JP2004536104A5 - - Google Patents
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- JP2004536104A5 JP2004536104A5 JP2003510038A JP2003510038A JP2004536104A5 JP 2004536104 A5 JP2004536104 A5 JP 2004536104A5 JP 2003510038 A JP2003510038 A JP 2003510038A JP 2003510038 A JP2003510038 A JP 2003510038A JP 2004536104 A5 JP2004536104 A5 JP 2004536104A5
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- Prior art keywords
- branched
- alkyl
- linear
- patient
- aryl
- 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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- 125000003118 aryl group Chemical group 0.000 description 39
- 150000001875 compounds Chemical class 0.000 description 37
- 125000001072 heteroaryl group Chemical group 0.000 description 36
- 238000000034 method Methods 0.000 description 21
- 125000000753 cycloalkyl group Chemical group 0.000 description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 14
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 12
- 201000010099 disease Diseases 0.000 description 10
- 239000000203 mixture Substances 0.000 description 10
- 125000000304 alkynyl group Chemical group 0.000 description 9
- 125000000392 cycloalkenyl group Chemical group 0.000 description 9
- 239000008194 pharmaceutical composition Substances 0.000 description 9
- 208000019901 Anxiety disease Diseases 0.000 description 8
- 0 CC1C(N*)=CC=CC1 Chemical compound CC1C(N*)=CC=CC1 0.000 description 8
- 101150104680 MCH1 gene Proteins 0.000 description 8
- 208000008589 Obesity Diseases 0.000 description 8
- 101100382379 Rattus norvegicus Cap1 gene Proteins 0.000 description 8
- 208000000921 Urge Urinary Incontinence Diseases 0.000 description 8
- 239000005557 antagonist Substances 0.000 description 8
- 230000036506 anxiety Effects 0.000 description 8
- -1 cyclopentane Nyl Chemical group 0.000 description 8
- 235000020824 obesity Nutrition 0.000 description 8
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 8
- 206010046494 urge incontinence Diseases 0.000 description 8
- 230000004580 weight loss Effects 0.000 description 8
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 7
- 206010020853 Hypertonic bladder Diseases 0.000 description 6
- 208000009722 Overactive Urinary Bladder Diseases 0.000 description 6
- 125000000217 alkyl group Chemical group 0.000 description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 description 6
- 208000020629 overactive bladder Diseases 0.000 description 6
- 238000009472 formulation Methods 0.000 description 5
- UJOBWOGCFQCDNV-UHFFFAOYSA-N 9H-carbazole Chemical compound C1=CC=C2C3=CC=CC=C3NC2=C1 UJOBWOGCFQCDNV-UHFFFAOYSA-N 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 208000024891 symptom Diseases 0.000 description 4
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 description 3
- 125000003342 alkenyl group Chemical group 0.000 description 3
- 125000004103 aminoalkyl group Chemical group 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- XKJCHHZQLQNZHY-UHFFFAOYSA-N phthalimide Chemical compound C1=CC=C2C(=O)NC(=O)C2=C1 XKJCHHZQLQNZHY-UHFFFAOYSA-N 0.000 description 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 description 2
- 238000011914 asymmetric synthesis Methods 0.000 description 2
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 description 2
- 150000003857 carboxamides Chemical class 0.000 description 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 2
- 125000003709 fluoroalkyl group Chemical group 0.000 description 2
- 125000005842 heteroatom Chemical group 0.000 description 2
- PQNFLJBBNBOBRQ-UHFFFAOYSA-N indane Chemical compound C1=CC=C2CCCC2=C1 PQNFLJBBNBOBRQ-UHFFFAOYSA-N 0.000 description 2
- 125000001041 indolyl group Chemical group 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 229910052757 nitrogen Inorganic materials 0.000 description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000829 suppository Substances 0.000 description 2
- 125000000335 thiazolyl group Chemical group 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 1
- 150000001204 N-oxides Chemical class 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
- 150000001335 aliphatic alkanes Chemical class 0.000 description 1
- 125000000278 alkyl amino alkyl group Chemical group 0.000 description 1
- 125000002877 alkyl aryl group Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 description 1
- 125000004603 benzisoxazolyl group Chemical group O1N=C(C2=C1C=CC=C2)* 0.000 description 1
- 125000005605 benzo group Chemical group 0.000 description 1
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000004202 carbamide Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 125000004432 carbon atom Chemical group C* 0.000 description 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 description 1
- 238000004587 chromatography analysis Methods 0.000 description 1
- 125000000259 cinnolinyl group Chemical group N1=NC(=CC2=CC=CC=C12)* 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 150000002466 imines Chemical class 0.000 description 1
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 description 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 description 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 description 1
- 125000003406 indolizinyl group Chemical group C=1(C=CN2C=CC=CC12)* 0.000 description 1
- 125000000904 isoindolyl group Chemical group C=1(NC=C2C=CC=CC12)* 0.000 description 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 description 1
- 125000002183 isoquinolinyl group Chemical group C1(=NC=CC2=CC=CC=C12)* 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 125000001624 naphthyl group Chemical group 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 125000005545 phthalimidyl group Chemical group 0.000 description 1
- 125000001844 prenyl group Chemical group [H]C([*])([H])C([H])=C(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001042 pteridinyl group Chemical group N1=C(N=CC2=NC=CN=C12)* 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US89979401A | 2001-07-05 | 2001-07-05 | |
| US4258202A | 2002-01-09 | 2002-01-09 | |
| PCT/US2002/021063 WO2003004027A1 (en) | 2001-07-05 | 2002-07-03 | Substituted anilinic piperidines as mch selective antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2004536104A JP2004536104A (ja) | 2004-12-02 |
| JP2004536104A5 true JP2004536104A5 (https=) | 2006-01-05 |
Family
ID=26719414
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003510038A Withdrawn JP2004536104A (ja) | 2001-07-05 | 2002-07-03 | Ｍｃｈ選択的アンタゴニストとしての置換されたアニリン−ピペリジン誘導体 |
Country Status (15)
| Country | Link |
|---|---|
| EP (1) | EP1411942A4 (https=) |
| JP (1) | JP2004536104A (https=) |
| KR (1) | KR20040027870A (https=) |
| CN (1) | CN1671386A (https=) |
| CA (1) | CA2454613A1 (https=) |
| CO (1) | CO5670352A2 (https=) |
| EA (1) | EA005934B1 (https=) |
| HU (1) | HUP0401880A2 (https=) |
| IL (1) | IL159697A0 (https=) |
| IS (1) | IS7085A (https=) |
| MX (1) | MXPA03011886A (https=) |
| NO (1) | NO20040028L (https=) |
| NZ (1) | NZ530221A (https=) |
| PL (1) | PL366624A1 (https=) |
| WO (1) | WO2003004027A1 (https=) |
Families Citing this family (104)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6727264B1 (en) | 2001-07-05 | 2004-04-27 | Synaptic Pharmaceutical Corporation | Substituted anilinic piperidines as MCH selective antagonists |
| US7105544B2 (en) * | 2001-07-05 | 2006-09-12 | Synaptic Pharmaceutical Corporation | Substituted alkyl amido piperidines |
| US7199135B2 (en) | 2001-07-05 | 2007-04-03 | H. Lundbeck A/S | Substituted alkyl amido piperidines |
| CA2468015A1 (en) | 2001-11-27 | 2003-06-05 | Merck & Co., Inc. | 2-aminoquinoline compounds |
| EP1465888A2 (en) | 2002-01-10 | 2004-10-13 | Neurogen Corporation | Melanin concentrating hormone receptor ligands: substituted benzoimidazole analogues |
| CA2473236A1 (en) | 2002-01-10 | 2003-07-24 | Neurogen Corporation | Melanin concentrating hormone receptor ligands: substituted 2-(4-benzyl-piperazin-1-ylmethyl)- and 2-(4-benzyl-diazepan-1-ylmethyl)-1h-benzoimidazole analogues |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| UA77536C2 (en) | 2002-07-03 | 2006-12-15 | Lundbeck & Co As H | Secondary aminoaniline piperidines as mch1 antagonists and their use |
| UA77814C2 (en) | 2002-07-03 | 2007-01-15 | Lundbeck & Co As H | Spirocyclic piperidines as antagonists of mch1 and use thereof |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| BRPI0407088A (pt) * | 2003-01-28 | 2006-01-24 | Aventis Pharma Sa | Produtos n-aril-heteroaromáticos, composições contendo os mesmos e seu uso |
| FR2850379B1 (fr) * | 2003-01-28 | 2006-11-17 | Aventis Pharma Sa | Produits n-aryl-heteroaromatiques, compositions les contenant et utilisation |
| US7727998B2 (en) * | 2003-02-10 | 2010-06-01 | Banyu Pharmaceutical Co., Ltd. | Melanin-concentrating hormone receptor antagonists containing piperidine derivatives as the active ingredient |
| CN100448870C (zh) * | 2003-05-21 | 2009-01-07 | 万有制药株式会社 | 2-氨基喹啉衍生物 |
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| EP2308839B1 (en) * | 2005-04-20 | 2017-03-01 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compounds |
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| BRPI0616463A2 (pt) | 2005-09-29 | 2011-06-21 | Merck & Co Inc | composto, composição farmacêutica, e, uso de um composto |
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| US8158791B2 (en) | 2005-11-10 | 2012-04-17 | Msd K.K. | Aza-substituted spiro derivatives |
| JP5015172B2 (ja) | 2005-12-23 | 2012-08-29 | エフ．ホフマン−ラ ロシュ アーゲー | アリール−イソオキサゾロ−４−イル−オキサジアゾール誘導体 |
| ATE527255T1 (de) | 2005-12-27 | 2011-10-15 | Hoffmann La Roche | Aryl-isoxazol-4-yl-imidazol-derivate |
| WO2007082806A1 (en) | 2006-01-17 | 2007-07-26 | F. Hoffmann-La Roche Ag | Aryl-isoxazol-4-yl-imidazo[1,2-a]pyridine useful for the treatment of alzheimer’s disease via gaba receptors |
| CN101484424B (zh) * | 2006-02-28 | 2014-05-14 | 达特神经科学(开曼)有限公司 | 治疗化合物 |
| AU2007267183B2 (en) | 2006-05-31 | 2011-10-20 | F. Hoffmann-La Roche Ag | Aryl-4-ethynyl-isoxazole derivatives |
| JP2010500300A (ja) | 2006-08-08 | 2010-01-07 | サノフィ−アベンティス | アリールアミノアリール−アルキル−置換イミダゾリジン−２，４−ジオン、それらの製造法、それらの化合物を含有する薬剤、およびそれらの使用 |
| JP5489333B2 (ja) | 2006-09-22 | 2014-05-14 | メルク・シャープ・アンド・ドーム・コーポレーション | 脂肪酸合成阻害剤を用いた治療の方法 |
| AU2007301126A1 (en) | 2006-09-28 | 2008-04-03 | Banyu Pharmaceutical Co., Ltd. | Diaryl ketimine derivative |
| CA2682727C (en) | 2007-04-02 | 2016-03-22 | Banyu Pharmaceutical Co., Ltd. | Indoledione derivative |
| US8198307B2 (en) * | 2007-05-11 | 2012-06-12 | Korea Research Institute Of Chemical Technology | Imidazole derivatives having aryl piperidine substituent, method for preparation thereof and pharmaceutical compositions containing same |
| US8969514B2 (en) | 2007-06-04 | 2015-03-03 | Synergy Pharmaceuticals, Inc. | Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases |
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| EP2810951B1 (en) | 2008-06-04 | 2017-03-15 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| AU2009261248A1 (en) | 2008-06-19 | 2009-12-23 | Banyu Pharmaceutical Co., Ltd. | Spirodiamine-diarylketoxime derivative |
| WO2010003624A2 (en) | 2008-07-09 | 2010-01-14 | Sanofi-Aventis | Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof |
| EP3241839B1 (en) | 2008-07-16 | 2019-09-04 | Bausch Health Ireland Limited | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
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| JP5635991B2 (ja) | 2008-10-30 | 2014-12-03 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | イソニコチンアミドオレキシン受容体アンタゴニスト |
| JP5557845B2 (ja) | 2008-10-31 | 2014-07-23 | メルク・シャープ・アンド・ドーム・コーポレーション | 糖尿病用剤として有用な新規環状ベンゾイミダゾール誘導体 |
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| BRPI1013766A2 (pt) | 2009-05-07 | 2016-04-05 | Hoffmann La Roche | "derivados de isoxazol-piridina como moduladores de gaba" |
| AU2010270464B2 (en) * | 2009-07-06 | 2015-01-22 | Syngenta Participations Ag | Insecticidal compounds |
| MX2012001729A (es) | 2009-08-26 | 2012-06-13 | Sanofi Sa | Nuevos hidratos cristalinos de fluoroglicosido heteroaromatico, productos farmaceuticos que comprenden estos compuestos, y su empleo. |
| US8895596B2 (en) | 2010-02-25 | 2014-11-25 | Merck Sharp & Dohme Corp | Cyclic benzimidazole derivatives useful as anti-diabetic agents |
| RU2436786C1 (ru) * | 2010-07-23 | 2011-12-20 | Александр Васильевич Иващенко | Замещенные индолы, противовирусный активный компонент, способ получения и применения |
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Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9810671D0 (en) * | 1998-05-18 | 1998-07-15 | Pfizer Ltd | Anti-pruritic agents |
| GB9912413D0 (en) * | 1999-05-28 | 1999-07-28 | Pfizer Ltd | Compounds useful in therapy |
| JP2004502423A (ja) * | 2000-07-05 | 2004-01-29 | シナプティック・ファーマスーティカル・コーポレーション | ヒトメラニン濃縮ホルモン受容体（ｍｃｈ１）をコードするｄｎａ及びその使用 |
-
2002
- 2002-07-03 EP EP02746843A patent/EP1411942A4/en not_active Withdrawn
- 2002-07-03 MX MXPA03011886A patent/MXPA03011886A/es not_active Application Discontinuation
- 2002-07-03 EA EA200400146A patent/EA005934B1/ru not_active IP Right Cessation
- 2002-07-03 JP JP2003510038A patent/JP2004536104A/ja not_active Withdrawn
- 2002-07-03 HU HU0401880A patent/HUP0401880A2/hu unknown
- 2002-07-03 WO PCT/US2002/021063 patent/WO2003004027A1/en not_active Ceased
- 2002-07-03 PL PL02366624A patent/PL366624A1/xx not_active Application Discontinuation
- 2002-07-03 CN CNA028172124A patent/CN1671386A/zh active Pending
- 2002-07-03 NZ NZ530221A patent/NZ530221A/xx unknown
- 2002-07-03 CA CA002454613A patent/CA2454613A1/en not_active Abandoned
- 2002-07-03 KR KR10-2004-7000087A patent/KR20040027870A/ko not_active Ceased
- 2002-07-03 IL IL15969702A patent/IL159697A0/xx unknown
-
2003
- 2003-12-18 IS IS7085A patent/IS7085A/is unknown
-
2004
- 2004-01-05 NO NO20040028A patent/NO20040028L/no not_active Application Discontinuation
- 2004-02-02 CO CO04007748A patent/CO5670352A2/es not_active Application Discontinuation
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