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 thereofInfo
- 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
Links
- 239000013078 crystal Substances 0.000 title abstract 3
- 125000000350 glycoloyl group Chemical group O=C([*])C([H])([H])O[H] 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title abstract 2
- 229960003966 nicotinamide Drugs 0.000 title abstract 2
- 239000011570 nicotinamide Substances 0.000 title abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 title abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 title abstract 2
- 125000000446 sulfanediyl group Chemical group *S* 0.000 title abstract 2
- SRSXLGNVWSONIS-UHFFFAOYSA-M benzenesulfonate Chemical compound [O-]S(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-M 0.000 title 1
- 229940077388 benzenesulfonate Drugs 0.000 title 1
- 229940126062 Compound A Drugs 0.000 abstract 5
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 abstract 5
- 150000003839 salts Chemical class 0.000 abstract 3
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 230000008021 deposition Effects 0.000 abstract 1
- 229910052500 inorganic mineral Inorganic materials 0.000 abstract 1
- 239000011707 mineral Substances 0.000 abstract 1
- 235000005152 nicotinamide Nutrition 0.000 abstract 1
- DFPAKSUCGFBDDF-UHFFFAOYSA-N nicotinic acid amide Natural products NC(=O)C1=CC=CN=C1 DFPAKSUCGFBDDF-UHFFFAOYSA-N 0.000 abstract 1
- 210000002784 stomach Anatomy 0.000 abstract 1
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
- A61K31/435—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
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.
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)
| 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)
| 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 |
-
2010
- 2010-07-16 WO PCT/JP2010/062071 patent/WO2011007870A1/en not_active Ceased
- 2010-07-16 US US13/384,590 patent/US9029398B2/en not_active Expired - Fee Related
- 2010-07-16 CA CA2767992A patent/CA2767992C/en not_active Expired - Fee Related
- 2010-07-16 NZ NZ597495A patent/NZ597495A/en not_active IP Right Cessation
- 2010-07-16 AU AU2010271746A patent/AU2010271746B2/en not_active Ceased
- 2010-07-16 MY MYPI2011006369A patent/MY157122A/en unknown
- 2010-07-16 KR KR1020127003670A patent/KR101710740B1/en not_active Expired - Fee Related
- 2010-07-16 EA EA201200146A patent/EA019689B1/en not_active IP Right Cessation
- 2010-07-16 CN CN201080031652.1A patent/CN102471273B/en not_active Expired - Fee Related
- 2010-07-16 JP JP2010161881A patent/JP5662719B2/en not_active Expired - Fee Related
- 2010-07-16 IN IN1152DEN2012 patent/IN2012DN01152A/en unknown
- 2010-07-16 BR BR112012001159A patent/BR112012001159A2/en not_active IP Right Cessation
- 2010-07-16 EP EP10799928.6A patent/EP2455368B1/en not_active Not-in-force
- 2010-07-16 ES ES10799928.6T patent/ES2554360T3/en active Active
- 2010-07-16 SG SG2012001467A patent/SG177576A1/en unknown
- 2010-07-16 MX MX2012000749A patent/MX2012000749A/en active IP Right Grant
-
2015
- 2015-04-14 US US14/686,577 patent/US9359328B2/en not_active Expired - Fee Related
-
2016
- 2016-05-10 US US15/150,901 patent/US9546140B2/en not_active Expired - Fee Related
- 2016-12-02 US US15/368,028 patent/US9902698B2/en not_active Expired - Fee Related
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 |
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