CN104837821B - 作为谷氨酰胺转移酶的抑制剂的酰基哌嗪类及其在药物中的用途 - Google Patents
作为谷氨酰胺转移酶的抑制剂的酰基哌嗪类及其在药物中的用途 Download PDFInfo
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- CN104837821B CN104837821B CN201380052683.9A CN201380052683A CN104837821B CN 104837821 B CN104837821 B CN 104837821B CN 201380052683 A CN201380052683 A CN 201380052683A CN 104837821 B CN104837821 B CN 104837821B
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- 0 CC1CC(CC2C*CC2)(CC2C3)CC2C3C1 Chemical compound CC1CC(CC2C*CC2)(CC2C3)CC2C3C1 0.000 description 7
- QXZJSDFORNSPNW-UHFFFAOYSA-N C=CS(NCC(N(CC1)CCN1C(OCc1ccccc1)=O)=O)(=O)=O Chemical compound C=CS(NCC(N(CC1)CCN1C(OCc1ccccc1)=O)=O)(=O)=O QXZJSDFORNSPNW-UHFFFAOYSA-N 0.000 description 1
- ILJKDNBADMIJDG-UHFFFAOYSA-N CC(C)(C)OC(NCC(N(CC1)CCN1C(OCc1ccccc1)=O)=O)=O Chemical compound CC(C)(C)OC(NCC(N(CC1)CCN1C(OCc1ccccc1)=O)=O)=O ILJKDNBADMIJDG-UHFFFAOYSA-N 0.000 description 1
- KKPLUMCFGZQHKW-UHFFFAOYSA-N CCC1(CCOC(N(CC2)CCN2C(CNC(CBr)=O)=O)=O)CC(CCC2)CC2C1 Chemical compound CCC1(CCOC(N(CC2)CCN2C(CNC(CBr)=O)=O)=O)CC(CCC2)CC2C1 KKPLUMCFGZQHKW-UHFFFAOYSA-N 0.000 description 1
- ZIMVKXWFGJIILY-UHFFFAOYSA-N CCSc1[n+](C)c(C)c(C)[n]1C Chemical compound CCSc1[n+](C)c(C)c(C)[n]1C ZIMVKXWFGJIILY-UHFFFAOYSA-N 0.000 description 1
- AKDZQWVPFDRSPE-AWEZNQCLSA-N C[C@@H](C(N(CC1)CCN1C(OCCc1ccccc1)=O)=O)NC(CBr)=O Chemical compound C[C@@H](C(N(CC1)CCN1C(OCCc1ccccc1)=O)=O)NC(CBr)=O AKDZQWVPFDRSPE-AWEZNQCLSA-N 0.000 description 1
- DHKWTIUSYGCKGG-IBGZPJMESA-N N[C@@H](Cc1ccccc1)C(N(CC1)CCN1C(OCc1ccccc1)=O)=O Chemical compound N[C@@H](Cc1ccccc1)C(N(CC1)CCN1C(OCc1ccccc1)=O)=O DHKWTIUSYGCKGG-IBGZPJMESA-N 0.000 description 1
- ZSWUPAWQGAUGGX-UHFFFAOYSA-N OC(C1(C2C(C3)C4)C2C3CC4C1)N(CC1)CCN1C(CNC(CBr)=O)=O Chemical compound OC(C1(C2C(C3)C4)C2C3CC4C1)N(CC1)CCN1C(CNC(CBr)=O)=O ZSWUPAWQGAUGGX-UHFFFAOYSA-N 0.000 description 1
- KSOJGWOMZGWJHF-UHFFFAOYSA-N [O-][N+](c(cc1)ccc1OC(OCc1cc(cccc2)c2cc1)=O)=O Chemical compound [O-][N+](c(cc1)ccc1OC(OCc1cc(cccc2)c2cc1)=O)=O KSOJGWOMZGWJHF-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D233/84—Sulfur atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
- C07D295/26—Sulfur atoms
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
- C07D295/185—Radicals derived from carboxylic acids from aliphatic carboxylic acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/20—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
- C07D295/205—Radicals derived from carbonic acid
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Immunology (AREA)
- Psychology (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Communicable Diseases (AREA)
- Diabetes (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hematology (AREA)
- AIDS & HIV (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1218084.0A GB201218084D0 (en) | 2012-10-09 | 2012-10-09 | Novel compounds and methods for use in medicine |
| GB1218084.0 | 2012-10-09 | ||
| PCT/GB2013/052631 WO2014057266A1 (en) | 2012-10-09 | 2013-10-09 | Acylpiperazines as inhibitors of transglutaminase and their use in medicine |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN104837821A CN104837821A (zh) | 2015-08-12 |
| CN104837821B true CN104837821B (zh) | 2018-11-13 |
Family
ID=47294510
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380052683.9A Active CN104837821B (zh) | 2012-10-09 | 2013-10-09 | 作为谷氨酰胺转移酶的抑制剂的酰基哌嗪类及其在药物中的用途 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9656978B2 (enExample) |
| EP (1) | EP2906543B1 (enExample) |
| JP (1) | JP6138950B2 (enExample) |
| CN (1) | CN104837821B (enExample) |
| GB (1) | GB201218084D0 (enExample) |
| WO (1) | WO2014057266A1 (enExample) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201218084D0 (en) | 2012-10-09 | 2012-11-21 | Univ Aston | Novel compounds and methods for use in medicine |
| EP3607948A1 (en) | 2018-08-07 | 2020-02-12 | Aarhus Universitet | Tissue transglutaminase modulators for medicinal use |
| WO2022213198A1 (en) * | 2021-04-08 | 2022-10-13 | University Of Ottawa | Arylacetyl inhibitors of tg2 and uses thereof |
| WO2023135425A1 (en) * | 2022-01-13 | 2023-07-20 | Aston University | Inhibitors of transglutaminase |
| GB202310246D0 (en) | 2023-07-04 | 2023-08-16 | Univ Aston | New compounds |
| GB202310233D0 (en) | 2023-07-04 | 2023-08-16 | Univ Aston | New compounds |
| WO2025153465A1 (en) | 2024-01-15 | 2025-07-24 | UCB Biopharma SRL | Method for the treatment of fibrotic-related disorder associated to ibd |
Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0411909A1 (en) * | 1989-07-31 | 1991-02-06 | Merck & Co. Inc. | Imidazole compounds and their use as transglutaminase inhibitors |
| WO1996030378A1 (en) * | 1995-03-31 | 1996-10-03 | Nippon Chemiphar Co., Ltd. | Bisphosphonic acid derivatives |
| EP0771565A2 (en) * | 1995-10-25 | 1997-05-07 | Senju Pharmaceutical Co., Ltd. | Angiogenesis inhibitor |
| US5721365A (en) * | 1989-09-15 | 1998-02-24 | Us Health | N-substituted piperazine NONOates |
| EP0838460A1 (en) * | 1995-07-13 | 1998-04-29 | Senju Pharmaceutical Co., Ltd. | Piperazine derivatives and use of the same |
| US6030946A (en) * | 1995-06-07 | 2000-02-29 | Axys Pharmaceuticals, Inc. | Reversible cysteine protease inhibitors |
| WO2001007440A1 (en) * | 1999-07-21 | 2001-02-01 | Boehringer Ingelheim Pharmaceuticals, Inc. | Imidazoimidazoles and triazoles as anti-inflammatory agents |
| CN1293666A (zh) * | 1998-03-17 | 2001-05-02 | 阿斯特拉曾尼卡有限公司 | 苯硫酰胺衍生物及其作为药物的用途 |
| WO2004089470A2 (en) * | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | New amide derivatives and pharmaceutical use thereof |
| WO2013022550A2 (en) * | 2011-08-10 | 2013-02-14 | President And Fellows Of Harvard College | Small molecule inhibitors of ebola and lassa fever viruses |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2628199B2 (ja) | 1988-09-26 | 1997-07-09 | 富士薬品工業株式会社 | 新規なアシルアミノ酸およびアシルペプチド化合物 |
| US6861424B2 (en) * | 2001-06-06 | 2005-03-01 | Schering Aktiengesellschaft | Platelet adenosine diphosphate receptor antagonists |
| EP2607362B1 (en) * | 2005-02-17 | 2014-12-31 | Astellas Pharma Inc. | Piperidine and piperazine carboxylates as FAAH inhibitors |
| CA2709784A1 (en) * | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| WO2010075356A1 (en) * | 2008-12-23 | 2010-07-01 | Forest Laboratories Holdings Limited | Novel piperazine derivatives as inhibitors of stearoyl-coa desaturase |
| GB201218084D0 (en) | 2012-10-09 | 2012-11-21 | Univ Aston | Novel compounds and methods for use in medicine |
-
2012
- 2012-10-09 GB GBGB1218084.0A patent/GB201218084D0/en not_active Ceased
-
2013
- 2013-10-09 JP JP2015536220A patent/JP6138950B2/ja active Active
- 2013-10-09 WO PCT/GB2013/052631 patent/WO2014057266A1/en not_active Ceased
- 2013-10-09 EP EP13802694.3A patent/EP2906543B1/en active Active
- 2013-10-09 US US14/431,472 patent/US9656978B2/en active Active
- 2013-10-09 CN CN201380052683.9A patent/CN104837821B/zh active Active
Patent Citations (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0411909A1 (en) * | 1989-07-31 | 1991-02-06 | Merck & Co. Inc. | Imidazole compounds and their use as transglutaminase inhibitors |
| US5721365A (en) * | 1989-09-15 | 1998-02-24 | Us Health | N-substituted piperazine NONOates |
| WO1996030378A1 (en) * | 1995-03-31 | 1996-10-03 | Nippon Chemiphar Co., Ltd. | Bisphosphonic acid derivatives |
| US6030946A (en) * | 1995-06-07 | 2000-02-29 | Axys Pharmaceuticals, Inc. | Reversible cysteine protease inhibitors |
| EP0838460A1 (en) * | 1995-07-13 | 1998-04-29 | Senju Pharmaceutical Co., Ltd. | Piperazine derivatives and use of the same |
| EP0771565A2 (en) * | 1995-10-25 | 1997-05-07 | Senju Pharmaceutical Co., Ltd. | Angiogenesis inhibitor |
| CN1293666A (zh) * | 1998-03-17 | 2001-05-02 | 阿斯特拉曾尼卡有限公司 | 苯硫酰胺衍生物及其作为药物的用途 |
| WO2001007440A1 (en) * | 1999-07-21 | 2001-02-01 | Boehringer Ingelheim Pharmaceuticals, Inc. | Imidazoimidazoles and triazoles as anti-inflammatory agents |
| WO2004089470A2 (en) * | 2003-04-11 | 2004-10-21 | Novo Nordisk A/S | New amide derivatives and pharmaceutical use thereof |
| WO2013022550A2 (en) * | 2011-08-10 | 2013-02-14 | President And Fellows Of Harvard College | Small molecule inhibitors of ebola and lassa fever viruses |
Non-Patent Citations (6)
| Title |
|---|
| CAS号: 1371000-53-1,1321660-27-8,1276484-50-4,1214799-76-4,338734-10-4,338733-99-6,337508-08-4;Chemical Abstracts Service;《Database Registry》;20120429;第5-8页 * |
| Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group;Takashi Kondo等;《Bioorganic & Medicinal Chemistry》;20071117;第16卷;第1613-1631页 * |
| PubChem CID: 3291454,3254510,55477654,42658068,42658077,51135247,5252414,52522415;Compound;《Database Pubchem》;20120125;全文 * |
| Structure-Activity Relationship Analysis of the Selective Inhibition of Transglutaminase 2 by Dihydroisoxazoles;R.Edward Watts等;《Journal of Medicinal Chemistry》;20061110;第49卷(第25期);第7493-7501页 * |
| Transglutaminase 2 inhibitors and their therapeutic role in disease states;Matthew Siegel等;《Pharmacology & Therapeutics》;20070513;第115卷(第2期);第232-245页 * |
| 组织型谷氨酰胺转移酶抑制剂对凝血酶脑组织毒性的影响;黄亚林等;《卒中与神经疾病》;20060831;第13卷(第4期);第215-218页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| JP2015533154A (ja) | 2015-11-19 |
| EP2906543B1 (en) | 2019-01-02 |
| GB201218084D0 (en) | 2012-11-21 |
| US20150259310A1 (en) | 2015-09-17 |
| WO2014057266A1 (en) | 2014-04-17 |
| US9656978B2 (en) | 2017-05-23 |
| EP2906543A1 (en) | 2015-08-19 |
| JP6138950B2 (ja) | 2017-05-31 |
| CN104837821A (zh) | 2015-08-12 |
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