SI2909169T1 - Kristalna faza (3s, 3s') 4,4'-disulfanediilbis(3-aminobutan 1-sulfonske kisline) z l-lizinom - Google Patents

Kristalna faza (3s, 3s') 4,4'-disulfanediilbis(3-aminobutan 1-sulfonske kisline) z l-lizinom Download PDF

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Publication number
SI2909169T1
SI2909169T1 SI201330952T SI201330952T SI2909169T1 SI 2909169 T1 SI2909169 T1 SI 2909169T1 SI 201330952 T SI201330952 T SI 201330952T SI 201330952 T SI201330952 T SI 201330952T SI 2909169 T1 SI2909169 T1 SI 2909169T1
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Slovenia
Prior art keywords
lysine
process according
crystalline form
absd
crystalline phase
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SI201330952T
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English (en)
Inventor
Fabrice Balavoine
Jean-Marie Schneider
Gerard Coquerel
Nicolas Couvrat
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Quantum Genomics
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Publication of SI2909169T1 publication Critical patent/SI2909169T1/sl

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/26—Separation; Purification; Stabilisation; Use of additives
    • C07C319/28—Separation; Purification
    • 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
    • A61K31/13—Amines
    • A61K31/145—Amines having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/38—Separation; Purification; Stabilisation; Use of additives
    • C07C227/40—Separation; Purification
    • C07C227/42—Crystallisation
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C229/26—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having more than one amino group bound to the carbon skeleton, e.g. lysine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/64—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
    • C07C323/66—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton containing sulfur atoms of sulfo, esterified sulfo or halosulfonyl groups, bound to the carbon skeleton
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Crystallography & Structural Chemistry (AREA)
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  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
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  • Hematology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Emergency Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (14)

  1. KRISTALNA FAZA (3S, 3S') 4,4'-DISULFANEDIILBIS(3-AMINOBUTAN 1-SULFONSKE KISLINE) Z L-LIZINOM PATENTNI ZAHTEVKI
    1. Kristalinična oblika (3S,3S')4,4'-disulfandiilbis(3-aminobutan 1-sulfonske kisline) ABSD z L-lizinom.
  2. 2. Kristalinična oblika po zahtevku 1, kjer je stehiometrija kristalne oblike <ABSD. (L-lizin)2>.
  3. 3. Kristalinična oblika po zahtevku 1 ali 2, kjer rentgenski difrakcijski vzorec kristalne oblike obsega naslednje vrhove:
    kjer je vzorec rentgenske difrakcije dobljen z anodo Cu Ka.
  4. 4. Proces za pripravo kristalne oblike ABSD in L-lizina, ki obsega korake: a. kontaktiranje z ABSD ali njene soli ali njene zmesi z L-lizinom, b. po izbiri sproženje formacije kristalne faze in/ali po izbiri izboljšanje kristaliničnosti kristalne faze, c. Izoliranje kristalne faze, dobljene v koraku (b) (ali (a)).
  5. 5. Proces po zahtevku 4, kjer je ABSD:L-lizin stehiometrija v koraku (a) zaobsežena med 1:1,5 in 1: 2,5.
  6. 6. Proces po zahtevku 4 ali 5, pri čemer se korak (a) izvede v raztopini.
  7. 7. Proces po zahtevku 6, kjer sta ABSD in L-lizin suspendirana v vodi.
  8. 8. Proces po zahtevku 4 ali 5, pri čemer se korak (a) izvede v trdnem stanju, prednostno z visoko energijskim mletjem.
  9. 9. Proces po zahtevku 6, kjer korak (b) izvedemo z dodatkom anti-topila, prednostno etanola.
  10. 10. Proces po katerem koli od zahtevkov 4 do 9, pri katerem se izvede izboljšanje kristaliničnosti koraka (b) s temperaturnim cikliranjem.
  11. 11. Proces po zahtevku 10, kjer se temperaturno cikliranje ponovi večkrat.
  12. 12. Proces po zahtevku 11, kjer se temperaturno cikliranje ponovi med 5 in 15-krat, prednostno 10-krat.
  13. 13. Farmacevtski sestavek, ki obsega kristalno obliko po katerem koli od zahtevkov 1 do 3 v kombinaciji s farmacevtsko sprejemljivim nosilcem ali razredčilom.
  14. 14. Kristalna oblika po katerem koli od zahtevkov 1 do 3 ali farmacevtski sestavek po zahtevku 13, za uporabo pri zdravljenju hipertenzije in/ali sorodnih boleznih.
SI201330952T 2012-10-22 2013-10-22 Kristalna faza (3s, 3s') 4,4'-disulfanediilbis(3-aminobutan 1-sulfonske kisline) z l-lizinom SI2909169T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12306307.5A EP2722327A1 (en) 2012-10-22 2012-10-22 Crystalline phase of (3S,3S') 4,4'-disulfanediylbis (3-aminobutane 1-sulfonic acid) with L-lysine
PCT/EP2013/072028 WO2014064077A1 (en) 2012-10-22 2013-10-22 Crystalline phase of (3s.3s') 4,4'-disulfanediylbis(3-aminobutane 1 -sulfonic acid) with l-lysine
EP13779603.3A EP2909169B1 (en) 2012-10-22 2013-10-22 Crystalline phase of (3s,3s') 4,4'-disulfanediylbis(3-aminobutane 1-sulfonic acid) with l-lysine

Publications (1)

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SI2909169T1 true SI2909169T1 (sl) 2018-04-30

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SI201330952T SI2909169T1 (sl) 2012-10-22 2013-10-22 Kristalna faza (3s, 3s') 4,4'-disulfanediilbis(3-aminobutan 1-sulfonske kisline) z l-lizinom

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US (2) US9278921B2 (sl)
EP (2) EP2722327A1 (sl)
JP (1) JP6317358B2 (sl)
KR (1) KR102103407B1 (sl)
CN (1) CN104768927B (sl)
AR (1) AR093070A1 (sl)
AU (1) AU2013336738B2 (sl)
BR (1) BR112015008931B1 (sl)
CA (1) CA2884914C (sl)
CY (1) CY1119913T1 (sl)
DK (1) DK2909169T3 (sl)
EA (1) EA024460B1 (sl)
ES (1) ES2658413T3 (sl)
HK (1) HK1212321A1 (sl)
HR (1) HRP20180189T1 (sl)
HU (1) HUE036037T2 (sl)
IL (1) IL237733B (sl)
IN (1) IN2015DN02807A (sl)
LT (1) LT2909169T (sl)
ME (1) ME02955B (sl)
MX (1) MX353693B (sl)
NO (1) NO2909169T3 (sl)
NZ (1) NZ706070A (sl)
PL (1) PL2909169T3 (sl)
PT (1) PT2909169T (sl)
RS (1) RS56896B1 (sl)
SI (1) SI2909169T1 (sl)
TW (1) TWI643842B (sl)
WO (1) WO2014064077A1 (sl)
ZA (1) ZA201503574B (sl)

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CN103951562B (zh) * 2014-05-09 2016-04-20 四川九章生物化工科技发展有限公司 一种绿原酸晶型及其制备方法
WO2022225712A1 (en) * 2021-04-22 2022-10-27 Teva Pharmaceuticals International Gmbh Solid state forms of firibastat and processes for preparation thereof

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Publication number Priority date Publication date Assignee Title
WO2004007441A2 (fr) 2002-07-16 2004-01-22 Institut National De La Sante Et De La Recherche Medicale (Inserm) Derives de 4,4' -dithiobis- (3-aminobutane-1-sulfonates) nouveaux et compositions les contenant
FR2858617A1 (fr) * 2003-08-06 2005-02-11 Inst Nat Sante Rech Med Derives de 4',4'-dithiobis-(3-aminobutane-1-sulfonate-1- sulfonates) nouveaux et compositions les contenant
TWI370818B (en) * 2006-04-05 2012-08-21 Astellas Pharma Inc Cocrystal of c-glycoside derivative and l-proline
EP2439192A1 (en) 2010-10-07 2012-04-11 Quantum Genomics Method for the preparation of (3S,3S') 4,4'-disulfanediylbis (3-aminobutane 1-sulfonic acid)
WO2012138907A2 (en) * 2011-04-05 2012-10-11 Translational Genomics Research Institute Solid forms of curcumin

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Publication number Publication date
EP2909169A1 (en) 2015-08-26
US9487477B2 (en) 2016-11-08
ES2658413T3 (es) 2018-03-09
HK1212321A1 (en) 2016-06-10
PL2909169T3 (pl) 2018-07-31
NO2909169T3 (sl) 2018-06-02
EA024460B1 (ru) 2016-09-30
AU2013336738B2 (en) 2017-05-18
WO2014064077A1 (en) 2014-05-01
TWI643842B (zh) 2018-12-11
CA2884914C (en) 2021-01-05
JP6317358B2 (ja) 2018-04-25
LT2909169T (lt) 2018-04-25
BR112015008931B1 (pt) 2021-05-18
US20150284325A1 (en) 2015-10-08
US20160221940A1 (en) 2016-08-04
ZA201503574B (en) 2016-01-27
KR102103407B1 (ko) 2020-04-22
RS56896B1 (sr) 2018-04-30
MX2015005059A (es) 2015-11-23
TW201418202A (zh) 2014-05-16
CN104768927A (zh) 2015-07-08
JP2015536316A (ja) 2015-12-21
CN104768927B (zh) 2017-06-09
EA201500438A1 (ru) 2015-09-30
EP2909169B1 (en) 2018-01-03
PT2909169T (pt) 2018-02-26
AU2013336738A1 (en) 2015-04-09
MX353693B (es) 2018-01-24
CA2884914A1 (en) 2014-05-01
IL237733B (en) 2019-03-31
ME02955B (me) 2018-07-20
DK2909169T3 (en) 2018-02-26
EP2722327A1 (en) 2014-04-23
NZ706070A (en) 2018-11-30
CY1119913T1 (el) 2018-06-27
AR093070A1 (es) 2015-05-13
HRP20180189T1 (hr) 2018-04-20
BR112015008931A2 (pt) 2017-07-04
HUE036037T2 (hu) 2018-06-28
KR20150072454A (ko) 2015-06-29
IN2015DN02807A (sl) 2015-09-11
US9278921B2 (en) 2016-03-08

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