Indazole compounds and pharmaceutical compositions for inhibiting protein kinases, and methods for their use
Abstract
Indazole compounds are described which modulate and / or inhibit the activity of certain protein kinases having formula III: wherein: r 'is C 6 -C 14 aryl or C 2 -C 9 heteroaryl, or a group of formula CH = CH-R 6 or CH = NR 4, wherein R 2 is C 1 -C 12 alkyl, C 3 -C 12 cycloalkyl, C 2 -C 9 heterocycloalkyl, C 6 -C 12 aryl or C 2 -C 9 heteroaryl; Y is O, S, C = CH 2, C = O, S = O, S, SO 2, CHCH 3, NH, or V 1 - (C 1 -C 8 alkyl); R * is C 1 -C 12 alkyl, C 2 -C 12 alkyl, C 3 -C 12 cycloalkyl, C 2 -C 9 heterocycloalkyl, C 6 -C 12 aryl, C 2 -C 9 heteroaryl, C 1 -C 12 alkoxyl or C 6 -C 8 aryloxyl; R 10 is independently selected from hydrogen, halogen and C 1 -C 6 alkyl; wherein each of the R 1, R 3 and R 9 groups may be optionally substituted by halogen, C 1 -C 6 alkyl, -OH, -NO 2, -CN, -CO 2 H, -O- (C 1 -C 8 alkyl), -C 6 -C 14 aryl - C 6 -C 11 aryl-C 1 -C 8 alkyl, -CO 2 CH 3, -CONH 2, -OCH 2 CONH 2, -NH 2, -SO 2 NH 2, haloalkyl or -O-haloalkyl; or a pharmaceutically acceptable salt thereof. These compounds, and their pharmaceutical materials, are capable of mediating tyrosine kinase signaling, thereby modulating and / or inhibiting unwanted cell proliferation. The invention also relates to the therapeutic and prophylactic use of pharmaceutical materials containing such compounds, to treat cancer and also to other forms of disease associated with undesirable angiogenesis and / or cellular progression, such as diabetes retinopathy, neovascular glaucoma, rheumatoid arthritis and psoriasis.

Term
No projected expiry on record.
- Priority
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- Today
1 claim: 1 independent, 0 dependent
- 1H ra Hra
24 paragraphs, as filed
(71) Seeking (72) Inventor (74) Proxy
Agouron Pharmaceuticals Inc., 10350 North Torrey Pines Road, La Jolla, CA 92037-1020, US
Michael David Johnson, 4776 Del Mar Avenue, CA92107 SAN DIEGO, US
Theodore Otto Johnson Jr., 3612 Torrey View Court, CA92130 SAN DIEGO, US
Hiep The Luu, 10330 Penrod Lane, CA92126 SAN DIEGO, US
Siegfried Heinz Reich, 311 Glenmont Drive, CA92075 SOLANA BEACH, US
Anna Maria Tempczyk-Russell, 320 Wood Meadow Lane, CA92065 RAMONA, US
Christine Thomas, 3550 Lebon Drive, CA92122 SAN DIEGO, US
Michael Brennan Wallace, 7532 Charmant Drive #311, CA92117 SAN DIEGO, US
Michael Raymond Collins, 10770 Science Center Drive, CA92121 SAN DIEGO, US
Michael D Varney, 738 Barbara Avenue, CA92075 SOLANA BEACH, US
Robert Steven Kania, 4284 Corte Favor, CA92130 SAN DIEGO, US
Allen John Borchardt, 5419 Via Carancho, CA92111 SAN DIEGO, US
John F Braganza, 3145 Cowley Way # 134, CA92117 SAN DIEGO, US
Stephen James Cripps, 11056 Pallon Way, CA92124 SAN DIEGO, US
Steven Lee Bender, 915 Reese Street, CA92054 OCEANSIDE, US
Ye Hua, 8671 via Mallorca #46, CA92037 LA JOLLA, US
Cynthia Louise Palmer, 9847 Ogram Drive, CA91941 SAN DIEGO, US
Min Teng, 5185 Seachase Street, CA92130 SAN DIEGO, US
Acapo AS, Postboks 1880 Nordnes, 5817 BERGEN, NO (54) Benevnelse Indazolforbindelser og farmasøytiske forbindelser for inhibering av proteingkinaser, og fremgangsmåter til anvendelse derav (57) Sammendrag
Det beskrives indazol-forbindelser som modulerer og/eller inhiberer aktiviteten av visse proteinkinaser, som har formel III: hvor:
R<sup>1</sup> er C6-Ci4 aryl eller C2-C9 heteroaryl, eller en gruppe med formel CH=CH-R<sup>3</sup> eller CH=N-R<sup>3</sup>, hvor R<sup>3 </sup>er C1-C12 alkyl, C3-Ci<sub>2</sub> cykloalkyl, C<sub>2</sub>-C<sub>9</sub> heterocykloalkyl, C<sub>5</sub>-C<sub>]4</sub> aryl eller C<sub>2</sub>-C<sub>9</sub> heteroaryl; Y er 0, S, C=CH<sub>2</sub>, C=0, S=0, S, S0<sub>2</sub>, CHCH<sub>3</sub>, NH eller JV-(C<sub>r</sub>Cg alkyl); R<sup>8</sup> er C<sub>r</sub>C<sub>12</sub> alkyl, C<sub>2</sub>-C<sub>12</sub> aleknyl,
C<sub>3</sub>-Ci2 cykloalkyl, C<sub>2</sub>-C<sub>9</sub> heterocykloalkyl, C<sub>6</sub>-Ci<sub>4</sub> aryl, C<sub>2</sub>-C<sub>9</sub> heteroaryl, C1-C12 alkoksyl eller C<sub>6</sub>-Ci<sub>4 </sub>aryloksyl; R<sup>10</sup> er uavhengig valgt fra hydrogen, halogen og Ci-Cg alkyl; hvor hver av de nevnte R<sub>b</sub> R<sub>3</sub> og Rs gruppene may optionally be substituted by halogen, C 1 -C 5 alkyl, -OH, -NO<sub>2</sub>, -CN, -CO<sub>2</sub>H, -O- (C 1 -C 6 alkyl), -C<sub>6</sub>-ci<sub>4</sub> aryl, - C<sub>6</sub>-ci<sub>4</sub> aryl-C 1 -C 6 alkyl, -CO<sub>2</sub>CH<sub>3</sub>, -CONH<sub>2</sub>, -OCH<sub>2</sub>CONH<sub>2</sub>, -NH<sub>2</sub>, -SO<sub>2</sub>NH<sub>2</sub>, haloalkyl or -O-haloalkyl; or a pharmaceutically acceptable salt thereof. These compounds, and pharmaceutical materials containing them, are capable of mediating tyrosine kinase signal transduction, thereby modulating and / or inhibiting unwanted cell proliferation. The invention also relates to the therapeutic and prophylactic use of pharmaceutical materials containing such compounds, to treat cancer and also other forms of disease associated with undesirable angiogenesis and / or cellular proliferation, such as diabetes retinopathy, neovascular glaucoma, rheumatoid arthritis and psoriasis.
<img file="NO20060596A_D0001.tif" />
1 sheet
Sheet 1
106 members in 54 offices
Priority claims8
| Document | Office | Kind | Date |
|---|---|---|---|
| 14213099 | United States of America | P | |
| 14213099 | United States of America | P | |
| 0018263 | United States of America | W | |
| 0018263 | United States of America | W | |
| 60142130 | – | – | – |
| PCTUS200018263 | – | – | – |
| US19990142130P | – | – | – |
| WO2000US18263 | – | – | – |
Members106
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1 legal event, as the office reported them to INPADOC
Events
| Event | Code | |
|---|---|---|
| Withdrawal, rejection or dismissal of laid open patent applicationFC2A | FC2A |
Numbers
- Publication, DOCDB
- 20060596
- Publication, EPODOC
- NO20060596L
- Application
- 596
- Application, DOCDB
- 20060596
- Application, EPODOC
- NO20060000596
Titles2
- Norwegian
- Indazolforbindelser og farmasoytiske forbindelser for inhibering av proteingkinaser, og fremgangsmater til anvendelse derav
- English
- Indazole Compounds and Pharmaceutical Compounds for Inhibition of Protein Kinases, and Methods for Use therein
Classification
- CPC, 33
- C07D403/12
- C07D209/18
- C07D231/56
- C07D401/04
- C07D401/06
- C07D401/12
- C07D401/14
- C07D403/04
- C07D405/04
- C07D405/06
- C07D405/14
- C07D409/06
- C07D409/14
- C07D413/12
- C07D417/06
- C07D417/12
- C07D417/14
- C07D471/04
- C07D491/04
- A61P17/00
- A61P17/06
- A61P19/00
- A61P19/02
- A61P27/00
- A61P27/02
- A61P27/06
- A61P29/00
- A61P3/00
- A61P35/00
- A61P43/00
- A61P9/00
- A61P9/10
- A61P3/10
- IPC, 47
- C07D231 56
- A61K31 416
- A61K31 4178
- A61K31 4184
- A61K31 4188
- A61K31 4196
- A61K31 4245
- A61K31 427
- A61K31 437
- A61K31 4439
- A61K31 444
- A61K31 454
- A61K31 4709
- A61K31 496
- A61K31 5377
- A61P3 10
- A61P9 10
- A61P17 06
- A61P19 02
- A61P27 02
- A61P27 06
- A61P29 00
- A61P35 00
- A61P43 00
- C07D209 18
- C07D231 00
- C07D401 04
- C07D401 06
- C07D401 12
- C07D401 14
- C07D403 04
- C07D403 12
- C07D403 14
- C07D405 04
- C07D405 06
- C07D405 14
- C07D409 06
- C07D409 12
- C07D409 14
- C07D413 12
- C07D413 14
- C07D417 06
- C07D417 12
- C07D417 14
- C07D471 04
- C07D491 04
- C07D491 056