HRP20200580T1 - Novi spojevi - Google Patents
Novi spojevi Download PDFInfo
- Publication number
- HRP20200580T1 HRP20200580T1 HRP20200580TT HRP20200580T HRP20200580T1 HR P20200580 T1 HRP20200580 T1 HR P20200580T1 HR P20200580T T HRP20200580T T HR P20200580TT HR P20200580 T HRP20200580 T HR P20200580T HR P20200580 T1 HRP20200580 T1 HR P20200580T1
- Authority
- HR
- Croatia
- Prior art keywords
- methyl
- compound
- trifluoromethyl
- phenyl
- pyrimidin
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims 14
- 238000000034 method Methods 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 6
- NZFPEZSHJULZDR-IBGZPJMESA-N (3s)-3-amino-1-methyl-3-[3-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]prop-2-ynyl]pyrrolidin-2-one Chemical compound O=C1N(C)CC[C@@]1(N)CC#CC1=NC(C)=CC(C=2C=CC(=CC=2)C(F)(F)F)=N1 NZFPEZSHJULZDR-IBGZPJMESA-N 0.000 claims 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 claims 4
- 238000007363 ring formation reaction Methods 0.000 claims 4
- NZFPEZSHJULZDR-LJQANCHMSA-N (3r)-3-amino-1-methyl-3-[3-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]prop-2-ynyl]pyrrolidin-2-one Chemical compound O=C1N(C)CC[C@]1(N)CC#CC1=NC(C)=CC(C=2C=CC(=CC=2)C(F)(F)F)=N1 NZFPEZSHJULZDR-LJQANCHMSA-N 0.000 claims 3
- CZKMPDNXOGQMFW-UHFFFAOYSA-N chloro(triethyl)germane Chemical compound CC[Ge](Cl)(CC)CC CZKMPDNXOGQMFW-UHFFFAOYSA-N 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- -1 (5S)-7-Methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-ene Chemical compound 0.000 claims 1
- CIBIQCRUDYBRJO-LJQANCHMSA-N (5r)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one Chemical compound O=C1N(C)CC[C@@]11N=C(C=2N=C(C=C(C)N=2)C=2C=CC(=CC=2)C(F)(F)F)CC1 CIBIQCRUDYBRJO-LJQANCHMSA-N 0.000 claims 1
- CIBIQCRUDYBRJO-IBGZPJMESA-N (5s)-7-methyl-2-[4-methyl-6-[4-(trifluoromethyl)phenyl]pyrimidin-2-yl]-1,7-diazaspiro[4.4]non-1-en-6-one Chemical compound O=C1N(C)CC[C@]11N=C(C=2N=C(C=C(C)N=2)C=2C=CC(=CC=2)C(F)(F)F)CC1 CIBIQCRUDYBRJO-IBGZPJMESA-N 0.000 claims 1
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 1
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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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- A—HUMAN NECESSITIES
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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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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- 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
- C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
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- 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
- C07D471/10—Spiro-condensed systems
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- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
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- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Rheumatology (AREA)
- Psychology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Anesthesiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Reproductive Health (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Claims (13)
1. Spoj koji je (5R)-7-Metil-2-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]non-1-en-6-on ili (5S)-7-Metil-2-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]non-1-en-6-on.
2. Spoj prema patentnom zahtjevu 1, naznačen time što je spoj (5S)-7-Metil-2-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]-1,7-diazaspiro[4.4]non-1-en-6-on.
3. Postupak za pripravu spoja prema patentnom zahtjevu 1 ili zahtjevu 2, naznačen time što obuhvaća provođenje reakcije zatvaranja prstena na (3R)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-onu ili (3S)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-onu.
4. Postupak kako je definirano u patentnom zahtjevu 3, naznačen time što se reakcija zatvaranja prstena provodi na (3S)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-onu.
5. Postupak za pripravu spoja s formulom (I):
[image]
ili njegove farmaceutski prihvatljive soli ili solvata, naznačen time što sadrži redukciju spoja prema patentnom zahtjevu 1 ili zahtjevu 2.
6. Postupak kako je definirano u patentnom zahtjevu 5, naznačen time što spoj s formulom (I) je spoj s formulom (Ia):
[image]
ili njegova farmaceutski prihvatljiva sol ili solvat.
7. Postupak kako je definirano u patentnom zahtjevu 5 ili zahtjevu 6, naznačen time što je spoj s formulom (I) hidrokloridna sol.
8. Postupak kako je definirano u patentnom zahtjevu 5 ili zahtjevu 6, naznačen time što je spoj s formulom (I) sol sumporne kiseline.
9. Postupak kako je definirano u patentnom zahtjevu 5 ili zahtjevu 6, naznačen time što je spoj s formulom (I) hidrat soli sumporne kiseline.
10. Postupak prema patentnom zahtjevu 3, naznačen time što provođenje reakcije zatvaranja prstena na (3R)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-onu sadrži dodavanje srebrovog trifluorometansulfonata u (3R)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-on.
11. Postupak prema patentnom zahtjevu 3, naznačen time što provođenje reakcije zatvaranja prstena na (3S)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-onu sadrži dodavanje srebrovog trifluorometansulfonata u (3S)-3-Amino-1-metil-3-[3-[4-metil-6-[4-(trifluorometil)fenil]pirimidin-2-il]prop-2-inil]pirolidin-2-on.
12. Postupak prema patentnom zahtjevu 5, naznačen time što je postupak za pripravu spoja s formulom (I) ili njegove farmaceutski prihvatljive soli.
13. Postupak prema patentnom zahtjevu 6, naznačen time što je postupak za pripravu spoja s formulom (Ia) ili njegove farmaceutski prihvatljive soli.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261650325P | 2012-05-22 | 2012-05-22 | |
GB201209015A GB201209015D0 (en) | 2012-05-22 | 2012-05-22 | Novel compounds |
US201361773710P | 2013-03-06 | 2013-03-06 | |
EP16177700.8A EP3106464B1 (en) | 2012-05-22 | 2013-05-22 | Novel compounds |
Publications (1)
Publication Number | Publication Date |
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HRP20200580T1 true HRP20200580T1 (hr) | 2020-10-02 |
Family
ID=46546493
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20161349TT HRP20161349T1 (hr) | 2012-05-22 | 2016-10-17 | 7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]piramidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on |
HRP20200580TT HRP20200580T1 (hr) | 2012-05-22 | 2020-04-06 | Novi spojevi |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20161349TT HRP20161349T1 (hr) | 2012-05-22 | 2016-10-17 | 7-metil-2-[4-metil-6-[4-(trifluorometil)-fenil]piramidin-2-il]-1,7-diazaspiro[4.4]nonan-6-on |
Country Status (28)
Country | Link |
---|---|
US (7) | US9309254B2 (hr) |
EP (3) | EP2861602B1 (hr) |
JP (3) | JP2015517562A (hr) |
KR (2) | KR102161101B1 (hr) |
CN (2) | CN107344942B (hr) |
AU (3) | AU2013265001B2 (hr) |
BR (1) | BR112014029280B1 (hr) |
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DK (2) | DK3106464T3 (hr) |
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SG (2) | SG11201407755UA (hr) |
SI (2) | SI2861602T1 (hr) |
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GB201122113D0 (en) | 2011-12-22 | 2012-02-01 | Convergence Pharmaceuticals | Novel compounds |
GB201209015D0 (en) | 2012-05-22 | 2012-07-04 | Convergence Pharmaceuticals | Novel compounds |
CA3074923A1 (en) * | 2017-09-28 | 2019-04-04 | Biogen Inc. | Novel salts |
MX2020003821A (es) | 2017-10-10 | 2023-01-12 | Biogen Inc | Proceso de elaboración de espiroderivados. |
WO2022133097A1 (en) * | 2020-12-17 | 2022-06-23 | Biogen Ma Inc. | Synthesis of compounds that modulate use-dependent voltage-gated sodium channels |
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WO2004005293A2 (en) * | 2002-07-05 | 2004-01-15 | Targacept, Inc. | N-aryl diazaspiracyclic compounds and methods of preparation and use thereof |
GB0520578D0 (en) * | 2005-10-10 | 2005-11-16 | Glaxo Group Ltd | Novel compounds |
TW200728258A (en) | 2005-10-10 | 2007-08-01 | Glaxo Group Ltd | Novel compounds |
US8143306B2 (en) | 2005-10-10 | 2012-03-27 | Convergence Pharmaceuticals Limited | Methods of treating bipolar disorders |
TW200730494A (en) | 2005-10-10 | 2007-08-16 | Glaxo Group Ltd | Novel compounds |
WO2007042250A1 (en) | 2005-10-10 | 2007-04-19 | Glaxo Group Limited | Prolinamide derivatives as sodium channel modulators |
JP2009511599A (ja) * | 2005-10-12 | 2009-03-19 | バーテックス ファーマシューティカルズ インコーポレイテッド | 電位依存性イオンチャネルの調整剤としてのビフェニル誘導体 |
US7998959B2 (en) * | 2006-01-12 | 2011-08-16 | Incyte Corporation | Modulators of 11-β hydroxyl steroid dehydrogenase type 1, pharmaceutical compositions thereof, and methods of using the same |
CL2007002953A1 (es) | 2006-10-12 | 2008-02-01 | Xenon Pharmaceuticals Inc | Compuestos derivados de espiro-oxindol; composicion farmaceutica que comprende a dicho compuesto; y uso del compuesto en el tratamiento del dolor, cancer, prurito, hiperplasia prostatica benigna, hipercolesterolemia. |
CN101522685A (zh) * | 2006-10-12 | 2009-09-02 | 泽农医药公司 | 三环螺-吲哚酮衍生物及其作为治疗剂的用途 |
CN101641099A (zh) | 2007-01-24 | 2010-02-03 | 葛兰素集团有限公司 | 包含3,5-二氨基-6-(2,3-二氯苯基)-1,2,4-三嗪或r(-)-2,4-二氨基-5-(2,3-二氯苯基)-6-氟甲基嘧啶和nk1的药物组合物 |
GB0701365D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
GB0701366D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
GB0706630D0 (en) | 2007-04-04 | 2007-05-16 | Glaxo Group Ltd | Novel compounds |
AR077252A1 (es) * | 2009-06-29 | 2011-08-10 | Xenon Pharmaceuticals Inc | Enantiomeros de compuestos de espirooxindol y sus usos como agentes terapeuticos |
US8759542B2 (en) | 2009-09-14 | 2014-06-24 | Convergence Pharmaceuticals Limited | Process for preparing alpha-carboxamide derivatives |
GB201122113D0 (en) | 2011-12-22 | 2012-02-01 | Convergence Pharmaceuticals | Novel compounds |
TWI625046B (zh) * | 2012-03-21 | 2018-05-21 | 內數位專利控股公司 | 在無線網路中行動站贊助方法及裝置 |
GB201209015D0 (en) | 2012-05-22 | 2012-07-04 | Convergence Pharmaceuticals | Novel compounds |
GB201209670D0 (en) | 2012-05-31 | 2012-07-18 | Convergence Pharmaceuticals | Novel compounds |
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