公开(公告)号：WO2019035775A1

公开(公告)日：2019-02-21

申请号：PCT/SK2018/000005

申请日：2018-08-14

Applicant: SANECA PHARMACEUTICALS A.S.

Inventor： BERKEŠ, Dušan ,  MARKUS, Jozef

IPC: C07C213/00 ,  C07C213/08 ,  C07C215/54 ,  C07C217/62 ,  C07C217/72 ,  C07C219/28 ,  C07C221/00 ,  C07C225/16 ,  C07B53/00

Abstract: A method for the preparation of tapentadol in the form of a base or its hydrogen chloride, which involves the preparation of a salt (III) from a mixture of diastereomers (II) by means of crystallization-induced asymmetric transformation (CIAT) through oxo-enol tautomeric equilibrium of covalently linked diastereomers, shifted towards the desired diastereomer without the use of chiral resolution with chiral carboxyl acids.

公开(公告)号：WO2013113946A3

公开(公告)日：2013-08-08

申请号：PCT/EP2013/058756

申请日：2013-04-26

Applicant: CRYSTAL PHARMA, S.A.U.

Inventor： LORENTE BONDE-LARSEN, Antonio ,  GALLO NIETO, Francisco Javier ,  FERREIRO GIL, Juan José ,  MARTÍN PASCUAL, Pablo

IPC: C07C213/00 ,  C07C213/06 ,  C07C215/54 ,  C07C219/28 ,  C07C227/16 ,  C07C227/18 ,  C07C227/34 ,  C07C229/38

Abstract: The invention relates to a process for obtaining 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, comprising treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV'), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R 1 is C 1 -C 8 alkyl; and R 2 and R 3 , independently of one another, represent H or C 1 -C 6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound.

公开(公告)号：WO2011154854A1

公开(公告)日：2011-12-15

申请号：PCT/IB2011/051896

申请日：2011-04-29

Applicant: CHEMI SPA ,  CIAMBECCHINI, Umberto ,  TURCHETTA, Stefano ,  DE FERRA, Lorenzo ,  ZENONI, Maurizio

Inventor： CIAMBECCHINI, Umberto ,  TURCHETTA, Stefano ,  DE FERRA, Lorenzo ,  ZENONI, Maurizio

IPC: C07D311/20 ,  C07C215/54 ,  C07C219/28

CPC classification number: C07D311/20 ,  C07C213/00 ,  C07C213/02 ,  C07C213/10 ,  C07C215/54

Abstract: The present invention regards an improved and industrially advantageous process for the preparation of the 2-hyaroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called "feso chromenyl" and (R)-2-[3-(diisopropylamino)-l- phenylpropyl]-4-(hydroxymethyl)phenol, also called "(R)-feso deacyl", which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine furnarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate "(R)-feso deacyl", called form B.

Abstract translation: 本发明涉及一种改进和工业上有利的制备2-羟基-4-苯基-3,4-二氢-2H-色烯-6-基 - 甲醇中间体的方法，也称为“feso chromenyl”和（R） -2- [3-（二异丙基氨基）-1-苯基丙基] -4-（羟甲基）苯酚，也称为“（R） - 非索酰基”，它们又用于合成非索特罗定，特别是拟西索罗定。 该方法利用在工业水平上无毒且易于管理的试剂，能够获得称为B型关键中间体“（R） - feso deacyl”的新型稳定和非吸湿结晶形式。

公开(公告)号：WO2011029005A1

公开(公告)日：2011-03-10

申请号：PCT/US2010/047820

申请日：2010-09-03

Applicant: TEVA GYOGYSZERGYAR ZARTKORUEN MUKODO RESZVENYTARSASAG ,  TEVA PHARMACEUTICALS USA, INC. ,  KEREKES, Peter ,  NEMETHNE RACZ, Csilla ,  HAJKO, Janos ,  ARONHIME, Judith ,  SZABO, Csaba ,  TAMAS, Tivadar ,  GAVENDA, Ales ,  KOVACSNE MEZEI, Adrienne

Inventor： KEREKES, Peter ,  NEMETHNE RACZ, Csilla ,  HAJKO, Janos ,  ARONHIME, Judith ,  SZABO, Csaba ,  TAMAS, Tivadar ,  GAVENDA, Ales ,  KOVACSNE MEZEI, Adrienne

IPC: C07C219/28 ,  C07C57/15 ,  A61K31/222 ,  A61P13/00

CPC classification number: C07C219/28 ,  C07B2200/13 ,  C07C57/15

Abstract: Polymorphically pure crystalline forms of fesoterodine fumarate and fesoterodine base are described and characterized.

Abstract translation: 描述和表征富马酸非索罗定和非索罗定碱的多晶型纯结晶形式。

公开(公告)号：WO2007147252A1

公开(公告)日：2007-12-27

申请号：PCT/CA2007/001106

申请日：2007-06-21

Applicant: THE UNIVERSITY OF BRITISH COLUMBIA ,  ANDERSEN, Raymond ,  NODWELL, Matthew ,  MUI, Alice

Inventor： ANDERSEN, Raymond ,  NODWELL, Matthew ,  MUI, Alice

IPC: C07C219/28 ,  A61K31/222 ,  A61K31/417 ,  A61K31/661 ,  C07C235/74 ,  C07C237/12 ,  C07C279/14 ,  C07C323/52 ,  C07D233/64 ,  C07F9/12

CPC classification number: C07C39/17 ,  C07C43/23 ,  C07C45/29 ,  C07C47/57 ,  C07C65/17 ,  C07C229/08 ,  C07C229/24 ,  C07C229/26 ,  C07C279/14 ,  C07C323/52 ,  C07C2603/40 ,  C07F9/12 ,  C07J61/00

Abstract: The present invention provides the use of prodrugs of pelorol and homopelorol, related compounds and pharmaceutical compositions thereof as modulators of SHIPl activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

Abstract translation: 本发明提供了作为SHIP1活性的调节剂的用于制备托泊酮和高麦芽凌醇的前体药物，相关化合物及其药物组合物的用途。 本发明的化合物或药物组合物除了其它病症和病症之外，还可用于治疗或预防炎症，肿瘤，造血或免疫疾病或病症。

公开(公告)号：WO0135957A3

公开(公告)日：2001-12-27

申请号：PCT/EP0011309

申请日：2000-11-15

Applicant: SANOL ARZNEI SCHWARZ GMBH ,  MEESE CLAUS

Inventor： MEESE CLAUS

IPC: A61P13/00 ,  A61K31/24 ,  A61P13/06 ,  C07B61/00 ,  C07C213/06 ,  C07C215/54 ,  C07C219/28 ,  C07C229/38

CPC classification number: C07C215/54 ,  C07B2200/07 ,  C07C219/28 ,  C07C229/38

Abstract: The invention relates to highly pure, crystalline, stable compounds of 3,3-diphenylpropylamine derivatives, in the form of their salts, a method for their production and highly pure, stable, intermediate products. The method is particularly characterized by regio- and chemo-selectivity and high yields and provides salts of phenolic monoesters of 3,3-diphenylpropylamines, which are particularly suitable for application in technical pharmaceutic formulations. Preferred compounds are R -(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenyl isobutyrate hydrogenfumarate and R -(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenyl isobutyrate hydrochloride hydrate. The method further provides essential, stable, crystalline intermediate products for the production of the above salts. A preferred intermediate product is R -(-)-3-(3-diisopropylaminophenylpropyl)-4-hydroxybenzoic acid methyl ester.

公开(公告)号：WO2013046194A3

公开(公告)日：2013-09-19

申请号：PCT/IB2013050141

申请日：2013-01-08

Applicant: ALEMBIC PHARMACEUTICALS LTD ,  JAYARAMAN VENKAT RAMAN

Inventor： JAYARAMAN VENKAT RAMAN ,  BALAJI SUNDARA KALYANA ,  PATEL SAMIR ,  THAKOR INDRAJIT ,  PAREKH VIRAL MAHESHBHAI ,  LADANI MAHESH ,  PATIL CHETAN ,  PATEL RONAK ,  PARMAR DARSHAN

IPC: C07C217/48 ,  A61K31/222 ,  C07C219/22 ,  C07C219/28 ,  G01N33/15

CPC classification number: C07C219/22 ,  A61J1/10 ,  A61K31/222 ,  B65D81/2023 ,  B65D81/264 ,  C07C213/06 ,  C07C213/10 ,  C07C217/48 ,  C07C219/28 ,  G01N33/15

Abstract: The present invention relates to the new impurities of Fesoterodine, Fesoterodine symmetric dimer impurity and asymmetric dimer impurity, process for preparing and isolating thereof. The invention also deals with analytical standards and analytical methods used for the control of the production process and final quality of Fesoterodine.

Abstract translation: 本发明涉及非索罗定，非索罗定对称二聚体杂质和不对称二聚体杂质的新杂质及其制备和分离方法。 本发明还涉及用于控制非索罗定的生产过程和最终质量的分析标准和分析方法。

公开(公告)号：WO2012098560A2

公开(公告)日：2012-07-26

申请号：PCT/IN2012000039

申请日：2012-01-16

Applicant: MSN LAB LTD ,  SATYANARAYANA REDDY MANNE ,  THIRUMALAI RAJAN SRINIVASAN ,  ESWARAIAH SAJJA ,  RAGHURAM SURAPARAJU ,  SEETHA RAMA SARMA PERI

Inventor： SATYANARAYANA REDDY MANNE ,  THIRUMALAI RAJAN SRINIVASAN ,  ESWARAIAH SAJJA ,  RAGHURAM SURAPARAJU ,  SEETHA RAMA SARMA PERI

IPC: C07C219/28

CPC classification number: C07C213/06 ,  C07C213/08 ,  C07C219/28

Abstract: The present invention relates to novel and improved processes for the preparation of (r)-2-(3-(diisopropylamino)-1-phenylpropyl)-4-(hydroxymethyl)phenylisobutyrate represented by the following structural formula-1 and its pharmaceutically acceptable salts thereof.

Abstract translation: 本发明涉及制备由以下结构式-1表示的（R）-2-（3-（二异丙基氨基）-1-苯基丙基）-4-（羟甲基）苯基异丁酸酯及其药学上可接受的盐 它们。

公开(公告)号：WO2012041013A1

公开(公告)日：2012-04-05

申请号：PCT/CN2011/001637

申请日：2011-09-28

Applicant: SHAN DONG LUYE PHARMACEUTICAL CO., LTD. ,  LI, Youxin ,  LIU, Wanhui ,  LV, Yang ,  DU, Guanhua ,  MENG, Qingguo ,  YANG, Mina ,  ZHOU, Fengmei ,  LI, Ju ,  ZHANG, Xuemei

Inventor： LI, Youxin ,  LIU, Wanhui ,  LV, Yang ,  DU, Guanhua ,  MENG, Qingguo ,  YANG, Mina ,  ZHOU, Fengmei ,  LI, Ju ,  ZHANG, Xuemei

IPC: C07C219/28 ,  C07C213/10 ,  A61K31/235 ,  A61P25/00 ,  A61P25/24 ,  A61P25/22 ,  A61P3/04 ,  A61P25/16

CPC classification number: C07C215/64 ,  A61K31/235 ,  C07B2200/13 ,  C07C213/10 ,  C07C215/20 ,  C07C219/28

Abstract: The present disclosure relates to polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods for preparing the same and use of the same.

Abstract translation: 本公开内容涉及4- [2-二甲基氨基-1-（1-羟基环己基）乙基] -4-甲基苯甲酸苯酯盐酸盐的多晶型物，其制备方法和用途。

公开(公告)号：WO2012025941A2

公开(公告)日：2012-03-01

申请号：PCT/IN2011/000575

申请日：2011-08-25

Applicant: CADILA HEALTHCARE LIMITED ,  DWIVEDI, Shriprakash Dhar ,  PRASAD, Ashok ,  JAIN, Kuldeep Natwarlal

Inventor： DWIVEDI, Shriprakash Dhar ,  PRASAD, Ashok ,  JAIN, Kuldeep Natwarlal

IPC: C07C219/28

CPC classification number: C07C219/28 ,  C07B2200/07 ,  C07B2200/13 ,  C07C41/26 ,  C07C51/43 ,  C07C59/56 ,  C07C67/03 ,  C07C213/00 ,  C07C213/06 ,  C07C213/08 ,  C07C213/10 ,  C07C217/62 ,  C07C303/28 ,  C07C309/66 ,  C07C309/67 ,  C07C215/54 ,  C07C43/23 ,  C07C69/734

Abstract: The invention relates to improved process for the preparation of fesoterodine and its pharmaceutically acceptable salt, specifically fesoterodine fumarate of formula (1). The invention relates to solid state forms of a novel salt of fesoterodine and process for the preparation thereof. The invention also relates to highly pure fesoterodine fumarate substantially free of impurity X at RRT 1.37. The invention also provides solid particles of pure fesoterodine fumarate wherein 90 volume-percent of the particles (D90) have a size of higher than 200 microns.

Abstract translation: 本发明涉及用于制备非索罗定及其药学上可接受的盐，特别是式（1）的非索拉罗定富马酸盐的改进方法。 本发明涉及非索罗定的新盐的固态形式及其制备方法。 本发明还涉及在RRT 1.37下基本上不含杂质X的高纯度的富马酸菲斯卓罗因。 本发明还提供了纯非法罗索丁富马酸盐的固体颗粒，其中90体积％的颗粒（D90）具有高于200微米的尺寸。