. The present technology additionally relates to oral formulations and pharmaceutical kits comprising at least one d-threo-methylphenidate conjugate. The pharmaceutical kit may comprise a specified amount of individual doses in a package. Each individual dose in the package may contain a pharmaceutically effective amount of a conjugate of d-threo methylphenidate.

4. 发明申请

WO2017005884A1 DEVELOPMENT OF RADICAL PROBES HIGHLY SENSITIVE TO THE POLARITY 审中-公开
标题翻译：发展对极地敏感的雷达探测器
公开(公告)号：WO2017005884A1
公开(公告)日：2017-01-12
申请号：PCT/EP2016/066208
申请日：2016-07-07
申请人： UNIVERSITE D'AIX MARSEILLE , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
发明人： MARQUE, Sylvain , BUTSCHER, Teddy , AUDRAN, Gérard , BREMOND, Paul , BOSCO, Lionel
IPC分类号： C07F9/59
CPC分类号： C07F9/597
摘要： The present invention relates to a compound of formula (I) or (II) and its use for detecting and/or quantifying a solvent S 1 in a solvent S 2 , S 1 and S 2 being distinct, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y and n are as defined in claim 1.
摘要翻译：本发明涉及式（I）或（II）化合物及其在溶剂S2，S1和S2中检测和/或定量溶剂S1的用途，其中R1，R2，R3，R4，R5， R6，X，Y和n如权利要求1所定义。

5. 发明申请

WO2008076269A3 MONOPHOSPHATES AS MUTUAL PRODRUGS OF MUSCARINIC RECEPTOR ANTAGONISTS AND ß-AGONISTS FOR THE TREATMENT OF COPD AND CHRONIC BRONCHITIS 审中-公开
标题翻译：作为MUSCARINIC受体拮抗剂的相互作用的单磷酸酯和用于治疗COPD和慢性BRONCHITIS的β-AGONISTS
公开(公告)号：WO2008076269A3
公开(公告)日：2008-08-21
申请号：PCT/US2007025375
申请日：2007-12-12
申请人： GILEAD SCIENCES INC , BAKER WILLIAM R , STASIAK MARCIN , SWAMINATHAN SUNDARAMOORTHI
发明人： BAKER WILLIAM R , STASIAK MARCIN , SWAMINATHAN SUNDARAMOORTHI
IPC分类号： C07F9/6558 , A61K31/661 , A61K31/665 , A61K31/675 , A61P11/06 , C07F9/553 , C07F9/572 , C07F9/59 , C07F9/6561
CPC分类号： C07F9/65583 , C07F9/5532 , C07F9/572 , C07F9/591 , C07F9/65586 , C07F9/6561
摘要： A mutual prodrug of a MRA and a ß-agonist for formulation for delivery by aerosolization to inhibit pulmonary bronchoconstriction is described. The mutual prodrug is preferably formulated in a small volume solution (10-500 µL) dissolved in a quarter normal saline having pH between 5.0 and 7.0 for the treatment of respiratory tract bronchoconstriction by an aerosol having mass median average diameter predominantly between 1 to 5 µ, produced by nebulization or by dry powder inhaler.
摘要翻译：描述了MRA和β激动剂的联合前药，其用于通过气雾化用于递送以抑制肺支气管收缩的制剂。共聚前体药物优选配制在溶解在pH5.0和7.0之间的四分之一生理盐水中的小体积溶液（10-500μL）中，用于通过气溶胶处理呼吸道支气管收缩，其质量中值平均直径主要在1至5μ ，通过雾化或干粉吸入器生产。

6. 发明申请

WO2005118601A3 SULFONYLETHYL PHOSPHORODIAMIDATES FOR USE IN THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的磺酰氟磷酰胆碱酯酶
公开(公告)号：WO2005118601A3
公开(公告)日：2006-04-06
申请号：PCT/US2005017880
申请日：2005-05-20
申请人： TELIK INC , ALLEN DAVID R , MA WENLI , PETERSON BRIAN T , ROBINSON LOUISE , SCHOW STEVEN R , SHI SONGYUAN , SIMON REYNA J , WEBER KEVIN T , WICK MICHAEL M
发明人： ALLEN DAVID R , MA WENLI , PETERSON BRIAN T , ROBINSON LOUISE , SCHOW STEVEN R , SHI SONGYUAN , SIMON REYNA J , WEBER KEVIN T , WICK MICHAEL M
IPC分类号： A61K31/66 , C07F9/00 , C07F9/02 , C07F9/24 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6509 , C07F9/6533 , C07F9/655 , C07F9/6553 , C07F9/6561 , A61K31/664 , A61P35/04
CPC分类号： C07F9/2458 , C07F9/2408 , C07F9/5721 , C07F9/581 , C07F9/582 , C07F9/591 , C07F9/598 , C07F9/650958 , C07F9/6533 , C07F9/65515 , C07F9/655345 , C07F9/65616
摘要： Sulfonylethyl and thioethyl phosphorodiamidates, their preparation and intermediates in their preparation, formulations containing them, and their pharmaceutical use. The compounds are useful for treating cancer, alone and in combination with other anticancer therapies.
摘要翻译：磺基乙基和硫代乙基磷酰二胺，它们的制备和中间体在制备中，含有它们的制剂及其药物用途。该化合物可用于单独治疗和与其它抗癌疗法组合治疗癌症。

7. 发明申请

WO2006020573A2 NONCARDIOTOXIC PHARMACEUTICAL COMPOUNDS 审中-公开
标题翻译：非药用药物化合物
公开(公告)号：WO2006020573A2
公开(公告)日：2006-02-23
申请号：PCT/US2005/028137
申请日：2005-08-09
申请人： BARBEAU, Donald, L.
发明人： BARBEAU, Donald, L.
IPC分类号： A61K31/675 , C07F9/59
CPC分类号： C07F9/2458 , C07F9/2462 , C07F9/2466 , C07F9/247 , C07F9/2475 , C07F9/5532 , C07F9/5535 , C07F9/5728 , C07F9/588 , C07F9/591 , C07F9/65061 , C07F9/650958 , C07F9/6533 , C07F9/6547 , C07F9/65517 , C07F9/65527 , C07F9/655345 , C07F9/65583 , C07F9/65586 , C07F9/6561
摘要： The present invention relates to novel noncardiotoxic compounds and pharmaceutical compositions useful in the treatment of a variety of disorders including the treatment of depression, allergies, psychoses, cancer and gastrointestinal disorders. In particular, the present invention describes pharmaceutical compositions that mitigate life-threatening arrhythmias such as torsade de pointes. Torsade de pointes is a particular cardiac problem associated with many therapeutic agents and has been implicated as a possible cause of sudden death, particularly in those individuals with a past history of disturbances of cardiac rhythm, myocardial infarction, congenital repolarization abnormalities and cardiac risk factors such as hyperlipidemia and age. This arrhythmia is a variant of paroxysmal ventricular tachycardia associated with a prolonged QTc interval or prominent U waves on the ECG. Torsade de pointes is potentially lethal because it can progress to ventricular fibrillation, life-threatening arrhythmias or precipitate sudden death.
摘要翻译：本发明涉及用于治疗各种障碍的新型非心脏毒性化合物和药物组合物，包括治疗抑郁症，过敏反应，精神病，癌症和胃肠道疾病。特别地，本发明描述了减轻危及生命的心律失常的药物组合物，例如尖端扭转型室性心律失常。特征是与许多治疗剂相关的特定的心脏问题，并且已经被认为是猝死的可能原因，特别是在具有过去心律失调史，心肌梗死，先天性复极化异常和心脏危险因素的个体中作为高脂血症和年龄。这种心律失常是与心电图延长的QTc间期或突出的U波相关的阵发性室性心动过速的变体。由于可能会导致心室纤维性颤动，危及生命的心律失常或突然猝死，可能导致脚部扭转。

8. 发明申请

WO2004062596A3 ANTINEOPLASTIC ETHER LIPID COMPOUNDS HAVING A FOUR CARBON BACKBONE 审中-公开
标题翻译：具有四个碳背景的抗微生物醚类脂质化合物
公开(公告)号：WO2004062596A3
公开(公告)日：2004-11-04
申请号：PCT/US2004000360
申请日：2004-01-09
申请人： ELAN PHARM INC , PERKINS WALTER R
发明人： PERKINS WALTER R
IPC分类号： A61K20060101 , A61K31/662 , A61K31/675 , C07F9/10 , C07F9/40 , C07F9/564 , C07F9/572 , C07F9/58 , C07F9/59 , C07F9/6533
CPC分类号： C07F9/595 , C07F9/10 , C07F9/564 , C07F9/5725 , C07F9/581 , C07F9/6533
摘要： Ether lipid compounds of formula (I), pharmaceutically-acceptable salts, prodrugs or isomers thereof are provided, where 5 the variables are as defined herein. The compounds of the invention have antineoplastic activity, and accordingly have utility in treating cancer and related diseases. Enantiomers of these compounds, pharmaceutical compositions, and methods for treating cancer with the pharmaceutical compositions are also provided.

9. 发明申请

WO0226750A8 PHOSPHINO-AMINOPHOSPHINES, CATALYST COMPLEXES AND ENANTIOSELECTIVE HYDROGENATION 审中-公开
标题翻译：磷酸 - 氨基磷酸，催化剂复合物和选择性氢化
公开(公告)号：WO0226750A8
公开(公告)日：2003-05-08
申请号：PCT/US0130663
申请日：2001-09-28
申请人： EASTMAN CHEM CO
发明人： BOAZ NEIL WARREN , DEBENHAM SHERYL DAVIS
IPC分类号： B01J31/24 , C07B61/00 , C07C51/36 , C07C55/02 , C07C67/31 , C07C69/675 , C07C227/16 , C07C229/14 , C07C231/18 , C07C233/47 , C07C233/83 , C07C233/84 , C07C253/30 , C07C255/60 , C07C269/06 , C07C271/12 , C07C271/22 , C07D203/04 , C07D205/08 , C07D207/26 , C07D207/27 , C07D211/76 , C07D223/10 , C07D225/02 , C07F9/24 , C07F9/553 , C07F9/564 , C07F9/568 , C07F9/572 , C07F9/59 , C07F17/00 , C07F17/02 , C07F9/50 , C07C5/02 , C07C5/03
CPC分类号： C07D203/04 , C07B2200/07 , C07C231/18 , C07C253/30 , C07C269/06 , C07C2601/02 , C07D205/08 , C07D207/27 , C07D211/76 , C07D223/10 , C07D225/02 , C07F9/5532 , C07F9/564 , C07F9/5683 , C07F9/5721 , C07F9/591 , C07F17/02 , C07C233/47 , C07C233/83 , C07C233/84 , C07C255/60 , C07C271/22
摘要： Disclosed are substantially enantiomerically pure bis-phosphine compounds comprising a substantially enantiomerically pure chiral backbone linking two phosphine residues wherein one of the phosphine residues has three phosphorus-carbon bonds and the other phosphine residue has two phosphorus-carbon bonds and one phosphorus-nitrogen bond wherein the nitrogen is part of the chiral backbone. The compounds, which have exhibited surprising air stability, are useful as ligands for metal catalysts for asymmetric reactions and have demonstrated excellent results, in particular as rhodium complexes for asymmetric hydrogenation of enamide, itaconate, and alpha -ketoester compounds. Also disclosed are novel processes for the preparation of the bis-phosphine compounds and novel intermediate compounds useful in the preparation of the bis-phosphine compounds.
摘要翻译：公开了基本上是对映异构体纯的双膦化合物，其包含连接两个膦残基的基本上对映体纯的手性主链，其中一个膦残基具有三个磷 - 碳键，另一个膦残基具有两个磷 - 碳键和一个磷 - 氮键，其中氮是手性主链的一部分。具有惊人的空气稳定性的化合物可用作用于不对称反应的金属催化剂的配体，并且已经证明了优异的结果，特别是作为用于酰胺，衣康酸酯和α-酮酯化合物的不对称氢化的铑络合物。还公开了用于制备双膦化合物和可用于制备双膦化合物的新型中间体化合物的新方法。

10. 发明申请

WO0224650A3 PYRIDINONE AND PYRIDINETHIONE DERIVATIVES HAVING HIV INHIBITING PROPERTIES 审中-公开
标题翻译：具有HIV抑制性质的吡啶酮和吡啶衍生物衍生物
公开(公告)号：WO0224650A3
公开(公告)日：2002-08-08
申请号：PCT/IB0102082
申请日：2001-09-18
申请人： JANSSEN PHARMACEUTICA NV , CENTRE NAT RECH SCIENT , INST CURIE , GUILLEMONT JEROME , BENJAHAD ABDELLAH , MABIRE DOMINIQUE , N GUYEN CHI HUNG , GRIERSON DAVID , MONNERET CLAUDE , BISAGNI EMILE , SANZ GERARD , DECRANE LAURENCE
发明人： GUILLEMONT JEROME , BENJAHAD ABDELLAH , MABIRE DOMINIQUE , N GUYEN CHI HUNG , GRIERSON DAVID , MONNERET CLAUDE , BISAGNI EMILE , SANZ GERARD , DECRANE LAURENCE
IPC分类号： A61K31/428 , A61K31/4365 , A61K31/4412 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/453 , A61K31/454 , A61K31/4545 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/675 , A61K45/00 , A61P31/18 , C07D213/64 , C07D213/69 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/78 , C07D213/80 , C07D213/81 , C07D213/82 , C07D213/84 , C07D213/85 , C07D213/89 , C07D215/22 , C07D215/227 , C07D215/36 , C07D221/04 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/04 , C07D407/06 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D471/04 , C07D491/04 , C07D495/04 , C07F9/59 , C07F9/6584
CPC分类号： C07D213/64 , C07D213/69 , C07D213/70 , C07D213/71 , C07D213/78 , C07D213/80 , C07D213/82 , C07D213/85 , C07D213/89 , C07D215/22 , C07D215/227 , C07D215/36 , C07D401/06 , C07D401/12 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/06 , C07D407/12 , C07D407/14 , C07D409/04 , C07D409/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D491/04
摘要： The present invention is concerned among others with compounds of formula (1), the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein Q is halo, C1-6 alkyl or C2-6 alkenyl; X is (a-2) with q and r being O and Z being O, S or SO; R1 is aryl; R2 is selected from formyl; C1-6alkyloxycarbonylalkyl; Het ; Het C1-6alkyl, C1-6alkylthio; C1-6alkyl optionally substituted with one or two substituents each independently selected from hydroxy, and halo; R3 is selected from formyl; C1-6alkyl optionally substituted with one or two C1-6alkyloxy; R4 is hydrogen, with HIV inhibiting properties.
摘要翻译：本发明涉及式（1）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中Q为卤素，C 1-6烷基或C 2-6烯基; X为（a-2），q和r为O，Z为O，S或SO; R1是芳基; R2选自甲酰基; C1-6alkyloxycarbonylalkyl; 的Het <2>; Het 2 C 1-6烷基，C 1-6烷硫基; 任选被一个或两个独立地选自羟基和卤素的取代基取代的C 1-6烷基; R3选自甲酰基; 任选被一个或两个C 1-6烷氧基取代的C 1-6烷基; R4是氢，具有HIV抑制性质。

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