ATE305932T1 - Rapanycin29-enole - Google Patents
Rapanycin29-enoleInfo
- Publication number
- ATE305932T1 ATE305932T1 AT02768642T AT02768642T ATE305932T1 AT E305932 T1 ATE305932 T1 AT E305932T1 AT 02768642 T AT02768642 T AT 02768642T AT 02768642 T AT02768642 T AT 02768642T AT E305932 T1 ATE305932 T1 AT E305932T1
- Authority
- AT
- Austria
- Prior art keywords
- enole
- enols
- useful
- treatment
- solid tumors
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 230000001506 immunosuppresive effect Effects 0.000 abstract 1
- 230000000508 neurotrophic effect Effects 0.000 abstract 1
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 abstract 1
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 abstract 1
- 229960002930 sirolimus Drugs 0.000 abstract 1
- 208000019553 vascular disease Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- 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
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
- C07D493/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31421101P | 2001-08-22 | 2001-08-22 | |
| PCT/US2002/026622 WO2003018573A1 (en) | 2001-08-22 | 2002-08-21 | Rapamycin 29-enols |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ATE305932T1 true ATE305932T1 (de) | 2005-10-15 |
Family
ID=23219037
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AT02768642T ATE305932T1 (de) | 2001-08-22 | 2002-08-21 | Rapanycin29-enole |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6677357B2 (de) |
| EP (1) | EP1419154B1 (de) |
| JP (1) | JP2005501868A (de) |
| CN (1) | CN1310908C (de) |
| AT (1) | ATE305932T1 (de) |
| BR (1) | BR0211986A (de) |
| CA (1) | CA2455308A1 (de) |
| DE (1) | DE60206512T2 (de) |
| DK (1) | DK1419154T3 (de) |
| ES (1) | ES2246409T3 (de) |
| MX (1) | MXPA04001524A (de) |
| WO (1) | WO2003018573A1 (de) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE60231868D1 (de) * | 2001-04-24 | 2009-05-20 | Purdue Research Foundation | Folat-mimetika und deren folatrezeptorbindende konjugate |
| US20030176455A1 (en) * | 2002-03-13 | 2003-09-18 | Wyeth | Method of inhibiting cell death |
| CA2484640C (en) * | 2002-05-15 | 2012-01-17 | Endocyte, Inc. | Vitamin-mitomycin conjugates |
| RU2344821C2 (ru) | 2002-07-30 | 2009-01-27 | Уайт | Парентеральные композиции, содержащие гидроксиэфиры рапамицина |
| EP2517729A3 (de) | 2003-01-27 | 2013-01-02 | Endocyte, Inc. | Vitaminrezeptorbindende Wirkstofffreisetzungskonjugate |
| US20070155771A1 (en) * | 2003-04-11 | 2007-07-05 | David Rubinsztein | Methods and means for treating protein conformational disorders |
| US7349971B2 (en) * | 2004-02-05 | 2008-03-25 | Scenera Technologies, Llc | System for transmitting data utilizing multiple communication applications simultaneously in response to user request without specifying recipient's communication information |
| JP5149620B2 (ja) | 2004-07-23 | 2013-02-20 | エンドサイト,インコーポレイテッド | 2価リンカーおよびその結合体 |
| US8313763B2 (en) | 2004-10-04 | 2012-11-20 | Tolmar Therapeutics, Inc. | Sustained delivery formulations of rapamycin compounds |
| CA2582374A1 (en) * | 2004-10-04 | 2006-04-20 | Qlt Usa, Inc. | Ocular delivery of polymeric delivery formulations |
| US8021849B2 (en) | 2004-11-05 | 2011-09-20 | Siemens Healthcare Diagnostics Inc. | Methods and kits for the determination of sirolimus in a sample |
| US7632307B2 (en) * | 2004-12-16 | 2009-12-15 | Advanced Cardiovascular Systems, Inc. | Abluminal, multilayer coating constructs for drug-delivery stents |
| US7273874B2 (en) | 2004-12-20 | 2007-09-25 | Wyeth | Rapamycin derivatives and the uses thereof in the treatment of neurological disorders |
| WO2006068932A2 (en) | 2004-12-20 | 2006-06-29 | Wyeth | Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders |
| BRPI0607932A2 (pt) | 2005-02-09 | 2016-11-08 | Wyeth Corp | polimorfo cci-779, processo para preparar polimorfo cci-779, composição farmacêutica, kit, e método para preparar uma composição farmacêutica |
| WO2006096325A1 (en) * | 2005-03-07 | 2006-09-14 | Wyeth | Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin |
| JP2008537543A (ja) * | 2005-03-07 | 2008-09-18 | ノバルティス アクチエンゲゼルシャフト | 神経変性状態に関与する遺伝子 |
| CN101175757B (zh) * | 2005-03-16 | 2012-11-14 | 恩多塞特公司 | 蝶酸及其缀合物的合成和纯化 |
| NZ563003A (en) * | 2005-04-27 | 2011-03-31 | Univ Florida | Use of a farnesyl transferase inhibitor to enhance autophagic protein degradation in protein conformation disorders |
| US7189582B2 (en) * | 2005-04-27 | 2007-03-13 | Dade Behring Inc. | Compositions and methods for detection of sirolimus |
| KR20130113543A (ko) * | 2005-08-19 | 2013-10-15 | 엔도사이트, 인코포레이티드 | 복수-약제 리간드 공액체 |
| US20080280937A1 (en) * | 2005-08-19 | 2008-11-13 | Christopher Paul Leamon | Ligand Conjugates of Vinca Alkaloids, Analogs, and Derivatives |
| AR058561A1 (es) * | 2005-12-20 | 2008-02-13 | Wyeth Corp | Control de la estabilidad de la forma de dosificacion de cci -779 a traves del control de impurezas de sustancias de farmaco |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| US20080175887A1 (en) | 2006-11-20 | 2008-07-24 | Lixiao Wang | Treatment of Asthma and Chronic Obstructive Pulmonary Disease With Anti-proliferate and Anti-inflammatory Drugs |
| US9737640B2 (en) | 2006-11-20 | 2017-08-22 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414526B2 (en) * | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising oils, fatty acids, and/or lipids |
| US20080276935A1 (en) | 2006-11-20 | 2008-11-13 | Lixiao Wang | Treatment of asthma and chronic obstructive pulmonary disease with anti-proliferate and anti-inflammatory drugs |
| US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| WO2008101231A2 (en) * | 2007-02-16 | 2008-08-21 | Endocyte, Inc. | Methods and compositions for treating and diagnosing kidney disease |
| CN101678124A (zh) * | 2007-03-14 | 2010-03-24 | 恩多塞特公司 | 结合配体连接的微管溶素递药缀合物 |
| JP2008305262A (ja) * | 2007-06-08 | 2008-12-18 | Konica Minolta Business Technologies Inc | サーバ及びシンクライアント環境でのプリンタ紹介方法 |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| CN101784565B (zh) | 2007-06-25 | 2014-12-10 | 恩多塞特公司 | 含有亲水性间隔区接头的共轭物 |
| EP2209374B1 (de) | 2007-10-25 | 2014-12-03 | Endocyte, Inc. | Tubulysine und verfahren zu ihrer herstellung |
| WO2010024898A2 (en) | 2008-08-29 | 2010-03-04 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| PT2365802T (pt) | 2008-11-11 | 2017-11-14 | Univ Texas | Microcápsulas de rapamicina e utilização para o tratamento de cancro |
| US9283211B1 (en) | 2009-11-11 | 2016-03-15 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
| WO2013013708A1 (en) | 2011-07-26 | 2013-01-31 | Fundació Institut D'investigació Biomèdica De Bellvitge | Treatment of acute rejection in renal transplant |
| EP2589383A1 (de) | 2011-11-06 | 2013-05-08 | Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Berlin | FKBP-subtypspezifisches Rapamycin-Analogon zur Verwendung bei der Behandlung von Erkrankungen |
| WO2013126797A1 (en) | 2012-02-24 | 2013-08-29 | Purdue Research Foundation | Cholecystokinin b receptor targeting for imaging and therapy |
| US20140080175A1 (en) | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
| CN103705925B (zh) | 2012-09-29 | 2018-03-30 | 段磊 | 抑制PI3K/AKT/mTOR信号通路的药物组合 |
| US9750728B2 (en) | 2012-09-29 | 2017-09-05 | Targeted Therapeutics, Llc | Method and pharmaceutical composition for inhibiting PI3K/AKT/mTOR signaling pathway |
| US20150290176A1 (en) | 2012-10-12 | 2015-10-15 | The Board Of Regents Of The University Of Texas System | Use of mtor inhibitors to treat vascular cognitive impairment |
| CN104869998A (zh) | 2012-10-16 | 2015-08-26 | 恩多塞特公司 | 含有非天然氨基酸的药物递送缀合物以及其使用方法 |
| EP2968281B1 (de) | 2013-03-13 | 2020-08-05 | The Board of Regents of The University of Texas System | Mtor-hemmer zur vorbeugung von darmpolypenwachstum |
| US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
| DK3089737T3 (da) | 2013-12-31 | 2021-12-13 | Rapamycin Holdings Llc | Orale rapamycin-nanopartikelpræparater og anvendelse. |
| CA2968049A1 (en) | 2014-04-16 | 2015-10-22 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
| CN114949250A (zh) | 2016-04-14 | 2022-08-30 | 斯宾纳克生物科学公司 | 用于递送治疗剂的组合物、药物组合物、制备方法以及用途 |
| EP3624863B1 (de) | 2017-05-15 | 2021-04-14 | C.R. Bard, Inc. | Medizinische vorrichtung mit wirkstofffreisetzender beschichtung und zwischenschicht |
| JP7262581B2 (ja) | 2018-11-14 | 2023-04-21 | ルトニックス,インコーポレーテッド | 改質されたデバイス表面に薬物溶出コーティングを有する医療用デバイス |
| JP7487228B2 (ja) | 2019-04-08 | 2024-05-20 | バード・ペリフェラル・バスキュラー・インコーポレーテッド | 改質されたデバイス表面に薬物溶出コーティングを有する医療用デバイス |
Family Cites Families (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ZA737247B (en) | 1972-09-29 | 1975-04-30 | Ayerst Mckenna & Harrison | Rapamycin and process of preparation |
| US3993749A (en) | 1974-04-12 | 1976-11-23 | Ayerst Mckenna And Harrison Ltd. | Rapamycin and process of preparation |
| US5206018A (en) | 1978-11-03 | 1993-04-27 | Ayerst, Mckenna & Harrison, Inc. | Use of rapamycin in treatment of tumors |
| US4885171A (en) | 1978-11-03 | 1989-12-05 | American Home Products Corporation | Use of rapamycin in treatment of certain tumors |
| US4401653A (en) | 1981-03-09 | 1983-08-30 | Ayerst, Mckenna & Harrison Inc. | Combination of rapamycin and picibanil for the treatment of tumors |
| EP0378318A1 (de) * | 1989-01-11 | 1990-07-18 | Merck & Co. Inc. | Verfahren zur Herstellung von FK-506 sowie Tricarbonylzwischenprodukten |
| US5100899A (en) | 1989-06-06 | 1992-03-31 | Roy Calne | Methods of inhibiting transplant rejection in mammals using rapamycin and derivatives and prodrugs thereof |
| GB2247456A (en) * | 1990-09-03 | 1992-03-04 | Fujisawa Pharmaceutical Co | Tetrahydropyrane compounds, a process for their production and a pharmaceutical composition containing the same |
| US5078999A (en) | 1991-02-22 | 1992-01-07 | American Home Products Corporation | Method of treating systemic lupus erythematosus |
| US5080899A (en) | 1991-02-22 | 1992-01-14 | American Home Products Corporation | Method of treating pulmonary inflammation |
| US5321009A (en) | 1991-04-03 | 1994-06-14 | American Home Products Corporation | Method of treating diabetes |
| ES2084940T3 (es) | 1991-06-18 | 1996-05-16 | American Home Prod | Uso de la rapamicina para el tratamiento de la leucemia/linfoma de las celulas t adultas. |
| ZA924953B (en) | 1991-07-25 | 1993-04-28 | Univ Louisville Res Found | Method of treating ocular inflammation |
| US5286730A (en) | 1991-09-17 | 1994-02-15 | American Home Products Corporation | Method of treating immunoinflammatory disease |
| US5286731A (en) | 1991-09-17 | 1994-02-15 | American Home Products Corporation | Method of treating immunoinflammatory bowel disease |
| US5516781A (en) | 1992-01-09 | 1996-05-14 | American Home Products Corporation | Method of treating restenosis with rapamycin |
| US5288711A (en) | 1992-04-28 | 1994-02-22 | American Home Products Corporation | Method of treating hyperproliferative vascular disease |
| US5362718A (en) * | 1994-04-18 | 1994-11-08 | American Home Products Corporation | Rapamycin hydroxyesters |
| US5621108A (en) * | 1994-12-05 | 1997-04-15 | Trustees Of The University Of Pennsylvania | Processes and intermediates for preparing macrocycles |
| US5563145A (en) * | 1994-12-07 | 1996-10-08 | American Home Products Corporation | Rapamycin 42-oximes and hydroxylamines |
| US5561138A (en) | 1994-12-13 | 1996-10-01 | American Home Products Corporation | Method of treating anemia |
| US5496832A (en) | 1995-03-09 | 1996-03-05 | American Home Products Corporation | Method of treating cardiac inflammatory disease |
| EP0927182A2 (de) * | 1996-09-09 | 1999-07-07 | American Home Products Corporation | Alkylierte rapamycinderivate |
| US6002008A (en) | 1997-04-03 | 1999-12-14 | American Cyanamid Company | Substituted 3-cyano quinolines |
| US6277983B1 (en) | 2000-09-27 | 2001-08-21 | American Home Products Corporation | Regioselective synthesis of rapamycin derivatives |
| CA2455311A1 (en) | 2001-08-22 | 2003-03-06 | Wyeth | Rapamycin dialdehydes |
-
2002
- 2002-08-21 WO PCT/US2002/026622 patent/WO2003018573A1/en not_active Ceased
- 2002-08-21 ES ES02768642T patent/ES2246409T3/es not_active Expired - Lifetime
- 2002-08-21 CN CNB028163052A patent/CN1310908C/zh not_active Expired - Fee Related
- 2002-08-21 JP JP2003523235A patent/JP2005501868A/ja active Pending
- 2002-08-21 CA CA002455308A patent/CA2455308A1/en not_active Withdrawn
- 2002-08-21 MX MXPA04001524A patent/MXPA04001524A/es active IP Right Grant
- 2002-08-21 BR BR0211986-2A patent/BR0211986A/pt not_active IP Right Cessation
- 2002-08-21 AT AT02768642T patent/ATE305932T1/de not_active IP Right Cessation
- 2002-08-21 DK DK02768642T patent/DK1419154T3/da active
- 2002-08-21 DE DE60206512T patent/DE60206512T2/de not_active Expired - Fee Related
- 2002-08-21 EP EP02768642A patent/EP1419154B1/de not_active Expired - Lifetime
- 2002-08-22 US US10/224,971 patent/US6677357B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| WO2003018573A1 (en) | 2003-03-06 |
| CN1310908C (zh) | 2007-04-18 |
| US20030114477A1 (en) | 2003-06-19 |
| DK1419154T3 (da) | 2006-01-09 |
| EP1419154A1 (de) | 2004-05-19 |
| US6677357B2 (en) | 2004-01-13 |
| ES2246409T3 (es) | 2006-02-16 |
| CN1545511A (zh) | 2004-11-10 |
| CA2455308A1 (en) | 2003-03-06 |
| DE60206512D1 (de) | 2006-02-16 |
| MXPA04001524A (es) | 2004-05-31 |
| DE60206512T2 (de) | 2006-06-22 |
| BR0211986A (pt) | 2004-09-28 |
| JP2005501868A (ja) | 2005-01-20 |
| EP1419154B1 (de) | 2005-10-05 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |