HUP0104029A2 - A 3-(2,4-diklór-benzil)-2-metil-N-(pentil-szulfonil)-3H-benzimidazol-5-karboxamid új kristályformái és azokat hatóanyagként tartalmazó gyógyszerkészítmények - Google Patents

A 3-(2,4-diklór-benzil)-2-metil-N-(pentil-szulfonil)-3H-benzimidazol-5-karboxamid új kristályformái és azokat hatóanyagként tartalmazó gyógyszerkészítmények

Info

Publication number
HUP0104029A2
HUP0104029A2 HU0104029A HUP0104029A HUP0104029A2 HU P0104029 A2 HUP0104029 A2 HU P0104029A2 HU 0104029 A HU0104029 A HU 0104029A HU P0104029 A HUP0104029 A HU P0104029A HU P0104029 A2 HUP0104029 A2 HU P0104029A2
Authority
HU
Hungary
Prior art keywords
approximately
pentylsulfonyl
dichlorobenzyl
benzimidazole
methyl
Prior art date
Application number
HU0104029A
Other languages
English (en)
Inventor
Takafumi Imoto
Kunihiko Mititsu
Yoshiyuki Murai
Masahiro Nishikawa
Noritsugu Yamasaki
Original Assignee
Daicel Chemical Industries, Ltd.
Fujisawa Pharmaceutical Co., Ltd.
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 Daicel Chemical Industries, Ltd., Fujisawa Pharmaceutical Co., Ltd. filed Critical Daicel Chemical Industries, Ltd.
Publication of HUP0104029A2 publication Critical patent/HUP0104029A2/hu
Publication of HUP0104029A3 publication Critical patent/HUP0104029A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/24—Benzimidazoles; Hydrogenated benzimidazoles 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10—Radicals substituted by halogen atoms or nitro radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Reproductive Health (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

A találmány vércukorszint-csökkentő vagy PDE5-gátló hatássalrendelkező 3-(2,4-diklór-benzil)-2-metil-N-(pentil-szulfonil)-3H-benzimidazol-5-karboxamid kristályformáira és az ezeket a formákathatóanyagként tartalmazó gyógyszerkészítményekre vonatkozik. A 3-(2,4-diklór-benzil)-2-metil-N-(pentil-szulfonil)-3H-benzimidazol-5-karboxamidnak a találmány szerinti két, lényegileg és kristálytaniszempontból tiszta kristályformájának pormintái a CuK ALFA-sugaraknakmint karakterisztikus röntgensugaraknak az alkalmazásával elvégzettröntgendiffrakciós vizsgálat szerint a következő, <0,2°hibatartománnyal megadott 28 röntgendiffrakciós értékeket mutatják:körülbelül 4,7°, körülbelül 9,5°, körülbelül 10,5°, körülbelül 15,6°és körülbelül 18,4°, illetve körülbelül 4,4°, körülbelül 8,9° éskörülbelül 13,4°. A találmány szerinti gyógyszerkészítményekhatóanyagként az említett két kristályforma egyikét tartalmazzák. Ó
HU0104029A 1998-11-13 1999-11-11 New crystalline forms of 3-(2,4-dichlorobenzyl)-2-methyl-n-(pentylsulfonyl)-3h-benzimidazole-5-carboxamide and medicaments containing them HUP0104029A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
JP32402698 1998-11-13

Publications (2)

Publication Number Publication Date
HUP0104029A2 true HUP0104029A2 (hu) 2002-05-29
HUP0104029A3 HUP0104029A3 (en) 2002-07-29

Family

ID=18161331

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0104029A HUP0104029A3 (en) 1998-11-13 1999-11-11 New crystalline forms of 3-(2,4-dichlorobenzyl)-2-methyl-n-(pentylsulfonyl)-3h-benzimidazole-5-carboxamide and medicaments containing them

Country Status (11)

Country Link
US (1) US6703410B1 (hu)
EP (2) EP1132087A4 (hu)
KR (1) KR20010080444A (hu)
CN (1) CN1136196C (hu)
AU (1) AU764594B2 (hu)
BR (1) BR9915315A (hu)
CA (1) CA2350520A1 (hu)
HK (1) HK1040078B (hu)
HU (1) HUP0104029A3 (hu)
RU (1) RU2228931C2 (hu)
WO (2) WO2000028991A1 (hu)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000028991A1 (fr) 1998-11-13 2000-05-25 Fujisawa Pharmaceutical Co., Ltd. Remedes contre le syndrome des ovaires polykystiques
WO2000039099A1 (fr) * 1998-12-24 2000-07-06 Fujisawa Pharmaceutical Co., Ltd. Derives de benzimidazole
ATE374028T1 (de) * 2001-03-27 2007-10-15 Dainippon Sumitomo Pharma Co Kristallines isoxazol-derivat und medizinisches präparat daraus
CA2475377A1 (en) * 2002-02-07 2003-08-14 Pfizer Inc. Use of pde5 inhibitors such as sildenafil in the treatment of polycystic ovary syndrome
EP1581247A4 (en) * 2002-12-11 2007-09-12 Amylin Pharmaceuticals Inc METHODS AND COMPOSITIONS FOR TREATING STEIN-LEVENTHAL SYNDROME
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
US20080194860A1 (en) * 2006-10-10 2008-08-14 Transform Pharmaceuticals, Inc. Novel crystal of (s)-(+)-2-(2-chlorophenyl)-2-hydroxy-ethyl carbamate
CA2769508C (en) 2009-07-30 2020-01-07 Aestus Therapeutics, Inc. Methods of treating neuropathic pain with benzimidazole derivative agonists of ppargamma

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3342874B2 (ja) 1995-04-21 2002-11-11 ニューロサーチ、アクティーゼルスカブ ベンズイミダゾール化合物、およびｇａｂａａレセプター複合体モジュレーターとしてのその使用
CZ293016B6 (cs) * 1995-06-01 2004-01-14 Sankyo Company Limited Benzimidazolové deriváty a farmaceutické prostředky s jejich obsahem
JPH09165371A (ja) * 1995-10-09 1997-06-24 Sankyo Co Ltd 複素環化合物を含有する医薬
ATE303365T1 (de) 1995-12-28 2005-09-15 Fujisawa Pharmaceutical Co Benzimidazolderivate
AU4400597A (en) * 1996-10-08 1998-05-05 Fujisawa Pharmaceutical Co., Ltd. Indole derivatives
JP3268242B2 (ja) * 1996-11-14 2002-03-25 三共株式会社 縮合複素環化合物を含有する医薬
TW453999B (en) * 1997-06-27 2001-09-11 Fujisawa Pharmaceutical Co Benzimidazole derivatives
CN1150167C (zh) * 1998-04-06 2004-05-19 藤泽药品工业株式会社 吲哚衍生物
WO2000028991A1 (fr) 1998-11-13 2000-05-25 Fujisawa Pharmaceutical Co., Ltd. Remedes contre le syndrome des ovaires polykystiques

Also Published As

Publication number Publication date
RU2228931C2 (ru) 2004-05-20
WO2000028991A1 (fr) 2000-05-25
HUP0104029A3 (en) 2002-07-29
CN1330641A (zh) 2002-01-09
EP1138674A1 (en) 2001-10-04
WO2000029383A1 (fr) 2000-05-25
AU1178300A (en) 2000-06-05
HK1040078A1 (en) 2002-05-24
EP1138674A4 (en) 2002-08-21
CN1136196C (zh) 2004-01-28
US6703410B1 (en) 2004-03-09
HK1040078B (zh) 2004-07-09
CA2350520A1 (en) 2000-05-25
AU764594B2 (en) 2003-08-21
KR20010080444A (ko) 2001-08-22
BR9915315A (pt) 2001-08-07
EP1132087A4 (en) 2002-06-26
EP1132087A1 (en) 2001-09-12

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Legal Events

Date Code Title Description
GB9A Succession in title

Owner name: DAICEL CHEMICAL INDUSTRIES, LTD., JP

Free format text: FORMER OWNER(S): FUJISAWA PHARMACEUTICAL CO., LTD., JP; DAICEL CHEMICAL INDUSTRIES, LTD., JP; YAMANOUCHI PHARMACEUTICAL CO., LTD., JP

Owner name: ASTELLAS PHARMA INC., JP

Free format text: FORMER OWNER(S): FUJISAWA PHARMACEUTICAL CO., LTD., JP; DAICEL CHEMICAL INDUSTRIES, LTD., JP; YAMANOUCHI PHARMACEUTICAL CO., LTD., JP