HRP20030735B1 - Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors - Google Patents
Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitorsInfo
- Publication number
- HRP20030735B1 HRP20030735B1 HR20030735A HRP20030735A HRP20030735B1 HR P20030735 B1 HRP20030735 B1 HR P20030735B1 HR 20030735 A HR20030735 A HR 20030735A HR P20030735 A HRP20030735 A HR P20030735A HR P20030735 B1 HRP20030735 B1 HR P20030735B1
- Authority
- HR
- Croatia
- Prior art keywords
- 4alkyl
- aryl
- het2
- het2c1
- arylc1
- Prior art date
Links
- -1 2-(substituted-amino)-benzothiazole sulfonamide Chemical class 0.000 title abstract 8
- 239000004030 hiv protease inhibitor Substances 0.000 title 1
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 10
- 125000003118 aryl group Chemical group 0.000 abstract 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 6
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 4
- 150000002431 hydrogen Chemical class 0.000 abstract 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical class 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000001424 substituent group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 abstract 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
-
- 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
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
- C07D277/62—Benzothiazoles
- C07D277/68—Benzothiazoles 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 in position 2
- C07D277/82—Nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Virology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01200529 | 2001-02-14 | ||
| US28775801P | 2001-05-02 | 2001-05-02 | |
| PCT/EP2002/001788 WO2002083657A2 (en) | 2001-02-14 | 2002-02-14 | Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HRP20030735A2 HRP20030735A2 (en) | 2005-08-31 |
| HRP20030735B1 true HRP20030735B1 (en) | 2012-02-29 |
Family
ID=26076833
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HR20030735A HRP20030735B1 (en) | 2001-02-14 | 2003-09-12 | Broadspectrum 2-(substituted-amino)-benzothiazole sulfonamide hiv protease inhibitors |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US7659404B2 (sl) |
| EP (1) | EP1370543B1 (sl) |
| JP (1) | JP4530612B2 (sl) |
| KR (1) | KR100870184B1 (sl) |
| CN (2) | CN101230067B (sl) |
| AP (1) | AP1504A (sl) |
| AT (1) | ATE343567T1 (sl) |
| AU (1) | AU2002302363B2 (sl) |
| BG (1) | BG66301B1 (sl) |
| BR (1) | BR0207862A (sl) |
| CA (1) | CA2438304C (sl) |
| CY (1) | CY1108073T1 (sl) |
| CZ (1) | CZ304273B6 (sl) |
| DE (1) | DE60215623T2 (sl) |
| DK (1) | DK1370543T3 (sl) |
| EA (1) | EA006096B1 (sl) |
| EE (1) | EE05385B1 (sl) |
| ES (1) | ES2275866T3 (sl) |
| HK (1) | HK1061233A1 (sl) |
| HR (1) | HRP20030735B1 (sl) |
| HU (1) | HU229224B1 (sl) |
| IL (2) | IL157171A0 (sl) |
| MX (1) | MXPA03007236A (sl) |
| NO (1) | NO326174B1 (sl) |
| NZ (1) | NZ527391A (sl) |
| PL (1) | PL213327B1 (sl) |
| PT (1) | PT1370543E (sl) |
| SI (1) | SI1370543T1 (sl) |
| SK (1) | SK287582B6 (sl) |
| WO (1) | WO2002083657A2 (sl) |
| ZA (1) | ZA200306086B (sl) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2003501051A (ja) | 1999-05-28 | 2003-01-14 | ビルコ・エヌ・ブイ | 表現型薬物耐性と相関するｈｉｖ−１逆転写酵素における新規な変異プロフィル |
| EP1356082A2 (en) | 2000-10-20 | 2003-10-29 | Virco Bvba | Mutational profiles in hiv-1 reverse transcriptase correlated with phenotypic drug resistance |
| ATE343567T1 (de) | 2001-02-14 | 2006-11-15 | Tibotec Pharm Ltd | Breitspektrum 2-(substituierte-amino)- benzothiazol-sulfonamide hiv protease inhibitoren |
| WO2003064406A1 (en) | 2002-01-07 | 2003-08-07 | Sequoia Pharmaceuticals | Resistance-repellent retroviral protease inhibitors |
| US7157489B2 (en) | 2002-03-12 | 2007-01-02 | The Board Of Trustees Of The University Of Illinois | HIV protease inhibitors |
| US7473524B2 (en) | 2002-07-01 | 2009-01-06 | Hilde Azijn | Mutational profiles in HIV-1 protease correlated with phenotypic drug resistance |
| DE60327768D1 (de) | 2002-07-01 | 2009-07-09 | Tibotec Pharm Ltd | Mutationsprofile bei mit phänotypischer medikamentenresistenz korrelierter hiv-1-protease |
| EP1545518A1 (en) * | 2002-08-02 | 2005-06-29 | Tibotec Pharmaceuticals Ltd. | Broadspectrum 2-amino-benzothiazole sulfonamide hiv protease inhibitors |
| JP4879484B2 (ja) * | 2002-08-02 | 2012-02-22 | テイボテク・フアーマシユーチカルズ・リミテツド | 広スペクトルの２−アミノ−ベンゾチアゾールスルホンアミドｈｉｖプロテアーゼ阻害剤 |
| BRPI0414916A (pt) * | 2003-09-30 | 2006-11-07 | Tibotec Pharm Ltd | métodos para a preparação de compostos de sulfonamida de benzoxazol e intermediários dos mesmos |
| DE10360835A1 (de) * | 2003-12-23 | 2005-07-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische Imidazolverbindungen, deren Herstellung und deren Verwendung als Arzneimittel |
| CA2566340C (en) * | 2004-05-07 | 2014-05-06 | Sequoia Pharmaceuticals, Inc. | Resistance-repellent retroviral protease inhibitors |
| BRPI0607827B8 (pt) | 2005-02-25 | 2021-05-25 | Janssen R & D Ireland | composto precursor de inibidor de protease, processo para a produção do referido composto e seu uso |
| AR053845A1 (es) | 2005-04-15 | 2007-05-23 | Tibotec Pharm Ltd | 5-tiazolilmetil[(1s,2r)-3-[[(2-amino-6-benzoxazolil)sulfonil)](2-metilpropil)amino]-2-hidroxi-1-(fenilmetil)propil]carbamato como mejorador de farmacos metabolizados por el citocromo p450 |
| JO2841B1 (en) * | 2006-06-23 | 2014-09-15 | تيبوتيك فارماسيوتيكالز ليمتد | 2-(substituted-amino) -benzothiazole sulfonamide as protease inhibitors HIV (HIV) |
| WO2011061590A1 (en) | 2009-11-17 | 2011-05-26 | Hetero Research Foundation | Novel carboxamide derivatives as hiv inhibitors |
| JO3090B1 (ar) * | 2009-12-11 | 2017-03-15 | Janssen Sciences Ireland Uc | 5- امينو-4- هيدروكسي-بنتويل اميدات |
| US9024038B2 (en) | 2010-12-27 | 2015-05-05 | Purdue Research Foundation | Compunds and methods for treating HIV |
| SG11201401189WA (en) | 2012-04-20 | 2014-09-26 | Gilead Sciences Inc | Benzothiazol- 6 -yl acetic acid derivatives and their use for treating an hiv infection |
| CN104000824B (zh) * | 2014-05-28 | 2016-07-06 | 中山大学 | 苯并五元杂环类化合物在制备抗hiv-1病毒药物中的应用 |
| US11439608B2 (en) | 2017-09-25 | 2022-09-13 | Qun Lu | Roles of modulators of intersectin-CDC42 signaling in Alzheimer's disease |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
Family Cites Families (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0445926B1 (en) | 1990-03-09 | 1996-08-21 | Milliken Research Corporation | Organic materials having sulfonamido linked poly(oxyalkylene) moieties and their preparation |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| KR100336699B1 (ko) * | 1992-08-25 | 2002-05-13 | 윌리암스 로저 에이 | 레트로바이러스 프로테아제 저해제로서 유용한히드록시에틸아미노 술폰아미드 |
| PH30929A (en) | 1992-09-03 | 1997-12-23 | Janssen Pharmaceutica Nv | Beads having a core coated with an antifungal and a polymer. |
| IS2334B (is) | 1992-09-08 | 2008-02-15 | Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) | Aspartyl próteasi hemjari af nýjum flokki súlfonamíða |
| DK0721331T3 (da) | 1993-10-01 | 2002-02-11 | Astrazeneca Ab | Fremgangsmåde |
| CA2210889C (en) | 1995-01-20 | 2007-08-28 | G.D. Searle & Co. | Bis-sulfonamide hydroxyethylamino retroviral protease inhibitors |
| US6140505A (en) * | 1995-03-10 | 2000-10-31 | G. D. Searle & Co. | Synthesis of benzo fused heterocyclic sulfonyl chlorides |
| US6150556A (en) * | 1995-03-10 | 2000-11-21 | G. D. Dearle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| PL184771B1 (pl) | 1995-03-10 | 2002-12-31 | Searle & Co | Związek stanowiący hydroksyetyloaminosulfonamid pirolidynokarbonyloaminokwasu, kompozycja zawierająca ten związek, jego zastosowanie do wytwarzania kompozycji do leczenia infekcji retrowirusowej i sposób zapobiegania replikacji retrowirusa in vitro |
| US6861539B1 (en) * | 1995-03-10 | 2005-03-01 | G. D. Searle & Co. | Bis-amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| US6143788A (en) * | 1995-03-10 | 2000-11-07 | G.D. Searle & Co. | Bis-amino acid hydroxyethlamino sulfonamide retroviral protease inhibitors |
| US5705500A (en) | 1995-03-10 | 1998-01-06 | G.D. Searle & Co. | Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| AU7722296A (en) | 1995-11-15 | 1997-06-05 | G.D. Searle & Co. | Substituted sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors |
| EE03902B1 (et) | 1996-05-20 | 2002-12-16 | Janssen Pharmaceutica N.V. | Osakesed, nende valmistamismeetod ja kasutamine, farmatseutiline doseerimisvorm ja selle valmistamismeetod, tahke dispersioon ning farmatseutiline pakend |
| ATE241969T1 (de) | 1997-03-26 | 2003-06-15 | Janssen Pharmaceutica Nv | Tabletten mit einem kern, der mit einem pilzbekämpfungsmittel und einem polymeren beschichtet ist |
| AU2010299A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs os aspartyl protease inhibitors |
| ID25551A (id) | 1997-12-24 | 2000-10-12 | Vertex Pharma | Bahan baku obat penghambat protease aspartil |
| US6436989B1 (en) | 1997-12-24 | 2002-08-20 | Vertex Pharmaceuticals, Incorporated | Prodrugs of aspartyl protease inhibitors |
| AU2012199A (en) | 1997-12-24 | 1999-07-19 | Vertex Pharmaceuticals Incorporated | Prodrugs of aspartyl protease inhibitors |
| AU4828199A (en) | 1998-06-23 | 2000-01-10 | Board Of Trustees Of The University Of Illinois, The | Multi-drug resistant retroviral protease inhibitors and associated methods |
| DK1088098T4 (en) | 1998-06-23 | 2015-09-14 | Us Of America Represented By The Secretary Dept Of Health And Human Services | Fitnessassay and methods for reducing HIV resistance to therapy |
| AR031520A1 (es) * | 1999-06-11 | 2003-09-24 | Vertex Pharma | Un compuesto inhibidor de aspartilo proteasa, una composicion que lo comprende y un metodo para tratar un paciente con dicha composicion |
| ATE343567T1 (de) | 2001-02-14 | 2006-11-15 | Tibotec Pharm Ltd | Breitspektrum 2-(substituierte-amino)- benzothiazol-sulfonamide hiv protease inhibitoren |
-
2002
- 2002-02-14 AT AT02729930T patent/ATE343567T1/de active
- 2002-02-14 BR BR0207862-7A patent/BR0207862A/pt not_active IP Right Cessation
- 2002-02-14 DE DE60215623T patent/DE60215623T2/de not_active Expired - Lifetime
- 2002-02-14 HU HU0303257A patent/HU229224B1/hu not_active IP Right Cessation
- 2002-02-14 EP EP02729930A patent/EP1370543B1/en not_active Expired - Lifetime
- 2002-02-14 DK DK02729930T patent/DK1370543T3/da active
- 2002-02-14 US US10/467,609 patent/US7659404B2/en not_active Expired - Fee Related
- 2002-02-14 CA CA2438304A patent/CA2438304C/en not_active Expired - Fee Related
- 2002-02-14 JP JP2002581413A patent/JP4530612B2/ja not_active Expired - Fee Related
- 2002-02-14 CN CN2007101997173A patent/CN101230067B/zh not_active Expired - Fee Related
- 2002-02-14 PL PL363778A patent/PL213327B1/pl unknown
- 2002-02-14 MX MXPA03007236A patent/MXPA03007236A/es active IP Right Grant
- 2002-02-14 NZ NZ527391A patent/NZ527391A/xx not_active IP Right Cessation
- 2002-02-14 WO PCT/EP2002/001788 patent/WO2002083657A2/en active IP Right Grant
- 2002-02-14 EE EEP200300381A patent/EE05385B1/xx not_active IP Right Cessation
- 2002-02-14 AU AU2002302363A patent/AU2002302363B2/en not_active Ceased
- 2002-02-14 IL IL15717102A patent/IL157171A0/xx unknown
- 2002-02-14 CN CNB028049829A patent/CN100369904C/zh not_active Expired - Fee Related
- 2002-02-14 SK SK1102-2003A patent/SK287582B6/sk not_active IP Right Cessation
- 2002-02-14 SI SI200230467T patent/SI1370543T1/sl unknown
- 2002-02-14 ES ES02729930T patent/ES2275866T3/es not_active Expired - Lifetime
- 2002-02-14 EA EA200300891A patent/EA006096B1/ru not_active IP Right Cessation
- 2002-02-14 KR KR1020037010506A patent/KR100870184B1/ko not_active IP Right Cessation
- 2002-02-14 PT PT02729930T patent/PT1370543E/pt unknown
- 2002-02-14 AP APAP/P/2003/002856A patent/AP1504A/en active
- 2002-02-14 CZ CZ2003-2415A patent/CZ304273B6/cs not_active IP Right Cessation
-
2003
- 2003-07-30 IL IL157171A patent/IL157171A/en not_active IP Right Cessation
- 2003-08-06 ZA ZA2003/06086A patent/ZA200306086B/en unknown
- 2003-08-13 NO NO20033584A patent/NO326174B1/no not_active IP Right Cessation
- 2003-09-01 BG BG108143A patent/BG66301B1/bg unknown
- 2003-09-12 HR HR20030735A patent/HRP20030735B1/xx not_active IP Right Cessation
-
2004
- 2004-06-03 HK HK04104020A patent/HK1061233A1/xx not_active IP Right Cessation
-
2007
- 2007-01-25 CY CY20071100088T patent/CY1108073T1/el unknown
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1995006030A1 (en) * | 1993-08-24 | 1995-03-02 | G.D. Searle & Co. | Hydroxyethylamino sulphonamides useful as retroviral protease inhibitors |
| WO1996028463A1 (en) * | 1995-03-10 | 1996-09-19 | G.D. Searle & Co. | Amino acid hydroxyethylamino sulfonamide retroviral protease inhibitors |
| WO1999065870A2 (en) * | 1998-06-19 | 1999-12-23 | Vertex Pharmaceuticals Incorporated | Sulfonamide inhibitors of aspartyl protease |
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| A1OB | Publication of a patent application | ||
| ARAI | Request for the grant of a patent on the basis of the submitted results of a substantive examination of a patent application | ||
| B1PR | Patent granted | ||
| ODRP | Renewal fee for the maintenance of a patent |
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