PE20140002A1 - Proceso de elaboracion para derivados de pirimidina - Google Patents
Proceso de elaboracion para derivados de pirimidinaInfo
- Publication number
- PE20140002A1 PE20140002A1 PE2013000654A PE2013000654A PE20140002A1 PE 20140002 A1 PE20140002 A1 PE 20140002A1 PE 2013000654 A PE2013000654 A PE 2013000654A PE 2013000654 A PE2013000654 A PE 2013000654A PE 20140002 A1 PE20140002 A1 PE 20140002A1
- Authority
- PE
- Peru
- Prior art keywords
- whose
- shows peaks
- diffraction angle
- theta
- trifluoro
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical class C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 title 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 title 1
- CWHUFRVAEUJCEF-UHFFFAOYSA-N BKM120 Chemical compound C1=NC(N)=CC(C(F)(F)F)=C1C1=CC(N2CCOCC2)=NC(N2CCOCC2)=N1 CWHUFRVAEUJCEF-UHFFFAOYSA-N 0.000 abstract 2
- 238000002441 X-ray diffraction Methods 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 201000009030 Carcinoma Diseases 0.000 abstract 1
- 201000004681 Psoriasis Diseases 0.000 abstract 1
- 206010039491 Sarcoma Diseases 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 239000013078 crystal Substances 0.000 abstract 1
- 208000032839 leukemia Diseases 0.000 abstract 1
- 150000004682 monohydrates Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000002935 phosphatidylinositol 3 kinase inhibitor Substances 0.000 abstract 1
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- A61K31/535—Heterocyclic 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
-
- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D213/72—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/025—Boronic and borinic acid compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/04—Esters of boric acids
-
- 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)
- 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)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyridine Compounds (AREA)
Abstract
SE REFIERE A FORMAS CRISTALINAS DEL COMPUESTO 5-(2,6-DI-4-MORFOLINIL-4-PIRIMIDINIL)-4-TRIFLUORO-METIL-PIRIDIN-2-AMINA TALES COMO: i) UN HEMI-HIDRATO EN LA FORMA POLIMORFA HA CUYA DIFRACCION DE RAYOS-X MUESTRA PICOS EN UN ANGULO DE DIFRACCION 2-THETA DE 19.2 +/- 0.3� Y 18.7 +/- 0.3�; ii) LA FORMA POLIMORFA A ANHIDRA CUYA DIFRACCION DE RAYOS-X MUESTRA PICOS EN UN ANGULO DE DIFRACCION 2-THETA DE 14.8 +/- 0.3� Y 10.2 +/- 0.3�; iii) UN MONO-HIDRATO DE LA SAL DE MONO-CLORHIDRATO EN LA FORMA POLIMORFA HA CUYA DIFRACCION DE RAYOS-X MUESTRA PICOS EN UN ANGULO DE DIFRACCION 2-THETA DE 9.3 +/- 0.3� Y 15.8 +/- 0.3�; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION DE DICHAS FORMAS CRISTALINAS. DICHO COMPUESTO 5-(2,6-DI-4-MORFOLINIL-4-PIRIMIDINIL)-4-TRIFLUORO-METIL-PIRIDIN-2-AMINA ES UN INHIBIDOR DE CINASA DE FOSFATIDIL-INOSITOL-3 SIENDO UTIL EN EL TRATAMIENTO DE CARCINOMA DEL CEREBRO, SARCOMA, LEUCEMIA, PSORIASIS
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 |
|---|---|
| PE20140002A1 true PE20140002A1 (es) | 2014-01-21 |
Family
ID=44773179
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013000654A PE20140002A1 (es) | 2010-10-01 | 2011-09-29 | Proceso de elaboracion para derivados de pirimidina |
Country Status (30)
| Country | Link |
|---|---|
| US (3) | US9181215B2 (es) |
| EP (2) | EP2621908A2 (es) |
| JP (3) | JP5998145B2 (es) |
| KR (2) | KR20130119928A (es) |
| CN (3) | CN103140479B (es) |
| AR (1) | AR083213A1 (es) |
| AU (4) | AU2011308856B2 (es) |
| BR (1) | BR112013007123B1 (es) |
| CA (1) | CA2813333C (es) |
| CL (2) | CL2013000850A1 (es) |
| CO (1) | CO6700837A2 (es) |
| DK (1) | DK3040333T3 (es) |
| EC (1) | ECSP13012596A (es) |
| ES (1) | ES2699951T3 (es) |
| GT (1) | GT201300080A (es) |
| HU (1) | HUE041326T2 (es) |
| IL (3) | IL225113A (es) |
| LT (1) | LT3040333T (es) |
| MX (1) | MX354482B (es) |
| MY (1) | MY160785A (es) |
| NZ (1) | NZ608285A (es) |
| PE (1) | PE20140002A1 (es) |
| PH (2) | PH12013500579A1 (es) |
| PL (1) | PL3040333T3 (es) |
| PT (1) | PT3040333T (es) |
| RU (2) | RU2015150728A (es) |
| SG (1) | SG188439A1 (es) |
| SI (1) | SI3040333T1 (es) |
| TW (1) | TWI540133B (es) |
| WO (1) | WO2012044727A2 (es) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013006532A1 (en) | 2011-07-01 | 2013-01-10 | Novartis Ag | Combination therapy comprising a cdk4/6 inhibitor and a pi3k inhibitor for use in the treatment of cancer |
| GEP20166432B (en) | 2011-09-27 | 2016-02-10 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| IN2015DN01331A (es) * | 2012-10-23 | 2015-07-03 | Novartis Ag | |
| 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 |
| WO2014141104A1 (en) | 2013-03-14 | 2014-09-18 | 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 |
| CN104557872B (zh) * | 2013-10-16 | 2017-05-24 | 上海璎黎药业有限公司 | 稠合杂环化合物、其制备方法、药物组合物和用途 |
| SG11201608658SA (en) * | 2014-04-22 | 2016-11-29 | Univ Basel | Novel manufacturing process for triazine, pyrimidine and pyridine derivatives |
| 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 |
| US10227324B2 (en) | 2014-12-17 | 2019-03-12 | 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 |
| WO2016151501A1 (en) | 2015-03-25 | 2016-09-29 | 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 |
| AU2016369528B2 (en) * | 2015-12-16 | 2021-04-22 | Genentech, Inc. | Process for the preparation of tricyclic PI3K inhibitor compounds and methods for using the same for the treatment of cancer |
| 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)
| 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 |
| EP2316831B1 (en) | 2002-11-21 | 2013-03-06 | Novartis AG | 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| KR101435231B1 (ko) | 2006-08-24 | 2014-10-02 | 아스트라제네카 아베 | 증식성 질환의 치료에 유용한 모르폴리노 피리미딘 유도체 |
| KR20090108124A (ko) * | 2007-02-06 | 2009-10-14 | 노파르티스 아게 | Ｐｉ 3-키나제 억제제 및 그의 사용 방법 |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| JP2012526772A (ja) * | 2009-05-15 | 2012-11-01 | ノバルティス アーゲー | ホスホイノシチド３−キナーゼ阻害剤および抗糖尿病性化合物の組合せ剤 |
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2011
- 2011-09-29 CN CN201180047753.2A patent/CN103140479B/zh active Active
- 2011-09-29 US US13/825,880 patent/US9181215B2/en active Active
- 2011-09-29 EP EP11767362.4A patent/EP2621908A2/en not_active Withdrawn
- 2011-09-29 PL PL16151719T patent/PL3040333T3/pl unknown
- 2011-09-29 KR KR1020137011172A patent/KR20130119928A/ko not_active Ceased
- 2011-09-29 JP JP2013531796A patent/JP5998145B2/ja active Active
- 2011-09-29 CA CA2813333A patent/CA2813333C/en active Active
- 2011-09-29 PE PE2013000654A patent/PE20140002A1/es active IP Right Grant
- 2011-09-29 PT PT16151719T patent/PT3040333T/pt unknown
- 2011-09-29 ES ES16151719T patent/ES2699951T3/es active Active
- 2011-09-29 CN CN201510156027.4A patent/CN104987321A/zh active Pending
- 2011-09-29 CN CN201510157366.4A patent/CN104945373A/zh active Pending
- 2011-09-29 MX MX2013003507A patent/MX354482B/es active IP Right Grant
- 2011-09-29 SG SG2013016837A patent/SG188439A1/en unknown
- 2011-09-29 NZ NZ608285A patent/NZ608285A/en not_active IP Right Cessation
- 2011-09-29 HU HUE16151719A patent/HUE041326T2/hu unknown
- 2011-09-29 AR ARP110103595A patent/AR083213A1/es unknown
- 2011-09-29 BR BR112013007123-0A patent/BR112013007123B1/pt active IP Right Grant
- 2011-09-29 RU RU2015150728A patent/RU2015150728A/ru unknown
- 2011-09-29 MY MYPI2013000811A patent/MY160785A/en unknown
- 2011-09-29 RU RU2013120326/04A patent/RU2576619C2/ru active
- 2011-09-29 PH PH1/2013/500579A patent/PH12013500579A1/en unknown
- 2011-09-29 LT LTEP16151719.8T patent/LT3040333T/lt unknown
- 2011-09-29 KR KR1020187032263A patent/KR20180123586A/ko not_active Ceased
- 2011-09-29 DK DK16151719.8T patent/DK3040333T3/da active
- 2011-09-29 EP EP16151719.8A patent/EP3040333B1/en active Active
- 2011-09-29 AU AU2011308856A patent/AU2011308856B2/en active Active
- 2011-09-29 SI SI201131619T patent/SI3040333T1/sl unknown
- 2011-09-29 WO PCT/US2011/053808 patent/WO2012044727A2/en not_active Ceased
- 2011-09-30 TW TW100135673A patent/TWI540133B/zh active
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2013
- 2013-03-07 IL IL225113A patent/IL225113A/en unknown
- 2013-03-22 CO CO13057091A patent/CO6700837A2/es unknown
- 2013-03-22 GT GT201300080A patent/GT201300080A/es unknown
- 2013-03-28 CL CL2013000850A patent/CL2013000850A1/es unknown
- 2013-04-30 EC ECSP13012596 patent/ECSP13012596A/es unknown
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2014
- 2014-06-19 IL IL233282A patent/IL233282A/en unknown
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2015
- 2015-02-24 AU AU2015200938A patent/AU2015200938B2/en not_active Ceased
- 2015-02-24 AU AU2015200936A patent/AU2015200936A1/en not_active Abandoned
- 2015-03-30 IL IL238046A patent/IL238046A/en not_active IP Right Cessation
- 2015-04-27 CL CL2015001088A patent/CL2015001088A1/es unknown
- 2015-05-06 US US14/705,013 patent/US9359326B2/en not_active Expired - Fee Related
- 2015-07-20 PH PH12015501585A patent/PH12015501585A1/en unknown
- 2015-10-23 AU AU2015246141A patent/AU2015246141B2/en not_active Ceased
- 2015-12-17 JP JP2015246502A patent/JP2016106091A/ja active Pending
- 2015-12-17 JP JP2015246501A patent/JP2016128414A/ja active Pending
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2016
- 2016-05-06 US US15/147,986 patent/US9452994B2/en not_active Expired - Fee Related
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