RS54901B1 - Biciklično supstituisani uracili i njihova upotreba - Google Patents
Biciklično supstituisani uracili i njihova upotrebaInfo
- Publication number
- RS54901B1 RS54901B1 RS20160510A RSP20160510A RS54901B1 RS 54901 B1 RS54901 B1 RS 54901B1 RS 20160510 A RS20160510 A RS 20160510A RS P20160510 A RSP20160510 A RS P20160510A RS 54901 B1 RS54901 B1 RS 54901B1
- Authority
- RS
- Serbia
- Prior art keywords
- alkyl
- halogen
- hydrogen
- trifluoromethyl
- difluoromethyl
- Prior art date
Links
Classifications
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- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/536—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
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- 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
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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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- 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
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- 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
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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
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- 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
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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- 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
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- C—CHEMISTRY; METALLURGY
- 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
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D405/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Pulmonology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Jedinjenje sa formulom (I)naznačeno time štoR1 je vodonik ili (C1-C4)-alkil,gde* je mesto spajanja na atom azota na uracilu,A je -CH2-, -CH2-CH2-, - O-CH2-## ili kiseonik, gde## je mesto spajanja na fenil prsten,m je broj 0, 1 ili 2,R4 je halogen, difluorometil, trifluorometil, (C1-C4)-alkil, difluorometoksi,trifluorometoksi ili (C1-C4)-alkoksi,R3A je vodonik ili deuterijum,R5B je vodonik, deuterijum ili (C1-C4)-alkil,R6 je vodonik ili fluor,R7 je vodonik ili fluor,R8 je halogen, difluorometil, trifiuorometil, (C1-C4)-alkil ili nitro,R9 je vodonik, halogen, difluorometil, trifluorometil, (C1-C4)-alkil, nitro ili (C1-C4)-alkiltio,R3 je grupa sa formulomgde# je mesto spajanja na atom azota na uracilu,prsten Q je 5- do 7-člani heterociklil ili 5- ili 6-člani heteroaril,gde 5- do 7-člani heterociklil i 5- ili 6-člani heteroaril može biti supstituisan sa 1 do 4 supstituenata koji su nezavisno izabrani iz grupe koja obuhvata halogen, difluorometil, trifluorometil, trideuterometil, (C1-C6)-alkil, (C3-C7)-cikloalkil, okso, hidroksil, (C1-C4)-alkilkarbonil, (C1-C4)-alkoksikarbonil, aminokarbonil i (C1-C4)-alkilsulfonil,gde (C1-C6)-alkil i (C3-C7)-cikloalkil mogu opet da budu supstituisani sa 1 do 3 supstituenata koji su nezavisno izabrani iz grupe koja obuhvata halogen, cijano, trifluorometil, (C3-C7)-cikloalkil, hidroksil, (C1-C4)-alkoksi i 4- do 7-člani heterociklil, igde dva (C1-C6)-alkil radikala vezana na atom ugljenika u 5- do 7-članom heterociklilu i 5- ili 6-članom heteroarilu, zajedno sa atomom ugljenika na koji su vezani, mogu da grade 3- do 6-člani karbocikl,R24 je halogen, (C1-C4)-alkil ili (C1-C4)-alkoksi,n je broj 0, 1, 2 ili 3,i soli, solvati i solvati njihovih soli.Prijava sadrži još 16 patentnih zahteva.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP12167231 | 2012-05-09 | ||
| EP13720407.9A EP2847190B1 (de) | 2012-05-09 | 2013-05-03 | Bicyclisch-substituierte uracile und ihre verwendung |
| PCT/EP2013/059286 WO2013167495A1 (de) | 2012-05-09 | 2013-05-03 | Bicyclisch-substituierte uracile und ihre verwendung |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RS54901B1 true RS54901B1 (sr) | 2016-10-31 |
Family
ID=48289199
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RS20180076A RS56784B1 (sr) | 2012-05-09 | 2013-05-03 | Biciklično supstituisani uracili i njihova upotreba |
| RS20160510A RS54901B1 (sr) | 2012-05-09 | 2013-05-03 | Biciklično supstituisani uracili i njihova upotreba |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RS20180076A RS56784B1 (sr) | 2012-05-09 | 2013-05-03 | Biciklično supstituisani uracili i njihova upotreba |
Country Status (44)
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA112897C2 (uk) * | 2012-05-09 | 2016-11-10 | Байєр Фарма Акцієнгезелльшафт | Біциклічно заміщені урацили та їх застосування для лікування і/або профілактики захворювань |
| EP3066097B1 (de) * | 2013-11-08 | 2017-08-16 | Bayer Pharma Aktiengesellschaft | Salze von 1-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1r)-4-(trifluormethyl)-2,3-dihydro-1h-inden-1-yl]-1,2,3,4-tetrahydropyrimidin-5-carbonsäure |
| WO2015067650A1 (de) * | 2013-11-08 | 2015-05-14 | Bayer Pharma Aktiengesellschaft | Substituierte 1,2,4-triazin-3,5-dione und ihre verwendung als chymase hemmern |
| EP3066098A1 (de) * | 2013-11-08 | 2016-09-14 | Bayer Pharma Aktiengesellschaft | Substituierte uracile und ihre verwendung |
| CN105873919A (zh) * | 2013-11-08 | 2016-08-17 | 拜耳医药股份有限公司 | 作为类糜蛋白酶抑制剂的取代的尿嘧啶 |
| WO2017162661A1 (en) | 2016-03-22 | 2017-09-28 | Bayer Pharma Aktiengesellschaft | 1h-benzo[de]isoquinoline-1,3(2h)-diones |
| EP3338780A1 (de) | 2016-12-20 | 2018-06-27 | Bayer Pharma Aktiengesellschaft | Verwendung von chymaseinhibitoren zur behandlung von endometriose, post-operativer fibrose und erkrankungen die durch fibrosebildung gekennzeichnet sind |
| CA3061444A1 (en) | 2017-04-27 | 2018-11-01 | Bayer Aktiengesellschaft | Selective adrenoreceptor .alpha.2c receptor antagonists alone, or in combination with chymase inhibitors for use in the treatment and/or prophylaxis of peripheral artery diseases (pad) |
| BR112020022340A2 (pt) | 2018-05-15 | 2021-02-02 | Bayer Aktiengesellschaft | benzamidas substituídas por 1,3-tiazol-2-il para o tratamento de doenças associadas com sensibilização de fibras nervosas |
| CN110229067A (zh) * | 2019-06-05 | 2019-09-13 | 南京焕然生物科技有限公司 | 一种2-氨基茚制备方法 |
| CN113811530B (zh) * | 2019-07-03 | 2022-07-19 | 南京明德新药研发有限公司 | 作为糜酶抑制剂的嘧啶酮类化合物及其应用 |
| CN111440141A (zh) * | 2020-05-20 | 2020-07-24 | 安徽泽升科技有限公司 | 一种羟甲基取代芳杂环类化合物的制备方法 |
| WO2022135534A1 (zh) * | 2020-12-25 | 2022-06-30 | 广东东阳光药业有限公司 | 取代的含氮双环化合物及其用途 |
| CN114671856B (zh) * | 2020-12-25 | 2023-10-20 | 广东东阳光药业股份有限公司 | 多取代的尿嘧啶衍生物及其用途 |
| WO2022135514A1 (zh) * | 2020-12-25 | 2022-06-30 | 广东东阳光药业有限公司 | 多取代的尿嘧啶衍生物及其用途 |
| TW202339706A (zh) * | 2021-12-06 | 2023-10-16 | 美商普萊萃歐治療公司 | 含醯胺的ｌｏｎｐ１抑制劑化合物、用途及方法 |
| US11618751B1 (en) | 2022-03-25 | 2023-04-04 | Ventus Therapeutics U.S., Inc. | Pyrido-[3,4-d]pyridazine amine derivatives useful as NLRP3 derivatives |
| TW202404601A (zh) | 2022-04-05 | 2024-02-01 | 加拿大商索科普拉健康與人類科學兩合公司 | 用於選擇性消退血栓性或血栓栓塞性疾病中血栓的凝乳酶抑制劑 |
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