RU2016147704A - Производные циклогексилпиридина - Google Patents
Производные циклогексилпиридина Download PDFInfo
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- RU2016147704A RU2016147704A RU2016147704A RU2016147704A RU2016147704A RU 2016147704 A RU2016147704 A RU 2016147704A RU 2016147704 A RU2016147704 A RU 2016147704A RU 2016147704 A RU2016147704 A RU 2016147704A RU 2016147704 A RU2016147704 A RU 2016147704A
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- Prior art keywords
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- chem
- pharmaceutically acceptable
- acceptable salt
- compound represented
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- HUTHUTALXJNNRS-UHFFFAOYSA-N 2-cyclohexylpyridine Chemical class C1CCCCC1C1=CC=CC=N1 HUTHUTALXJNNRS-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 206010047700 Vomiting Diseases 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000001093 anti-cancer Effects 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
-
- 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
- A61K31/435—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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/72—Nitrogen atoms
- C07D213/76—Nitrogen atoms to which a second hetero atom is attached
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/84—Nitriles
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Claims (74)
1. Соединение, представленное формулой (I):
[Хим. формула 1]
где
кольцо А является группой, представленной следующей формулой:
[Хим. формула 2]
X представляет собой атом водорода, циано, галоген, C1-6алкил или гидроксиметил;
R1 является группой, представленной следующей формулой:
[Хим. формула 3]
где
R1a и R1b, каждый независимо друг от друга, представляет собой атом водорода, атом фтора или C1-6алкил;
m равен 0, 1 или 2;
когда m равен 2, тогда R1a и R1b необязательно отличаются друг от друга;
R2 представляет собой C1-6алкил, гидроксигруппу или C1-6алкокси;
U является группой, представленной следующей формулой:
[Хим. формула 4]
где
R3a и R3b, каждый независимо, представляет собой атом водорода, C1-6алкил, гидроксиC1-6алкил или C1-6алкоксиC1-6алкил;
Y равен 0, 1 или 2;
когда Y равен 2, два R2 необязательно отличаются друг от друга;
или его фармацевтически приемлемая соль.
2. Соединение, представленное формулой (Ia), по п.1:
[Хим. формула 5]
где
кольцо A и X имеют такие же значения, как определено в п.1;
R1c и R1d, каждый независимо, представляет собой атом водорода или метил;
U1 является группой, представленной следующей формулой:
[Хим. формула 6]
в которой
R3c и R3d, каждый независимо, представляет собой атом водорода, метил или гидроксиметил;
n равен 0, 1 или 2;
когда n равен 2, тогда R1c и R1d необязательно отличаются друг от друга;
или его фармацевтически приемлемая соль.
3. Соединение, представленное формулой (Ib), по п.2:
[Хим. формула 7]
где
R1c и R1d имеют такие же значения, как определено в п.2,
или его фармацевтически приемлемая соль.
4. Соединение, представленное следующей формулой:
[Хим. формула 8]
или его фармацевтически приемлемая соль.
5. Соединение, представленное следующей формулой:
[Хим. формула 9]
или его фармацевтически приемлемая соль.
6. Соединение, представленное следующей формулой:
[Хим. формула 10]
или его фармацевтически приемлемая соль.
7. Соединение, представленное следующей формулой:
[Хим. формула 11]
или его фармацевтически приемлемая соль.
8. Соединение, представленное следующей формулой:
[Хим. формула 12]
или его фармацевтически приемлемая соль.
9. Соединение, представленное следующей формулой:
[Хим. формула 13]
или его фармацевтически приемлемая соль.
10. Соединение, представленное следующей формулой:
[Хим. формула 14]
или его фармацевтически приемлемая соль.
11. Фармацевтическая композиция, содержащая в качестве активного ингредиента соединение по любому из пп.1-10 или его фармацевтически приемлемую соль.
12. Фармацевтическая композиция по п.11, для применения при предупреждении тошноты и рвоты, вызванных противораковой химиотерапией.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2014-095776 | 2014-05-07 | ||
| JP2014095776 | 2014-05-07 | ||
| PCT/JP2015/063154 WO2015170693A1 (ja) | 2014-05-07 | 2015-05-07 | シクロヘキシルピリジン誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| RU2016147704A true RU2016147704A (ru) | 2018-06-09 |
| RU2016147704A3 RU2016147704A3 (ru) | 2018-09-19 |
| RU2681316C2 RU2681316C2 (ru) | 2019-03-06 |
Family
ID=54392543
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2016147704A RU2681316C2 (ru) | 2014-05-07 | 2015-05-07 | Производные циклогексилпиридина |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US9708266B2 (ru) |
| EP (1) | EP3141541B1 (ru) |
| JP (1) | JP5847362B1 (ru) |
| KR (1) | KR102061544B1 (ru) |
| CN (1) | CN106414406B (ru) |
| AU (1) | AU2015257007B2 (ru) |
| BR (1) | BR112016025984B1 (ru) |
| CA (1) | CA2946523C (ru) |
| DK (1) | DK3141541T3 (ru) |
| ES (1) | ES2704709T3 (ru) |
| HU (1) | HUE042659T2 (ru) |
| IL (1) | IL248772B (ru) |
| MX (1) | MX2016014566A (ru) |
| PL (1) | PL3141541T3 (ru) |
| PT (1) | PT3141541T (ru) |
| RU (1) | RU2681316C2 (ru) |
| SG (1) | SG11201609298TA (ru) |
| TW (1) | TWI649307B (ru) |
| WO (1) | WO2015170693A1 (ru) |
| ZA (1) | ZA201607847B (ru) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016021562A1 (ja) * | 2014-08-06 | 2016-02-11 | キッセイ薬品工業株式会社 | シアノチオフェン誘導体 |
| JPWO2017099049A1 (ja) * | 2015-12-07 | 2018-09-27 | キッセイ薬品工業株式会社 | Ｎｋ１受容体拮抗剤 |
| CA3068350A1 (en) | 2017-06-30 | 2019-01-03 | Bayer Animal Health Gmbh | New azaquinoline derivatives |
| MX2022005867A (es) | 2019-11-15 | 2022-06-14 | Kandy Therapeutics Ltd | Nuevo proceso quimico para la elaboracion de 6-cloro-4-(4-fluoro-2 -metilfenil)piridin-3-amina, un intermediario clave de nt-814. |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4068305B2 (ja) | 1999-02-24 | 2008-03-26 | エフ．ホフマン−ラ ロシュ アーゲー | ３−フェニルピリジン誘導体、およびそのｎｋ−１受容体拮抗薬としての用途 |
| DK1394150T3 (da) | 1999-02-24 | 2011-03-21 | Hoffmann La Roche | 4-phenylpyridinderivater og deres anvendelse som NK-1-receptorantagonister |
| SI1103545T1 (en) | 1999-11-29 | 2004-02-29 | F. Hoffmann-La Roche Ag | 2-(3,5-Bis-trifluoromethyl-phenyl)-N-methyl-N-(6-morpholin-4-yl-4-o-tolyl-pyridin-3-yl)-isobutyramide |
| NZ523273A (en) | 2000-07-14 | 2004-08-27 | F | N-oxides as NK1 receptor antagonist prodrugs of 4-phenyl-pyridine derivatives |
| TWI287003B (en) | 2000-07-24 | 2007-09-21 | Hoffmann La Roche | 4-phenyl-pyridine derivatives |
| TWI259180B (en) | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
| CA2444395C (en) | 2001-04-23 | 2010-12-21 | F. Hoffmann-La Roche Ag | Use of nk-1 receptor antagonists against benign prostatic hyperplasia |
| US20030083345A1 (en) | 2001-07-10 | 2003-05-01 | Torsten Hoffmann | Method of treatment and/or prevention of brain, spinal or nerve injury |
| US6849624B2 (en) | 2001-07-31 | 2005-02-01 | Hoffmann-La Roche Inc. | Aromatic and heteroaromatic substituted amides |
| DE602004008631T2 (de) * | 2003-07-03 | 2008-07-10 | F. Hoffmann-La Roche Ag | Duale nk1/nk3 antagonisten zur behandlung von schizophrenie |
| US20060030600A1 (en) | 2004-08-06 | 2006-02-09 | Patrick Schnider | Dual NK1/NK3 receptor antagonists for the treatment of schizophrenia |
| EP1863767B1 (en) | 2005-03-23 | 2009-03-11 | F. Hoffmann-Roche AG | Metabolites for nk-i antagonists for emesis |
| MY145713A (en) | 2005-09-09 | 2012-03-30 | Smithkline Beecham Corp | Hexahydropyrazino [2,1-c][1,4]oxazin-8(1h)-yl pyridine derivatives and their use in the treatment of psychotic disorders |
| SI1928427T1 (sl) | 2005-09-23 | 2010-03-31 | Hoffmann La Roche | Nove formulacije za doziranje |
| US8003797B2 (en) | 2007-08-09 | 2011-08-23 | Merck Sharp & Dohme Corp. | Pyridine carboxamide orexin receptor antagonists |
| GB0808747D0 (en) * | 2008-05-14 | 2008-06-18 | Glaxo Wellcome Mfg Pte Ltd | Novel compounds |
| WO2011054773A1 (en) * | 2009-11-03 | 2011-05-12 | Glaxosmithkline Llc | Novel lactam compounds |
| US8426450B1 (en) | 2011-11-29 | 2013-04-23 | Helsinn Healthcare Sa | Substituted 4-phenyl pyridines having anti-emetic effect |
| ES2671418T3 (es) * | 2013-11-08 | 2018-06-06 | Kissei Pharmaceutical Co., Ltd. | Derivado de carboximetilpiperidina |
-
2015
- 2015-05-06 TW TW104114465A patent/TWI649307B/zh active
- 2015-05-07 BR BR112016025984-0A patent/BR112016025984B1/pt active IP Right Grant
- 2015-05-07 EP EP15789561.6A patent/EP3141541B1/en active Active
- 2015-05-07 KR KR1020167032705A patent/KR102061544B1/ko active Active
- 2015-05-07 US US15/308,996 patent/US9708266B2/en active Active
- 2015-05-07 PL PL15789561T patent/PL3141541T3/pl unknown
- 2015-05-07 MX MX2016014566A patent/MX2016014566A/es active IP Right Grant
- 2015-05-07 WO PCT/JP2015/063154 patent/WO2015170693A1/ja not_active Ceased
- 2015-05-07 HU HUE15789561A patent/HUE042659T2/hu unknown
- 2015-05-07 SG SG11201609298TA patent/SG11201609298TA/en unknown
- 2015-05-07 CA CA2946523A patent/CA2946523C/en active Active
- 2015-05-07 JP JP2015528113A patent/JP5847362B1/ja active Active
- 2015-05-07 DK DK15789561.6T patent/DK3141541T3/en active
- 2015-05-07 ES ES15789561T patent/ES2704709T3/es active Active
- 2015-05-07 AU AU2015257007A patent/AU2015257007B2/en active Active
- 2015-05-07 RU RU2016147704A patent/RU2681316C2/ru active
- 2015-05-07 CN CN201580030418.XA patent/CN106414406B/zh active Active
- 2015-05-07 PT PT15789561T patent/PT3141541T/pt unknown
-
2016
- 2016-11-06 IL IL248772A patent/IL248772B/en active IP Right Grant
- 2016-11-14 ZA ZA2016/07847A patent/ZA201607847B/en unknown
-
2017
- 2017-06-22 US US15/630,238 patent/US10011568B2/en active Active
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