RU2461542C2 - Новый способ получения соли - Google Patents

Новый способ получения соли Download PDF

Info

Publication number
RU2461542C2
RU2461542C2 RU2009102279/04A RU2009102279A RU2461542C2 RU 2461542 C2 RU2461542 C2 RU 2461542C2 RU 2009102279/04 A RU2009102279/04 A RU 2009102279/04A RU 2009102279 A RU2009102279 A RU 2009102279A RU 2461542 C2 RU2461542 C2 RU 2461542C2
Authority
RU
Russia
Prior art keywords
organic amine
solvent
addition salt
acid addition
acid
Prior art date
Application number
RU2009102279/04A
Other languages
English (en)
Other versions
RU2009102279A (ru
Inventor
Йозеф Визер (AT)
Йозеф ВИЗЕР
Ханнес ЛЕНГАУЕР (AT)
Ханнес ЛЕНГАУЕР
Эльфриде КЛИНГЛЕР (AT)
Эльфриде КЛИНГЛЕР
Артур ПИХЛЕР (AT)
Артур Пихлер
Хуберт ШТУРМ (AT)
Хуберт Штурм
Original Assignee
Сандоз Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37450796&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RU2461542(C2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Сандоз Аг filed Critical Сандоз Аг
Publication of RU2009102279A publication Critical patent/RU2009102279A/ru
Application granted granted Critical
Publication of RU2461542C2 publication Critical patent/RU2461542C2/ru

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C213/00—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
    • C07C213/02—Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton by reactions involving the formation of amino groups from compounds containing hydroxy groups or etherified or esterified hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/08—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/30—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom
    • C07D211/32—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by doubly bound oxygen or sulfur atoms or by two oxygen or sulfur atoms singly bound to the same carbon atom by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/22—Oxygen atoms attached in position 2 or 4
    • C07D215/227—Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/48—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D215/54—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3
    • C07D215/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 3 with oxygen atoms in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C07D277/82—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/14—Radicals substituted by singly bound hetero atoms other than halogen
    • C07D333/16—Radicals substituted by singly bound hetero atoms other than halogen by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Diabetes (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Quinoline Compounds (AREA)
  • Furan Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Seasonings (AREA)

Abstract

Изобретение относится к новому способу получения одной кристаллической полиморфной формы гидрогалогенида органического амина предпочтительно в сравнении с другой кристаллической полиморфной формой гидрогалогенида органического амина. Способ включает добавление триалкилсилилгалогенида к органическому амину в растворителе, где триалкилсилилгалогенид добавляется в условиях, в которых одна полиморфная форма кристаллизуется предпочтительно в сравнении с другой полиморфной формой, и где органический амин находится в форме свободного основания или кислотно-аддитивной соли. Причем, если органический амин находится в форме кислотно-аддитивной соли, сопряженная кислота кислотно-аддитивной соли является более слабой, чем гидрогалогеновая кислота, и растворитель представляет собой апротонный растворитель, а если органический амин находится в форме свободного основания, то он растворяется в апротонном растворителе, а триалкилсилилгалогенид добавляется в протонном растворителе. Органический амин представляет собой фармацевтически активное соединение, которое включает первичную, вторичную, третичную или четвертичную аминогруппу. 5 з.п. ф-лы, 66 ил., 30 пр.

Description

Текст описания приведен в факсимильном виде.
Figure 00000001
Figure 00000002
Figure 00000003
Figure 00000004
Figure 00000005
Figure 00000006
Figure 00000007
Figure 00000008
Figure 00000009
Figure 00000010
Figure 00000011
Figure 00000012
Figure 00000013
Figure 00000014
Figure 00000015
Figure 00000016
Figure 00000017
Figure 00000018
Figure 00000019
Figure 00000020
Figure 00000021
Figure 00000022
Figure 00000023
Figure 00000024
Figure 00000025
Figure 00000026
Figure 00000027
Figure 00000028
Figure 00000029
Figure 00000030
Figure 00000031
Figure 00000032
Figure 00000033
Figure 00000034
Figure 00000035
Figure 00000036
Figure 00000037
Figure 00000038
Figure 00000039
Figure 00000040
Figure 00000041
Figure 00000042
Figure 00000043
Figure 00000044
Figure 00000046
Figure 00000047
Figure 00000048
Figure 00000049

Claims (6)

1. Способ получения одной кристаллической полиморфной формы гидрогалогенида органического амина предпочтительно в сравнении с другой кристаллической полиморфной формой гидрогалогенида органического амина, включающий:
добавление триалкилсилилгалогенида к органическому амину в растворителе,
где триалкилсилилгалогенид добавляется в условиях, в которых одна полиморфная форма кристаллизуется предпочтительно в сравнении с другой полиморфной формой;
где органический амин находится в форме свободного основания или кислотно-аддитивной соли,
где, если органический амин находится в форме кислотно-аддитивной соли, сопряженная кислота кислотно-аддитивной соли является более слабой, чем гидрогалогеновая кислота, а растворитель представляет собой апротонный растворитель,
где, если органический амин находится в форме свободного основания, то он растворяется в апротонном растворителе, а триалкилсилилгалогенид добавляется в протонном растворителе, и
где органический амин представляет собой фармацевтически активное соединение, которое включает первичную, вторичную, третичную или четвертичную аминогруппу.
2. Способ по п.1, в котором условия, в которых одна полиморфная форма кристаллизуется предпочтительно в сравнении с другой полиморфной формой, представляют собой выбор растворителя или температуру.
3. Способ по п.1 или 2, где способ включает стадии:
(а) растворение или суспендирование органического амина в апротонном растворителе,
(б) добавление триалкилсилилгалогенида и по меньшей мере одного эквивалента протонного растворителя, по отношению к органическому амину,
(в) образование кристаллов, и
(г) сбор образовавшихся кристаллов.
4. Способ по п.3, в котором протонный растворитель представляет собой соединение, содержащее гидроксильную группу или карбоксильную группу.
5. Способ по п.1 или 2, где способ включает стадии:
а) растворение, суспендирование или генерирование кислотно-аддитивной соли органического амина в апротонном растворителе, причем сопряженная кислота кислотно-аддитивной соли является более слабой, чем гидрогалогеновая кислота,
(б) добавление триалкилсилилгалогенида,
(в) образование кристаллов, и
(г) сбор образовавшихся кристаллов.
6. Способ по любому из пп.1-5, в котором триалкилсилилгалогенид представляет собой триметилсилилхлорид, триметилсилилбромид или триметилсилилйодид.
RU2009102279/04A 2006-06-27 2007-06-25 Новый способ получения соли RU2461542C2 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP06116134.5 2006-06-27
EP06116134 2006-06-27

Publications (2)

Publication Number Publication Date
RU2009102279A RU2009102279A (ru) 2010-08-10
RU2461542C2 true RU2461542C2 (ru) 2012-09-20

Family

ID=37450796

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2009102279/04A RU2461542C2 (ru) 2006-06-27 2007-06-25 Новый способ получения соли

Country Status (14)

Country Link
US (1) US20100204470A1 (ru)
EP (3) EP2032521B1 (ru)
JP (1) JP2009541385A (ru)
CN (1) CN101484411A (ru)
AT (1) ATE446946T1 (ru)
AU (1) AU2007264030B2 (ru)
CA (1) CA2655061A1 (ru)
DE (1) DE602007003024D1 (ru)
DK (1) DK2032521T3 (ru)
ES (1) ES2335369T3 (ru)
PL (1) PL2032521T3 (ru)
RU (1) RU2461542C2 (ru)
SI (1) SI2032521T1 (ru)
WO (1) WO2008000418A2 (ru)

Families Citing this family (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8546423B2 (en) 2005-05-18 2013-10-01 Mpex Pharmaceuticals, Inc. Aerosolized fluoroquinolones and uses thereof
US20100113793A1 (en) * 2006-03-20 2010-05-06 Ind-Swift Laboratories Limited Process for the Preparation of Highly Pure Donepezil
WO2008130630A2 (en) * 2007-04-16 2008-10-30 Teva Pharmaceutical Industries Ltd. Polymorphic form of rimonabant hydrochloride and processes for preparation thereof
EP2213665A1 (en) 2007-08-17 2010-08-04 Hetero Drugs Limited Erlotinib hydrochloride
EP2257556A1 (en) 2008-02-06 2010-12-08 Helm AG Prasugrel salts with improved properties
WO2009125426A2 (en) * 2008-02-08 2009-10-15 Neuland Laboratories Ltd NOVEL PROCESS FOR THE PREPARATION OF (3SM-[2-(2 J-DIHYDRO-5- BENZOFURANYLϊETHYL]-α.α -DIPHENYL-3-PYRROLIDINEACETAMIDE HYDROBROMIDE
NO2344129T3 (ru) 2008-10-07 2018-07-21
PT2346509T (pt) 2008-10-07 2020-08-05 Horizon Orphan Llc Inalação de levofloxacina para redução da inflamação pulmonar
CN102438995B (zh) 2009-03-26 2014-12-17 兰贝克赛实验室有限公司 厄洛替尼或其药学上可接受的盐的制备工艺
JP5501438B2 (ja) * 2009-03-31 2014-05-21 上海医薬工業研究院 プラスグレル臭化水素酸塩の結晶
EP2236509A1 (en) 2009-04-01 2010-10-06 Ragactives, S.L. Method for obtaining 1,3-difunctionalized pyrrolidine derivatives
SI2473170T1 (sl) 2009-09-04 2019-10-30 Horizon Orphan Llc Uporaba aerosoliziranega levofloksacina za zdravljenje cistične fibroze
WO2011058525A2 (en) 2009-11-12 2011-05-19 Ranbaxy Laboratories Limited Processes for the preparation of erlotinib hydrochloride form a and erlotinib hydrochloride form b
CZ2009828A3 (cs) 2009-12-09 2011-06-22 Zentiva, K.S. Zpusob prípravy hydrochloridu 5-[2-cyklopropyl-1-(2-fluorfenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetátu (prasugrelu hydrochloridu) v polymorfní forme B
CN102212071B (zh) * 2010-04-08 2014-03-26 上海医药工业研究院 普拉格雷盐酸盐乙酸溶剂合物及其结晶和制备方法
JP5730986B2 (ja) * 2010-04-08 2015-06-10 テバ ファーマシューティカル インダストリーズ リミティド プラスグレル塩の結晶性形態
CN102342921B (zh) * 2010-08-01 2013-09-11 江苏正大天晴药业股份有限公司 普拉格雷氢溴酸盐醋酸合物的药物组合物
EP2447256A1 (en) * 2010-10-21 2012-05-02 Laboratorios Lesvi, S.L. Process for obtaining dronedarone
IT1403083B1 (it) * 2010-10-25 2013-10-04 Fidia Farmaceutici Nuova forma polimorfa di raloxifene cloridrato
JP2014510071A (ja) 2011-03-03 2014-04-24 カディラ・ヘルスケア・リミテッド Ｄｐｐ−ｉｖ阻害剤の新規な塩
EA029539B8 (ru) * 2011-03-29 2018-06-29 Крка, Товарна Здравил, Д.Д., Ново Место Фармацевтическая композиция ситаглиптина
KR101766835B1 (ko) 2011-05-04 2017-08-09 에스프린팅솔루션 주식회사 화상형성장치 및 그 제어 방법
US20150025080A1 (en) 2011-06-29 2015-01-22 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation
US20150051213A1 (en) 2011-06-30 2015-02-19 Suresh Babu Jayachandra Novel salts of sitagliptin
US20140350023A1 (en) 2011-12-08 2014-11-27 Ranbaxy Laboratories Limited Amorphous form of sitagliptin salts
WO2014024202A1 (en) * 2012-08-07 2014-02-13 Zcl Chemicals Limited An improved process for the preparation of memantine hydrochloride
WO2014037961A1 (en) 2012-09-04 2014-03-13 Shilpa Medicare Limited Crystalline erlotinib hydrochloride process
CN103012427B (zh) * 2012-11-26 2015-07-08 天津大学 一种普拉格雷盐酸盐乙醇溶剂化物及其制备方法
PL402028A1 (pl) 2012-12-12 2014-06-23 Instytut Farmaceutyczny Sposób wytwarzania postaci polimorficznej B chlorowodorku prasugrelu o czystości farmaceutycznej
CN103739500B (zh) * 2012-12-27 2016-03-23 国药一心制药有限公司 一种盐酸西那卡塞的合成与精制方法
WO2014118737A1 (en) 2013-01-31 2014-08-07 Ranbaxy Laboratories Limited Erlotinib salts
WO2014135834A1 (en) * 2013-03-05 2014-09-12 Cipla House Oxalic acid addition salts and/or solvates of a selective estrogen receptor modulator
CN103145628B (zh) * 2013-03-18 2015-04-22 齐鲁制药有限公司 一种厄洛替尼一水合物晶型i的制备方法
CN104072442B (zh) * 2013-03-28 2016-09-28 成都弘达药业有限公司 一种化合物及其制备方法
CN103396371B (zh) * 2013-08-26 2015-12-02 南京优科生物医药研究有限公司 一种盐酸埃罗替尼晶型a的制备方法
IN2014MU00651A (ru) 2014-02-25 2015-10-23 Cadila Healthcare Ltd
WO2015170340A2 (en) * 2014-05-06 2015-11-12 Laurus Labs Private Limited Novel polymorphs of sitagliptin hydrochloride, processes for its preparation and pharmaceutical composition thereof
CN107540632A (zh) * 2016-06-27 2018-01-05 江苏神龙药业股份有限公司 一种普拉克索单盐酸盐的新晶型及其制备方法
CN107540634A (zh) * 2016-06-27 2018-01-05 江苏神龙药业股份有限公司 一种普拉克索单盐酸盐的新晶型及其制备方法
MX2020007271A (es) * 2017-09-26 2020-08-17 Intra Cellular Therapies Inc Sales y cristales novedosos.
KR20210031867A (ko) * 2018-06-06 2021-03-23 미노릭스 테라퓨틱스 에스.엘. 5-[[4-[2-[5-아세틸피리딘-2-일]에톡시]벤질]-1,3-티아졸리딘-2,4-디온 및 이의 염의 용도

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1757471A3 (ru) * 1988-07-13 1992-08-23 Крка, Товарна Здравил, Н.Сол., О. (Фирма) Способ получени производных L-аланил-L-пролина или их фармацевтически приемлемых солей
US6414002B1 (en) * 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
WO2005012285A1 (en) * 2003-08-05 2005-02-10 Matrix Laboratories Ltd An improved process for the preparation of moxifloxacin hydrochloride
WO2005108380A2 (en) * 2004-05-04 2005-11-17 Bristol-Myers Squibb Company Process employing controlled crystallization in forming crystals of a pharmaceutical
US20050288343A1 (en) * 2004-05-19 2005-12-29 Andrew Rusowicz Process of preparing substituted carbamates and intermediates thereof
US20060025456A1 (en) * 2002-12-20 2006-02-02 Gruenenthal Gmbh Saturated and unsaturated heteroarylcycloalkylmethyl amines as anti-depressants

Family Cites Families (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW209865B (ru) 1992-01-10 1993-07-21 Bayer Ag
FR2713225B1 (fr) 1993-12-02 1996-03-01 Sanofi Sa N-pipéridino-3-pyrazolecarboxamide substitué.
JP3411038B2 (ja) 1993-09-15 2003-05-26 シンテックス（ユー・エス・エイ）・インコーポレイテッド ミコフェノール酸モフェチルの結晶質無水物およびその静注用製剤
DE19546249A1 (de) 1995-12-12 1997-06-19 Bayer Ag Neue Kristallmodifikation des 1-Cyclopropyl-7-([S,S]-2,8-diazabicyclo[4,3,0]non-8-yl)-6-fluor-1,4-dihydro-8-methoxy-4-oxo-3-chinolincarbonsäure Hydrochlorid (CDCH), Verfahren zu dessen Herstellung und diese enthaltende pharmazeutische Zubereitungen
CA2252806C (en) 1996-06-07 2005-11-22 Eisai Co., Ltd. Polymorphs of donepezil hydrochloride and process for production
GB2346877B (en) 1997-11-12 2001-12-05 Bayer Ag 2-phenyl substituted imidazotriazinones as phosphodiesterase inhibitors
US6500987B1 (en) * 1998-11-27 2002-12-31 Teva Pharmaceutical Industries Ltd. Sertraline hydrochloride polymorphs
AU2001267916B2 (en) * 2000-07-06 2004-09-09 Daiichi Sankyo Company, Limited Hydropyridine derivative acid addition salts
CA2426158A1 (en) 2000-10-19 2002-06-13 Teva Pharmaceutical Industries Ltd. Crystalline venlafaxine base and novel polymorphs of venlafaxine hydrochloride, processes for preparing thereof
AU2002212340B2 (en) 2000-10-31 2006-12-14 Sandoz Ag Crystalline forms of venlafaxine hydrochloride
CZ297570B6 (cs) * 2000-12-25 2007-02-07 Sankyo Company, Limited Farmaceutický prípravek obsahující 2-acetoxypyridinový derivát a aspirin, které spolu pusobí v synergickém úcinku, kit jej obsahující a pouzití
DE10153345A1 (de) * 2001-10-29 2003-05-08 Gruenenthal Gmbh Substituierte 1H-Chinoxalin-2-on-Verbindungen und substituierte 4-Aryl- und 4-Heteroarylcyclohexan-Verbindungen
UA77234C2 (en) 2001-12-05 2006-11-15 Wyeth Corp Monohydrate of venlafaxine hydrochloride and methods for its preparation (variants)
DE10161818A1 (de) * 2001-12-14 2003-06-26 Gruenenthal Gmbh Substituierte 1,5-Diaminopentan-3-ol-Verbindungen
US7148231B2 (en) 2003-02-17 2006-12-12 Hoffmann-La Roche Inc. [6,7-Bis(2-methoxy-ethoxy)-quinazolin-4-yl]-(3-ethynyl-phenyl)amine hydrochloride polymorph
AU2003230192A1 (en) 2003-03-21 2004-10-11 Hetero Drugs Limited Novel crystalline forms of aripiprazole
WO2004098713A2 (en) * 2003-05-05 2004-11-18 Eli Lilly And Company Treating cardiovascular diseases with a compound of formula (i) (cs 747 - prasugrel; rn 150322-43-4)
WO2005054240A1 (en) 2003-11-20 2005-06-16 Chemi Spa Polymorphs of 1-cyclopropyl-7-([s,s]-2,8-diazadicyclo[4.3.0]non-8-yl)-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinoline carboxylic acid hydrochloride and methods for the preparation thereof
JP2008512417A (ja) * 2004-09-10 2008-04-24 ユセベ ファルマ ソシエテ アノニム シグマ受容体リガンド

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SU1757471A3 (ru) * 1988-07-13 1992-08-23 Крка, Товарна Здравил, Н.Сол., О. (Фирма) Способ получени производных L-аланил-L-пролина или их фармацевтически приемлемых солей
US6414002B1 (en) * 1999-09-22 2002-07-02 Bristol-Myers Squibb Company Substituted acid derivatives useful as antidiabetic and antiobesity agents and method
US20060025456A1 (en) * 2002-12-20 2006-02-02 Gruenenthal Gmbh Saturated and unsaturated heteroarylcycloalkylmethyl amines as anti-depressants
WO2005012285A1 (en) * 2003-08-05 2005-02-10 Matrix Laboratories Ltd An improved process for the preparation of moxifloxacin hydrochloride
WO2005108380A2 (en) * 2004-05-04 2005-11-17 Bristol-Myers Squibb Company Process employing controlled crystallization in forming crystals of a pharmaceutical
US20050288343A1 (en) * 2004-05-19 2005-12-29 Andrew Rusowicz Process of preparing substituted carbamates and intermediates thereof

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
J.C.TERRENCE, "Assessment of reductive animation route to methyl(3-nitrobenzyl)amine hydrochloride". Organic Process Research & Development, 2005, vol.9, pp.837-842. КАШУТИНА M.B. и др. Силилирование органических соединений. Успехи химии, 1975, т. XLIV, вып.9, с.1620-1648. WEISS R. et al. Geminal Bis-onio Substitution at trigonal electron-deficient carbon, Synthesis, 10, 1987, pp.870-872. G.NORONHA, Preparation of a new class of cleavable surfactants based on the silicon-carbon bond, Tetrahedron Letters, 40, 1999, pp.4935-4938. *

Also Published As

Publication number Publication date
US20100204470A1 (en) 2010-08-12
CN101484411A (zh) 2009-07-15
ES2335369T3 (es) 2010-03-25
SI2032521T1 (sl) 2010-02-26
EP2436381A1 (en) 2012-04-04
EP2145890B1 (en) 2012-08-01
RU2009102279A (ru) 2010-08-10
EP2032521A2 (en) 2009-03-11
EP2032521B1 (en) 2009-10-28
DK2032521T3 (da) 2010-01-25
DE602007003024D1 (de) 2009-12-10
EP2145890A2 (en) 2010-01-20
CA2655061A1 (en) 2008-01-03
EP2145890A3 (en) 2010-03-31
JP2009541385A (ja) 2009-11-26
PL2032521T3 (pl) 2010-05-31
ATE446946T1 (de) 2009-11-15
AU2007264030A1 (en) 2008-01-03
AU2007264030B2 (en) 2012-04-05
WO2008000418A2 (en) 2008-01-03
WO2008000418A3 (en) 2008-02-28

Similar Documents

Publication Publication Date Title
RU2461542C2 (ru) Новый способ получения соли
ES2390952T3 (es) Procedimiento para la preparación de 2-(N,N-dimetilamino)-propionato de dodecilo
RU2013133870A (ru) Оптически активное производное диазабициклооктана и способ его получения
JP2013136728A5 (ru)
CO5650237A2 (es) Procedimiento de sintesis selectiva de drivados de 2-amino-5-trifluorometil-pirimidina en presencia de un acido de lewis
JP2018522012A5 (ru)
JP2016204383A5 (ru)
BRPI0516735B1 (pt) métodos para produção de (r)-2-acetamido-n-benzil-3-metoxipropionamida (lacosamida) e de uma formulação farmacêutica, e uso de (r)-n-benzil-2-nboc-amino-3-metoxipropionamida (c-937)
RU2585762C2 (ru) Способ получения лакосамида
ES2364502T3 (es) Alquilación asimétrica de carbonilo.
ES2558856T3 (es) Síntesis de compuestos de pirrolidina
ES2922158T3 (es) Compuestos cristalinos
RU2021138005A (ru) Способы получения цитотоксических производных бензодиазепина
RU2006133312A (ru) Способ получения соединения 4-нитроимидазола
AR081890A1 (es) Procesos para la preparacion de cloruro de glicopirronio, composiciones farmaceuticas que lo contienen y su uso para tratar enfermedades respiratorias
PT2044021E (pt) Processo para preparar o remifentanilo, seus intermediários, utilização dos referidos intermediários e processos para a sua preparação
US8071808B2 (en) Processes for preparing a substituted gamma-amino acid
AR032433A1 (es) Proceso para la preparacion de un isomero de anillo de 5 miembros 3-sustituido y compuestos intermediarios utiles en el mismo
ES2358298T3 (es) Procedimiento para preparar haluros de alquilamonio cuaternario.
JP2009535327A (ja) ロピバカイン塩酸塩無水物およびその調製
JP5191267B2 (ja) スルホンイミド塩の精製方法
JP2006169251A5 (ru)
EA200900294A1 (ru) Кристаллический толтеродина тартрат и фармацевтическая композиция, содержащая его
JP2007031344A5 (ru)
JP2013129607A5 (ru)

Legal Events

Date Code Title Description
MM4A The patent is invalid due to non-payment of fees

Effective date: 20130626