JP2016537389A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016537389A5 JP2016537389A5 JP2016533532A JP2016533532A JP2016537389A5 JP 2016537389 A5 JP2016537389 A5 JP 2016537389A5 JP 2016533532 A JP2016533532 A JP 2016533532A JP 2016533532 A JP2016533532 A JP 2016533532A JP 2016537389 A5 JP2016537389 A5 JP 2016537389A5
- Authority
- JP
- Japan
- Prior art keywords
- thio
- indol
- pyrazol
- fluoro
- cyclopropyl
- 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
- 150000003839 salts Chemical class 0.000 claims 18
- 239000012453 solvate Substances 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 17
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000002733 (C1-C6) fluoroalkyl group Chemical group 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- -1 L 1 is absent Chemical group 0.000 claims 3
- 229910052794 bromium Inorganic materials 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 125000005345 deuteroalkyl group Chemical group 0.000 claims 3
- 229910052740 iodine Inorganic materials 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 2
- 125000003709 fluoroalkyl group Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 1
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 1
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 1
- SCVJRXQHFJXZFZ-KVQBGUIXSA-N 2-amino-9-[(2r,4s,5r)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-3h-purine-6-thione Chemical compound C1=2NC(N)=NC(=S)C=2N=CN1[C@H]1C[C@H](O)[C@@H](CO)O1 SCVJRXQHFJXZFZ-KVQBGUIXSA-N 0.000 claims 1
- SOVLUELSMIRMNB-UHFFFAOYSA-N 3-(2,6-dichloro-7-fluoro-1-pyridin-3-ylindol-3-yl)sulfanyl-2-fluorobenzoic acid Chemical compound ClC=1N(C2=C(C(=CC=C2C1SC=1C(=C(C(=O)O)C=CC1)F)Cl)F)C=1C=NC=CC1 SOVLUELSMIRMNB-UHFFFAOYSA-N 0.000 claims 1
- WSYHMZGUKCDJFT-UHFFFAOYSA-N 3-(2-bromo-6-chloro-7-fluoro-1-pyridin-3-ylindol-3-yl)sulfanyl-2-fluorobenzoic acid Chemical compound BrC=1N(C2=C(C(=CC=C2C1SC=1C(=C(C(=O)O)C=CC1)F)Cl)F)C=1C=NC=CC1 WSYHMZGUKCDJFT-UHFFFAOYSA-N 0.000 claims 1
- KKJFSHJWWLQTLF-UHFFFAOYSA-N 3-(6-chloro-2-cyclopropyl-7-fluoro-1-pyridin-3-ylindol-3-yl)sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NC=CC=1)C1CC1)SC=1C(=C(C(=O)O)C=CC=1)F KKJFSHJWWLQTLF-UHFFFAOYSA-N 0.000 claims 1
- KTYKEXDWYCABHF-UHFFFAOYSA-N 3-[1-[1-(2-aminoethyl)pyrazol-4-yl]-6-chloro-2-cyclopropyl-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound NCCN1N=CC(=C1)N1C(=C(C2=CC=C(C(=C12)F)Cl)SC=1C(=C(C(=O)O)C=CC1)F)C1CC1 KTYKEXDWYCABHF-UHFFFAOYSA-N 0.000 claims 1
- DQTBLWSPQCAUDQ-UHFFFAOYSA-N 3-[1-[1-(2-carbamoyloxyethyl)pyrazol-4-yl]-6-chloro-2-cyclopropyl-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound C(N)(=O)OCCN1N=CC(=C1)N1C(=C(C2=CC=C(C(=C12)F)Cl)SC=1C(=C(C(=O)O)C=CC1)F)C1CC1 DQTBLWSPQCAUDQ-UHFFFAOYSA-N 0.000 claims 1
- NLLDWNTWQXLYJQ-UHFFFAOYSA-N 3-[1-[1-(3-carboxypropyl)pyrazol-4-yl]-6-chloro-2-cyclopropyl-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound C(=O)(O)CCCN1N=CC(=C1)N1C(=C(C2=CC=C(C(=C12)F)Cl)SC=1C(=C(C(=O)O)C=CC1)F)C1CC1 NLLDWNTWQXLYJQ-UHFFFAOYSA-N 0.000 claims 1
- GQVSMWUXZKOCGP-UHFFFAOYSA-N 3-[1-[1-(4-amino-4-oxobutyl)pyrazol-4-yl]-6-chloro-2-cyclopropyl-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound NC(CCCN1N=CC(=C1)N1C(=C(C2=CC=C(C(=C12)F)Cl)SC=1C(=C(C(=O)O)C=CC1)F)C1CC1)=O GQVSMWUXZKOCGP-UHFFFAOYSA-N 0.000 claims 1
- HHKSNXCCWSWZRQ-UHFFFAOYSA-N 3-[1-[1-[2-(carbamoylamino)ethyl]pyrazol-4-yl]-6-chloro-2-cyclopropyl-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CCNC(=O)N)C1CC1)SC=1C(=C(C(=O)O)C=CC1)F HHKSNXCCWSWZRQ-UHFFFAOYSA-N 0.000 claims 1
- JVJBBGAETSKIOQ-UHFFFAOYSA-N 3-[2,6-dichloro-1-(1-ethylpyrazol-4-yl)-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC=1N(C2=C(C(=CC=C2C1SC=1C(=C(C(=O)O)C=CC1)F)Cl)F)C=1C=NN(C1)CC JVJBBGAETSKIOQ-UHFFFAOYSA-N 0.000 claims 1
- XKZONGFBKCVJIJ-UHFFFAOYSA-N 3-[2,6-dichloro-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound C1=NN(CCC)C=C1N1C2=CC(Cl)=CC=C2C(SC=2C=C(C=CC=2)C(O)=O)=C1Cl XKZONGFBKCVJIJ-UHFFFAOYSA-N 0.000 claims 1
- KMKNLPHJEJMJOM-UHFFFAOYSA-N 3-[2,6-dichloro-7-fluoro-1-(1-methylpyrazol-4-yl)indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC=1N(C2=C(C(=CC=C2C1SC=1C(=C(C(=O)O)C=CC1)F)Cl)F)C=1C=NN(C1)C KMKNLPHJEJMJOM-UHFFFAOYSA-N 0.000 claims 1
- NMDFAQXLJQRHMS-UHFFFAOYSA-N 3-[2,6-dichloro-7-fluoro-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound C1=NN(CCC)C=C1N1C2=C(F)C(Cl)=CC=C2C(SC=2C(=C(C(O)=O)C=CC=2)F)=C1Cl NMDFAQXLJQRHMS-UHFFFAOYSA-N 0.000 claims 1
- CHFTWRTZSPUBLH-UHFFFAOYSA-N 3-[2,6-dichloro-7-fluoro-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound ClC=1N(C2=C(C(=CC=C2C1SC=1C=C(C(=O)O)C=CC1)Cl)F)C=1C=NN(C1)CCC CHFTWRTZSPUBLH-UHFFFAOYSA-N 0.000 claims 1
- SAHGEMBFMJNJBH-UHFFFAOYSA-N 3-[2-bromo-6-chloro-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound BrC=1N(C2=CC(=CC=C2C1SC=1C=C(C(=O)O)C=CC1)Cl)C=1C=NN(C1)CCC SAHGEMBFMJNJBH-UHFFFAOYSA-N 0.000 claims 1
- KOCAUNIBIIJPAY-UHFFFAOYSA-N 3-[6-chloro-2-cyano-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1)C=1C=NN(C1)CCC)C#N)SC=1C=C(C(=O)O)C=CC1 KOCAUNIBIIJPAY-UHFFFAOYSA-N 0.000 claims 1
- BQMMCRXYIIKAOB-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-1-(1-ethylpyrazol-4-yl)-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CC)C1CC1)SC=1C(=C(C(=O)O)C=CC1)F BQMMCRXYIIKAOB-UHFFFAOYSA-N 0.000 claims 1
- AQYXZSLWKGMODC-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1)C=1C=NN(C1)CCC)C1CC1)SC=1C=C(C(=O)O)C=CC1 AQYXZSLWKGMODC-UHFFFAOYSA-N 0.000 claims 1
- AKPNMORVNGXMAR-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-1-[1-[6-[(3',6'-dihydroxy-3-oxospiro[2-benzofuran-1,9'-xanthene]-5-yl)carbamoylamino]hexyl]pyrazol-4-yl]-7-fluoroindol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C=1)CCCCCCNC(=O)NC=1C=C2C(OC3(C4=CC=C(C=C4OC=4C=C(C=CC3=4)O)O)C2=CC=1)=O)C1CC1)SC=1C(=C(C(=O)O)C=CC=1)F AKPNMORVNGXMAR-UHFFFAOYSA-N 0.000 claims 1
- BXVVWSMGIFMPDK-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CCC)C1CC1)SC=1C(=C(C(=O)O)C=CC1)F BXVVWSMGIFMPDK-UHFFFAOYSA-N 0.000 claims 1
- ZGMRPBQYGJRCSH-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-(1-propylpyrazol-4-yl)indol-3-yl]sulfanylbenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CCC)C1CC1)SC=1C=C(C(=O)O)C=CC1 ZGMRPBQYGJRCSH-UHFFFAOYSA-N 0.000 claims 1
- IIMOPZDZUCECRV-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-(1H-pyrazol-4-yl)indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NNC1)C1CC1)SC=1C(=C(C(=O)O)C=CC1)F IIMOPZDZUCECRV-UHFFFAOYSA-N 0.000 claims 1
- BQMMCRXYIIKAOB-ZBJDZAJPSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-[1-(1,1,2,2,2-pentadeuterioethyl)pyrazol-4-yl]indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C=1)C(C([2H])([2H])[2H])([2H])[2H])C1CC1)SC=1C(=C(C(=O)O)C=CC=1)F BQMMCRXYIIKAOB-ZBJDZAJPSA-N 0.000 claims 1
- XLYDPYXDKFQHGA-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-[1-(2,2,2-trifluoroethyl)pyrazol-4-yl]indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CC(F)(F)F)C1CC1)SC=1C(=C(C(=O)O)C=CC1)F XLYDPYXDKFQHGA-UHFFFAOYSA-N 0.000 claims 1
- PMYABKQWACWHAZ-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-[1-(2-hydroxyethyl)pyrazol-4-yl]indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CCO)C1CC1)SC=1C(=C(C(=O)O)C=CC1)F PMYABKQWACWHAZ-UHFFFAOYSA-N 0.000 claims 1
- YKZDBHMPBGUICX-UHFFFAOYSA-N 3-[6-chloro-2-cyclopropyl-7-fluoro-1-[1-(3-hydroxy-2,2-dimethylpropyl)pyrazol-4-yl]indol-3-yl]sulfanyl-2-fluorobenzoic acid Chemical compound OCC(CN1N=CC(=C1)N1C(=C(C2=CC=C(C(=C12)F)Cl)SC=1C(=C(C(=O)O)C=CC1)F)C1CC1)(C)C YKZDBHMPBGUICX-UHFFFAOYSA-N 0.000 claims 1
- JVMQTLLAGLHIKA-UHFFFAOYSA-N 6-[6-chloro-2-cyclopropyl-1-(1-ethylpyrazol-4-yl)-7-fluoroindol-3-yl]sulfanylpyridine-2-carboxylic acid Chemical compound ClC1=CC=C2C(=C(N(C2=C1F)C=1C=NN(C1)CC)C1CC1)SC1=CC=CC(=N1)C(=O)O JVMQTLLAGLHIKA-UHFFFAOYSA-N 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000006185 dispersion Substances 0.000 claims 1
- 239000000839 emulsion Substances 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 239000000499 gel Substances 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 239000002674 ointment Substances 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000006187 pill Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- 239000000725 suspension Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361907965P | 2013-11-22 | 2013-11-22 | |
| US61/907,965 | 2013-11-22 | ||
| US201462038121P | 2014-08-15 | 2014-08-15 | |
| US62/038,121 | 2014-08-15 | ||
| PCT/US2014/066706 WO2015077503A1 (en) | 2013-11-22 | 2014-11-20 | Autotaxin inhibitor compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016537389A JP2016537389A (ja) | 2016-12-01 |
| JP2016537389A5 true JP2016537389A5 (enExample) | 2017-12-28 |
| JP6501367B2 JP6501367B2 (ja) | 2019-04-17 |
Family
ID=53180152
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016533532A Active JP6501367B2 (ja) | 2013-11-22 | 2014-11-20 | オートタキシン阻害剤化合物 |
Country Status (31)
| Country | Link |
|---|---|
| US (7) | US9334261B2 (enExample) |
| EP (2) | EP3878848A1 (enExample) |
| JP (1) | JP6501367B2 (enExample) |
| KR (2) | KR102515248B1 (enExample) |
| CN (2) | CN105793253B (enExample) |
| AU (2) | AU2014352888B2 (enExample) |
| BR (1) | BR112016010220B1 (enExample) |
| CA (1) | CA2930737C (enExample) |
| CL (1) | CL2016001231A1 (enExample) |
| CR (2) | CR20160289A (enExample) |
| CY (1) | CY1124407T1 (enExample) |
| DK (1) | DK3071561T3 (enExample) |
| EA (1) | EA030068B1 (enExample) |
| ES (1) | ES2875899T3 (enExample) |
| HR (1) | HRP20210957T1 (enExample) |
| HU (1) | HUE055213T2 (enExample) |
| IL (2) | IL245383B (enExample) |
| LT (1) | LT3071561T (enExample) |
| MX (2) | MX375706B (enExample) |
| MY (1) | MY182095A (enExample) |
| NI (1) | NI201600071A (enExample) |
| NZ (1) | NZ720478A (enExample) |
| PE (1) | PE20160654A1 (enExample) |
| PH (1) | PH12016500862B1 (enExample) |
| PL (1) | PL3071561T3 (enExample) |
| PT (1) | PT3071561T (enExample) |
| RS (1) | RS62027B1 (enExample) |
| SI (1) | SI3071561T1 (enExample) |
| SM (1) | SMT202100531T1 (enExample) |
| WO (1) | WO2015077503A1 (enExample) |
| ZA (2) | ZA201603083B (enExample) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2861566T1 (sl) | 2012-06-13 | 2017-03-31 | F. Hoffmann-La Roche Ag | Novi diazaspirocikloalkan in azaspirocikloalkan |
| DK2900669T3 (da) | 2012-09-25 | 2019-11-04 | Hoffmann La Roche | Hexahydropyrrolo[3,4-C]pyrrolderivater og relaterede forbindelser som autotaxin (ATX)-inhibitorer og som inhibitorer af lysophosphatidsyre (LPA)-produktion til behandling af f.eks. nyresygdomme |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| WO2015042052A1 (en) | 2013-09-17 | 2015-03-26 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| WO2015042053A1 (en) | 2013-09-17 | 2015-03-26 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3049405A4 (en) | 2013-09-26 | 2017-03-08 | Pharmakea Inc. | Autotaxin inhibitor compounds |
| AU2014352888B2 (en) | 2013-11-22 | 2019-05-09 | Sabre Therapeutics Llc | Autotaxin inhibitor compounds |
| CA2930735A1 (en) | 2013-11-22 | 2015-05-28 | Pharmakea, Inc. | Tetracyclic autotaxin inhibitors |
| JP6496730B2 (ja) | 2013-11-26 | 2019-04-03 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新規なオクタヒドロ−シクロブタ［１，２−ｃ；３，４−ｃ’］ジピロール−２−イル |
| CN106103446B (zh) | 2014-03-26 | 2019-07-30 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物 |
| AU2015238541B2 (en) | 2014-03-26 | 2019-09-19 | F. Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (ATX) and lysophosphatidic acid (LPA) production inhibitors |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| KR102663569B1 (ko) * | 2015-05-27 | 2024-05-03 | 사브레 테라퓨틱스 엘엘씨 | 오토탁신 억제제 및 이의 용도 |
| KR20180043837A (ko) | 2015-09-04 | 2018-04-30 | 에프. 호프만-라 로슈 아게 | 페녹시메틸 유도체 |
| RU2018114289A (ru) | 2015-09-24 | 2019-10-24 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов аутотаксина (atx) |
| MX2018001890A (es) | 2015-09-24 | 2018-06-20 | Hoffmann La Roche | Compuestos biciclicos como inhibidores de autotaxina (atx). |
| EP3353181B1 (en) | 2015-09-24 | 2021-08-11 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| US11000142B2 (en) | 2016-12-06 | 2021-05-11 | John Joseph Girard | Flexible floor mat incorporating LED lighting |
| JP7090099B2 (ja) | 2017-03-16 | 2022-06-23 | エフ．ホフマン－ラ ロシュ アーゲー | Ａｔｘインヒビターとしての新規二環式化合物 |
| CR20190423A (es) | 2017-03-16 | 2019-11-01 | Hoffmann La Roche | Nuevos compuestos biciclícos como inhibidores dobles de atx/ca |
| EP3675906A4 (en) | 2017-08-28 | 2021-05-26 | Angiex, Inc. | ANTI-TM4SF1 ANTIBODIES AND METHOD OF USING THEREOF |
| CN113874051A (zh) | 2019-02-27 | 2021-12-31 | 安吉克公司 | 包含抗tm4sf1抗体的抗体-药物缀合物及其使用方法 |
| US20250282759A1 (en) * | 2022-05-03 | 2025-09-11 | Sabre Therapeutics Llc | Polymorphic and salt forms of the autotaxin inhibitor cudetaxestat |
| CN116239577A (zh) * | 2023-03-27 | 2023-06-09 | 沈阳药科大学 | 一种制备Cudetaxestat的方法 |
| CN116396205B (zh) * | 2023-04-20 | 2024-10-01 | 沈阳药科大学 | 一种n-芳基吲哚衍生物及其制备方法和应用 |
Family Cites Families (80)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5210574A (en) | 1991-03-08 | 1993-05-11 | Mita Industrial Co., Ltd. | Photosensitive drum body-mounting mechanism including a drive coupling member with a coupling protrusion adapted to bite into the inner surface of the mechanism's photosensitive drum |
| US5186522A (en) | 1991-09-24 | 1993-02-16 | Midland Brake, Inc. | Air dryer purge line |
| AU663990B2 (en) | 1992-11-10 | 1995-10-26 | Caterpillar Inc. | Solenoid valve assembly |
| US5407368A (en) | 1992-12-15 | 1995-04-18 | Minnesota Mining And Manufacturing Company | Electrode connector |
| US5761473A (en) | 1993-01-08 | 1998-06-02 | International Business Machines Corporation | Method and system for increased instruction synchronization efficiency in a superscalar processsor system utilizing partial data dependency interlocking |
| US5564949A (en) | 1995-01-05 | 1996-10-15 | Thomas & Betts Corporation | Shielded compact data connector |
| JP2664048B2 (ja) | 1995-03-27 | 1997-10-15 | 科学技術庁金属材料技術研究所長 | 六フッ化二ケイ素の合成法 |
| GB9514473D0 (en) | 1995-07-14 | 1995-09-13 | Glaxo Lab Sa | Chemical compounds |
| EP1284728A4 (en) | 1999-10-22 | 2004-05-19 | Merck & Co Inc | MEDICINES FOR TREATING ADDICTIC ADDICTION |
| US6890933B1 (en) | 2000-02-24 | 2005-05-10 | President And Fellows Of Harvard College | Kinesin inhibitors |
| US6858620B2 (en) | 2000-10-03 | 2005-02-22 | Lilly Icos, Llc | Condensed pyridoindole derivatives |
| AU2002254616B2 (en) | 2001-04-11 | 2007-09-06 | Idenix (Cayman) Limited | Phenylindoles for the treatment of HIV |
| ATE292115T1 (de) | 2001-09-27 | 2005-04-15 | Hoffmann La Roche | Indolderivate als cox-ii-inhibitoren |
| US7528165B2 (en) | 2001-12-13 | 2009-05-05 | National Health Research Institutes | Indole compounds |
| NZ538031A (en) | 2002-08-29 | 2007-10-26 | Merck & Co Inc | Indoles having anti-diabetic activity |
| EP1546142A4 (en) | 2002-08-29 | 2007-10-17 | Merck & Co Inc | INDOLES HAVING ANTIDIABETIC EFFECT |
| ES2379169T3 (es) | 2003-05-19 | 2012-04-23 | Irm Llc | Composiciones y compuestos inmunosupresores |
| JP4090491B2 (ja) | 2003-12-23 | 2008-05-28 | ハー・ルンドベック・アクチエゼルスカベット | ２−（１ｈ−インドリルスルファニル）−ベンジルアミン誘導体 |
| JP4714143B2 (ja) | 2004-05-19 | 2011-06-29 | 住友電気工業株式会社 | Ｉｉｉ族窒化物半導体結晶の製造方法 |
| KR101141650B1 (ko) | 2004-09-30 | 2012-05-17 | 엘지전자 주식회사 | 매체접속제어 계층에서의 데이터 처리 방법 및 이동통신용단말 |
| WO2006041961A1 (en) | 2004-10-05 | 2006-04-20 | GOVERNMENT OF THE UNITED STATES OF AMERICA, as represented by THE SECRETARY, DEPARTMENT OF HEALTHAND HUMAN SERVICES | Arylthioindole tubulin polymerization inhibitors and methods of treating or preventing cancer using same |
| WO2007134169A2 (en) | 2006-05-10 | 2007-11-22 | Nuada, Llc | Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof and methods of use thereof |
| WO2006050236A2 (en) | 2004-11-01 | 2006-05-11 | Nuada, Llc | Compounds and methods of use thereof |
| US20060270634A1 (en) | 2005-05-06 | 2006-11-30 | Miller Duane D | Acetal phosphate-derived LPA mimics, PPARgamma activators, and autotaxin inhibitors |
| AR054394A1 (es) | 2005-06-17 | 2007-06-20 | Lundbeck & Co As H | Derivados de 2- (1h-indolilsulfanil)-aril amina |
| WO2007041600A2 (en) | 2005-10-03 | 2007-04-12 | Luminescent Technologies, Inc. | Mask-pattern determination using topology types |
| JP5081161B2 (ja) | 2005-12-19 | 2012-11-21 | スミスクライン ビーチャム コーポレーション | ファルネソイドｘ受容体アゴニスト |
| WO2008157361A1 (en) | 2007-06-15 | 2008-12-24 | University Of Utah Research Foundation | α-CHLORO AND α-BROMO PHOSPHONATE ANALOGS OF LYSOPHOSPHATIDIC ACID AND METHODS OF MAKING AND USING THEREOF |
| DE102007047737A1 (de) | 2007-10-05 | 2009-04-30 | Merck Patent Gmbh | Piperidin- und Piperazinderivate |
| DE102007047738A1 (de) | 2007-10-05 | 2009-04-09 | Merck Patent Gmbh | Imidazolderivate |
| DE102007047735A1 (de) | 2007-10-05 | 2009-04-09 | Merck Patent Gmbh | Thiazolderivate |
| US8268891B1 (en) | 2007-11-13 | 2012-09-18 | University Of Memphis Research Foundation | Autotaxin inhibitors |
| US8378100B2 (en) | 2008-01-09 | 2013-02-19 | University Of Virginia Patent Foundation | Phosphonate derivatives as autotaxin inhibitors |
| US20110110886A1 (en) | 2008-06-13 | 2011-05-12 | Yale University | Small molecule inhibitors of autotaxin and methods of use |
| US8022239B2 (en) | 2008-10-03 | 2011-09-20 | The University Of Memphis Research Foundation | Mechanism-based inactivators of autotaxin |
| DE102008059578A1 (de) | 2008-11-28 | 2010-06-10 | Merck Patent Gmbh | Benzo-Naphtyridin Verbindungen |
| MX2011005720A (es) | 2008-12-01 | 2011-06-17 | Merck Patent Gmbh | Pirido [4,3-d] pirimidinas 2,5-diamino sustituidas como inhibidores de autotaxina contra cancer. |
| EP2414327B1 (de) | 2009-04-02 | 2014-11-19 | Merck Patent GmbH | Heterocyclische verbindungen als autotaxin-inhibitoren |
| ES2422718T3 (es) | 2009-04-02 | 2013-09-13 | Merck Patent Gmbh | Derivados de piperidina y piperazina como inhibidores de la autotaxina |
| WO2010112124A1 (en) * | 2009-04-02 | 2010-10-07 | Merck Patent Gmbh | Autotaxin inhibitors |
| US8445200B2 (en) | 2009-04-15 | 2013-05-21 | The Regents Of The University Of California | Genotoxicity as a biomarker for inflammation |
| JP5903734B2 (ja) | 2009-05-11 | 2016-04-13 | バーグ エルエルシー | エピメタボリックシフター、多次元細胞内分子、または環境影響因子を使用する腫瘍性障害の処置方法 |
| CN105935365B (zh) | 2009-05-20 | 2018-12-21 | Eth苏黎世公司 | 用于代谢紊乱的靶向微小rna |
| WO2011002918A1 (en) | 2009-06-30 | 2011-01-06 | The University Of Memphis Research Foundation | Novel diverse lead compound autotaxin inhibitors |
| DE102009033392A1 (de) | 2009-07-16 | 2011-01-20 | Merck Patent Gmbh | Heterocyclische Verbindungen als Autotaxin-Inhibitoren II |
| DE102009049211A1 (de) | 2009-10-13 | 2011-04-28 | Merck Patent Gmbh | Sulfoxide |
| WO2011049433A1 (en) | 2009-10-23 | 2011-04-28 | Academisch Ziekenhuis Bij De Universiteit Van Amsterdam | Diagnosis and treatment of pruritis |
| WO2011053597A1 (en) | 2009-10-26 | 2011-05-05 | The University Of Memphis Research Foundation | Pipemidic acid derivative autotaxin inhibitors |
| US8497371B2 (en) | 2009-10-26 | 2013-07-30 | University Of Memphis Research Foundation | Pipemidic acid derivative autotaxin inhibitors |
| US9187471B2 (en) | 2010-02-19 | 2015-11-17 | Medivation Technologies, Inc. | Pyrido [4,3-b] indole and pyrido [3,4-b] indole derivatives and methods of use |
| CA2794211A1 (en) | 2010-03-26 | 2011-09-29 | Wolfgang Staehle | Benzonaphthyridinamines as autotaxin inhibitors |
| US20130116171A1 (en) | 2010-04-16 | 2013-05-09 | Salk Institute For Biological Studies | Methods for treating metabolic disorders using fgf |
| ES2646834T3 (es) * | 2010-08-20 | 2017-12-18 | Amira Pharmaceuticals, Inc. | Inhibidores de autotaxina y usos de los mismos |
| US8771696B2 (en) | 2010-11-23 | 2014-07-08 | Regeneron Pharmaceuticals, Inc. | Method of reducing the severity of stress hyperglycemia with human antibodies to the glucagon receptor |
| WO2012100018A1 (en) | 2011-01-20 | 2012-07-26 | University Of Tennessee Research Foundation | Inhibitors of autotaxin |
| EP2675459A4 (en) | 2011-02-18 | 2014-08-06 | Medivation Technologies Inc | COMPOUNDS AND METHOD FOR THE TREATMENT OF DIABETES |
| WO2012112964A2 (en) | 2011-02-18 | 2012-08-23 | Medivation Technologies, Inc. | PYRIDO[4,3-b]INDOLE AND PYRIDO[3,4-b]INDOLE DERIVATIVES AND METHODS OF USE |
| US20140086839A1 (en) | 2011-03-17 | 2014-03-27 | Tel Hashomer Medical Research Infrastructure And Services Ltd. | Quinolone analogs for treating autoimmune diseases |
| WO2012166415A1 (en) * | 2011-05-27 | 2012-12-06 | Amira Pharmaceuticals, Inc. | Heterocyclic autotaxin inhibitors and uses thereof |
| GB2494154B (en) | 2011-08-31 | 2017-11-29 | Metaswitch Networks Ltd | Conditional telecommunications |
| WO2013054185A1 (en) | 2011-10-13 | 2013-04-18 | Pfizer, Inc. | Pyrimidine and pyridine derivatives useful in therapy |
| IN2014DN03063A (enExample) | 2011-10-28 | 2015-05-15 | Inhibitaxin Ltd | |
| JP2013129632A (ja) | 2011-12-22 | 2013-07-04 | Ono Pharmaceut Co Ltd | Ｅｎｐｐ２阻害化合物 |
| US20130270634A1 (en) | 2012-04-12 | 2013-10-17 | Richtek Technology Corporation | High voltage device and manufacturing method thereof |
| SI2861566T1 (sl) | 2012-06-13 | 2017-03-31 | F. Hoffmann-La Roche Ag | Novi diazaspirocikloalkan in azaspirocikloalkan |
| WO2014031170A1 (en) | 2012-08-22 | 2014-02-27 | Medivation Technologies, Inc. | Pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives and methods of use |
| DK2900669T3 (da) | 2012-09-25 | 2019-11-04 | Hoffmann La Roche | Hexahydropyrrolo[3,4-C]pyrrolderivater og relaterede forbindelser som autotaxin (ATX)-inhibitorer og som inhibitorer af lysophosphatidsyre (LPA)-produktion til behandling af f.eks. nyresygdomme |
| US9409895B2 (en) | 2012-12-19 | 2016-08-09 | Novartis Ag | Autotaxin inhibitors |
| EA028509B1 (ru) | 2012-12-19 | 2017-11-30 | Новартис Аг | Ингибиторы аутотаксина, фармацевтические композиции и комбинации, содержащие их, и их применение в лечении заболеваний и состояний, опосредованных аутотаксином |
| TWI499591B (zh) | 2013-01-11 | 2015-09-11 | Lilly Co Eli | 雙環嘧啶化合物 |
| WO2015042052A1 (en) | 2013-09-17 | 2015-03-26 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| WO2015042053A1 (en) | 2013-09-17 | 2015-03-26 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3049405A4 (en) | 2013-09-26 | 2017-03-08 | Pharmakea Inc. | Autotaxin inhibitor compounds |
| HUE038663T2 (hu) | 2013-11-05 | 2018-12-28 | Bayer Cropscience Ag | Szubsztituált benzamid-származékok ízeltlábúak irtására |
| CA2930735A1 (en) | 2013-11-22 | 2015-05-28 | Pharmakea, Inc. | Tetracyclic autotaxin inhibitors |
| AU2014352888B2 (en) | 2013-11-22 | 2019-05-09 | Sabre Therapeutics Llc | Autotaxin inhibitor compounds |
| KR20160079137A (ko) | 2013-11-22 | 2016-07-05 | 바스프 에스이 | N-아실이미노 헤테로시클릭 화합물 |
| CL2016001118A1 (es) | 2013-11-22 | 2016-12-02 | Basf Se | Compuestos heterocíclicos de n-acilimino |
| US9051320B1 (en) * | 2014-08-18 | 2015-06-09 | Pharmakea, Inc. | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
| KR102663569B1 (ko) | 2015-05-27 | 2024-05-03 | 사브레 테라퓨틱스 엘엘씨 | 오토탁신 억제제 및 이의 용도 |
-
2014
- 2014-11-20 AU AU2014352888A patent/AU2014352888B2/en active Active
- 2014-11-20 WO PCT/US2014/066706 patent/WO2015077503A1/en not_active Ceased
- 2014-11-20 LT LTEP14864293.7T patent/LT3071561T/lt unknown
- 2014-11-20 EP EP21156420.8A patent/EP3878848A1/en active Pending
- 2014-11-20 NZ NZ720478A patent/NZ720478A/en unknown
- 2014-11-20 DK DK14864293.7T patent/DK3071561T3/da active
- 2014-11-20 EA EA201690881A patent/EA030068B1/ru unknown
- 2014-11-20 HU HUE14864293A patent/HUE055213T2/hu unknown
- 2014-11-20 PL PL14864293T patent/PL3071561T3/pl unknown
- 2014-11-20 EP EP14864293.7A patent/EP3071561B1/en active Active
- 2014-11-20 SI SI201431843T patent/SI3071561T1/sl unknown
- 2014-11-20 PE PE2016000669A patent/PE20160654A1/es unknown
- 2014-11-20 PT PT148642937T patent/PT3071561T/pt unknown
- 2014-11-20 CR CR20160289A patent/CR20160289A/es unknown
- 2014-11-20 SM SM20210531T patent/SMT202100531T1/it unknown
- 2014-11-20 MY MYPI2016000959A patent/MY182095A/en unknown
- 2014-11-20 BR BR112016010220-7A patent/BR112016010220B1/pt active IP Right Grant
- 2014-11-20 MX MX2016006623A patent/MX375706B/es active IP Right Grant
- 2014-11-20 JP JP2016533532A patent/JP6501367B2/ja active Active
- 2014-11-20 KR KR1020227005531A patent/KR102515248B1/ko active Active
- 2014-11-20 ES ES14864293T patent/ES2875899T3/es active Active
- 2014-11-20 CN CN201480063881.XA patent/CN105793253B/zh active Active
- 2014-11-20 CR CR20190394A patent/CR20190394A/es unknown
- 2014-11-20 KR KR1020167014496A patent/KR102367876B1/ko active Active
- 2014-11-20 RS RS20210786A patent/RS62027B1/sr unknown
- 2014-11-20 CN CN201910686732.3A patent/CN110372671B/zh active Active
- 2014-11-20 HR HRP20210957TT patent/HRP20210957T1/hr unknown
- 2014-11-20 CA CA2930737A patent/CA2930737C/en active Active
-
2015
- 2015-10-29 US US14/926,877 patent/US9334261B2/en active Active
-
2016
- 2016-03-03 US US15/060,398 patent/US9468628B2/en active Active
- 2016-05-02 IL IL24538316A patent/IL245383B/en active IP Right Grant
- 2016-05-09 ZA ZA2016/03083A patent/ZA201603083B/en unknown
- 2016-05-10 PH PH12016500862A patent/PH12016500862B1/en unknown
- 2016-05-20 CL CL2016001231A patent/CL2016001231A1/es unknown
- 2016-05-20 MX MX2020009780A patent/MX2020009780A/es unknown
- 2016-05-20 NI NI201600071A patent/NI201600071A/es unknown
- 2016-09-09 US US15/261,659 patent/US9999615B2/en active Active
-
2018
- 2018-05-03 US US15/970,337 patent/US10688081B2/en active Active
-
2019
- 2019-08-09 AU AU2019213425A patent/AU2019213425B2/en active Active
- 2019-10-24 IL IL270168A patent/IL270168B/en unknown
-
2020
- 2020-05-14 US US16/874,073 patent/US11344533B2/en active Active
- 2020-08-05 ZA ZA2020/05029A patent/ZA202005029B/en unknown
-
2021
- 2021-06-23 CY CY20211100562T patent/CY1124407T1/el unknown
-
2022
- 2022-05-06 US US17/662,403 patent/US11779568B2/en active Active
-
2023
- 2023-10-04 US US18/481,141 patent/US12268668B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016537389A5 (enExample) | ||
| ES3049520T3 (en) | Farnesoid x receptor agonists and uses thereof | |
| AU2013322854B2 (en) | Combination of regorafenib and acetylsalicylic acid for treating cancer | |
| JP2016535772A5 (enExample) | ||
| RU2015138964A (ru) | Полициклические модуляторы рецептора эстрогена и их применения | |
| HRP20210957T1 (hr) | Spojevi inhibitori autotaksina | |
| JP2013510883A5 (enExample) | ||
| JP2004504301A5 (enExample) | ||
| JP2017502940A5 (enExample) | ||
| JP2014139226A5 (enExample) | ||
| JP2016532673A5 (enExample) | ||
| JP5075821B2 (ja) | Ｈｉｖ逆転写酵素阻害剤 | |
| HRP20220003T1 (hr) | Spojevi derivata 1,3,4-oksadiazola kao inhibitori histonske deacetilaze 6, i farmaceutski pripravak koji ih sadrži | |
| JP2015529229A5 (enExample) | ||
| JP2004502670A5 (enExample) | ||
| JP2012504141A5 (enExample) | ||
| JP2013536200A (ja) | オートタキシン阻害剤およびその使用 | |
| JP2014525444A5 (enExample) | ||
| JP2013534245A5 (enExample) | ||
| BRPI0720270B1 (pt) | Compostos 4-fenil-6-(2,2,2-triflúor-1-fenil etoxi) pirimidina, composição e forma de dosagem sólida | |
| JP2016534124A5 (enExample) | ||
| HRP20140098T1 (hr) | Derivati piridin-4-ila kao agonisti s1p1/edg1 | |
| HRP20171248T1 (hr) | Amino-supstituirani imidazopiridazini | |
| CN107635975B (zh) | Dgat2抑制剂 | |
| JP2020532550A (ja) | リゾホスファチジン酸受容体１（ｌｐａｒ１）阻害剤化合物 |