IN2012DN01152A - 2-[[[2-[(hydroxyacetyl)amino]-4-pyridinyl]methyl]thio]-n-[4-(trifluoromethoxy)phenyl]-3-pyridinecarboxamide benzenesulfonate crystal of same crystal polymorph thereof and methods for production thereof - Google Patents

2-[[[2-[(hydroxyacetyl)amino]-4-pyridinyl]methyl]thio]-n-[4-(trifluoromethoxy)phenyl]-3-pyridinecarboxamide benzenesulfonate crystal of same crystal polymorph thereof and methods for production thereof

Info

Publication number
IN2012DN01152A
IN2012DN01152A IN1152DEN2012A IN2012DN01152A IN 2012DN01152 A IN2012DN01152 A IN 2012DN01152A IN 1152DEN2012 A IN1152DEN2012 A IN 1152DEN2012A IN 2012DN01152 A IN2012DN01152 A IN 2012DN01152A
Authority
IN
India
Prior art keywords
compound
hydroxyacetyl
trifluoromethoxy
pyridinyl
thio
Prior art date
Application number
Inventor
Niwa Masashi
Deguchi Hiroshi
Original Assignee
Santen 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 Santen Pharmaceutical Co Ltd filed Critical Santen Pharmaceutical Co Ltd
Publication of IN2012DN01152A publication Critical patent/IN2012DN01152A/en

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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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • 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
    • C07D213/60—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 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

Abstract

In the course of developing 2-[[[2 - [(hydroxyacetyl) amino]- 4 -pyridinyl] methyl] thio]- N -[4 -(trifluoromethoxy) phenyl]- 3 -pyridinecarboxamide(compound A)  there are the multiple problems: 1) compound A or its salt is difficult to be recrystallized  the storage stability largely differs depending on the kind of the salt  and it is very difficult to obtain a salt of compound A having excellent storage stability; 2) in a crystallization process of compound A  it is very difficult to control a crystal polymorph  and 3) compound A (free body) causes mineral deposition in the stomach when it is orally administered repeatedly.
IN1152DEN2012 2009-07-17 2010-07-16 2-[[[2-[(hydroxyacetyl)amino]-4-pyridinyl]methyl]thio]-n-[4-(trifluoromethoxy)phenyl]-3-pyridinecarboxamide benzenesulfonate crystal of same crystal polymorph thereof and methods for production thereof IN2012DN01152A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2009169130 2009-07-17
PCT/JP2010/062071 WO2011007870A1 (en) 2009-07-17 2010-07-16 2-[[[2-[(hydroxyacetyl)amino]-4-pyridinyl]methyl]thio]-n-[4-(trifluoromethoxy)phenyl]-3-pyridinecarboxamide benzene- sulfonate, crystals of same, polymorphs thereof, and processes for production thereof

Publications (1)

Publication Number Publication Date
IN2012DN01152A true IN2012DN01152A (en) 2015-04-10

Family

ID=43449480

Family Applications (1)

Application Number Title Priority Date Filing Date
IN1152DEN2012 IN2012DN01152A (en) 2009-07-17 2010-07-16 2-[[[2-[(hydroxyacetyl)amino]-4-pyridinyl]methyl]thio]-n-[4-(trifluoromethoxy)phenyl]-3-pyridinecarboxamide benzenesulfonate crystal of same crystal polymorph thereof and methods for production thereof

Country Status (17)

Country Link
US (4) US9029398B2 (en)
EP (1) EP2455368B1 (en)
JP (1) JP5662719B2 (en)
KR (1) KR101710740B1 (en)
CN (1) CN102471273B (en)
AU (1) AU2010271746B2 (en)
BR (1) BR112012001159A2 (en)
CA (1) CA2767992C (en)
EA (1) EA019689B1 (en)
ES (1) ES2554360T3 (en)
HK (2) HK1167644A1 (en)
IN (1) IN2012DN01152A (en)
MX (1) MX2012000749A (en)
MY (1) MY157122A (en)
NZ (1) NZ597495A (en)
SG (1) SG177576A1 (en)
WO (1) WO2011007870A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2014DN06911A (en) 2012-01-31 2015-05-15 Santen Pharmaceutical Co Ltd
MX2016003566A (en) 2013-09-20 2016-06-02 Santen Pharmaceutical Co Ltd Polyethylene glycol-containing composition.
TW201609145A (en) 2013-12-25 2016-03-16 參天製藥股份有限公司 Injectable agent and depot formation method
RU2726625C2 (en) * 2015-03-17 2020-07-15 Сантен Фармасьютикал Ко., Лтд. Pharmaceutical composition comprising a polypeptide
WO2016148227A1 (en) * 2015-03-18 2016-09-22 参天製薬株式会社 Stable storage of pharmaceutical composition
JP2016175900A (en) * 2015-03-18 2016-10-06 参天製薬株式会社 Sustained-release pharmaceutical composition
WO2016178900A1 (en) * 2015-05-01 2016-11-10 Odin Biotech Ocular implant for delivery of pyridinecarboxamide derivative

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4626353B2 (en) * 2004-02-17 2011-02-09 参天製薬株式会社 Novel cyclic compound having a 4-pyridylalkylthio group having a substituted or unsubstituted amino group introduced
ES2368153T3 (en) 2004-02-17 2011-11-14 Santen Pharmaceutical Co., Ltd. NEW CYCLIC COMPOUND PRESENTING A 4-PIRIDILALQUILTIO GROUP THAT PRESENTS AMINO (NOT) REPLACED INTRODUCED IN THE SAME.
NZ548949A (en) * 2004-02-17 2009-09-25 Santen Pharmaceutical Co Ltd Novel cyclic compound having 4-pyridylalkylthio group having substituted or unsubstituted amino group introduced therein
WO2006106914A1 (en) 2005-03-31 2006-10-12 Santen Pharmaceutical Co., Ltd. Novel cyclic compound having pyrimidinylalkylthio group
JP4834441B2 (en) * 2005-03-31 2011-12-14 参天製薬株式会社 Novel cyclic compounds having pyrimidinylalkylthio groups

Also Published As

Publication number Publication date
ES2554360T3 (en) 2015-12-18
US20150291560A1 (en) 2015-10-15
MX2012000749A (en) 2012-01-27
US20170081286A1 (en) 2017-03-23
US20120116088A1 (en) 2012-05-10
NZ597495A (en) 2013-08-30
MY157122A (en) 2016-05-13
HK1167644A1 (en) 2012-12-07
CN102471273B (en) 2014-07-16
EA019689B1 (en) 2014-05-30
CA2767992A1 (en) 2011-01-20
EA201200146A1 (en) 2012-06-29
US9359328B2 (en) 2016-06-07
AU2010271746B2 (en) 2014-07-03
KR20130025857A (en) 2013-03-12
EP2455368A1 (en) 2012-05-23
AU2010271746A1 (en) 2012-02-02
CA2767992C (en) 2017-03-21
JP5662719B2 (en) 2015-02-04
KR101710740B1 (en) 2017-02-27
EP2455368B1 (en) 2015-09-16
WO2011007870A1 (en) 2011-01-20
US9902698B2 (en) 2018-02-27
BR112012001159A2 (en) 2016-03-01
SG177576A1 (en) 2012-02-28
HK1167647A1 (en) 2012-12-07
CN102471273A (en) 2012-05-23
EP2455368A4 (en) 2013-01-09
US9029398B2 (en) 2015-05-12
JP2011037844A (en) 2011-02-24
US20160251314A1 (en) 2016-09-01
US9546140B2 (en) 2017-01-17

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