UA77812C2 - Anelated pyrrol substances as proton pump inhibitors for treating gastric ulcer - Google Patents

Anelated pyrrol substances as proton pump inhibitors for treating gastric ulcer Download PDF

Info

Publication number: UA77812C2
Authority: UA; Ukraine
Prior art keywords: acid; formula; gastric; agents; compounds
Prior art date: 2002-05-17

Application number

UA20041210349A

Other languages

English (en)

Ukrainian (uk)

Inventor

Adams G Smolka

Charles E Hammond

Sandeep E Gupta

Original Assignee

Merckle Gmbh

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.)

2002-05-17

Filing date

2003-05-16

Publication date

2007-01-15

2003-05-16 Application filed by Merckle Gmbh filed Critical Merckle Gmbh

2007-01-15 Publication of UA77812C2 publication Critical patent/UA77812C2/uk

Links

208000007107 Stomach Ulcer Diseases 0.000 title claims description 7
201000005917 gastric ulcer Diseases 0.000 title claims 2
229940126409 proton pump inhibitor Drugs 0.000 title description 9
239000000612 proton pump inhibitor Substances 0.000 title description 9
239000000126 substance Substances 0.000 title description 2
KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 title 2
150000001875 compounds Chemical class 0.000 claims abstract description 86
230000002496 gastric effect Effects 0.000 claims abstract description 63
241000124008 Mammalia Species 0.000 claims abstract description 36
230000002401 inhibitory effect Effects 0.000 claims abstract description 22
230000006378 damage Effects 0.000 claims abstract description 16
108010083204 Proton Pumps Proteins 0.000 claims abstract description 14
210000001156 gastric mucosa Anatomy 0.000 claims abstract description 13
102100021904 Potassium-transporting ATPase alpha chain 1 Human genes 0.000 claims abstract 3
-1 trifluoromethoxy, hydroxy Chemical group 0.000 claims description 74
125000000217 alkyl group Chemical group 0.000 claims description 47
150000003254 radicals Chemical class 0.000 claims description 34
230000005764 inhibitory process Effects 0.000 claims description 24
125000003545 alkoxy group Chemical group 0.000 claims description 22
125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 21
125000001188 haloalkyl group Chemical group 0.000 claims description 20
125000003118 aryl group Chemical group 0.000 claims description 18
229910052736 halogen Inorganic materials 0.000 claims description 16
150000002367 halogens Chemical class 0.000 claims description 16
239000003112 inhibitor Substances 0.000 claims description 15
229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 15
239000002253 acid Substances 0.000 claims description 14
CGIGDMFJXJATDK-UHFFFAOYSA-N indomethacin Chemical compound CC1=C(CC(O)=O)C2=CC(OC)=CC=C2N1C(=O)C1=CC=C(Cl)C=C1 CGIGDMFJXJATDK-UHFFFAOYSA-N 0.000 claims description 14
239000008194 pharmaceutical composition Substances 0.000 claims description 14
125000000753 cycloalkyl group Chemical group 0.000 claims description 13
230000002178 gastroprotective effect Effects 0.000 claims description 13
125000001424 substituent group Chemical group 0.000 claims description 13
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims description 12
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150000003839 salts Chemical class 0.000 claims description 12
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BSYNRYMUTXBXSQ-UHFFFAOYSA-N Aspirin Chemical compound CC(=O)OC1=CC=CC=C1C(O)=O BSYNRYMUTXBXSQ-UHFFFAOYSA-N 0.000 claims description 10
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125000004644 alkyl sulfinyl group Chemical group 0.000 claims description 9
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CNBGNNVCVSKAQZ-UHFFFAOYSA-N benzydamine Chemical compound C12=CC=CC=C2C(OCCCN(C)C)=NN1CC1=CC=CC=C1 CNBGNNVCVSKAQZ-UHFFFAOYSA-N 0.000 claims description 6
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ABBQHOQBGMUPJH-UHFFFAOYSA-M Sodium salicylate Chemical compound [Na+].OC1=CC=CC=C1C([O-])=O ABBQHOQBGMUPJH-UHFFFAOYSA-M 0.000 claims description 3
125000004183 alkoxy alkyl group Chemical group 0.000 claims description 3
VEQOALNAAJBPNY-UHFFFAOYSA-N antipyrine Chemical compound CN1C(C)=CC(=O)N1C1=CC=CC=C1 VEQOALNAAJBPNY-UHFFFAOYSA-N 0.000 claims description 3
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WOIIIUDZSOLAIW-NSHDSACASA-N azapropazone Chemical compound C1=C(C)C=C2N3C(=O)[C@H](CC=C)C(=O)N3C(N(C)C)=NC2=C1 WOIIIUDZSOLAIW-NSHDSACASA-N 0.000 claims description 3
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FEJKLNWAOXSSNR-UHFFFAOYSA-N benorilate Chemical compound C1=CC(NC(=O)C)=CC=C1OC(=O)C1=CC=CC=C1OC(C)=O FEJKLNWAOXSSNR-UHFFFAOYSA-N 0.000 claims description 3
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SYTBZMRGLBWNTM-UHFFFAOYSA-N flurbiprofen Chemical compound FC1=CC(C(C(O)=O)C)=CC=C1C1=CC=CC=C1 SYTBZMRGLBWNTM-UHFFFAOYSA-N 0.000 claims description 3
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239000011975 tartaric acid Substances 0.000 description 1
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IWVCMVBTMGNXQD-UHFFFAOYSA-N terramycin dehydrate Natural products C1=CC=C2C(O)(C)C3C(O)C4C(N(C)C)C(O)=C(C(N)=O)C(=O)C4(O)C(O)=C3C(=O)C2=C1O IWVCMVBTMGNXQD-UHFFFAOYSA-N 0.000 description 1
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125000001113 thiadiazolyl group Chemical group 0.000 description 1
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OTVAEFIXJLOWRX-NXEZZACHSA-N thiamphenicol Chemical compound CS(=O)(=O)C1=CC=C([C@@H](O)[C@@H](CO)NC(=O)C(Cl)Cl)C=C1 OTVAEFIXJLOWRX-NXEZZACHSA-N 0.000 description 1
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NLVFBUXFDBBNBW-PBSUHMDJSA-N tobramycin Chemical compound N[C@@H]1C[C@H](O)[C@@H](CN)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O[C@@H]2[C@@H]([C@@H](N)[C@H](O)[C@@H](CO)O2)O)[C@H](N)C[C@@H]1N NLVFBUXFDBBNBW-PBSUHMDJSA-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
- A61K31/395—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
- A61K31/403—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 condensed with carbocyclic rings, e.g. carbazole
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/5415—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

Health & Medical Sciences (AREA)
Pharmacology & Pharmacy (AREA)
Veterinary Medicine (AREA)
Chemical & Material Sciences (AREA)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Animal Behavior & Ethology (AREA)
Life Sciences & Earth Sciences (AREA)
Epidemiology (AREA)
Organic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Steroid Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

UA20041210349A 2002-05-17 2003-05-16 Anelated pyrrol substances as proton pump inhibitors for treating gastric ulcer UA77812C2 (en)

Applications Claiming Priority (2)

Application Number	Priority Date	Filing Date	Title
EP02011081		2002-05-17
PCT/EP2003/005171 WO2003097041A1 (en)	2002-05-17	2003-05-16	Annelated pyrrole compounds as proton pump inhibitors for treating ulcer

Publications (1)

Publication Number	Publication Date
UA77812C2 true UA77812C2 (en)	2007-01-15

Family

ID=37725454

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
UA20041210349A UA77812C2 (en)	2002-05-17	2003-05-16	Anelated pyrrol substances as proton pump inhibitors for treating gastric ulcer

Country Status (15)

Country	Link
EP (1)	EP1505964B1 (pt)
JP (1)	JP2006509720A (pt)
CN (1)	CN1309383C (pt)
AU (1)	AU2003232788B2 (pt)
BR (1)	BR0310068A (pt)
CA (1)	CA2484238A1 (pt)
DE (1)	DE60317661T2 (pt)
ES (1)	ES2297204T3 (pt)
MX (1)	MXPA04011097A (pt)
NZ (1)	NZ536444A (pt)
PT (1)	PT1505964E (pt)
RU (1)	RU2336872C2 (pt)
UA (1)	UA77812C2 (pt)
WO (1)	WO2003097041A1 (pt)
ZA (1)	ZA200410123B (pt)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
DE10351035A1 (de) *	2003-10-31	2005-05-25	Merckle Gmbh Chemisch Pharmazeutische Fabrik	Pharmazeutische Licofelone-Formulierung
PE20070540A1 (es) *	2005-08-30	2007-06-26	Takeda Pharmaceutical	Derivados de pirrol como inhibidores de la secrecion acida
WO2007072503A2 (en) *	2005-12-21	2007-06-28	Panacea Biotec Ltd.	Combinations for managing inflammation and associated disorders
ES2534772T3 (es)	2008-10-31	2015-04-28	C-A-I-R Biosciences Gmbh	Sal de colina y trometamina de licofelona
CN104447490B (zh) *	2014-11-19	2017-06-06	连云港恒运医药有限公司	一种质子泵抑制剂的晶型、制备中间体及其合成方法和医药用途
CN113549079A (zh)	2018-05-25	2021-10-26	正大天晴药业集团股份有限公司	2,3-二氢-1h-吡咯嗪-7-甲酰胺类衍生物及其应用

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DE4419246A1 (de) *	1994-06-01	1995-12-07	Merckle Gmbh	Heteroarylsubstituierte Pyrrolizinverbindungen und deren Anwendung in der Pharmazie
DE4419247A1 (de) *	1994-06-01	1995-12-07	Merckle Gmbh	Sulfonylierte Pyrrolizincarbonsäureamide und deren Anwendung in der Pharmazie
SE9500478D0 (sv) *	1995-02-09	1995-02-09	Astra Ab	New pharmaceutical formulation and process
ES2247604T3 (es) *	1995-06-12	2006-03-01	G.D. SEARLE & CO.	Composiciones que comprenden un inhibidor de ciclooxigenasa-2 y un inhibidor de 5-lipoxigenasa.
US5852033A (en) *	1995-06-29	1998-12-22	Pharma Mar, S.A.	Methods of treatment using lamellarin-class alkaloids
KR100447918B1 (ko) *	1996-07-25	2005-09-28	동아제약주식회사	대장을포함한위장관보호작용을갖는플라본및플라바논화합물
HUP0204336A3 (en) *	1999-11-23	2006-01-30	Merckle Gmbh	Anti-inflammatory oxo derivatives and hydroxy derivatives of pyrrolizines, and their pharmaceutical use and pharmaceutical compositions containing them their
EP1142889A1 (en) *	2000-04-03	2001-10-10	Pfizer Products Inc.	Pyrazole derivatives as anti-inflammatory/analgesic agents

2003
- 2003-05-16 PT PT03752754T patent/PT1505964E/pt unknown
- 2003-05-16 BR BR0310068-5A patent/BR0310068A/pt not_active IP Right Cessation
- 2003-05-16 NZ NZ536444A patent/NZ536444A/en unknown
- 2003-05-16 EP EP03752754A patent/EP1505964B1/en not_active Expired - Lifetime
- 2003-05-16 DE DE60317661T patent/DE60317661T2/de not_active Expired - Fee Related
- 2003-05-16 CN CNB038112469A patent/CN1309383C/zh not_active Expired - Fee Related
- 2003-05-16 RU RU2004136994/15A patent/RU2336872C2/ru not_active IP Right Cessation
- 2003-05-16 WO PCT/EP2003/005171 patent/WO2003097041A1/en not_active Ceased
- 2003-05-16 UA UA20041210349A patent/UA77812C2/uk unknown
- 2003-05-16 CA CA002484238A patent/CA2484238A1/en not_active Abandoned
- 2003-05-16 MX MXPA04011097A patent/MXPA04011097A/es active IP Right Grant
- 2003-05-16 AU AU2003232788A patent/AU2003232788B2/en not_active Ceased
- 2003-05-16 JP JP2004505040A patent/JP2006509720A/ja active Pending
- 2003-05-16 ES ES03752754T patent/ES2297204T3/es not_active Expired - Lifetime
2004
- 2004-12-15 ZA ZA200410123A patent/ZA200410123B/en unknown

Also Published As

Publication number	Publication date
AU2003232788A1 (en)	2003-12-02
JP2006509720A (ja)	2006-03-23
ES2297204T3 (es)	2008-05-01
DE60317661T2 (de)	2008-10-30
RU2336872C2 (ru)	2008-10-27
PT1505964E (pt)	2008-02-28
ZA200410123B (en)	2006-07-26
CA2484238A1 (en)	2003-11-27
WO2003097041A1 (en)	2003-11-27
AU2003232788B2 (en)	2008-10-02
EP1505964A1 (en)	2005-02-16
CN1309383C (zh)	2007-04-11
NZ536444A (en)	2006-12-22
RU2004136994A (ru)	2005-06-10
MXPA04011097A (es)	2005-02-14
CN1652771A (zh)	2005-08-10
EP1505964B1 (en)	2007-11-21
BR0310068A (pt)	2005-03-08
DE60317661D1 (de)	2008-01-03

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Sachs et al.	2010	Novel approaches to inhibition of gastric acid secretion
Patrignani et al.	2011	Managing the adverse effects of nonsteroidal anti-inflammatory drugs
RU2252032C2 (ru)	2005-05-20	Новое применение соединений в качестве антибактериальных средств
Fock et al.	2008	Proton pump inhibitors: do differences in pharmacokinetics translate into differences in clinical outcomes?
US20080255209A1 (en)	2008-10-16	Combination of a NSAID and a PDE-4 inhibitor
CN1178648C (zh)	2004-12-08	H+ 、k+ －atp酶抑制剂在制备用于增强抑制胃酸分泌的口服药物中的用途
JP2009540014A (ja)	2009-11-19	胃障害を処置または予防するためのテガセロドを単独でまたはプロトンポンプ阻害剤と組合せて含む組成物
EP1365806A2 (en)	2003-12-03	Use of no acttivators for treatment and prevention of gastrointestinal disorders
TW201002311A (en)	2010-01-16	Novel compositions and methods for treating hyperproliferative diseases
ES2996895T3 (en)	2025-02-13	Pharmaceutical composition comprising antiplatelet agent and gastric acid secretion inhibitor
TW201136916A (en)	2011-11-01	New uses
Dajani et al.	2000	Novel therapeutic approaches to gastric and duodenal ulcers: an update
JP2003521511A (ja)	2003-07-15	便秘のためのｃｏｘ−２阻害剤の使用
UA77812C2 (en)	2007-01-15	Anelated pyrrol substances as proton pump inhibitors for treating gastric ulcer
US20060040945A1 (en)	2006-02-23	Annellated pyrrole compounds as proton pump inhibitors for treating ulcer
US7271146B2 (en)	2007-09-18	Methods for treatment of Helicobacter pylori-associated disorders
JP2005145894A (ja)	2005-06-09	固形製剤
WO2005074930A1 (en)	2005-08-18	Pharmaceutical combinations of (s) -pantoprazole with nsaid or corticosteroids
McCormack	1999	The evolving NSAID: focus on lornoxicam
WO2009114516A1 (en)	2009-09-17	Therapy for disorders of the proximal digestive tract
WO2002053099A2 (en)	2002-07-11	Methods and compositions for treating periodontal disease
AU2002246757A1 (en)	2003-01-23	Methods and compositions for treating periodontal disease
HK1072379B (en)	2008-05-09	Annelated pyrrole compounds as proton pump inhibitors for treating ulcer
ULC	2018	Esomeprazole Magnesium Delayed Release Tablets 20 and 40 mg esomeprazole (as esomeprazole magnesium)