BR112013007123B1 - Forma cristalina do sal de monocloridrato de um composto a, seu uso, e composição farmacêutica - Google Patents

Forma cristalina do sal de monocloridrato de um composto a, seu uso, e composição farmacêutica Download PDF

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Publication number
BR112013007123B1
BR112013007123B1 BR112013007123-0A BR112013007123A BR112013007123B1 BR 112013007123 B1 BR112013007123 B1 BR 112013007123B1 BR 112013007123 A BR112013007123 A BR 112013007123A BR 112013007123 B1 BR112013007123 B1 BR 112013007123B1
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compound
formula
substituted
unsubstituted
groups
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BR112013007123-0A
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English (en)
Portuguese (pt)
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BR112013007123A2 (pt
Inventor
John Vincent Calienni
Marilyn De La Cruz
Dietmar Flubacher
Baoqing Gong
Prasad Koteswara Kapa
Piotr H. Karpinski
Hui Liu
Pascal Michel
Rasmus Mose
Maria Caterina Testa
Liladhar Murlidhar Waykole
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Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of BR112013007123A2 publication Critical patent/BR112013007123A2/pt
Publication of BR112013007123B1 publication Critical patent/BR112013007123B1/pt

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    • 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • 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
    • C07D213/72Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02Boron compounds
    • C07F5/04Esters of boric acids
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pyridine Compounds (AREA)
BR112013007123-0A 2010-10-01 2011-09-29 Forma cristalina do sal de monocloridrato de um composto a, seu uso, e composição farmacêutica BR112013007123B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US38872110P 2010-10-01 2010-10-01
US61/388,721 2010-10-01
US201161494915P 2011-06-09 2011-06-09
US61/494,915 2011-06-09
PCT/US2011/053808 WO2012044727A2 (en) 2010-10-01 2011-09-29 Manufacturing process for pyrimidine derivatives

Publications (2)

Publication Number Publication Date
BR112013007123A2 BR112013007123A2 (pt) 2016-06-14
BR112013007123B1 true BR112013007123B1 (pt) 2021-11-09

Family

ID=44773179

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BR112013007123-0A BR112013007123B1 (pt) 2010-10-01 2011-09-29 Forma cristalina do sal de monocloridrato de um composto a, seu uso, e composição farmacêutica

Country Status (30)

Country Link
US (3) US9181215B2 (https=)
EP (2) EP2621908A2 (https=)
JP (3) JP5998145B2 (https=)
KR (2) KR20180123586A (https=)
CN (3) CN103140479B (https=)
AR (1) AR083213A1 (https=)
AU (4) AU2011308856B2 (https=)
BR (1) BR112013007123B1 (https=)
CA (1) CA2813333C (https=)
CL (2) CL2013000850A1 (https=)
CO (1) CO6700837A2 (https=)
DK (1) DK3040333T3 (https=)
EC (1) ECSP13012596A (https=)
ES (1) ES2699951T3 (https=)
GT (1) GT201300080A (https=)
HU (1) HUE041326T2 (https=)
IL (3) IL225113A (https=)
LT (1) LT3040333T (https=)
MX (1) MX354482B (https=)
MY (1) MY160785A (https=)
NZ (1) NZ608285A (https=)
PE (1) PE20140002A1 (https=)
PH (2) PH12013500579A1 (https=)
PL (1) PL3040333T3 (https=)
PT (1) PT3040333T (https=)
RU (2) RU2576619C2 (https=)
SG (1) SG188439A1 (https=)
SI (1) SI3040333T1 (https=)
TW (1) TWI540133B (https=)
WO (1) WO2012044727A2 (https=)

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Publication number Priority date Publication date Assignee Title
CN103635189B (zh) 2011-07-01 2016-05-04 诺华股份有限公司 用于治疗癌症的含有cdk4/6抑制剂和pi3k抑制剂的联合治疗
KR20140069235A (ko) 2011-09-27 2014-06-09 노파르티스 아게 돌연변이체 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온
UY34632A (es) 2012-02-24 2013-05-31 Novartis Ag Compuestos de oxazolidin- 2- ona y usos de los mismos
PL2912030T3 (pl) * 2012-10-23 2017-02-28 Novartis Ag Ulepszony sposób wytwarzania 5-(2,6-di-4-morfolinylo-4-pirymidynylo)-4- trifluorometylopirydyno-2-aminy
US9296733B2 (en) 2012-11-12 2016-03-29 Novartis Ag Oxazolidin-2-one-pyrimidine derivative and use thereof for the treatment of conditions, diseases and disorders dependent upon PI3 kinases
EP2970240B1 (en) 2013-03-14 2018-01-10 Novartis AG 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh
US9318944B2 (en) 2013-04-29 2016-04-19 Rockwell Automation Technologies, Inc. Methods and apparatus for active front end filter capacitor degradation detection
US9294005B2 (en) 2013-10-01 2016-03-22 Rockwell Automation Technologies, Inc. Method and apparatus for detecting AFE filter capacitor degradation
NZ718487A (en) * 2013-10-16 2020-01-31 Shanghai Yingli Pharm Co Ltd Fused heterocyclic compound, preparation method therefor, pharmaceutical composition, and uses thereof
RU2688665C2 (ru) * 2014-04-22 2019-05-22 Университет Базель Новый способ получения производных триазина, пиримидина и пиридина
CN105085476B (zh) * 2014-11-24 2018-03-09 苏州晶云药物科技有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺二盐酸盐的晶型及其制备方法
AU2015366357B2 (en) * 2014-12-17 2018-07-19 Shanghai Haiyan Pharmaceutical Technology Co. Ltd. 2-morpholin-4,6-disubstituted pyrimidine derivative, and preparation method and pharmaceutical use thereof
US9481665B2 (en) * 2015-03-13 2016-11-01 Yong Xu Process for preparing PI3K inhibitor buparsilib
EP3273959A1 (en) 2015-03-25 2018-01-31 Novartis Ag Pharmaceutical combinations
CN105001151B (zh) * 2015-08-28 2017-07-14 苏州明锐医药科技有限公司 布帕尼西中间体及其制备方法
CN106543140A (zh) * 2015-09-21 2017-03-29 苏州晶云药物科技有限公司 5-[2,6-二(4-吗啉基)-4-嘧啶基]-4-(三氟甲基)-2-吡啶胺盐酸盐的晶型及其制备方法
PL3978500T3 (pl) * 2015-12-16 2024-03-11 Genentech, Inc. Sposób wytwarzania tricyklicznych związków inhibitorów pi3k
CN106905294A (zh) * 2016-07-08 2017-06-30 苏州科睿思制药有限公司 5‑[2,6‑二(4‑吗啉基)‑4‑嘧啶基]‑4‑(三氟甲基)‑2‑吡啶胺的晶型及其制备方法
CN107793394A (zh) * 2017-08-03 2018-03-13 上海厚璞生物科技有限公司 一种生产选择性pi3k抑制剂的系列关键中间体
CN110016142B (zh) * 2019-04-30 2021-08-03 合肥工业大学 一种含嘧啶硼酸结构的硅油及其制备方法

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US6124476A (en) 1998-04-17 2000-09-26 Symyx Technologies, Inc. Catalyst ligands, catalyst compositions, catalyst metal complexes and processes for cross-coupling aromatic boron compounds with aromatic halogens or perfluoroalkylsulfonates
CN1735598A (zh) * 2002-11-11 2006-02-15 拜耳医药保健股份公司 作为ip受体拮抗剂的苯基或杂芳基氨基烷烃衍生物
US7423148B2 (en) 2002-11-21 2008-09-09 Chiron Corporation Small molecule PI 3-kinase inhibitors and methods of their use
JO2660B1 (en) * 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
MX2009002046A (es) 2006-08-24 2009-03-06 Astrazeneca Ab Derivados de morfolino pirimidina utiles en el tratamiento de trastornos proliferativos.
WO2008098058A1 (en) 2007-02-06 2008-08-14 Novartis Ag Pi 3-kinase inhibitors and methods of their use
WO2009066084A1 (en) * 2007-11-21 2009-05-28 F. Hoffmann-La Roche Ag 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors
CN102958518A (zh) * 2009-05-15 2013-03-06 诺瓦提斯公司 磷脂酰肌醇3-激酶抑制剂和抗糖尿病化合物的组合

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US9452994B2 (en) 2016-09-27
JP2016128414A (ja) 2016-07-14
US9359326B2 (en) 2016-06-07
JP2013541536A (ja) 2013-11-14
RU2576619C2 (ru) 2016-03-10
CL2013000850A1 (es) 2013-09-27
TW201215605A (en) 2012-04-16
US20130225571A1 (en) 2013-08-29
JP5998145B2 (ja) 2016-09-28
EP3040333A1 (en) 2016-07-06
AU2015246141B2 (en) 2016-07-07
IL238046A (en) 2016-08-31
ES2699951T3 (es) 2019-02-13
AU2015200938A1 (en) 2015-03-12
LT3040333T (lt) 2018-12-10
AR083213A1 (es) 2013-02-06
IL233282A0 (en) 2014-08-31
WO2012044727A2 (en) 2012-04-05
SG188439A1 (en) 2013-05-31
ECSP13012596A (es) 2013-07-31
IL225113A (en) 2016-08-31
HUE041326T2 (hu) 2019-05-28
KR20130119928A (ko) 2013-11-01
CA2813333A1 (en) 2012-04-05
US20150232446A1 (en) 2015-08-20
BR112013007123A2 (pt) 2016-06-14
SI3040333T1 (sl) 2019-01-31
IL233282A (en) 2016-08-31
AU2015200936A1 (en) 2015-03-12
PH12013500579A1 (en) 2016-06-10
AU2015246141A1 (en) 2015-11-12
PL3040333T3 (pl) 2019-03-29
KR20180123586A (ko) 2018-11-16
AU2011308856A1 (en) 2013-03-28
EP2621908A2 (en) 2013-08-07
US20160251334A1 (en) 2016-09-01
CN103140479B (zh) 2015-04-08
RU2015150728A (ru) 2019-01-15
CN103140479A (zh) 2013-06-05
GT201300080A (es) 2014-07-18
MX354482B (es) 2018-03-07
US9181215B2 (en) 2015-11-10
EP3040333B1 (en) 2018-09-12
MX2013003507A (es) 2013-05-20
DK3040333T3 (da) 2019-01-02
MY160785A (en) 2017-03-15
CL2015001088A1 (es) 2015-07-10
JP2016106091A (ja) 2016-06-16
CA2813333C (en) 2019-01-15
WO2012044727A3 (en) 2012-06-07
HK1220686A1 (en) 2017-05-12
AU2015200938B2 (en) 2015-11-19
CN104987321A (zh) 2015-10-21
CN104945373A (zh) 2015-09-30
AU2011308856B2 (en) 2015-04-23
RU2013120326A (ru) 2014-11-20
CO6700837A2 (es) 2013-06-28
NZ608285A (en) 2014-06-27
PT3040333T (pt) 2018-12-04
PH12015501585A1 (en) 2015-09-21
PE20140002A1 (es) 2014-01-21
TWI540133B (zh) 2016-07-01

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 29/09/2011, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO.