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

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/14Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/32Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of salts of sulfonic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/28Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/78Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81Amides; Imides
    • C07D213/82Amides; Imides in position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)

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 (16)

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)
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
KR20150000874A (en) 2012-01-31 2015-01-05 산텐 세이야꾸 가부시키가이샤 Non-aqueous liquid composition
BR112016006153A2 (en) * 2013-09-20 2017-08-01 Santen Pharmaceutical Co Ltd composition containing polyethylene glycol
TW201609145A (en) 2013-12-25 2016-03-16 參天製藥股份有限公司 Injection and method for forming a depot
CA2979802C (en) * 2015-03-17 2023-06-27 Santen Pharmaceutical Co., Ltd. Pharmaceutical composition comprising polypeptide
TWI731853B (en) 2015-03-18 2021-07-01 日商參天製藥股份有限公司 Xufang drug composition and its stabilization method
JP2016175899A (en) * 2015-03-18 2016-10-06 参天製薬株式会社 Stable preservation of 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
EP1717229B1 (en) * 2004-02-17 2011-06-15 Santen Pharmaceutical Co., Ltd. Novel cyclic compound having 4-pyridylalkylthio group having (un)substituted amino introduced therein
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.
ES2548729T3 (en) 2005-03-31 2015-10-20 Santen Pharmaceutical Co., Ltd. New 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
BR112012001159A2 (en) 2016-03-01
CN102471273A (en) 2012-05-23
EA019689B1 (en) 2014-05-30
AU2010271746A1 (en) 2012-02-02
KR101710740B1 (en) 2017-02-27
WO2011007870A1 (en) 2011-01-20
JP2011037844A (en) 2011-02-24
MX2012000749A (en) 2012-01-27
EP2455368B1 (en) 2015-09-16
CA2767992A1 (en) 2011-01-20
US9029398B2 (en) 2015-05-12
JP5662719B2 (en) 2015-02-04
US9546140B2 (en) 2017-01-17
US20120116088A1 (en) 2012-05-10
AU2010271746B2 (en) 2014-07-03
US9902698B2 (en) 2018-02-27
NZ597495A (en) 2013-08-30
HK1167647A1 (en) 2012-12-07
US9359328B2 (en) 2016-06-07
ES2554360T3 (en) 2015-12-18
CA2767992C (en) 2017-03-21
HK1167644A1 (en) 2012-12-07
US20150291560A1 (en) 2015-10-15
MY157122A (en) 2016-05-13
EA201200146A1 (en) 2012-06-29
KR20130025857A (en) 2013-03-12
SG177576A1 (en) 2012-02-28
CN102471273B (en) 2014-07-16
US20160251314A1 (en) 2016-09-01
EP2455368A4 (en) 2013-01-09
US20170081286A1 (en) 2017-03-23
EP2455368A1 (en) 2012-05-23

Similar Documents

Publication Publication Date Title
IN2012DN01152A (en) 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
TW200738716A (en) Specific salt, anhydrous and crystalline form of a dihydropteridione derivative
IL217962A (en) Intermediate useful in the preparation of n-[2-( 2-pyridinyl)ethyl]carboxamide derivatives
ZA201208760B (en) Crystalline polymorph of 4-[5-[3-chloro-5-(trifluoromethyl)phenyl]-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-n-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-1-naphthalenecarboxamide
WO2005095379A3 (en) Crystalline methanesulfonic acid addition salts of imatinib
IL205872A0 (en) Process for the production of 2-[4-(3-or 2-fluorobenzyloxy)benzylamino]propanamides with high purity degree
WO2011141933A3 (en) Process for preparation of 2-[3-cyano-4-(2-methylpropoxy)phenyl]-4-methylthiazole-5-carboxylic acid and its pharmaceutically acceptable salts
PE20161369A1 (en) DIHYDROPYRIDINONE MONOACILGLYCEROL INHIBITORS 2 (MGAT2) SUBSTITUTE WITH TETRAZOLONE
EP2200991A1 (en) Antibacterial agents
EA201270099A1 (en) TRANS-4 - [[(5S) -5 - [[[3,5-BIS (TRIFTOROMETYL) PHENYL] METHYL] (2-METHYL-2H-TETRAZOL-5-IL) AMINO] -2,3,4,5 -TETRAHYDRO-7,9-DIMETHYL-1H-1-BENZAZEPIN-1-IL] METHYL] CYCLOHEXANKARBONIC ACID
TNSN06338A1 (en) Substantially pure 2-{[2-(2-methylamino-pyrimidin-4-yl)-1h-indole-5-carbonyl]-amino}-3-(phenylpyridin-2-yl-amino)-propionic acid as an ikb kinase inhibitor
Kilburn et al. N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors
BR112014023995B1 (en) HERBICIDALLY ACTIVE THIAZOLOPYRIDINES, HERBICIDES AND INSECTICIDES COMPOSITIONS, METHODS FOR THE CONTROL OF UNWANTED PLANTS AND INSECTS AND USE OF COMPOUNDS AND HERBICIDE COMPOSITION
PL1829868T3 (en) Process for production of (4,5-dihydroisoxazol-3-yl)thio- carboxamidine salts
IL193671A0 (en) Crystalline forms of n-{2-tert-butyl-1-[(4,4-difluorocyclohexyl)methyl]-lh-ben-imidazol-5-yl}ethanesulfonamide salts
Robichaud et al. Rational design of potent and selective NH-linked aryl/heteroaryl cathepsin K inhibitors
NZ598693A (en) Maleic acid salt and crystal thereof
MXPA05007847A (en) Acylaminothiazole derivatives, preparation method thereof and use of same as beta-amyloid peptide production inhibitors.
IL216661A0 (en) Crystalline phases of 2'-{[2-(4-methoxy-phenyl)-acetylamino]-methyl}-biphenyl-2-carboxylic acid (2-pyridin-3-yl-ethyl)-amide
WO2009027811A3 (en) Polymorphs of 3- ( ( (4-tert-butyl-benzyl) - (pyridine-3-sulfonyl) -amino) -methyl) -phenoxy) -acetic acid sodium salt or a hydrate thereof and methods for making the same
HK1167644B (en) 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
WO2008010089A3 (en) Process for preparation of intermediates of rosiglitazone, rosiglitazone and polymorphic forms thereof
TH145939A (en) Crystalline form of inhibitors of inter-action of MDM2 / 4 and p53.
BRPI0811995A2 (en) "METHODS FOR PRODUCTION OF ALPHA-GLUTAMIC ACID CRYSTALS AND FOR PRODUCTION OF MONOSODIC GLUTAMATE MONOIDRATE."
HK1144070A1 (en) Peptide deformylase inhibitors