HRP20191353T1 - Supstituirani biciklički dihidropirimidinoni i njihova uporaba u svrhu inhibitora aktivnosti neutrofilne elastaze - Google Patents
Supstituirani biciklički dihidropirimidinoni i njihova uporaba u svrhu inhibitora aktivnosti neutrofilne elastaze Download PDFInfo
- Publication number
- HRP20191353T1 HRP20191353T1 HRP20191353T HRP20191353T1 HR P20191353 T1 HRP20191353 T1 HR P20191353T1 HR P20191353 T HRP20191353 T HR P20191353T HR P20191353 T1 HRP20191353 T1 HR P20191353T1
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- Prior art keywords
- formula
- compound
- acceptable salt
- pharmaceutically acceptable
- represented
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- 239000003112 inhibitor Substances 0.000 title claims 2
- 108010028275 Leukocyte Elastase Proteins 0.000 title 1
- 102000016799 Leukocyte elastase Human genes 0.000 title 1
- 125000002619 bicyclic group Chemical group 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 5
- 201000003883 Cystic fibrosis Diseases 0.000 claims 3
- 206010019708 Hepatic steatosis Diseases 0.000 claims 2
- 206010064911 Pulmonary arterial hypertension Diseases 0.000 claims 2
- 206010069351 acute lung injury Diseases 0.000 claims 2
- 208000006682 alpha 1-Antitrypsin Deficiency Diseases 0.000 claims 2
- 201000009267 bronchiectasis Diseases 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims 2
- -1 5LOinhibitor Substances 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
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 206010006458 Bronchitis chronic Diseases 0.000 claims 1
- 229940122524 Cathepsin C inhibitor Drugs 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 206010014561 Emphysema Diseases 0.000 claims 1
- 208000027004 Eosinophilic disease Diseases 0.000 claims 1
- 208000004930 Fatty Liver Diseases 0.000 claims 1
- 208000017415 Functional neutrophil defect Diseases 0.000 claims 1
- 208000017189 Gastrointestinal inflammatory disease Diseases 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 229940122236 Histamine receptor antagonist Drugs 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- 206010047115 Vasculitis Diseases 0.000 claims 1
- 208000002223 abdominal aortic aneurysm Diseases 0.000 claims 1
- 239000013543 active substance Substances 0.000 claims 1
- 239000000808 adrenergic beta-agonist Substances 0.000 claims 1
- 208000026935 allergic disease Diseases 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims 1
- 239000000739 antihistaminic agent Substances 0.000 claims 1
- 208000007474 aortic aneurysm Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 230000003454 betamimetic effect Effects 0.000 claims 1
- 206010006451 bronchitis Diseases 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 208000007451 chronic bronchitis Diseases 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229960001334 corticosteroids Drugs 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 229940121647 egfr inhibitor Drugs 0.000 claims 1
- 208000010706 fatty liver disease Diseases 0.000 claims 1
- 208000015181 infectious disease Diseases 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- YEESKJGWJFYOOK-IJHYULJSSA-N leukotriene D4 Chemical compound CCCCC\C=C/C\C=C/C=C/C=C/[C@H]([C@@H](O)CCCC(O)=O)SC[C@H](N)C(=O)NCC(O)=O YEESKJGWJFYOOK-IJHYULJSSA-N 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 230000001717 pathogenic effect Effects 0.000 claims 1
- 239000002587 phosphodiesterase IV inhibitor Substances 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 231100000240 steatosis hepatitis Toxicity 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P37/00—Drugs for immunological or allergic disorders
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- Pharmacology & Pharmacy (AREA)
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- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Hematology (AREA)
- Pulmonology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
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- Orthopedic Medicine & Surgery (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (15)
1. Spoj, naznačen time, da je predstavljen formulom 1
u kojoj
R1 je
,
R2 je
,
i R3 je H;
ili
R1 je
,
R2 je
;
i R3 je CH3;
ili
R1 je
,
R2 je
,
i R3 je CH3;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom 1.a
ili njegova farmaceutski prihvatljiva sol.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom 1.b
ili njegova farmaceutski prihvatljiva sol.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time, da je predstavljen formulom 1.c
ili njegova farmaceutski prihvatljiva sol.
5. Spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 4, naznačen time, da konfiguracija formule 1 predstavlja formulu 1'
ili njegova farmaceutski prihvatljiva sol.
6. Spoj u skladu s patentnim zahtjevom 5, naznačen time, da je predstavljen formulom 1.a'
ili njegova farmaceutski prihvatljiva sol.
7. Spoj u skladu s patentnim zahtjevom 5, naznačen time, da je predstavljen formulom 1.b'
ili njegova farmaceutski prihvatljiva sol.
8. Spoj u skladu s patentnim zahtjevom 5, naznačen time, da je predstavljen formulom 1.c'
ili njegova farmaceutski prihvatljiva sol.
9. Spoj formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da se upotrebljava kao lijek.
10. Spoj formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da se upotrebljava kao lijek za liječenje astme i alergijskih bolesti, gastrointestinalnih upalnih bolesti, glomerulonefritisa, eozinofilnih bolesti, kronične opstrukcijske plućne bolesti, infekcije putem patogenih mikroba i reumatoidnog artritisa.
11. Spoj formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da se upotrebljava kao lijek za liječenje neutrofilnih bolesti, cistične fibroze (CF), ne-cistične fibroze, idiopatske plućne fibroze, bronhiektaze, vaskultisa povezanog s ANCA, raka pluća, ne-cistične fibrozne bronhiektaze, emfizema, kroničnog bronhitisa, aktne plućne ozljede (ALI), sindroma akutnog respiratornog poremećaja (ARDS), plućne hipertenzije, plućne arterijske hipertenzije (PAH) i deficijencije alfa-1-antitripsina (AATD).
12. Spoj formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da se upotrebljava kao lijek za liječenje pretilosti i upala koje su povezane s time, otpornosti na inzulin, dijabetesa, masne jetre i jetrene steatoze.
13. Spoj formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8, naznačen time, da se upotrebljava kao lijek za liječenje traumatske ozljede mozga, abdominalne aneurizme aorte i bolesti presadak protiv domaćina (GvHD - eng. Graft vs. Host Disease).
14. Farmaceutski pripravak, naznačen time, da sadrži jedan ili više spojeva formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8 ili njegovu farmaceutski aktivnu sol.
15. Farmaceutski pripravak, naznačen time, da obuhvaća dodatno uz spoj formule 1 u skladu s bilo kojim od patentnih zahtjeva 1 do 8, farmaceutski aktivni spoj koji je odabran iz skupine koja se sastoji od betamimetika, antikolinergika, kortikosteroida, PDE4inhibitora, LTD4antagonista, EGFRinhibitora, katepsin C-inhibitora, CRTH2-inhibitora, 5LOinhibitora, antagonista histaminskog receptora i SYKinhibitora, ali također od kombinacija od dvije ili tri aktivne tvari.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP14179288 | 2014-07-31 | ||
| EP15744229.4A EP3174861B1 (en) | 2014-07-31 | 2015-07-30 | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
| PCT/EP2015/067501 WO2016016365A1 (en) | 2014-07-31 | 2015-07-30 | Substituted bicyclic dihydropyrimidinones and their use as inhibitors of neutrophil elastase activity |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20191353T1 true HRP20191353T1 (hr) | 2019-11-01 |
Family
ID=51257371
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20191353 HRP20191353T1 (hr) | 2014-07-31 | 2019-07-26 | Supstituirani biciklički dihidropirimidinoni i njihova uporaba u svrhu inhibitora aktivnosti neutrofilne elastaze |
Country Status (32)
| Country | Link |
|---|---|
| US (1) | US9475779B2 (hr) |
| EP (2) | EP3539952B1 (hr) |
| JP (1) | JP6345337B2 (hr) |
| KR (1) | KR102420210B1 (hr) |
| CN (2) | CN107253933B (hr) |
| AP (1) | AP2016009632A0 (hr) |
| AU (1) | AU2015295283B2 (hr) |
| CA (1) | CA2956745C (hr) |
| CL (1) | CL2017000117A1 (hr) |
| CO (1) | CO2017000745A2 (hr) |
| CY (1) | CY1121933T1 (hr) |
| DK (1) | DK3174861T3 (hr) |
| EA (1) | EA033263B1 (hr) |
| ES (1) | ES2740428T3 (hr) |
| HR (1) | HRP20191353T1 (hr) |
| HU (1) | HUE045530T2 (hr) |
| IL (1) | IL249687B (hr) |
| LT (1) | LT3174861T (hr) |
| ME (1) | ME03526B (hr) |
| MX (1) | MX2017001347A (hr) |
| MY (1) | MY182438A (hr) |
| NZ (1) | NZ727554A (hr) |
| PE (1) | PE20170524A1 (hr) |
| PH (1) | PH12017500114A1 (hr) |
| PL (1) | PL3174861T3 (hr) |
| PT (1) | PT3174861T (hr) |
| RS (1) | RS59040B1 (hr) |
| SA (1) | SA517380781B1 (hr) |
| SG (1) | SG11201700658UA (hr) |
| SI (1) | SI3174861T1 (hr) |
| UA (1) | UA118130C2 (hr) |
| WO (1) | WO2016016365A1 (hr) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210002573A (ko) | 2018-04-24 | 2021-01-08 | 주식회사 피에이치파마 | 간 질환에 호중구 엘라스타제 저해제의 사용 |
| BR112022004861A2 (pt) | 2019-09-17 | 2022-06-07 | Univ Duke | Alvelestat para uso no tratamento de rejeição de transplante, síndrome de bronquiolite obliterante e doença de transplante versus hospedeiro |
| IL297211A (en) | 2020-04-16 | 2022-12-01 | Mereo Biopharma 4 Ltd | Methods involving the neutrophil elastase inhibitor albalstat for the treatment of respiratory disease mediated by alpha-1 antitrypsin deficiency |
| TW202325294A (zh) | 2021-10-20 | 2023-07-01 | 英商梅瑞奧生物製藥４有限公司 | 用於治療纖維化之嗜中性球彈性蛋白酶抑制劑 |
| CN115109066B (zh) * | 2022-06-30 | 2023-04-07 | 武汉工程大学 | 一种大斯托克斯位移检测弹性蛋白酶的荧光探针及其制备方法与应用 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6207665B1 (en) | 1997-06-12 | 2001-03-27 | Schering Aktiengesellschaft | Piperazine derivatives and their use as anti-inflammatory agents |
| WO2003053930A1 (en) | 2001-12-20 | 2003-07-03 | Bayer Healthcare Ag | 1,4-dihydro-1,4-diphenylpyridine derivatives |
| WO2004020410A2 (en) | 2002-08-27 | 2004-03-11 | Bayer Healthcare Ag | Dihydropyridinone derivatives as hne inhibitors |
| GB0219896D0 (en) | 2002-08-27 | 2002-10-02 | Bayer Ag | Dihydropyridine derivatives |
| AU2003282006C1 (en) | 2002-09-10 | 2009-11-26 | Bayer Schering Pharma Aktiengesellschaft | Pyrimidinone derivatives as therapeutic agents against acute and chronic inflammatory ischaemic and remodelling processes |
| GB2392910A (en) | 2002-09-10 | 2004-03-17 | Bayer Ag | 2-Oxopyrimidine derivatives and their use as human leukocyte elastase inhibitors |
| EP1539710B1 (en) | 2002-09-10 | 2010-10-27 | Bayer Schering Pharma Aktiengesellschaft | Heterocyclic derivatives |
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