NZ591945A - Disubstituted phthalazine hedgehog pathway antagonists - Google Patents
Disubstituted phthalazine hedgehog pathway antagonistsInfo
- Publication number
- NZ591945A NZ591945A NZ591945A NZ59194509A NZ591945A NZ 591945 A NZ591945 A NZ 591945A NZ 591945 A NZ591945 A NZ 591945A NZ 59194509 A NZ59194509 A NZ 59194509A NZ 591945 A NZ591945 A NZ 591945A
- Authority
- NZ
- New Zealand
- Prior art keywords
- cancer
- fluorophenyl
- hydrogen
- fluoro
- compounds
- Prior art date
Links
- 241000289669 Erinaceus europaeus Species 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 230000037361 pathway Effects 0.000 title 1
- LFSXCDWNBUNEEM-UHFFFAOYSA-N phthalazine Chemical class C1=NN=CC2=CC=CC=C21 LFSXCDWNBUNEEM-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000001153 fluoro group Chemical group F* 0.000 abstract 3
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- -1 difluoromethoxy, methoxy Chemical group 0.000 abstract 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 2
- BPOQPMSRUDFRCM-URBRKQAFSA-N (2s,5r)-n-(4-fluorophenyl)-4-[4-(4-fluorophenyl)phthalazin-1-yl]-2,5-dimethylpiperazine-1-carboxamide;hydrochloride Chemical compound Cl.C([C@@H](C)N(C[C@@H]1C)C=2C3=CC=CC=C3C(C=3C=CC(F)=CC=3)=NN=2)N1C(=O)NC1=CC=C(F)C=C1 BPOQPMSRUDFRCM-URBRKQAFSA-N 0.000 abstract 1
- 208000003950 B-cell lymphoma Diseases 0.000 abstract 1
- 206010004146 Basal cell carcinoma Diseases 0.000 abstract 1
- 208000003174 Brain Neoplasms Diseases 0.000 abstract 1
- 206010006187 Breast cancer Diseases 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 abstract 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 abstract 1
- 208000008839 Kidney Neoplasms Diseases 0.000 abstract 1
- 208000034578 Multiple myelomas Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010033128 Ovarian cancer Diseases 0.000 abstract 1
- 206010061535 Ovarian neoplasm Diseases 0.000 abstract 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 1
- 206010035226 Plasma cell myeloma Diseases 0.000 abstract 1
- 206010060862 Prostate cancer Diseases 0.000 abstract 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 abstract 1
- 206010038389 Renal cancer Diseases 0.000 abstract 1
- 206010041067 Small cell lung cancer Diseases 0.000 abstract 1
- 208000005718 Stomach Neoplasms Diseases 0.000 abstract 1
- 201000009036 biliary tract cancer Diseases 0.000 abstract 1
- 208000020790 biliary tract neoplasm Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 201000004101 esophageal cancer Diseases 0.000 abstract 1
- 206010017758 gastric cancer Diseases 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 201000010982 kidney cancer Diseases 0.000 abstract 1
- 201000007270 liver cancer Diseases 0.000 abstract 1
- 208000014018 liver neoplasm Diseases 0.000 abstract 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- VWVTVUOMKSFMFG-UHFFFAOYSA-N n-(4-cyanophenyl)-2-methyl-4-(4-phenylphthalazin-1-yl)piperazine-1-carboxamide;hydrochloride Chemical compound Cl.CC1CN(C=2C3=CC=CC=C3C(C=3C=CC=CC=3)=NN=2)CCN1C(=O)NC1=CC=C(C#N)C=C1 VWVTVUOMKSFMFG-UHFFFAOYSA-N 0.000 abstract 1
- VGVMZZXUJBGLCX-UHFFFAOYSA-N n-(4-fluorophenyl)-4-[4-(4-fluorophenyl)phthalazin-1-yl]-2-(hydroxymethyl)piperazine-1-carboxamide;hydrochloride Chemical compound Cl.OCC1CN(C=2C3=CC=CC=C3C(C=3C=CC(F)=CC=3)=NN=2)CCN1C(=O)NC1=CC=C(F)C=C1 VGVMZZXUJBGLCX-UHFFFAOYSA-N 0.000 abstract 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 abstract 1
- 201000002528 pancreatic cancer Diseases 0.000 abstract 1
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000000587 small cell lung carcinoma Diseases 0.000 abstract 1
- 201000011549 stomach cancer Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US11070308P | 2008-11-03 | 2008-11-03 | |
| PCT/US2009/061573 WO2010062507A1 (en) | 2008-11-03 | 2009-10-22 | Disubstituted phthalazine hedgehog pathway antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| NZ591945A true NZ591945A (en) | 2012-10-26 |
Family
ID=41566219
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ591945A NZ591945A (en) | 2008-11-03 | 2009-10-22 | Disubstituted phthalazine hedgehog pathway antagonists |
Country Status (29)
| Country | Link |
|---|---|
| US (1) | US8404687B2 (https=) |
| EP (1) | EP2364185B1 (https=) |
| JP (1) | JP2012507535A (https=) |
| KR (1) | KR101335746B1 (https=) |
| CN (1) | CN102202737B (https=) |
| AU (1) | AU2009320251C1 (https=) |
| BR (1) | BRPI0921437A2 (https=) |
| CA (1) | CA2742539C (https=) |
| CL (1) | CL2011000979A1 (https=) |
| CO (1) | CO6382123A2 (https=) |
| CR (1) | CR20110202A (https=) |
| CY (1) | CY1114023T1 (https=) |
| DK (1) | DK2364185T3 (https=) |
| EA (1) | EA018931B1 (https=) |
| EC (1) | ECSP11011021A (https=) |
| ES (1) | ES2418479T3 (https=) |
| HR (1) | HRP20130527T1 (https=) |
| IL (1) | IL211841A0 (https=) |
| MA (1) | MA32726B1 (https=) |
| MX (1) | MX2011004683A (https=) |
| NZ (1) | NZ591945A (https=) |
| PE (1) | PE20110433A1 (https=) |
| PL (1) | PL2364185T3 (https=) |
| PT (1) | PT2364185E (https=) |
| SI (1) | SI2364185T1 (https=) |
| TN (1) | TN2011000166A1 (https=) |
| UA (1) | UA102115C2 (https=) |
| WO (1) | WO2010062507A1 (https=) |
| ZA (1) | ZA201102448B (https=) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2681162C (en) * | 2007-03-15 | 2015-11-24 | Novartis Ag | Benzyl and pyridine derivatives as modulators of hedgehog pathway |
| UA102250C2 (ru) | 2008-04-29 | 2013-06-25 | Эли Лилли Энд Компани | Двухзамещенные фталазины - антагонисты проводящего пути hedgehog |
| US20100041663A1 (en) | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
| KR101342184B1 (ko) | 2008-11-17 | 2013-12-19 | 일라이 릴리 앤드 캄파니 | 사치환된 피리다진 헷지호그 경로 길항제 |
| BRPI0921777A2 (pt) | 2008-11-17 | 2016-01-12 | Lilly Co Eli | antagonistas da via hedgehog de piridazina tetrassubstituída |
| AR077014A1 (es) | 2009-06-19 | 2011-07-27 | Lilly Co Eli | Compuesto derivado de ftalazina 1,4-disustituida, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para el tratamiento de cancer |
| WO2015073691A1 (en) | 2013-11-14 | 2015-05-21 | The Board Of Trustees Of The Leland Stanford Junior University | Methods for treating cancer by activation of bmp signaling |
| CN105985319B (zh) * | 2015-02-11 | 2019-02-26 | 复旦大学 | 芳基酞嗪化合物及其制备方法和用途 |
| CN105985321B (zh) * | 2015-02-11 | 2018-10-26 | 复旦大学 | 吡唑酞嗪化合物及其制备方法和用途 |
| CN105985320B (zh) * | 2015-02-11 | 2018-10-26 | 复旦大学 | 苄基酞嗪化合物及其制备方法和用途 |
| JP2023546536A (ja) | 2020-10-13 | 2023-11-02 | エンデバー バイオメディシンズ， インコーポレイテッド | 線維症を処置する方法 |
| US12605377B2 (en) | 2020-10-13 | 2026-04-21 | Endeavor Biomedicines, Inc. | Methods of treating fibrosis |
| IL319619A (en) * | 2022-09-23 | 2025-05-01 | Merck Sharp & Dohme Llc | Phthalazine derivatives used as NOD-LIKE PROTEIN 3 receptor inhibitors |
| WO2025188802A1 (en) | 2024-03-05 | 2025-09-12 | Endeavor Biomedicines, Inc. | Methods of improving lung function |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB1293565A (en) * | 1969-05-03 | 1972-10-18 | Aspro Nicholas Ltd | Aminophthalazines and pharmaceutical compositions thereof |
| MY117098A (en) * | 1996-01-15 | 2004-05-31 | Janssen Pharmaceutica Nv | Angiogenesis inhibiting pyridazinamines |
| EP0882717B1 (en) * | 1996-10-01 | 2010-09-08 | Kyowa Hakko Kirin Co., Ltd. | Nitrogenous heterocyclic compounds |
| US6432970B2 (en) * | 1998-04-09 | 2002-08-13 | Johns Hopkins University School Of Medicine | Inhibitors of hedgehog signaling pathways, compositions and uses related thereto |
| JP5067986B2 (ja) | 1998-04-09 | 2012-11-07 | ジョンズ ホプキンズ ユニヴァーシティー スクール オブ メディシン | ヘッジホッグシグナリング経路の阻害剤としてのステロイドアルカロイド誘導体の使用 |
| ATE283700T1 (de) | 1999-06-08 | 2004-12-15 | Lorantis Ltd | Therapeutische verwendung eines inhibitors des hedgehog signalübertragungsweges |
| EP1496905B1 (en) | 2002-04-22 | 2008-08-13 | Johns Hopkins University School of Medicine | Modulators of hedgehog signaling pathways, compositions and uses related thereto |
| WO2004020599A2 (en) | 2002-08-29 | 2004-03-11 | Curis, Inc. | Hedgehog antagonists, methods and uses related thereto |
| WO2005033288A2 (en) | 2003-09-29 | 2005-04-14 | The Johns Hopkins University | Hedgehog pathway antagonists |
| TW200533356A (en) | 2004-02-24 | 2005-10-16 | Mitsubishi Pharma Corp | Fused pyridazine derivatives |
| WO2006004589A2 (en) | 2004-05-08 | 2006-01-12 | Neurogen Corporation | 3-aryl-5,6-disubstituted pyridazines |
| ES2377430T3 (es) * | 2004-09-02 | 2012-03-27 | Genentech, Inc. | Inhibidores piridílicos de la señalización de hedgehog |
| EP1900731A1 (de) | 2006-09-07 | 2008-03-19 | Bayer Schering Pharma Aktiengesellschaft | N-(1-Phthalazin-1-yl-piperidin-4-yl)-amide als EP2-Rezeptor Modulatoren |
| CA2681162C (en) * | 2007-03-15 | 2015-11-24 | Novartis Ag | Benzyl and pyridine derivatives as modulators of hedgehog pathway |
| US8153633B2 (en) * | 2007-06-25 | 2012-04-10 | Amgen Inc. | Phthalazine compounds, compositions and methods of use |
| US8222251B2 (en) | 2007-09-07 | 2012-07-17 | Amgen Inc. | Pyridopyridazine compounds, compositions and methods of use |
| UA102250C2 (ru) * | 2008-04-29 | 2013-06-25 | Эли Лилли Энд Компани | Двухзамещенные фталазины - антагонисты проводящего пути hedgehog |
| US20100041663A1 (en) | 2008-07-18 | 2010-02-18 | Novartis Ag | Organic Compounds as Smo Inhibitors |
| BRPI0921777A2 (pt) | 2008-11-17 | 2016-01-12 | Lilly Co Eli | antagonistas da via hedgehog de piridazina tetrassubstituída |
| KR101342184B1 (ko) | 2008-11-17 | 2013-12-19 | 일라이 릴리 앤드 캄파니 | 사치환된 피리다진 헷지호그 경로 길항제 |
| AR077014A1 (es) * | 2009-06-19 | 2011-07-27 | Lilly Co Eli | Compuesto derivado de ftalazina 1,4-disustituida, composicion farmaceutica que lo comprende y uso para preparar un medicamento util para el tratamiento de cancer |
-
2009
- 2009-10-22 MX MX2011004683A patent/MX2011004683A/es active IP Right Grant
- 2009-10-22 ES ES09740613T patent/ES2418479T3/es active Active
- 2009-10-22 NZ NZ591945A patent/NZ591945A/xx not_active IP Right Cessation
- 2009-10-22 AU AU2009320251A patent/AU2009320251C1/en not_active Ceased
- 2009-10-22 JP JP2011534624A patent/JP2012507535A/ja active Pending
- 2009-10-22 WO PCT/US2009/061573 patent/WO2010062507A1/en not_active Ceased
- 2009-10-22 SI SI200930625T patent/SI2364185T1/sl unknown
- 2009-10-22 CN CN200980143394.3A patent/CN102202737B/zh not_active Expired - Fee Related
- 2009-10-22 EA EA201170640A patent/EA018931B1/ru not_active IP Right Cessation
- 2009-10-22 CA CA2742539A patent/CA2742539C/en not_active Expired - Fee Related
- 2009-10-22 DK DK09740613.6T patent/DK2364185T3/da active
- 2009-10-22 PT PT97406136T patent/PT2364185E/pt unknown
- 2009-10-22 PE PE2011000937A patent/PE20110433A1/es not_active Application Discontinuation
- 2009-10-22 BR BRPI0921437A patent/BRPI0921437A2/pt not_active IP Right Cessation
- 2009-10-22 PL PL09740613T patent/PL2364185T3/pl unknown
- 2009-10-22 HR HRP20130527AT patent/HRP20130527T1/hr unknown
- 2009-10-22 UA UAA201105364A patent/UA102115C2/ru unknown
- 2009-10-22 EP EP09740613.6A patent/EP2364185B1/en active Active
- 2009-10-22 KR KR1020117010063A patent/KR101335746B1/ko not_active Expired - Fee Related
- 2009-10-22 US US13/122,212 patent/US8404687B2/en not_active Expired - Fee Related
-
2011
- 2011-03-21 IL IL211841A patent/IL211841A0/en unknown
- 2011-04-01 ZA ZA2011/02448A patent/ZA201102448B/en unknown
- 2011-04-07 TN TN2011000166A patent/TN2011000166A1/fr unknown
- 2011-04-15 CR CR20110202A patent/CR20110202A/es not_active Application Discontinuation
- 2011-04-22 MA MA33790A patent/MA32726B1/fr unknown
- 2011-05-02 CL CL2011000979A patent/CL2011000979A1/es unknown
- 2011-05-02 EC EC2011011021A patent/ECSP11011021A/es unknown
- 2011-05-11 CO CO11058054A patent/CO6382123A2/es active IP Right Grant
-
2013
- 2013-06-05 CY CY20131100447T patent/CY1114023T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PSEA | Patent sealed | ||
| RENW | Renewal (renewal fees accepted) |
Free format text: PATENT RENEWED FOR 3 YEARS UNTIL 22 OCT 2016 BY THOMSON REUTERS Effective date: 20130920 |
|
| LAPS | Patent lapsed |