JP2010143943A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2010143943A5 JP2010143943A5 JP2010024303A JP2010024303A JP2010143943A5 JP 2010143943 A5 JP2010143943 A5 JP 2010143943A5 JP 2010024303 A JP2010024303 A JP 2010024303A JP 2010024303 A JP2010024303 A JP 2010024303A JP 2010143943 A5 JP2010143943 A5 JP 2010143943A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkoxy
- halogen
- phenyl
- substituted
- 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.)
- Granted
Links
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical group 0.000 claims 18
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 13
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 125000003118 aryl group Chemical group 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 150000008048 phenylpyrazoles Chemical class 0.000 claims 8
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000004754 (C2-C12) dialkylamino group Chemical group 0.000 claims 1
- 125000006828 (C2-C7) alkoxycarbonyl group Chemical group 0.000 claims 1
- PJZXYQHKCKLJLX-CQSZACIVSA-N 1-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carboxamide Chemical compound C[C@@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(N)=O)C=C1 PJZXYQHKCKLJLX-CQSZACIVSA-N 0.000 claims 1
- PJZXYQHKCKLJLX-AWEZNQCLSA-N 1-[4-[3-[(2s)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carboxamide Chemical compound C[C@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(N)=O)C=C1 PJZXYQHKCKLJLX-AWEZNQCLSA-N 0.000 claims 1
- LMOCKQBKIUCUBU-QGZVFWFLSA-N 2-[2-hydroxyethyl-[1-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carbonyl]amino]acetic acid Chemical compound C[C@@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)N(CCO)CC(O)=O)C=C1 LMOCKQBKIUCUBU-QGZVFWFLSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000036864 Attention deficit/hyperactivity disease Diseases 0.000 claims 1
- 208000017164 Chronobiology disease Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010012289 Dementia Diseases 0.000 claims 1
- 208000030814 Eating disease Diseases 0.000 claims 1
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 206010039085 Rhinitis allergic Diseases 0.000 claims 1
- 201000010105 allergic rhinitis Diseases 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 235000014632 disordered eating Nutrition 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- -1 hydroxy, Hydroxy Chemical group 0.000 claims 1
- QIYOBDVDGIIVEJ-GOSISDBHSA-N n,n-bis(2-hydroxyethyl)-1-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carboxamide Chemical compound C[C@@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)N(CCO)CCO)C=C1 QIYOBDVDGIIVEJ-GOSISDBHSA-N 0.000 claims 1
- ROQMVNDSPDGQJP-UHFFFAOYSA-N n,n-dimethyl-1-[4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound CC1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)N(C)C)C=C1 ROQMVNDSPDGQJP-UHFFFAOYSA-N 0.000 claims 1
- PZRVQACPBLRYTI-MRXNPFEDSA-N n-(2-hydroxyethyl)-1-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carboxamide Chemical compound C[C@@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NCCO)C=C1 PZRVQACPBLRYTI-MRXNPFEDSA-N 0.000 claims 1
- GRQMLKRQGYDTPY-UHFFFAOYSA-N n-(4-fluorophenyl)-1-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]pyrazole-4-carboxamide Chemical compound C1=CC(F)=CC=C1NC(=O)C1=CN(C=2C=CC(OCCCN3CCCC3)=CC=2)N=C1 GRQMLKRQGYDTPY-UHFFFAOYSA-N 0.000 claims 1
- ZJHLDPLSPGJKEZ-UHFFFAOYSA-N n-(4-fluorophenyl)-1-[4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound CC1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NC=2C=CC(F)=CC=2)C=C1 ZJHLDPLSPGJKEZ-UHFFFAOYSA-N 0.000 claims 1
- KTFZYZYJJHRYCS-UHFFFAOYSA-N n-(4-methylphenyl)-1-[4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound CC1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NC=2C=CC(C)=CC=2)C=C1 KTFZYZYJJHRYCS-UHFFFAOYSA-N 0.000 claims 1
- RBOZCHRUDZMTBT-UHFFFAOYSA-N n-[(4-fluorophenyl)methyl]-1-[4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound CC1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NCC=2C=CC(F)=CC=2)C=C1 RBOZCHRUDZMTBT-UHFFFAOYSA-N 0.000 claims 1
- TYMPTWLKVMOQKK-GOSISDBHSA-N n-[2-(2-hydroxyethoxy)ethyl]-1-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carboxamide Chemical compound C[C@@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NCCOCCO)C=C1 TYMPTWLKVMOQKK-GOSISDBHSA-N 0.000 claims 1
- JTFNUJVNNVEWOB-UHFFFAOYSA-N n-tert-butyl-1-[4-(3-pyrrolidin-1-ylpropoxy)phenyl]pyrazole-4-carboxamide Chemical compound C1=C(C(=O)NC(C)(C)C)C=NN1C(C=C1)=CC=C1OCCCN1CCCC1 JTFNUJVNNVEWOB-UHFFFAOYSA-N 0.000 claims 1
- ULYGNJDYFKUSCV-UHFFFAOYSA-N n-tert-butyl-1-[4-[3-(2,5-dimethylpyrrolidin-1-yl)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound CC1CCC(C)N1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NC(C)(C)C)C=C1 ULYGNJDYFKUSCV-UHFFFAOYSA-N 0.000 claims 1
- BRZFMWDQFKUEDE-UHFFFAOYSA-N n-tert-butyl-1-[4-[3-(2-methylpyrrolidin-1-yl)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound CC1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)NC(C)(C)C)C=C1 BRZFMWDQFKUEDE-UHFFFAOYSA-N 0.000 claims 1
- KIYXNAQGDBHYKC-UHFFFAOYSA-N n-tert-butyl-1-[4-[3-(diethylamino)propoxy]phenyl]pyrazole-4-carboxamide Chemical compound C1=CC(OCCCN(CC)CC)=CC=C1N1N=CC(C(=O)NC(C)(C)C)=C1 KIYXNAQGDBHYKC-UHFFFAOYSA-N 0.000 claims 1
- 201000003631 narcolepsy Diseases 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 201000002859 sleep apnea Diseases 0.000 claims 1
- 208000019116 sleep disease Diseases 0.000 claims 1
- BPPLZEUEZFFAGT-HXUWFJFHSA-N tert-butyl 2-[2-hydroxyethyl-[1-[4-[3-[(2r)-2-methylpyrrolidin-1-yl]propoxy]phenyl]pyrazole-4-carbonyl]amino]acetate Chemical compound C[C@@H]1CCCN1CCCOC1=CC=C(N2N=CC(=C2)C(=O)N(CCO)CC(=O)OC(C)(C)C)C=C1 BPPLZEUEZFFAGT-HXUWFJFHSA-N 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- 0 CC(CC(C)COc(cc1)ccc1-[n]1ncc(*)c1)CN(*)* Chemical compound CC(CC(C)COc(cc1)ccc1-[n]1ncc(*)c1)CN(*)* 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2010024303A JP5375639B2 (ja) | 2007-11-13 | 2010-02-05 | フェニルピラゾール誘導体 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2007294040 | 2007-11-13 | ||
| JP2007294040 | 2007-11-13 | ||
| JP2008153736 | 2008-06-12 | ||
| JP2008153736 | 2008-06-12 | ||
| JP2010024303A JP5375639B2 (ja) | 2007-11-13 | 2010-02-05 | フェニルピラゾール誘導体 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009541174A Division JP4543344B2 (ja) | 2007-11-13 | 2008-11-13 | フェニルピラゾール誘導体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010143943A JP2010143943A (ja) | 2010-07-01 |
| JP2010143943A5 true JP2010143943A5 (enExample) | 2012-01-05 |
| JP5375639B2 JP5375639B2 (ja) | 2013-12-25 |
Family
ID=40638800
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009541174A Expired - Fee Related JP4543344B2 (ja) | 2007-11-13 | 2008-11-13 | フェニルピラゾール誘導体 |
| JP2010024303A Expired - Fee Related JP5375639B2 (ja) | 2007-11-13 | 2010-02-05 | フェニルピラゾール誘導体 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009541174A Expired - Fee Related JP4543344B2 (ja) | 2007-11-13 | 2008-11-13 | フェニルピラゾール誘導体 |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US7888354B2 (enExample) |
| EP (1) | EP2221298B1 (enExample) |
| JP (2) | JP4543344B2 (enExample) |
| KR (1) | KR101571176B1 (enExample) |
| CN (1) | CN101855211B (enExample) |
| AU (1) | AU2008321823B2 (enExample) |
| BR (1) | BRPI0820432B8 (enExample) |
| CA (1) | CA2705502C (enExample) |
| CY (1) | CY1114877T1 (enExample) |
| DK (1) | DK2221298T3 (enExample) |
| ES (1) | ES2436146T3 (enExample) |
| HR (1) | HRP20131060T1 (enExample) |
| IL (2) | IL205509A (enExample) |
| MX (1) | MX2010005225A (enExample) |
| MY (1) | MY173546A (enExample) |
| NZ (1) | NZ585661A (enExample) |
| PH (1) | PH12012501917A1 (enExample) |
| PL (1) | PL2221298T3 (enExample) |
| PT (1) | PT2221298E (enExample) |
| RS (1) | RS53125B (enExample) |
| RU (1) | RU2480456C2 (enExample) |
| SI (1) | SI2221298T1 (enExample) |
| WO (1) | WO2009063953A1 (enExample) |
| ZA (1) | ZA201003111B (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20100113776A1 (en) * | 2006-12-14 | 2010-05-06 | Taisho Pharmaceutical Co.,Ltd. | Pyrazole derivative |
| CN101855211B (zh) * | 2007-11-13 | 2013-06-12 | 大正制药株式会社 | 苯基吡唑衍生物 |
| JP5740838B2 (ja) * | 2009-05-12 | 2015-07-01 | 大正製薬株式会社 | フェニルピラゾール誘導体 |
| BR112014013461A2 (pt) * | 2011-12-08 | 2017-06-13 | Taisho Pharmaceutical Co Ltd | derivado de fenilpirrol |
| US20150045553A1 (en) * | 2011-12-27 | 2015-02-12 | Taisho Pharmaceutical Co., Ltd | Phenyltriazole derivative |
| WO2013151982A1 (en) | 2012-04-03 | 2013-10-10 | Arena Pharmaceuticals, Inc. | Methods and compounds useful in treating pruritus, and methods for identifying such compounds |
| EP2928474B1 (en) | 2012-12-07 | 2018-11-14 | ChemoCentryx, Inc. | Diazole lactams |
| JP6263553B2 (ja) * | 2013-01-17 | 2018-01-17 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | Ｃｎｓ疾患の処置のためのオキシトシン受容体アゴニスト |
| SG11201808626WA (en) | 2016-04-07 | 2018-10-30 | Chemocentryx Inc | Reducing tumor burden by administering ccr1 antagonists in combination with pd-1 inhibitors or pd-l1 inhibitors |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL104311A (en) * | 1992-02-05 | 1997-07-13 | Fujisawa Pharmaceutical Co | Pyrazole derivatives, processes for the preparation thereof and pharmaceutical compositions containing the same |
| ATE354568T1 (de) | 2000-08-08 | 2007-03-15 | Ortho Mcneil Pharm Inc | Nicht-imidazol aryloxypiperidine als h3 rezeptor liganden |
| US6316475B1 (en) * | 2000-11-17 | 2001-11-13 | Abbott Laboratories | Aminoalkoxybiphenylcarboxamides as histamine-3 receptor ligands and their therapeutic applications |
| EP1370546A2 (en) * | 2001-03-16 | 2003-12-17 | Abbott Laboratories | Novel amines as histamine-3 receptor ligands and their therapeutic applications |
| AU2004257025B9 (en) | 2003-06-27 | 2010-05-27 | Msd K.K. | Heteroaryloxy nitrogenous saturated heterocyclic derivative |
| US7423147B2 (en) | 2004-03-31 | 2008-09-09 | Janssen Pharmaceutical, N.V. | Pyridine compounds as histamine H3 modulators |
| GB0408083D0 (en) | 2004-04-08 | 2004-05-12 | Glaxo Group Ltd | Novel compounds |
| FR2870846B1 (fr) * | 2004-05-25 | 2006-08-04 | Sanofi Synthelabo | Derives de tetrahydroisoquinolylsulfonamides, leur preparation et leur utilisation en therapeutique |
| SE0401971D0 (sv) | 2004-08-02 | 2004-08-02 | Astrazeneca Ab | Piperidne derivatives |
| CN101006082B (zh) | 2004-08-23 | 2010-09-29 | 伊莱利利公司 | 组胺h3受体药剂、制备方法和治疗用途 |
| MX2007004465A (es) | 2004-10-19 | 2007-05-07 | Hoffmann La Roche | Derivados de quinolina. |
| WO2006046131A1 (en) | 2004-10-29 | 2006-05-04 | Pfizer Products Inc. | Tetralin histamine-3 receptor antagonists |
| CA2588867A1 (en) | 2004-12-01 | 2006-06-08 | Banyu Pharmaceutical Co., Ltd. | Substituted pyridone derivative |
| US20090306052A1 (en) | 2004-12-07 | 2009-12-10 | Glaxo Group Limited | Indenyl derivatives and use thereof for the treatment of neurological disorders |
| CA2602336A1 (en) * | 2005-03-31 | 2006-10-05 | Ucb Pharma S.A. | Compounds comprising an oxazole or thiazole moiety, processes for making them, and their uses |
| AU2006232871B9 (en) | 2005-04-01 | 2011-11-24 | Eli Lilly And Company | Histamine H3 receptor agents, preparation and therapeutic uses |
| DE102005033448A1 (de) * | 2005-07-18 | 2007-01-25 | Josef Gail | Druckgas-Zylinderläufermotor |
| GB0514812D0 (en) * | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| GB0514811D0 (en) * | 2005-07-19 | 2005-08-24 | Glaxo Group Ltd | Compounds |
| ATE525072T1 (de) | 2006-02-09 | 2011-10-15 | Athersys Inc | Pyrazole zur behandlung von adipositas und anderen zns-erkrankungen |
| US20100113776A1 (en) | 2006-12-14 | 2010-05-06 | Taisho Pharmaceutical Co.,Ltd. | Pyrazole derivative |
| CN101711232A (zh) * | 2007-04-12 | 2010-05-19 | Dsm精细化学奥地利Nfg两合公司 | 邻-氯甲基苯基乙醛酸酯、(e)-2-(2-氯甲基苯基)-2-烷氧亚胺基乙酸酯的改进制备方法以及用于这些制备方法的新型中间体 |
| CN101855211B (zh) * | 2007-11-13 | 2013-06-12 | 大正制药株式会社 | 苯基吡唑衍生物 |
-
2008
- 2008-11-13 CN CN200880115707XA patent/CN101855211B/zh not_active Expired - Fee Related
- 2008-11-13 AU AU2008321823A patent/AU2008321823B2/en not_active Ceased
- 2008-11-13 SI SI200831096T patent/SI2221298T1/sl unknown
- 2008-11-13 HR HRP20131060AT patent/HRP20131060T1/hr unknown
- 2008-11-13 KR KR1020107009179A patent/KR101571176B1/ko not_active Expired - Fee Related
- 2008-11-13 MX MX2010005225A patent/MX2010005225A/es active IP Right Grant
- 2008-11-13 JP JP2009541174A patent/JP4543344B2/ja not_active Expired - Fee Related
- 2008-11-13 RU RU2010123924/04A patent/RU2480456C2/ru active
- 2008-11-13 PT PT88497250T patent/PT2221298E/pt unknown
- 2008-11-13 US US12/741,754 patent/US7888354B2/en active Active
- 2008-11-13 NZ NZ585661A patent/NZ585661A/en not_active IP Right Cessation
- 2008-11-13 PL PL08849725T patent/PL2221298T3/pl unknown
- 2008-11-13 ES ES08849725T patent/ES2436146T3/es active Active
- 2008-11-13 MY MYPI2010002187A patent/MY173546A/en unknown
- 2008-11-13 RS RS20130586A patent/RS53125B/sr unknown
- 2008-11-13 DK DK08849725.0T patent/DK2221298T3/da active
- 2008-11-13 CA CA2705502A patent/CA2705502C/en active Active
- 2008-11-13 WO PCT/JP2008/070712 patent/WO2009063953A1/ja not_active Ceased
- 2008-11-13 BR BRPI0820432A patent/BRPI0820432B8/pt not_active IP Right Cessation
- 2008-11-13 PH PH1/2012/501917A patent/PH12012501917A1/en unknown
- 2008-11-13 EP EP08849725.0A patent/EP2221298B1/en active Active
-
2010
- 2010-02-05 JP JP2010024303A patent/JP5375639B2/ja not_active Expired - Fee Related
- 2010-05-03 IL IL205509A patent/IL205509A/en active IP Right Grant
- 2010-05-04 ZA ZA2010/03111A patent/ZA201003111B/en unknown
- 2010-11-22 US US12/951,964 patent/US8183387B2/en not_active Expired - Fee Related
- 2010-11-22 US US12/951,978 patent/US8193176B2/en not_active Expired - Fee Related
-
2014
- 2014-01-09 CY CY20141100018T patent/CY1114877T1/el unknown
- 2014-12-04 IL IL236083A patent/IL236083A/en active IP Right Grant