ES2699951T3 - Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 - Google Patents

Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 Download PDF

Info

Publication number
ES2699951T3
ES2699951T3 ES16151719T ES16151719T ES2699951T3 ES 2699951 T3 ES2699951 T3 ES 2699951T3 ES 16151719 T ES16151719 T ES 16151719T ES 16151719 T ES16151719 T ES 16151719T ES 2699951 T3 ES2699951 T3 ES 2699951T3
Authority
ES
Spain
Prior art keywords
compound
polymorph
formula
ray powder
monohydrochloride
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES16151719T
Other languages
English (en)
Spanish (es)
Inventor
John Vincent Calienni
La Cruz Marilyn De
Dietmar Flubacher
Baoqing Gong
Prasad Koteswara Kapa
Piotr H Karpinski
Hui Liu
Pascal Michel
Rasmus Mose
Maria Caterina Testa
Liladhar Murlidhar Waykole
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44773179&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2699951(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis AG filed Critical Novartis AG
Application granted granted Critical
Publication of ES2699951T3 publication Critical patent/ES2699951T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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

Landscapes

  • 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)
ES16151719T 2010-10-01 2011-09-29 Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3 Active ES2699951T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38872110P 2010-10-01 2010-10-01
US201161494915P 2011-06-09 2011-06-09

Publications (1)

Publication Number Publication Date
ES2699951T3 true ES2699951T3 (es) 2019-02-13

Family

ID=44773179

Family Applications (1)

Application Number Title Priority Date Filing Date
ES16151719T Active ES2699951T3 (es) 2010-10-01 2011-09-29 Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3

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=)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

Also Published As

Publication number Publication date
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
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
BR112013007123B1 (pt) 2021-11-09
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

Similar Documents

Publication Publication Date Title
ES2699951T3 (es) Formas cristalinas de 5-(2,6-di-4-morfolinil-4-pirimidinil)-4-trifluorometilpiridin-2-amina, un inhibidor PIK3
ES2772498T3 (es) Preparación de un inhibidor mek y formulación que comprende el mismo
US12570641B2 (en) Solid forms of a CDK4 inhibitor
ES2808988T3 (es) Composiciones y métodos para inhibir la actividad arginasa
ES2261186T3 (es) Agente para aliviar efectos secundarios.
ES3057374T3 (en) Cdk9 inhibitors and polymorphs thereof for use as agents for treatment of cancer
US11052091B2 (en) BRK inhibitory compound
CN104684901A (zh) 胱硫醚-γ-裂合酶(CSE)抑制剂
US20230167077A1 (en) Crystal forms of immunomodulators
KR20170005106A (ko) 암을 치료하기 위한 약학적 조합물
JP7618445B2 (ja) 3-置換1,2,4-オキサジアゾールの結晶形態
JP2021518842A (ja) グルココルチコイド受容体アンタゴニストを含む固体の形態と製剤、およびその使用
ES2945865T3 (es) Combinación de un derivado de 6-oxo-1,6-dihidropiridazina que tiene actividad anticancerígena con un derivado de quinazolina
CN103864764A (zh) 吲唑取代的嘧啶胺衍生物、其制备方法和用途
ES2429941T3 (es) Candesartán cilexetilo micronizado estable y métodos para preparar el mismo
ES2679372T3 (es) Combinación de un derivado de 6-oxo-1,6-dihidro-piridazina que tiene actividad contra el cáncer con un inhibidor de MEK
CN103130774B (zh) 具有酪氨酸激酶抑制作用的化合物及其制备方法和应用
ES2845639T3 (es) Forma cristalina de 6-[(4R)-4-metil-1,2-dióxido-1,2,6-tiadiazinan-2-il]isoquinolin-1-carbonitrilo
US20220227759A1 (en) Amorphous pi3k inhibitor and pharmaceutical composition comprising same
CA3195063C (en) Solid forms of the cdk4 inhibitor pf-07220060
HK1220686B (en) Crystalline forms of 5-(2,6-di-4-morpholinyl-4-pyridmidinyl)-4-trifluoromethylpyridin-2-amine, a pik3 inhibitor
ES2354286T3 (es) Cristal de un compuesto de indol que contiene sulfonamida y procedimiento de producción del mismo.
TW201620500A (zh) 醫藥調製劑
BR112019019948A2 (pt) derivado de 6-pirimidina-isoindol como inibidor de erk1/2
CN110885316A (zh) 作为组蛋白去乙酰化酶抑制剂的巯基化合物及其用途