JP2004505085A5 - - Google Patents
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- JP2004505085A5 JP2004505085A5 JP2002515898A JP2002515898A JP2004505085A5 JP 2004505085 A5 JP2004505085 A5 JP 2004505085A5 JP 2002515898 A JP2002515898 A JP 2002515898A JP 2002515898 A JP2002515898 A JP 2002515898A JP 2004505085 A5 JP2004505085 A5 JP 2004505085A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- hydrogen
- alkyl
- formula
- cycloalkyl
- 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
- 150000001875 compounds Chemical class 0.000 description 55
- 229910052739 hydrogen Inorganic materials 0.000 description 35
- 239000001257 hydrogen Substances 0.000 description 35
- 125000000217 alkyl group Chemical group 0.000 description 28
- 150000002431 hydrogen Chemical class 0.000 description 28
- 125000000753 cycloalkyl group Chemical group 0.000 description 26
- 238000000034 method Methods 0.000 description 21
- -1 1H-pyrrolo (2,3-b) pyridin-3-ylmethyl Chemical group 0.000 description 17
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 9
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 8
- 125000005161 aryl oxy carbonyl group Chemical group 0.000 description 8
- 125000000623 heterocyclic group Chemical group 0.000 description 8
- 238000004519 manufacturing process Methods 0.000 description 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 6
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 6
- 125000004093 cyano group Chemical group *C#N 0.000 description 6
- 125000003545 alkoxy group Chemical group 0.000 description 5
- 125000005078 alkoxycarbonylalkyl group Chemical group 0.000 description 5
- 125000005242 carbamoyl alkyl group Chemical group 0.000 description 5
- 125000001188 haloalkyl group Chemical group 0.000 description 5
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 229940086609 Lipase inhibitor Drugs 0.000 description 4
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 description 4
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 description 4
- 125000004448 alkyl carbonyl group Chemical group 0.000 description 4
- 125000004390 alkyl sulfonyl group Chemical group 0.000 description 4
- 125000004414 alkyl thio group Chemical group 0.000 description 4
- 125000003710 aryl alkyl group Chemical group 0.000 description 4
- 125000005129 aryl carbonyl group Chemical group 0.000 description 4
- 125000003118 aryl group Chemical group 0.000 description 4
- 125000004391 aryl sulfonyl group Chemical group 0.000 description 4
- 125000005110 aryl thio group Chemical group 0.000 description 4
- 125000004104 aryloxy group Chemical group 0.000 description 4
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 description 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 4
- 208000015114 central nervous system disease Diseases 0.000 description 4
- 239000003638 chemical reducing agent Substances 0.000 description 4
- 125000004473 dialkylaminocarbonyl group Chemical group 0.000 description 4
- 239000003814 drug Substances 0.000 description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 4
- 125000001160 methoxycarbonyl group Chemical group [H]C([H])([H])OC(*)=O 0.000 description 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 description 4
- 125000001400 nonyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 4
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 4
- 208000008589 Obesity Diseases 0.000 description 3
- 125000004438 haloalkoxy group Chemical group 0.000 description 3
- 235000020824 obesity Nutrition 0.000 description 3
- 239000008194 pharmaceutical composition Substances 0.000 description 3
- 238000011282 treatment Methods 0.000 description 3
- 0 *C(c1c(*)c(c(*)c(*)c(*)c2*)c2[n]1)=O Chemical compound *C(c1c(*)c(c(*)c(*)c(*)c2*)c2[n]1)=O 0.000 description 2
- 208000024172 Cardiovascular disease Diseases 0.000 description 2
- 208000018522 Gastrointestinal disease Diseases 0.000 description 2
- 125000005081 alkoxyalkoxyalkyl group Chemical group 0.000 description 2
- 230000003542 behavioural effect Effects 0.000 description 2
- 125000002837 carbocyclic group Chemical group 0.000 description 2
- 125000004432 carbon atom Chemical group C* 0.000 description 2
- 210000003169 central nervous system Anatomy 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 150000002148 esters Chemical class 0.000 description 2
- 208000015181 infectious disease Diseases 0.000 description 2
- 230000002458 infectious effect Effects 0.000 description 2
- AHLBNYSZXLDEJQ-FWEHEUNISA-N orlistat Chemical group CCCCCCCCCCC[C@H](OC(=O)[C@H](CC(C)C)NC=O)C[C@@H]1OC(=O)[C@H]1CCCCCC AHLBNYSZXLDEJQ-FWEHEUNISA-N 0.000 description 2
- 229960001243 orlistat Drugs 0.000 description 2
- 239000000546 pharmaceutical excipient Substances 0.000 description 2
- 150000003839 salts Chemical class 0.000 description 2
- 239000012453 solvate Substances 0.000 description 2
- 231100000331 toxic Toxicity 0.000 description 2
- 230000002588 toxic effect Effects 0.000 description 2
- NGNJCNYNDBMXSG-ZWNOBZJWSA-N (4r,10ar)-4,6,7-trimethyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound C1=C(C)C(C)=C2N3[C@H](C)CNC[C@H]3CC2=C1 NGNJCNYNDBMXSG-ZWNOBZJWSA-N 0.000 description 1
- OTCYUUXMBOVVSQ-ZYHUDNBSSA-N (4r,10ar)-4,6-dimethyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound C1=CC(C)=C2N3[C@H](C)CNC[C@H]3CC2=C1 OTCYUUXMBOVVSQ-ZYHUDNBSSA-N 0.000 description 1
- GKCUTGZGZISWAV-MWLCHTKSSA-N (4r,10ar)-4,8-dimethyl-7-(trifluoromethyl)-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound CC1=C(C(F)(F)F)C=C2N3[C@H](C)CNC[C@H]3CC2=C1 GKCUTGZGZISWAV-MWLCHTKSSA-N 0.000 description 1
- SYNUFLXJJGLJER-BXKDBHETSA-N (4r,10ar)-4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole-6-carbonitrile Chemical compound C1=CC(C#N)=C2N3[C@H](C)CNC[C@H]3CC2=C1 SYNUFLXJJGLJER-BXKDBHETSA-N 0.000 description 1
- OFZCNKHDZGJKCK-VXGBXAGGSA-N (4r,10ar)-7-bromo-4-ethyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound C1=C(Br)C=C2N3[C@H](CC)CNC[C@H]3CC2=C1 OFZCNKHDZGJKCK-VXGBXAGGSA-N 0.000 description 1
- XWXVGQFTZHFUNL-LDYMZIIASA-N (4r,10ar)-7-bromo-4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound C1=C(Br)C=C2N3[C@H](C)CNC[C@H]3CC2=C1 XWXVGQFTZHFUNL-LDYMZIIASA-N 0.000 description 1
- XTQKZPARPUBXCZ-LDYMZIIASA-N (4r,10ar)-7-chloro-4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound C1=C(Cl)C=C2N3[C@H](C)CNC[C@H]3CC2=C1 XTQKZPARPUBXCZ-LDYMZIIASA-N 0.000 description 1
- ZFJVQQQPMHYSOA-NEPJUHHUSA-N (4r,10as)-4,6,9-trimethyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound CC1=CC=C(C)C2=C1N1[C@H](C)CNC[C@@H]1C2 ZFJVQQQPMHYSOA-NEPJUHHUSA-N 0.000 description 1
- SZWVUASESVZMCY-KCJUWKMLSA-N (4r,10as)-7-chloro-4,6-dimethyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indole Chemical compound C1=C(Cl)C(C)=C2N3[C@H](C)CNC[C@@H]3CC2=C1 SZWVUASESVZMCY-KCJUWKMLSA-N 0.000 description 1
- IZXIZTKNFFYFOF-UHFFFAOYSA-N 2-Oxazolidone Chemical compound O=C1NCCO1 IZXIZTKNFFYFOF-UHFFFAOYSA-N 0.000 description 1
- 208000007848 Alcoholism Diseases 0.000 description 1
- 208000000103 Anorexia Nervosa Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 208000020925 Bipolar disease Diseases 0.000 description 1
- 208000032841 Bulimia Diseases 0.000 description 1
- 206010006550 Bulimia nervosa Diseases 0.000 description 1
- 206010008874 Chronic Fatigue Syndrome Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 206010022773 Intracranial pressure increased Diseases 0.000 description 1
- 201000009906 Meningitis Diseases 0.000 description 1
- 208000019695 Migraine disease Diseases 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000027626 Neurocognitive disease Diseases 0.000 description 1
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 description 1
- 208000028017 Psychotic disease Diseases 0.000 description 1
- 201000001880 Sexual dysfunction Diseases 0.000 description 1
- 206010041250 Social phobia Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- 208000007536 Thrombosis Diseases 0.000 description 1
- 102100026383 Vasopressin-neurophysin 2-copeptin Human genes 0.000 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 230000010933 acylation Effects 0.000 description 1
- 238000005917 acylation reaction Methods 0.000 description 1
- 230000016571 aggressive behavior Effects 0.000 description 1
- 230000002152 alkylating effect Effects 0.000 description 1
- 208000025748 atypical depressive disease Diseases 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000010511 deprotection reaction Methods 0.000 description 1
- 201000010064 diabetes insipidus Diseases 0.000 description 1
- 208000010643 digestive system disease Diseases 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 206010013663 drug dependence Diseases 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 206010014599 encephalitis Diseases 0.000 description 1
- 206010015037 epilepsy Diseases 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 230000005176 gastrointestinal motility Effects 0.000 description 1
- 208000018685 gastrointestinal system disease Diseases 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000003037 imidazol-2-yl group Chemical group [H]N1C([*])=NC([H])=C1[H] 0.000 description 1
- 208000014674 injury Diseases 0.000 description 1
- 206010027175 memory impairment Diseases 0.000 description 1
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 description 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 1
- 206010027599 migraine Diseases 0.000 description 1
- 208000029766 myalgic encephalomeyelitis/chronic fatigue syndrome Diseases 0.000 description 1
- 230000004770 neurodegeneration Effects 0.000 description 1
- 208000015122 neurodegenerative disease Diseases 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
- 208000022821 personality disease Diseases 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 238000011321 prophylaxis Methods 0.000 description 1
- 208000020016 psychiatric disease Diseases 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 231100000872 sexual dysfunction Toxicity 0.000 description 1
- 201000002859 sleep apnea Diseases 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000020685 sleep-wake disease Diseases 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 125000001981 tert-butyldimethylsilyl group Chemical group [H]C([H])([H])[Si]([H])(C([H])([H])[H])[*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP00116517 | 2000-07-31 | ||
| PCT/EP2001/008520 WO2002010169A1 (en) | 2000-07-31 | 2001-07-24 | Piperazine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2004505085A JP2004505085A (ja) | 2004-02-19 |
| JP2004505085A5 true JP2004505085A5 (enExample) | 2008-09-04 |
| JP4180365B2 JP4180365B2 (ja) | 2008-11-12 |
Family
ID=8169405
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2002515898A Expired - Fee Related JP4180365B2 (ja) | 2000-07-31 | 2001-07-24 | ピペラジン誘導体 |
Country Status (20)
| Country | Link |
|---|---|
| US (4) | US20020035110A1 (enExample) |
| EP (1) | EP1325008B1 (enExample) |
| JP (1) | JP4180365B2 (enExample) |
| KR (1) | KR100539139B1 (enExample) |
| CN (1) | CN1277828C (enExample) |
| AR (1) | AR030306A1 (enExample) |
| AT (1) | ATE305933T1 (enExample) |
| AU (2) | AU2001283955B2 (enExample) |
| BR (1) | BR0112918A (enExample) |
| CA (1) | CA2417106C (enExample) |
| DE (1) | DE60113865T2 (enExample) |
| DK (1) | DK1325008T3 (enExample) |
| ES (1) | ES2250459T3 (enExample) |
| GT (1) | GT200100155A (enExample) |
| MX (1) | MXPA03000906A (enExample) |
| PA (1) | PA8523601A1 (enExample) |
| PE (1) | PE20020366A1 (enExample) |
| UY (1) | UY26863A1 (enExample) |
| WO (1) | WO2002010169A1 (enExample) |
| ZA (1) | ZA200300525B (enExample) |
Families Citing this family (87)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE305933T1 (de) * | 2000-07-31 | 2005-10-15 | Hoffmann La Roche | Piperazin derivate |
| GB0106177D0 (en) * | 2001-03-13 | 2001-05-02 | Hoffmann La Roche | Piperazine derivatives |
| EP1491212B1 (en) * | 2002-03-29 | 2012-08-08 | Mitsubishi Tanabe Pharma Corporation | Remedy for sleep disturbance |
| JP4460450B2 (ja) | 2002-06-19 | 2010-05-12 | ビオヴィトルム・アクチボラゲット（プブリクト） | 新規化合物、その使用および製造法 |
| US7105526B2 (en) | 2002-06-28 | 2006-09-12 | Banyu Pharmaceuticals Co., Ltd. | Benzimidazole derivatives |
| US7772188B2 (en) | 2003-01-28 | 2010-08-10 | Ironwood Pharmaceuticals, Inc. | Methods and compositions for the treatment of gastrointestinal disorders |
| DE10319612A1 (de) | 2003-05-02 | 2004-11-18 | Bayer Healthcare Ag | Substituierte Dihydrochinazoline |
| DE10320780A1 (de) * | 2003-05-09 | 2005-01-20 | Bayer Healthcare Ag | Heterocyclyl-substituierte Dihydrochinazoline |
| GB0314967D0 (en) * | 2003-06-26 | 2003-07-30 | Hoffmann La Roche | Piperazine derivatives |
| US20050032930A1 (en) * | 2003-07-02 | 2005-02-10 | Christian Jackson | Inkjet ink |
| JP4765627B2 (ja) | 2003-09-22 | 2011-09-07 | Ｍｓｄ株式会社 | 新規ピペリジン誘導体 |
| DE10352499A1 (de) * | 2003-11-11 | 2005-06-09 | Bayer Healthcare Ag | Substituierte Dihydrochinazoline II |
| US20080125403A1 (en) | 2004-04-02 | 2008-05-29 | Merck & Co., Inc. | Method of Treating Men with Metabolic and Anthropometric Disorders |
| DE102004022672A1 (de) * | 2004-05-07 | 2005-11-24 | Bayer Healthcare Ag | Substituierte Azachinazoline |
| EP2400300A1 (en) | 2004-08-25 | 2011-12-28 | Takeda Pharmaceutical Company Limited | Method of screening preventives/remedies for stress urinary incontinence |
| EP2286837A3 (en) | 2004-11-01 | 2013-09-04 | Amylin Pharmaceuticals, LLC | Treatment of obesity and obesity related diseases |
| AU2005333165B2 (en) | 2004-11-12 | 2012-07-19 | Asuragen, Inc. | Methods and compositions involving miRNA and miRNA inhibitor molecules |
| US7790712B2 (en) | 2005-03-17 | 2010-09-07 | Boehringer Ingelheim Pharmaceutical, Inc. | Substituted [1,4]diazepino[1,2-A]indoles and azepino[1,2-A]indoles as anti-cytokine inhibitors |
| WO2006117304A1 (en) * | 2005-05-03 | 2006-11-09 | F. Hoffmann-La Roche Ag | Tetracyclic azapyrazinoindolines as 5-ht2 ligands |
| US7737155B2 (en) | 2005-05-17 | 2010-06-15 | Schering Corporation | Nitrogen-containing heterocyclic compounds and methods of use thereof |
| US8138206B2 (en) | 2005-05-30 | 2012-03-20 | Msd. K.K. | Piperidine derivative |
| DE102005027517A1 (de) * | 2005-06-15 | 2006-12-21 | Bayer Healthcare Ag | Verfahren zur Herstellung von Dihydrochinazolinen |
| US20100216758A1 (en) | 2005-08-10 | 2010-08-26 | Makoto Ando | Pyridone Compounds |
| EP2330125A3 (en) | 2005-08-11 | 2012-12-12 | Amylin Pharmaceuticals, Inc. | Hybrid polypeptides with selectable properties |
| AU2006279680B2 (en) | 2005-08-11 | 2012-12-06 | Amylin Pharmaceuticals, Llc | Hybrid polypeptides with selectable properties |
| CA2619770A1 (en) | 2005-08-24 | 2007-03-01 | Banyu Pharmaceutical Co., Ltd. | Phenylpyridone derivative |
| US20090264426A1 (en) | 2005-09-07 | 2009-10-22 | Shunji Sakuraba | Bicyclic aromatic substituted pyridone derivative |
| RU2008116844A (ru) | 2005-09-29 | 2009-11-10 | Мерк энд Ко., Инк. (US) | Ацилированные производные спиропиперидина как модуляторы рецептора меланокортина-4 |
| JP2009511606A (ja) * | 2005-10-14 | 2009-03-19 | ハー・ルンドベック・アクチエゼルスカベット | エスシタロプラムおよびブプロピオンの低用量の併用を用いる中枢神経系障害の治療方法 |
| AU2006304836A1 (en) | 2005-10-21 | 2007-04-26 | Novartis Ag | Combination of a renin-inhibitor and an anti-dyslipidemic agent and/or an antiobesity agent |
| US8163770B2 (en) | 2005-10-27 | 2012-04-24 | Msd. K. K. | Benzoxathiin derivative |
| EP1953165B1 (en) | 2005-11-10 | 2012-02-01 | Msd K.K. | Aza-substituted spiro derivative |
| WO2007065820A1 (en) | 2005-12-09 | 2007-06-14 | F. Hoffmann-La Roche Ag | Tricyclic amide derivatives useful for treating obesity |
| UA95788C2 (en) | 2005-12-15 | 2011-09-12 | Ф. Хоффманн-Ля Рош Аг | Fused pyrrole derivatives |
| JP5528699B2 (ja) | 2006-05-16 | 2014-06-25 | 武田薬品工業株式会社 | 縮合複素環化合物およびその用途 |
| EP2946778A1 (en) | 2006-09-22 | 2015-11-25 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
| EP2072519A4 (en) | 2006-09-28 | 2009-10-21 | Banyu Pharma Co Ltd | DIARYLKETIMINDERIVAT |
| TWI440456B (zh) | 2007-01-16 | 2014-06-11 | 用於治療代謝性症候群之新穎化合物 | |
| FR2912145B1 (fr) * | 2007-02-02 | 2009-03-06 | Servier Lab | Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| US8106086B2 (en) | 2007-04-02 | 2012-01-31 | Msd K.K. | Indoledione derivative |
| ES2705599T3 (es) | 2007-04-16 | 2019-03-26 | Abbvie Inc | Indoles sustituidos en la posición 7 como inhibidores de mcl-1 |
| 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 |
| CN101772513B (zh) | 2007-06-04 | 2013-11-13 | 协同医药品公司 | 有效用于胃肠功能紊乱、炎症、癌症和其他疾病治疗的鸟苷酸环化酶激动剂 |
| JP5520051B2 (ja) | 2007-11-15 | 2014-06-11 | 武田薬品工業株式会社 | 縮合ピリジン誘導体およびその用途 |
| WO2009110510A1 (ja) | 2008-03-06 | 2009-09-11 | 萬有製薬株式会社 | アルキルアミノピリジン誘導体 |
| WO2009119726A1 (ja) | 2008-03-28 | 2009-10-01 | 萬有製薬株式会社 | メラニン凝集ホルモン受容体拮抗作用を有するジアリールメチルアミド誘導体 |
| ES2588193T3 (es) | 2008-03-28 | 2016-10-31 | Nerviano Medical Sciences S.R.L. | Derivados de 3,4-dihidro-2H-pirazino[1,2-a]indol-1-ona activos como inhibidores de cinasa, proceso para su preparación y composiciones farmacéuticas que los comprenden |
| CA2722653A1 (en) * | 2008-04-28 | 2009-11-05 | Kuraray Medical Inc. | Dental composition and composite resin |
| CA2666036C (en) | 2008-05-16 | 2017-09-12 | Chien-Hung Chen | Novel compositions and methods for treating hyperproliferative diseases |
| CA2726917C (en) | 2008-06-04 | 2018-06-26 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| US20110071129A1 (en) | 2008-06-19 | 2011-03-24 | Makoto Ando | Spirodiamine-diaryl ketoxime derivative |
| WO2010009319A2 (en) | 2008-07-16 | 2010-01-21 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal, inflammation, cancer and other disorders |
| WO2010013595A1 (ja) | 2008-07-30 | 2010-02-04 | 萬有製薬株式会社 | ５員－５員又は５員－６員縮環シクロアルキルアミン誘導体 |
| WO2010047982A1 (en) | 2008-10-22 | 2010-04-29 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| NZ592544A (en) | 2008-10-30 | 2013-01-25 | Merck Sharp & Dohme | Isonicotinamide orexin receptor antagonists |
| EP2362731B1 (en) | 2008-10-31 | 2016-04-06 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| WO2010075069A1 (en) | 2008-12-16 | 2010-07-01 | Schering Corporation | Bicyclic pyranone derivatives as nicotinic acid receptor agonists |
| EP2379547A1 (en) | 2008-12-16 | 2011-10-26 | Schering Corporation | Pyridopyrimidine derivatives and methods of use thereof |
| FI122466B (fi) * | 2009-08-21 | 2012-01-31 | Hollming Oy | Menetelmä työstettävän metallikappaleen kuumentamiseksi ja induktiokuumennustyökalu |
| JPWO2011071136A1 (ja) | 2009-12-11 | 2013-04-22 | アステラス製薬株式会社 | 線維筋痛症治療剤 |
| EP2538784B1 (en) | 2010-02-25 | 2015-09-09 | Merck Sharp & Dohme Corp. | Benzimidazole derivatives useful anti-diabetic agents |
| US9616097B2 (en) | 2010-09-15 | 2017-04-11 | Synergy Pharmaceuticals, Inc. | Formulations of guanylate cyclase C agonists and methods of use |
| CA2826649C (en) | 2011-02-25 | 2016-07-26 | Merck Sharp & Dohme Corp. | Novel cyclic azabenzimidazole derivatives useful as anti-diabetic agents |
| CN108676076A (zh) | 2011-03-01 | 2018-10-19 | 辛纳吉制药公司 | 制备鸟苷酸环化酶c激动剂的方法 |
| AR088352A1 (es) | 2011-10-19 | 2014-05-28 | Merck Sharp & Dohme | Antagonistas del receptor de 2-piridiloxi-4-nitrilo orexina |
| ES2607113T3 (es) | 2012-03-16 | 2017-03-29 | Vitae Pharmaceuticals, Inc. | Moduladores de los receptores X del hígado |
| DK2825541T3 (en) | 2012-03-16 | 2016-10-03 | Vitae Pharmaceuticals Inc | LIVER-X-receptor modulators |
| TWI579274B (zh) * | 2012-04-20 | 2017-04-21 | 龍馬躍公司 | 製備１－芳基－５－烷基吡唑化合物的改良方法 |
| CA2880901A1 (en) | 2012-08-02 | 2014-02-06 | Merck Sharp & Dohme Corp. | Antidiabetic tricyclic compounds |
| WO2014139388A1 (en) | 2013-03-14 | 2014-09-18 | Merck Sharp & Dohme Corp. | Novel indole derivatives useful as anti-diabetic agents |
| HK1220611A1 (zh) | 2013-03-15 | 2017-05-12 | Bausch Health Ireland Limited | 用於治疗胃肠道病症的组成物 |
| AU2014235215A1 (en) | 2013-03-15 | 2015-10-01 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase and their uses |
| JP6347830B2 (ja) | 2013-04-23 | 2018-06-27 | ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ | ピラジノ［１，２−ａ］インドール化合物、その調製および医薬としての使用 |
| JP6291567B2 (ja) * | 2013-04-23 | 2018-03-14 | ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ | ピラジノ［１，２−ａ］インドール化合物、その調製および医薬としての使用 |
| HRP20240805T1 (hr) | 2013-06-05 | 2024-09-27 | Bausch Health Ireland Limited | Ultra-pročišćeni agonisti guanilat-ciklaze c, postupak njihove pripreme i uporabe |
| US9714258B2 (en) | 2014-01-24 | 2017-07-25 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| ES2901114T3 (es) | 2014-08-29 | 2022-03-21 | Tes Pharma S R L | Inhibidores de ácido alfa-amino-beta-carboximucónico semialdehído descarboxilasa |
| CR20170572A (es) | 2015-06-17 | 2018-03-20 | Pfizer | Compuestos tricíclicos y su uso como inhibidores de la fosfodiesterasa |
| MX2017017097A (es) | 2015-07-02 | 2018-05-23 | Tp Therapeutics Inc | Macrociclos diarílicos quirales como moduladores de proteínas quinasas. |
| MX386680B (es) | 2015-07-06 | 2025-03-19 | Turning Point Therapeutics Inc | Polimorfo de macrociclo de diarilo. |
| CN109952292A (zh) | 2016-10-14 | 2019-06-28 | Tes制药有限责任公司 | α-氨基-β-羧基己二烯二酸半醛去羧酶的抑制剂 |
| US20210052600A1 (en) | 2017-12-27 | 2021-02-25 | Takeda Pharmaceutical Company Limited | Therapeutic agents for stress urinary incontinence and incotinence of feces |
| JP7638868B2 (ja) | 2018-11-20 | 2025-03-04 | ティエエッセ ファルマ ソチエタ レスポンサビリタ リミタータ | α－アミノ－β－カルボキシムコン酸セミアルデヒドデカルボキシラーゼ阻害剤 |
| US11098029B2 (en) | 2019-02-13 | 2021-08-24 | Merck Sharp & Dohme Corp. | 5-alkyl pyrrolidine orexin receptor agonists |
| WO2020167701A1 (en) | 2019-02-13 | 2020-08-20 | Merck Sharp & Dohme Corp. | Pyrrolidine orexin receptor agonists |
| EP4010314B1 (en) | 2019-08-08 | 2024-02-28 | Merck Sharp & Dohme LLC | Heteroaryl pyrrolidine and piperidine orexin receptor agonists |
| WO2022040070A1 (en) | 2020-08-18 | 2022-02-24 | Merck Sharp & Dohme Corp. | Bicycloheptane pyrrolidine orexin receptor agonists |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US652018A (en) * | 1900-02-15 | 1900-06-19 | John C Duner | Gate. |
| US3317524A (en) | 1965-02-04 | 1967-05-02 | American Home Prod | Substituted 1, 2, 3, 4-tetrahydro-pyrazino[1, 2-a]indoles |
| DE2162422A1 (de) | 1971-12-16 | 1973-06-20 | Merck Patent Gmbh | Pyrazinoindol-derivate und verfahren zu ihrer herstellung |
| EP0572863A1 (de) * | 1992-06-05 | 1993-12-08 | F. Hoffmann-La Roche Ag | ZNS Pyrazinoindole |
| NZ261593A (en) | 1993-03-01 | 1996-09-25 | Merck Sharp & Dohme | 3-piperazinylmethly-1h-indolopyridine derivatives and pharmaceutical compositions |
| US5622950A (en) * | 1993-03-01 | 1997-04-22 | Merck, Sharp & Dohme Ltd. | Pyrrolo-pyridine derivatives |
| US5576319A (en) * | 1993-03-01 | 1996-11-19 | Merck, Sharp & Dohme Ltd. | Pyrrolo-pyridine derivatives |
| US6169086B1 (en) | 1997-01-27 | 2001-01-02 | Daiichi Pharmaceutical Co., Ltd. | Pyrazole derivatives |
| JP2000169475A (ja) | 1998-07-24 | 2000-06-20 | Dai Ichi Seiyaku Co Ltd | ピラゾ―ル誘導体およびその塩 |
| CA2351385A1 (en) * | 1998-12-17 | 2000-06-22 | American Home Products Corporation | 2,3,4,4a-tetrahydro-1h-pyrazino(1,2-a)quinoxalin-5(6h)one derivates being 5ht2c agonists |
| GB9902047D0 (en) * | 1999-01-29 | 1999-03-17 | Cerebrus Ltd | Chemical compounds XI |
| ATE305933T1 (de) * | 2000-07-31 | 2005-10-15 | Hoffmann La Roche | Piperazin derivate |
-
2001
- 2001-07-24 AT AT01962869T patent/ATE305933T1/de not_active IP Right Cessation
- 2001-07-24 ES ES01962869T patent/ES2250459T3/es not_active Expired - Lifetime
- 2001-07-24 DK DK01962869T patent/DK1325008T3/da active
- 2001-07-24 AU AU2001283955A patent/AU2001283955B2/en not_active Ceased
- 2001-07-24 DE DE60113865T patent/DE60113865T2/de not_active Expired - Fee Related
- 2001-07-24 AU AU8395501A patent/AU8395501A/xx active Pending
- 2001-07-24 WO PCT/EP2001/008520 patent/WO2002010169A1/en not_active Ceased
- 2001-07-24 EP EP01962869A patent/EP1325008B1/en not_active Expired - Lifetime
- 2001-07-24 CA CA002417106A patent/CA2417106C/en not_active Expired - Fee Related
- 2001-07-24 MX MXPA03000906A patent/MXPA03000906A/es active IP Right Grant
- 2001-07-24 JP JP2002515898A patent/JP4180365B2/ja not_active Expired - Fee Related
- 2001-07-24 BR BR0112918-0A patent/BR0112918A/pt not_active IP Right Cessation
- 2001-07-24 CN CNB018152260A patent/CN1277828C/zh not_active Expired - Fee Related
- 2001-07-24 KR KR10-2003-7001439A patent/KR100539139B1/ko not_active Expired - Fee Related
- 2001-07-25 PE PE2001000749A patent/PE20020366A1/es not_active Application Discontinuation
- 2001-07-25 US US09/912,949 patent/US20020035110A1/en not_active Abandoned
- 2001-07-27 AR ARP010103589A patent/AR030306A1/es unknown
- 2001-07-30 PA PA20018523601A patent/PA8523601A1/es unknown
- 2001-07-30 GT GT200100155A patent/GT200100155A/es unknown
- 2001-07-30 UY UY26863A patent/UY26863A1/es not_active Application Discontinuation
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2003
- 2003-01-20 ZA ZA200300525A patent/ZA200300525B/en unknown
- 2003-03-25 US US10/396,242 patent/US6933387B2/en not_active Expired - Fee Related
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2005
- 2005-06-28 US US11/169,079 patent/US7253281B2/en not_active Expired - Fee Related
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2007
- 2007-01-03 US US11/649,132 patent/US20070106076A1/en not_active Abandoned
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