IL126899A - Preparations for once-daily treatment of diseases mediated by cyclooxygenase-2 - Google Patents

Preparations for once-daily treatment of diseases mediated by cyclooxygenase-2

Info

Publication number: IL126899A
Authority: IL; Israel
Prior art keywords: treatment; phenyl; use according; furanone; once
Prior art date: 1996-05-17

Application number

IL12689997A

Other languages

English (en)

Hebrew (he)

Other versions

IL126899A0 (en

Original Assignee

Merck & Co Inc

Merck Frosst Canada Inc

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.)

1996-05-17

Filing date

1997-05-13

Publication date

2004-03-28

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26309472&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=IL126899(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1996-06-10 Priority claimed from GBGB9612063.9A external-priority patent/GB9612063D0/en

1997-05-13 Application filed by Merck & Co Inc, Merck Frosst Canada Inc filed Critical Merck & Co Inc

1999-09-22 Publication of IL126899A0 publication Critical patent/IL126899A0/xx

2004-03-28 Publication of IL126899A publication Critical patent/IL126899A/en

Links

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239000008194 pharmaceutical composition Substances 0.000 claims abstract description 7
239000004480 active ingredient Substances 0.000 claims abstract description 4
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PXKGDTZJJAGTOP-UHFFFAOYSA-N 1-ethynyl-2-(4-methylsulfonylphenyl)benzene Chemical group C1=CC(S(=O)(=O)C)=CC=C1C1=CC=CC=C1C#C PXKGDTZJJAGTOP-UHFFFAOYSA-N 0.000 description 1
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Classifications

- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/365—Lactones
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
- A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
- 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
- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- 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
- 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
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
- 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
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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IL12689997A 1996-05-17 1997-05-13 Preparations for once-daily treatment of diseases mediated by cyclooxygenase-2 IL126899A (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US1787896P	1996-05-17	1996-05-17
GBGB9612063.9A GB9612063D0 (en)	1996-06-10	1996-06-10	Compositions for a once a day treatment of cyclooxygenase-2 mediated diseases
PCT/US1997/008041 WO1997044028A1 (en)	1996-05-17	1997-05-13	Compositions for a once a day treatment of cyclooxygenase-2 mediated diseases

Publications (2)

Publication Number	Publication Date
IL126899A0 IL126899A0 (en)	1999-09-22
IL126899A true IL126899A (en)	2004-03-28

Family

ID=26309472

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
IL12689997A IL126899A (en)	1996-05-17	1997-05-13	Preparations for once-daily treatment of diseases mediated by cyclooxygenase-2

Country Status (28)

Country	Link
US (1)	US6063811A (is)
EP (1)	EP0910368A1 (is)
JP (1)	JPH11512754A (is)
KR (1)	KR100373622B1 (is)
CN (1)	CN1140267C (is)
AR (1)	AR012014A1 (is)
AU (1)	AU3004997A (is)
BG (1)	BG103000A (is)
BR (1)	BR9709097A (is)
CA (1)	CA2254061C (is)
CO (1)	CO5050370A1 (is)
CZ (1)	CZ291463B6 (is)
DZ (1)	DZ2200A1 (is)
EA (1)	EA001596B1 (is)
EE (1)	EE03746B1 (is)
HR (1)	HRP970262A2 (is)
HU (1)	HUP9902889A3 (is)
ID (1)	ID16921A (is)
IL (1)	IL126899A (is)
IS (1)	IS4891A (is)
MY (1)	MY116201A (is)
NO (1)	NO985342D0 (is)
NZ (1)	NZ332670A (is)
PE (1)	PE66998A1 (is)
PL (1)	PL188649B1 (is)
SK (1)	SK284330B6 (is)
TR (1)	TR199802345T2 (is)
WO (1)	WO1997044028A1 (is)

Families Citing this family (26)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
JP2002506024A (ja) *	1998-03-13	2002-02-26	メルクエンドカムパニーインコーポレーテッド	急性冠動脈虚血症候群および関連状態に対する併用療法および組成物
US6136804A (en) *	1998-03-13	2000-10-24	Merck & Co., Inc.	Combination therapy for treating, preventing, or reducing the risks associated with acute coronary ischemic syndrome and related conditions
SA99191255B1 (ar) *	1998-11-30	2006-11-25	جي دي سيرل اند كو	مركبات سيليكوكسيب celecoxib
CO5190664A1 (es)	1999-06-30	2002-08-29	Pfizer Prod Inc	Terapia de combinacion para el tratamiento de migrana administracion de un receptor 5ht, cafeina y un inhibidor de ciclooxigenasa-2
GB9920558D0 (en) *	1999-08-31	1999-11-03	Bradford Particle Design Ltd	Methods for particle formation and their products
EP1239856A1 (en) *	1999-12-22	2002-09-18	Pharmacia Corporation	Sustained-release formulation of a cyclooxygenase-2 inhibitor
EA011309B1 (ru)	2000-06-13	2009-02-27	Вайет	Составы для ослабления боли, содержащие целекоксиб
EP1309315B1 (en) *	2000-08-18	2006-06-14	Pharmacia Corporation	Rapidly disintegrating oral formulation of valdecoxib
CN1638739A (zh) *	2000-08-18	2005-07-13	法玛西雅厄普约翰美国公司	治疗成瘾性障碍的化合物
WO2002017896A2 (en) *	2000-08-29	2002-03-07	Peter Van Patten	Combination for the treatment of migraine comprising a cyclooxygenase-2 inhibitor and acetylsalicylic acid
PE20020351A1 (es) *	2000-09-11	2002-06-14	Novartis Ag	Composiciones farmaceuticas que comprenden acido 5-metil-2-(2'-cloro-6'-fluoroanilino)fenilacetico como inhibidor de la ciclooxigenasa-2
US7115565B2 (en) *	2001-01-18	2006-10-03	Pharmacia & Upjohn Company	Chemotherapeutic microemulsion compositions of paclitaxel with improved oral bioavailability
EP1423114A4 (en) *	2001-05-04	2006-05-17	Merck & Co Inc	METHOD AND COMPOSITIONS FOR TREATING MIGRAINE
AR036312A1 (es) *	2001-08-31	2004-08-25	Novartis Ag	Composicion farmaceutica
PL369298A1 (en) *	2001-09-26	2005-04-18	Pharmacia Corporation	Intraorally disintegrating valdecoxib compositions
CA2462881A1 (en) *	2001-10-10	2003-04-17	Pharmacia Corporation	Intraorally disintegrating valdecoxib compositions prepared by spray drying process
KR20040089654A (ko) *	2002-03-07	2004-10-21	노파르티스 아게	약제학적 조성물
ES2214129B1 (es) *	2003-02-13	2005-12-01	Almirall Prodesfarma, S.A.	3-fenilfuran-2-onas.
ES2213485B1 (es)	2003-02-13	2005-12-16	Almirall Prodesfarma, S.A.	Derivados de la 2-fenilpiran-4-ona.
ES2275218T3 (es)	2003-05-07	2007-06-01	Osteologix A/S	Sales de estroncio hidrosolubles para el tratamiento de afecciones de cartilagos y/o huesos.
TR200301552A1 (tr) *	2003-09-18	2005-10-21	Nobel İlaç Sanayi̇ Ve Ti̇caret A. Ş.	Rofekoksib' in yeni oral farmakolojik formülasyonları.
CA2676413A1 (en) *	2007-01-19	2008-07-31	Mallinckrodt Inc.	Diagnostic and therapeutic cyclooxygenase-2 binding ligands
CA3119728A1 (en)	2018-11-21	2020-05-28	Tremeau Pharmaceuticals, Inc.	Purified forms of rofecoxib, methods of manufacture and use
US20200323830A1 (en) *	2019-04-09	2020-10-15	Tremeau Pharmaceuticals, Inc.	Treatment of viral hemorrhagic fevers with etoricoxib
US10945992B1 (en)	2019-11-13	2021-03-16	Tremeau Pharmaceuticals, Inc.	Dosage forms of rofecoxib and related methods
US11161833B1 (en)	2021-04-09	2021-11-02	Tremeau Pharmaceuticals, Inc.	Deuterated etoricoxib, methods of manufacture, and use thereof

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US5474995A (en) *	1993-06-24	1995-12-12	Merck Frosst Canada, Inc.	Phenyl heterocycles as cox-2 inhibitors
WO1995018799A1 (en) *	1994-01-10	1995-07-13	Merck Frosst Canada Inc.	Phenyl heterocycles as cox-2 inhibitors

1997
- 1997-05-13 SK SK1567-98A patent/SK284330B6/sk unknown
- 1997-05-13 CA CA002254061A patent/CA2254061C/en not_active Expired - Fee Related
- 1997-05-13 US US09/180,647 patent/US6063811A/en not_active Expired - Lifetime
- 1997-05-13 CZ CZ19983738A patent/CZ291463B6/cs not_active IP Right Cessation
- 1997-05-13 IL IL12689997A patent/IL126899A/en not_active IP Right Cessation
- 1997-05-13 EP EP97924688A patent/EP0910368A1/en not_active Withdrawn
- 1997-05-13 EE EE9800393A patent/EE03746B1/xx not_active IP Right Cessation
- 1997-05-13 NZ NZ332670A patent/NZ332670A/xx unknown
- 1997-05-13 TR TR1998/02345T patent/TR199802345T2/xx unknown
- 1997-05-13 AU AU30049/97A patent/AU3004997A/en not_active Abandoned
- 1997-05-13 JP JP9542486A patent/JPH11512754A/ja active Pending
- 1997-05-13 KR KR10-1998-0709239A patent/KR100373622B1/ko not_active Expired - Fee Related
- 1997-05-13 EA EA199801017A patent/EA001596B1/ru not_active IP Right Cessation
- 1997-05-13 BR BR9709097A patent/BR9709097A/pt not_active IP Right Cessation
- 1997-05-13 CN CNB971963150A patent/CN1140267C/zh not_active Expired - Fee Related
- 1997-05-13 HU HU9902889A patent/HUP9902889A3/hu unknown
- 1997-05-13 WO PCT/US1997/008041 patent/WO1997044028A1/en not_active Ceased
- 1997-05-14 AR ARP970102021A patent/AR012014A1/es unknown
- 1997-05-14 DZ DZ970087A patent/DZ2200A1/fr active
- 1997-05-15 PE PE1997000379A patent/PE66998A1/es not_active Application Discontinuation
- 1997-05-16 HR HR9612063.9A patent/HRP970262A2/xx not_active Application Discontinuation
- 1997-05-16 ID IDP971640A patent/ID16921A/id unknown
- 1997-05-16 MY MYPI97002138A patent/MY116201A/en unknown
- 1997-05-16 CO CO97026568A patent/CO5050370A1/es unknown
1998
- 1998-11-10 IS IS4891A patent/IS4891A/is unknown
- 1998-11-16 NO NO985342A patent/NO985342D0/no not_active Application Discontinuation
- 1998-12-08 BG BG103000A patent/BG103000A/xx unknown
1999
- 1999-01-11 PL PL97329940A patent/PL188649B1/pl not_active IP Right Cessation

Also Published As

Publication number	Publication date
HK1021623A1 (en)	2000-06-23
HRP970262A2 (en)	1998-06-30
EA001596B1 (ru)	2001-06-25
SK156798A3 (en)	2000-01-18
EP0910368A1 (en)	1999-04-28
EE9800393A (et)	1999-06-15
DZ2200A1 (fr)	2004-06-20
PL188649B1 (pl)	2005-03-31
BR9709097A (pt)	1999-08-03
IS4891A (is)	1998-11-10
KR20000011082A (ko)	2000-02-25
HUP9902889A3 (en)	2002-04-29
CZ291463B6 (cs)	2003-03-12
PL329940A1 (en)	1999-04-26
NO985342L (no)	1998-11-16
ID16921A (id)	1997-11-20
CA2254061C (en)	2003-12-02
IL126899A0 (en)	1999-09-22
EE03746B1 (et)	2002-06-17
CN1140267C (zh)	2004-03-03
NZ332670A (en)	2000-07-28
CN1225010A (zh)	1999-08-04
CO5050370A1 (es)	2001-06-27
CZ373898A3 (cs)	1999-06-16
AU3004997A (en)	1997-12-09
WO1997044028A1 (en)	1997-11-27
HUP9902889A2 (hu)	2002-01-28
TR199802345T2 (xx)	1999-03-22
PE66998A1 (es)	1998-10-24
SK284330B6 (sk)	2005-01-03
US6063811A (en)	2000-05-16
JPH11512754A (ja)	1999-11-02
CA2254061A1 (en)	1997-11-27
EA199801017A1 (ru)	1999-04-29
NO985342D0 (no)	1998-11-16
KR100373622B1 (ko)	2003-07-12
AR012014A1 (es)	2000-09-27
MY116201A (en)	2003-11-28
BG103000A (en)	1999-09-30

Legal Events

Date	Code	Title
2005-09-25	FF	Patent granted
2005-09-25	KB	Patent renewed
2007-07-06	KB	Patent renewed
2015-12-31	MM9K	Patent not in force due to non-payment of renewal fees

Publication	Publication Date	Title
CA2254061C (en)	2003-12-02	Compositions for a once a day treatment of cyclooxygenase-2 mediated diseases
US5521213A (en)	1996-05-28	Diaryl bicyclic heterocycles as inhibitors of cyclooxygenase-2
CA2278241C (en)	2006-03-14	Phenyl heterocycles as cyclooxygenase-2 inhibitors
JP2788677B2 (ja)	1998-08-20	Ｃｏｘ−２阻害剤としてのフェニル複素環
RO118585B1 (ro)	2003-07-30	Procedeu pentru prepararea unor derivati de furanona folositi ca inhibitori de ciclooxigenaza - 2
JP2001199954A (ja)	2001-07-24	Ｃｏｘ−２インヒビターとしての（メチルスルホニル）フェニル−２−（５ｈ）−フラノン類
EP0808305A1 (en)	1997-11-26	3,4-diaryl substituted pyridines for the treatment of inflammation
JPH11500748A (ja)	1999-01-19	Ｃｏｘ−２阻害剤のプロドラッグとしての３，４−ジアリール−２−ヒドロキシ−２，５−ジヒドロフラン
NO311761B1 (no)	2002-01-21	2-(3H)-Oksazolonderivater og deres anvendelse
CA2301590C (en)	2007-05-01	2-aminopyridines as inhibitors of cyclooxygenase-2
AU4622101A (en)	2001-07-26	Compositions for a once a day treatment of cyclooxygenase-2 mediated diseases
CA2254121A1 (en)	1997-11-27	Compositions for a once a day treatment of cyclooxygenase-2 mediated diseases
AU774172B2 (en)	2004-06-17	Polymorphic b form of 3-(cyclopropylmethoxy)-4-(4-(methylsulfonyl)phenyl)-5,5- dimethyl-5h-furan-2-one
US5939417A (en)	1999-08-17	1,3,6-trihydro-6-aza-3-oxapentalen-2-one derivatives for the treatment of neoplasia
JP2006517562A (ja)	2006-07-27	選択的ｃｏｘ−２阻害剤としての２，３’−ビピリジン誘導体
US6455703B2 (en)	2002-09-24	1,3,6,-Trihydro-6-aza-3-oxapentalen-2-one derivatives for the treatment of neoplasia
HK1021623B (en)	2004-12-31	Compositions for a once a day treatment of cyclooxygenase-2 mediated diseases
UA51706C2 (uk)	2002-12-16	Спосіб лікування запального захворювання за допомогою 3-феніл-4-(4-метилсульфоніл)феніл)-2-(5н)-фуранону