TWI427062B - Ｎ－（２－胺基苯基）－４－〔ｎ－（吡啶－３－基）－甲氧羰基－胺基甲基〕－苯甲醯胺（ｍｓ－２７５）之多晶形ｂ - Google Patents

Ｎ－（２－胺基苯基）－４－〔ｎ－（吡啶－３－基）－甲氧羰基－胺基甲基〕－苯甲醯胺（ｍｓ－２７５）之多晶形ｂ Download PDF

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Publication number
TWI427062B
TWI427062B TW098129170A TW98129170A TWI427062B TW I427062 B TWI427062 B TW I427062B TW 098129170 A TW098129170 A TW 098129170A TW 98129170 A TW98129170 A TW 98129170A TW I427062 B TWI427062 B TW I427062B
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TW
Taiwan
Prior art keywords
aminophenyl
methoxycarbonyl
pyridin
aminomethyl
benzamide
Prior art date
Application number
TW098129170A
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English (en)
Chinese (zh)
Other versions
TW201014820A (en
Inventor
馬夏司 史耐德
麥可 葛福德
珍斯 吉斯勒
加布立爾 溫特
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拜耳知識產權公司
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Application filed by 拜耳知識產權公司 filed Critical 拜耳知識產權公司
Publication of TW201014820A publication Critical patent/TW201014820A/zh
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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P37/08—Antiallergic agents
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Diabetes (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Transplantation (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
TW098129170A 2008-08-29 2009-08-28 Ｎ－（２－胺基苯基）－４－〔ｎ－（吡啶－３－基）－甲氧羰基－胺基甲基〕－苯甲醯胺（ｍｓ－２７５）之多晶形ｂ TWI427062B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9304608P 2008-08-29 2008-08-29
EP08163274 2008-08-29

Publications (2)

Publication Number Publication Date
TW201014820A TW201014820A (en) 2010-04-16
TWI427062B true TWI427062B (zh) 2014-02-21

Family

ID=41133825

Family Applications (1)

Application Number Title Priority Date Filing Date
TW098129170A TWI427062B (zh) 2008-08-29 2009-08-28 Ｎ－（２－胺基苯基）－４－〔ｎ－（吡啶－３－基）－甲氧羰基－胺基甲基〕－苯甲醯胺（ｍｓ－２７５）之多晶形ｂ

Country Status (35)

Country Link
US (2) US7973166B2 (enExample)
EP (1) EP2350005B1 (enExample)
JP (1) JP4921616B2 (enExample)
KR (1) KR101073760B1 (enExample)
CN (1) CN102137846B (enExample)
AR (1) AR073226A1 (enExample)
AT (1) ATE538094T1 (enExample)
AU (1) AU2009286982C1 (enExample)
BR (1) BRPI0918580B8 (enExample)
CA (1) CA2735294C (enExample)
CO (1) CO6351736A2 (enExample)
CR (2) CR20110107A (enExample)
CY (1) CY1112645T1 (enExample)
DK (1) DK2350005T3 (enExample)
DO (1) DOP2011000064A (enExample)
EA (1) EA016811B1 (enExample)
EC (1) ECSP11010849A (enExample)
ES (1) ES2378640T3 (enExample)
HN (1) HN2011000609A (enExample)
HR (1) HRP20120183T8 (enExample)
IL (1) IL211276A (enExample)
MA (1) MA32610B1 (enExample)
MX (1) MX2011002248A (enExample)
MY (1) MY149058A (enExample)
NZ (1) NZ591387A (enExample)
PE (2) PE20110677A1 (enExample)
PL (1) PL2350005T3 (enExample)
PT (1) PT2350005E (enExample)
RS (1) RS52164B (enExample)
SI (1) SI2350005T1 (enExample)
SM (1) SMT201200026B (enExample)
SV (1) SV2011003846A (enExample)
TW (1) TWI427062B (enExample)
WO (1) WO2010022988A1 (enExample)
ZA (1) ZA201102285B (enExample)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RS52164B (sr) 2008-08-29 2012-08-31 Bayer Pharma Aktiengesellschaft N-(2-aminofenil)-4-[n-(piridin-3-il)-metoksikarbonilaminometil]-benzamid (ms-275)polimorf b
US8221753B2 (en) 2009-09-30 2012-07-17 Tracon Pharmaceuticals, Inc. Endoglin antibodies
FR2977492B1 (fr) * 2011-07-04 2013-07-05 Servier Lab Nouvelle association entre le n-hydroxy-4-{2-[3-(n,n-dimethylaminomethyl) benzofuran-2-ylcarbonylamino]ethoxy}benzamide et le folfox
UA115789C2 (uk) 2012-09-05 2017-12-26 Трейкон Фармасутікалз, Інк. Композиція антитіла до cd105 та її застосування
AU2015346444A1 (en) 2014-11-12 2017-05-04 Tracon Pharmaceuticals, Inc. Anti-endoglin antibodies and uses thereof
US9926375B2 (en) 2014-11-12 2018-03-27 Tracon Pharmaceuticals, Inc. Anti-endoglin antibodies and uses thereof
EP3168210A1 (en) 2015-11-13 2017-05-17 Sandoz Ag Crystalline forms of entinostat
WO2017216761A1 (en) * 2016-06-17 2017-12-21 Dr. Reddy's Laboratories Limited Solid forms of entinostat
CN110944978A (zh) * 2017-07-28 2020-03-31 杭州领业医药科技有限公司 含恩替诺特的化合物,其化合物晶型及其制备方法和药物组合物
CA3218617A1 (en) 2021-05-10 2022-11-17 Thierry Bonnaud Novel forms of entinostat

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0847992A1 (en) * 1996-09-30 1998-06-17 Mitsui Chemicals, Inc. Benzamide derivatives, useful as cell differentiation inducers
JP2001131130A (ja) * 1999-11-09 2001-05-15 Mitsui Chemicals Inc モノアシルフェニレンジアミン誘導体の精製法

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP3354090B2 (ja) * 1996-09-30 2002-12-09 シエーリング アクチエンゲゼルシャフト 分化誘導剤
US6320078B1 (en) * 1998-07-24 2001-11-20 Mitsui Chemicals, Inc. Method of producing benzamide derivatives
JP4030683B2 (ja) * 1998-07-24 2008-01-09 三井化学株式会社 ベンズアミド誘導体の合成法
JP2001064177A (ja) * 1999-08-16 2001-03-13 Schering Ag ベンズアミド誘導体を有効成分とする製剤
PE20050206A1 (es) * 2003-05-26 2005-03-26 Schering Ag Composicion farmaceutica que contiene un inhibidor de histona deacetilasa
RS52164B (sr) 2008-08-29 2012-08-31 Bayer Pharma Aktiengesellschaft N-(2-aminofenil)-4-[n-(piridin-3-il)-metoksikarbonilaminometil]-benzamid (ms-275)polimorf b

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0847992A1 (en) * 1996-09-30 1998-06-17 Mitsui Chemicals, Inc. Benzamide derivatives, useful as cell differentiation inducers
JP2001131130A (ja) * 1999-11-09 2001-05-15 Mitsui Chemicals Inc モノアシルフェニレンジアミン誘導体の精製法

Also Published As

Publication number Publication date
CY1112645T1 (el) 2016-02-10
EP2350005B1 (en) 2011-12-21
SV2011003846A (es) 2011-07-27
DK2350005T3 (da) 2012-03-19
CN102137846B (zh) 2014-04-23
ZA201102285B (en) 2011-12-28
KR101073760B1 (ko) 2011-10-13
JP4921616B2 (ja) 2012-04-25
US20100056585A1 (en) 2010-03-04
PE20141062A1 (es) 2014-09-19
KR20110038187A (ko) 2011-04-13
MY149058A (en) 2013-07-15
PE20110677A1 (es) 2011-09-16
MX2011002248A (es) 2011-03-29
HRP20120183T1 (hr) 2012-03-31
ECSP11010849A (es) 2011-03-31
HRP20120183T8 (en) 2012-11-30
CR20110107A (es) 2011-04-28
CA2735294A1 (en) 2010-03-04
EP2350005A1 (en) 2011-08-03
NZ591387A (en) 2012-03-30
RS52164B (sr) 2012-08-31
PT2350005E (pt) 2012-03-12
PL2350005T3 (pl) 2012-05-31
US7973166B2 (en) 2011-07-05
CA2735294C (en) 2013-10-15
SI2350005T1 (sl) 2012-03-30
JP2012500819A (ja) 2012-01-12
SMT201200026B (it) 2012-07-10
AU2009286982B2 (en) 2011-06-23
USRE45499E1 (en) 2015-04-28
HK1160107A1 (en) 2012-08-10
CO6351736A2 (es) 2011-12-20
AR073226A1 (es) 2010-10-20
ES2378640T3 (es) 2012-04-16
WO2010022988A1 (en) 2010-03-04
CR20160465A (es) 2016-12-06
AU2009286982A1 (en) 2010-03-04
MA32610B1 (fr) 2011-09-01
IL211276A (en) 2014-07-31
DOP2011000064A (es) 2011-03-31
BRPI0918580B1 (pt) 2020-11-24
IL211276A0 (en) 2011-04-28
HN2011000609A (es) 2014-09-29
BRPI0918580A8 (pt) 2017-07-11
CN102137846A (zh) 2011-07-27
AU2009286982C1 (en) 2012-04-26
EA016811B1 (ru) 2012-07-30
ATE538094T1 (de) 2012-01-15
EA201100354A1 (ru) 2011-10-31
TW201014820A (en) 2010-04-16
BRPI0918580B8 (pt) 2021-05-25
BRPI0918580A2 (pt) 2015-12-01

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