BRPI0917196A2 - método para a preparação de um complexo, e, forma cristalina de um composto. - Google Patents

método para a preparação de um complexo, e, forma cristalina de um composto.

Info

Publication number
BRPI0917196A2
BRPI0917196A2 BRPI0917196A BRPI0917196A BRPI0917196A2 BR PI0917196 A2 BRPI0917196 A2 BR PI0917196A2 BR PI0917196 A BRPI0917196 A BR PI0917196A BR PI0917196 A BRPI0917196 A BR PI0917196A BR PI0917196 A2 BRPI0917196 A2 BR PI0917196A2
Authority
BR
Brazil
Prior art keywords
preparing
complex
compound
crystalline form
crystalline
Prior art date
Application number
BRPI0917196A
Other languages
English (en)
Inventor
Ge Xu
Jason Liou
Shengbin Li
Yuelin Wu
Original Assignee
Theracos Inc
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 Theracos Inc filed Critical Theracos Inc
Publication of BRPI0917196A2 publication Critical patent/BRPI0917196A2/pt
Publication of BRPI0917196B1 publication Critical patent/BRPI0917196B1/pt
Publication of BRPI0917196B8 publication Critical patent/BRPI0917196B8/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/351Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom not condensed with another ring
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/06Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds 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
    • C07C229/34Compounds 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 containing six-membered aromatic rings
    • C07C229/36Compounds 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 containing six-membered aromatic rings with at least one amino group and one carboxyl group bound to the same carbon atom of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/12Oxygen or sulfur atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
    • C07D207/16Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D309/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members 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
    • C07D309/10Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/20Carbocyclic rings
    • C07H15/203Monocyclic carbocyclic rings other than cyclohexane rings; Bicyclic carbocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26Acyclic or carbocyclic radicals, substituted by hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
    • A61K31/3533,4-Dihydrobenzopyrans, e.g. chroman, catechin
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H7/00Compounds containing non-saccharide radicals linked to saccharide radicals by a carbon-to-carbon bond
    • C07H7/04Carbocyclic radicals

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
BRPI0917196A 2008-08-22 2009-08-21 forma cristalina de um composto sendo complexo de (2s,3r,4r,5s,6r)- 2- (4- cloro- 3- (4- (2- ciclopropoxietóxi) benzil)fenil)- 6- (hidroximetil) tetraidro- 2h- piran- 3,4,5- triol, bis(l-prolina) BRPI0917196B8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US9124808P 2008-08-22 2008-08-22
PCT/US2009/054585 WO2010022313A2 (en) 2008-08-22 2009-08-21 Processes for the preparation of sglt2 inhibitors

Publications (3)

Publication Number Publication Date
BRPI0917196A2 true BRPI0917196A2 (pt) 2015-11-10
BRPI0917196B1 BRPI0917196B1 (pt) 2019-11-12
BRPI0917196B8 BRPI0917196B8 (pt) 2021-05-25

Family

ID=41707668

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0917196A BRPI0917196B8 (pt) 2008-08-22 2009-08-21 forma cristalina de um composto sendo complexo de (2s,3r,4r,5s,6r)- 2- (4- cloro- 3- (4- (2- ciclopropoxietóxi) benzil)fenil)- 6- (hidroximetil) tetraidro- 2h- piran- 3,4,5- triol, bis(l-prolina)

Country Status (30)

Country Link
US (2) US8283454B2 (pt)
EP (1) EP2324002B1 (pt)
JP (2) JP5749168B2 (pt)
KR (2) KR101654231B1 (pt)
CN (3) CN103910702A (pt)
AR (1) AR073118A1 (pt)
AU (1) AU2009282739B2 (pt)
BR (1) BRPI0917196B8 (pt)
CA (2) CA2935838C (pt)
CY (1) CY1118280T1 (pt)
DK (1) DK2324002T3 (pt)
ES (1) ES2599330T3 (pt)
HR (1) HRP20161648T1 (pt)
HU (1) HUE029970T2 (pt)
IL (2) IL211300A (pt)
LT (1) LT2324002T (pt)
ME (1) ME02702B (pt)
MX (1) MX2011001855A (pt)
NZ (2) NZ604897A (pt)
PL (1) PL2324002T3 (pt)
PT (1) PT2324002T (pt)
RS (1) RS55555B1 (pt)
RU (2) RU2530494C2 (pt)
SG (1) SG193168A1 (pt)
SI (1) SI2324002T1 (pt)
SM (2) SMT201600475T1 (pt)
TW (2) TWI441831B (pt)
UA (1) UA103050C2 (pt)
WO (1) WO2010022313A2 (pt)
ZA (1) ZA201401468B (pt)

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WO2012003811A1 (en) * 2010-07-09 2012-01-12 Zhejiang Beta Pharma Inc. C-aryl glucoside sglt2 inhibitors and method
CN102372722A (zh) 2010-08-10 2012-03-14 江苏恒瑞医药股份有限公司 C-芳基葡萄糖苷衍生物、其制备方法及其在医药上的应用
EP2697218B1 (en) 2011-04-13 2016-05-25 Janssen Pharmaceutica NV Process for the preparation of compounds useful as inhibitors of sglt2
TWI542596B (zh) * 2011-05-09 2016-07-21 健生藥品公司 (2s,3r,4r,5s,6r)-2-(3-((5-(4-氟苯基)噻吩-2-基)甲基)-4-甲基苯基)-6-(羥甲基)四氫-2h-哌喃-3,4,5-三醇之l-脯胺酸及檸檬酸共晶體
US9018249B2 (en) 2011-09-13 2015-04-28 Panacea Biotec Limited SGLT inhibitors
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CN103910719B (zh) * 2012-12-31 2018-05-01 上海璎黎药业有限公司 葡萄糖衍生物与苯丙氨酸复合物、晶体、制备方法及应用
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CN105611920B (zh) * 2013-10-12 2021-07-16 泰拉科斯萨普有限责任公司 羟基-二苯甲烷衍生物的制备
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CN103694230B (zh) * 2013-12-06 2016-04-13 江苏奥赛康药业股份有限公司 一种高纯度卡格列净化合物及其制备方法
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CN115671290A (zh) 2014-01-23 2023-02-03 勃林格殷格翰动物保健有限公司 犬科动物中代谢紊乱的治疗
CN104829572B (zh) 2014-02-10 2019-01-04 江苏豪森药业集团有限公司 达格列净新晶型及其制备方法
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CN104031098A (zh) * 2014-06-21 2014-09-10 李友香 降糖药物
CN105481915A (zh) * 2014-09-19 2016-04-13 北京万生药业有限责任公司 一种sglt-2抑制剂化合物的制备方法
WO2016046150A1 (en) 2014-09-25 2016-03-31 Boehringer Ingelheim Vetmedica Gmbh Combination treatment of sglt2 inhibitors and dopamine agonists for preventing metabolic disorders in equine animals
WO2016088081A1 (en) * 2014-12-03 2016-06-09 Sun Pharmaceutical Industries Limited Processes for the preparation of ertugliflozin
EP3256482B1 (en) 2015-02-09 2019-11-27 Indoco Remedies Limited Process for the preparation of sglt inhibitor compounds
WO2016178148A1 (en) * 2015-05-05 2016-11-10 Glenmark Pharmaceuticals Limited Process for preparation of dapagliflozin
KR102659761B1 (ko) 2015-08-27 2024-04-24 베링거잉겔하임베트메디카게엠베하 Sglt-2 억제제를 포함하는 액상 약제학적 조성물
CN105061373B (zh) * 2015-09-06 2017-10-20 合肥华方医药科技有限公司 一种达格列净异构体杂质的合成方法
KR20160001719A (ko) 2015-09-11 2016-01-06 주식회사 대한아이엠 연약지반 개량을 위한 수직과 수평 배수재 시공방법 및 그 수평배수재의 부직포
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KR102226465B1 (ko) * 2016-05-28 2021-03-11 하이난 수안주 파마 코포레이션 리미티드 나트륨-글루코스 공수송체 2에 대한 억제제의 결정형
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CN110790735A (zh) * 2018-08-03 2020-02-14 北京海晶生物医药科技有限公司 一种达格列净新晶型n及其制备方法
WO2020084559A1 (en) 2018-10-26 2020-04-30 Janssen Pharmaceutica Nv Glucopyranose derivatives useful as sglt2 inhibitors
WO2020084560A1 (en) 2018-10-26 2020-04-30 Janssen Pharmaceutica Nv Glucopyranose derivatives useful as sglt2 inhibitors
WO2020151672A1 (zh) * 2019-01-23 2020-07-30 苏州科睿思制药有限公司 一种达格列净晶型及其制备方法和用途
CN113613719A (zh) 2019-03-14 2021-11-05 印可瑞维特有限公司 控制猫糖尿病的化合物
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