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)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Veterinary Medicine (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (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)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (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 (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE427948T1 (de) | 2001-04-24 | 2009-04-15 | 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 |
| AR040693A1 (es) | 2002-07-30 | 2005-04-13 | Wyeth Corp | Formulaciones parenterales |
| WO2004069159A2 (en) | 2003-01-27 | 2004-08-19 | Endocyte, Inc. | Vitamin receptor binding drug delivery conjugates |
| 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 |
| CN101098854B (zh) * | 2004-07-23 | 2012-12-05 | 恩多塞特公司 | 二价连接体及其轭合物 |
| MX2007003789A (es) * | 2004-10-04 | 2007-07-20 | Qlt Usa Inc | Suministro ocular de formulaciones polimericas para suministro. |
| US8313763B2 (en) | 2004-10-04 | 2012-11-20 | Tolmar Therapeutics, Inc. | Sustained delivery formulations of rapamycin compounds |
| 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 |
| RU2007119585A (ru) | 2004-12-20 | 2009-01-27 | Вайет (Us) | Производные рапамицина и их применение при лечении неврологических заболеваний |
| NZ574663A (en) | 2004-12-20 | 2010-05-28 | Wyeth Corp | Rapamycin analogues and the uses thereof in the treatment of neurological, proliferative, and inflammatory disorders |
| CA2595766A1 (en) | 2005-02-09 | 2006-08-17 | Wyeth | Cci-779 polymorph and use thereof |
| EP1859274A2 (de) * | 2005-03-07 | 2007-11-28 | Novartis AG | An neurodegenerativen leiden beteiligte gene |
| CA2602010A1 (en) * | 2005-03-07 | 2006-09-14 | Wyeth | Oxepane isomer of 42-o-(2-hydroxy)ethyl-rapamycin |
| 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 |
| US7189582B2 (en) * | 2005-04-27 | 2007-03-13 | Dade Behring Inc. | Compositions and methods for detection of sirolimus |
| CA2606226A1 (en) * | 2005-04-27 | 2006-11-02 | University Of Florida Research Foundation, Inc. | Materials and methods for enhanced degradation of mutant proteins associated with human disease |
| BRPI0615354A2 (pt) * | 2005-08-19 | 2011-05-17 | Endocyte, Inc. | conjugado de liberação de fármaco de ligação de receptor, composição farmacêutica que o compreende, bem como seu uso |
| EP2382995A3 (de) * | 2005-08-19 | 2013-09-25 | Endocyte, Inc. | Ligandenkonjugate von Vincaalkaloiden, Analoga und Derivaten |
| US20070142422A1 (en) * | 2005-12-20 | 2007-06-21 | Wyeth | Control of CCI-779 dosage form stability through control of drug substance impurities |
| 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 |
| US8414525B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8414910B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| US8430055B2 (en) | 2008-08-29 | 2013-04-30 | Lutonix, Inc. | Methods and apparatuses for coating balloon catheters |
| US8425459B2 (en) | 2006-11-20 | 2013-04-23 | Lutonix, Inc. | Medical device rapid drug releasing coatings comprising a therapeutic agent and a contrast agent |
| US8998846B2 (en) | 2006-11-20 | 2015-04-07 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US8414909B2 (en) | 2006-11-20 | 2013-04-09 | Lutonix, Inc. | Drug releasing coatings for medical devices |
| 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 |
| US9700704B2 (en) | 2006-11-20 | 2017-07-11 | Lutonix, Inc. | Drug releasing coatings for balloon catheters |
| US20100104626A1 (en) * | 2007-02-16 | 2010-04-29 | Endocyte, Inc. | Methods and compositions for treating and diagnosing kidney disease |
| AU2008224988A1 (en) * | 2007-03-14 | 2008-09-18 | Endocyte, Inc. | Binding ligand linked drug delivery conjugates of tubulysins |
| 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 |
| 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 |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| CN101909441B (zh) | 2007-10-25 | 2015-05-13 | 恩多塞特公司 | 微管蛋白抑制剂及其制备方法 |
| ES2645692T3 (es) | 2008-11-11 | 2017-12-07 | The Board Of Regents,The University Of Texas System | Microcápsulas de rapamicina y su uso para el tratamiento del cáncer |
| WO2015161139A1 (en) | 2014-04-16 | 2015-10-22 | Rapamycin Holdings, Llc | Oral rapamycin preparation and use for stomatitis |
| 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 |
| US10080805B2 (en) | 2012-02-24 | 2018-09-25 | 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 |
| WO2014059295A1 (en) | 2012-10-12 | 2014-04-17 | The Board Of Regents Of The University Of Texas System | Use of mtor inhibitors to treat vascular cognitive impairment |
| BR112015008365A2 (pt) | 2012-10-16 | 2017-07-04 | Endocyte Inc | composto da fórmula b-l(d)x, ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, uso de um composto, composição de forma de dosagem unitária ou dose unitária, composição para tratar um câncer em um paciente, e método para tratar um câncer em um paciente |
| WO2014160328A1 (en) | 2013-03-13 | 2014-10-02 | The Board Of Regents Of The University Of Texas System | Mtor inhibitors for prevention of intestinal polyp growth |
| US9700544B2 (en) | 2013-12-31 | 2017-07-11 | Neal K Vail | Oral rapamycin nanoparticle preparations |
| EP3089737B1 (de) | 2013-12-31 | 2021-11-03 | Rapamycin Holdings, LLC | Orale rapamycinnanopartikelzubereitungen und verwendung |
| WO2017181115A1 (en) | 2016-04-14 | 2017-10-19 | Spinnaker Biosciences, Inc. | Porous silicon materials comprising a metal silicate for delivery of therapeutic agents |
| US20210154372A1 (en) | 2017-05-15 | 2021-05-27 | C.R. Bard, Inc. | Medical device with drug-eluting coating and intermediate layer |
| EP3880266B1 (de) | 2018-11-14 | 2025-05-07 | Lutonix, Inc. | Medizinische vorrichtung mit wirkstofffreisetzender beschichtung auf modifizierter vorrichtungsoberfläche |
| EP3952937A1 (de) | 2019-04-08 | 2022-02-16 | Bard Peripheral Vascular, Inc. | Medizinische vorrichtung mit wirkstofffreisetzender beschichtung auf modifizierter vorrichtungsoberfläche |
| GB202415232D0 (en) | 2024-10-16 | 2024-11-27 | Nacamed As | Composition |
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 |
| DK0525960T3 (da) | 1991-06-18 | 1996-04-15 | American Home Prod | Anvendelse af rapamycin til behandling af T-celle leukæmi/lymfon |
| 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 |
| EP1419153A1 (de) | 2001-08-22 | 2004-05-19 | Wyeth | Rapamycindialdehyde |
-
2002
- 2002-08-21 DK DK02768642T patent/DK1419154T3/da active
- 2002-08-21 MX MXPA04001524A patent/MXPA04001524A/es active IP Right Grant
- 2002-08-21 CA CA002455308A patent/CA2455308A1/en not_active Withdrawn
- 2002-08-21 WO PCT/US2002/026622 patent/WO2003018573A1/en not_active Ceased
- 2002-08-21 BR BR0211986-2A patent/BR0211986A/pt not_active IP Right Cessation
- 2002-08-21 EP EP02768642A patent/EP1419154B1/de not_active Expired - Lifetime
- 2002-08-21 AT AT02768642T patent/ATE305932T1/de not_active IP Right Cessation
- 2002-08-21 JP JP2003523235A patent/JP2005501868A/ja active Pending
- 2002-08-21 ES ES02768642T patent/ES2246409T3/es not_active Expired - Lifetime
- 2002-08-21 DE DE60206512T patent/DE60206512T2/de not_active Expired - Fee Related
- 2002-08-21 CN CNB028163052A patent/CN1310908C/zh not_active Expired - Fee Related
- 2002-08-22 US US10/224,971 patent/US6677357B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| EP1419154B1 (de) | 2005-10-05 |
| DK1419154T3 (da) | 2006-01-09 |
| DE60206512D1 (de) | 2006-02-16 |
| CN1310908C (zh) | 2007-04-18 |
| BR0211986A (pt) | 2004-09-28 |
| ES2246409T3 (es) | 2006-02-16 |
| JP2005501868A (ja) | 2005-01-20 |
| EP1419154A1 (de) | 2004-05-19 |
| DE60206512T2 (de) | 2006-06-22 |
| WO2003018573A1 (en) | 2003-03-06 |
| US6677357B2 (en) | 2004-01-13 |
| US20030114477A1 (en) | 2003-06-19 |
| CA2455308A1 (en) | 2003-03-06 |
| CN1545511A (zh) | 2004-11-10 |
| MXPA04001524A (es) | 2004-05-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| RER | Ceased as to paragraph 5 lit. 3 law introducing patent treaties |