EA200500420A1 - Бензолсульфонатные соли производных 4-фтор-2-цианопирролидина - Google Patents

Бензолсульфонатные соли производных 4-фтор-2-цианопирролидина

Info

Publication number
EA200500420A1
EA200500420A1 EA200500420A EA200500420A EA200500420A1 EA 200500420 A1 EA200500420 A1 EA 200500420A1 EA 200500420 A EA200500420 A EA 200500420A EA 200500420 A EA200500420 A EA 200500420A EA 200500420 A1 EA200500420 A1 EA 200500420A1
Authority
EA
Eurasian Patent Office
Prior art keywords
benzolsulphonate
cyanopyrrolidine
fluor
stability
salts derivatives
Prior art date
Application number
EA200500420A
Other languages
English (en)
Other versions
EA007613B1 (ru
Inventor
Хироси Фукусима
Акира Хиратате
Масато Такахаси
Казуя Камео
Original Assignee
Тайсо Фармасьютикал Ко., Лтд.
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
Application filed by Тайсо Фармасьютикал Ко., Лтд. filed Critical Тайсо Фармасьютикал Ко., Лтд.
Publication of EA200500420A1 publication Critical patent/EA200500420A1/ru
Publication of EA007613B1 publication Critical patent/EA007613B1/ru

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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 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
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Immunology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Соль бензолсульфонат (2S,4S)-2-циано-4-фтор-1-[(2-гидрокси-1,1-диметил)этиламино]ацетилпирролидина, которая имеет превосходную активность ингибирования ДПП IV, а также физические свойства (например, стабильность), необходимые для фармацевтических препаратов. Настоящее изобретение позволяет легко получить соединение в виде высокочистого однородного кристалла с превосходной стабильностью в твердом состоянии.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200500420A 2002-08-29 2003-08-27 Бензолсульфонатная соль (2s,4s)-1-циано-4-фтор-1-[(2-гидрокси-1,1-диметил)этиламино]ацетилпирролидина EA007613B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2002249821 2002-08-29
PCT/JP2003/010828 WO2004020407A1 (ja) 2002-08-29 2003-08-27 ４−フルオロ−２−シアノピロリジン誘導体ベンゼンスルホン酸塩

Publications (2)

Publication Number Publication Date
EA200500420A1 true EA200500420A1 (ru) 2005-08-25
EA007613B1 EA007613B1 (ru) 2006-12-29

Family

ID=31972599

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200500420A EA007613B1 (ru) 2002-08-29 2003-08-27 Бензолсульфонатная соль (2s,4s)-1-циано-4-фтор-1-[(2-гидрокси-1,1-диметил)этиламино]ацетилпирролидина

Country Status (19)

Country Link
US (1) US7304166B2 (ru)
EP (1) EP1535907A4 (ru)
JP (1) JP3746063B2 (ru)
KR (1) KR100582141B1 (ru)
CN (1) CN1310885C (ru)
AU (1) AU2003261748B2 (ru)
BR (1) BR0313831A (ru)
CA (1) CA2496623C (ru)
EA (1) EA007613B1 (ru)
EC (1) ECSP055708A (ru)
HK (1) HK1082497A1 (ru)
HR (1) HRP20050205A2 (ru)
MX (1) MXPA05002253A (ru)
NO (1) NO20050867L (ru)
NZ (1) NZ538956A (ru)
PL (1) PL374664A1 (ru)
UA (1) UA78104C2 (ru)
WO (1) WO2004020407A1 (ru)
ZA (1) ZA200501418B (ru)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DOP2006000008A (es) 2005-01-10 2006-08-31 Arena Pharm Inc Terapia combinada para el tratamiento de la diabetes y afecciones relacionadas y para el tratamiento de afecciones que mejoran mediante un incremento de la concentración sanguínea de glp-1
US20080114053A1 (en) 2005-01-27 2008-05-15 Mitsui Chemicals, Inc. Method for Producing Fluorinated Proline Derivative
JP2008024592A (ja) * 2005-01-28 2008-02-07 Taisho Pharmaceut Co Ltd シアノピロリジン誘導体含有固形製剤用組成物、それを含有する固形製剤及びその製造方法
CA2600203C (en) 2005-03-22 2012-12-04 F.Hoffmann-La Roche Ag New salt and polymorphs of a dpp-iv inhibitor
RS52110B2 (sr) 2005-09-14 2018-05-31 Takeda Pharmaceuticals Co Inhibitori dipeptidil peptidaze za lečenje dijabetesa
CN101360723A (zh) 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
WO2007112347A1 (en) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
PE20071221A1 (es) 2006-04-11 2007-12-14 Arena Pharm Inc Agonistas del receptor gpr119 en metodos para aumentar la masa osea y para tratar la osteoporosis y otras afecciones caracterizadas por masa osea baja, y la terapia combinada relacionada a estos agonistas
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
KR101361427B1 (ko) 2007-04-03 2014-02-10 미쓰비시 타나베 파마 코퍼레이션 디펩티딜 펩티다아제 4 저해 화합물과 감미료와의 병용
CL2008003653A1 (es) * 2008-01-17 2010-03-05 Mitsubishi Tanabe Pharma Corp Uso de un inhibidor de sglt derivado de glucopiranosilo y un inhibidor de dppiv seleccionado para tratar la diabetes; y composicion farmaceutica.
EP2146210A1 (en) 2008-04-07 2010-01-20 Arena Pharmaceuticals, Inc. Methods of using A G protein-coupled receptor to identify peptide YY (PYY) secretagogues and compounds useful in the treatment of conditions modulated by PYY
AR077642A1 (es) 2009-07-09 2011-09-14 Arena Pharm Inc Moduladores del metabolismo y el tratamiento de trastornos relacionados con el mismo
EP2556056A1 (en) 2010-04-06 2013-02-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
EA201390421A1 (ru) 2010-09-22 2013-09-30 Арена Фармасьютикалз, Инк. Модуляторы рецептора gpr119 и лечение связанных с ним нарушений
US20140018371A1 (en) 2011-04-01 2014-01-16 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012145361A1 (en) 2011-04-19 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2012145603A1 (en) 2011-04-22 2012-10-26 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
US20140051714A1 (en) 2011-04-22 2014-02-20 Arena Pharmaceuticals, Inc. Modulators Of The GPR119 Receptor And The Treatment Of Disorders Related Thereto
WO2012170702A1 (en) 2011-06-08 2012-12-13 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2013055910A1 (en) 2011-10-12 2013-04-18 Arena Pharmaceuticals, Inc. Modulators of the gpr119 receptor and the treatment of disorders related thereto
WO2014074668A1 (en) 2012-11-08 2014-05-15 Arena Pharmaceuticals, Inc. Modulators of gpr119 and the treatment of disorders related thereto
JP2018507914A (ja) 2015-03-09 2018-03-22 インテクリン・セラピューティクス・インコーポレイテッド 非アルコール性脂肪肝疾患および／またはリポジストロフィーの処置のための方法
JP2020515639A (ja) 2017-04-03 2020-05-28 コヒラス・バイオサイエンシズ・インコーポレイテッド 進行性核上性麻痺の処置のためのＰＰＡＲγアゴニスト

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4432987A (en) 1982-04-23 1984-02-21 Pfizer Inc. Crystalline benzenesulfonate salts of sultamicillin
GB8608335D0 (en) 1986-04-04 1986-05-08 Pfizer Ltd Pharmaceutically acceptable salts
TW492957B (en) * 1996-11-07 2002-07-01 Novartis Ag N-substituted 2-cyanopyrrolidnes
US6011155A (en) * 1996-11-07 2000-01-04 Novartis Ag N-(substituted glycyl)-2-cyanopyrrolidines, pharmaceutical compositions containing them and their use in inhibiting dipeptidyl peptidase-IV
TW486475B (en) 1996-12-26 2002-05-11 Ube Industries Acid addition salt of optically active piperidine compound and process for preparing the same
JP3107784B2 (ja) 1996-12-26 2000-11-13 宇部興産株式会社 光学活性ピペリジン誘導体の酸付加塩及びその製法
US6252063B1 (en) 1998-12-01 2001-06-26 Merck & Co., Inc. Crystalline salts of a carbapenem antibiotic
TWI243162B (en) 2000-11-10 2005-11-11 Taisho Pharmaceutical Co Ltd Cyanopyrrolidine derivatives

Also Published As

Publication number Publication date
US7304166B2 (en) 2007-12-04
WO2004020407A1 (ja) 2004-03-11
EP1535907A1 (en) 2005-06-01
UA78104C2 (en) 2007-02-15
CN1310885C (zh) 2007-04-18
AU2003261748A1 (en) 2004-03-19
KR100582141B1 (ko) 2006-05-22
US20060106087A1 (en) 2006-05-18
CN1678575A (zh) 2005-10-05
JPWO2004020407A1 (ja) 2005-12-15
NO20050867L (no) 2005-02-18
ZA200501418B (en) 2006-10-25
EP1535907A4 (en) 2006-11-29
CA2496623C (en) 2008-02-12
HRP20050205A2 (en) 2005-10-31
MXPA05002253A (es) 2005-06-08
EA007613B1 (ru) 2006-12-29
CA2496623A1 (en) 2004-03-11
KR20050059094A (ko) 2005-06-17
HK1082497A1 (en) 2006-06-09
JP3746063B2 (ja) 2006-02-15
NZ538956A (en) 2006-08-31
ECSP055708A (es) 2005-08-11
AU2003261748B2 (en) 2006-11-23
PL374664A1 (en) 2005-10-31
BR0313831A (pt) 2005-07-05

Similar Documents

Publication Publication Date Title
EA200500420A1 (ru) Бензолсульфонатные соли производных 4-фтор-2-цианопирролидина
NO20052884L (no) Substituerte indolpyridinforbindelser som anti-infeksjonsmidler.
EA200301289A1 (ru) Новые производные пиррола в качестве фармацевтических средств
EA200500312A1 (ru) Новые спироконденсированные хиназолиноны и их применение в качестве ингибиторов фосфодиэстераз
EA200500203A1 (ru) Новый способ синтеза и новая кристаллическая форма агомелатина и фармацевтические композиции, которые её содержат
EA200401526A1 (ru) Новые соединения и их применение
EA200300211A1 (ru) Азабициклические соединения, способ их получения и их применение в качестве лекарственных средств, в частности в качестве антибактериальных средств
AR057325A1 (es) Sintesis de (s)-n-metilnaltrexona, composiciones farmaceuticas y usos
CR7950A (es) Sintesis de los cloruros de 4amino -2butenoilo y su uso en la preparacion of 3- cianoquinolinas
RU2014105650A (ru) Производное азабензимидазола, обладающее амрк-активирующей активностью
BR0206433A (pt) Composto, composição farmacêutica, processo para a prepapação de um composto, e, uso de um composto
AR049401A1 (es) Aza-biciclononanos
EA200300103A1 (ru) НОВАЯ β КРИСТАЛЛИЧЕСКАЯ ФОРМА ТРЕТ-БУТИЛАМИНОВОЙ СОЛИ ПЕРИНДОПРИЛА, СПОСОБ ЕЕ ПОЛУЧЕНИЯ И СОДЕРЖАЩИЕ ЕЕ ФАРМАЦЕВТИЧЕСКИЕ КОМПОЗИЦИИ
NO20054787D0 (no) Indenderivater som farmasotiske midler
EA200702375A1 (ru) Производные мочевины, способы их получения и применения
DK1467706T3 (da) Dermalt applikationssystem for aminolevulinsyre-derivater
BRPI0408353A (pt) composto, composição farmacêutica, métodos para o tratamento de neoplasias suscetìveis e para o tratamento de infecções virais, e, uso de um composto
PA8575601A1 (es) Procedimiento para su preparacion, medicamentos que comprenden estos compuestos y su uso
EA200600605A1 (ru) Перегруппированные пентанолы, способ их получения и их применение в качестве противовоспалительных средств
CR9391A (es) Derivados de indanil-piperazinas, su procedimiento de preparacion y las composiciones farmaceuticas que los contienen
EA200500690A1 (ru) Новые соединения пиридопиримидинона, способ их получения и фармацевтические композиции, которые их содержат
EA200600760A1 (ru) Новые соединения фенилпиридилпиперазина, способ их получения и фармацевтические композиции, содержащие их
ECSP034531A (es) Derivados sustituidos de c-ciclohexilmetilamina
EA200400848A1 (ru) Производные триазолохинолина, применимые в качестве лигандов аденозиновых рецепторов
EA200801137A1 (ru) Соединения для ингибирования апоптоза

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): RU