AR068932A1 - Metodos para preparar (e) .n-(4-( 3- cloro-4-(2- piridinilmetoxi ) anilino )-3- ciano-7-etoxi-6 quinolinil) -4 - (dimetilamino) -2- butenamida como una sal de maleato, composiciones farmaceuticas para la inhibicion de la actividad cinasa her-2 y formas cristalinas aisladas de dichas sales de maleato - Google Patents
Metodos para preparar (e) .n-(4-( 3- cloro-4-(2- piridinilmetoxi ) anilino )-3- ciano-7-etoxi-6 quinolinil) -4 - (dimetilamino) -2- butenamida como una sal de maleato, composiciones farmaceuticas para la inhibicion de la actividad cinasa her-2 y formas cristalinas aisladas de dichas sales de maleatoInfo
- Publication number
- AR068932A1 AR068932A1 ARP080104565A ARP080104565A AR068932A1 AR 068932 A1 AR068932 A1 AR 068932A1 AR P080104565 A ARP080104565 A AR P080104565A AR P080104565 A ARP080104565 A AR P080104565A AR 068932 A1 AR068932 A1 AR 068932A1
- Authority
- AR
- Argentina
- Prior art keywords
- butenamide
- anilino
- ethoxy
- quinolinyl
- dimethylamino
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 4
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 150000003839 salts Chemical class 0.000 title 2
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 title 1
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 title 1
- HSMPSHPWCOOUJH-UHFFFAOYSA-N anilinyl Chemical class [NH]C1=CC=CC=C1 HSMPSHPWCOOUJH-UHFFFAOYSA-N 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- -1 2- pyridinylmethoxy Chemical group 0.000 abstract 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 abstract 6
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 5
- 239000003960 organic solvent Substances 0.000 abstract 5
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 abstract 5
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical group OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 abstract 4
- JWNPDZNEKVCWMY-VQHVLOKHSA-N neratinib Chemical compound C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 JWNPDZNEKVCWMY-VQHVLOKHSA-N 0.000 abstract 4
- 150000002688 maleic acid derivatives Chemical class 0.000 abstract 3
- VXZCUHNJXSIJIM-MEBGWEOYSA-N (z)-but-2-enedioic acid;(e)-n-[4-[3-chloro-4-(pyridin-2-ylmethoxy)anilino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide Chemical compound OC(=O)\C=C/C(O)=O.C=12C=C(NC(=O)\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 VXZCUHNJXSIJIM-MEBGWEOYSA-N 0.000 abstract 2
- 238000002441 X-ray diffraction Methods 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 2
- 102000001301 EGF receptor Human genes 0.000 abstract 1
- 108060006698 EGF receptor Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 238000000113 differential scanning calorimetry Methods 0.000 abstract 1
- 238000001914 filtration Methods 0.000 abstract 1
- 239000011976 maleic acid Substances 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/12—Antidiarrhoeals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- 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
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- 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
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
- C07C51/41—Preparation of salts of carboxylic acids
- C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
- C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
- C07C57/13—Dicarboxylic acids
- C07C57/145—Maleic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Urology & Nephrology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Hospice & Palliative Care (AREA)
- Otolaryngology (AREA)
- Pulmonology (AREA)
- Endocrinology (AREA)
- Reproductive Health (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US12479607P | 2007-10-17 | 2007-10-17 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR068932A1 true AR068932A1 (es) | 2009-12-16 |
Family
ID=40347915
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP080104565A AR068932A1 (es) | 2007-10-17 | 2008-10-17 | Metodos para preparar (e) .n-(4-( 3- cloro-4-(2- piridinilmetoxi ) anilino )-3- ciano-7-etoxi-6 quinolinil) -4 - (dimetilamino) -2- butenamida como una sal de maleato, composiciones farmaceuticas para la inhibicion de la actividad cinasa her-2 y formas cristalinas aisladas de dichas sales de maleato |
| ARP160100590A AR103866A2 (es) | 2007-10-17 | 2016-03-04 | Composición farmacéutica para la inhibición de la actividad cinasa her-2, compuesto, formas cristalinas aisladas de monohidrato de maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro y maleato parcialmente hidratado de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y métodos para preparar (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato y maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160100590A AR103866A2 (es) | 2007-10-17 | 2016-03-04 | Composición farmacéutica para la inhibición de la actividad cinasa her-2, compuesto, formas cristalinas aisladas de monohidrato de maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida, maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro y maleato parcialmente hidratado de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida y métodos para preparar (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida como una sal de maleato y maleato de (e)-n-{4-[3-cloro-4-(2-piridinilmetoxi)anilino]-3-ciano-7-etoxi-6-quinolinil}-4-(dimetilamino)-2-butenamida anhidro |
Country Status (20)
| Country | Link |
|---|---|
| US (6) | US8022216B2 (enExample) |
| EP (6) | EP3088398A1 (enExample) |
| JP (11) | JP2011500712A (enExample) |
| KR (5) | KR20150039872A (enExample) |
| CN (7) | CN110452221A (enExample) |
| AR (2) | AR068932A1 (enExample) |
| AU (1) | AU2008312474B2 (enExample) |
| BR (2) | BR122019023745B8 (enExample) |
| CA (2) | CA2702930C (enExample) |
| CL (1) | CL2008003088A1 (enExample) |
| ES (3) | ES2612273T3 (enExample) |
| IL (3) | IL308687A (enExample) |
| IN (1) | IN2015DN01135A (enExample) |
| MX (5) | MX387683B (enExample) |
| NZ (3) | NZ705641A (enExample) |
| PA (1) | PA8800701A1 (enExample) |
| RU (2) | RU2463300C2 (enExample) |
| SG (2) | SG185312A1 (enExample) |
| TW (1) | TW200934761A (enExample) |
| WO (1) | WO2009052264A2 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10349113A1 (de) | 2003-10-17 | 2005-05-12 | Boehringer Ingelheim Pharma | Verfahren zur Herstellung von Aminocrotonylverbindungen |
| SI1848414T1 (sl) | 2005-02-03 | 2011-08-31 | Gen Hospital Corp | Postopek za zdravljenje raka, odpornega na gefitinib |
| RU2451524C2 (ru) | 2005-11-04 | 2012-05-27 | Вайет | Противоопухолевые комбинации с ингибиторами mtor, герцептином и/или hki-272 |
| US8022216B2 (en) | 2007-10-17 | 2011-09-20 | Wyeth Llc | Maleate salts of (E)-N-{4-[3-chloro-4-(2-pyridinylmethoxy)anilino]-3-cyano-7-ethoxy-6-quinolinyl}-4-(dimethylamino)-2-butenamide and crystalline forms thereof |
| NZ590009A (en) | 2008-06-17 | 2012-08-31 | Wyeth Llc | Antineoplastic combinations containing hki-272 and vinorelbine |
| KR101434009B1 (ko) | 2008-08-04 | 2014-08-25 | 와이어쓰 엘엘씨 | 4-아닐리노-3-사이아노퀴놀린과 카페시타빈의 항신생물성 조합물 |
| CN103989681A (zh) | 2009-04-06 | 2014-08-20 | 惠氏有限责任公司 | 用于乳腺癌的利用奈拉替尼的治疗方案 |
| CN102428086B (zh) * | 2009-04-29 | 2014-08-20 | 内尔维阿诺医学科学有限公司 | Cdk抑制剂的盐类 |
| WO2011056741A2 (en) | 2009-11-09 | 2011-05-12 | Wyeth Llc | Coated drug spheroids and uses thereof for eliminating or reducing conditions such as emesis and diarrhea |
| WO2011070499A1 (en) | 2009-12-11 | 2011-06-16 | Wyeth Llc | Phosphatidylinositol-3-kinase pathway biomarkers |
| EP2524231B1 (en) | 2010-01-13 | 2017-06-28 | Wyeth LLC | A CUT-POINT IN PTEN PROTEIN EXPRESSION THAT ACCURATELY IDENTIFIES TUMORS AND IS PREDICTIVE OF DRUG RESPONSE TO A PAN-ErbB INHIBITOR |
| CN102675287A (zh) * | 2011-03-11 | 2012-09-19 | 江苏恒瑞医药股份有限公司 | (e)-n-[4-[[3-氯-4-(2-吡啶基甲氧基)苯基]氨基]-3-氰基-7-乙氧基-6-喹啉基]-3-[(2r)-1-甲基吡咯烷-2-基]丙-2-烯酰胺的可药用的盐、其制备方法及其在医药上的应用 |
| CN103748080B (zh) * | 2011-05-26 | 2016-09-28 | 山东轩竹医药科技有限公司 | 喹唑啉衍生物类酪氨酸激酶抑制剂及其制备方法与应用 |
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| WO2016092057A1 (en) * | 2014-12-12 | 2016-06-16 | Sanofi | Medical apparatus package |
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| WO2016210345A1 (en) * | 2015-06-25 | 2016-12-29 | The California Institute For Biomedical Research | Composition and methods for inhibiting mammalian sterile 20-like kinase 1 |
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