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
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- 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 (88)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60113865T2 (de) * | 2000-07-31 | 2006-07-20 | Vernalis Research Ltd., Winnersh | Piperazin derivate |
| GB0106177D0 (en) | 2001-03-13 | 2001-05-02 | Hoffmann La Roche | Piperazine derivatives |
| PT1491212E (pt) * | 2002-03-29 | 2012-11-16 | Mitsubishi Tanabe Pharma Corp | Medicamento para distúrbios de sono |
| AU2003243089B2 (en) | 2002-06-19 | 2010-01-07 | Biovitrum Ab (Publ) | Novel compounds, their use and preparation |
| 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 |
| EP1792629A4 (en) | 2004-08-25 | 2010-08-25 | Takeda Pharmaceutical | MEANS FOR THE PREVENTION / TREATMENT OF STRESS-RELATED HARNINE INCONTINENCE AND PRECAUTIONARY METHOD FOR THIS |
| ES2325773T5 (es) | 2004-11-01 | 2014-02-24 | Amylin Pharmaceuticals, Llc. | Tratamiento de la obesidad y de los trastornos relacionados |
| CA2857878A1 (en) | 2004-11-12 | 2006-12-28 | 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 |
| AU2006243243B2 (en) * | 2005-05-03 | 2009-05-14 | 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 |
| CA2618112A1 (en) | 2005-08-10 | 2007-02-15 | Banyu Pharmaceutical Co., Ltd. | Pyridone compound |
| BRPI0614649A2 (pt) | 2005-08-11 | 2011-04-12 | Amylin Pharmaceuticals Inc | polipeptìdeos hìbridos com propriedades selecionáveis |
| AU2006279680B2 (en) | 2005-08-11 | 2012-12-06 | Amylin Pharmaceuticals, Llc | Hybrid polypeptides with selectable properties |
| WO2007024004A1 (ja) | 2005-08-24 | 2007-03-01 | Banyu Pharmaceutical Co., Ltd. | フェニルピリドン誘導体 |
| AU2006288153A1 (en) | 2005-09-07 | 2007-03-15 | Msd K.K. | Bicyclic aromatic substituted pyridone derivative |
| KR20080048502A (ko) | 2005-09-29 | 2008-06-02 | 머크 앤드 캄파니 인코포레이티드 | 멜라노코르틴-4 수용체 조절제로서의 아실화스피로피페리딘 유도체 |
| EP1954257A4 (en) * | 2005-10-14 | 2009-05-20 | Lundbeck & Co As H | METHOD FOR TREATING DISORDERS OF THE CENTRAL NERVOUS SYSTEM WITH A LOW-DOSED COMBINATION OF ESCITALOPRAM AND BUPROPION |
| RU2008119687A (ru) | 2005-10-21 | 2009-11-27 | Новартис АГ (CH) | Комбинации органических соединений |
| CA2627139A1 (en) | 2005-10-27 | 2007-05-03 | Banyu Pharmaceutical Co., Ltd. | Novel benzoxathiin derivative |
| ES2381205T3 (es) | 2005-11-10 | 2012-05-24 | Msd K.K. | Derivado espiro aza-sustituido |
| 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 |
| EP2727585A1 (en) | 2006-05-16 | 2014-05-07 | Takeda Pharmaceutical Company Limited | In-vivo screening method |
| US8173629B2 (en) | 2006-09-22 | 2012-05-08 | Merck Sharp & Dohme Corp. | Method of treatment using fatty acid synthesis inhibitors |
| WO2008047544A1 (en) | 2006-09-28 | 2008-04-24 | Banyu Pharmaceutical Co., Ltd. | Diaryl ketimine derivative |
| DK2118279T3 (en) | 2007-01-16 | 2018-02-26 | Ipintl Llc | HIS UNKNOWN COMPOSITION FOR TREATMENT OF METABOLIC SYNDROME |
| FR2912145B1 (fr) * | 2007-02-02 | 2009-03-06 | Servier Lab | Nouveaux derives tricycliques,leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| JP5319518B2 (ja) | 2007-04-02 | 2013-10-16 | Msd株式会社 | インドールジオン誘導体 |
| ES2705599T3 (es) | 2007-04-16 | 2019-03-26 | Abbvie Inc | Indoles sustituidos en la posición 7 como inhibidores de mcl-1 |
| MX2009013293A (es) | 2007-06-04 | 2010-02-15 | Synergy Pharmaceuticals Inc | Agonistas de guanilato ciclasa útiles para el tratamiento de trastornos gastrointestinales, inflamación, cáncer y otros trastornos. |
| 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 |
| EP2216023A4 (en) | 2007-11-15 | 2013-03-13 | Takeda Pharmaceutical | CONDENSED PYRIDINE DERIVATIVE AND ITS USE |
| JPWO2009110510A1 (ja) | 2008-03-06 | 2011-07-14 | Msd株式会社 | アルキルアミノピリジン誘導体 |
| US20110015198A1 (en) | 2008-03-28 | 2011-01-20 | Banyu Pharmaceutical Co., Inc. | Diarylmethylamide derivative having melanin-concentrating hormone receptor antagonism |
| WO2009118411A2 (en) * | 2008-03-28 | 2009-10-01 | Nerviano Medical Sciences S.R.L. | 3,4-dihydro-2h-pyrazino[1,2-a]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| WO2009133911A1 (ja) * | 2008-04-28 | 2009-11-05 | クラレメディカル株式会社 | 歯科用組成物及びコンポジットレジン |
| CA2666036C (en) | 2008-05-16 | 2017-09-12 | Chien-Hung Chen | Novel compositions and methods for treating hyperproliferative diseases |
| 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 |
| JPWO2009154132A1 (ja) | 2008-06-19 | 2011-12-01 | Msd株式会社 | スピロジアミン−ジアリールケトオキシム誘導体 |
| CA2730603C (en) | 2008-07-16 | 2019-09-24 | Synergy Pharmaceuticals Inc. | Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders |
| JPWO2010013595A1 (ja) | 2008-07-30 | 2012-01-12 | Msd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 |
| EP2348857B1 (en) | 2008-10-22 | 2016-02-24 | Merck Sharp & Dohme Corp. | Novel cyclic benzimidazole derivatives useful anti-diabetic agents |
| EP2350010B1 (en) | 2008-10-30 | 2014-03-26 | Merck Sharp & Dohme Corp. | Isonicotinamide orexin receptor antagonists |
| 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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| US652018A (en) * | 1900-02-15 | 1900-06-19 | John C Duner | Gate. |
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-
2001
- 2001-07-24 DE DE60113865T patent/DE60113865T2/de not_active Expired - Fee Related
- 2001-07-24 ES ES01962869T patent/ES2250459T3/es not_active Expired - Lifetime
- 2001-07-24 JP JP2002515898A patent/JP4180365B2/ja not_active Expired - Fee Related
- 2001-07-24 AU AU2001283955A patent/AU2001283955B2/en not_active Ceased
- 2001-07-24 AU AU8395501A patent/AU8395501A/xx active Pending
- 2001-07-24 BR BR0112918-0A patent/BR0112918A/pt not_active IP Right Cessation
- 2001-07-24 EP EP01962869A patent/EP1325008B1/en not_active Expired - Lifetime
- 2001-07-24 WO PCT/EP2001/008520 patent/WO2002010169A1/en not_active Ceased
- 2001-07-24 DK DK01962869T patent/DK1325008T3/da active
- 2001-07-24 CN CNB018152260A patent/CN1277828C/zh not_active Expired - Fee Related
- 2001-07-24 AT AT01962869T patent/ATE305933T1/de not_active IP Right Cessation
- 2001-07-24 MX MXPA03000906A patent/MXPA03000906A/es active IP Right Grant
- 2001-07-24 KR KR10-2003-7001439A patent/KR100539139B1/ko not_active Expired - Fee Related
- 2001-07-24 CA CA002417106A patent/CA2417106C/en not_active Expired - Fee Related
- 2001-07-25 US US09/912,949 patent/US20020035110A1/en not_active Abandoned
- 2001-07-25 PE PE2001000749A patent/PE20020366A1/es not_active Application Discontinuation
- 2001-07-27 AR ARP010103589A patent/AR030306A1/es unknown
- 2001-07-30 GT GT200100155A patent/GT200100155A/es unknown
- 2001-07-30 PA PA20018523601A patent/PA8523601A1/es unknown
- 2001-07-30 UY UY26863A patent/UY26863A1/es not_active Application Discontinuation
-
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
-
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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