JP2007509110A - Ｃｂ１拮抗活性を有する４，５−ジヒドロ−１ｈ−ピラゾール誘導体とリパーゼ阻害剤とを含む組み合わせでの肥満症治療 - Google Patents
Ｃｂ１拮抗活性を有する４，５−ジヒドロ−１ｈ−ピラゾール誘導体とリパーゼ阻害剤とを含む組み合わせでの肥満症治療 Download PDFInfo
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- JP2007509110A JP2007509110A JP2006536092A JP2006536092A JP2007509110A JP 2007509110 A JP2007509110 A JP 2007509110A JP 2006536092 A JP2006536092 A JP 2006536092A JP 2006536092 A JP2006536092 A JP 2006536092A JP 2007509110 A JP2007509110 A JP 2007509110A
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- SCJVBJZQVUMHTE-UHFFFAOYSA-N n-[amino-[5-(4-chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]methylidene]naphthalene-1-carboxamide Chemical compound C=1C=CC2=CC=CC=C2C=1C(=O)N=C(N)N(N=1)CC(C=2C=CC=CC=2)C=1C1=CC=C(Cl)C=C1 SCJVBJZQVUMHTE-UHFFFAOYSA-N 0.000 description 1
- IWWDPIHULYTKIS-UHFFFAOYSA-N n-[c-[5-(4-chlorophenyl)-4-phenyl-3,4-dihydropyrazol-2-yl]-n-methylcarbonimidoyl]-3-(trifluoromethyl)benzamide Chemical compound C1C(C=2C=CC=CC=2)C(C=2C=CC(Cl)=CC=2)=NN1C(=NC)NC(=O)C1=CC=CC(C(F)(F)F)=C1 IWWDPIHULYTKIS-UHFFFAOYSA-N 0.000 description 1
- SCGPTIIGSPSBRD-UHFFFAOYSA-N n-acetamido-5-(4-chlorophenyl)-n'-(4-chlorophenyl)sulfonyl-4-phenyl-3,4-dihydropyrazole-2-carboximidamide Chemical compound C1C(C=2C=CC=CC=2)C(C=2C=CC(Cl)=CC=2)=NN1C(/NNC(=O)C)=N/S(=O)(=O)C1=CC=C(Cl)C=C1 SCGPTIIGSPSBRD-UHFFFAOYSA-N 0.000 description 1
- 229930014626 natural product Natural products 0.000 description 1
- 230000018791 negative regulation of catalytic activity Effects 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000002547 new drug Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 description 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 description 1
- 231100000956 nontoxicity Toxicity 0.000 description 1
- SFBTTWXNCQVIEC-UHFFFAOYSA-N o-Vinylanisole Chemical compound COC1=CC=CC=C1C=C SFBTTWXNCQVIEC-UHFFFAOYSA-N 0.000 description 1
- 208000001797 obstructive sleep apnea Diseases 0.000 description 1
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 description 1
- 230000000399 orthopedic effect Effects 0.000 description 1
- 210000001672 ovary Anatomy 0.000 description 1
- 208000027753 pain disease Diseases 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 229920000083 poly(allylamine) Polymers 0.000 description 1
- 229920002401 polyacrylamide Polymers 0.000 description 1
- 239000004584 polyacrylic acid Substances 0.000 description 1
- 229920001515 polyalkylene glycol Polymers 0.000 description 1
- 229920002647 polyamide Polymers 0.000 description 1
- 201000010065 polycystic ovary syndrome Diseases 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 229920001155 polypropylene Polymers 0.000 description 1
- 229920002223 polystyrene Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 1
- 230000008569 process Effects 0.000 description 1
- 235000018102 proteins Nutrition 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 229960004431 quetiapine Drugs 0.000 description 1
- URKOMYMAXPYINW-UHFFFAOYSA-N quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 description 1
- 239000002287 radioligand Substances 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000004044 response Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 229960001534 risperidone Drugs 0.000 description 1
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 230000000862 serotonergic effect Effects 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000005062 synaptic transmission Effects 0.000 description 1
- 229920001059 synthetic polymer Polymers 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 239000007885 tablet disintegrant Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 150000003573 thiols Chemical class 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 description 1
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
- 229960000607 ziprasidone Drugs 0.000 description 1
- MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/74—Synthetic polymeric materials
- A61K31/785—Polymers containing nitrogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Child & Adolescent Psychology (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP03103961 | 2003-10-24 | ||
| PCT/EP2004/052618 WO2005039566A1 (en) | 2003-10-24 | 2004-10-22 | Combination treatment of obesity involving 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity and lipase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2007509110A true JP2007509110A (ja) | 2007-04-12 |
| JP2007509110A5 JP2007509110A5 (https=) | 2007-09-06 |
Family
ID=34486362
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2006536092A Withdrawn JP2007509110A (ja) | 2003-10-24 | 2004-10-22 | Ｃｂ１拮抗活性を有する４，５−ジヒドロ−１ｈ−ピラゾール誘導体とリパーゼ阻害剤とを含む組み合わせでの肥満症治療 |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1680106B1 (https=) |
| JP (1) | JP2007509110A (https=) |
| CN (2) | CN1921849A (https=) |
| AR (1) | AR046132A1 (https=) |
| AT (1) | ATE438394T1 (https=) |
| AU (1) | AU2004283055A1 (https=) |
| BR (1) | BRPI0415463A (https=) |
| CA (1) | CA2543342A1 (https=) |
| DE (1) | DE602004022445D1 (https=) |
| MX (1) | MXPA06004390A (https=) |
| RU (1) | RU2006117639A (https=) |
| TW (1) | TW200528102A (https=) |
| WO (1) | WO2005039566A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20080039996A (ko) * | 2005-08-17 | 2008-05-07 | 솔베이 파머슈티컬스 게엠베하 | 칼륨 채널 억제 화합물의 사용 방법 |
| CN102731418B (zh) * | 2012-07-15 | 2015-03-11 | 浙江大学 | 1-取代-1h-1,2,4-三氮唑-甲酰胺衍生物及其制备和用途 |
| CN113166068B (zh) * | 2018-11-20 | 2024-08-16 | 上海科技大学 | MmpL3抑制剂、组合物及其用途 |
| CN117551046B (zh) * | 2023-11-17 | 2025-10-28 | 广东药科大学附属第一医院 | 二氨基脲类hsl抑制剂、制备方法及其用途 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DZ3335A1 (fr) * | 2000-03-23 | 2001-09-27 | Solvay Pharm Bv | Derives de 4,5-dihydro-1h-pyrazole ayant une activite antagoniste de cb1 |
| PL363751A1 (en) * | 2001-03-22 | 2004-11-29 | Solvay Pharmaceuticals B.V. | 4,5-dihydro-1h-pyrazole derivatives having cb1-antagonistic activity |
| KR100903760B1 (ko) * | 2001-09-21 | 2009-06-19 | 솔베이 파마슈티칼스 비. 브이 | Ｃｂ1-길항 작용을 가지는 신규한4,5-디하이드로-1ｈ-피라졸 유도체 |
| IL157704A0 (en) * | 2001-09-21 | 2004-03-28 | Solvay Pharm Bv | 4,5-dihydro-1h-pyrazole derivatives having potent cbi-antagonistic activity |
| SE0104330D0 (sv) * | 2001-12-19 | 2001-12-19 | Astrazeneca Ab | Therapeutic agents |
| GB0202015D0 (en) * | 2002-01-29 | 2002-03-13 | Hoffmann La Roche | Piperazine Derivatives |
| AU2003209388A1 (en) * | 2002-01-29 | 2003-09-02 | Merck And Co., Inc. | Substituted imidazoles as cannabinoid receptor modulators |
| TW200412942A (en) * | 2002-08-06 | 2004-08-01 | Abbott Lab | Appetite control method |
| US20040122033A1 (en) * | 2002-12-10 | 2004-06-24 | Nargund Ravi P. | Combination therapy for the treatment of obesity |
| RU2344132C2 (ru) * | 2003-06-20 | 2009-01-20 | Ф.Хоффманн-Ля Рош Аг | 2-аминобензотиазолы в качестве обратных агонистов рецепторов cb1 |
| MXPA06002064A (es) * | 2003-10-20 | 2006-05-19 | Solvay Pharm Bv | Derivados e 1h imidazol como moduladores del receptor cannabinoide. |
| MXPA06004434A (es) * | 2003-10-24 | 2006-06-20 | Solvay Pharm Gmbh | Usos medicos novedosos de compuestos que muestran actividad antagonista cb1 y tratamiento de combinacion que involucra tales compuestos. |
-
2004
- 2004-10-20 TW TW093131751A patent/TW200528102A/zh unknown
- 2004-10-20 AR ARP040103804A patent/AR046132A1/es unknown
- 2004-10-22 AT AT04791282T patent/ATE438394T1/de not_active IP Right Cessation
- 2004-10-22 CA CA002543342A patent/CA2543342A1/en not_active Abandoned
- 2004-10-22 RU RU2006117639/15A patent/RU2006117639A/ru unknown
- 2004-10-22 WO PCT/EP2004/052618 patent/WO2005039566A1/en not_active Ceased
- 2004-10-22 AU AU2004283055A patent/AU2004283055A1/en not_active Abandoned
- 2004-10-22 CN CNA2004800300871A patent/CN1921849A/zh active Pending
- 2004-10-22 EP EP04791282A patent/EP1680106B1/en not_active Expired - Lifetime
- 2004-10-22 DE DE602004022445T patent/DE602004022445D1/de not_active Expired - Fee Related
- 2004-10-22 JP JP2006536092A patent/JP2007509110A/ja not_active Withdrawn
- 2004-10-22 MX MXPA06004390A patent/MXPA06004390A/es not_active Application Discontinuation
- 2004-10-22 CN CNA2004800301164A patent/CN1997364A/zh active Pending
- 2004-10-22 BR BRPI0415463-0A patent/BRPI0415463A/pt not_active IP Right Cessation
Also Published As
| Publication number | Publication date |
|---|---|
| CA2543342A1 (en) | 2005-05-06 |
| EP1680106B1 (en) | 2009-08-05 |
| DE602004022445D1 (de) | 2009-09-17 |
| BRPI0415463A (pt) | 2006-12-19 |
| RU2006117639A (ru) | 2007-12-10 |
| TW200528102A (en) | 2005-09-01 |
| EP1680106A1 (en) | 2006-07-19 |
| AU2004283055A1 (en) | 2005-05-06 |
| CN1997364A (zh) | 2007-07-11 |
| WO2005039566A1 (en) | 2005-05-06 |
| ATE438394T1 (de) | 2009-08-15 |
| AR046132A1 (es) | 2005-11-23 |
| MXPA06004390A (es) | 2006-06-14 |
| CN1921849A (zh) | 2007-02-28 |
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