TW200916126A - Organic compounds - Google Patents

Organic compounds Download PDF

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Publication number: TW200916126A
Authority: TW; Taiwan
Prior art keywords: lipid; dry powder; drug; powder formulation; dispersion
Prior art date: 2007-08-24

Application number

TW097132233A

Other languages

English (en)

Chinese (zh)

Inventor

Fadi Eskandar

Original Assignee

Novartis Ag

Priority date (The priority date 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 date listed.)

2007-08-24

Filing date

2008-08-22

Publication date

2009-04-16

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40149638&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=TW200916126(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

2008-08-22 Application filed by Novartis Ag filed Critical Novartis Ag

2009-04-16 Publication of TW200916126A publication Critical patent/TW200916126A/zh

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150000002894 organic compounds Chemical class 0.000 title description 2
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239000006185 dispersion Substances 0.000 claims abstract description 81
238000000034 method Methods 0.000 claims abstract description 75
239000008194 pharmaceutical composition Substances 0.000 claims abstract description 46
239000003623 enhancer Substances 0.000 claims abstract description 36
239000002245 particle Substances 0.000 claims description 131
239000008186 active pharmaceutical agent Substances 0.000 claims description 74
108020004459 Small interfering RNA Proteins 0.000 claims description 60
238000002156 mixing Methods 0.000 claims description 29
230000008021 deposition Effects 0.000 claims description 28
HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 26
229960001231 choline Drugs 0.000 claims description 24
OEYIOHPDSNJKLS-UHFFFAOYSA-N choline Chemical compound C[N+](C)(C)CCO OEYIOHPDSNJKLS-UHFFFAOYSA-N 0.000 claims description 24
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Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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TW097132233A 2007-08-24 2008-08-22 Organic compounds TW200916126A (en)

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EP07114981		2007-08-24
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EP2054042B8 (en)	2006-06-30	2020-06-10	iCeutica Pty Ltd	Methods for the preparation of biologically active compounds in nanoparticulate form
MY159208A (en)	2009-04-24	2016-12-30	Iceutica Pty Ltd	A novel formulation of indomethacin
US8808734B2 (en)	2011-07-11	2014-08-19	Full Spectrum Laboratories Limited	Cannabinoid formulations
US9682096B2 (en) *	2012-05-02	2017-06-20	Janssen R & D Ireland	Polyinosinic-polycytidylic acid (poly (I:C)) formulations for the treatment of upper respiratory tract infections
WO2018160295A1 (en) *	2017-01-25	2018-09-07	Yiannios James John	Dietary supplement compositions with enhanced delivery matrix, gummies, chocolates, atomizers and powders containing same, and methods of making same
US9526734B2 (en)	2014-06-09	2016-12-27	Iceutica Pty Ltd.	Formulation of meloxicam
EP3520782A3 (en) *	2018-02-01	2019-11-13	Corvus Pharmaceuticals, Inc.	Pharmaceutical formulations containing adenosine a2a receptor antagonists
KR20200117998A (ko)	2018-02-01	2020-10-14	코버스 파마슈티칼스, 인크.	약학적 조성물
MX2021005508A (es) *	2018-11-13	2021-09-08	Civitas Therapeutics Inc	Fórmulaciones y procesos de polinucleótido en polvo respirable para inhalación.
US10729687B1 (en) *	2019-07-09	2020-08-04	Orexo Ab	Pharmaceutical composition for nasal delivery
WO2021004524A1 (en) *	2019-07-10	2021-01-14	The University Of Hong Kong	PEGylated synthetic KL4 peptide, Compositions and Methods Thereof
CN114209651A (zh) *	2021-11-18	2022-03-22	上海欣峰制药有限公司	头孢噻肟钠化合物的药物制剂及其制备方法
CN114053226A (zh) *	2021-11-18	2022-02-18	上海欣峰制药有限公司	头孢米诺钠化合物的药物制剂及其制备方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE69629702T2 (de) *	1995-08-01	2004-06-17	Isis Pharmaceuticals, Inc., Carlsbad	Liposomale oligonukleotidzusammensetzungen
ES2702942T3 (es) *	2003-04-17	2019-03-06	Alnylam Pharmaceuticals Inc	Agentes de ARNi modificados
JPWO2005011632A1 (ja) *	2003-08-01	2006-09-14	独立行政法人産業技術総合研究所	糖鎖を有する標的指向性および腸管吸収制御性リポソームならびにそれを含む癌治療薬および診断薬
CA2565633C (en) *	2004-05-05	2016-04-26	Atugen Ag	Lipids, lipid complexes and use thereof
GB0418172D0 (en) *	2004-08-13	2004-09-15	Ic Vec Ltd	Vector
CN101111269A (zh) *	2005-01-28	2008-01-23	协和发酵工业株式会社	抑制靶基因表达的组合物
US20070172430A1 (en) *	2006-01-20	2007-07-26	Nastech Pharmaceutical Company Inc.	Dry powder compositions for rna influenza therapeutics
ES2549728T3 (es) *	2006-04-20	2015-11-02	Silence Therapeutics Gmbh	Formulaciones de lipoplexo para la administración específica al endotelio vascular
GB0608838D0 (en) *	2006-05-04	2006-06-14	Novartis Ag	Organic compounds

2008
- 2008-08-21 AR ARP080103643A patent/AR067997A1/es unknown
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AR067997A1 (es)	2009-10-28
WO2009027337A1 (en)	2009-03-05
PE20090607A1 (es)	2009-06-11
CL2008002479A1 (es)	2009-05-08

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