DK2619182T3 - Farmaceutisk sammensætning - Google Patents
Farmaceutisk sammensætning Download PDFInfo
- Publication number
- DK2619182T3 DK2619182T3 DK11760631.9T DK11760631T DK2619182T3 DK 2619182 T3 DK2619182 T3 DK 2619182T3 DK 11760631 T DK11760631 T DK 11760631T DK 2619182 T3 DK2619182 T3 DK 2619182T3
- Authority
- DK
- Denmark
- Prior art keywords
- methyl
- hydrogen
- compound
- pharmaceutically acceptable
- cancer
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
- C07D231/18—One oxygen or sulfur atom
- C07D231/20—One oxygen atom attached in position 3 or 5
- C07D231/22—One oxygen atom attached in position 3 or 5 with aryl radicals attached to ring nitrogen atoms
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P25/28—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Rheumatology (AREA)
- Immunology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Claims (20)
1. Forbindelse med formel I:
hvor: den ene af Rid og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; Rs er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Rs er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R6 er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor den ene af Ri£ og Rib er hydrogen, og den anden er methyl; R2 er methyl, difluormethyl eller trifluormethyl; R3 er methyl; R4 er chlor, fluor, trifluormethyl, difluormethyl, methyl, methoxy, difluormethoxy eller trifluormethoxy; Rs er hydrogen, chlor, fluor, methyl eller methoxy; Re og R7 er hydrogen; eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 2, hvor Rs er hydrogen; eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge krav 3, hvor R4 er udvalgt blandt chlor, trifluormethyl, difluormethyl, difluormethoxy og trifluormethoxy; eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge et hvilket som helst af kravene 1-4, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og forbindelsen med formel I består af en blanding af stereoisomerer; eller et farmaceutisk acceptabelt salt deraf.
6. Forbindelse ifølge et hvilket som helst af kravene 1-4, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og forbindelsen med formel I består af en i det væsentlige ren stereoisomer; eller et farmaceutisk acceptabelt salt deraf.
7. Forbindelse ifølge krav 6, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og carbonatomet i forbindelsen med formel I markeret med en * har i det væsentlige S-konfigurationen; eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse ifølge krav 6, hvor den ene af Ria og Rib er hydrogen, og den anden er methyl, og carbonatomet i forbindelsen med formel I markeret med en * har i det væsentlige R-konfigurationen; eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse ifølge krav 1, hvor Ria og Rib sammen danner en cyclopropylring; R2 er methyl, trifluormethyl eller difluormethyl; R.3 er methyl; R4 er trifluormethyl, difluormethyl, chlor eller fluor; Re og R7 er hydrogen; eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse ifølge krav 1 udvalgt fra gruppen, der består af:
og farmaceutisk acceptable salte deraf.
11. Forbindelse ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf.
13. Farmaceutical sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ri^ og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; R3 er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Rs er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Re er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale eller (b) en forbindelse ifølge krav 10 eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale eller (c) forbindelsen, som er:
eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale.
14. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf; og et farmaceutisk acceptabelt bæremateriale.
15. Farmaceutisk sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ria og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; Ra er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R5 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Re er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller et farmaceutisk acceptabelt salt deraf eller (b) en forbindelse ifølge krav 10; eller et farmaceutisk acceptabelt salt deraf eller (c) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf eller (d) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af multipel sklerose hos et pattedyr.
16. Farmaceutisk sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ria og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; R3 er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R5 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; Re er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller farmaceutisk acceptable salte deraf eller (b) en forbindelse ifølge krav 10; eller et farmaceutisk acceptabelt salt deraf eller (c) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf eller (d) forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af rheumatoid arthritis hos et pattedyr.
17. Farmaceutisk sammensætning, der omfatter: (a) en forbindelse med formel I:
hvor: den ene af Ri£ og Rib er hydrogen, og den anden er methyl; eller Ria og Rib sammen danner en cyclopropylring; R2 er methyl eller fluormethyl; R3 er methyl; R4 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R5 er hydrogen, halogen, fluormethyl, methyl, methoxy eller fluormethoxy; R.6 er hydrogen, halogen, methyl eller methoxy; R7 er hydrogen, halogen, methyl eller methoxy; og X er oxygen; eller farmaceutisk acceptable salte deraf eller (b) en forbindelse ifølge krav 10; eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af cancer hos et pattedyr, hvor canceren eventuelt er udvalgt fra gruppen, der består af hudcancer, brystcancer, colorektal cancer, prostatacancer, nyrecancer, ovariecancer, cervixcancer, endometriumcancer, glioblastom, lungecancer, hoved- og halscancer, medulloblastom og urinvejscancer.
18. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af cancer hos et pattedyr.
19. Farmaceutisk sammensætning ifølge krav 18, hvor canceren er udvalgt fra gruppen, der består af hudcancer, brystcancer, colorektal cancer, prostatacancer, nyrecancer, ovariecancer, cervixcancer, endometriumcancer, glioblastom, lungecancer, hoved- og halscancer, medulloblastom og urinvejscancer.
20. Farmaceutisk sammensætning, der omfatter forbindelsen ifølge krav 10, som er:
eller et farmaceutisk acceptabelt salt deraf, til anvendelse til behandling af cancer hos et pattedyr, hvor canceren eventuelt er udvalgt fra gruppen, der består af hudcancer, brystcancer, colorektal cancer, prostatacancer, nyrecancer, ovariecancer, cervixcancer, endometriumcancer, glioblastom, lungecancer, hoved- og halscancer, medulloblastom og urinvejscancer.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US38478110P | 2010-09-21 | 2010-09-21 | |
PCT/US2011/051163 WO2012039972A1 (en) | 2010-09-21 | 2011-09-12 | Pharmaceutical composition |
Publications (1)
Publication Number | Publication Date |
---|---|
DK2619182T3 true DK2619182T3 (da) | 2017-01-30 |
Family
ID=44674894
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DK11760631.9T DK2619182T3 (da) | 2010-09-21 | 2011-09-12 | Farmaceutisk sammensætning |
Country Status (30)
Country | Link |
---|---|
US (2) | US8686018B2 (da) |
EP (2) | EP2619182B1 (da) |
JP (1) | JP5956448B2 (da) |
KR (1) | KR101911105B1 (da) |
CN (1) | CN103097358B (da) |
AU (1) | AU2011305872B2 (da) |
BR (1) | BR112013002484B1 (da) |
CA (1) | CA2806121C (da) |
CL (1) | CL2013000675A1 (da) |
CY (1) | CY1118680T1 (da) |
DK (1) | DK2619182T3 (da) |
ES (1) | ES2610185T3 (da) |
HR (1) | HRP20170042T1 (da) |
HU (1) | HUE031408T2 (da) |
IL (1) | IL224288A (da) |
LT (1) | LT2619182T (da) |
ME (1) | ME02575B (da) |
MX (1) | MX2013003162A (da) |
MY (1) | MY162146A (da) |
NZ (1) | NZ606629A (da) |
PE (1) | PE20131343A1 (da) |
PL (1) | PL2619182T3 (da) |
PT (1) | PT2619182T (da) |
RS (1) | RS55566B1 (da) |
RU (1) | RU2606510C2 (da) |
SG (1) | SG188188A1 (da) |
SI (1) | SI2619182T1 (da) |
SM (1) | SMT201700008B (da) |
UA (1) | UA113499C2 (da) |
WO (1) | WO2012039972A1 (da) |
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TW201623277A (zh) | 2014-03-26 | 2016-07-01 | 安斯泰來製藥股份有限公司 | 醯胺化合物 |
KR102535283B1 (ko) * | 2014-05-23 | 2023-05-22 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 암의 치료를 위한 조합 요법 |
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US10316040B2 (en) | 2015-10-16 | 2019-06-11 | Eisai R&D Management Co., Ltd. | EP4 antagonists |
CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
MX2019013639A (es) | 2017-05-18 | 2020-01-21 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituidos. |
TW201900179A (zh) | 2017-05-18 | 2019-01-01 | 瑞士商愛杜西亞製藥有限公司 | 作為pge2受體調節劑之苯并呋喃及苯并噻吩衍生物 |
DK3625222T3 (da) | 2017-05-18 | 2021-10-25 | Idorsia Pharmaceuticals Ltd | Phenylderivater som pge2-receptormodulatorer |
CA3063788A1 (en) | 2017-05-18 | 2018-11-22 | Idorsia Pharmaceuticals Ltd | Pyrimidine derivatives |
HUE056382T2 (hu) | 2017-05-18 | 2022-02-28 | Idorsia Pharmaceuticals Ltd | Pirimidin-származékok mint PGE2 receptor modulátorok |
CN108929281B (zh) * | 2017-05-27 | 2021-12-24 | 华东师范大学 | 三氮唑类化合物及其合成方法和应用 |
CN117643587A (zh) * | 2018-02-05 | 2024-03-05 | 深圳市原力生命科学有限公司 | 用于治疗癌症的杂二环羧酸 |
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CN114075140A (zh) * | 2020-08-18 | 2022-02-22 | 武汉人福创新药物研发中心有限公司 | 作为ep4受体拮抗剂的吡唑酰胺衍生物及其在癌症和炎症中的用途 |
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TW202227089A (zh) | 2020-11-30 | 2022-07-16 | 大陸商杭州阿諾生物醫藥科技有限公司 | 用於治療pik3ca突變癌症的組合療法 |
WO2022161418A1 (zh) * | 2021-01-28 | 2022-08-04 | 深圳晶泰科技有限公司 | 吡唑酰胺衍生物及其制备方法和应用 |
TW202328073A (zh) * | 2021-09-03 | 2023-07-16 | 大陸商武漢人福創新藥物研發中心有限公司 | Ep4拮抗劑化合物及其鹽、多晶型及其製備方法和用途 |
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