JP2010513523A5 - - Google Patents
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- Publication number
- JP2010513523A5 JP2010513523A5 JP2009542923A JP2009542923A JP2010513523A5 JP 2010513523 A5 JP2010513523 A5 JP 2010513523A5 JP 2009542923 A JP2009542923 A JP 2009542923A JP 2009542923 A JP2009542923 A JP 2009542923A JP 2010513523 A5 JP2010513523 A5 JP 2010513523A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- nhc
- independently
- cycloalkyl
- alkyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 20
- 125000000753 cycloalkyl group Chemical group 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 10
- -1 diastereomers Chemical class 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims 8
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 6
- 125000001475 halogen functional group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 125000000304 alkynyl group Chemical group 0.000 claims 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000003937 drug carrier Substances 0.000 claims 3
- 239000001257 hydrogen Substances 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 150000002431 hydrogen Chemical class 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- FLBAYUMRQUHISI-UHFFFAOYSA-N 1,8-naphthyridine Chemical compound N1=CC=CC2=CC=CN=C21 FLBAYUMRQUHISI-UHFFFAOYSA-N 0.000 claims 1
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 1
- PCDPMVJGEGAJBI-UHFFFAOYSA-N 6,7-dimethoxyquinoline Chemical compound C1=CN=C2C=C(OC)C(OC)=CC2=C1 PCDPMVJGEGAJBI-UHFFFAOYSA-N 0.000 claims 1
- JJTNLWSCFYERCK-UHFFFAOYSA-N 7h-pyrrolo[2,3-d]pyrimidine Chemical compound N1=CN=C2NC=CC2=C1 JJTNLWSCFYERCK-UHFFFAOYSA-N 0.000 claims 1
- 125000004411 C5-C6 heterocyclyl group Chemical group 0.000 claims 1
- 101100516568 Caenorhabditis elegans nhr-7 gene Proteins 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 102000014150 Interferons Human genes 0.000 claims 1
- 108010050904 Interferons Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 125000004450 alkenylene group Chemical group 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 229940100198 alkylating agent Drugs 0.000 claims 1
- 239000002168 alkylating agent Substances 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000000340 anti-metabolite Effects 0.000 claims 1
- 229940100197 antimetabolite Drugs 0.000 claims 1
- 239000002256 antimetabolite Substances 0.000 claims 1
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 230000017531 blood circulation Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 229940125697 hormonal agent Drugs 0.000 claims 1
- 229940124452 immunizing agent Drugs 0.000 claims 1
- LPAGFVYQRIESJQ-UHFFFAOYSA-N indoline Chemical compound C1=CC=C2NCCC2=C1 LPAGFVYQRIESJQ-UHFFFAOYSA-N 0.000 claims 1
- 229940079322 interferon Drugs 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 230000035755 proliferation Effects 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical compound N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 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 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US87628306P | 2006-12-20 | 2006-12-20 | |
| US60/876,283 | 2006-12-20 | ||
| PCT/US2007/026064 WO2008079292A1 (en) | 2006-12-20 | 2007-12-19 | Heterocyclic compounds and their use in treating inflammation, angiogenesis and cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010513523A JP2010513523A (ja) | 2010-04-30 |
| JP2010513523A5 true JP2010513523A5 (enExample) | 2011-01-20 |
| JP5528812B2 JP5528812B2 (ja) | 2014-06-25 |
Family
ID=39281186
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009542923A Expired - Fee Related JP5528812B2 (ja) | 2006-12-20 | 2007-12-19 | 複素環式化合物ならびに炎症、血管形成および癌の治療におけるこれらの使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US8338455B2 (enExample) |
| EP (1) | EP2118088B1 (enExample) |
| JP (1) | JP5528812B2 (enExample) |
| AU (1) | AU2007338793B2 (enExample) |
| CA (1) | CA2672903C (enExample) |
| ES (1) | ES2387471T3 (enExample) |
| MX (1) | MX2009006543A (enExample) |
| WO (1) | WO2008079292A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI1966202T1 (sl) | 2005-12-13 | 2012-01-31 | Incyte Corp | S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze |
| EP4606378A3 (en) | 2007-06-13 | 2025-11-05 | Incyte Holdings Corporation | Salts of the janus kinase inhibitor (r)-3-( 4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3- cyclopentylprop anenitrile |
| JP5444239B2 (ja) | 2007-11-02 | 2014-03-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | タンパク質キナーゼＣ−θとしての［１Ｈ−ピラゾロ［３，４−Ｂ］ピリジン−４−イル］−フェニレンまたは−ピリジン−２−イル誘導体 |
| CL2009001884A1 (es) * | 2008-10-02 | 2010-05-14 | Incyte Holdings Corp | Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco. |
| WO2010080503A1 (en) * | 2008-12-19 | 2010-07-15 | Genentech, Inc. | Heterocyclic compounds and methods of use |
| UA106078C2 (uk) | 2009-05-22 | 2014-07-25 | Інсайт Корпорейшн | 3-[4-(7H-ПІРОЛО[2,3-d]ПІРИМІДИН-4-ІЛ)-1H-ПІРАЗОЛ-1-ІЛ]ОКТАН- АБО ГЕПТАННІТРИЛ ЯК JAK-ІНГІБІТОРИ |
| AU2010249380B2 (en) | 2009-05-22 | 2015-08-20 | Incyte Holdings Corporation | N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as Janus kinase inhibitors |
| JP2011057661A (ja) * | 2009-08-14 | 2011-03-24 | Bayer Cropscience Ag | 殺虫性カルボキサミド類 |
| TW201113285A (en) | 2009-09-01 | 2011-04-16 | Incyte Corp | Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors |
| SI2545045T1 (sl) | 2010-03-10 | 2016-05-31 | Incyte Holdings Corporation | Derivati piperidin-4-ila kot zaviralci JAK1 |
| MX338228B (es) | 2010-05-21 | 2016-04-08 | Incyte Corp | Formulacion topica para inhibidor de cinasas janus (jak). |
| US9034884B2 (en) | 2010-11-19 | 2015-05-19 | Incyte Corporation | Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors |
| US8933085B2 (en) | 2010-11-19 | 2015-01-13 | Incyte Corporation | Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| EP2721006A1 (en) | 2011-06-20 | 2014-04-23 | E. I. Du Pont de Nemours and Company | Heterocyclic compounds for treating helminth infections |
| WO2012177606A1 (en) | 2011-06-20 | 2012-12-27 | Incyte Corporation | Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors |
| 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 |
| TW201326128A (zh) | 2011-11-28 | 2013-07-01 | Du Pont | 磺醯胺驅蟲劑 |
| US9193733B2 (en) | 2012-05-18 | 2015-11-24 | Incyte Holdings Corporation | Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors |
| WO2014071031A1 (en) | 2012-11-01 | 2014-05-08 | Incyte Corporation | Tricyclic fused thiophene derivatives as jak inhibitors |
| IL297429A (en) | 2012-11-15 | 2022-12-01 | Incyte Holdings Corp | Sustained release dosage forms of roxolitinib |
| WO2014099837A1 (en) | 2012-12-18 | 2014-06-26 | E. I. Du Pont De Nemours And Company | Sulfonamide anthelmintics |
| PT3489239T (pt) | 2013-03-06 | 2021-12-17 | Incyte Holdings Corp | Processos e intermediários para a preparação de um inibidor de jak |
| CN114010611B (zh) | 2013-08-07 | 2023-11-28 | 因赛特控股公司 | Jak1抑制剂的持续释放剂型 |
| JP2017514832A (ja) | 2014-04-30 | 2017-06-08 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | Ｊａｋ１抑制剤を調製する方法及びその新しい形態 |
| WO2015184305A1 (en) | 2014-05-30 | 2015-12-03 | Incyte Corporation | TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1 |
| US10596161B2 (en) | 2017-12-08 | 2020-03-24 | Incyte Corporation | Low dose combination therapy for treatment of myeloproliferative neoplasms |
| UA127488C2 (uk) | 2018-01-30 | 2023-09-06 | Інсайт Корпорейшн | Способи одержання (1-(3-фтор-2-(трифторметил)ізонікотиноїл)піперидин-4-ону) |
| PT3773593T (pt) | 2018-03-30 | 2024-06-25 | Incyte Corp | Tratamento da hidradenite supurativa com inibidores de jak |
| CN115397412B (zh) * | 2020-04-17 | 2025-03-25 | 伊赛恩特制药公司 | Mas相关g蛋白受体x4的调节剂及相关产物和方法 |
| CN115996721A (zh) * | 2020-05-08 | 2023-04-21 | 乔治穆内有限责任公司 | Akt3调节剂 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IE903196A1 (en) * | 1989-09-05 | 1991-03-13 | Searle & Co | Substituted n-benzylpiperidine amides |
| EP0860433B1 (en) | 1995-11-07 | 2002-07-03 | Kirin Beer Kabushiki Kaisha | Quinoline derivatives and quinazoline derivatives inhibiting autophosphorylation of growth factor receptor originating in platelet and pharmaceutical compositions containing the same |
| GB9815880D0 (en) * | 1998-07-21 | 1998-09-16 | Pfizer Ltd | Heterocycles |
| EE05708B1 (et) | 1999-02-10 | 2014-04-15 | Astrazeneca Ab | Kinasoliini derivaat angiogeneesi inhibiitorina ja selle kasutamine |
| EE200200123A (et) | 1999-09-10 | 2003-08-15 | Merck & Co., Inc. | Türosiinkinaasi pärssiv ühend, seda sisaldav farmatseutiline kompositsioon ning raviotstarbeline kasutamine |
| CN1308310C (zh) | 2000-10-20 | 2007-04-04 | 卫材R&D管理有限公司 | 含氮芳环衍生物 |
| FR2816940A1 (fr) * | 2000-11-23 | 2002-05-24 | Lipha | Derives de 4-(biphenylcarbonylamino)-piperidine, compositions les contenant et leur utilisation |
| KR100883731B1 (ko) | 2001-06-22 | 2009-02-12 | 기린 파마 가부시끼가이샤 | 간세포 증식 인자 수용체 자기 인산화를 저해하는 퀴놀린유도체 및 퀴나졸린 유도체 및 이들을 함유하는 의약 조성물 |
| WO2005073224A2 (en) | 2004-01-23 | 2005-08-11 | Amgen Inc | Quinoline quinazoline pyridine and pyrimidine counds and their use in the treatment of inflammation angiogenesis and cancer |
| WO2005070891A2 (en) | 2004-01-23 | 2005-08-04 | Amgen Inc | Compounds and methods of use |
| JO2787B1 (en) | 2005-04-27 | 2014-03-15 | امجين إنك, | Alternative amide derivatives and methods of use |
-
2007
- 2007-12-19 AU AU2007338793A patent/AU2007338793B2/en not_active Ceased
- 2007-12-19 ES ES07863179T patent/ES2387471T3/es active Active
- 2007-12-19 JP JP2009542923A patent/JP5528812B2/ja not_active Expired - Fee Related
- 2007-12-19 WO PCT/US2007/026064 patent/WO2008079292A1/en not_active Ceased
- 2007-12-19 MX MX2009006543A patent/MX2009006543A/es active IP Right Grant
- 2007-12-19 EP EP07863179A patent/EP2118088B1/en active Active
- 2007-12-19 US US12/004,156 patent/US8338455B2/en not_active Expired - Fee Related
- 2007-12-19 CA CA2672903A patent/CA2672903C/en not_active Expired - Fee Related