BR112013007123A2 - processo de fabricação para derivados depirimidina - Google Patents
processo de fabricação para derivados depirimidinaInfo
- Publication number
- BR112013007123A2 BR112013007123A2 BR112013007123A BR112013007123A BR112013007123A2 BR 112013007123 A2 BR112013007123 A2 BR 112013007123A2 BR 112013007123 A BR112013007123 A BR 112013007123A BR 112013007123 A BR112013007123 A BR 112013007123A BR 112013007123 A2 BR112013007123 A2 BR 112013007123A2
- Authority
- BR
- Brazil
- Prior art keywords
- manufacturing process
- derivatives
- depyrimidine
- solid forms
- compound
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 4
- 239000007787 solid Substances 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 241001465754 Metazoa Species 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
-
- 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
-
- 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
processo de fabricação para derivados de pirimidina. a invenção refere-se a processos para fabricar um composto de fórmula 5, ou um estereoisômero, tautômero ou um sal do mesmo, emq que os substituintes são como definidos na especificação. a invenção também refere-se a novos processos de fabricação para formas sólidas específicas do composto a e seus sais, a tais formas sólidas e ao uso das referidas formas sólidas para o tratamento terapêutico de animais homeotérmicos.
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 true BR112013007123A2 (pt) | 2016-06-14 |
| BR112013007123B1 BR112013007123B1 (pt) | 2021-11-09 |
Family
ID=44773179
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 (31)
| Country | Link |
|---|---|
| US (3) | US9181215B2 (pt) |
| EP (2) | EP2621908A2 (pt) |
| JP (3) | JP5998145B2 (pt) |
| KR (2) | KR20180123586A (pt) |
| CN (3) | CN104945373A (pt) |
| AR (1) | AR083213A1 (pt) |
| AU (4) | AU2011308856B2 (pt) |
| BR (1) | BR112013007123B1 (pt) |
| CA (1) | CA2813333C (pt) |
| CL (2) | CL2013000850A1 (pt) |
| CO (1) | CO6700837A2 (pt) |
| DK (1) | DK3040333T3 (pt) |
| EC (1) | ECSP13012596A (pt) |
| ES (1) | ES2699951T3 (pt) |
| GT (1) | GT201300080A (pt) |
| HK (1) | HK1220686A1 (pt) |
| HU (1) | HUE041326T2 (pt) |
| IL (3) | IL225113A (pt) |
| LT (1) | LT3040333T (pt) |
| MX (1) | MX354482B (pt) |
| MY (1) | MY160785A (pt) |
| NZ (1) | NZ608285A (pt) |
| PE (1) | PE20140002A1 (pt) |
| PH (1) | PH12015501585A1 (pt) |
| PL (1) | PL3040333T3 (pt) |
| PT (1) | PT3040333T (pt) |
| RU (2) | RU2576619C2 (pt) |
| SG (1) | SG188439A1 (pt) |
| SI (1) | SI3040333T1 (pt) |
| TW (1) | TWI540133B (pt) |
| WO (1) | WO2012044727A2 (pt) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA114178C2 (uk) | 2011-07-01 | 2017-05-10 | Новартіс Аг | Комбінація, що включає інгібітор cdk4/6 і інгібітор pi3k, для лікування раку |
| PE20141581A1 (es) | 2011-09-27 | 2014-11-14 | Novartis Ag | 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante |
| UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
| MX360703B (es) * | 2012-10-23 | 2018-11-14 | Novartis Ag | Proceso mejorado para la elaboración de 5-(2, 6-di-4-morfolinil-4-pirimidinil)-4-trifluoro-metil-piridin-2-amin a. |
| 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 |
| PE20151939A1 (es) | 2013-03-14 | 2016-01-08 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidores de idh mutante |
| 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 |
| JP6139789B2 (ja) * | 2013-10-16 | 2017-05-31 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 縮合複素環化合物、その調製方法、医薬組成物及びその使用 |
| AU2015250994B2 (en) * | 2014-04-22 | 2018-12-20 | Torqur Ag | 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 |
| CN108697713B (zh) * | 2015-12-16 | 2021-10-26 | 基因泰克公司 | 用于制备三环pi3k抑制剂化合物的方法及用其治疗癌症的方法 |
| 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 |
| MXPA05005477A (es) | 2002-11-21 | 2005-07-25 | Chiron Corp | Pirimidinas 2,4,6-trisustituidas como inhibidores de fosfotidilinositol (pi) 3-cinasa y su uso en el tratamiento del cancer. |
| JO2660B1 (en) * | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| AU2007287428B2 (en) | 2006-08-24 | 2011-08-11 | Astrazeneca Ab | Morpholino pyrimidine derivatives useful in the treatment of proliferative disorders |
| CN101711241A (zh) | 2007-02-06 | 2010-05-19 | 诺瓦提斯公司 | Pi3-激酶抑制剂和它们的使用方法 |
| WO2009066084A1 (en) * | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
| RU2011150619A (ru) * | 2009-05-15 | 2013-06-20 | Новартис Аг | Комбинация ингибитора фосфоинозитид-3-киназы и противодиабетического соединения |
-
2011
- 2011-09-29 LT LTEP16151719.8T patent/LT3040333T/lt unknown
- 2011-09-29 KR KR1020187032263A patent/KR20180123586A/ko not_active Application Discontinuation
- 2011-09-29 AU AU2011308856A patent/AU2011308856B2/en active Active
- 2011-09-29 CA CA2813333A patent/CA2813333C/en active Active
- 2011-09-29 NZ NZ608285A patent/NZ608285A/en not_active IP Right Cessation
- 2011-09-29 AR ARP110103595A patent/AR083213A1/es unknown
- 2011-09-29 JP JP2013531796A patent/JP5998145B2/ja active Active
- 2011-09-29 CN CN201510157366.4A patent/CN104945373A/zh active Pending
- 2011-09-29 RU RU2013120326/04A patent/RU2576619C2/ru active
- 2011-09-29 BR BR112013007123-0A patent/BR112013007123B1/pt active IP Right Grant
- 2011-09-29 EP EP11767362.4A patent/EP2621908A2/en not_active Withdrawn
- 2011-09-29 PE PE2013000654A patent/PE20140002A1/es active IP Right Grant
- 2011-09-29 US US13/825,880 patent/US9181215B2/en active Active
- 2011-09-29 ES ES16151719T patent/ES2699951T3/es active Active
- 2011-09-29 SG SG2013016837A patent/SG188439A1/en unknown
- 2011-09-29 DK DK16151719.8T patent/DK3040333T3/da active
- 2011-09-29 PT PT16151719T patent/PT3040333T/pt unknown
- 2011-09-29 RU RU2015150728A patent/RU2015150728A/ru unknown
- 2011-09-29 CN CN201180047753.2A patent/CN103140479B/zh active Active
- 2011-09-29 EP EP16151719.8A patent/EP3040333B1/en active Active
- 2011-09-29 MX MX2013003507A patent/MX354482B/es active IP Right Grant
- 2011-09-29 SI SI201131619T patent/SI3040333T1/sl unknown
- 2011-09-29 PL PL16151719T patent/PL3040333T3/pl unknown
- 2011-09-29 HU HUE16151719A patent/HUE041326T2/hu unknown
- 2011-09-29 MY MYPI2013000811A patent/MY160785A/en unknown
- 2011-09-29 CN CN201510156027.4A patent/CN104987321A/zh active Pending
- 2011-09-29 KR KR1020137011172A patent/KR20130119928A/ko active Application Filing
- 2011-09-29 WO PCT/US2011/053808 patent/WO2012044727A2/en active Application Filing
- 2011-09-30 TW TW100135673A patent/TWI540133B/zh active
-
2013
- 2013-03-07 IL IL225113A patent/IL225113A/en unknown
- 2013-03-22 GT GT201300080A patent/GT201300080A/es unknown
- 2013-03-22 CO CO13057091A patent/CO6700837A2/es unknown
- 2013-03-28 CL CL2013000850A patent/CL2013000850A1/es unknown
- 2013-04-30 EC ECSP13012596 patent/ECSP13012596A/es unknown
- 2013-09-24 HK HK16108618.7A patent/HK1220686A1/zh unknown
-
2014
- 2014-06-19 IL IL233282A patent/IL233282A/en unknown
-
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 JP2015246501A patent/JP2016128414A/ja active Pending
- 2015-12-17 JP JP2015246502A patent/JP2016106091A/ja active Pending
-
2016
- 2016-05-06 US US15/147,986 patent/US9452994B2/en not_active Expired - Fee Related
Also Published As
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 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] |
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