公开(公告)号：WO2020170388A1

公开(公告)日：2020-08-27

申请号：PCT/JP2019/006547

申请日：2019-02-21

Applicant: 株式会社ドクターズチョイス

Inventor： 中野　昌彦 ,  山本　明男

IPC: A61K31/198 ,  A61K8/44 ,  A61K8/9706 ,  A61K31/197 ,  A61K36/02 ,  A61P17/00 ,  A61P43/00 ,  A61Q19/00 ,  C07C229/14 ,  C07C251/20

Abstract: 新たなＩ型コラーゲン又はエラスチンの産生促進剤の提供。　マイコスポリン様アミノ酸又はその塩を有効成分とするＩ型コラーゲン又はエラスチンの産生促進剤。

公开(公告)号：WO2014057414A1

公开(公告)日：2014-04-17

申请号：PCT/IB2013059191

申请日：2013-10-08

Applicant: AUCKLAND UNISERVICES LTD ,  SLEIGH JAMES WALLACE ,  DENNY WILLIAM ALEXANDER ,  JOSE JINEY ,  GAMAGE SWARNALATHA AKURATIYA ,  HARVEY MARTYN GREGORY ,  VOSS LOGAN JAMES

Inventor： SLEIGH JAMES WALLACE ,  DENNY WILLIAM ALEXANDER ,  JOSE JINEY ,  GAMAGE SWARNALATHA AKURATIYA ,  HARVEY MARTYN GREGORY ,  VOSS LOGAN JAMES

IPC: C07C219/06 ,  A61K31/222 ,  A61P23/00 ,  C07C229/14

CPC classification number: C07C229/14 ,  C07C225/20 ,  C07C229/46

Abstract: The present invention relates to ketamine derivatives of the formula (I), pharmaceutical compositions comprising them, and methods for treating pain comprising administering them, and their use in the manufacture of medicaments for treating pain. The present invention also relates to methods for anaesthetizing and methods for sedating a subject comprising administering ketamine derivatives of the formula (II).

Abstract translation: 本发明涉及式（I）的氯胺酮衍生物，包含它们的药物组合物，以及治疗疼痛的方法，其包括施用它们，以及它们在制造用于治疗疼痛的药物中的用途。 本发明还涉及用于麻醉麻醉的方法和用于镇静受试者的方法，其包括施用式（II）的氯胺酮衍生物。

公开(公告)号：WO2014028487A1

公开(公告)日：2014-02-20

申请号：PCT/US2013/054726

申请日：2013-08-13

Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGY

Inventor： ANDERSON, Daniel, Griffith ,  WHITEHEAD, Kathryn, Ann ,  DORKIN, Joseph, R. ,  VEGAS, Arturo, Jose ,  ZHANG, Yunlong ,  LANGER, Robert, S.

IPC: C07C229/12 ,  C07C229/14 ,  C07D295/13 ,  C07D211/14 ,  C07D319/18 ,  C07D207/09 ,  C07D211/26 ,  C07D487/04 ,  A61K47/18 ,  A61K9/127 ,  A61K9/51 ,  A61K31/496 ,  C12N15/11 ,  C12N15/88

CPC classification number: A61K47/22 ,  A61K9/1272 ,  A61K9/5123 ,  A61K31/225 ,  A61K31/357 ,  A61K31/40 ,  A61K31/445 ,  A61K31/495 ,  A61K31/4985 ,  A61K31/573 ,  A61K31/704 ,  A61K31/713 ,  A61K45/06 ,  A61K47/18 ,  A61K47/542 ,  A61K47/543 ,  A61K47/6925 ,  C07C225/06 ,  C07C229/12 ,  C07C229/14 ,  C07C229/24 ,  C07C229/26 ,  C07C229/28 ,  C07C229/34 ,  C07C2601/14 ,  C07D207/09 ,  C07D211/14 ,  C07D211/26 ,  C07D211/34 ,  C07D241/04 ,  C07D295/13 ,  C07D295/15 ,  C07D295/16 ,  C07D319/16 ,  C07D319/18 ,  C07D487/04 ,  C12N15/111 ,  C12N15/1137 ,  C12N15/88 ,  C12N2310/14 ,  C12N2320/32 ,  A61K2300/00

Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.

Abstract translation: 本文提供的是可以通过将烷基胺偶联加成丙烯酸酯制备的类脂。 在一些实施方案中，提供的类脂质是可生物降解的并且可以用于多种药物递送系统中。 考虑到类固醇的氨基部分，除了其它药剂之外，它们非常适合于递送多核苷酸。 已经制备了含有本发明的类脂和多核苷酸的纳米颗粒，并且已显示其在递送siRNA方面是有效的。

公开(公告)号：WO2012074921A1

公开(公告)日：2012-06-07

申请号：PCT/US2011/062234

申请日：2011-11-28

Applicant: ALLERGAN, INC. ,  SINHA, Santosh C. ,  BHAT, Smita S. ,  CORPUZ, Evelyn G. ,  CHOW, Ken ,  FANG, Wenkui K. ,  IM, Wha Bin

Inventor： SINHA, Santosh C. ,  BHAT, Smita S. ,  CORPUZ, Evelyn G. ,  CHOW, Ken ,  FANG, Wenkui K. ,  IM, Wha Bin

IPC: C07C43/23 ,  C07C229/14 ,  C07F9/38 ,  A61K31/085 ,  A61K31/197 ,  A61K31/662 ,  A61P27/02

CPC classification number: C07C229/14 ,  C07C43/23 ,  C07F9/3808 ,  C07F9/3834 ,  C07F9/65515 ,  C07F9/655345

Abstract: The present invention relates to novel alkyne and alkene derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract translation: 本发明涉及新的炔烃和烯烃衍生物，其制备方法，含有它们的药物组合物及其作为药物作为鞘氨醇-1-磷酸受体调节剂的用途。

公开(公告)号：WO2012055455A1

公开(公告)日：2012-05-03

申请号：PCT/EP2011/004400

申请日：2011-08-31

Applicant: COGNIS IP MANAGEMENT GMBH ,  GΟΟSSΕΝ, Lukas J . ,  OHLMANN, Dominik ,  DIERKER, Markus

Inventor： GΟΟSSΕΝ, Lukas J . ,  OHLMANN, Dominik ,  DIERKER, Markus

IPC: C07C69/612 ,  C07C229/12 ,  C07C229/14 ,  C07C229/18 ,  C07D295/15 ,  C07C67/347 ,  C07C227/08

CPC classification number: C07C67/347 ,  C07C227/06 ,  C07C227/08 ,  C07C2601/14 ,  C07D211/34 ,  C07D211/62 ,  C07D211/76 ,  C07D295/15 ,  C07C69/612 ,  C07C229/12

Abstract: The invention pertains to a new route to prepare β-functionalized carboxylic acid esters in a one-pot reaction, by reacting an olefinic acid ester in the presence of a catalyst system, comprising a Rh(I)-complex, together with an aryl boron or a diamine as nucleophilic compounds, and under oxygen-free conditions and elevated temperatures.

Abstract translation: 本发明涉及一种在一锅反应中制备β-官能化羧酸酯的新途径，通过在包含Rh（I） - 复合物的催化剂体系存在下使烯酸酯与芳基硼 或二胺作为亲核化合物，并在无氧条件和升高的温度下进行。

公开(公告)号：WO2009004643A3

公开(公告)日：2009-04-30

申请号：PCT/IN2008000287

申请日：2008-05-08

Applicant: CADILA HEALTHCARE LTD ,  TIPPANU THIRUPATHI RAO ,  DWIVEDI SHRIPRAKASH DHAR ,  DOSHI KETAN AMBALAL ,  SAHAY RAKESH BRIJNANDAN ,  ROY RUSHIKESH UDAYKUMAR

Inventor： TIPPANU THIRUPATHI RAO ,  DWIVEDI SHRIPRAKASH DHAR ,  DOSHI KETAN AMBALAL ,  SAHAY RAKESH BRIJNANDAN ,  ROY RUSHIKESH UDAYKUMAR

IPC: C07C227/32 ,  C07C229/08 ,  C07C229/14 ,  C07C233/05 ,  C07C271/22

CPC classification number: C07C233/05 ,  C07C211/63 ,  C07C227/04 ,  C07C227/06 ,  C07C227/32 ,  C07C229/08

Abstract: The present invention relates to an improved process for the preparation of (S)- Pregabalin of formula (I) and its intermediates thereof. Particularly, the present invention relates to the process for the preparation (S)-Pregabalin having chiral purity not less than 99.0% by area percentage of HPLC. Further, the present invention relates to the process for the preparation of (S)-Pregabalin having low level of impurities, determined by area percentage of HPLC.

Abstract translation: 本发明涉及制备式（I）的（S） - 普瑞巴林及其中间体的改进方法。 特别地，本发明涉及制备具有不小于99.0％面积百分比的HPLC的手性纯度（S） - 普瑞巴林的方法。 此外，本发明涉及制备具有低水平杂质的（S）-Pregabalin的方法，其由HPLC的面积百分数确定。

公开(公告)号：WO2007088558A3

公开(公告)日：2007-10-25

申请号：PCT/IN2007000021

申请日：2007-01-19

Applicant: ALEMBIC LTD ,  DESHPANDE PANDURANG BALWANT ,  LUTHRA PARVEN KUMAR ,  PANDEY ANAND KUMAR ,  SHAH HETAL RAMESHCHANDRA

Inventor： DESHPANDE PANDURANG BALWANT ,  LUTHRA PARVEN KUMAR ,  PANDEY ANAND KUMAR ,  SHAH HETAL RAMESHCHANDRA

IPC: C07D257/04 ,  C07C229/14

CPC classification number: C07D257/04

Abstract: The present invention relates to a process for purification of Valsartan comprising steps of: (i) crystallizing from an organic solvent (ii) washing the crystallized product obtained in step (i) with a solvent selected from a group consisting of aliphatic hydrocarbon solvent.

Abstract translation: 本发明涉及一种纯化缬沙坦的方法，其包括以下步骤：（i）从有机溶剂中结晶，（ii）用选自脂族烃溶剂的溶剂洗涤步骤（i）中获得的结晶产物。

公开(公告)号：WO2007009944A1

公开(公告)日：2007-01-25

申请号：PCT/EP2006/064242

申请日：2006-07-13

Applicant: Università degli Studi di Roma "La Sapienza" ,  MALTESE, Maurizio

Inventor： MALTESE, Maurizio

IPC: C07C227/18 ,  C07C229/14

CPC classification number: C07C227/18 ,  C07B2200/05 ,  C07C229/14

Abstract: The invention relates to a method for preparing tritylated compounds in which protic functional groups are protected with the triphenylmethyl group, method based on the homogeneous catalysis exercised by salts or metal complexes in organic solvents. The invention relates in particular to a method for the selective tritylation of some groups, obtained both directly and by selective detritylation, with methods based on metallic catalysis. The application to amino acids, typical substrates not suitable to be subjected as such to homogeneous tritylations in organic solvents, indicates the ability of the method to extend also to hydrophilic substrates. The method allows to obtain with high yield pertrityl amino acids, N-tritylamino acids or amino acids tritylated only in lateral chain, compounds which heretofore were either difficult to obtain in aqueous solvents or obtainable through indirect methods. All, in any case, are important intermediates in peptide synthesis.

Abstract translation: 本发明涉及一种制备三苯甲基化合物的方法，其中质子官能团用三苯基甲基保护，基于在有机溶剂中由盐或金属络合物进行均相催化的方法。 本发明特别涉及一种通过直接和通过选择性不相关获得的一些基团的选择性三苯甲基化方法与基于金属催化的方法。 对氨基酸的应用，不适合在有机溶剂中进行均匀三苯甲基化的典型基质表明该方法也延伸到亲水性底物的能力。 该方法允许以高产率的三苯甲基氨基酸，N-三苯甲基氨基酸或仅在侧链中三取代的氨基酸获得，其在以前难以在含水溶剂中获得或通过间接方法获得的化合物。 无论如何，所有这些都是肽合成中的重要中间体。

公开(公告)号：WO2005087708A1

公开(公告)日：2005-09-22

申请号：PCT/DK2005/000152

申请日：2005-03-08

Applicant: H. LUNDBECK A/S ,  SMITH, Garrick, Paul ,  ANDERSEN, Kim ,  WREN, Stephen, P. ,  HARRIS, Neil ,  BRANDT, Guillaume

Inventor： SMITH, Garrick, Paul ,  ANDERSEN, Kim ,  WREN, Stephen, P. ,  HARRIS, Neil ,  BRANDT, Guillaume

IPC: C07C229/14

CPC classification number: C07C229/14 ,  C07C2602/08 ,  C07D295/135

Abstract: This invention relates to novel compounds which are glycine transporter inhibitors and as such effective in the treatment of disorders in the CNS, such as schizophrenia.

Abstract translation: 本发明涉及作为甘氨酸转运蛋白抑制剂的新化合物，并且在治疗CNS中的疾病如精神分裂症中有效。

公开(公告)号：WO2004016583A8

公开(公告)日：2004-05-27

申请号：PCT/IB0303708

申请日：2003-08-04

Applicant: PFIZER LTD ,  BLAKEMORE DAVID CLIVE ,  BRYANS JUSTIN STEPHEN ,  MAW GRAHAM NIGEL ,  RAWSON DAVID JAMES ,  THOMPSON LISA ROSEMARY ,  CHU WAI-LAM ALEXIS ,  PFIZER

Inventor： BLAKEMORE DAVID CLIVE ,  BRYANS JUSTIN STEPHEN ,  MAW GRAHAM NIGEL ,  RAWSON DAVID JAMES ,  THOMPSON LISA ROSEMARY ,  CHU WAI-LAM ALEXIS

IPC: A61K31/198 ,  A61K31/223 ,  A61K31/47 ,  A61K31/472 ,  A61P1/00 ,  A61P1/18 ,  A61P13/10 ,  A61P19/02 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/10 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  C07C227/18 ,  C07C229/10 ,  C07C229/12 ,  C07C229/14 ,  C07C319/20 ,  C07C323/25 ,  C07C323/32 ,  C07D217/02

CPC classification number: C07C323/25 ,  A61K31/198 ,  A61K31/223 ,  A61K31/47 ,  C07C229/12 ,  C07C229/14 ,  C07C323/32 ,  C07D217/02

Abstract: The compounds of formula (I) are substituted glycine derivatives useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, arthritis, neuropathological disorders, sleep disorders, visceral pain disorders and gastrointestinal disorders. Processes for the preparation of the final products and intermediates useful in the process are included. Pharmaceutical compositions containing one or more of the compounds are also included. Formula (I) wherein R' is hydroxycarbonyl, a carboxylic acid biostere or prodrug thereof; R , R , R and R are independently selected from H, C1-C6 alkyl, and Cl-C6 alkoxy Cl-C6 alkyl.

Abstract translation: 式（I）化合物是用于治疗癫痫，昏厥发作，运动机能减退，颅脑疾病，神经变性疾病，抑郁症，焦虑症，恐慌症，疼痛，关节炎，神经病理疾病，睡眠障碍，内脏疼痛疾病和胃肠道疾病的取代甘氨酸衍生物 障碍。 包括制备用于该方法的最终产物和中间体的方法。 还包括含有一种或多种化合物的药物组合物。 式（I）其中R'是羟基羰基，羧酸生物等排物或其前药; R 3，R 3a，R 2和R 2a独立地选自H，C 1 -C 6烷基和C 1 -C 6烷氧基C 1 -C 6烷基。