JP2016537389A5 - - Google Patents
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- 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
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- 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 (OSRAM) | 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 (OSRAM) |
| EP (2) | EP3878848A1 (OSRAM) |
| JP (1) | JP6501367B2 (OSRAM) |
| KR (2) | KR102515248B1 (OSRAM) |
| CN (2) | CN105793253B (OSRAM) |
| AU (2) | AU2014352888B2 (OSRAM) |
| BR (1) | BR112016010220B1 (OSRAM) |
| CA (1) | CA2930737C (OSRAM) |
| CL (1) | CL2016001231A1 (OSRAM) |
| CR (2) | CR20160289A (OSRAM) |
| CY (1) | CY1124407T1 (OSRAM) |
| DK (1) | DK3071561T3 (OSRAM) |
| EA (1) | EA030068B1 (OSRAM) |
| ES (1) | ES2875899T3 (OSRAM) |
| HR (1) | HRP20210957T1 (OSRAM) |
| HU (1) | HUE055213T2 (OSRAM) |
| IL (2) | IL245383B (OSRAM) |
| LT (1) | LT3071561T (OSRAM) |
| MX (2) | MX375706B (OSRAM) |
| MY (1) | MY182095A (OSRAM) |
| NI (1) | NI201600071A (OSRAM) |
| NZ (1) | NZ720478A (OSRAM) |
| PE (1) | PE20160654A1 (OSRAM) |
| PH (1) | PH12016500862B1 (OSRAM) |
| PL (1) | PL3071561T3 (OSRAM) |
| PT (1) | PT3071561T (OSRAM) |
| RS (1) | RS62027B1 (OSRAM) |
| SI (1) | SI3071561T1 (OSRAM) |
| SM (1) | SMT202100531T1 (OSRAM) |
| WO (1) | WO2015077503A1 (OSRAM) |
| ZA (2) | ZA201603083B (OSRAM) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN2014DN09346A (OSRAM) | 2012-06-13 | 2015-07-17 | Hoffmann La Roche | |
| MA37940B1 (fr) | 2012-09-25 | 2018-09-28 | Hoffmann La Roche | Derives d'octahydro-cyclopenta(c)pyrrole substitues inhibiteurs de l'autotaxine, utiles pour traiter les affections renales, hepatiques et inflammatoires, les affections du systeme nerveux, les maladies fibreuses. |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| US9714240B2 (en) | 2013-09-17 | 2017-07-25 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3046909A4 (en) | 2013-09-17 | 2017-03-29 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| JP2016531874A (ja) | 2013-09-26 | 2016-10-13 | ファーマケア，インク． | オートタキシン阻害剤化合物 |
| EA201690880A1 (ru) | 2013-11-22 | 2016-12-30 | Фармакеа, Инк. | Тетрациклические ингибиторы аутотаксина |
| CA2930737C (en) | 2013-11-22 | 2023-02-21 | Pharmakea, Inc. | Autotaxin inhibitor compounds |
| UA118201C2 (uk) | 2013-11-26 | 2018-12-10 | Ф. Хоффманн-Ля Рош Аг | НОВИЙ ОКТАГІДРОЦИКЛОБУТА[1,2-c;3,4-c']ДИПІРОЛ-2-ІЛ |
| EP3590939A1 (en) | 2014-03-26 | 2020-01-08 | F. Hoffmann-La Roche AG | Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| WO2015144609A1 (en) | 2014-03-26 | 2015-10-01 | 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 |
| SG10201911204WA (en) | 2015-05-27 | 2020-02-27 | Pharmakea Inc | Autotaxin inhibitors and uses thereof |
| PE20180479A1 (es) | 2015-09-04 | 2018-03-07 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
| CA2984585A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| CR20180057A (es) | 2015-09-24 | 2018-04-02 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx/ca. |
| MX2018002217A (es) | 2015-09-24 | 2018-03-23 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de autotaxina (atx). |
| PE20180451A1 (es) | 2015-09-24 | 2018-03-05 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores de atx |
| US11000142B2 (en) | 2016-12-06 | 2021-05-11 | John Joseph Girard | Flexible floor mat incorporating LED lighting |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| WO2019046338A1 (en) | 2017-08-28 | 2019-03-07 | Angiex, Inc. | ANTI-TM4SF1 ANTIBODIES AND METHODS OF USE |
| AU2020228060A1 (en) | 2019-02-27 | 2021-09-16 | Angiex, Inc. | Antibody-drug conjugates comprising anti-TM4SF1 antibodies and methods of using the same |
| CN120112527A (zh) * | 2022-05-03 | 2025-06-06 | 迪方知识产权收购有限责任公司 | 自分泌运动因子抑制剂cudetaxestat的多晶型形式和盐形式 |
| 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 |
| DE69316741T2 (de) | 1992-11-10 | 1998-09-10 | Caterpillar Inc | Magnetventil |
| 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 |
| WO2001030343A1 (en) | 1999-10-22 | 2001-05-03 | Merck & Co., Inc. | Pharmaceuticals for treating obesity |
| US6890933B1 (en) | 2000-02-24 | 2005-05-10 | President And Fellows Of Harvard College | Kinesin inhibitors |
| ATE332903T1 (de) | 2000-10-03 | 2006-08-15 | Lilly Icos Llc | Kondensierte pyridoindolderivate |
| CA2444501C (en) | 2001-04-11 | 2009-11-17 | Idenix (Cayman) Limited | Phenylindoles for the treatment of hiv |
| IL160752A0 (en) * | 2001-09-27 | 2004-08-31 | Hoffmann La Roche | Indole derivatives as cox ii inhibitors |
| US7528165B2 (en) | 2001-12-13 | 2009-05-05 | National Health Research Institutes | Indole compounds |
| DK1537078T3 (da) | 2002-08-29 | 2010-08-02 | Merck Sharp & Dohme | Indoler med anti-diabetisk aktivitet |
| US7393960B2 (en) | 2002-08-29 | 2008-07-01 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| AU2004240649A1 (en) | 2003-05-19 | 2004-12-02 | Irm, Llc | Immunosuppressant compounds and compositions |
| 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 |
| WO2006050236A2 (en) | 2004-11-01 | 2006-05-11 | Nuada, Llc | Compounds and methods of use thereof |
| WO2007134169A2 (en) | 2006-05-10 | 2007-11-22 | Nuada, Llc | Indole, benzimidazole, and benzolactam boronic acid compounds, analogs thereof 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 |
| US8722649B2 (en) | 2007-06-15 | 2014-05-13 | University Of Utah Research Foundation | Alpha-chloro and alpha-bromo phosphonate analogs of lysophosphatidic acid and methods of making and using thereof |
| DE102007047738A1 (de) | 2007-10-05 | 2009-04-09 | Merck Patent Gmbh | Imidazolderivate |
| DE102007047737A1 (de) | 2007-10-05 | 2009-04-30 | Merck Patent Gmbh | Piperidin- und Piperazinderivate |
| 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 |
| WO2009151644A2 (en) | 2008-06-13 | 2009-12-17 | Yale University | Small molecule inhibitors of autotaxin 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 |
| US8530650B2 (en) | 2008-12-01 | 2013-09-10 | Merck Patent Gmbh | 2, 5-diamino-substituted pyrido [4, 3-D] pyrimidines as autotaxin inhibitors against cancer |
| US8841324B2 (en) * | 2009-04-02 | 2014-09-23 | Merck Patent Gmbh | Heterocyclic compounds as autotaxin inhibitors |
| AU2010234087B2 (en) | 2009-04-02 | 2016-05-12 | Merck Patent Gmbh | Piperidine and piperazine derivatives as autotaxin inhibitors |
| JP5779172B2 (ja) | 2009-04-02 | 2015-09-16 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | オートタキシン阻害剤 |
| US8445200B2 (en) | 2009-04-15 | 2013-05-21 | The Regents Of The University Of California | Genotoxicity as a biomarker for inflammation |
| EP2429511B1 (en) | 2009-05-11 | 2019-02-20 | Berg LLC | Methods for treatment of oncological disorders using epimetabolic shifters, multidimensional intracellular molecules, or environmental influencers |
| WO2010133970A1 (en) | 2009-05-20 | 2010-11-25 | Eth Zurich | Targeting micrornas for metabolic disorders |
| 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 |
| WO2011103430A1 (en) | 2010-02-19 | 2011-08-25 | Medivation Technologies, Inc. | Pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives and methods of use |
| JP5827677B2 (ja) * | 2010-03-26 | 2015-12-02 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | オートタキシン阻害剤としてのベンゾナフチリジンアミン |
| JP5767314B2 (ja) | 2010-04-16 | 2015-08-19 | ソーク インスティチュート フォー バイオロジカル スタディーズ | Ｆｇｆを用いて代謝障害を処置するための方法 |
| US9000025B2 (en) | 2010-08-20 | 2015-04-07 | Amira Pharmaceuticals, Inc. | Autotaxin inhibitors and uses thereof |
| 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 |
| US8673882B2 (en) | 2011-01-20 | 2014-03-18 | University Of Tennessee Research Foundation | Inhibitors of autotaxin |
| US8815843B2 (en) | 2011-02-18 | 2014-08-26 | Medivation Technologies, Inc. | Compounds and methods of treating 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 |
| US9260416B2 (en) | 2011-05-27 | 2016-02-16 | 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 |
| CA2853231C (en) | 2011-10-28 | 2020-08-04 | Inhibitaxin Limited | Pyridazine derivatives with autotaxin activity for use in therapy |
| 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 |
| IN2014DN09346A (OSRAM) | 2012-06-13 | 2015-07-17 | Hoffmann La Roche | |
| 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 |
| MA37940B1 (fr) | 2012-09-25 | 2018-09-28 | Hoffmann La Roche | Derives d'octahydro-cyclopenta(c)pyrrole substitues inhibiteurs de l'autotaxine, utiles pour traiter les affections renales, hepatiques et inflammatoires, les affections du systeme nerveux, les maladies fibreuses. |
| US9409895B2 (en) | 2012-12-19 | 2016-08-09 | Novartis Ag | Autotaxin inhibitors |
| HK1212348A1 (en) | 2012-12-19 | 2016-06-10 | Novartis Ag | Autotaxin inhibitors |
| TWI499591B (zh) | 2013-01-11 | 2015-09-11 | Lilly Co Eli | 雙環嘧啶化合物 |
| US9714240B2 (en) | 2013-09-17 | 2017-07-25 | Pharmakea, Inc. | Vinyl autotaxin inhibitor compounds |
| EP3046909A4 (en) | 2013-09-17 | 2017-03-29 | Pharmakea, Inc. | Heterocyclic vinyl autotaxin inhibitor compounds |
| JP2016531874A (ja) * | 2013-09-26 | 2016-10-13 | ファーマケア，インク． | オートタキシン阻害剤化合物 |
| DK3066080T5 (en) | 2013-11-05 | 2018-09-17 | Bayer Cropscience Ag | SUBSTITUTED BENZAMIDES FOR TREATMENT OF ARTHROPODS |
| EA201690880A1 (ru) | 2013-11-22 | 2016-12-30 | Фармакеа, Инк. | Тетрациклические ингибиторы аутотаксина |
| CL2016001118A1 (es) | 2013-11-22 | 2016-12-02 | Basf Se | Compuestos heterocíclicos de n-acilimino |
| CA2930737C (en) | 2013-11-22 | 2023-02-21 | Pharmakea, Inc. | Autotaxin inhibitor compounds |
| PL3071560T3 (pl) | 2013-11-22 | 2018-07-31 | Basf Se | N-acyloiminowe związki heterocykliczne |
| US9051320B1 (en) * | 2014-08-18 | 2015-06-09 | Pharmakea, Inc. | Methods for the treatment of metabolic disorders by a selective small molecule autotaxin inhibitor |
| SG10201911204WA (en) | 2015-05-27 | 2020-02-27 | Pharmakea Inc | Autotaxin inhibitors and uses thereof |
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