BRPI0414457A - formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóico - Google Patents
formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóicoInfo
- Publication number
- BRPI0414457A BRPI0414457A BRPI0414457-0A BRPI0414457A BRPI0414457A BR PI0414457 A BRPI0414457 A BR PI0414457A BR PI0414457 A BRPI0414457 A BR PI0414457A BR PI0414457 A BRPI0414457 A BR PI0414457A
- Authority
- BR
- Brazil
- Prior art keywords
- phenylamino
- fluorophenyl
- phenyl
- heptanoic
- pyrrol
- Prior art date
Links
- 239000002253 acid Substances 0.000 title abstract 3
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 title 1
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 title 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 title 1
- -1 4-FLUOROPHENYL Chemical class 0.000 abstract 2
- XUKUURHRXDUEBC-KAYWLYCHSA-N Atorvastatin Chemical compound C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CC[C@@H](O)C[C@@H](O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-KAYWLYCHSA-N 0.000 abstract 2
- HCPLPXQDAYFYCK-UHFFFAOYSA-N 7-[2-(phenylcarbamoyl)pyrrol-1-yl]heptanoic acid Chemical compound OC(=O)CCCCCCN1C=CC=C1C(=O)NC1=CC=CC=C1 HCPLPXQDAYFYCK-UHFFFAOYSA-N 0.000 abstract 1
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- XUKUURHRXDUEBC-UHFFFAOYSA-N Atorvastatin Natural products C=1C=CC=CC=1C1=C(C=2C=CC(F)=CC=2)N(CCC(O)CC(O)CC(O)=O)C(C(C)C)=C1C(=O)NC1=CC=CC=C1 XUKUURHRXDUEBC-UHFFFAOYSA-N 0.000 abstract 1
- 206010004446 Benign prostatic hyperplasia Diseases 0.000 abstract 1
- 208000035150 Hypercholesterolemia Diseases 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 238000005481 NMR spectroscopy Methods 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 208000004403 Prostatic Hyperplasia Diseases 0.000 abstract 1
- HSMPSHPWCOOUJH-UHFFFAOYSA-N anilinyl Chemical class [NH]C1=CC=CC=C1 HSMPSHPWCOOUJH-UHFFFAOYSA-N 0.000 abstract 1
- 229960005370 atorvastatin Drugs 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000000634 powder X-ray diffraction Methods 0.000 abstract 1
- 239000007787 solid Substances 0.000 abstract 1
- 238000001228 spectrum Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 to ring carbon atoms
-
- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
Abstract
"FORMAS CRISTALINAS DO áCIDO ¢R-(R*,R*)!-2-(4-FLUOROFENIL)-BETA,DELTA-DIHIDRóXI-5-(1-M ETILETIL)-3-FENIL-4¢(FENILAMINO)-CARBONIL!-1H-PIRROL-1 -HEPTANóICO". A presente invenção refere-se a novas formas cristalinas do ácido ¢R-(R*,R*)!-2-(4-fluorofenil)-<225>,<SYM>-dihidróxi-5-(1-metiletil)-3-fe nil-4-¢(fenilamino)-carbonil!-1H-pirrol-l-heptanóico (ácido livre de atorvastatina) designado Forma A e Forma B, caracterizadas pelos seus padrões de difração de raios X de pó e os seus espectros de RMN no estado sólido são descritos, bem como os métodos de preparação de composição farmacêutica do mesmo, que são úteis como agentes para tratar hiperlipidemia, hipercolesterolemia, osteoporose, hiperplasia prostática benigna, e Doença de Alzheimer, e para preparar sais de atorvastatina.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50359203P | 2003-09-17 | 2003-09-17 | |
| PCT/IB2004/002919 WO2005026116A1 (en) | 2003-09-17 | 2004-09-06 | Crystalline forms of `r-(r*,r*)]-2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-`(phenylamino)carbonyl!-1h-pyrrole-1-heptanoic acid |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0414457A true BRPI0414457A (pt) | 2006-11-14 |
Family
ID=34312443
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0414457-0A BRPI0414457A (pt) | 2003-09-17 | 2004-09-06 | formas cristalinas do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)-c arbonil]-1h-pirrol-1-heptanóico |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20070276027A1 (pt) |
| EP (1) | EP1663969A1 (pt) |
| JP (1) | JP2007505885A (pt) |
| KR (1) | KR100781420B1 (pt) |
| CN (2) | CN101318923A (pt) |
| AR (1) | AR045654A1 (pt) |
| AU (1) | AU2004272365A1 (pt) |
| BR (1) | BRPI0414457A (pt) |
| CA (1) | CA2539158A1 (pt) |
| IL (1) | IL173651A0 (pt) |
| MX (1) | MXPA06003003A (pt) |
| NO (1) | NO20060716L (pt) |
| RU (1) | RU2315755C2 (pt) |
| TW (1) | TW200524862A (pt) |
| WO (1) | WO2005026116A1 (pt) |
| ZA (1) | ZA200602222B (pt) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8080672B2 (en) | 2005-12-13 | 2011-12-20 | Teva Pharmaceutical Industries Ltd. | Crystal form of atorvastatin hemi-calcium and processes for preparation thereof |
| MX2009011009A (es) * | 2007-04-13 | 2009-10-30 | Nicox Sa | Formas cristalinas de atorvastatin 4-(nitrooxi)butil ester. |
| WO2010080971A1 (en) * | 2009-01-12 | 2010-07-15 | Merck Sharp & Dohme Corp. | Crystalline polymorphic forms of an antidiabetic compound |
| CA3065589C (en) | 2010-06-03 | 2022-04-26 | Catalent Ontario Limited | Multi phase soft gel capsules, apparatus and method thereof |
| CA2706270C (en) * | 2010-06-03 | 2020-01-07 | Accucaps Industries Limited | Pharmaceutical formulations of statins and omega-3 fatty acids for encapsulation |
| KR20120011249A (ko) | 2010-07-28 | 2012-02-07 | 주식회사 경보제약 | 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법 |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4681873A (en) * | 1985-07-29 | 1987-07-21 | Warner-Lambert Company | 4-amino-3-halo-2-pyridinone nucleoside and nucleotide compounds |
| US4681893A (en) * | 1986-05-30 | 1987-07-21 | Warner-Lambert Company | Trans-6-[2-(3- or 4-carboxamido-substituted pyrrol-1-yl)alkyl]-4-hydroxypyran-2-one inhibitors of cholesterol synthesis |
| US5003080A (en) * | 1988-02-22 | 1991-03-26 | Warner-Lambert Company | Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis |
| US5097045A (en) * | 1989-02-01 | 1992-03-17 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5216174A (en) * | 1988-02-22 | 1993-06-01 | Warner-Lambert Co. | Process for trans-6-[12-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5149837A (en) * | 1988-02-22 | 1992-09-22 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| US5124482A (en) * | 1988-02-22 | 1992-06-23 | Warner-Lambert Company | Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis |
| US5245047A (en) * | 1988-02-22 | 1993-09-14 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| FI94339C (fi) * | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
| US5248793A (en) * | 1990-10-17 | 1993-09-28 | Warner-Lambert Company | Process for the synthesis of (4R-cis)-1,1-dimethylethyl 6-iodomethyl or 6-(phenyl-substituted)sulfonyloxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate |
| US5103024A (en) * | 1990-10-17 | 1992-04-07 | Warner-Lambert Company | Process for the synthesis of (4r-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate |
| US5155251A (en) * | 1991-10-11 | 1992-10-13 | Warner-Lambert Company | Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate |
| US5213995A (en) * | 1992-04-16 | 1993-05-25 | At&T Bell Laboratories | Method of making an article comprising a periodic heteroepitaxial semiconductor structure |
| JP3254219B2 (ja) * | 1993-01-19 | 2002-02-04 | ワーナー−ランバート・コンパニー | 安定な経口用のci−981製剤およびその製法 |
| US5298627A (en) * | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
| HRP960313B1 (en) * | 1995-07-17 | 2002-08-31 | Warner Lambert Co | Form iii crystalline (r- (r*, r*)-2- (4-fluorophenyl) -beta-delta-hydroxy-5-(1-methylethyl) -3-phenyl-4- ((phenylamino) carbonyl -1h-pyrrole-1-heptanoic acid calcium salt (2:1) |
| GEP20002029B (en) * | 1995-07-17 | 2000-04-10 | Warner Lambert Company Us | (54) Crystalline [R-(R*,R*,]–2-(4-Fluorophenyl)-Beta,Delta-Dihydroxy-5-(1-Methyl-Ethyl)-3-Phenyl–4-{Phenylamino) Carbonyl} - 1H - Pyrrole - 1 - Heptanoic Acid Hemi Calcium Salt (Atorvastatin) |
| US6087511A (en) * | 1996-07-16 | 2000-07-11 | Warner-Lambert Company | Process for the production of amorphous [R-(R*,R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl )-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid) calcium salt (2:1) |
| TR199900191T2 (xx) * | 1996-07-29 | 1999-04-21 | Warner-Lambert Company | (S)-3,4-Dihidroksibutirik asitin korumal� esterlerinin sentezi i�in geli�tirilmi� proses. |
| EP1054860B1 (en) * | 1997-12-19 | 2007-04-25 | Pfizer Ireland Pharmaceuticals | Process for the synthesis of 1,3-diols |
| SI20070A (sl) | 1998-09-18 | 2000-04-30 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Nove soli inhibitorjev HMG-CoA reduktaze |
| PL362981A1 (en) * | 2000-11-16 | 2004-11-02 | Teva Pharmaceutical Industries Ltd. | Hydrolysis of [r(r*,r*)]-2-(4-fluorophenyl)-beta,delta -dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrrole-1-heptanoic acid esters with calcium hydroxide |
| US6476235B2 (en) * | 2001-01-09 | 2002-11-05 | Warner-Lambert Company | Process for the synthesis of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide |
-
2004
- 2004-09-06 CN CNA2008101341489A patent/CN101318923A/zh active Pending
- 2004-09-06 KR KR1020067005316A patent/KR100781420B1/ko not_active Expired - Fee Related
- 2004-09-06 CN CNA2004800269756A patent/CN1852894A/zh active Pending
- 2004-09-06 JP JP2006526717A patent/JP2007505885A/ja active Pending
- 2004-09-06 RU RU2006108385/04A patent/RU2315755C2/ru not_active IP Right Cessation
- 2004-09-06 BR BRPI0414457-0A patent/BRPI0414457A/pt not_active IP Right Cessation
- 2004-09-06 US US10/572,324 patent/US20070276027A1/en not_active Abandoned
- 2004-09-06 WO PCT/IB2004/002919 patent/WO2005026116A1/en not_active Ceased
- 2004-09-06 EP EP04769318A patent/EP1663969A1/en not_active Withdrawn
- 2004-09-06 MX MXPA06003003A patent/MXPA06003003A/es unknown
- 2004-09-06 AU AU2004272365A patent/AU2004272365A1/en not_active Abandoned
- 2004-09-06 CA CA002539158A patent/CA2539158A1/en not_active Abandoned
- 2004-09-15 TW TW093127885A patent/TW200524862A/zh unknown
- 2004-09-15 AR ARP040103296A patent/AR045654A1/es unknown
-
2006
- 2006-02-09 IL IL173651A patent/IL173651A0/en unknown
- 2006-02-14 NO NO20060716A patent/NO20060716L/no not_active Application Discontinuation
- 2006-03-16 ZA ZA200602222A patent/ZA200602222B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200602222B (en) | 2007-07-25 |
| IL173651A0 (en) | 2006-07-05 |
| US20070276027A1 (en) | 2007-11-29 |
| CA2539158A1 (en) | 2005-03-24 |
| CN1852894A (zh) | 2006-10-25 |
| NO20060716L (no) | 2006-06-16 |
| TW200524862A (en) | 2005-08-01 |
| EP1663969A1 (en) | 2006-06-07 |
| JP2007505885A (ja) | 2007-03-15 |
| KR100781420B1 (ko) | 2007-12-03 |
| WO2005026116A1 (en) | 2005-03-24 |
| AR045654A1 (es) | 2005-11-02 |
| MXPA06003003A (es) | 2006-06-23 |
| RU2315755C2 (ru) | 2008-01-27 |
| RU2006108385A (ru) | 2006-08-10 |
| AU2004272365A1 (en) | 2005-03-24 |
| KR20060037467A (ko) | 2006-05-03 |
| CN101318923A (zh) | 2008-12-10 |
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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 AS 6A E 7A ANUIDADES. |
|
| 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 2159 DE 22/05/2012. |