JPWO2022223805A5 - - Google Patents
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- Publication number
- JPWO2022223805A5 JPWO2022223805A5 JP2023565327A JP2023565327A JPWO2022223805A5 JP WO2022223805 A5 JPWO2022223805 A5 JP WO2022223805A5 JP 2023565327 A JP2023565327 A JP 2023565327A JP 2023565327 A JP2023565327 A JP 2023565327A JP WO2022223805 A5 JPWO2022223805 A5 JP WO2022223805A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- alkyl
- propanamido
- acetamido
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims 12
- 230000003287 optical effect Effects 0.000 claims 12
- 239000000651 prodrug Substances 0.000 claims 12
- 229940002612 prodrug Drugs 0.000 claims 12
- 150000003839 salts Chemical class 0.000 claims 12
- 239000012453 solvate Substances 0.000 claims 12
- 150000001204 N-oxides Chemical class 0.000 claims 11
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 7
- WWZKQHOCKIZLMA-UHFFFAOYSA-N Caprylic acid Natural products CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 claims 5
- 206010011878 Deafness Diseases 0.000 claims 5
- GONOPSZTUGRENK-UHFFFAOYSA-N benzyl(trichloro)silane Chemical compound Cl[Si](Cl)(Cl)CC1=CC=CC=C1 GONOPSZTUGRENK-UHFFFAOYSA-N 0.000 claims 5
- 230000010370 hearing loss Effects 0.000 claims 5
- 231100000888 hearing loss Toxicity 0.000 claims 5
- 208000016354 hearing loss disease Diseases 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- FUZZWVXGSFPDMH-UHFFFAOYSA-N n-hexanoic acid Natural products CCCCCC(O)=O FUZZWVXGSFPDMH-UHFFFAOYSA-N 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000001475 halogen functional group Chemical group 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 2
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 2
- 125000006655 (C3-C8) heteroaryl group Chemical group 0.000 claims 2
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 2
- CEGGNTZMXNFHEO-JTQLQIEISA-N CC(C)(C)CC[C@@H](C(O)=O)NC(CNC(C1=NC=CN=C1)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC(CNC(C1=NC=CN=C1)=O)=O CEGGNTZMXNFHEO-JTQLQIEISA-N 0.000 claims 2
- APZSCTWKLHQKTJ-HOTGVXAUSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=CC=C1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=CC=C1)NC(C)=O)=O APZSCTWKLHQKTJ-HOTGVXAUSA-N 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical group C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- IPWFJLQDVFKJDU-UHFFFAOYSA-N pentanamide Chemical compound CCCCC(N)=O IPWFJLQDVFKJDU-UHFFFAOYSA-N 0.000 claims 2
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 claims 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006583 (C1-C3) haloalkyl group Chemical group 0.000 claims 1
- -1 -OH Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 1
- IQSWQCFHCXFPCR-VIFPVBQESA-N CC(C)(C)CC[C@@H](C(O)=O)NC(CNC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC(CNC(C)=O)=O IQSWQCFHCXFPCR-VIFPVBQESA-N 0.000 claims 1
- GSBCZCUNGGVJCP-ZWKOTPCHSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@@H](CC1=CNC2=CC=CC=C12)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@@H](CC1=CNC2=CC=CC=C12)NC(C)=O)=O GSBCZCUNGGVJCP-ZWKOTPCHSA-N 0.000 claims 1
- UQMKOIQMCJWAPA-HOTGVXAUSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC(C=C1)=CC=C1F)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC(C=C1)=CC=C1F)NC(C)=O)=O UQMKOIQMCJWAPA-HOTGVXAUSA-N 0.000 claims 1
- UVCZNZMAQFQZGW-HOTGVXAUSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC(F)=CC(F)=C1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC(F)=CC(F)=C1)NC(C)=O)=O UVCZNZMAQFQZGW-HOTGVXAUSA-N 0.000 claims 1
- LTDXNWRWDPMOAR-IRXDYDNUSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=CC=C1)NC(C1=NC=CN=C1)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=CC=C1)NC(C1=NC=CN=C1)=O)=O LTDXNWRWDPMOAR-IRXDYDNUSA-N 0.000 claims 1
- MHKNSUPVBDRZBV-GJZGRUSLSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=CN=C1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=CN=C1)NC(C)=O)=O MHKNSUPVBDRZBV-GJZGRUSLSA-N 0.000 claims 1
- CBONMSATJGWZRV-GJZGRUSLSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=NC=C1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CC=NC=C1)NC(C)=O)=O CBONMSATJGWZRV-GJZGRUSLSA-N 0.000 claims 1
- MUOFLSOVWGTRTM-HOTGVXAUSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C(C)=N1)N(C)C(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C(C)=N1)N(C)C(C)=O)=O MUOFLSOVWGTRTM-HOTGVXAUSA-N 0.000 claims 1
- PEXQVNTWOQNBMN-ROUUACIJSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C2=CC=CC=C12)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C2=CC=CC=C12)NC(C)=O)=O PEXQVNTWOQNBMN-ROUUACIJSA-N 0.000 claims 1
- AVKASUVLEMUHGO-GJZGRUSLSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C=N1)N(C)C(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C=N1)N(C)C(C)=O)=O AVKASUVLEMUHGO-GJZGRUSLSA-N 0.000 claims 1
- JBHCDTGGZYWMFF-GJZGRUSLSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C=N1)N(CCC1)C1=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C=N1)N(CCC1)C1=O)=O JBHCDTGGZYWMFF-GJZGRUSLSA-N 0.000 claims 1
- WDGLEYISFNGFSP-KBPBESRZSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C=N1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN(C)C=N1)NC(C)=O)=O WDGLEYISFNGFSP-KBPBESRZSA-N 0.000 claims 1
- RBGCPEFBISJKBF-GJZGRUSLSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN=CN1C)N(C)C(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN=CN1C)N(C)C(C)=O)=O RBGCPEFBISJKBF-GJZGRUSLSA-N 0.000 claims 1
- YKNUOZDAHUREFB-KBPBESRZSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN=CN1C)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CN=CN1C)NC(C)=O)=O YKNUOZDAHUREFB-KBPBESRZSA-N 0.000 claims 1
- GSBCZCUNGGVJCP-ROUUACIJSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CNC2=CC=CC=C12)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CNC2=CC=CC=C12)NC(C)=O)=O GSBCZCUNGGVJCP-ROUUACIJSA-N 0.000 claims 1
- KNDLNTBZYQQJIB-KBPBESRZSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CSC=C1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CSC=C1)NC(C)=O)=O KNDLNTBZYQQJIB-KBPBESRZSA-N 0.000 claims 1
- JCEDJOPAKAVBEM-STQMWFEESA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CSC=N1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=CSC=N1)NC(C)=O)=O JCEDJOPAKAVBEM-STQMWFEESA-N 0.000 claims 1
- WNKVGLUDNFZKGZ-GJZGRUSLSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=NC=CC=C1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CC1=NC=CC=C1)NC(C)=O)=O WNKVGLUDNFZKGZ-GJZGRUSLSA-N 0.000 claims 1
- YTBGDPAKQZCDOC-KBPBESRZSA-N CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CN1CCOCC1)NC(C)=O)=O Chemical compound CC(C)(C)CC[C@@H](C(O)=O)NC([C@H](CN1CCOCC1)NC(C)=O)=O YTBGDPAKQZCDOC-KBPBESRZSA-N 0.000 claims 1
- OBLBJDXCEJCGAA-DRZSPHRISA-N CC[C@H](C)[C@@H](C(N[C@@H](CCC(C)(C)C)C(O)=O)=O)NC(C)=O Chemical compound CC[C@H](C)[C@@H](C(N[C@@H](CCC(C)(C)C)C(O)=O)=O)NC(C)=O OBLBJDXCEJCGAA-DRZSPHRISA-N 0.000 claims 1
- NRBUSESFBQIFPI-WPRPVWTQSA-N C[C@@H](C(N[C@@H](CCC(C)(C)C)C(O)=O)=O)NC(C)=O Chemical compound C[C@@H](C(N[C@@H](CCC(C)(C)C)C(O)=O)=O)NC(C)=O NRBUSESFBQIFPI-WPRPVWTQSA-N 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 206010011903 Deafness traumatic Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- 208000010412 Glaucoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 claims 1
- 208000002946 Noise-Induced Hearing Loss Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Chemical group C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010061373 Sudden Hearing Loss Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000003959 neuroinflammation Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- QLNJFJADRCOGBJ-UHFFFAOYSA-N propionamide Chemical compound CCC(N)=O QLNJFJADRCOGBJ-UHFFFAOYSA-N 0.000 claims 1
- 208000020431 spinal cord injury Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 231100000331 toxic Toxicity 0.000 claims 1
- 230000002588 toxic effect Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP21170274.1 | 2021-04-23 | ||
| EP21170274.1A EP4079748A1 (en) | 2021-04-23 | 2021-04-23 | Modulators of sortilin activity |
| PCT/EP2022/060742 WO2022223805A1 (en) | 2021-04-23 | 2022-04-22 | Modulators of sortilin activity |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024517678A JP2024517678A (ja) | 2024-04-23 |
| JP2024517678A5 JP2024517678A5 (https=) | 2025-04-21 |
| JPWO2022223805A5 true JPWO2022223805A5 (https=) | 2025-04-21 |
Family
ID=75674611
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023565327A Pending JP2024517678A (ja) | 2021-04-23 | 2022-04-22 | ソルチリン活性の修飾物質 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20240217922A1 (https=) |
| EP (2) | EP4079748A1 (https=) |
| JP (1) | JP2024517678A (https=) |
| KR (1) | KR20240000510A (https=) |
| CN (1) | CN117677627A (https=) |
| AU (1) | AU2022260554A1 (https=) |
| CA (1) | CA3215848A1 (https=) |
| WO (1) | WO2022223805A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4471047A1 (en) * | 2023-05-31 | 2024-12-04 | Insusense ApS | Modulators of sortilin activity |
| EP4361165A1 (en) * | 2022-10-24 | 2024-05-01 | Insusense ApS | Modulators of sortilin activity |
| CN116143648A (zh) * | 2022-12-05 | 2023-05-23 | 河北远大九孚生物科技有限公司 | 一种n-乙酰-l-苯丙氨酸的合成方法 |
| EP4428124A1 (en) * | 2023-03-07 | 2024-09-11 | Vesper Bio Aps | Modulators of sortilin activity |
| EP4428121A1 (en) * | 2023-03-07 | 2024-09-11 | Vesper Bio Aps | Modulators of sortilin activity |
| EP4719366A1 (en) | 2023-05-26 | 2026-04-08 | Bertram Wiedenmann | Sortilin inhibitors for treatment of patients with functional neuroendocrine tumors |
| TW202600557A (zh) * | 2024-02-20 | 2026-01-01 | 日商大塚製藥股份有限公司 | 作為sort1抑制劑之哌啶-及嗎啉-羧酸鹽化合物 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DD262583A5 (de) * | 1986-10-31 | 1988-12-07 | Pfizer Inc.,Us | Verfahren zur herstellung von nor-statin- und nor-cyclostatin-polypeptiden |
| DE3842067A1 (de) * | 1988-12-14 | 1990-06-21 | Hoechst Ag | Enzym-hemmende aminosaeurederivate, verfahren zu ihrer herstellung, diese enthaltende mittel und ihre verwendung |
| JPH05345754A (ja) * | 1992-06-15 | 1993-12-27 | Suntory Ltd | ジペプチド誘導体およびそれを有効成分とする骨疾患の予防または治療剤 |
| DE19546532C2 (de) * | 1995-12-13 | 2000-04-20 | Degussa | Verfahren zur Gewinnung von optisch aktiven L-alpha-Aminocarbonsäuren aus entsprechenden racemischen D,L-alpha-Aminocarbonsäuren |
| WO2004037159A2 (en) * | 2002-10-23 | 2004-05-06 | Obetherapy Biotechnology | Compounds, compositions and methods for modulating fat metabolism |
| WO2006050861A2 (en) * | 2004-11-10 | 2006-05-18 | Boehringer Ingelheim International Gmbh | Statine derivatives for the treatment of alzheimer's disease |
| CA2617294A1 (en) * | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Substituted ethane-1,2-diamines for the treatment of alzheimer's disease ii |
| PT3309157T (pt) | 2009-05-13 | 2019-12-02 | Gilead Pharmasset Llc | Compostos antivirais |
| GB201011411D0 (en) * | 2010-07-06 | 2010-08-18 | St Georges Hosp Medical School | Therapeutic compounds and their use |
| CN104955456B (zh) * | 2013-01-28 | 2018-07-03 | H.隆德贝克有限公司 | 作为分拣蛋白抑制剂的n-取代的-5-取代的邻氨甲酰苯甲酸 |
| WO2015131100A1 (en) | 2014-02-28 | 2015-09-03 | The Scripps Research Institute | Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids |
| US20160331746A1 (en) | 2015-05-12 | 2016-11-17 | University Of South Florida | Sortilin-Binding Small Molecules for Increasing Glucose Uptake |
-
2021
- 2021-04-23 EP EP21170274.1A patent/EP4079748A1/en not_active Withdrawn
-
2022
- 2022-04-22 CN CN202280030307.9A patent/CN117677627A/zh active Pending
- 2022-04-22 KR KR1020237037613A patent/KR20240000510A/ko active Pending
- 2022-04-22 EP EP22724745.9A patent/EP4326742A1/en active Pending
- 2022-04-22 US US18/556,406 patent/US20240217922A1/en active Pending
- 2022-04-22 AU AU2022260554A patent/AU2022260554A1/en not_active Abandoned
- 2022-04-22 CA CA3215848A patent/CA3215848A1/en active Pending
- 2022-04-22 JP JP2023565327A patent/JP2024517678A/ja active Pending
- 2022-04-22 WO PCT/EP2022/060742 patent/WO2022223805A1/en not_active Ceased
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