ES2241507T1 - Nuevas formas de cristal de atorvastatina semicalcica y procedimientos para su preparacion, asi como nuevos procedimientos para la preparacion de las formas i, viii y ix de atorvastatina semicalcica. - Google Patents
Nuevas formas de cristal de atorvastatina semicalcica y procedimientos para su preparacion, asi como nuevos procedimientos para la preparacion de las formas i, viii y ix de atorvastatina semicalcica.Info
- Publication number
- ES2241507T1 ES2241507T1 ES03713610T ES03713610T ES2241507T1 ES 2241507 T1 ES2241507 T1 ES 2241507T1 ES 03713610 T ES03713610 T ES 03713610T ES 03713610 T ES03713610 T ES 03713610T ES 2241507 T1 ES2241507 T1 ES 2241507T1
- Authority
- ES
- Spain
- Prior art keywords
- atorvastatin
- semi
- calcic
- approximately
- characteristic
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 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 title claims abstract 40
- 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 title claims abstract 40
- 229960005370 atorvastatin Drugs 0.000 title claims abstract 40
- 238000000034 method Methods 0.000 title claims 33
- 238000002360 preparation method Methods 0.000 title claims 10
- 239000007787 solid Substances 0.000 claims abstract 33
- 239000012453 solvate Substances 0.000 claims abstract 19
- 238000000634 powder X-ray diffraction Methods 0.000 claims abstract 11
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims 24
- 239000000203 mixture Substances 0.000 claims 17
- 239000000725 suspension Substances 0.000 claims 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 10
- 239000013078 crystal Substances 0.000 claims 4
- 230000005855 radiation Effects 0.000 claims 4
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 3
- 239000011575 calcium Substances 0.000 claims 3
- 229910052791 calcium Inorganic materials 0.000 claims 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 238000006243 chemical reaction Methods 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 238000010992 reflux Methods 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 102000004895 Lipoproteins Human genes 0.000 claims 1
- 108090001030 Lipoproteins Proteins 0.000 claims 1
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims 1
- 235000010627 Phaseolus vulgaris Nutrition 0.000 claims 1
- 244000046052 Phaseolus vulgaris Species 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 239000002552 dosage form Substances 0.000 claims 1
- 238000001035 drying Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 238000011002 quantification Methods 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 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
- C07D207/32—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- C07D207/325—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom
- C07D207/327—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US35718102P | 2002-02-15 | 2002-02-15 | |
| US357181P | 2002-02-15 | ||
| US42532502P | 2002-11-12 | 2002-11-12 | |
| US425325P | 2002-11-12 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ES2241507T1 true ES2241507T1 (es) | 2005-11-01 |
Family
ID=27760457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES03713610T Pending ES2241507T1 (es) | 2002-02-15 | 2003-02-19 | Nuevas formas de cristal de atorvastatina semicalcica y procedimientos para su preparacion, asi como nuevos procedimientos para la preparacion de las formas i, viii y ix de atorvastatina semicalcica. |
Country Status (14)
| Country | Link |
|---|---|
| EP (1) | EP1480950A4 (pl) |
| JP (2) | JP2005519076A (pl) |
| KR (1) | KR100724515B1 (pl) |
| CN (1) | CN100406436C (pl) |
| AU (1) | AU2003217653A1 (pl) |
| CA (1) | CA2475864A1 (pl) |
| DE (1) | DE03713610T1 (pl) |
| ES (1) | ES2241507T1 (pl) |
| HR (1) | HRP20040768A2 (pl) |
| IS (1) | IS7402A (pl) |
| MX (1) | MXPA04007939A (pl) |
| NO (1) | NO20043842L (pl) |
| PL (1) | PL372303A1 (pl) |
| WO (1) | WO2003070702A1 (pl) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7411075B1 (en) | 2000-11-16 | 2008-08-12 | Teva Pharmaceutical Industries Ltd. | Polymorphic form of atorvastatin calcium |
| IL156055A0 (en) | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
| US7501450B2 (en) | 2000-11-30 | 2009-03-10 | Teva Pharaceutical Industries Ltd. | Crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms |
| HRP20040767A2 (en) | 2002-02-19 | 2004-12-31 | Teva Pharma | Desolvating solvates of atorvastatin hemi-calcium |
| WO2004050618A2 (en) * | 2002-11-28 | 2004-06-17 | Teva Pharmaceutical Industries Ltd. | Crystalline form f of atorvastatin hemi-calcium salt |
| US7655692B2 (en) | 2003-06-12 | 2010-02-02 | Pfizer Inc. | Process for forming amorphous atorvastatin |
| US20050271717A1 (en) | 2003-06-12 | 2005-12-08 | Alfred Berchielli | Pharmaceutical compositions of atorvastatin |
| JP2008506764A (ja) | 2004-07-20 | 2008-03-06 | ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー | [R−(R*,R*)]−2−(4−フルオロフェニル)−β、δ−ジヒドロキシ−5−(1−メチルエチル)−3−フェニル−4−[(フェニルアミノ)カルボニル]−1H−ピロール−1−ヘプタン酸カルシウム塩(2:1)の新規形態 |
| WO2006012499A2 (en) * | 2004-07-22 | 2006-02-02 | Teva Pharmaceutical Industries Ltd. | Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation |
| WO2006048894A1 (en) * | 2004-11-05 | 2006-05-11 | Morepen Laboratories Limited | Novel crystalline forms of atorvastatin calcium and processes for preparing them. |
| SK288276B6 (sk) * | 2005-04-08 | 2015-06-02 | Egis Gyógyszergyár, Nyilvánosan Működő Részvénytársaság | Spôsob prípravy kryštalickej polymorfnej formy hemivápenatej soli atorvastatínu |
| ATE466840T1 (de) | 2005-11-21 | 2010-05-15 | Warner Lambert Co | Neue formen von är-(r*,r*)ü-2-(4-fluorphenyl)-b,d-dihydroxy-5-( -methylethyl)-3-phenyl-4- ä(phenylamino)carbonylü-1h-pyrrol-1-heptansäure magnesium |
| US8080672B2 (en) | 2005-12-13 | 2011-12-20 | Teva Pharmaceutical Industries Ltd. | Crystal form of atorvastatin hemi-calcium and processes for preparation thereof |
| US20070265456A1 (en) * | 2006-05-09 | 2007-11-15 | Judith Aronhime | Novel crystal forms of atorvastatin hemi-calcium and processes for their preparation as well as novel processes for preparing other forms |
| JP2010520273A (ja) * | 2007-03-02 | 2010-06-10 | ドン・ア・ファーム・カンパニー・リミテッド | ピロリルヘプタン酸誘導体の新規な結晶形態 |
| KR20120011249A (ko) * | 2010-07-28 | 2012-02-07 | 주식회사 경보제약 | 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법 |
| KR101324862B1 (ko) * | 2011-07-12 | 2013-11-01 | (주)에이에스텍 | 클로피도그렐 황산수소염의 구형 입자, 이를 포함하는 약학적 조성물 및 이의 제조방법 |
| MY180626A (en) | 2013-11-15 | 2020-12-03 | Akebia Therapeutics Inc | Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof |
| CN105055357A (zh) * | 2015-09-25 | 2015-11-18 | 青岛华之草医药科技有限公司 | 一种治疗高胆固醇血症的药物阿托伐他汀钙组合物片剂 |
| KR101723783B1 (ko) * | 2017-02-24 | 2017-04-07 | 주식회사 경보제약 | 아토바스타틴 헤미칼슘염의 신규한 결정형, 이의 수화물, 및 그의 제조방법 |
| WO2025147589A1 (en) | 2024-01-05 | 2025-07-10 | Osanni Bio, Inc. | Implants, compositions, and methods for treating retinal diseases and disorders |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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) |
| 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) |
| 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) |
| ES2234699T3 (es) * | 1999-11-17 | 2005-07-01 | Teva Pharmaceutical Industries Ltd. | Forma polimorfica de atorvastatina calcio. |
| ES2258030T3 (es) * | 1999-12-17 | 2006-08-16 | Pfizer Science And Technology Ireland Limited | Procedimiento para producir atorvastatina calcio cristalina. |
| EP1584616A1 (en) * | 1999-12-17 | 2005-10-12 | Pfizer Science and Technology Ireland Limited | Industrial process for the production of crystalline atorvastatin trihydrate hemi calcium salt |
| KR100704213B1 (ko) * | 2000-11-03 | 2007-04-10 | 테바 파마슈티컬 인더스트리즈 리미티드 | 아토르바스타틴 헤미-칼슘 vii형 |
| IL156055A0 (en) * | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
| CA2622477A1 (en) * | 2000-12-27 | 2002-07-04 | Teva Pharmaceutical Industries Ltd. | Crystalline forms of atorvastatin |
| WO2002057229A1 (en) * | 2001-01-19 | 2002-07-25 | Biocon India Limited | FORM V CRYSTALLINE [R-(R*,R*)]-2-(4-FLUOROPHENYL)-ß,$G(D)-DIHYDROXY-5-(1-METHYLETHYL)-3-PHENYL-4-[(PHENYLAMINO)CARBONYL]-1H-PYRROLE-1- HEPTANOIC ACID HEMI CALCIUM SALT. (ATORVASTATIN) |
| BR0210666A (pt) * | 2001-06-29 | 2004-10-05 | Warner Lambert Co | Formas cristalinas do sal de cálcio do ácido [r-(r*,r*)]-2-(4-fluorofenil)-beta, delta-dihidróxi-5-(1-metiletil)-3-fenil-4-[(fenilamino)c arbonil]-1h-pirrol-1-heptanóico (2:1) (atorvastatina) |
| AU2002255479B2 (en) * | 2001-07-30 | 2008-09-11 | Dr. Reddy's Laboratories Ltd. | Crystalline forms VI and VII of atorvastatin clacium |
| UA77990C2 (en) * | 2001-12-12 | 2007-02-15 | Crystalline calcium salt of (2:1) [r-(r*,r*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1h-pyrroleheptanic acid | |
| WO2004022053A1 (en) * | 2002-09-03 | 2004-03-18 | Morepen Laboratories Limited | Atorvastatin calcium form vi or hydrates thereof |
| WO2004050618A2 (en) * | 2002-11-28 | 2004-06-17 | Teva Pharmaceutical Industries Ltd. | Crystalline form f of atorvastatin hemi-calcium salt |
-
2003
- 2003-02-19 CA CA002475864A patent/CA2475864A1/en not_active Abandoned
- 2003-02-19 PL PL03372303A patent/PL372303A1/pl not_active Application Discontinuation
- 2003-02-19 DE DE03713610T patent/DE03713610T1/de active Pending
- 2003-02-19 KR KR1020047012591A patent/KR100724515B1/ko not_active Expired - Fee Related
- 2003-02-19 AU AU2003217653A patent/AU2003217653A1/en not_active Abandoned
- 2003-02-19 CN CNB038082071A patent/CN100406436C/zh not_active Expired - Fee Related
- 2003-02-19 WO PCT/US2003/005384 patent/WO2003070702A1/en not_active Ceased
- 2003-02-19 JP JP2003569609A patent/JP2005519076A/ja not_active Withdrawn
- 2003-02-19 EP EP03713610A patent/EP1480950A4/en not_active Withdrawn
- 2003-02-19 HR HR20040768A patent/HRP20040768A2/hr not_active Application Discontinuation
- 2003-02-19 MX MXPA04007939A patent/MXPA04007939A/es unknown
- 2003-02-19 ES ES03713610T patent/ES2241507T1/es active Pending
-
2004
- 2004-08-13 IS IS7402A patent/IS7402A/is unknown
- 2004-09-14 NO NO20043842A patent/NO20043842L/no not_active Application Discontinuation
-
2009
- 2009-06-08 JP JP2009137400A patent/JP2009235083A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| PL372303A1 (pl) | 2005-07-11 |
| CN1646490A (zh) | 2005-07-27 |
| MXPA04007939A (es) | 2004-11-26 |
| NO20043842L (no) | 2004-09-14 |
| AU2003217653A1 (en) | 2003-09-09 |
| EP1480950A1 (en) | 2004-12-01 |
| KR100724515B1 (ko) | 2007-06-04 |
| EP1480950A4 (en) | 2005-05-18 |
| JP2005519076A (ja) | 2005-06-30 |
| DE03713610T1 (de) | 2005-10-20 |
| HRP20040768A2 (en) | 2005-06-30 |
| CN100406436C (zh) | 2008-07-30 |
| WO2003070702A1 (en) | 2003-08-28 |
| KR20040081202A (ko) | 2004-09-20 |
| CA2475864A1 (en) | 2003-08-28 |
| JP2009235083A (ja) | 2009-10-15 |
| IS7402A (is) | 2004-08-13 |
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