ES2431163T3 - Inhibidores de PIM quinasa y métodos para su uso - Google Patents
Inhibidores de PIM quinasa y métodos para su uso Download PDFInfo
- Publication number
- ES2431163T3 ES2431163T3 ES08731299T ES08731299T ES2431163T3 ES 2431163 T3 ES2431163 T3 ES 2431163T3 ES 08731299 T ES08731299 T ES 08731299T ES 08731299 T ES08731299 T ES 08731299T ES 2431163 T3 ES2431163 T3 ES 2431163T3
- Authority
- ES
- Spain
- Prior art keywords
- substituted
- cycloalkyl
- alkyl
- amino
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- -1 amino, aminocarbonyl Chemical group 0.000 abstract 11
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 229910052739 hydrogen Inorganic materials 0.000 abstract 3
- 239000001257 hydrogen Substances 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 abstract 2
- 150000002431 hydrogen Chemical group 0.000 abstract 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 2
- 229910006069 SO3H Inorganic materials 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000004423 acyloxy group Chemical group 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000006598 aminocarbonylamino group Chemical group 0.000 abstract 1
- 125000004682 aminothiocarbonyl group Chemical group NC(=S)* 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 125000005415 substituted alkoxy group Chemical group 0.000 abstract 1
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 abstract 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 abstract 1
- 125000003441 thioacyl group Chemical group 0.000 abstract 1
- 125000003396 thiol group Chemical class [H]S* 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- 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
- 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un compuesto de Fórmula II, o un estereoisómero, tautómero, o sal farmacéuticamente aceptable de los mismos, **Fórmula** en donde, Y es cicloalquilo, heterocicloalquilo, arilo o heteroarilo sustituidos o no sustituidos; Z3 se seleccionan a partir de CR2 y N; R1 se selecciona a partir del grupo que consiste en hidrógeno, halógeno, alquilo, cicloalquilo, -CN, -NO2, y -NHR3; cada R2 se selecciona independientemente a partir del grupo que consiste en hidrógeno, halógeno, hidroxilo, nitro, ciano, SO3H y alquilo, alquenilo, alquinilo, alcoxilo, amino, aminocarbonilo, aminotiocarboniio, aminocarbonilamino, aminotiocarboniIamino, aminocarboniloxi, aminosuifonilo, aminosulfoniloxi, aminosulfonilamino, amidino, carboxilo, carboxil éster, (carboxiI éster)amino, (carboxiI éster)oxi, sulfonilo, sulfoniloxi, tioacilo, tiol, alquiltio, arilo, heteroarilo, cicloalquilo, hetero cicloalquilo, cicloalquilo parcialmente saturado, ariloxi, heteroariloxi, heterocicliloxi, cicloalquiloxi, acilo, aciIamino, y aciloxi sustituidos o no sustituidos; R3 se selecciona a partir del grupo que consiste de hidrógeno, -CO-R4 y alquilo, cicloalquilo, heterociclilo, arilo, y heteroarilo sustituidos o no sustituidos; y R4 se selecciona a partir del grupo que consiste de alquilo, alquilo sustituido, alcoxi, alcoxi sustituido, amino, amino sustituido, y aIquiIamino.
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89244407P | 2007-03-01 | 2007-03-01 | |
| US892444P | 2007-03-01 | ||
| US2377708P | 2008-01-25 | 2008-01-25 | |
| US23777 | 2008-01-25 | ||
| PCT/US2008/055724 WO2008106692A1 (en) | 2007-03-01 | 2008-03-03 | Pim kinase inhibitors and methods of their use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2431163T3 true ES2431163T3 (es) | 2013-11-25 |
Family
ID=39433847
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES08731299T Active ES2431163T3 (es) | 2007-03-01 | 2008-03-03 | Inhibidores de PIM quinasa y métodos para su uso |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US8822497B2 (es) |
| EP (1) | EP2132177B1 (es) |
| JP (1) | JP5330274B2 (es) |
| KR (1) | KR101514853B1 (es) |
| CN (1) | CN101679266B (es) |
| AU (1) | AU2008221263B2 (es) |
| BR (1) | BRPI0808523A2 (es) |
| CA (1) | CA2679659C (es) |
| EA (1) | EA019951B1 (es) |
| ES (1) | ES2431163T3 (es) |
| MX (1) | MX2009009304A (es) |
| WO (1) | WO2008106692A1 (es) |
Families Citing this family (155)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8088928B2 (en) | 2005-08-04 | 2012-01-03 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| US8093401B2 (en) | 2005-08-04 | 2012-01-10 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| AU2006278504B2 (en) | 2005-08-04 | 2013-01-17 | Sirtris Pharmaceuticals, Inc. | Imidazopyridine derivatives as sirtuin modulating agents |
| US7855289B2 (en) | 2005-08-04 | 2010-12-21 | Sirtris Pharmaceuticals, Inc. | Sirtuin modulating compounds |
| KR101391900B1 (ko) | 2005-12-13 | 2014-05-02 | 인사이트 코포레이션 | 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로[2,3-b]피리딘 및 피롤로[2,3-b]피리미딘 |
| AU2007314305B2 (en) | 2006-10-31 | 2013-01-24 | Merck Sharp & Dohme Corp. | 2-aminothiazole-4-carboxylic amides as protein kinase inhibitors |
| AU2007314342B2 (en) | 2006-10-31 | 2013-02-21 | Merck Sharp & Dohme Corp. | Anilinopiperazine Derivatives and methods of use thereof |
| US20140249135A1 (en) * | 2007-03-01 | 2014-09-04 | Novartis Ag | Pim kinase inhibitors and methods of their use |
| KR20100007956A (ko) | 2007-05-03 | 2010-01-22 | 화이자 리미티드 | 나트륨 채널 조절제로서의 2-피리딘 카복스아마이드 유도체 |
| WO2008157208A2 (en) | 2007-06-13 | 2008-12-24 | Incyte Corporation | Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile |
| CL2008001822A1 (es) | 2007-06-20 | 2009-03-13 | Sirtris Pharmaceuticals Inc | Compuestos derivados de tiazolo[5,4-b]piridina; composicion farmaceutica que comprende a dichos compuestos; y uso del compuesto en el tratamiento de la resistencia a la insulina, sindrome metabolico, diabetes, entre otras. |
| TW200918542A (en) | 2007-06-20 | 2009-05-01 | Sirtris Pharmaceuticals Inc | Sirtuin modulating compounds |
| PE20090837A1 (es) | 2007-07-02 | 2009-07-24 | Boehringer Ingelheim Int | Nuevos compuestos quimicos |
| CN101801958B (zh) * | 2007-07-19 | 2014-01-29 | 默沙东公司 | 作为蛋白质激酶抑制剂的杂环酰胺化合物 |
| JP5349309B2 (ja) * | 2007-08-03 | 2013-11-20 | 株式会社キノファーマ | 抗dnaウイルス作用を有するアニリン誘導体 |
| AU2008319267A1 (en) * | 2007-11-01 | 2009-05-07 | Sirtris Pharmaceuticals, Inc. | Amide derivatives as sirtuin modulators |
| AR070531A1 (es) * | 2008-03-03 | 2010-04-14 | Novartis Ag | Inhibidores de cinasa pim y metodos para su uso |
| CL2009001152A1 (es) | 2008-05-13 | 2009-10-16 | Array Biopharma Inc | Compuestos derivados de n-(4-(cicloalquilo nitrogenado-1-il)-1h-pirrolo[2,3-b]piridin-3-il)amida, inhibidores de cinasa; proceso de preparacion; composicion farmaceutica; y su uso para el tratamiento de una enfermedad proliferativa. |
| BRPI0918268B1 (pt) | 2008-09-02 | 2021-08-03 | Novartis Ag | Derivados de picolinamida, seu uso, e composição farmacêutica |
| AU2011265439B2 (en) * | 2008-09-02 | 2012-09-20 | Novartis Ag | Picolinamide derivatives as kinase inhibitors |
| JP5603869B2 (ja) * | 2008-09-29 | 2014-10-08 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規化合物 |
| US8110578B2 (en) | 2008-10-27 | 2012-02-07 | Signal Pharmaceuticals, Llc | Pyrazino[2,3-b]pyrazine mTOR kinase inhibitors for oncology indications and diseases associated with the mTOR/PI3K/Akt pathway |
| WO2010054398A1 (en) | 2008-11-10 | 2010-05-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| AU2009327357C1 (en) | 2008-12-19 | 2017-02-02 | Vertex Pharmaceuticals Incorporated | Pyrazine derivatives useful as inhibitors of ATR kinase |
| CN102388054B (zh) | 2008-12-19 | 2015-03-04 | 西特里斯药业公司 | 噻唑并吡啶沉默调节蛋白调节剂的化合物 |
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| DK2432472T3 (da) | 2009-05-22 | 2019-11-18 | Incyte Holdings Corp | 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer |
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| WO2012178123A1 (en) | 2011-06-22 | 2012-12-27 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
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| ES2649995T3 (es) | 2011-07-18 | 2018-01-16 | Merck Patent Gmbh | Benzamidas |
| US9416132B2 (en) | 2011-07-21 | 2016-08-16 | Tolero Pharmaceuticals, Inc. | Substituted imidazo[1,2-b]pyridazines as protein kinase inhibitors |
| US9458151B2 (en) | 2011-08-11 | 2016-10-04 | Jikai Biosciences, Inc. | Isothiazole derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| CN102924446B (zh) * | 2011-08-11 | 2015-08-26 | 上海吉铠医药科技有限公司 | Pim激酶抑制剂及其制备方法与在制药中的应用 |
| US9452995B2 (en) | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyridine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| US9453003B2 (en) | 2011-08-11 | 2016-09-27 | Jikai Biosciences, Inc. | Pyrimidine derivatives as PIM kinase inhibitors and preparation methods and use in medicinal manufacture thereof |
| TW201313721A (zh) | 2011-08-18 | 2013-04-01 | Incyte Corp | 作為jak抑制劑之環己基氮雜環丁烷衍生物 |
| UA111854C2 (uk) | 2011-09-07 | 2016-06-24 | Інсайт Холдінгс Корпорейшн | Способи і проміжні сполуки для отримання інгібіторів jak |
| KR20140074964A (ko) | 2011-09-27 | 2014-06-18 | 에프. 호프만-라 로슈 아게 | 피라졸-4-일-헤테로사이클릴-카복사마이드 화합물 및 사용 방법 |
| WO2013049720A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
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-
2008
- 2008-03-03 EA EA200901144A patent/EA019951B1/ru not_active IP Right Cessation
- 2008-03-03 CA CA2679659A patent/CA2679659C/en active Active
- 2008-03-03 EP EP08731299.7A patent/EP2132177B1/en active Active
- 2008-03-03 CN CN200880011679.7A patent/CN101679266B/zh active Active
- 2008-03-03 JP JP2009551895A patent/JP5330274B2/ja active Active
- 2008-03-03 BR BRPI0808523-4A patent/BRPI0808523A2/pt not_active Application Discontinuation
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- 2008-03-03 MX MX2009009304A patent/MX2009009304A/es active IP Right Grant
- 2008-03-03 KR KR1020097020450A patent/KR101514853B1/ko active Active
- 2008-03-03 US US12/449,701 patent/US8822497B2/en active Active
- 2008-03-03 ES ES08731299T patent/ES2431163T3/es active Active
- 2008-03-03 WO PCT/US2008/055724 patent/WO2008106692A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| CA2679659A1 (en) | 2008-09-04 |
| JP5330274B2 (ja) | 2013-10-30 |
| EA019951B1 (ru) | 2014-07-30 |
| KR20100015331A (ko) | 2010-02-12 |
| CA2679659C (en) | 2016-01-19 |
| BRPI0808523A2 (pt) | 2014-08-19 |
| CN101679266B (zh) | 2015-05-06 |
| US8822497B2 (en) | 2014-09-02 |
| AU2008221263A1 (en) | 2008-09-04 |
| JP2010520228A (ja) | 2010-06-10 |
| EP2132177B1 (en) | 2013-07-17 |
| EP2132177A1 (en) | 2009-12-16 |
| WO2008106692A1 (en) | 2008-09-04 |
| WO2008106692B1 (en) | 2008-10-30 |
| AU2008221263B2 (en) | 2012-02-23 |
| CN101679266A (zh) | 2010-03-24 |
| MX2009009304A (es) | 2009-11-18 |
| US20120208815A1 (en) | 2012-08-16 |
| KR101514853B1 (ko) | 2015-04-24 |
| EA200901144A1 (ru) | 2010-04-30 |
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