PE20030418A1 - Pirrolo pirimidinas como inhibidores de cisteina proteasas - Google Patents
Pirrolo pirimidinas como inhibidores de cisteina proteasasInfo
- Publication number
- PE20030418A1 PE20030418A1 PE2002000833A PE2002000833A PE20030418A1 PE 20030418 A1 PE20030418 A1 PE 20030418A1 PE 2002000833 A PE2002000833 A PE 2002000833A PE 2002000833 A PE2002000833 A PE 2002000833A PE 20030418 A1 PE20030418 A1 PE 20030418A1
- Authority
- PE
- Peru
- Prior art keywords
- aryl
- alkyl
- cycloalkyl
- pyrimidines
- inhibitors
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 102000005927 Cysteine Proteases Human genes 0.000 title 1
- 108010005843 Cysteine Proteases Proteins 0.000 title 1
- -1 PIRROLO PYRIMIDINES Chemical class 0.000 title 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-M hydroxide Chemical class [OH-] XLYOFNOQVPJJNP-UHFFFAOYSA-M 0.000 abstract 3
- 101100295738 Gallus gallus COR3 gene Proteins 0.000 abstract 1
- 101100533890 Hypocrea jecorina (strain QM6a) sor3 gene Proteins 0.000 abstract 1
- 101100533874 Hypocrea jecorina (strain QM6a) sor5 gene Proteins 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 201000008482 osteoarthritis Diseases 0.000 abstract 1
- 150000003230 pyrimidines Chemical class 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 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
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
-
- 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
- A61P37/02—Immunomodulators
-
- 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
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Communicable Diseases (AREA)
- Neurosurgery (AREA)
- Hematology (AREA)
- Pulmonology (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
SE REFIERE A PIRROLO PIRIMIDINAS DE FORMULA I DONDE R ES H, R2, OR2, NR1R2; R1 ES H, ALQUILO, CICLOALQUILO C3-C10; R2 ES ALQUILO, CICLOALQUILO C3-C10; R1 Y R2 SON OPCIONALMENTE SUSTITUIDOS CON HALO, HIDROXI, ALCOXI, CN, NOS; X ES =N, =CZ; Z ES H, CONR3R4, NHCOR3, CH2NHCOR3, COR3, SOR3, PC=CQR4, ENTRE OTROS; P Y Q SON H, ALQUILO, ARILO; R3 ES ARILO, ARILO-ALQUILO, CICLOALQUILO C3-C10, ENTRE OTROS; R4 ES H, ARILO, ARILO-ALQUILO, ARILO-ALQUENILO, CICLOALQUILO C3-C10, ENTRE OTROS, O R3 Y R4 FORMAN JUNTO A N UN N-HETEROCICLO; R6 ES H, ALQUILO, CARBOXI, ACILO, ENTRE OTROS; R5 ES ARILO, ARILO-ALQUILO, ARILOXI, AROILO, N-HETEROCICLILO OPCIONALMENTE SUSTITUIDO CON R7; R7 ES HALO, HIDROXI; R13 ES ALQUILO, CICLOALQUILO C3-10, CICLOALQUILO C3-C10-ALQUILO OPCIONALMENTE SUSTITUIDOS CON HALO, HIDROXI, CN, NO2; R14 ES H, ARILO, ARILO-ALQUILO-W, CICLOALQUILO, N-HETEROCICLILO, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION; LOS COMPUESTOS SON INHIBIDORES DE CATEPSINA K Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE INFLAMACION, ARTRITIS REUMATOIDE, OSTEOARTRITIS, OSTEOPOROSIS, TUMORES
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0121033.5A GB0121033D0 (en) | 2001-08-30 | 2001-08-30 | Organic compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20030418A1 true PE20030418A1 (es) | 2003-06-12 |
Family
ID=9921234
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2002000833A PE20030418A1 (es) | 2001-08-30 | 2002-08-29 | Pirrolo pirimidinas como inhibidores de cisteina proteasas |
Country Status (29)
| Country | Link |
|---|---|
| US (2) | US7452886B2 (es) |
| EP (1) | EP1423391B8 (es) |
| JP (1) | JP4629334B2 (es) |
| KR (1) | KR100695845B1 (es) |
| CN (1) | CN100372849C (es) |
| AR (1) | AR036374A1 (es) |
| AT (1) | ATE326469T1 (es) |
| AU (1) | AU2002333760B2 (es) |
| BR (1) | BR0212226A (es) |
| CA (1) | CA2458684C (es) |
| CY (1) | CY1105573T1 (es) |
| DE (1) | DE60211530T2 (es) |
| DK (1) | DK1423391T3 (es) |
| EC (1) | ECSP044998A (es) |
| ES (1) | ES2262888T3 (es) |
| GB (1) | GB0121033D0 (es) |
| HU (1) | HUP0401301A3 (es) |
| IL (3) | IL160367A0 (es) |
| MX (1) | MXPA04001935A (es) |
| MY (1) | MY157368A (es) |
| NO (1) | NO328890B1 (es) |
| NZ (1) | NZ531343A (es) |
| PE (1) | PE20030418A1 (es) |
| PL (1) | PL368280A1 (es) |
| PT (1) | PT1423391E (es) |
| RU (1) | RU2331644C2 (es) |
| TW (1) | TWI297690B (es) |
| WO (1) | WO2003020721A1 (es) |
| ZA (1) | ZA200401042B (es) |
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| US20030144234A1 (en) * | 2001-08-30 | 2003-07-31 | Buxton Francis Paul | Methods for the treatment of chronic pain and compositions therefor |
| SE0201980D0 (sv) | 2002-06-24 | 2002-06-24 | Astrazeneca Ab | Novel compounds |
| GB0220187D0 (en) * | 2002-08-30 | 2002-10-09 | Novartis Ag | Organic compounds |
| NZ538961A (en) | 2002-09-24 | 2008-02-29 | Novartis Ag | Sphingosine-1-phosphate receptor agonists in the treatment of demyelinating disorders |
| AR043692A1 (es) * | 2003-02-06 | 2005-08-10 | Novartis Ag | 2-cianopirrolopirimidinas y sus usos farmaceuticos |
| GB0304640D0 (en) * | 2003-02-28 | 2003-04-02 | Novartis Ag | Organic compounds |
| US7498323B2 (en) | 2003-04-18 | 2009-03-03 | Ono Pharmaceuticals Co., Ltd. | Spiro-piperidine compounds and medicinal use thereof |
| US20070037835A1 (en) * | 2003-04-28 | 2007-02-15 | Pamposh Ganju | Pharmaceutical composition comprising a cathepsin s inhibitor and an opioid |
| EP1797883A3 (en) * | 2003-04-28 | 2007-08-01 | Novartis AG | Pharmaceutical composition comprising a cathepsin S inhibitor and an opioid |
| BRPI0409684A (pt) * | 2003-04-30 | 2006-04-18 | Fmc Corp | derivados de dihidrobenzofurano e dihidrobenzopirano (dihalopropenil) fenilalquila substituìdos inseticidas |
| WO2005011703A1 (en) * | 2003-08-04 | 2005-02-10 | Akzo Nobel N.V. | 2-cyano-1,3,5-triazine-4,6-diamine derivatives |
| WO2005023810A1 (en) | 2003-09-10 | 2005-03-17 | Virochem Pharma Inc. | Spirohydantoin compounds and methods for the modulation of chemokine receptor activity |
| CN1918137B (zh) | 2004-02-18 | 2012-08-01 | 阿斯利康(瑞典)有限公司 | 四唑化合物及其作为代谢型谷氨酸受体拮抗剂的应用 |
| US20070197510A1 (en) * | 2004-03-10 | 2007-08-23 | Kazuyuki Ohmoto | Nitriles and medicinal compositions containing the same as the active ingredient |
| ES2251292B1 (es) | 2004-04-20 | 2007-07-01 | Inke, S.A. | Procedimiento para la obtencion de un compuesto farmaceuticamente activo y de sus intermedios de sintesis. |
| EP1756109B1 (en) | 2004-05-03 | 2016-07-13 | Janssen Pharmaceutica NV | Novel indole derivatives as selective androgen receptor modulators (sarms) |
| TW200614993A (en) | 2004-06-11 | 2006-05-16 | Akzo Nobel Nv | 4-phenyl-pyrimidine-2-carbonitrile derivatives |
| WO2006022454A1 (ja) | 2004-08-27 | 2006-03-02 | Ono Pharmaceutical Co., Ltd | 塩基性基を含有する化合物およびその用途 |
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| CA2617725C (en) * | 2005-08-05 | 2012-04-03 | Hybrigenics Sa | Novel cysteine protease inhibitors and their therapeutic applications |
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| TW200745055A (en) * | 2005-09-23 | 2007-12-16 | Organon Nv | 4-Phenyl-6-substituted-pyrimidine-2-carbonitrile derivatives |
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| PE20070530A1 (es) * | 2005-10-26 | 2007-05-31 | Smithkline Beecham Corp | Compuestos derivados de tiazoles sustituidos como agentes de apertura de canales de potasio activados por calcio de alta conductancia |
| DK1961744T3 (da) | 2005-11-18 | 2013-07-15 | Ono Pharmaceutical Co | Forbindelse indeholdende basiske grupper samt anvendelse deraf |
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| BRPI0914139A2 (pt) | 2008-06-20 | 2015-10-20 | Novartis Ag | composições pediátricas para o tratamento de esclerose múltipla |
| US8026236B2 (en) | 2009-01-16 | 2011-09-27 | N.V. Organon | 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives |
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| WO2011086125A1 (en) | 2010-01-15 | 2011-07-21 | N.V. Organon | 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES |
| JP5816678B2 (ja) | 2010-04-14 | 2015-11-18 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | ＰＩ３Ｋδ阻害剤としての縮合誘導体 |
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| WO2012027495A1 (en) | 2010-08-27 | 2012-03-01 | University Of The Pacific | Piperazinylpyrimidine analogues as protein kinase inhibitors |
| CN103339265B (zh) | 2010-10-06 | 2018-03-30 | 生物医学研究机构私人基金会 | 用于乳腺癌转移的诊断、预后和治疗的方法 |
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| ES2873001T3 (es) | 2011-09-02 | 2021-11-03 | Incyte Holdings Corp | Heterociclaminas como inhibidores de PI3K |
| AR090548A1 (es) | 2012-04-02 | 2014-11-19 | Incyte Corp | Azaheterociclobencilaminas biciclicas como inhibidores de pi3k |
| EP2650682A1 (en) | 2012-04-09 | 2013-10-16 | Fundació Privada Institut de Recerca Biomèdica | Method for the prognosis and treatment of cancer metastasis |
| ES2644965T3 (es) * | 2012-04-17 | 2017-12-01 | Astellas Pharma Inc. | Compuesto heterocíclico aromático bicíclico nitrogenado |
| TR201819859T4 (tr) | 2012-06-06 | 2019-01-21 | Fundacio Inst De Recerca Biomedica Irb Barcelona | Akciğer kanseri metastazının tanısı ve prognozu için yöntem. |
| US10119171B2 (en) | 2012-10-12 | 2018-11-06 | Inbiomotion S.L. | Method for the diagnosis, prognosis and treatment of prostate cancer metastasis |
| CN104995313A (zh) | 2012-10-12 | 2015-10-21 | 生物运动有限公司 | 使用c-maf的前列腺癌转移的诊断、预后和治疗的方法 |
| WO2014184679A2 (en) | 2013-03-15 | 2014-11-20 | Inbiomotion S.L. | Method for the prognosis and treatment of renal cell carcinoma metastasis |
| EP2971113B1 (en) | 2013-03-15 | 2020-08-12 | Fundació Institut de Recerca Biomèdica (IRB Barcelona) | Method for the prognosis and treatment of cancer metastasis |
| DK3055429T3 (en) | 2013-10-09 | 2019-04-23 | Fundacio Inst De Recerca Biomedica Irb Barcelona | Procedure for the prognosis and treatment of metastatic bone cancer resulting from breast cancer |
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| JP6816005B2 (ja) | 2015-02-27 | 2021-01-20 | インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ | Ｐｉ３ｋ阻害剤の塩及びその調製のためのプロセス |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE609808A (es) | 1960-11-02 | |||
| CH627919A5 (de) | 1977-04-14 | 1982-02-15 | Ciba Geigy Ag | Herbizide mittel. |
| US5958930A (en) * | 1991-04-08 | 1999-09-28 | Duquesne University Of The Holy Ghost | Pyrrolo pyrimidine and furo pyrimidine derivatives |
| ATE159257T1 (de) * | 1994-05-03 | 1997-11-15 | Ciba Geigy Ag | Pyrrolopyrimidinderivate mit antiproliferativer wirkung |
| US5683999A (en) * | 1995-03-17 | 1997-11-04 | The Dupont Merck Pharmaceutical Company | Cyclic urea HIV protease inhibitors |
| DK0831829T3 (da) * | 1995-06-07 | 2003-12-15 | Pfizer | Heterocykliske, ringkondenserede pyrimidinderivater |
| CA2283961A1 (en) * | 1997-03-19 | 1998-09-24 | Basf Aktiengesellschaft | Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors |
| AU4710699A (en) * | 1998-06-30 | 2000-01-17 | Eli Lilly And Company | Bicyclic sPLA2 inhibitors |
| KR20010085824A (ko) * | 1998-09-18 | 2001-09-07 | 스타르크, 카르크 | 단백질 키나아제 억제제로서의 피롤로피리미딘 |
| HRP20020509B1 (en) * | 1999-12-10 | 2005-06-30 | Pfizer Products Inc. | PYRROLO[2,3-d]PYRIMIDINE COMPOUNDS |
| US20030225036A1 (en) * | 2000-03-20 | 2003-12-04 | Aleksandr Kolesnikov | Non-amidine containing protease inhibitors |
| CN1657523A (zh) | 2000-04-28 | 2005-08-24 | 田边制药株式会社 | 环状化合物 |
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2001
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