MX355945B - 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. - Google Patents
3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante.Info
- Publication number
- MX355945B MX355945B MX2015012552A MX2015012552A MX355945B MX 355945 B MX355945 B MX 355945B MX 2015012552 A MX2015012552 A MX 2015012552A MX 2015012552 A MX2015012552 A MX 2015012552A MX 355945 B MX355945 B MX 355945B
- Authority
- MX
- Mexico
- Prior art keywords
- mutant idh
- oxazolidin
- pyrimidin
- inhibitors
- ones
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- 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
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Abstract
La invención se refiere a la fórmula (I): (ver Fórmula) o a una sal farmacéuticamente aceptable de la misma, en donde R1, R2a, R2b y R3-R7 se describen en la presente. La invención también se refiere a un composición que contiene un compuesto de la fórmula (I), y al uso de estos compuestos en la inhibición de las proteínas de IDH mutante que tienen una actividad neomórfica. La invención se refiere además al uso de un compuesto de la fórmula (I) en el tratamiento de las enfermedades o los trastornos asociados con dichas proteínas de IDH mutante, incluyendo, pero no limitándose a, trastornos de proliferación celular, tales como cáncer.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361783210P | 2013-03-14 | 2013-03-14 | |
US201361892131P | 2013-10-17 | 2013-10-17 | |
PCT/IB2014/059695 WO2014141104A1 (en) | 2013-03-14 | 2014-03-12 | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2015012552A MX2015012552A (es) | 2016-04-18 |
MX355945B true MX355945B (es) | 2018-05-07 |
Family
ID=50382516
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015012552A MX355945B (es) | 2013-03-14 | 2014-03-12 | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. |
Country Status (29)
Country | Link |
---|---|
US (4) | US9434719B2 (es) |
EP (1) | EP2970240B1 (es) |
JP (1) | JP6387360B2 (es) |
KR (1) | KR20150131224A (es) |
CN (1) | CN105263929B (es) |
AP (1) | AP2015008707A0 (es) |
AR (1) | AR095311A1 (es) |
AU (1) | AU2014229313B2 (es) |
BR (1) | BR112015023412A8 (es) |
CA (1) | CA2903979A1 (es) |
CL (1) | CL2015002472A1 (es) |
CR (1) | CR20150491A (es) |
CU (1) | CU20150119A7 (es) |
DO (1) | DOP2015000240A (es) |
EA (1) | EA028033B1 (es) |
ES (1) | ES2665619T3 (es) |
GE (1) | GEP201706699B (es) |
HK (1) | HK1213251A1 (es) |
IL (1) | IL240972A0 (es) |
MX (1) | MX355945B (es) |
NI (1) | NI201500128A (es) |
PE (1) | PE20151939A1 (es) |
PH (1) | PH12015502018A1 (es) |
SG (1) | SG11201507063YA (es) |
TN (1) | TN2015000392A1 (es) |
TW (1) | TW201444831A (es) |
UY (1) | UY35470A (es) |
WO (1) | WO2014141104A1 (es) |
ZA (1) | ZA201506452B (es) |
Families Citing this family (44)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
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 |
ES2665619T3 (es) * | 2013-03-14 | 2018-04-26 | Novartis Ag | 3-Pirimidin-4-il-oxazolidin-2-onas como inhibidores de IDH mutante |
TW201522307A (zh) | 2013-03-14 | 2015-06-16 | 百靈佳殷格翰國際股份有限公司 | 經取代2-氮雜-雙環[2.2.1]庚烷-3-羧酸(苄基-氰基-甲基)-醯胺組織蛋白酶c抑制劑 |
PL3041827T3 (pl) | 2013-09-06 | 2018-09-28 | Aurigene Discovery Tech Limited | Pochodne 1,2,4-oksadiazolu jako immunomodulatory |
JOP20200094A1 (ar) | 2014-01-24 | 2017-06-16 | Dana Farber Cancer Inst Inc | جزيئات جسم مضاد لـ pd-1 واستخداماتها |
JOP20200096A1 (ar) | 2014-01-31 | 2017-06-16 | Children’S Medical Center Corp | جزيئات جسم مضاد لـ tim-3 واستخداماتها |
CN106103484B (zh) | 2014-03-14 | 2021-08-20 | 诺华股份有限公司 | 针对lag-3的抗体分子及其用途 |
SI3191487T1 (sl) | 2014-09-12 | 2019-12-31 | Boehringer Ingelheim International Gmbh | Spirociklični inhibitorji katepsina C |
MA41044A (fr) | 2014-10-08 | 2017-08-15 | Novartis Ag | Compositions et procédés d'utilisation pour une réponse immunitaire accrue et traitement contre le cancer |
CU20170052A7 (es) | 2014-10-14 | 2017-11-07 | Dana Farber Cancer Inst Inc | Moléculas de anticuerpo que se unen a pd-l1 |
EP3233918A1 (en) | 2014-12-19 | 2017-10-25 | Novartis AG | Combination therapies |
MY190404A (en) | 2015-03-10 | 2022-04-21 | Aduro Biotech Inc | Compositions and methods for activating "stimulator of interferon gene"-dependent signalling |
AU2016230793B2 (en) | 2015-03-10 | 2021-03-25 | Aurigene Discovery Technologies Limited | 1,2,4-oxadiazole and thiadiazole compounds as immunomodulators |
ES2764523T3 (es) | 2015-07-27 | 2020-06-03 | Lilly Co Eli | Compuestos de 7-feniletilamino-4H-pirimido[4,5-D][1,3]oxazin-2-ona y su uso como inhibidores de IDH1 mutantes |
EP3316902A1 (en) | 2015-07-29 | 2018-05-09 | Novartis AG | Combination therapies comprising antibody molecules to tim-3 |
SI3317301T1 (sl) | 2015-07-29 | 2021-10-29 | Novartis Ag | Kombinirane terapije, ki obsegajo molekule protitelesa na LAG-3 |
BR112018008904A2 (pt) | 2015-11-03 | 2018-11-27 | Janssen Biotech Inc | anticorpos que se ligam especificamente a tim-3 e seus usos |
CA3007671A1 (en) | 2015-12-17 | 2017-06-22 | Novartis Ag | Antibody molecules to pd-1 and uses thereof |
WO2017140758A1 (en) | 2016-02-19 | 2017-08-24 | Debiopharm International S.A. | Derivatives of 2-amino-4-(2-oxazolidinon-3-yl)-pyrimidine fused with a five-membered heteroaromatic ring in 5,6-position which are useful for the treatment of various cancers |
CN107216312B (zh) * | 2016-03-22 | 2023-08-01 | 上海海和药物研究开发股份有限公司 | 一种具有突变型idh抑制活性的化合物、其制备方法及用途 |
EP3507367A4 (en) | 2016-07-05 | 2020-03-25 | Aduro BioTech, Inc. | CYCLIC DINUCLEOTID COMPOUNDS WITH INCLUDED NUCLEIC ACIDS AND USES THEREOF |
UY37695A (es) | 2017-04-28 | 2018-11-30 | Novartis Ag | Compuesto dinucleótido cíclico bis 2’-5’-rr-(3’f-a)(3’f-a) y usos del mismo |
US10800760B2 (en) | 2017-05-31 | 2020-10-13 | Nantbio, Inc. | Trk inhibition |
WO2018237173A1 (en) | 2017-06-22 | 2018-12-27 | Novartis Ag | ANTIBODY MOLECULES DIRECTED AGAINST CD73 AND CORRESPONDING USES |
WO2019061324A1 (en) | 2017-09-29 | 2019-04-04 | Curis Inc. | CRYSTALLINE FORMS OF IMMUNOMODULATORS |
SG11202003081WA (en) | 2017-10-11 | 2020-05-28 | Aurigene Discovery Tech Ltd | Crystalline forms of 3-substituted 1,2,4-oxadiazole |
WO2019087087A1 (en) | 2017-11-03 | 2019-05-09 | Aurigene Discovery Technologies Limited | Dual inhibitors of tim-3 and pd-1 pathways |
CN111386128A (zh) | 2017-11-06 | 2020-07-07 | 奥瑞基尼探索技术有限公司 | 用于免疫调节的联合疗法 |
CN115448923B (zh) * | 2018-02-13 | 2024-03-22 | 上海青煜医药科技有限公司 | 嘧啶并环化合物及其制备方法和应用 |
CN110407855A (zh) * | 2018-04-26 | 2019-11-05 | 上海嗣新生物科技有限公司 | 2-氨基嘧啶啶衍生物及其制备方法和用途 |
PL3797107T3 (pl) | 2018-05-21 | 2022-12-05 | Nerviano Medical Sciences S.R.L. | Heteroskondensowane związki pirydonów oraz ich zastosowanie jako inhibitory idh |
TW202015726A (zh) | 2018-05-30 | 2020-05-01 | 瑞士商諾華公司 | Entpd2抗體、組合療法、及使用該等抗體和組合療法之方法 |
CN109659001B (zh) * | 2018-12-18 | 2023-08-04 | 延安大学 | 一种防癌监管系统及方法 |
AU2020214804A1 (en) | 2019-02-01 | 2021-08-12 | Fmc Corporation | Diamino-substituted pyridines and pyrimidines as herbicides |
SG11202110376XA (en) | 2019-03-19 | 2021-10-28 | Voronoi Inc | Heteroaryl derivative, method for producing the same, and pharmaceutical composition comprising same as effective component |
WO2020227101A1 (en) * | 2019-05-03 | 2020-11-12 | Praxis Precision Medicines, Inc. | Kcnt1 inhibitors and methods of use |
JP2022548881A (ja) | 2019-09-18 | 2022-11-22 | ノバルティス アーゲー | Entpd2抗体、組合せ療法並びに抗体及び組合せ療法を使用する方法 |
CN111057051A (zh) * | 2019-12-16 | 2020-04-24 | 武汉九州钰民医药科技有限公司 | PI3K抑制剂Alpelisib的新合成方法 |
CN110964005A (zh) * | 2019-12-16 | 2020-04-07 | 武汉九州钰民医药科技有限公司 | 一种Alpelisib的制备工艺 |
CN111362925B (zh) * | 2020-05-26 | 2020-09-08 | 北京鑫开元医药科技有限公司 | 一种4-嘧啶甲酰胺类化合物、药物组合物、制备方法及应用 |
CA3189348A1 (en) | 2020-07-21 | 2022-01-27 | Daiichi Sankyo Company, Limited | Combination pharmaceutical of temozolomide and mutant idh1 enzyme inhibitor |
WO2022056453A1 (en) * | 2020-09-14 | 2022-03-17 | Totus Medicines Inc. | Therapeutic conjugates |
EP4356914A1 (en) * | 2021-06-15 | 2024-04-24 | Wigen Biomedicine Technology (Shanghai) Co., Ltd. | Idh mutant inhibitor and use thereof |
Family Cites Families (130)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB581334A (en) | 1943-09-29 | 1946-10-09 | Francis Henry Swinden Curd | New pyrimidine compounds |
JPS4921148B1 (es) | 1970-12-28 | 1974-05-30 | ||
JPS4921149B1 (es) | 1970-12-28 | 1974-05-30 | ||
AT340933B (de) | 1973-08-20 | 1978-01-10 | Thomae Gmbh Dr K | Verfahren zur herstellung neuer pyrimidinderivate und ihrer saureadditionssalze |
DE2341925A1 (de) | 1973-08-20 | 1975-03-06 | Thomae Gmbh Dr K | Neue pyrimidinderivate und verfahren zu ihrer herstellung |
US4994386A (en) | 1987-07-13 | 1991-02-19 | Pharmacia Diagnostics, Inc. | Production of HBLV virus in the HSB-2 cell line |
US4929726A (en) | 1988-02-09 | 1990-05-29 | Georgia State University Foundation, Inc. | Novel diazines and their method of preparation |
EP0330263A1 (en) | 1988-02-25 | 1989-08-30 | Merck & Co. Inc. | Piperazinylalkylpyrimidines as hypoglycemic agents |
GB9012311D0 (en) | 1990-06-01 | 1990-07-18 | Wellcome Found | Pharmacologically active cns compounds |
WO1992000970A1 (fr) | 1990-07-03 | 1992-01-23 | Mitsui Petrochemical Industries, Limited | Compose de pyrimidine et sel pharmaceutiquement acceptable de ce compose |
JP3145410B2 (ja) | 1995-04-13 | 2001-03-12 | 大鵬薬品工業株式会社 | 新規な4,6−ジアリールピリミジン誘導体及びその塩 |
JP3734907B2 (ja) | 1996-12-19 | 2006-01-11 | 富士写真フイルム株式会社 | 現像処理方法 |
AU727013B2 (en) | 1997-07-24 | 2000-11-30 | Zenyaku Kogyo Kabushiki Kaisha | Heterocyclic compound and antitumor agent comprising the same as effective component |
JPH11158073A (ja) | 1997-09-26 | 1999-06-15 | Takeda Chem Ind Ltd | アデノシンa3拮抗剤 |
US6440965B1 (en) | 1997-10-15 | 2002-08-27 | Krenitsky Pharmaceuticals, Inc. | Substituted pyrimidine derivatives, their preparation and their use in the treatment of neurodegenerative or neurological disorders of the central nervous system |
US6150362A (en) | 1997-12-12 | 2000-11-21 | Henkin; Jack | Triazine angiogenesis inhibitors |
DK0930302T3 (da) | 1998-01-16 | 2003-07-21 | Hoffmann La Roche | Benzosulfonderivater |
DE69919707T2 (de) | 1998-06-19 | 2005-09-01 | Chiron Corp., Emeryville | Glycogen synthase kinase 3 inhibitoren |
US7045519B2 (en) | 1998-06-19 | 2006-05-16 | Chiron Corporation | Inhibitors of glycogen synthase kinase 3 |
US6495558B1 (en) | 1999-01-22 | 2002-12-17 | Amgen Inc. | Kinase inhibitors |
AU768201B2 (en) | 1999-01-22 | 2003-12-04 | Amgen, Inc. | Kinase inhibitors |
CA2376951A1 (en) | 1999-06-30 | 2001-01-04 | Peter J. Sinclair | Src kinase inhibitor compounds |
US6498165B1 (en) | 1999-06-30 | 2002-12-24 | Merck & Co., Inc. | Src kinase inhibitor compounds |
AU6605200A (en) | 1999-06-30 | 2001-01-31 | Merck & Co., Inc. | Src kinase inhibitor compounds |
PE20010306A1 (es) | 1999-07-02 | 2001-03-29 | Agouron Pharma | Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa |
WO2001005783A1 (en) | 1999-07-15 | 2001-01-25 | Pharmacopeia, Inc. | Bradykinin b1 receptor antagonists |
JP2001089452A (ja) | 1999-09-22 | 2001-04-03 | Sankyo Co Ltd | ピリミジン誘導体 |
GB0018891D0 (en) | 2000-08-01 | 2000-09-20 | Novartis Ag | Organic compounds |
WO2001060816A1 (en) | 2000-02-17 | 2001-08-23 | Amgen Inc. | Kinase inhibitors |
EP1274705A1 (en) | 2000-03-29 | 2003-01-15 | Cyclacel Limited | 2-substituted 4-heteroaryl-pyrimidines and their use in the treatment of proliferative disorders |
CN100345830C (zh) | 2000-04-27 | 2007-10-31 | 安斯泰来制药有限公司 | 稠合杂芳基衍生物 |
WO2001083460A1 (fr) | 2000-04-28 | 2001-11-08 | Tanabe Seiyaku Co., Ltd. | Composes cycliques |
WO2002000647A1 (en) | 2000-06-23 | 2002-01-03 | Bristol-Myers Squibb Pharma Company | Heteroaryl-phenyl substituted factor xa inhibitors |
AU9502601A (en) | 2000-09-06 | 2002-03-22 | Chiron Corp | Inhibitors of glycogen synthase kinase 3 |
AU2001292670A1 (en) | 2000-09-15 | 2002-03-26 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
SE0004053D0 (sv) | 2000-11-06 | 2000-11-06 | Astrazeneca Ab | N-type calcium channel antagonists for the treatment of pain |
BR0116411A (pt) | 2000-12-21 | 2003-11-11 | Vertex Pharma | Compostos de pirazol úteis como inibidores de proteìna cinase |
US6995162B2 (en) | 2001-01-12 | 2006-02-07 | Amgen Inc. | Substituted alkylamine derivatives and methods of use |
EP1363890A4 (en) | 2001-02-07 | 2009-06-10 | Ore Pharmaceuticals Inc | MELANOCORTIN-4-RECEPTOR BINDING COMPOUNDS AND METHOD FOR THEIR APPLICATION |
AU2002258400A1 (en) | 2001-02-16 | 2002-08-28 | Tularik Inc. | Methods of using pyrimidine-based antiviral agents |
JP2004531571A (ja) | 2001-05-25 | 2004-10-14 | ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド | サイトカイン生産のインヒビターとしてのカルバメート及びオキサミド化合物 |
JP2005500294A (ja) | 2001-06-19 | 2005-01-06 | ブリストル−マイヤーズ スクイブ カンパニー | ホスホジエステラーゼ7に対するピリミジン阻害剤 |
US6603000B2 (en) | 2001-07-11 | 2003-08-05 | Boehringer Ingelheim Pharmaceuticals, Inc. | Synthesis for heteroarylamine compounds |
WO2003030909A1 (en) | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
DE60332433D1 (de) | 2002-03-15 | 2010-06-17 | Vertex Pharma | Azolylaminoazine als proteinkinasehemmer |
AU2003218215A1 (en) | 2002-03-15 | 2003-09-29 | Vertex Pharmaceuticals, Inc. | Azolylaminoazines as inhibitors of protein kinases |
WO2003078423A1 (en) | 2002-03-15 | 2003-09-25 | Vertex Pharmaceuticals, Inc. | Compositions useful as inhibitors of protein kinases |
EP1485381B8 (en) | 2002-03-15 | 2010-05-12 | Vertex Pharmaceuticals Incorporated | Azolylaminoazine as inhibitors of protein kinases |
US20040082627A1 (en) | 2002-06-21 | 2004-04-29 | Darrow James W. | Certain aromatic monocycles as kinase modulators |
AU2003275242B2 (en) | 2002-09-27 | 2010-03-04 | Merck Sharp & Dohme Corp. | Substituted pyrimidines |
AU2003288925A1 (en) | 2002-10-08 | 2004-05-04 | Massachusetts Institute Of Technology | Compounds for modulation of cholesterol transport |
US7223870B2 (en) | 2002-11-01 | 2007-05-29 | Pfizer Inc. | Methods for preparing N-arylated oxazolidinones via a copper catalyzed cross coupling reaction |
AU2003295776B2 (en) | 2002-11-21 | 2011-05-12 | Novartis Vaccines And Diagnostics, Inc. | 2,4,6-trisubstituted pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
EP1608622A4 (en) | 2003-03-24 | 2009-04-01 | Merck & Co Inc | BIARYLSUBSTITUTED 6-LOW HETEROCYCLES AS SODIUM CHANNEL BLOCKERS |
US20050014753A1 (en) | 2003-04-04 | 2005-01-20 | Irm Llc | Novel compounds and compositions as protein kinase inhibitors |
EP1610774A4 (en) | 2003-04-09 | 2008-07-16 | Exelixis Inc | TIE-2 MODULATORS AND METHODS OF USE |
CA2531490A1 (en) | 2003-07-15 | 2005-02-03 | Neurogen Corporation | Substituted pyrimidin-4-ylamina analogues as vanilloid receptor ligands |
AU2004257289A1 (en) | 2003-07-16 | 2005-01-27 | Neurogen Corporation | Biaryl piperazinyl-pyridine analogues |
PE20050952A1 (es) | 2003-09-24 | 2005-12-19 | Novartis Ag | Derivados de isoquinolina como inhibidores de b-raf |
AU2005232745A1 (en) | 2004-04-13 | 2005-10-27 | Astellas Pharma Inc. | Polycyclic pyrimidines as potassium ion channel modulators |
GB0415367D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
GB0415365D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
GB0415364D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
MY145822A (en) | 2004-08-13 | 2012-04-30 | Neurogen Corp | Substituted biaryl piperazinyl-pyridine analogues |
US7521457B2 (en) | 2004-08-20 | 2009-04-21 | Boehringer Ingelheim International Gmbh | Pyrimidines as PLK inhibitors |
EP1827434B1 (en) | 2004-11-30 | 2014-01-15 | Amgen Inc. | Quinolines and quinazoline analogs and their use as medicaments for treating cancer |
JP2008523156A (ja) | 2004-12-13 | 2008-07-03 | ニューロジェン・コーポレーション | 置換ビアリール類縁体 |
CN101080228A (zh) | 2004-12-13 | 2007-11-28 | 神经能质公司 | 哌嗪基-吡啶类似物 |
US7300931B2 (en) | 2004-12-28 | 2007-11-27 | Kinex Pharmaceuticals, Llc | Compositions for treating cell proliferation disorders |
AU2006206246A1 (en) | 2005-01-19 | 2006-07-27 | Neurogen Corporation | Heteroaryl substituted piperazinyl-pyridine analogues |
KR20070108916A (ko) | 2005-02-25 | 2007-11-13 | 쿠도스 파마슈티칼스 리미티드 | Mtor 억제제로서 작용하는 하이드라지노메틸,하이드라조노메틸 및 5-원 복소환 화합물 및 이의항암제로서의 용도 |
CA2606288A1 (en) | 2005-04-18 | 2006-10-26 | Neurogen Corporation | Subtituted heteroaryl cb1 antagonists |
GB2431156A (en) | 2005-10-11 | 2007-04-18 | Piramed Ltd | 1-cyclyl-3-substituted- -benzenes and -azines as inhibitors of phosphatidylinositol 3-kinase |
EP1979325A1 (en) | 2006-01-11 | 2008-10-15 | AstraZeneca AB | Morpholino pyrimidine derivatives and their use in therapy |
KR20080091814A (ko) | 2006-01-20 | 2008-10-14 | 쉐링 코포레이션 | 지질혈증장애의 치료를 위한 니코틴산 수용체 효능제로서의헤테로사이클 |
JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
RU2448964C2 (ru) | 2006-01-20 | 2012-04-27 | Шеринг Корпорейшн | КАРБОЦИКЛИЧЕСКИЕ И ГЕТЕРОЦИКЛИЧЕСКИЕ АРИЛСУЛЬФОНЫ, ИХ ПРИМЕНЕНИЕ И ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ НА ИХ ОСНОВЕ, ОБЛАДАЮЩАЯ СВОЙСТВАМИ ИНГИБИТОРА γ-СЕКРЕТАЗЫ |
RU2008130448A (ru) | 2006-01-27 | 2010-03-10 | Ф. Хоффманн-Ля Рош Аг (Ch) | Применение производных 4-имидазола для расстройств цнс |
WO2008080937A1 (en) | 2006-12-28 | 2008-07-10 | Basf Se | 2-substituted pyrimidines i in therapy |
CA2675558A1 (en) | 2007-02-06 | 2008-08-14 | Novartis Ag | Pi 3-kinase inhibitors and methods of their use |
US7957951B2 (en) | 2007-03-16 | 2011-06-07 | Robert Bosch Gmbh | Address translation system for use in a simulation environment |
AR067478A1 (es) | 2007-07-09 | 2009-10-14 | Astrazeneca Ab | Compuestos derivados de morfolina pirimidina |
WO2009066084A1 (en) | 2007-11-21 | 2009-05-28 | F. Hoffmann-La Roche Ag | 2 -morpholinopyrimidines and their use as pi3 kinase inhibitors |
AU2009221164B2 (en) | 2008-03-05 | 2012-07-26 | Novartis Ag | Use of pyrimidine derivatives for the treatment of EGFR dependent diseases or diseases that have acquired resistance to agents that target EGFR family members |
BRPI0909082A2 (pt) | 2008-03-26 | 2019-02-26 | Novartis Ag | imidazoquinolinas e derivados de pirimidina como moduladores potentes de processos angiogênicos acionados por vegf |
WO2009120094A2 (en) | 2008-03-27 | 2009-10-01 | Auckland Uniservices Limited | Substituted pyrimidines and triazines and their use in cancer therapy |
US8575338B2 (en) | 2008-04-09 | 2013-11-05 | Mitsubishi Tanabe Pharma Corporation | Pyrimidine, pyridine and triazine derivatives as maxi-K channel openers |
GB0815369D0 (en) | 2008-08-22 | 2008-10-01 | Summit Corp Plc | Compounds for treatment of duchenne muscular dystrophy |
EP2349275B1 (en) | 2008-10-31 | 2017-03-08 | Novartis AG | Combination of a phosphatidylinositol-3-kinase (pi3k) inhibitor and a mtor inhibitor. |
GB2465405A (en) | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
WO2010068863A2 (en) | 2008-12-12 | 2010-06-17 | Cystic Fibrosis Foundation Therapeutics, Inc. | Pyrimidine compounds and methods of making and using same |
AU2010211672B2 (en) | 2009-02-06 | 2016-08-04 | Nippon Shinyaku Co., Ltd. | Aminopyrazine derivative and medicine |
JP5747440B2 (ja) | 2009-02-06 | 2015-07-15 | 住友化学株式会社 | ヒドラジド化合物及びその有害生物防除用途 |
AU2010223919B2 (en) | 2009-03-13 | 2016-03-31 | Les Laboratoires Servier | Methods and compositions for cell-proliferation-related disorders |
WO2010120994A2 (en) | 2009-04-17 | 2010-10-21 | Wyeth Llc | Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis |
RU2011151603A (ru) | 2009-05-19 | 2013-06-27 | ДАУ АГРОСАЙЕНСИЗ ЭлЭсСи | Соединения и способы борьбы с грибами |
EP2451802A1 (en) | 2009-07-07 | 2012-05-16 | Pathway Therapeutics, Inc. | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
WO2011017296A1 (en) | 2009-08-04 | 2011-02-10 | Schering Corporation | 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors |
AR077999A1 (es) | 2009-09-02 | 2011-10-05 | Vifor Int Ag | Antagonistas de pirimidin y triazin-hepcidina |
CA2773848A1 (en) | 2009-09-09 | 2011-03-17 | Avila Therapeutics, Inc. | Pi3 kinase inhibitors and uses thereof |
US20120215788A1 (en) | 2009-11-18 | 2012-08-23 | Nokia Corporation | Data Processing |
ES2642109T3 (es) * | 2009-12-09 | 2017-11-15 | Agios Pharmaceuticals, Inc. | Compuestos terapéuticamente activos para su uso en el tratamiento de cáncer caracterizados por tener una mutación de IDH |
GB201004200D0 (en) | 2010-03-15 | 2010-04-28 | Univ Basel | Spirocyclic compounds and their use as therapeutic agents and diagnostic probes |
AR081626A1 (es) | 2010-04-23 | 2012-10-10 | Cytokinetics Inc | Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos |
US9133123B2 (en) | 2010-04-23 | 2015-09-15 | Cytokinetics, Inc. | Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use |
AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
US20130109643A1 (en) * | 2010-05-10 | 2013-05-02 | The Johns Hopkins University | Metabolic inhibitor against tumors having an idh mutation |
ES2704862T3 (es) | 2010-07-16 | 2019-03-20 | Agios Pharmaceuticals Inc | Composiciones terapéuticamente activas y su método de uso |
KR20130119928A (ko) | 2010-10-01 | 2013-11-01 | 노파르티스 아게 | 피리미딘 유도체의 제조 방법 |
LT2629776T (lt) | 2010-10-18 | 2017-11-10 | Cerenis Therapeutics Holding Sa | Junginiai, kompozicijos ir būdai, tinkami cholesterolio mobilizavimui |
GB201106829D0 (en) | 2011-04-21 | 2011-06-01 | Proximagen Ltd | Heterocyclic compounds |
CA2826387A1 (en) | 2011-02-11 | 2012-08-16 | Dana Farber Cancer Institute, Inc. | Method of inhibiting hamartoma tumor cells |
CN102827073A (zh) * | 2011-06-17 | 2012-12-19 | 安吉奥斯医药品有限公司 | 治疗活性组合物和它们的使用方法 |
CN103764130A (zh) | 2011-09-01 | 2014-04-30 | 诺华股份有限公司 | 用于治疗骨癌或者预防原发性癌细胞转移性播散入骨中的pi3k抑制剂 |
PE20141581A1 (es) | 2011-09-27 | 2014-11-14 | Novartis Ag | 3-pirmidin-4-il-oxazolidin-2-onas como inhibidores de la idh mutante |
CA2851082A1 (en) | 2011-10-06 | 2013-04-11 | Merck Sharp & Dohme Corp. | 1,3-substituted azetidine pde10 inhibitors |
UY34632A (es) | 2012-02-24 | 2013-05-31 | Novartis Ag | Compuestos de oxazolidin- 2- ona y usos de los mismos |
JP6345645B2 (ja) | 2012-04-02 | 2018-06-20 | サイトキネティックス, インコーポレイテッド | 横隔膜機能を向上させるための方法 |
CN104395458A (zh) | 2012-04-11 | 2015-03-04 | 赛特凯恩蒂克公司 | 改善对骨骼肌疲劳的抵抗力 |
JP6381523B2 (ja) | 2012-05-16 | 2018-08-29 | ノバルティス アーゲー | Pi−3キナーゼ阻害剤の投与レジメン |
BR112014028006A2 (pt) | 2012-05-30 | 2017-06-27 | Hoffmann La Roche | heterociclos de pirrolidino |
CN104349771A (zh) | 2012-06-06 | 2015-02-11 | 诺华股份有限公司 | 用于治疗肿瘤疾病的17α-羟化酶(C17,20-裂解酶)抑制剂和特定PI-3K抑制剂的组合 |
CN105050623B (zh) | 2012-08-16 | 2018-06-12 | 诺华股份有限公司 | Pi3k抑制剂和c-met抑制剂的组合 |
WO2014064058A1 (en) | 2012-10-23 | 2014-05-01 | Novartis Ag | Improved process for manufacturing 5-(2,6-di-4-morpholinyl-4-pyrimidinyl)-4-trifluoromethylpyridin-2-amine |
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 |
CN109568319A (zh) | 2013-01-10 | 2019-04-05 | 普尔莫凯恩股份有限公司 | 非选择性激酶抑制剂 |
ES2665619T3 (es) | 2013-03-14 | 2018-04-26 | Novartis Ag | 3-Pirimidin-4-il-oxazolidin-2-onas como inhibidores de IDH mutante |
WO2014181287A1 (en) | 2013-05-09 | 2014-11-13 | Piramal Enterprises Limited | Heterocyclyl compounds and uses thereof |
CN103483345B (zh) | 2013-09-25 | 2016-07-06 | 中山大学 | Pi3k激酶抑制剂、包含其的药物组合物及其应用 |
CN103694218B (zh) | 2013-12-05 | 2016-04-27 | 中山大学 | 嘧啶化合物、pi3k抑制剂、包含pi3k抑制剂的药物组合物及应用 |
-
2014
- 2014-03-12 ES ES14712785.6T patent/ES2665619T3/es active Active
- 2014-03-12 AU AU2014229313A patent/AU2014229313B2/en not_active Ceased
- 2014-03-12 GE GEAP201413934A patent/GEP201706699B/en unknown
- 2014-03-12 AP AP2015008707A patent/AP2015008707A0/xx unknown
- 2014-03-12 CN CN201480027484.7A patent/CN105263929B/zh active Active
- 2014-03-12 PE PE2015001929A patent/PE20151939A1/es not_active Application Discontinuation
- 2014-03-12 EA EA201591745A patent/EA028033B1/ru not_active IP Right Cessation
- 2014-03-12 KR KR1020157028897A patent/KR20150131224A/ko not_active Application Discontinuation
- 2014-03-12 WO PCT/IB2014/059695 patent/WO2014141104A1/en active Application Filing
- 2014-03-12 CA CA2903979A patent/CA2903979A1/en not_active Abandoned
- 2014-03-12 BR BR112015023412A patent/BR112015023412A8/pt not_active Application Discontinuation
- 2014-03-12 US US14/408,418 patent/US9434719B2/en active Active
- 2014-03-12 SG SG11201507063YA patent/SG11201507063YA/en unknown
- 2014-03-12 JP JP2015562496A patent/JP6387360B2/ja active Active
- 2014-03-12 EP EP14712785.6A patent/EP2970240B1/en active Active
- 2014-03-12 MX MX2015012552A patent/MX355945B/es active IP Right Grant
- 2014-03-13 US US14/208,015 patent/US20140275083A1/en not_active Abandoned
- 2014-03-13 TW TW103109158A patent/TW201444831A/zh unknown
- 2014-03-14 UY UY0001035470A patent/UY35470A/es not_active Application Discontinuation
- 2014-03-14 AR ARP140101012A patent/AR095311A1/es unknown
-
2015
- 2015-08-31 IL IL240972A patent/IL240972A0/en unknown
- 2015-09-02 ZA ZA2015/06452A patent/ZA201506452B/en unknown
- 2015-09-04 CL CL2015002472A patent/CL2015002472A1/es unknown
- 2015-09-04 TN TN2015000392A patent/TN2015000392A1/en unknown
- 2015-09-09 NI NI201500128A patent/NI201500128A/es unknown
- 2015-09-09 PH PH12015502018A patent/PH12015502018A1/en unknown
- 2015-09-14 CR CR20150491A patent/CR20150491A/es unknown
- 2015-09-14 DO DO2015000240A patent/DOP2015000240A/es unknown
- 2015-09-14 CU CUP2015000119A patent/CU20150119A7/es unknown
-
2016
- 2016-02-01 HK HK16101122.1A patent/HK1213251A1/zh unknown
- 2016-07-13 US US15/209,731 patent/US9688672B2/en active Active
-
2017
- 2017-04-27 US US15/499,824 patent/US10112931B2/en active Active
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PH12015502018A1 (en) | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh | |
MX2015012822A (es) | 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del idh mutante. | |
TN2014000128A1 (en) | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant idh | |
PH12018502125A1 (en) | Bipyrazole derivatives as jak inhibitors | |
PH12018500041A1 (en) | Substituted aza compoounds as irak-4 inhibitors | |
PH12016502382A1 (en) | Substituted indazole compounds as irak4 inhibitors | |
PH12017502407A1 (en) | Fused pyrimidine compound or salt thereof | |
GEP20207105B (en) | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors | |
MX2017004234A (es) | Inhibidor del egfr y preparacion y aplicacion del mismo. | |
MX2014002442A (es) | Inhibidores de pirrolopirazina cinasa. | |
MX2014005928A (es) | Inhibidores ciclicos de glutaminasa. | |
MX355088B (es) | Inhibidores de tienopirimidina de proteina cinasa c atipica. | |
EA201590661A1 (ru) | Азахиназолиновые ингибиторы атипичной протеинкиназы c | |
MX352928B (es) | Compuestos de piridazina-amida. | |
PH12016500225B1 (en) | Novel quinoline-substituted compound | |
GEP20166474B (en) | Pyrazolospiroketone derivatives for use as acetyl-coa carboxylase inhibitors | |
PH12016501461A1 (en) | 5-biphenyl-4-heteroarylcarbonylamino-pentanoic acid derivatives as neprilysin inhibitors | |
MX2016006975A (es) | Compuestos, composicion farmaceutica y metodos para su uso en el tratamiento de enfermedades inflamatorias. | |
MX2014013758A (es) | Derivados de tiazolcarboxamida para usarse como inhibidores de nampt. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant or registration |