JP2020522483A5 - - Google Patents
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- Publication number
- JP2020522483A5 JP2020522483A5 JP2019565826A JP2019565826A JP2020522483A5 JP 2020522483 A5 JP2020522483 A5 JP 2020522483A5 JP 2019565826 A JP2019565826 A JP 2019565826A JP 2019565826 A JP2019565826 A JP 2019565826A JP 2020522483 A5 JP2020522483 A5 JP 2020522483A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- acceptable salt
- group
- compound according
- 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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- 150000001875 compounds Chemical class 0.000 claims 32
- 150000003839 salts Chemical class 0.000 claims 27
- 125000000217 alkyl group Chemical group 0.000 claims 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 125000006648 (C1-C8) haloalkyl group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000001424 substituent group Chemical group 0.000 claims 5
- 201000009030 Carcinoma Diseases 0.000 claims 4
- 206010039491 Sarcoma Diseases 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 208000003200 Adenoma Diseases 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000001188 haloalkyl group Chemical group 0.000 claims 3
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 3
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 2
- 208000016323 C3 glomerulonephritis Diseases 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- 208000005777 Lupus Nephritis Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 201000004458 Myoma Diseases 0.000 claims 2
- 206010029379 Neutrophilia Diseases 0.000 claims 2
- 206010047115 Vasculitis Diseases 0.000 claims 2
- 208000009956 adenocarcinoma Diseases 0.000 claims 2
- 125000005218 alkyleneheteroaryl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000004438 haloalkoxy group Chemical group 0.000 claims 2
- 230000002949 hemolytic effect Effects 0.000 claims 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 201000008383 nephritis Diseases 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 208000003154 papilloma Diseases 0.000 claims 2
- 201000008171 proliferative glomerulonephritis Diseases 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 230000008359 toxicosis Effects 0.000 claims 2
- 230000002485 urinary effect Effects 0.000 claims 2
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 1
- XGWFJBFNAQHLEF-UHFFFAOYSA-N 9-anthroic acid Chemical compound C1=CC=C2C(C(=O)O)=C(C=CC=C3)C3=CC2=C1 XGWFJBFNAQHLEF-UHFFFAOYSA-N 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- 201000003076 Angiosarcoma Diseases 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 206010004146 Basal cell carcinoma Diseases 0.000 claims 1
- 206010006417 Bronchial carcinoma Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 201000005262 Chondroma Diseases 0.000 claims 1
- 208000005243 Chondrosarcoma Diseases 0.000 claims 1
- -1 Cyano, Hydroxy Chemical group 0.000 claims 1
- 201000005171 Cystadenoma Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 206010072579 Granulomatosis with polyangiitis Diseases 0.000 claims 1
- 206010018910 Haemolysis Diseases 0.000 claims 1
- 208000001258 Hemangiosarcoma Diseases 0.000 claims 1
- 208000010159 IgA glomerulonephritis Diseases 0.000 claims 1
- 206010021263 IgA nephropathy Diseases 0.000 claims 1
- 208000011200 Kawasaki disease Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025219 Lymphangioma Diseases 0.000 claims 1
- 208000004451 Membranoproliferative Glomerulonephritis Diseases 0.000 claims 1
- 208000015021 Meningeal Neoplasms Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000034541 Rare lymphatic malformation Diseases 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 201000010208 Seminoma Diseases 0.000 claims 1
- 206010052779 Transplant rejections Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 230000001363 autoimmune Effects 0.000 claims 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 1
- 208000003362 bronchogenic carcinoma Diseases 0.000 claims 1
- 125000002837 carbocyclic group Chemical group 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 230000034196 cell chemotaxis Effects 0.000 claims 1
- 208000026106 cerebrovascular disease Diseases 0.000 claims 1
- 210000004252 chorionic villi Anatomy 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 208000022401 dense deposit disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002526 effect on cardiovascular system Effects 0.000 claims 1
- 208000037828 epithelial carcinoma Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 206010016629 fibroma Diseases 0.000 claims 1
- 201000011066 hemangioma Diseases 0.000 claims 1
- 230000008588 hemolysis Effects 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000000265 leukocyte Anatomy 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 206010025135 lupus erythematosus Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 206010063344 microscopic polyangiitis Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 208000001725 mucocutaneous lymph node syndrome Diseases 0.000 claims 1
- 230000001613 neoplastic effect Effects 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 208000008798 osteoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 201000010198 papillary carcinoma Diseases 0.000 claims 1
- 230000001575 pathological effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000008753 synovium neoplasm Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 206010043554 thrombocytopenia Diseases 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 210000005239 tubule Anatomy 0.000 claims 1
- 208000013706 tumor of meninges Diseases 0.000 claims 1
- CERZCKSQHFDGBL-UHFFFAOYSA-N CC(C)Cc1c(C(F)(F)F)cc(C(F)(F)F)cc1 Chemical compound CC(C)Cc1c(C(F)(F)F)cc(C(F)(F)F)cc1 CERZCKSQHFDGBL-UHFFFAOYSA-N 0.000 description 1
- OYLQSCVLGSXASI-UHFFFAOYSA-N CC(C)Cc1c(C(F)(F)F)cccc1 Chemical compound CC(C)Cc1c(C(F)(F)F)cccc1 OYLQSCVLGSXASI-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762513025P | 2017-05-31 | 2017-05-31 | |
| US62/513,025 | 2017-05-31 | ||
| PCT/US2018/034908 WO2018222601A1 (en) | 2017-05-31 | 2018-05-29 | 5-5 FUSED RINGS AS C5a INHIBITORS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020522483A JP2020522483A (ja) | 2020-07-30 |
| JP2020522483A5 true JP2020522483A5 (enExample) | 2021-07-26 |
| JP7141129B2 JP7141129B2 (ja) | 2022-09-22 |
Family
ID=64455572
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019565826A Active JP7141129B2 (ja) | 2017-05-31 | 2018-05-29 | Ｃ５ａ阻害剤としての５－５融合環 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US10683294B2 (enExample) |
| EP (1) | EP3630774B1 (enExample) |
| JP (1) | JP7141129B2 (enExample) |
| KR (1) | KR102586710B1 (enExample) |
| CN (1) | CN111032658B (enExample) |
| AR (1) | AR111841A1 (enExample) |
| AU (1) | AU2018277523B2 (enExample) |
| CA (1) | CA3064025A1 (enExample) |
| ES (1) | ES2934507T3 (enExample) |
| IL (1) | IL270842B2 (enExample) |
| MA (1) | MA48800A (enExample) |
| MX (1) | MX391392B (enExample) |
| TW (1) | TWI813570B (enExample) |
| WO (1) | WO2018222601A1 (enExample) |
| ZA (1) | ZA201907755B (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111032658B (zh) | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的5-5稠合环类 |
| JP7141130B2 (ja) | 2017-05-31 | 2022-09-22 | ケモセントリックス，インコーポレイティド | Ｃ５ａ阻害剤としての６－５融合環 |
| MA51331A (fr) | 2017-12-22 | 2020-10-28 | Chemocentryx Inc | COMPOSÉS CYCLIQUES CONDENSÉS 6,5 À SUBSTITUTION DIARYLE, UTILISÉS EN TANT QU'INHIBITEURS DU C5aR |
| SG11202005799XA (en) | 2017-12-22 | 2020-07-29 | Chemocentryx Inc | DIARYL SUBSTITUTED 5,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS |
| BR112020019822A2 (pt) * | 2018-04-02 | 2021-03-16 | Chemocentryx, Inc. | Profármacos de antagonistas bicíclicos fundidos de c5ar |
| KR102890201B1 (ko) | 2019-07-10 | 2025-11-24 | 케모센트릭스, 인크. | Pd-l1 억제제로서의 인단 |
| CN112300169B (zh) * | 2019-07-26 | 2022-03-04 | 上海美迪西生物医药股份有限公司 | 吡咯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| EP4045036A4 (en) | 2019-10-16 | 2023-11-15 | ChemoCentryx, Inc. | Heteroaryl-biphenyl amides for the treatment of pd-l1 diseases |
| CR20220216A (es) | 2019-10-16 | 2023-01-09 | Chemocentryx Inc | Aminas de heteroaril-bifenilo para el tratamiento de enfermedades pd-l1 |
| JP2023542789A (ja) * | 2020-09-28 | 2023-10-12 | シチュアン ケルン－バイオテック バイオファーマシューティカル カンパニー リミテッド | ピラゾール化合物並びにその調製方法及び使用 |
| JP2023548117A (ja) | 2020-10-28 | 2023-11-15 | ケモセントリックス， インコーポレイテッド | 化膿性汗腺炎を処置する方法 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001287654B2 (en) | 2000-08-10 | 2006-12-14 | Pfizer Italia S.R.I. | Bicyclo-pyrazoles active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| CN1454086A (zh) | 2000-09-29 | 2003-11-05 | 神经能质公司 | 高亲和性小分子C5a受体调节物 |
| SE524438C2 (sv) | 2000-10-05 | 2004-08-10 | Magnus Georg Goertz | Fjärrstyrt dörrelaterat låsarrangemang, första och andra datorpogramprodukt, bärande medium och ett datorlösbart medium |
| EP1396493A4 (en) | 2001-04-26 | 2005-08-03 | Ajinomoto Kk | HETEROCYCLIC COMPOUNDS |
| ITMI20012025A1 (it) | 2001-09-28 | 2003-03-28 | Dompe Spa | Sali di ammonio quaternari di omega-amminoalchilammidi di acidi r 2-aril-propionici e composizioni farmaceutiche che li contengono |
| JP2006508894A (ja) | 2002-03-28 | 2006-03-16 | ニューロジェン・コーポレーション | Ｃ５ａ受容体調節因子としての置換テトラヒドロイソキノリン |
| EP1487796A4 (en) | 2002-03-28 | 2005-11-16 | Neurogen Corp | SUBSTITUTED BIARYLAMIDES AS MODULATORS OF THE C5A RECEPTOR |
| CA2480082A1 (en) | 2002-03-29 | 2003-10-16 | Neurogen Corporation | Combination therapy for the treatment of conditions with pathogenic inflammatory components |
| WO2004016592A1 (en) | 2002-08-14 | 2004-02-26 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
| US7169775B2 (en) | 2002-08-21 | 2007-01-30 | Neurogen Corporation | Amino methyl imidazoles as C5a receptor modulators |
| AU2003291403A1 (en) | 2002-11-08 | 2004-06-03 | Neurogen Corporation | 3-substituted-6-aryl pyridined as ligands of c5a receptors |
| US7145012B2 (en) | 2003-04-23 | 2006-12-05 | Pfizer Inc. | Cannabinoid receptor ligands and uses thereof |
| US20040214856A1 (en) | 2003-04-23 | 2004-10-28 | Pfizer Inc | Cannabinoid receptor ligands and uses thereof |
| AU2003902354A0 (en) | 2003-05-15 | 2003-05-29 | Harkin, Denis W. | Treatment of haemorrhagic shock |
| WO2005007087A2 (en) | 2003-07-03 | 2005-01-27 | Neurogen Corporation | Substituted (heterocycloalkyl)methyl azole derivatives as c5a receptor modulators |
| US7906528B2 (en) * | 2004-10-05 | 2011-03-15 | Novartis International Pharmaceutical Ltd. | Pyrrolo-pyridine, pyrrolo-pyrimidine and related heterocyclic compounds |
| US7598255B2 (en) | 2005-08-04 | 2009-10-06 | Janssen Pharmaceutica Nv | Pyrimidine compounds as serotonin receptor modulators |
| US20070112015A1 (en) * | 2005-10-28 | 2007-05-17 | Chemocentryx, Inc. | Substituted dihydropyridines and methods of use |
| KR20110031475A (ko) | 2008-06-20 | 2011-03-28 | 제넨테크, 인크. | 트리아졸로피리딘 ｊａｋ 억제제 화합물 및 방법 |
| US20110275639A1 (en) | 2008-12-22 | 2011-11-10 | Chemocentryx, Inc. | C5aR ANTAGONISTS |
| EP3508477B1 (en) | 2008-12-22 | 2021-11-10 | ChemoCentryx, Inc. | C5ar antagonists |
| DK2585064T3 (en) | 2010-06-24 | 2017-07-24 | Chemocentryx Inc | C5aR antagonists |
| US8846656B2 (en) | 2011-07-22 | 2014-09-30 | Novartis Ag | Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators |
| KR20150042271A (ko) | 2012-08-16 | 2015-04-20 | 얀센 파마슈티카 엔.브이. | N형 칼슘 채널 차단제로서의 치환된 피롤로피라졸 |
| CN103421006B (zh) | 2013-08-18 | 2016-06-22 | 上海师范大学 | 2,3,5,7-四取代二氢吡唑并六氢吡啶衍生物及其制备方法和应用 |
| GB201321746D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| WO2017176620A2 (en) | 2016-04-04 | 2017-10-12 | Chemocentryx, Inc. | SOLUBLE C5aR ANTAGONISTS |
| JP7141130B2 (ja) | 2017-05-31 | 2022-09-22 | ケモセントリックス，インコーポレイティド | Ｃ５ａ阻害剤としての６－５融合環 |
| CN111032658B (zh) | 2017-05-31 | 2022-12-20 | 凯莫森特里克斯股份有限公司 | 作为C5a抑制剂的5-5稠合环类 |
| SG11202005799XA (en) | 2017-12-22 | 2020-07-29 | Chemocentryx Inc | DIARYL SUBSTITUTED 5,5-FUSED RING COMPOUNDS AS C5aR INHIBITORS |
| MA51331A (fr) | 2017-12-22 | 2020-10-28 | Chemocentryx Inc | COMPOSÉS CYCLIQUES CONDENSÉS 6,5 À SUBSTITUTION DIARYLE, UTILISÉS EN TANT QU'INHIBITEURS DU C5aR |
| BR112020019822A2 (pt) | 2018-04-02 | 2021-03-16 | Chemocentryx, Inc. | Profármacos de antagonistas bicíclicos fundidos de c5ar |
-
2018
- 2018-05-29 CN CN201880036650.8A patent/CN111032658B/zh active Active
- 2018-05-29 WO PCT/US2018/034908 patent/WO2018222601A1/en not_active Ceased
- 2018-05-29 MX MX2019014292A patent/MX391392B/es unknown
- 2018-05-29 ES ES18809125T patent/ES2934507T3/es active Active
- 2018-05-29 MA MA048800A patent/MA48800A/fr unknown
- 2018-05-29 KR KR1020197038670A patent/KR102586710B1/ko active Active
- 2018-05-29 CA CA3064025A patent/CA3064025A1/en active Pending
- 2018-05-29 JP JP2019565826A patent/JP7141129B2/ja active Active
- 2018-05-29 US US15/991,747 patent/US10683294B2/en active Active
- 2018-05-29 EP EP18809125.0A patent/EP3630774B1/en active Active
- 2018-05-29 AU AU2018277523A patent/AU2018277523B2/en active Active
- 2018-05-31 AR ARP180101445A patent/AR111841A1/es unknown
- 2018-05-31 TW TW107118603A patent/TWI813570B/zh active
-
2019
- 2019-11-21 IL IL270842A patent/IL270842B2/en unknown
- 2019-11-22 ZA ZA2019/07755A patent/ZA201907755B/en unknown
-
2020
- 2020-05-04 US US16/865,648 patent/US11479553B2/en active Active
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