BRPI0607482A2 - derivados de aminoácidos fosfìnicos, o respectivo processo de preparo e as composições farmacêuticas que os contêm - Google Patents
derivados de aminoácidos fosfìnicos, o respectivo processo de preparo e as composições farmacêuticas que os contêmInfo
- Publication number
- BRPI0607482A2 BRPI0607482A2 BRPI0607482-0A BRPI0607482A BRPI0607482A2 BR PI0607482 A2 BRPI0607482 A2 BR PI0607482A2 BR PI0607482 A BRPI0607482 A BR PI0607482A BR PI0607482 A2 BRPI0607482 A2 BR PI0607482A2
- Authority
- BR
- Brazil
- Prior art keywords
- amino acid
- acid derivatives
- pharmaceutical compositions
- preparation process
- compositions containing
- Prior art date
Links
- 150000003862 amino acid derivatives Chemical class 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 3
- 238000002360 preparation method Methods 0.000 title abstract 3
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 abstract 2
- 102000048186 Endothelin-converting enzyme 1 Human genes 0.000 abstract 2
- 108030001679 Endothelin-converting enzyme 1 Proteins 0.000 abstract 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 abstract 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 abstract 2
- 125000005197 alkyl carbonyloxy alkyl group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 239000001257 hydrogen Substances 0.000 abstract 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- 150000004677 hydrates Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000001041 indolyl group Chemical group 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/653—Five-membered rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- 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
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic 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
-
- 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
- A61P9/10—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
-
- 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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/30—Phosphinic acids [R2P(=O)(OH)]; Thiophosphinic acids ; [R2P(=X1)(X2H) (X1, X2 are each independently O, S or Se)]
- C07F9/32—Esters thereof
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6596—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having atoms other than oxygen, sulfur, selenium, tellurium, nitrogen or phosphorus as ring hetero atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Cardiology (AREA)
- Biochemistry (AREA)
- Heart & Thoracic Surgery (AREA)
- Molecular Biology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Ophthalmology & Optometry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Hospice & Palliative Care (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
DERIVADOS DE AMINOáCIDOS FOSFìNICOS, O RESPECTIVO PROCESSO DE PREPARO E AS COMPOSIçõES FARMACêUTICAS QUE OS CONTêM. A presente invenção refere-se aos derivados de aminoácidos fosfínicos de fórmula (1), ao respectivo processo de preparo e às composições farmacêuticas que os contêm, na qual R~ 1~ representa hidrogênio, alquilacarboniloxialquila, alquilacarboniltioalquila, R~ 2~ representa hidrogênio, alquilacarboniloxialquila, arilcarboniltioalquila, arilalquila, eventualmente substituído, R~ 3~ representa fenila eventualmente substituído, indolila, seus isómeros, assim como seus sais de adição a um ácido ou a uma base farmaceuticamente aceitável, ou R~ 1~ pode também representar um grupamento alquila (C~ 1~-C~ 6~), linear ou ramificado, R~ 2~ representa um grupamento alquila (C~ 1~-C~ 6~), linear ou ramificado, quando R~ 3~ representa uma fenila substituida por um grupamento hidróxi, seus enantiómeros, diastereoisómeros, assim como seus sais de adição a uma base farmaceuticamente aceitável, assim como seus hidratos e seus solvatos. Os derivados de aminoácidos fosfínicos, de acordo com a invenção, apresentam a notável propriedade de inibir ao mesmo tempo a enzima de conversão da angiotensina I (ECA) e a enzima de conversão da endotelina (ECE).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR0502043A FR2882752B1 (fr) | 2005-03-01 | 2005-03-01 | Nouveaux derives d'aminoacides phosphiniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
| PCT/FR2006/000446 WO2006092495A1 (fr) | 2005-03-01 | 2006-02-28 | Nouveaux derives d'aminoacides phosphiniques, leur procede de preparation et les compositions pharmaceutiques qui les contiennent |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0607482A2 true BRPI0607482A2 (pt) | 2009-09-08 |
Family
ID=35033564
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0607482-0A BRPI0607482A2 (pt) | 2005-03-01 | 2006-02-28 | derivados de aminoácidos fosfìnicos, o respectivo processo de preparo e as composições farmacêuticas que os contêm |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US7521469B2 (pt) |
| EP (1) | EP1853615A1 (pt) |
| JP (1) | JP4659843B2 (pt) |
| KR (1) | KR20080011275A (pt) |
| CN (1) | CN101133070A (pt) |
| AR (1) | AR055565A1 (pt) |
| AU (1) | AU2006219790B2 (pt) |
| BR (1) | BRPI0607482A2 (pt) |
| CA (1) | CA2601025C (pt) |
| EA (1) | EA012447B1 (pt) |
| FR (1) | FR2882752B1 (pt) |
| GE (1) | GEP20105026B (pt) |
| MA (1) | MA29315B1 (pt) |
| MX (1) | MX2007010665A (pt) |
| MY (1) | MY143558A (pt) |
| NO (1) | NO20074942L (pt) |
| NZ (1) | NZ560750A (pt) |
| UA (1) | UA91214C2 (pt) |
| WO (1) | WO2006092495A1 (pt) |
| ZA (1) | ZA200707471B (pt) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2934267B1 (fr) * | 2008-07-23 | 2010-08-13 | Pharmaleads | Derives aminophosphiniques utiles dans le traitement de la douleur |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5476847A (en) * | 1994-06-29 | 1995-12-19 | Schering Corporation | Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors |
| IT1276710B1 (it) * | 1995-06-14 | 1997-11-03 | Zambon Spa | Derivati dell'acido fosfinico ad attivita' inibitrice delle metallopeptidasi |
| FR2755135B1 (fr) | 1996-10-25 | 2002-12-27 | Inst Nat Sante Rech Med | Nouveaux derives d'(alpha-aminophosphino)peptides, leur procede de preparation et les compositions qui les contiennent |
-
2005
- 2005-03-01 FR FR0502043A patent/FR2882752B1/fr not_active Expired - Fee Related
-
2006
- 2006-02-27 MY MYPI20060824A patent/MY143558A/en unknown
- 2006-02-28 KR KR1020077022456A patent/KR20080011275A/ko not_active Application Discontinuation
- 2006-02-28 WO PCT/FR2006/000446 patent/WO2006092495A1/fr active Application Filing
- 2006-02-28 AU AU2006219790A patent/AU2006219790B2/en not_active Expired - Fee Related
- 2006-02-28 NZ NZ560750A patent/NZ560750A/en unknown
- 2006-02-28 ZA ZA200707471A patent/ZA200707471B/xx unknown
- 2006-02-28 JP JP2007557535A patent/JP4659843B2/ja not_active Expired - Fee Related
- 2006-02-28 CN CNA2006800068686A patent/CN101133070A/zh active Pending
- 2006-02-28 EA EA200701819A patent/EA012447B1/ru not_active IP Right Cessation
- 2006-02-28 BR BRPI0607482-0A patent/BRPI0607482A2/pt not_active IP Right Cessation
- 2006-02-28 EP EP06725994A patent/EP1853615A1/fr not_active Withdrawn
- 2006-02-28 GE GEAP200610296A patent/GEP20105026B/en unknown
- 2006-02-28 UA UAA200710758A patent/UA91214C2/ru unknown
- 2006-02-28 MX MX2007010665A patent/MX2007010665A/es active IP Right Grant
- 2006-02-28 US US11/885,301 patent/US7521469B2/en not_active Expired - Fee Related
- 2006-02-28 CA CA2601025A patent/CA2601025C/fr not_active Expired - Fee Related
- 2006-03-01 AR ARP060100755A patent/AR055565A1/es not_active Application Discontinuation
-
2007
- 2007-09-06 MA MA30192A patent/MA29315B1/fr unknown
- 2007-10-01 NO NO20074942A patent/NO20074942L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20080153890A1 (en) | 2008-06-26 |
| NO20074942L (no) | 2007-10-01 |
| EA200701819A1 (ru) | 2008-02-28 |
| MA29315B1 (fr) | 2008-03-03 |
| CN101133070A (zh) | 2008-02-27 |
| JP4659843B2 (ja) | 2011-03-30 |
| AR055565A1 (es) | 2007-08-22 |
| CA2601025A1 (fr) | 2006-09-08 |
| US7521469B2 (en) | 2009-04-21 |
| ZA200707471B (en) | 2008-12-31 |
| FR2882752B1 (fr) | 2007-05-04 |
| AU2006219790B2 (en) | 2011-03-17 |
| FR2882752A1 (fr) | 2006-09-08 |
| GEP20105026B (en) | 2010-06-25 |
| EP1853615A1 (fr) | 2007-11-14 |
| AU2006219790A1 (en) | 2006-09-08 |
| MY143558A (en) | 2011-05-31 |
| MX2007010665A (es) | 2007-12-12 |
| KR20080011275A (ko) | 2008-02-01 |
| UA91214C2 (ru) | 2010-07-12 |
| JP2008531661A (ja) | 2008-08-14 |
| CA2601025C (fr) | 2011-01-25 |
| EA012447B1 (ru) | 2009-10-30 |
| WO2006092495A1 (fr) | 2006-09-08 |
| NZ560750A (en) | 2010-12-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 6A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012. |