JP2010523681A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010523681A5 JP2010523681A5 JP2010503085A JP2010503085A JP2010523681A5 JP 2010523681 A5 JP2010523681 A5 JP 2010523681A5 JP 2010503085 A JP2010503085 A JP 2010503085A JP 2010503085 A JP2010503085 A JP 2010503085A JP 2010523681 A5 JP2010523681 A5 JP 2010523681A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally
- methyl
- amino
- pyrido
- solvate
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 53
- 239000012453 solvate Substances 0.000 claims 45
- 150000003839 salts Chemical class 0.000 claims 31
- -1 cyano, amino Chemical group 0.000 claims 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 14
- WDHAAJIGSXNPFO-UHFFFAOYSA-N 8h-pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=CN=C2NC(=O)C=CC2=C1 WDHAAJIGSXNPFO-UHFFFAOYSA-N 0.000 claims 10
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 238000000034 method Methods 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 3
- 239000003085 diluting agent Substances 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 150000004677 hydrates Chemical class 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 125000006582 (C5-C6) heterocycloalkyl group Chemical group 0.000 claims 2
- ZGXPZZAXEDLDDX-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxan-3-yl)-6-(1,3-thiazol-2-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=CN=2)=CC=2C(C)=NC(N)=NC=2N1C1CCCOC1 ZGXPZZAXEDLDDX-UHFFFAOYSA-N 0.000 claims 2
- MILYRWPLUFALKR-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxan-3-yl)-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCCOC1 MILYRWPLUFALKR-UHFFFAOYSA-N 0.000 claims 2
- BLVOBRJOMRUEJA-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxan-3-yl)-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NN=CC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCCOC1 BLVOBRJOMRUEJA-UHFFFAOYSA-N 0.000 claims 2
- IHAQGJYSPJORGO-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxan-4-yl)-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOCC1 IHAQGJYSPJORGO-UHFFFAOYSA-N 0.000 claims 2
- NANHQKIPLBJMMG-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxan-4-yl)-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NN=CC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOCC1 NANHQKIPLBJMMG-UHFFFAOYSA-N 0.000 claims 2
- GXOWENLHPKJXCA-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxolan-3-yl)-6-(1,3-thiazol-2-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=CN=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOC1 GXOWENLHPKJXCA-UHFFFAOYSA-N 0.000 claims 2
- OCSCOUYGARUHSP-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxolan-3-yl)-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOC1 OCSCOUYGARUHSP-UHFFFAOYSA-N 0.000 claims 2
- JPKHSROONPXDEJ-SECBINFHSA-N 2-amino-4-methyl-8-[(3r)-oxolan-3-yl]-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NN=CC=2)=CC=2C(C)=NC(N)=NC=2N1[C@@H]1CCOC1 JPKHSROONPXDEJ-SECBINFHSA-N 0.000 claims 2
- JPKHSROONPXDEJ-VIFPVBQESA-N 2-amino-4-methyl-8-[(3s)-oxolan-3-yl]-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NN=CC=2)=CC=2C(C)=NC(N)=NC=2N1[C@H]1CCOC1 JPKHSROONPXDEJ-VIFPVBQESA-N 0.000 claims 2
- UISGLFKPJGARAG-GFCCVEGCSA-N 2-amino-6-[1-(ethoxymethyl)imidazol-2-yl]-4-methyl-8-[(3r)-oxolan-3-yl]pyrido[2,3-d]pyrimidin-7-one Chemical compound CCOCN1C=CN=C1C(C1=O)=CC2=C(C)N=C(N)N=C2N1[C@H]1COCC1 UISGLFKPJGARAG-GFCCVEGCSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000003282 alkyl amino group Chemical group 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 201000010881 cervical cancer Diseases 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 125000004663 dialkyl amino group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 208000005017 glioblastoma Diseases 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000005843 halogen group Chemical group 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 238000001794 hormone therapy Methods 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 238000009169 immunotherapy Methods 0.000 claims 2
- XMBWDFGMSWQBCA-RNFDNDRNSA-M iodine-131(1-) Chemical compound [131I-] XMBWDFGMSWQBCA-RNFDNDRNSA-M 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 230000005855 radiation Effects 0.000 claims 2
- 206010038038 rectal cancer Diseases 0.000 claims 2
- 201000001275 rectum cancer Diseases 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 238000011282 treatment Methods 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- GNXNJMVSAGUGPI-UHFFFAOYSA-N 2-(oxolan-3-yl)-8h-pyrido[2,3-d]pyrimidin-7-one Chemical compound N1=C2NC(=O)C=CC2=CN=C1C1CCOC1 GNXNJMVSAGUGPI-UHFFFAOYSA-N 0.000 claims 1
- JXYNHGDZJFQCAX-UHFFFAOYSA-N 2-amino-1h-pyrido[2,3-d]pyrimidin-4-one Chemical compound C1=CN=C2NC(N)=NC(=O)C2=C1 JXYNHGDZJFQCAX-UHFFFAOYSA-N 0.000 claims 1
- QWSSVQNJBJCOHH-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxan-4-yl)-6-(1,3-thiazol-2-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=CN=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOCC1 QWSSVQNJBJCOHH-UHFFFAOYSA-N 0.000 claims 1
- JPKHSROONPXDEJ-UHFFFAOYSA-N 2-amino-4-methyl-8-(oxolan-3-yl)-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NN=CC=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOC1 JPKHSROONPXDEJ-UHFFFAOYSA-N 0.000 claims 1
- MILYRWPLUFALKR-SNVBAGLBSA-N 2-amino-4-methyl-8-[(3r)-oxan-3-yl]-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1[C@@H]1CCCOC1 MILYRWPLUFALKR-SNVBAGLBSA-N 0.000 claims 1
- GXOWENLHPKJXCA-SECBINFHSA-N 2-amino-4-methyl-8-[(3r)-oxolan-3-yl]-6-(1,3-thiazol-2-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=CN=2)=CC=2C(C)=NC(N)=NC=2N1[C@@H]1CCOC1 GXOWENLHPKJXCA-SECBINFHSA-N 0.000 claims 1
- OCSCOUYGARUHSP-SECBINFHSA-N 2-amino-4-methyl-8-[(3r)-oxolan-3-yl]-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1[C@@H]1CCOC1 OCSCOUYGARUHSP-SECBINFHSA-N 0.000 claims 1
- MILYRWPLUFALKR-JTQLQIEISA-N 2-amino-4-methyl-8-[(3s)-oxan-3-yl]-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1[C@H]1CCCOC1 MILYRWPLUFALKR-JTQLQIEISA-N 0.000 claims 1
- BLVOBRJOMRUEJA-JTQLQIEISA-N 2-amino-4-methyl-8-[(3s)-oxan-3-yl]-6-(1h-pyrazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NN=CC=2)=CC=2C(C)=NC(N)=NC=2N1[C@H]1CCCOC1 BLVOBRJOMRUEJA-JTQLQIEISA-N 0.000 claims 1
- GXOWENLHPKJXCA-VIFPVBQESA-N 2-amino-4-methyl-8-[(3s)-oxolan-3-yl]-6-(1,3-thiazol-2-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=CN=2)=CC=2C(C)=NC(N)=NC=2N1[C@H]1CCOC1 GXOWENLHPKJXCA-VIFPVBQESA-N 0.000 claims 1
- OCSCOUYGARUHSP-VIFPVBQESA-N 2-amino-4-methyl-8-[(3s)-oxolan-3-yl]-6-(1,3-thiazol-5-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2SC=NC=2)=CC=2C(C)=NC(N)=NC=2N1[C@H]1CCOC1 OCSCOUYGARUHSP-VIFPVBQESA-N 0.000 claims 1
- NVNMVAGLZHFJQW-UHFFFAOYSA-N 2-amino-6-(1h-imidazol-2-yl)-4-methyl-8-(oxan-3-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NC=CN=2)=CC=2C(C)=NC(N)=NC=2N1C1CCCOC1 NVNMVAGLZHFJQW-UHFFFAOYSA-N 0.000 claims 1
- MOLBXGGAGOSDHD-UHFFFAOYSA-N 2-amino-6-(1h-imidazol-2-yl)-4-methyl-8-(oxan-4-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NC=CN=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOCC1 MOLBXGGAGOSDHD-UHFFFAOYSA-N 0.000 claims 1
- MFMFHJBNGPUUTB-UHFFFAOYSA-N 2-amino-6-(1h-imidazol-2-yl)-4-methyl-8-(oxolan-3-yl)pyrido[2,3-d]pyrimidin-7-one Chemical compound O=C1C(C=2NC=CN=2)=CC=2C(C)=NC(N)=NC=2N1C1CCOC1 MFMFHJBNGPUUTB-UHFFFAOYSA-N 0.000 claims 1
- UISGLFKPJGARAG-LBPRGKRZSA-N 2-amino-6-[1-(ethoxymethyl)imidazol-2-yl]-4-methyl-8-[(3s)-oxolan-3-yl]pyrido[2,3-d]pyrimidin-7-one Chemical compound CCOCN1C=CN=C1C(C1=O)=CC2=C(C)N=C(N)N=C2N1[C@@H]1COCC1 UISGLFKPJGARAG-LBPRGKRZSA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010041067 Small cell lung cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 125000004181 carboxyalkyl group Chemical group 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 229940044683 chemotherapy drug Drugs 0.000 claims 1
- 229940127089 cytotoxic agent Drugs 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 150000002431 hydrogen Chemical class 0.000 claims 1
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- UDJFFSGCRRMVFH-UHFFFAOYSA-N pyrido[2,3-d]pyrimidine Chemical compound N1=CN=CC2=CC=CN=C21 UDJFFSGCRRMVFH-UHFFFAOYSA-N 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
- 0 *C(C(N1[C@]2COCC2)=O)=Cc2c1nc(*)nc2* Chemical compound *C(C(N1[C@]2COCC2)=O)=Cc2c1nc(*)nc2* 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US91116007P | 2007-04-11 | 2007-04-11 | |
| PCT/US2008/004807 WO2008127712A1 (en) | 2007-04-11 | 2008-04-11 | Pyrido [2, 3-d] pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010523681A JP2010523681A (ja) | 2010-07-15 |
| JP2010523681A5 true JP2010523681A5 (enExample) | 2011-05-12 |
Family
ID=39642739
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010503085A Pending JP2010523681A (ja) | 2007-04-11 | 2008-04-11 | 癌の治療のためのＰＩ３Ｋ−αの阻害剤としてのピリド［２，３−Ｄ］ピリミジン−７−オン化合物 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US20100209340A1 (enExample) |
| EP (1) | EP2142544B8 (enExample) |
| JP (1) | JP2010523681A (enExample) |
| KR (1) | KR20090130104A (enExample) |
| CN (1) | CN101711249A (enExample) |
| AU (1) | AU2008239596B2 (enExample) |
| BR (1) | BRPI0810175A2 (enExample) |
| CA (1) | CA2683820A1 (enExample) |
| CO (1) | CO6241119A2 (enExample) |
| CR (1) | CR11098A (enExample) |
| DO (1) | DOP2009000242A (enExample) |
| EA (1) | EA018964B1 (enExample) |
| EC (1) | ECSP099722A (enExample) |
| ES (1) | ES2425068T3 (enExample) |
| IL (1) | IL201209A0 (enExample) |
| MA (1) | MA31336B1 (enExample) |
| MX (1) | MX2009010815A (enExample) |
| MY (1) | MY150747A (enExample) |
| NI (1) | NI200900183A (enExample) |
| NZ (1) | NZ579945A (enExample) |
| SV (1) | SV2009003389A (enExample) |
| TN (1) | TN2009000389A1 (enExample) |
| UA (1) | UA101315C2 (enExample) |
| WO (1) | WO2008127712A1 (enExample) |
| ZA (1) | ZA200906648B (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1828186A1 (en) * | 2004-12-13 | 2007-09-05 | Sunesis Pharmaceuticals, Inc. | Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as raf kinase inhibitors |
| HRP20130902T1 (hr) * | 2005-10-07 | 2013-11-08 | Exelixis Inc. | PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa |
| AU2006302179C1 (en) * | 2005-10-07 | 2013-06-20 | Exelixis, Inc. | N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors |
| CA2658725A1 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| AU2007297212B8 (en) * | 2006-09-15 | 2011-04-28 | Pfizer Products Inc. | Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors |
| EA020022B1 (ru) | 2007-04-10 | 2014-08-29 | Экселиксис, Инк. | Способы лечения с применением пиридопиримидиноновых ингибиторов pi3k-альфа |
| CA2683784A1 (en) * | 2007-04-11 | 2008-10-23 | Exelixis, Inc. | Pyrido[2,3-d]pyrimidin-7-one compounds as inhibitors of pi3k-alpha for the treatment of cancer |
| JP2012504628A (ja) * | 2008-09-30 | 2012-02-23 | エグゼリクシス， インコーポレイテッド | ＰＩ３ＫαおよびｍＴＯＲのピリドピリミジノン阻害剤 |
| EP3309152B1 (en) * | 2009-12-22 | 2020-09-09 | Vertex Pharmaceuticals Incorporated | Isoindolinone inhibitors of phosphatidylinositol 3-kinase |
| UY33221A (es) | 2010-02-09 | 2011-09-30 | Univ California | MÉTODOS PARA TRATAR CÁNCER USANDO INHIBIDORES DE PI3K Y mTOR EN COMBINACIÓN CON INHIBIDORES DE AUTOFAGIA |
| WO2012037204A1 (en) | 2010-09-14 | 2012-03-22 | Exelixis, Inc. | Inhibitors of pi3k-delta and methods of their use and manufacture |
| WO2013056067A1 (en) * | 2011-10-13 | 2013-04-18 | Exelixis, Inc. | Compounds for use in the treatment of basal cell carcinoma |
| PH12014500973A1 (en) | 2011-11-01 | 2014-06-16 | Exelixis Inc | Phosphatidylinositol 3-kinase inhibitors for the treatment of lymphoproliferative malignancies |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2937284A (en) * | 1958-05-01 | 1960-05-17 | Burroughs Wellcome Co | 2, 4-diamino-5, 6-dialkylpyrido (2, 3-d) pyrimidines and method |
| IL117923A (en) * | 1995-05-03 | 2000-06-01 | Warner Lambert Co | Anti-cancer pharmaceutical compositions containing polysubstituted pyrido¬2,3-d¾pyrimidine derivatives and certain such novel compounds |
| US7019002B2 (en) * | 2001-12-11 | 2006-03-28 | Pharmacia & Upjohn, S.P.A. | Pyridopyrimidinones derivatives as telomerase inhibitors |
| DE602005002562T2 (de) * | 2004-05-04 | 2008-01-31 | Warner-Lambert Company Llc | Pyrrolylsubstituierte pyridoä2,3-düpyrimidin-7-one und derivate davon als therapeutische mittel |
| HRP20130902T1 (hr) * | 2005-10-07 | 2013-11-08 | Exelixis Inc. | PIRIDOPIRIMIDINONSKI INHIBITORI PI3Kalfa |
| WO2007044698A1 (en) * | 2005-10-07 | 2007-04-19 | Exelixis, Inc. | PYRIDOPYRIMIDINONE INHIBITORS OF PI3Kα |
| CA2658725A1 (en) * | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| AU2007297212B8 (en) * | 2006-09-15 | 2011-04-28 | Pfizer Products Inc. | Pyrido (2, 3-d) pyrimidinone compounds and their use as pi3 inhibitors |
-
2008
- 2008-04-11 WO PCT/US2008/004807 patent/WO2008127712A1/en not_active Ceased
- 2008-04-11 ES ES08742864T patent/ES2425068T3/es active Active
- 2008-04-11 KR KR1020097023146A patent/KR20090130104A/ko not_active Ceased
- 2008-04-11 CN CN200880018758A patent/CN101711249A/zh active Pending
- 2008-04-11 EP EP08742864.5A patent/EP2142544B8/en active Active
- 2008-04-11 NZ NZ579945A patent/NZ579945A/en not_active IP Right Cessation
- 2008-04-11 MY MYPI20094194 patent/MY150747A/en unknown
- 2008-04-11 EA EA200970936A patent/EA018964B1/ru not_active IP Right Cessation
- 2008-04-11 MX MX2009010815A patent/MX2009010815A/es active IP Right Grant
- 2008-04-11 BR BRPI0810175-2A2A patent/BRPI0810175A2/pt not_active IP Right Cessation
- 2008-04-11 AU AU2008239596A patent/AU2008239596B2/en not_active Ceased
- 2008-04-11 JP JP2010503085A patent/JP2010523681A/ja active Pending
- 2008-04-11 US US12/595,233 patent/US20100209340A1/en not_active Abandoned
- 2008-04-11 CA CA002683820A patent/CA2683820A1/en not_active Abandoned
- 2008-04-11 UA UAA200911451A patent/UA101315C2/ru unknown
-
2009
- 2009-09-23 ZA ZA200906648A patent/ZA200906648B/xx unknown
- 2009-09-24 TN TNP2009000389A patent/TN2009000389A1/fr unknown
- 2009-09-29 IL IL201209A patent/IL201209A0/en unknown
- 2009-10-09 NI NI200900183A patent/NI200900183A/es unknown
- 2009-10-09 DO DO2009000242A patent/DOP2009000242A/es unknown
- 2009-10-09 SV SV2009003389A patent/SV2009003389A/es not_active Application Discontinuation
- 2009-10-30 MA MA32314A patent/MA31336B1/fr unknown
- 2009-11-09 CO CO09126919A patent/CO6241119A2/es not_active Application Discontinuation
- 2009-11-09 CR CR11098A patent/CR11098A/es unknown
- 2009-11-09 EC EC2009009722A patent/ECSP099722A/es unknown
-
2013
- 2013-01-03 US US13/694,772 patent/US20130343988A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2019290197B2 (en) | Protein tyrosine phosphatase inhibitors and methods of use thereof | |
| JP7034084B2 (ja) | Ｔａｍ阻害剤としてのピロロトリアジン化合物 | |
| AU2017260374B2 (en) | Modulators of the integrated stress pathway | |
| US10913727B2 (en) | Modulators of the integrated stress pathway | |
| US11046699B2 (en) | Pyrazolo-pyrimidin-amino-cycloalkyl compounds and their therapeutic uses | |
| JP5620417B2 (ja) | アミノピラゾール誘導体を含む医薬 | |
| WO2022228543A1 (zh) | 桥环类化合物、其制备方法及其在医药上的应用 | |
| WO2020010197A1 (en) | Fused pyrazine derivatives as a2a / a2b inhibitors | |
| IL274369B1 (en) | Modulators of the integrated stress pathway | |
| TW201825486A (zh) | 梅嫩蛋白（ｍｅｎｉｎ）-ＭＬＬ相互作用之抑制劑 | |
| US10722514B2 (en) | Ubiquitin-specific-processing protease 7 (USP7) modulators and uses thereof | |
| RU2612251C2 (ru) | Соединения диоксин- и оксазин[2,3-d]пиримидина в качестве ингибиторов фосфоинозитид-3-киназы и способы их применения | |
| AU2013286894A1 (en) | Heterocyclic modulators of lipid synthesis | |
| JP2015003909A (ja) | ベンゾピラン化合物の組合せ、その組成物および使用 | |
| US11040981B2 (en) | Pyrrolotriazine compounds and methods of inhibiting TAM kinases | |
| WO2020068600A1 (en) | Ubiquitin-specific-processing protease 7 (usp7) modulators and uses thereof | |
| WO2018191587A1 (en) | Tam kinase inhibitors | |
| JP2010523681A (ja) | 癌の治療のためのＰＩ３Ｋ−αの阻害剤としてのピリド［２，３−Ｄ］ピリミジン−７−オン化合物 | |
| TW202400579A (zh) | 含氮雜環類衍生物抑制劑、其製備方法和應用 | |
| EP3022207A2 (en) | Compounds and methods for treating cancer, neurological disorders, ethanol withdrawal, anxiety, depression, and neuropathic pain | |
| JP2017507988A (ja) | オキセパン−２−イル−ピラゾール−４−イル−ヘテロシクリル−カルボキサミド化合物と使用方法 | |
| US20260137674A1 (en) | Combination therapy using a kras g12d inhibitor, and a nucleoside analog, and/or a microtubule inhibitor | |
| WO2026090323A1 (en) | Combination therapy using a kras g12d inhibitor, and a nucleoside analog, and/or a microtubule inhibitor and its use in the treatment of cancer | |
| HK1185871B (en) | Tricyclic pi3k inhibitor compounds and methods of use | |
| HK1205512A1 (en) | Amino-substituted imidazopyridazines |