ES2610185T3 - Composición farmacéutica - Google Patents
Composición farmacéutica Download PDFInfo
- Publication number
- ES2610185T3 ES2610185T3 ES11760631.9T ES11760631T ES2610185T3 ES 2610185 T3 ES2610185 T3 ES 2610185T3 ES 11760631 T ES11760631 T ES 11760631T ES 2610185 T3 ES2610185 T3 ES 2610185T3
- Authority
- ES
- Spain
- Prior art keywords
- methyl
- pyrazol
- nmr
- mhz
- ppm
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims abstract description 50
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 34
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract description 22
- 150000002431 hydrogen Chemical group 0.000 claims abstract 15
- 239000001257 hydrogen Substances 0.000 claims abstract 15
- 229910052736 halogen Inorganic materials 0.000 claims abstract 12
- 150000002367 halogens Chemical group 0.000 claims abstract 12
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims abstract 12
- 125000004216 fluoromethyl group Chemical group [H]C([H])(F)* 0.000 claims abstract 9
- 150000003839 salts Chemical class 0.000 claims abstract 9
- 125000004785 fluoromethoxy group Chemical group [H]C([H])(F)O* 0.000 claims abstract 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims abstract 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims abstract 3
- 229910052760 oxygen Inorganic materials 0.000 claims abstract 3
- 239000001301 oxygen Substances 0.000 claims abstract 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 5
- 201000006417 multiple sclerosis Diseases 0.000 claims description 3
- 241000124008 Mammalia Species 0.000 claims 2
- OKKJLVBELUTLKV-MZCSYVLQSA-N Deuterated methanol Chemical compound [2H]OC([2H])([2H])[2H] OKKJLVBELUTLKV-MZCSYVLQSA-N 0.000 description 100
- 238000005160 1H NMR spectroscopy Methods 0.000 description 61
- 238000004519 manufacturing process Methods 0.000 description 44
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- SZUAJCIGBDCCPA-UHFFFAOYSA-N [1-(4-methoxycarbonylphenyl)cyclopropyl]azanium;chloride Chemical compound [Cl-].C1=CC(C(=O)OC)=CC=C1C1([NH3+])CC1 SZUAJCIGBDCCPA-UHFFFAOYSA-N 0.000 description 7
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- NMYPMEAFQUDCSC-UHFFFAOYSA-N 5-chloro-3-(difluoromethyl)-1-methylpyrazole-4-carbaldehyde Chemical compound CN1N=C(C(F)F)C(C=O)=C1Cl NMYPMEAFQUDCSC-UHFFFAOYSA-N 0.000 description 4
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Classifications
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Immunology (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US38478110P | 2010-09-21 | 2010-09-21 | |
| US384781P | 2010-09-21 | ||
| PCT/US2011/051163 WO2012039972A1 (en) | 2010-09-21 | 2011-09-12 | Pharmaceutical composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2610185T3 true ES2610185T3 (es) | 2017-04-26 |
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| ES11760631.9T Active ES2610185T3 (es) | 2010-09-21 | 2011-09-12 | Composición farmacéutica |
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| CA (1) | CA2806121C (OSRAM) |
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| CY (1) | CY1118680T1 (OSRAM) |
| DK (1) | DK2619182T3 (OSRAM) |
| ES (1) | ES2610185T3 (OSRAM) |
| HR (1) | HRP20170042T1 (OSRAM) |
| HU (1) | HUE031408T2 (OSRAM) |
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| LT (1) | LT2619182T (OSRAM) |
| ME (1) | ME02575B (OSRAM) |
| MX (1) | MX2013003162A (OSRAM) |
| MY (1) | MY162146A (OSRAM) |
| NZ (1) | NZ606629A (OSRAM) |
| PE (1) | PE20131343A1 (OSRAM) |
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| SM (2) | SMT201700008T1 (OSRAM) |
| UA (1) | UA113499C2 (OSRAM) |
| WO (1) | WO2012039972A1 (OSRAM) |
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| HRP20211380T1 (hr) | 2017-05-18 | 2021-11-26 | Idorsia Pharmaceuticals Ltd | Derivati pirimidina kao modulatori receptora pge2 |
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| TW202228674A (zh) | 2020-11-13 | 2022-08-01 | 日商小野藥品工業股份有限公司 | 藉由併用ｅｐ４拮抗藥與免疫檢查點抑制物質而進行之癌症治療 |
| TWI877433B (zh) | 2020-11-30 | 2025-03-21 | 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 |
| CA3230557A1 (en) * | 2021-09-03 | 2023-03-09 | Xuejun Zhang | Ep4 antagonist compound as well as salt, polymorph, and use thereof |
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