CA2397681A1 - Inhibiteurs calciques partiellement satures - Google Patents
Inhibiteurs calciques partiellement satures Download PDFInfo
- Publication number
- CA2397681A1 CA2397681A1 CA002397681A CA2397681A CA2397681A1 CA 2397681 A1 CA2397681 A1 CA 2397681A1 CA 002397681 A CA002397681 A CA 002397681A CA 2397681 A CA2397681 A CA 2397681A CA 2397681 A1 CA2397681 A1 CA 2397681A1
- Authority
- CA
- Canada
- Prior art keywords
- substituted
- unsubstituted
- rings
- heteroaromatic
- ring
- 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
- 229940127291 Calcium channel antagonist Drugs 0.000 title 1
- 150000001669 calcium Chemical class 0.000 title 1
- 239000000480 calcium channel blocker Substances 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 claims abstract 48
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract 42
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 32
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 28
- 150000001875 compounds Chemical class 0.000 claims abstract 18
- 125000000217 alkyl group Chemical group 0.000 claims abstract 16
- 125000005843 halogen group Chemical group 0.000 claims abstract 16
- 125000005842 heteroatom Chemical group 0.000 claims abstract 14
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 10
- 125000000520 N-substituted aminocarbonyl group Chemical group [*]NC(=O)* 0.000 claims abstract 8
- 125000003710 aryl alkyl group Chemical group 0.000 claims abstract 8
- 229910052757 nitrogen Inorganic materials 0.000 claims abstract 8
- 229910052698 phosphorus Inorganic materials 0.000 claims abstract 8
- 150000003839 salts Chemical class 0.000 claims abstract 8
- 229910052717 sulfur Inorganic materials 0.000 claims abstract 8
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 12
- 108090000312 Calcium Channels Proteins 0.000 claims 7
- 102000003922 Calcium Channels Human genes 0.000 claims 7
- 238000000034 method Methods 0.000 claims 7
- 230000002159 abnormal effect Effects 0.000 claims 6
- 230000000694 effects Effects 0.000 claims 6
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 5
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 5
- 239000000556 agonist Substances 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 102000004129 N-Type Calcium Channels Human genes 0.000 claims 2
- 108090000699 N-Type Calcium Channels Proteins 0.000 claims 2
- 230000004308 accommodation Effects 0.000 claims 2
- 102000004310 Ion Channels Human genes 0.000 claims 1
- 108090000862 Ion Channels Proteins 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/22—Anxiolytics
-
- 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
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- 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
- C07D295/04—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 substituted hydrocarbon radicals attached to ring nitrogen atoms
- C07D295/06—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 substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
- C07D295/073—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 substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents separated by carbocyclic rings or by carbon chains interrupted by carbocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C40—COMBINATORIAL TECHNOLOGY
- C40B—COMBINATORIAL CHEMISTRY; LIBRARIES, e.g. CHEMICAL LIBRARIES
- C40B40/00—Libraries per se, e.g. arrays, mixtures
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Investigating Or Analysing Biological Materials (AREA)
Abstract
L'invention concerne des composé représentés par la formule (1a) ou (1b) ou leurs sels, dans lesquelles chaque Z est indépendamment N ou CH, mais un Z doit être N; dans lesquelles n?1¿ est 1 et n?2¿ est 0 ou 1; X?1¿ et X?2¿ sont des segments de liaison; Ar représente un ou deux anneaux aromatiques ou hétéroaromatiques substitués ou non substitués, et Cy représente un ou deux anneaux aliphatiques cycliques ou hétérocycliques substitués ou non substitués, ou est composé d'un anneau aliphatique cyclique ou hétérocyclique substitué ou non substitué et d'un anneau aromatique ou hétéroaromatique substitué ou non substitué; Y¿a? et Y¿b? sont deux anneaux aromatiques ou hétéroaromatiques substitués ou non substitués, ou peuvent être deux anneaux aliphatiques cycliques ou hétérocycliques substitués ou non substitués, ou sont composés d'un anneau aliphatique cyclique ou hétérocyclique substitué ou non substitué et d'un anneau aromatique ou hétéroaromatique substitué ou non substitué; à condition que lesdits anneaux ne soient pas tous les deux un phényle lorsque les deux Ar comprennent un seul anneau de phényle et X?1¿ contient moins de 5C; et à condition que la formule (1b) contienne au moins un anneau aromatique ou hétéroaromatique; 1?1¿ est 0 ou 1; R?1¿ est un alkyle (1-6C) substitué ou non substitué, un aryle (6-10C) substitué ou non substitué ou un arylalkyle (7-16C) substitué ou non substitué contenant éventuellement 1-4 hétéroatomes sélectionnés dans le groupe composé de halo, N, P, O, et S ou pouvant être indépendamment halo, OR, SR, NR¿2?, OOCR, NROCR, COR, COOR, CONR¿2?, CF¿3?, CN ou NO¿2?, R étant H ou alkyle (1-6C).
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US17276599P | 1999-12-20 | 1999-12-20 | |
| US60/172,765 | 1999-12-20 | ||
| US47692999A | 1999-12-30 | 1999-12-30 | |
| US09/476,929 | 1999-12-30 | ||
| PCT/CA2000/001558 WO2001046166A2 (fr) | 1999-12-20 | 2000-12-20 | Inhibiteurs calciques partiellement satures |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CA2397681A1 true CA2397681A1 (fr) | 2001-06-28 |
| CA2397681C CA2397681C (fr) | 2011-03-15 |
Family
ID=26868438
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2397681A Expired - Fee Related CA2397681C (fr) | 1999-12-20 | 2000-12-20 | Inhibiteurs calciques partiellement satures |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1242398A2 (fr) |
| JP (1) | JP2003518107A (fr) |
| AU (1) | AU784848B2 (fr) |
| CA (1) | CA2397681C (fr) |
| MX (1) | MXPA02006137A (fr) |
| NO (1) | NO326939B1 (fr) |
| WO (1) | WO2001046166A2 (fr) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008031227A1 (fr) * | 2006-09-14 | 2008-03-20 | Neuromed Pharmaceuticals Ltd. | Composés de diaryle piperidine utilisés en tant que bloqueurs de canaux calciques |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2004233863B2 (en) | 2003-04-24 | 2010-06-17 | Incyte Holdings Corporation | Aza spiro alkane derivatives as inhibitors of metalloproteases |
| EP1558582B1 (fr) | 2003-07-22 | 2005-12-21 | Arena Pharmaceuticals, Inc. | Derives de diaryl et arylheteroaryl uree utilises en tant que modulateurs du recepteur de la serotonine 5-ht2a utiles pour la prophylaxie et le traitement de troubles associes a ce dernier |
| AU2005254800B2 (en) | 2004-06-15 | 2010-12-09 | Pfizer Inc. | Benzimidazolone carboxylic acid derivatives |
| US7737163B2 (en) | 2004-06-15 | 2010-06-15 | Pfizer Inc. | Benzimidazolone carboxylic acid derivatives |
| KR20070063526A (ko) | 2004-08-30 | 2007-06-19 | 뉴로메드 파머큐티칼즈 리미티드 | 칼슘 채널 차단제인 우레아 유도체 |
| US7511077B2 (en) | 2005-02-09 | 2009-03-31 | Neuromed Pharmaceuticals Ltd. | Diamine calcium channel blockers |
| NZ556627A (en) | 2005-02-22 | 2010-09-30 | Pfizer | Oxyindole derivatives as 5HT4 receptor agonists |
| TWI415845B (zh) | 2006-10-03 | 2013-11-21 | Arena Pharm Inc | 用於治療與5-ht2a血清素受體相關聯病症之作為5-ht2a血清素受體之調節劑的吡唑衍生物 |
| MY148880A (en) | 2006-10-20 | 2013-06-14 | Astrazeneca Ab | N-(2-hydroxyethyl)-n-methyl-4-(quinolin-8-yl(1-(thiazol-4-ylmethyl)piperidin-4-ylidene)methyl)benzamide, the process of making it as well as its use for the treatment of pain, anxiety and depression |
| US9567327B2 (en) | 2007-08-15 | 2017-02-14 | Arena Pharmaceuticals, Inc. | Imidazo[1,2-a]pyridine derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| WO2010062321A1 (fr) | 2008-10-28 | 2010-06-03 | Arena Pharmaceuticals, Inc. | Procédés utiles pour la préparation de 1-[3-(4-bromo-2-méthyl-2h-pyrazol-3-yl)-4-méthoxy-phényl]-3-(2,4-difluoro‑phényl)-urée, et formes cristallines associées |
| TR201805216T4 (en) | 2008-10-28 | 2018-06-21 | Arena Pharm Inc | COMPOSITIONS OF A USEFUL 5-HT2A SEROTONINE RECEPTOR MODULATOR FOR THE TREATMENT OF RELATED DISORDERS |
| US9365553B2 (en) | 2010-05-27 | 2016-06-14 | Aska Pharmaceutical Co., Ltd. | Heterocyclic compound and H1 receptor antagonist |
| EP3288926B1 (fr) | 2015-04-28 | 2021-01-20 | Unilever PLC | Composés d'aralkylcarboxamido-piperazine et -homopiperazine et des compositions de soins personnels comprenant ceux-ci |
| CN107548387B (zh) | 2015-04-28 | 2020-08-25 | 荷兰联合利华有限公司 | N-芳烷基羰基二胺化合物以及包含它们的个人护理组合物 |
| HK1245660A1 (zh) | 2015-06-12 | 2018-08-31 | Axovant Sciences Gmbh | 有用於预防和治疗rem睡眠行为障碍的二芳基脲和芳基脲衍生物 |
| WO2017011767A2 (fr) | 2015-07-15 | 2017-01-19 | Axovant Sciences Ltd. | Dérivés d'arylhérétoaryl urée en tant que modulateurs du récepteur sérotoninergique 5-ht2a utiles pour la prophylaxie et le traitement d'hallucinations associées à une maladie neurodégénérative |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5703071A (en) * | 1990-08-29 | 1997-12-30 | Pharmacia & Upjohn Company | Tropolone derivatives and pharmaceutical composition thereof for preventing and treating ischemic diseases |
| DE4111861A1 (de) | 1991-04-11 | 1992-10-15 | Schwabe Willmar Gmbh & Co | Benzopyranone, verfahren zu ihrer herstellung und verwendung |
| WO1992020661A1 (fr) * | 1991-05-22 | 1992-11-26 | Merck & Co., Inc. | N, n-diacylpiperazines |
| PT682664E (pt) | 1993-12-08 | 2001-06-29 | Alcon Laboratoires Inc | Compostos possuindo actividade potente como antagonistas do calcio e anti-oxidantes e sua utilizacao como agentes citoprotectores |
| DE69814089T2 (de) * | 1997-06-16 | 2004-02-19 | Janssen Pharmaceutica N.V. | Verwendung von einem draflazin analog zur schmerzbehandlung |
| US6251919B1 (en) * | 1998-02-27 | 2001-06-26 | Warner-Lambert | Heterocyclic substituted aniline calcium channel blockers |
| US6011035A (en) * | 1998-06-30 | 2000-01-04 | Neuromed Technologies Inc. | Calcium channel blockers |
-
2000
- 2000-12-20 MX MXPA02006137A patent/MXPA02006137A/es unknown
- 2000-12-20 EP EP00988532A patent/EP1242398A2/fr not_active Withdrawn
- 2000-12-20 WO PCT/CA2000/001558 patent/WO2001046166A2/fr not_active Ceased
- 2000-12-20 JP JP2001547077A patent/JP2003518107A/ja active Pending
- 2000-12-20 CA CA2397681A patent/CA2397681C/fr not_active Expired - Fee Related
- 2000-12-20 AU AU24957/01A patent/AU784848B2/en not_active Ceased
-
2002
- 2002-06-19 NO NO20022948A patent/NO326939B1/no not_active IP Right Cessation
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008031227A1 (fr) * | 2006-09-14 | 2008-03-20 | Neuromed Pharmaceuticals Ltd. | Composés de diaryle piperidine utilisés en tant que bloqueurs de canaux calciques |
Also Published As
| Publication number | Publication date |
|---|---|
| NO326939B1 (no) | 2009-03-16 |
| MXPA02006137A (es) | 2002-12-05 |
| AU784848B2 (en) | 2006-07-06 |
| WO2001046166A2 (fr) | 2001-06-28 |
| WO2001046166A3 (fr) | 2002-03-07 |
| CA2397681C (fr) | 2011-03-15 |
| JP2003518107A (ja) | 2003-06-03 |
| AU2495701A (en) | 2001-07-03 |
| NO20022948D0 (no) | 2002-06-19 |
| NO20022948L (no) | 2002-08-19 |
| EP1242398A2 (fr) | 2002-09-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| MKLA | Lapsed |
Effective date: 20141222 |