HUP0300527A2 - Pirrolopirimidinon-származékok, a vegyületek előállítása és alkalmazása - Google Patents
Pirrolopirimidinon-származékok, a vegyületek előállítása és alkalmazásaInfo
- Publication number
- HUP0300527A2 HUP0300527A2 HU0300527A HUP0300527A HUP0300527A2 HU P0300527 A2 HUP0300527 A2 HU P0300527A2 HU 0300527 A HU0300527 A HU 0300527A HU P0300527 A HUP0300527 A HU P0300527A HU P0300527 A2 HUP0300527 A2 HU P0300527A2
- Authority
- HU
- Hungary
- Prior art keywords
- optionally substituted
- substituted alkyl
- cycloalkyl
- hydrogen atom
- group
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- DXVAQZJPPDWTNY-UHFFFAOYSA-N pyrrolo[3,2-d]pyrimidin-2-one Chemical class O=C1N=CC2=NC=CC2=N1 DXVAQZJPPDWTNY-UHFFFAOYSA-N 0.000 title abstract 2
- 125000000547 substituted alkyl group Chemical group 0.000 abstract 10
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 7
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 3
- 125000000304 alkynyl group Chemical group 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- -1 piperidino, morpholino, piperazinyl Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/02—Nasal agents, e.g. decongestants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/14—Drugs for genital or sexual disorders; Contraceptives for lactation disorders, e.g. galactorrhoea
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
Abstract
A találmány (1) általános képletű pirrolopirimidinon-származékokra,előállításukra alkalmas eljárásra, az előállítás közbenső termékeire,a vegyületek terápiás szerként való alkalmazására és a vegyültekettartalmazó gyógyászati készítményekre vonatkozik, a képletben R1jelentése hidrogénatom; adott esetben helyettesített alkilcsoport;vagy cikloalkilcsoport; R2 jelentése hidrogénatom; halogénatom; adottesetben helyettesített alkilcsoport; cikloalkilcsoport;alkenilcsoport; vagy alkinilcsoport; R3 jelentése hidrogénatom; adottesetben helyettesített alkilcsoport; cikloalkilcsoport; alkenilcsoportvagy alkinilcsoport; R4 jelentése adott esetben helyettesítettalkilcsoport; alkenilcsoport; alkinilcsoport; vagy cikloalkilcsoport;R5 jelentése -SO2NR6R7, -NHSO2NR6R7, -NHCOCONR6R7, -NHSO2R8 vagy -NHCOR8 általános képletű csoport; vagy adott estben helyettesítettfenil- vagy heterociklusos csoport; R6 és R7 jelentése hidrogénatomvagy adott esetben helyettesített alkilcsoport; vagy R6 és R7 anitrogénatommal együtt, amelyhez kapcsolódnak, adott esetbenhelyettesített gyűrűt alkot; R8 jelentése adott esetben helyettesítettalkilcsoport; vagy cikloalkilcsoport; R9 jelentése adott esetbenhelyettesített alkilcsoport; vagy nitrogénatomot tartalmazó, adottesetben helyettesített heteroarilcsoport; R10 jelentése hidrogénatom;vagy adott esetben helyettesített alkilcsoport; R11 és R12 jelentéseegymástól függetlenül hidrogénatom vagy alkilcsoport; R13 jelentésehidrogénatom; adott esetben helyettesített alkilcsoport; vagycikloalkilcsoport; és R14 és R15 jelentése hidrogénatom vagy adottesetben helyettesített alkilcsoport; cikloalkilcsoport; vagy R14 ésR15 a nitrogénatommal együtt, amelyhez kapcsolódnak, adott esetbenhelyettesített pirrolidinil-, piperidino-, morfolino-, piperazinil-vagy homopiperazinilcsoportot alkot. A találmány szerinti vegyületek aGMP PDE V inhibitor hatásúak. Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR2000/7625 | 2000-02-17 | ||
| KR20000007625A KR100358083B1 (ko) | 2000-02-17 | 2000-02-17 | 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도 |
| PCT/KR2001/000227 WO2001060825A1 (en) | 2000-02-17 | 2001-02-15 | Pyrrolopyrimidinone derivatives, process of preparation and use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| HUP0300527A2 true HUP0300527A2 (hu) | 2003-07-28 |
| HUP0300527A3 HUP0300527A3 (en) | 2012-10-29 |
| HU230344B1 HU230344B1 (hu) | 2016-02-29 |
Family
ID=19647449
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0300527A HU230344B1 (hu) | 2000-02-17 | 2001-02-15 | Pirrolopirimidinon-származékok, a vegyületek előállítása és alkalmazása |
Country Status (23)
| Country | Link |
|---|---|
| US (1) | US6962911B2 (hu) |
| EP (1) | EP1257553B1 (hu) |
| JP (1) | JP4845076B2 (hu) |
| KR (1) | KR100358083B1 (hu) |
| CN (1) | CN1312153C (hu) |
| AT (1) | ATE267829T1 (hu) |
| AU (2) | AU3614001A (hu) |
| BR (1) | BRPI0108395B8 (hu) |
| CA (1) | CA2400268C (hu) |
| DE (1) | DE60103508T2 (hu) |
| DK (1) | DK1257553T3 (hu) |
| ES (1) | ES2222344T3 (hu) |
| HU (1) | HU230344B1 (hu) |
| IL (2) | IL151234A0 (hu) |
| MX (1) | MXPA02007942A (hu) |
| NO (1) | NO323553B1 (hu) |
| NZ (1) | NZ520842A (hu) |
| PL (1) | PL210796B1 (hu) |
| PT (1) | PT1257553E (hu) |
| RU (1) | RU2263676C2 (hu) |
| TR (1) | TR200402101T4 (hu) |
| WO (1) | WO2001060825A1 (hu) |
| ZA (1) | ZA200206587B (hu) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR100358083B1 (ko) * | 2000-02-17 | 2002-10-25 | 에스케이케미칼주식회사 | 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도 |
| EP1362858A1 (en) * | 2002-05-15 | 2003-11-19 | SK Chemicals Co., Ltd. | Pyrrolopyrimidinone derivates, process of preparation and use |
| DE10229778A1 (de) * | 2002-07-03 | 2004-01-29 | Bayer Ag | Neue Verwendung von Imidazotriazinonen |
| FR2842809A1 (fr) * | 2002-07-26 | 2004-01-30 | Greenpharma Sas | NOUVELLES PYRAZOLO[1,5-a]-1,3,5-TRIAZINES SUBSTITUEES ET LEURS ANALOGUES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT, UTILISATION A TITRE DE MEDICAMENT ET PROCEDES POUR LEUR PREPARATION |
| CN100374441C (zh) * | 2003-06-06 | 2008-03-12 | 天津倍方科技发展有限公司 | 二氢吡咯[2，3-d]嘧啶-4-酮衍生物，其制备方法及其制药用途 |
| AR058071A1 (es) * | 2005-10-03 | 2008-01-23 | Astrazeneca Ab | Derivados de dihidropirazolo (3,4-e)(1,4)diazepina. procesos de obtencion y composiciones farmaceuticas. |
| CA2666696C (en) | 2006-07-03 | 2013-01-15 | Sk Chemicals Co., Ltd. | Salts of pyrrolopyrimidinone derivatives and process for preparing the same |
| KR20080003599A (ko) * | 2006-07-03 | 2008-01-08 | 에스케이케미칼주식회사 | 피롤로피리미디논 유도체의 겐티세이트 염 및 이의제조방법 |
| KR101002490B1 (ko) * | 2007-06-09 | 2010-12-17 | 동아제약주식회사 | 유데나필을 유효성분으로 함유하는 만성 심부전증 치료용약학적 조성물 |
| WO2011047320A2 (en) | 2009-10-16 | 2011-04-21 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compounds and methods of making and using the same |
| EP2488525B1 (en) | 2009-10-16 | 2018-04-25 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
| CA2777741A1 (en) | 2009-10-16 | 2011-04-21 | Rib-X Pharmaceuticals, Inc. | Antimicrobial compounds and methods of making and using the same |
| EP2556820A4 (en) | 2010-04-05 | 2015-01-21 | Sk Chemicals Co Ltd | COMPOSITION CONTAINING PDE5 INHIBITOR FOR MITIGATION OF SKIN WRINKLES |
| CN102372730B (zh) * | 2010-08-19 | 2014-03-26 | 山东轩竹医药科技有限公司 | 桥环取代的磷酸二酯酶抑制剂 |
| CN102134242B (zh) * | 2011-01-21 | 2013-08-28 | 浙江大德药业集团有限公司 | 一种用于治疗阳痿的快速长效的化合物 |
| TWI490220B (zh) * | 2011-04-04 | 2015-07-01 | Sk Chemicals Co Ltd | 包含ｐｄｅ５抑制劑之用於減少皮膚皺紋之組成物 |
| CN103958514B (zh) * | 2011-04-15 | 2018-07-03 | 梅琳塔治疗公司 | 抗微生物化合物及制备和使用所述化合物的方法 |
| WO2013036081A2 (en) * | 2011-09-09 | 2013-03-14 | Sk Chemicals Co., Ltd. | Composition for reducing skin wrinkles including pde5 inhibitor |
| US9750743B2 (en) | 2012-12-04 | 2017-09-05 | Aribio Inc. | Composition comprising phosphodiesterase type 5 inhibitor for inhibiting apoptosis of nerve cells |
| AU2014315045A1 (en) | 2013-09-09 | 2016-03-24 | Melinta Therapeutics, Inc. | Antimicrobial compounds and methods of making and using the same |
| CN106103442A (zh) | 2013-09-09 | 2016-11-09 | 梅琳塔治疗公司 | 抗微生物化合物及制备和使用其的方法 |
| CN107922418A (zh) | 2015-03-11 | 2018-04-17 | 梅琳塔治疗公司 | 抗微生物化合物及制备和使用所述化合物的方法 |
| CN104744478B (zh) * | 2015-03-20 | 2016-08-24 | 中国人民解放军第二军医大学 | 一种防治辐射损伤的化合物、单晶及其制备方法和应用 |
| EP3377495B1 (en) | 2015-11-16 | 2022-03-16 | Topadur Pharma AG | 2-phenyl-3,4-dihydropyrrolo[2,1-f] [1,2,4]triazinone derivatives as phosphodiesterase inhibitors and uses thereof |
| US11155558B2 (en) | 2017-05-22 | 2021-10-26 | Topadur Pharma Ag | Dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof |
| JP2021533152A (ja) | 2018-08-06 | 2021-12-02 | ニコックス エス．エー． | 一酸化窒素放出性ホスホジエステラーゼ５型阻害薬 |
| EP3887376A1 (en) | 2018-11-28 | 2021-10-06 | Topadur Pharma AG | Novel dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof |
| KR102271305B1 (ko) | 2020-05-21 | 2021-06-30 | 주식회사 아리바이오 | 치매 예방 및 치료용 조성물 |
| WO2021245192A1 (en) | 2020-06-04 | 2021-12-09 | Topadur Pharma Ag | Novel dual mode of action soluble guanylate cyclase activators and phosphodiesterase inhibitors and uses thereof |
| CN111825593B (zh) * | 2020-08-19 | 2023-04-07 | 上海成澄科技有限公司 | 3-氨基吡咯-2-甲酰胺类化合物的合成方法 |
| KR102272907B1 (ko) | 2020-11-05 | 2021-07-05 | 주식회사 아리바이오 | 치매 예방 및 치료용 조성물 |
| KR102272910B1 (ko) | 2021-01-28 | 2021-07-06 | 주식회사 아리바이오 | 당뇨병을 동반한 치매 예방 및 치료용 조성물 |
| KR20220140960A (ko) | 2021-04-12 | 2022-10-19 | 주식회사 아리바이오 | 당뇨병을 동반한 치매 예방 및 치료용 조성물 |
| KR102311224B1 (ko) | 2021-04-23 | 2021-10-13 | 주식회사 아리바이오 | Pde5 억제제와 글루코코르티코이드 수용체 길항제 병용투여를 통한 치매 예방 및 치료용 조성물 |
| KR20220146095A (ko) | 2021-04-23 | 2022-11-01 | 주식회사 아리바이오 | Pde5 억제제와 글루코코르티코이드 수용체 길항제 병용투여를 통한 치매 예방 및 치료용 조성물 |
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| CN1281588C (zh) * | 1997-04-25 | 2006-10-25 | 美国辉瑞有限公司 | 制备吡唑并嘧啶酮类化合物的新型中间体 |
| PT1371647E (pt) * | 1998-04-20 | 2005-10-31 | Pfizer | Derivados do acido piridina-3-carboxilico e sua utilizacao como intermediarios |
| KR100358083B1 (ko) * | 2000-02-17 | 2002-10-25 | 에스케이케미칼주식회사 | 피롤로피리미디논 유도체와 이의 제조방법, 그리고 이의용도 |
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2000
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