KR20040095255A - Ｐｄｅ4 억제제 또는 ｐｄｅ3/4 억제제 및 히스타민수용체 길항제의 약학 조성물 - Google Patents
Ｐｄｅ4 억제제 또는 ｐｄｅ3/4 억제제 및 히스타민수용체 길항제의 약학 조성물 Download PDFInfo
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- KR20040095255A KR20040095255A KR10-2004-7013742A KR20047013742A KR20040095255A KR 20040095255 A KR20040095255 A KR 20040095255A KR 20047013742 A KR20047013742 A KR 20047013742A KR 20040095255 A KR20040095255 A KR 20040095255A
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- KR
- South Korea
- Prior art keywords
- inn
- tetrahydro
- phthalazin
- piperidin
- dimethoxyphenyl
- 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.)
- Ceased
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- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims description 37
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- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 36
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- DNCYBUMDUBHIJZ-UHFFFAOYSA-N 1h-pyrimidin-6-one Chemical compound O=C1C=CN=CN1 DNCYBUMDUBHIJZ-UHFFFAOYSA-N 0.000 claims description 28
- NPGREARFJMFTDF-UHFFFAOYSA-N n-(3,5-dichloro-1-hydroxypyridin-4-ylidene)-8-methoxy-2-(trifluoromethyl)quinoline-5-carboxamide Chemical compound C12=CC=C(C(F)(F)F)N=C2C(OC)=CC=C1C(=O)N=C1C(Cl)=CN(O)C=C1Cl NPGREARFJMFTDF-UHFFFAOYSA-N 0.000 claims description 28
- 239000002253 acid Substances 0.000 claims description 27
- CVDXFPBVOIERBH-JWQCQUIFSA-N 4-[(4ar,10bs)-9-ethoxy-8-methoxy-2-methyl-3,4,4a,10b-tetrahydro-1h-benzo[c][1,6]naphthyridin-6-yl]-n,n-di(propan-2-yl)benzamide Chemical compound N([C@@H]1CCN(C)C[C@@H]1C=1C=C(C(=CC=11)OC)OCC)=C1C1=CC=C(C(=O)N(C(C)C)C(C)C)C=C1 CVDXFPBVOIERBH-JWQCQUIFSA-N 0.000 claims description 26
- YPFLFUJKZDAXRA-UHFFFAOYSA-N [3-(carbamoylamino)-2-(2,4-dichlorobenzoyl)-1-benzofuran-6-yl] methanesulfonate Chemical compound O1C2=CC(OS(=O)(=O)C)=CC=C2C(NC(N)=O)=C1C(=O)C1=CC=C(Cl)C=C1Cl YPFLFUJKZDAXRA-UHFFFAOYSA-N 0.000 claims description 26
- DPHDSIQHVGSITN-UHFFFAOYSA-N n-(3,5-dichloropyridin-4-yl)-2-[1-[(4-fluorophenyl)methyl]-5-hydroxyindol-3-yl]-2-oxoacetamide Chemical compound C1=C(C(=O)C(=O)NC=2C(=CN=CC=2Cl)Cl)C2=CC(O)=CC=C2N1CC1=CC=C(F)C=C1 DPHDSIQHVGSITN-UHFFFAOYSA-N 0.000 claims description 26
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- DIGXMFZQXQUVMR-UHFFFAOYSA-N 5-hexyl-7-(methylsulfonimidoyl)-9-oxoxanthene-2-carboxylic acid Chemical compound O1C2=CC=C(C(O)=O)C=C2C(=O)C2=C1C(CCCCCC)=CC(S(C)(=N)=O)=C2 DIGXMFZQXQUVMR-UHFFFAOYSA-N 0.000 claims description 24
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- ZKLPARSLTMPFCP-OAQYLSRUSA-N 2-[2-[4-[(R)-(4-chlorophenyl)-phenylmethyl]-1-piperazinyl]ethoxy]acetic acid Chemical compound C1CN(CCOCC(=O)O)CCN1[C@@H](C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZKLPARSLTMPFCP-OAQYLSRUSA-N 0.000 claims description 22
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims description 22
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- LITNEAPWQHVPOK-FFSVYQOJSA-N 2(1h)-pyrimidinone, 5-[3-[(1s,2s,4r)-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl]tetrahydro- Chemical compound C1=C(O[C@@H]2[C@H]3CC[C@H](C3)C2)C(OC)=CC=C1C1CNC(=O)NC1 LITNEAPWQHVPOK-FFSVYQOJSA-N 0.000 claims description 21
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- IUVKMZGDUIUOCP-BTNSXGMBSA-N quinbolone Chemical compound O([C@H]1CC[C@H]2[C@H]3[C@@H]([C@]4(C=CC(=O)C=C4CC3)C)CC[C@@]21C)C1=CCCC1 IUVKMZGDUIUOCP-BTNSXGMBSA-N 0.000 claims description 18
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| EP02004987 | 2002-03-06 | ||
| EP02004987.0 | 2002-03-06 | ||
| PCT/EP2003/001876 WO2003074055A1 (en) | 2002-03-06 | 2003-02-25 | Pharmaceutical composition of a pde4 or a pde3/4 inhibitor and a histamine receptor antagonist |
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| US8067433B2 (en) * | 2005-11-09 | 2011-11-29 | Zalicus Inc. | Methods, compositions, and kits for the treatment of ophthalmic disorders |
| WO2008074803A2 (en) * | 2006-12-20 | 2008-06-26 | Glaxo Group Limited | 4-benzyl-l ( 2h) -phthalazinones as h1 receptor antagonists |
| US20090182035A1 (en) * | 2007-04-11 | 2009-07-16 | Alcon Research, Ltd. | Use of a combination of olopatadine and cilomilast to treat non-infectious rhinitis and allergic conjunctivitis |
| CA2682730A1 (en) * | 2007-04-11 | 2008-10-23 | Alcon Research, Ltd. | Use of an inhibitor of tnf.alpha. plus an antihistamine to treat allergic rhinitis and allergic conjunctivitis |
| WO2009067597A1 (en) * | 2007-11-21 | 2009-05-28 | Decode Genetics Ehf | 4- (or 5-) substituted catechol derivatives |
| KR20090061972A (ko) * | 2007-12-12 | 2009-06-17 | 한미약품 주식회사 | 베포타스틴 ｐ-톨루엔술폰산염의 결정형, 이의 제조방법 및이를 포함하는 약학 조성물 |
| RS55624B1 (sr) | 2011-02-07 | 2017-06-30 | Scipharm Sàrl | Nova kompozicija za lečenje cistične fibroze |
| KR102226833B1 (ko) * | 2013-06-28 | 2021-03-12 | 한미약품 주식회사 | 레보세티리진 및 몬테루카스트를 포함하는 안정성이 개선된 복합 과립 제형 |
| CN106604747A (zh) * | 2014-08-26 | 2017-04-26 | 基础应用医学研究基金会 | 用于治疗和预防伴随认知缺陷或缺损的神经障碍以及神经变性疾病的产品 |
| NZ731344A (en) | 2014-10-09 | 2018-08-31 | Guangdong Raynovent Biotech Co Ltd | Hydroxyl purine compounds and applications thereof |
| CN109956947A (zh) * | 2017-12-25 | 2019-07-02 | 江苏恒瑞医药股份有限公司 | 一种cns抑制剂的新晶型、制备方法及用途 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| DE2847693A1 (de) * | 1978-11-03 | 1980-05-22 | Hoechst Ag | Verfahren zur herstellung von pyrimido-(6,1-a)-isochinolin-2-onen |
| AU650953B2 (en) | 1991-03-21 | 1994-07-07 | Novartis Ag | Inhaler |
| CZ290266B6 (cs) * | 1993-07-02 | 2002-06-12 | Byk Gulden Lomberg Chemische Fabrik Gmbh | Substituované benzamidy, způsob jejich výroby a farmaceutické prostředky s jejich obsahem |
| US5900421A (en) * | 1997-02-11 | 1999-05-04 | Sepracor Inc. | Methods and compositions for treating allergic asthma and dermatitis using descarboethoxyloratadine |
| US5990147A (en) * | 1997-11-07 | 1999-11-23 | Schering Corporation | H3 receptor ligands of the phenyl-alkyl-imidazoles type |
| BR9804993A (pt) * | 1998-11-10 | 2000-06-06 | Panacea Biotec Ltd | Composição antialérgica e antiinflamatória |
| US6174878B1 (en) * | 1999-08-31 | 2001-01-16 | Alcon Laboratories, Inc. | Topical use of kappa opioid agonists to treat otic pain |
| AU781137B2 (en) * | 1999-10-25 | 2005-05-05 | Altana Pharma Ag | Tetrahydrothiopy ranphthalazinone derivatives as PDE4 inhibitors |
| US7585847B2 (en) * | 2000-02-03 | 2009-09-08 | Coley Pharmaceutical Group, Inc. | Immunostimulatory nucleic acids for the treatment of asthma and allergy |
| GB0115181D0 (en) * | 2001-06-20 | 2001-08-15 | Glaxo Group Ltd | Novel use |
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