JP2018502881A5 - - Google Patents
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- Publication number
- JP2018502881A5 JP2018502881A5 JP2017538582A JP2017538582A JP2018502881A5 JP 2018502881 A5 JP2018502881 A5 JP 2018502881A5 JP 2017538582 A JP2017538582 A JP 2017538582A JP 2017538582 A JP2017538582 A JP 2017538582A JP 2018502881 A5 JP2018502881 A5 JP 2018502881A5
- Authority
- JP
- Japan
- Prior art keywords
- cyano
- thiazol
- ylcarbamoyl
- group
- carboxylic acid
- 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 description 20
- 201000010099 disease Diseases 0.000 claims description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 11
- 239000003814 drug Substances 0.000 claims description 7
- 208000009304 Acute Kidney Injury Diseases 0.000 claims description 6
- 208000033626 Renal failure acute Diseases 0.000 claims description 6
- 201000011040 acute kidney failure Diseases 0.000 claims description 6
- 208000012998 acute renal failure Diseases 0.000 claims description 6
- 208000006673 asthma Diseases 0.000 claims description 6
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 6
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 6
- 208000010412 Glaucoma Diseases 0.000 claims description 5
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims description 3
- 208000023275 Autoimmune disease Diseases 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims description 3
- 208000018522 Gastrointestinal disease Diseases 0.000 claims description 3
- UCHDWCPVSPXUMX-TZIWLTJVSA-N Montelukast Chemical compound CC(C)(O)C1=CC=CC=C1CC[C@H](C=1C=C(\C=C\C=2N=C3C=C(Cl)C=CC3=CC=2)C=CC=1)SCC1(CC(O)=O)CC1 UCHDWCPVSPXUMX-TZIWLTJVSA-N 0.000 claims description 3
- 239000004012 Tofacitinib Substances 0.000 claims description 3
- 229960000997 bicalutamide Drugs 0.000 claims description 3
- 239000002934 diuretic Substances 0.000 claims description 3
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims description 3
- 229960002074 flutamide Drugs 0.000 claims description 3
- 229960002003 hydrochlorothiazide Drugs 0.000 claims description 3
- 208000017169 kidney disease Diseases 0.000 claims description 3
- WGFOBBZOWHGYQH-MXHNKVEKSA-N lubiprostone Chemical compound O1[C@](C(F)(F)CCCC)(O)CC[C@@H]2[C@@H](CCCCCCC(O)=O)C(=O)C[C@H]21 WGFOBBZOWHGYQH-MXHNKVEKSA-N 0.000 claims description 3
- 229960000345 lubiprostone Drugs 0.000 claims description 3
- 229960005127 montelukast Drugs 0.000 claims description 3
- 208000023504 respiratory system disease Diseases 0.000 claims description 3
- UJLAWZDWDVHWOW-YPMHNXCESA-N tofacitinib Chemical compound C[C@@H]1CCN(C(=O)CC#N)C[C@@H]1N(C)C1=NC=NC2=C1C=CN2 UJLAWZDWDVHWOW-YPMHNXCESA-N 0.000 claims description 3
- 229960001350 tofacitinib Drugs 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- -1 C 1 -C 6 alkoxyalkyl Chemical group 0.000 claims 25
- 125000005843 halogen group Chemical group 0.000 claims 11
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 229940124597 therapeutic agent Drugs 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 2
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000025966 Neurological disease Diseases 0.000 claims 2
- OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims 2
- 208000010643 digestive system disease Diseases 0.000 claims 2
- 208000018685 gastrointestinal system disease Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
- GNKMVTXKYXUROA-UHFFFAOYSA-N 1-[3-[(5-cyano-4-thiophen-2-yl-1,3-thiazol-2-yl)carbamoyl]benzoyl]piperidine-4-carboxylic acid Chemical compound C(#N)C1=C(N=C(S1)NC(=O)C=1C=C(C(=O)N2CCC(CC2)C(=O)O)C=CC=1)C=1SC=CC=1 GNKMVTXKYXUROA-UHFFFAOYSA-N 0.000 claims 1
- TZAXGJXOPBYRTJ-UHFFFAOYSA-N 1-[5-[(5-cyano-4-thiophen-2-yl-1,3-thiazol-2-yl)carbamoyl]thiophene-2-carbonyl]piperidine-4-carboxylic acid Chemical compound C(#N)C1=C(N=C(S1)NC(=O)C1=CC=C(S1)C(=O)N1CCC(CC1)C(=O)O)C=1SC=CC=1 TZAXGJXOPBYRTJ-UHFFFAOYSA-N 0.000 claims 1
- JHTLSTWSTCEOQN-UHFFFAOYSA-N 2-[[5-cyano-4-(4-methoxyphenyl)-1,3-thiazol-2-yl]carbamoyl]benzoic acid Chemical compound C(#N)C1=C(N=C(S1)NC(=O)C1=C(C(=O)O)C=CC=C1)C1=CC=C(C=C1)OC JHTLSTWSTCEOQN-UHFFFAOYSA-N 0.000 claims 1
- KOTLVAKDDWPYGM-UHFFFAOYSA-N 4-[[5-cyano-4-(1,3-thiazol-2-yl)-1,3-thiazol-2-yl]carbamoyl]benzoic acid Chemical compound C(#N)C1=C(N=C(S1)NC(=O)C1=CC=C(C(=O)O)C=C1)C=1SC=CN=1 KOTLVAKDDWPYGM-UHFFFAOYSA-N 0.000 claims 1
- 239000005711 Benzoic acid Substances 0.000 claims 1
- 239000002126 C01EB10 - Adenosine Substances 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 1
- 206010013774 Dry eye Diseases 0.000 claims 1
- 208000023105 Huntington disease Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 229960005305 adenosine Drugs 0.000 claims 1
- 235000010233 benzoic acid Nutrition 0.000 claims 1
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 1
- 206010009887 colitis Diseases 0.000 claims 1
- 239000013066 combination product Substances 0.000 claims 1
- 229940127555 combination product Drugs 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229940030606 diuretics Drugs 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- ORTFAQDWJHRMNX-UHFFFAOYSA-N hydroxidooxidocarbon(.) Chemical group O[C]=O ORTFAQDWJHRMNX-UHFFFAOYSA-N 0.000 claims 1
- SRJOCJYGOFTFLH-UHFFFAOYSA-N isonipecotic acid Chemical compound OC(=O)C1CCNCC1 SRJOCJYGOFTFLH-UHFFFAOYSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 239000000047 product Substances 0.000 claims 1
- 229940075993 receptor modulator Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 description 3
- 208000015114 central nervous system disease Diseases 0.000 description 1
- 230000001882 diuretic effect Effects 0.000 description 1
- 230000001613 neoplastic effect Effects 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ESP201530085 | 2015-01-22 | ||
| ES201530085A ES2578363B1 (es) | 2015-01-22 | 2015-01-22 | Moduladores de los receptores A3 de adenosina |
| PCT/ES2016/070032 WO2016116652A1 (es) | 2015-01-22 | 2016-01-22 | Moduladores de los receptores a3 de adenosina |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018502881A JP2018502881A (ja) | 2018-02-01 |
| JP2018502881A5 true JP2018502881A5 (enExample) | 2019-12-19 |
| JP6637983B2 JP6637983B2 (ja) | 2020-01-29 |
Family
ID=55359537
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017538582A Active JP6637983B2 (ja) | 2015-01-22 | 2016-01-22 | アデノシンａ３受容体の調節剤 |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US10238637B2 (enExample) |
| EP (1) | EP3248964B1 (enExample) |
| JP (1) | JP6637983B2 (enExample) |
| KR (1) | KR102424575B1 (enExample) |
| CN (1) | CN107207445B (enExample) |
| AU (1) | AU2016210091B2 (enExample) |
| BR (1) | BR112017015597B1 (enExample) |
| CA (1) | CA2974596C (enExample) |
| CY (1) | CY1122172T1 (enExample) |
| DK (1) | DK3248964T3 (enExample) |
| EA (1) | EA031627B1 (enExample) |
| ES (2) | ES2578363B1 (enExample) |
| HR (1) | HRP20191779T1 (enExample) |
| HU (1) | HUE046307T2 (enExample) |
| LT (1) | LT3248964T (enExample) |
| ME (1) | ME03570B (enExample) |
| MX (1) | MX2017009514A (enExample) |
| PL (1) | PL3248964T3 (enExample) |
| PT (1) | PT3248964T (enExample) |
| RS (1) | RS59388B1 (enExample) |
| SI (1) | SI3248964T1 (enExample) |
| SM (1) | SMT201900554T1 (enExample) |
| WO (1) | WO2016116652A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2676535B1 (es) * | 2017-01-20 | 2019-04-29 | Palobiofarma Sl | Moduladores de los receptores a3 de adenosina |
| KR102155406B1 (ko) | 2017-08-18 | 2020-09-11 | 주식회사 엘지화학 | 아연철산화물 내 잔류 Cl의 정량분석 방법 |
| US11458974B2 (en) * | 2019-07-08 | 2022-10-04 | Toyota Motor Engineering & Manufacturing North America, Inc. | Fleet-based average lane change and driver-specific behavior modelling for autonomous vehicle lane change operation |
| IT202300014340A1 (it) * | 2023-07-10 | 2025-01-10 | Consiglio Nazionale Ricerche | Trattamento di malattie associate alla disfunzione del gene ocrl. |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6436966B1 (en) * | 1997-10-27 | 2002-08-20 | Takeda Chemical Ind., Ltd. | Adenosine A3 receptor antagonists |
| US6303619B1 (en) | 1998-03-12 | 2001-10-16 | University Of Virginia | Meta-substituted acidic 8-phenylxanthine antagonists of A3 human adenosine receptors |
| US6686366B1 (en) | 1998-06-02 | 2004-02-03 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A3 receptor and uses thereof |
| AU4506399A (en) | 1998-06-05 | 1999-12-30 | Novartis Ag | Aryl pyridinyl thiazoles |
| ATE290910T1 (de) | 1998-07-16 | 2005-04-15 | Univ Pennsylvania | Verwendung von a3-adenosine antagonisten zur herstellung eines arzneimittels zur senkung des augeninnendrucks |
| US6448253B1 (en) | 1998-09-16 | 2002-09-10 | King Pharmaceuticals Research And Development, Inc. | Adenosine A3 receptor modulators |
| DE60033028T2 (de) | 1999-04-23 | 2007-11-15 | Takeda Pharmaceutical Co. Ltd. | 5-pyridyl-1,3-azol-derivate, verfahren zu ihrer herstellung und ihre verwendung |
| JP2003525291A (ja) | 2000-03-01 | 2003-08-26 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | ２，４−二置換チアゾリル誘導体 |
| US6673802B2 (en) | 2000-12-01 | 2004-01-06 | Osi Pharmaceuticals, Inc. | Compounds specific to adenosine A3 receptor and uses thereof |
| EP1390349B1 (en) | 2001-05-31 | 2012-07-25 | Sanofi | Aminoquinoline and aminopyridine derivatives and their use as adenosine a3 ligands |
| US20030020387A1 (en) | 2001-07-16 | 2003-01-30 | Wing Forrest F. | Refrigerator shelves with rolled hook for cantilever fastening |
| HUP0105406A3 (en) | 2001-12-21 | 2003-12-29 | Sanofi Aventis | Imidazo[1,2-a]quinolin derivatives, process for their preparation, pharmaceutical compositions thereof and intermediates |
| BRPI0412577A (pt) | 2003-07-31 | 2006-09-19 | Sanofi Aventis | derivados de aminoquinolina e seu uso como ligantes de adenosina a3 |
| TW200524887A (en) * | 2003-10-27 | 2005-08-01 | Lundbeck & Co As H | N-thiazol-2-yl-benzamide derivatives |
| JP4638355B2 (ja) | 2003-12-26 | 2011-02-23 | 協和発酵キリン株式会社 | チアゾール誘導体 |
| EP1983990B1 (en) | 2006-01-26 | 2011-03-23 | Government of the United States of America, Represented by the Secretary, Department of Health and Human Services | A3 adenosine receptor allosteric modulators |
| WO2007116106A1 (es) * | 2006-04-12 | 2007-10-18 | Palobiofarma, S.L. | Nuevos compuestos como antagonistas de los receptores a1 de adenosina |
| EP2054415A1 (en) | 2006-07-14 | 2009-05-06 | Santaris Pharma A/S | Adenosine receptor antagonists |
| JP2010505848A (ja) | 2006-10-06 | 2010-02-25 | ザ トラスティーズ オヴ ザ ユニヴァーシティー オヴ ペンシルバニア | 眼内圧を低下させるための種交差性ａ３アデノシン受容体アンタゴニストの効果的送達 |
| WO2008124000A2 (en) * | 2007-04-02 | 2008-10-16 | Ligand Pharmaceuticals Incorporated | Thiazole derivatives as androgen receptor modulator compounds |
| ES2331220B1 (es) | 2007-10-02 | 2010-09-23 | Palobiofarma, S.L. | Nuevos compuestos como antagonistas de los receptores a1 de adenosina. |
| WO2009052310A1 (en) | 2007-10-16 | 2009-04-23 | Cv Therapeutics, Inc | A3 adenosine receptor antagonists |
| US7973051B2 (en) | 2007-11-30 | 2011-07-05 | Hoffman-La Roche Inc. | Aminothiazoles as FBPase inhibitors for diabetes |
| WO2010009190A1 (en) | 2008-07-16 | 2010-01-21 | King Pharmaceuticals Research And Development, Inc. | Methods of treating atherosclerosis |
| EP2331542B1 (en) | 2008-08-01 | 2016-07-27 | The United States of America, as Represented by The Secretary, Department of Health and Human Services | A3 adenosine receptor antagonists and partial agonists |
| WO2011010306A1 (en) | 2009-07-21 | 2011-01-27 | Ramot At Tel-Aviv University Ltd. | A3 adenosine receptor ligands for modulation of pigmentation |
| WO2012030918A1 (en) | 2010-09-01 | 2012-03-08 | Ambit Biosciences Corporation | Adenosine a3 receptor modulating compounds and methods of use thereof |
-
2015
- 2015-01-22 ES ES201530085A patent/ES2578363B1/es active Active
-
2016
- 2016-01-22 CN CN201680006653.8A patent/CN107207445B/zh active Active
- 2016-01-22 RS RSP20191282 patent/RS59388B1/sr unknown
- 2016-01-22 ES ES16704680T patent/ES2750030T3/es active Active
- 2016-01-22 LT LTEP16704680.4T patent/LT3248964T/lt unknown
- 2016-01-22 ME MEP-2019-265A patent/ME03570B/me unknown
- 2016-01-22 BR BR112017015597-4A patent/BR112017015597B1/pt active IP Right Grant
- 2016-01-22 PT PT167046804T patent/PT3248964T/pt unknown
- 2016-01-22 EP EP16704680.4A patent/EP3248964B1/en active Active
- 2016-01-22 PL PL16704680T patent/PL3248964T3/pl unknown
- 2016-01-22 DK DK16704680.4T patent/DK3248964T3/da active
- 2016-01-22 MX MX2017009514A patent/MX2017009514A/es active IP Right Grant
- 2016-01-22 SI SI201630442T patent/SI3248964T1/sl unknown
- 2016-01-22 HR HRP20191779TT patent/HRP20191779T1/hr unknown
- 2016-01-22 HU HUE16704680A patent/HUE046307T2/hu unknown
- 2016-01-22 SM SM20190554T patent/SMT201900554T1/it unknown
- 2016-01-22 CA CA2974596A patent/CA2974596C/en active Active
- 2016-01-22 US US15/544,429 patent/US10238637B2/en active Active
- 2016-01-22 KR KR1020177023348A patent/KR102424575B1/ko active Active
- 2016-01-22 EA EA201791657A patent/EA031627B1/ru not_active IP Right Cessation
- 2016-01-22 AU AU2016210091A patent/AU2016210091B2/en active Active
- 2016-01-22 WO PCT/ES2016/070032 patent/WO2016116652A1/es not_active Ceased
- 2016-01-22 JP JP2017538582A patent/JP6637983B2/ja active Active
-
2019
- 2019-10-11 CY CY20191101070T patent/CY1122172T1/el unknown
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