PE20121159A1 - DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTOR - Google Patents
DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTORInfo
- Publication number
- PE20121159A1 PE20121159A1 PE2011001861A PE2011001861A PE20121159A1 PE 20121159 A1 PE20121159 A1 PE 20121159A1 PE 2011001861 A PE2011001861 A PE 2011001861A PE 2011001861 A PE2011001861 A PE 2011001861A PE 20121159 A1 PE20121159 A1 PE 20121159A1
- Authority
- PE
- Peru
- Prior art keywords
- amine
- mtor
- kinase
- pyridin
- methyl
- Prior art date
Links
- 108091007960 PI3Ks Proteins 0.000 title abstract 3
- 102000003993 Phosphatidylinositol 3-kinases Human genes 0.000 title abstract 3
- 108090000430 Phosphatidylinositol 3-kinases Proteins 0.000 title abstract 3
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 title abstract 2
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 title abstract 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 title 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 241000124008 Mammalia Species 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- JCXJVPUVTGWSNB-UHFFFAOYSA-N Nitrogen dioxide Chemical class O=[N]=O JCXJVPUVTGWSNB-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical group C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical group [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 abstract 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 abstract 1
- 229960002930 sirolimus Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
-
- 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
- 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
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)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17352009P | 2009-04-28 | 2009-04-28 | |
| US25853209P | 2009-11-05 | 2009-11-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20121159A1 true PE20121159A1 (es) | 2012-09-19 |
Family
ID=42315845
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001861A PE20121159A1 (es) | 2009-04-28 | 2010-04-27 | DERIVADOS DE PIRIDINA, PIRAZINA Y QUINOLINA COMO INHIBIDORES DE LA FOSFOINOSITIDA 3 CINASA Y LA mTOR |
Country Status (23)
| Country | Link |
|---|---|
| US (2) | US8362241B2 (enExample) |
| EP (1) | EP2424859B1 (enExample) |
| JP (1) | JP5697662B2 (enExample) |
| KR (1) | KR20120007540A (enExample) |
| CN (1) | CN102548984B (enExample) |
| AR (1) | AR076486A1 (enExample) |
| AU (1) | AU2010241723B2 (enExample) |
| BR (1) | BRPI1015262A2 (enExample) |
| CA (1) | CA2758986C (enExample) |
| CL (1) | CL2011002691A1 (enExample) |
| CO (1) | CO6440596A2 (enExample) |
| CR (1) | CR20110634A (enExample) |
| EA (1) | EA019700B1 (enExample) |
| IL (1) | IL215731A0 (enExample) |
| MA (1) | MA34207B1 (enExample) |
| MX (1) | MX2011011335A (enExample) |
| NZ (1) | NZ595572A (enExample) |
| PE (1) | PE20121159A1 (enExample) |
| SG (1) | SG175364A1 (enExample) |
| TW (1) | TW201103902A (enExample) |
| UY (1) | UY32582A (enExample) |
| WO (1) | WO2010126895A1 (enExample) |
| ZA (1) | ZA201108101B (enExample) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2474147T3 (es) * | 2008-05-30 | 2014-07-08 | Amgen, Inc | Inhibidores de PI3 cinasa |
| WO2010108074A2 (en) | 2009-03-20 | 2010-09-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| UY32582A (es) * | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| FR2958290B1 (fr) | 2010-03-30 | 2012-10-19 | Sanofi Aventis | Procede de preparation de derives de sulfonamido-benzofurane |
| JO2998B1 (ar) | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| HUP1000330A2 (en) | 2010-06-18 | 2011-12-28 | Sanofi Sa | Process for the preparation of dronedarone and the novel intermediates |
| US9216981B2 (en) | 2010-12-02 | 2015-12-22 | Medpacto, Inc. | Purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, pharmaceutically acceptable salt thereof, preparation method thereof, and pharmaceutical composition with inhibitory activity against Raf kinase, containing same as active ingredient |
| US9284270B2 (en) | 2011-02-14 | 2016-03-15 | The Governers Of The University Of Alberta | Boronic acid catalysts and methods of use thereof for activation and transformation of carboxylic acids |
| AU2012225382B2 (en) * | 2011-03-09 | 2016-10-27 | Celgene Avilomics Research, Inc. | PI3 kinase inhibitors and uses thereof |
| HUP1100165A2 (en) | 2011-03-29 | 2012-12-28 | Sanofi Sa | Process for preparation of dronedarone by n-butylation |
| HUP1100167A2 (en) | 2011-03-29 | 2012-11-28 | Sanofi Sa | Process for preparation of dronedarone by mesylation |
| HUE059230T2 (hu) * | 2011-06-10 | 2022-10-28 | Merck Patent Gmbh | Vegyületek és eljárások BTK-inhibitor aktivitású pirimidin és piridin vegyületek elõállítására |
| EP2760845B1 (en) | 2011-09-27 | 2016-11-16 | Amgen Inc. | Heterocyclic compounds as mdm2 inhibitors for the treatment of cancer |
| CN103102349B (zh) * | 2011-11-14 | 2017-03-15 | 北京赛林泰医药技术有限公司 | 蛋白激酶抑制剂及其组合物和用途 |
| CN103974954B (zh) * | 2011-11-14 | 2016-08-24 | 北京赛林泰医药技术有限公司 | 调节激酶的化合物、含有它们的组合物及其用途 |
| FR2983198B1 (fr) | 2011-11-29 | 2013-11-15 | Sanofi Sa | Procede de preparation de derives de 5-amino-benzoyl-benzofurane |
| EP2617718A1 (en) | 2012-01-20 | 2013-07-24 | Sanofi | Process for preparation of dronedarone by the use of dibutylaminopropanol reagent |
| US9221778B2 (en) | 2012-02-13 | 2015-12-29 | Sanofi | Process for preparation of dronedarone by removal of hydroxyl group |
| US9249119B2 (en) * | 2012-02-14 | 2016-02-02 | Sanofi | Process for the preparation of dronedarone by oxidation of a sulphenyl group |
| US9382223B2 (en) | 2012-02-22 | 2016-07-05 | Sanofi | Process for preparation of dronedarone by oxidation of a hydroxyl group |
| WO2013178337A1 (en) | 2012-05-31 | 2013-12-05 | Sanofi | Process for preparation of dronedarone by grignard reaction |
| HK1206331A1 (en) * | 2012-08-09 | 2016-01-08 | Neuropore Therapies, Inc. | Aryl-and heteroaryl-substituted benzene derivatives as modulators of pi3-kinase signalling pathways |
| FR2994572B1 (fr) * | 2012-08-17 | 2015-04-17 | Centre Nat Rech Scient | Pyrido[3,2-d]pyrimidines trisubstituees, leurs procedes de preparation et leurs utilisation en therapeutique |
| AU2014219075C1 (en) | 2013-02-19 | 2018-09-06 | Amgen Inc. | Cis-morpholinone and other compounds as MDM2 inhibitors for the treatment of cancer |
| MX374513B (es) | 2013-03-14 | 2025-03-06 | Amgen Inc | Compuestos de morfolinona de ácido heteroarilo como inhibidores mdm2 para el tratamiento de cáncer. |
| WO2014177915A1 (en) | 2013-05-01 | 2014-11-06 | Piramal Enterprises Limited | Cancer combination therapy using imidazo[4,5-c]quinoline derivatives |
| JOP20200296A1 (ar) | 2013-06-10 | 2017-06-16 | Amgen Inc | عمليات صنع وأشكال بلورية من mdm2 مثبط |
| EP3024456A4 (en) | 2013-07-26 | 2017-04-12 | Update Pharma Inc. | Combinatorial methods to improve the therapeutic benefit of bisantrene |
| CN104418849B (zh) * | 2013-09-02 | 2020-04-21 | 广东东阳光药业有限公司 | 取代的氨基嘧啶类化合物及其使用方法和用途 |
| WO2015048318A1 (en) * | 2013-09-25 | 2015-04-02 | Vertex Pharmaceuticals Incorporated | A selective inhibitor of phosphatidylinositol 3-kinase-gamma |
| AU2014346354A1 (en) | 2013-11-11 | 2016-05-26 | Amgen Inc. | Combination therapy including an MDM2 inhibitor and one or more additional pharmaceutically active agents for the treatment of cancers |
| CN104744446B (zh) * | 2013-12-30 | 2019-06-25 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| BR112016029662B1 (pt) | 2014-06-19 | 2023-10-24 | Takeda Pharmaceutical Company Limited | COMPOSTO DE FÓRMULA Bf OU UMA FORMA FARMACEUTICAMENTE ACEITÁVEL DO MESMO, COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO O MESMO E SEU USO |
| RU2760373C2 (ru) | 2015-09-18 | 2021-11-24 | Какен Фармасьютикал Ко., Лтд. | Биарильное производное и содержащее его лекарственное средство |
| KR102031033B1 (ko) | 2016-02-03 | 2019-11-18 | 삼진제약주식회사 | 라프 키나제 및 혈관내피성장인자 수용체(vegfr2)를 저해하는 피리딘 유도체, 이의 제조방법, 이를 포함하는 약제학적 조성물 및 이의 용도 |
| TW201825465A (zh) | 2016-09-23 | 2018-07-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201815787A (zh) | 2016-09-23 | 2018-05-01 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| TW201813963A (zh) | 2016-09-23 | 2018-04-16 | 美商基利科學股份有限公司 | 磷脂醯肌醇3-激酶抑制劑 |
| WO2018071794A1 (en) * | 2016-10-14 | 2018-04-19 | Nimbus Lakshmi, Inc. | Tyk2 inhibitors and uses thereof |
| EP3538091A4 (en) | 2016-11-08 | 2020-06-10 | Navitor Pharmaceuticals, Inc. | PHENYL AMINO PIPERIDINE MTORC INHIBITORS AND USES THEREOF |
| JP6469272B2 (ja) * | 2017-03-01 | 2019-02-13 | 科研製薬株式会社 | ビアリール誘導体又はその塩からなる医薬 |
| MX2019011002A (es) | 2017-03-14 | 2019-12-16 | Basf Se | Azinas herbicidas. |
| JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| CN116003405A (zh) | 2017-09-08 | 2023-04-25 | 美国安进公司 | Kras g12c的抑制剂及其使用方法 |
| CA3080578A1 (en) | 2017-10-30 | 2019-05-09 | Neuropore Therapies, Inc. | Substituted phenyl sulfonyl phenyl triazole thiones and uses thereof |
| BR112020018094A2 (pt) * | 2018-03-08 | 2020-12-22 | Incyte Corporation | Compostos de aminopirazina diol como inibidores de pi3k-¿ |
| EP3788038B1 (en) | 2018-05-04 | 2023-10-11 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| EP4234547A3 (en) | 2018-05-14 | 2023-11-01 | Takeda Pharmaceutical Company Limited | Pharmaceutical salts of pyrimidine derivatives and method of treating disorders |
| EP3807276B1 (en) | 2018-06-12 | 2025-12-10 | Amgen Inc. | Kras g12c inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer |
| WO2020010003A1 (en) | 2018-07-02 | 2020-01-09 | Incyte Corporation | AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS |
| KR20250171404A (ko) | 2018-08-31 | 2025-12-08 | 암젠 인크 | Mdm2 억제제의 제조 방법 |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| EP3898589A2 (de) * | 2018-12-21 | 2021-10-27 | Saltigo GmbH | Verfahren zur herstellung von 2-alkoxy-4-amino-5-methyl-pyridinen und/oder von 2-alkoxy-4-alkylamino-5-methyl-pyridinen |
| WO2020146779A1 (en) * | 2019-01-11 | 2020-07-16 | The Regents Of The University Of California | mTORC1 INHIBITORS FOR ACTIVATING AUTOPHAGY |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| KR20220011670A (ko) | 2019-05-21 | 2022-01-28 | 암젠 인크 | 고체 상태 형태 |
| US20240139193A1 (en) | 2019-10-15 | 2024-05-02 | Amgen Inc. | Combination therapy of kras inhibitor and shp2 inhibitor for treatment of cancers |
| US20230028414A1 (en) | 2019-12-16 | 2023-01-26 | Amgen Inc. | Dosing regimen of kras g12c inhibitor |
| KR102852061B1 (ko) * | 2020-03-09 | 2025-08-27 | 삼성중공업 주식회사 | 선박용 볼라드 |
| EP4169914A4 (en) * | 2020-06-23 | 2024-07-24 | Shenzhen Forward Pharmaceuticals Co., Ltd. | SALT OF A COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SALT |
| CN116283467B (zh) * | 2023-01-18 | 2024-06-11 | 四川大学 | 一种合成二芳基烷基甲烷的方法 |
Family Cites Families (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU6526896A (en) | 1995-07-22 | 1997-02-18 | Rhone-Poulenc Rorer Limited | Substituted aromatic compounds and their pharmaceutical use |
| CA2394639A1 (en) | 1999-12-15 | 2001-06-21 | Danny Peter Claude Mcgee | Salicylamides as serine protease and factor xa inhibitors |
| NZ521245A (en) | 2000-03-17 | 2004-04-30 | Bristol Myers Squibb Pharma Co | Beta-amino acid derivatives as inhibitors of matrix metalloproteases and TNF-alpha |
| CN1186324C (zh) | 2000-04-27 | 2005-01-26 | 山之内制药株式会社 | 稠合杂芳基衍生物 |
| US6864255B2 (en) | 2001-04-11 | 2005-03-08 | Amgen Inc. | Substituted triazinyl amide derivatives and methods of use |
| US20030187026A1 (en) | 2001-12-13 | 2003-10-02 | Qun Li | Kinase inhibitors |
| WO2003093297A2 (en) | 2002-05-03 | 2003-11-13 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| US7015227B2 (en) | 2002-06-21 | 2006-03-21 | Cgi Pharmaceuticals, Inc. | Certain amino-substituted monocycles as kinase modulators |
| US20040082627A1 (en) | 2002-06-21 | 2004-04-29 | Darrow James W. | Certain aromatic monocycles as kinase modulators |
| WO2004099127A1 (en) | 2003-05-07 | 2004-11-18 | Novo Nordisk A/S | Novel compounds as kinase inhibitors |
| US7781591B2 (en) | 2006-06-13 | 2010-08-24 | Wyeth Llc | Substituted 3-cyanopyridines as protein kinase inhibitors |
| US7435823B2 (en) | 2004-01-23 | 2008-10-14 | Amgen Inc. | Compounds and methods of use |
| CA2564355C (en) | 2004-05-07 | 2012-07-03 | Amgen Inc. | Protein kinase modulators and method of use |
| GB0415364D0 (en) | 2004-07-09 | 2004-08-11 | Astrazeneca Ab | Pyrimidine derivatives |
| ES2395196T3 (es) | 2005-03-11 | 2013-02-11 | Zenyaku Kogyo Kabushikikaisha | Agente inmunosupresor que comprende un compuesto heterocíclico como ingrediente activo |
| WO2006123165A2 (en) | 2005-05-19 | 2006-11-23 | Astex Therapeutics Limited | Pyrimidine derivatives as hsp90 inhibitors |
| WO2007011721A1 (en) | 2005-07-15 | 2007-01-25 | Kalypsys, Inc. | Inhibitors of mitotic kinesin |
| GB0520657D0 (en) * | 2005-10-11 | 2005-11-16 | Ludwig Inst Cancer Res | Pharmaceutical compounds |
| US7989461B2 (en) | 2005-12-23 | 2011-08-02 | Amgen Inc. | Substituted quinazolinamine compounds for the treatment of cancer |
| JO2660B1 (en) | 2006-01-20 | 2012-06-17 | نوفارتيس ايه جي | Pi-3 inhibitors and methods of use |
| WO2007087276A1 (en) | 2006-01-23 | 2007-08-02 | Amgen Inc. | Aurora kinase modulators and method of use |
| JP2009525978A (ja) * | 2006-02-06 | 2009-07-16 | アイアールエム・リミテッド・ライアビリティ・カンパニー | プロテインキナーゼ阻害剤としての化合物および組成物 |
| ES2365258T3 (es) * | 2006-06-26 | 2011-09-27 | Ucb Pharma S.A. | Derivados de tiazol condensados como inhibidores de quinasa. |
| WO2008032089A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidaz0lyl-2-m0rph0lin0-6-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| WO2008032041A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | Pyrimidine derivatives having inhibitory activity against pi3k enzymes |
| WO2008032077A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | Pyrimidine derivatives |
| WO2008032036A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 6-benzimidaz0lyl-2-m0rph0lin0-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| CN101595103A (zh) | 2006-09-14 | 2009-12-02 | 阿斯利康(瑞典)有限公司 | 嘧啶衍生物 |
| WO2008032028A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 2 -benzimidazolyl- 6 -morpholino-4- (azetidine, pyrrolidine, piperidine or azepine) pyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| US20090325954A1 (en) | 2006-09-14 | 2009-12-31 | Sam Butterworth | 2-benzimidazolyl-6-morpholino-4-phenylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| WO2008032060A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidaz0lyl-6-m0rph0lin0-2-piperazinylpyrimidine derivatives as p13k and mtor inhibitors for the treatment of proliferative disorders |
| WO2008032033A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidazolyl-2-morpholino-6-piperazinylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| EP2064203A1 (en) | 2006-09-14 | 2009-06-03 | AstraZeneca AB | 2-benzimidaz0lyl-6-m0rph0lin0-4-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| WO2008032091A1 (en) | 2006-09-14 | 2008-03-20 | Astrazeneca Ab | 4-benzimidaz0lyl-6-m0rph0lin0-2-piperidin-4-ylpyrimidine derivatives as pi3k and mtor inhibitors for the treatment of proliferative disorders |
| EA200901065A1 (ru) | 2007-02-06 | 2010-02-26 | Новартис Аг | Ингибиторы pi 3-киназы и способы их применения |
| WO2009007751A2 (en) | 2007-07-09 | 2009-01-15 | Astrazeneca Ab | Trisubstituted pyrimidine derivatives for the treatment of proliferative diseases |
| AR067478A1 (es) | 2007-07-09 | 2009-10-14 | Astrazeneca Ab | Compuestos derivados de morfolina pirimidina |
| ATE554075T1 (de) | 2007-07-09 | 2012-05-15 | Astrazeneca Ab | Bei mit mtor-kinase und/oder pi3k in zusammenhang stehenden krankheiten angewendete morpholinopyrimidinderivate |
| EA201000104A1 (ru) | 2007-07-26 | 2010-08-30 | Новартис Аг | Производные пиримидина, применимые для лечения воспалительных или аллергических патологических состояний |
| EP2211615A4 (en) | 2007-10-22 | 2010-10-13 | Glaxosmithkline Llc | PYRIDOSULFONAMIDE DERIVATIVES AS PI3 KINASE INHIBITORS |
| WO2009093981A1 (en) | 2008-01-23 | 2009-07-30 | S Bio Pte Ltd | Triazine compounds as kinase inhibitors |
| US8268834B2 (en) | 2008-03-19 | 2012-09-18 | Novartis Ag | Pyrazine derivatives that inhibit phosphatidylinositol 3-kinase enzyme |
| WO2009120094A2 (en) | 2008-03-27 | 2009-10-01 | Auckland Uniservices Limited | Substituted pyrimidines and triazines and their use in cancer therapy |
| AP2775A (en) | 2008-05-23 | 2013-09-30 | Wyeth Llc | Triazine compounds as P13 kinase and MTOR inhibitors |
| WO2010014939A1 (en) | 2008-07-31 | 2010-02-04 | Genentech, Inc. | Pyrimidine compounds, compositions and methods of use |
| TW201022208A (en) | 2008-10-30 | 2010-06-16 | Herbalscience Group Llc | Tryptase enzyme inhibiting aminopyridines |
| AU2009309019B2 (en) | 2008-10-31 | 2014-11-13 | Merck Sharp & Dohme Llc | P2X3, receptor antagonists for treatment of pain |
| GB2465405A (en) | 2008-11-10 | 2010-05-19 | Univ Basel | Triazine, pyrimidine and pyridine analogues and their use in therapy |
| WO2010061903A1 (ja) | 2008-11-27 | 2010-06-03 | 塩野義製薬株式会社 | Pi3k阻害活性を有するピリミジン誘導体およびピリジン誘導体 |
| MX2011006333A (es) | 2008-12-23 | 2011-06-27 | Abbott Lab | Compuestos antivirales. |
| BRPI1008376B1 (pt) | 2009-02-10 | 2021-08-31 | Janssen Pharmaceutica Nv | Quinazolinonas como inibidores de prolil hidroxilase |
| JP2012518037A (ja) | 2009-02-18 | 2012-08-09 | アムジエン・インコーポレーテツド | mTORキナーゼ阻害剤としてのインドール/ベンゾイミダゾール化合物 |
| EP2403847B1 (en) | 2009-03-06 | 2016-03-02 | UCB Biopharma SPRL | Triazine derivatives as kinase inhibitors |
| WO2010110686A1 (en) | 2009-03-27 | 2010-09-30 | Pathway Therapeutics Limited | Pyrimidinyl and 1,3,5 triazinyl benzimidazoles and their use in cancer therapy |
| SG174527A1 (en) | 2009-03-27 | 2011-11-28 | Pathway Therapeutics Inc | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
| UY32582A (es) * | 2009-04-28 | 2010-11-30 | Amgen Inc | Inhibidores de fosfoinositida 3 cinasa y/u objetivo mamífero |
| JP2012529512A (ja) | 2009-06-08 | 2012-11-22 | アブラクシス バイオサイエンス リミテッド ライアビリティー カンパニー | トリアジン誘導体類及びそれらの治療応用 |
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- 2010-04-27 EA EA201101583A patent/EA019700B1/ru not_active IP Right Cessation
- 2010-04-27 KR KR1020117028155A patent/KR20120007540A/ko not_active Withdrawn
- 2010-04-27 CN CN201080030184.6A patent/CN102548984B/zh not_active Expired - Fee Related
- 2010-04-27 US US12/768,602 patent/US8362241B2/en active Active
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- 2010-04-27 PE PE2011001861A patent/PE20121159A1/es not_active Application Discontinuation
- 2010-04-27 JP JP2012508595A patent/JP5697662B2/ja active Active
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- 2010-04-27 AU AU2010241723A patent/AU2010241723B2/en active Active
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- 2010-04-28 AR ARP100101435A patent/AR076486A1/es not_active Application Discontinuation
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Also Published As
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|---|---|
| US20100273764A1 (en) | 2010-10-28 |
| CR20110634A (es) | 2012-01-06 |
| CN102548984A (zh) | 2012-07-04 |
| TW201103902A (en) | 2011-02-01 |
| AU2010241723A1 (en) | 2011-11-17 |
| US20130079303A1 (en) | 2013-03-28 |
| EP2424859B1 (en) | 2015-04-08 |
| CA2758986A1 (en) | 2010-11-04 |
| KR20120007540A (ko) | 2012-01-20 |
| SG175364A1 (en) | 2011-11-28 |
| CL2011002691A1 (es) | 2012-03-16 |
| UY32582A (es) | 2010-11-30 |
| CA2758986C (en) | 2014-05-27 |
| MX2011011335A (es) | 2011-11-18 |
| IL215731A0 (en) | 2012-01-31 |
| NZ595572A (en) | 2013-07-26 |
| EP2424859A1 (en) | 2012-03-07 |
| US8772480B2 (en) | 2014-07-08 |
| EA201101583A1 (ru) | 2012-05-30 |
| JP5697662B2 (ja) | 2015-04-08 |
| MA34207B1 (fr) | 2013-05-02 |
| WO2010126895A1 (en) | 2010-11-04 |
| CO6440596A2 (es) | 2012-05-15 |
| ZA201108101B (en) | 2012-07-25 |
| CN102548984B (zh) | 2015-11-25 |
| AU2010241723B2 (en) | 2012-12-13 |
| EA019700B1 (ru) | 2014-05-30 |
| JP2012525395A (ja) | 2012-10-22 |
| AR076486A1 (es) | 2011-06-15 |
| HK1167862A1 (en) | 2012-12-14 |
| BRPI1015262A2 (pt) | 2016-05-03 |
| US8362241B2 (en) | 2013-01-29 |
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