OA12078A - Method for administering a phosphodiesterase 4 inhibitor. - Google Patents

Method for administering a phosphodiesterase 4 inhibitor. Download PDF

Info

Publication number: OA12078A
Authority: OA; OAPI
Prior art keywords: drug; administered; formulation; side effects; release
Prior art date: 1999-10-29

Application number

OA1200200126A

Other languages

English (en)

Inventor

Robert D Murdoch

Theodore J Torphy

Barry D Zussman

Original Assignee

Smithkline Beecham Corp

Smithkline Beecham Plc

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.)

1999-10-29

Filing date

2000-10-26

Publication date

2003-05-28

2000-10-26 Application filed by Smithkline Beecham Corp, Smithkline Beecham Plc filed Critical Smithkline Beecham Corp

2003-05-28 Publication of OA12078A publication Critical patent/OA12078A/en

Links

238000000034 method Methods 0.000 title claims abstract description 26
229940123932 Phosphodiesterase 4 inhibitor Drugs 0.000 title abstract description 10
239000002587 phosphodiesterase IV inhibitor Substances 0.000 title abstract description 10
230000036470 plasma concentration Effects 0.000 claims abstract description 31
229940079593 drug Drugs 0.000 claims description 94
239000003814 drug Substances 0.000 claims description 94
239000000203 mixture Substances 0.000 claims description 57
238000009472 formulation Methods 0.000 claims description 54
230000000694 effects Effects 0.000 claims description 39
238000013270 controlled release Methods 0.000 claims description 20
239000000546 pharmaceutical excipient Substances 0.000 claims description 9
238000011282 treatment Methods 0.000 claims description 7
230000001934 delay Effects 0.000 claims description 5
JVTIXNMXDLQEJE-UHFFFAOYSA-N 2-decanoyloxypropyl decanoate 2-octanoyloxypropyl octanoate Chemical compound C(CCCCCCC)(=O)OCC(C)OC(CCCCCCC)=O.C(=O)(CCCCCCCCC)OCC(C)OC(=O)CCCCCCCCC JVTIXNMXDLQEJE-UHFFFAOYSA-N 0.000 claims description 4
WLAMNBDJUVNPJU-UHFFFAOYSA-N 2-methylbutyric acid Chemical compound CCC(C)C(O)=O WLAMNBDJUVNPJU-UHFFFAOYSA-N 0.000 claims description 4
208000006673 asthma Diseases 0.000 claims description 4
208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 3
238000004519 manufacturing process Methods 0.000 claims description 3
229940002612 prodrug Drugs 0.000 claims description 3
239000000651 prodrug Substances 0.000 claims description 3
MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical compound FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 claims description 3
150000002148 esters Chemical class 0.000 claims description 2
229960002586 roflumilast Drugs 0.000 claims description 2
101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 claims 3
101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 claims 3
SGPGESCZOCHFCL-UHFFFAOYSA-N Tilisolol hydrochloride Chemical compound [Cl-].C1=CC=C2C(=O)N(C)C=C(OCC(O)C[NH2+]C(C)(C)C)C2=C1 SGPGESCZOCHFCL-UHFFFAOYSA-N 0.000 claims 1
238000010521 absorption reaction Methods 0.000 abstract description 17
239000003112 inhibitor Substances 0.000 abstract description 11
239000003826 tablet Substances 0.000 description 40
CFBUZOUXXHZCFB-OYOVHJISSA-N chembl511115 Chemical compound COC1=CC=C([C@@]2(CC[C@H](CC2)C(O)=O)C#N)C=C1OC1CCCC1 CFBUZOUXXHZCFB-OYOVHJISSA-N 0.000 description 26
229920002125 Sokalan® Polymers 0.000 description 20
150000001875 compounds Chemical class 0.000 description 13
239000012729 immediate-release (IR) formulation Substances 0.000 description 13
230000002411 adverse Effects 0.000 description 12
229940068196 placebo Drugs 0.000 description 12
239000000902 placebo Substances 0.000 description 12
NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 description 11
108010044467 Isoenzymes Proteins 0.000 description 10
229960001631 carbomer Drugs 0.000 description 9
206010028813 Nausea Diseases 0.000 description 8
238000004090 dissolution Methods 0.000 description 8
230000008693 nausea Effects 0.000 description 8
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 7
206010047700 Vomiting Diseases 0.000 description 6
238000013459 approach Methods 0.000 description 6
201000010099 disease Diseases 0.000 description 6
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
238000005516 engineering process Methods 0.000 description 6
230000002829 reductive effect Effects 0.000 description 6
ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 description 6
FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 description 5
230000006872 improvement Effects 0.000 description 5
230000002401 inhibitory effect Effects 0.000 description 5
230000008569 process Effects 0.000 description 5
230000001225 therapeutic effect Effects 0.000 description 5
239000002775 capsule Substances 0.000 description 4
239000000306 component Substances 0.000 description 4
230000003247 decreasing effect Effects 0.000 description 4
230000003111 delayed effect Effects 0.000 description 4
239000008213 purified water Substances 0.000 description 4
239000007787 solid Substances 0.000 description 4
210000001519 tissue Anatomy 0.000 description 4
230000008673 vomiting Effects 0.000 description 4
ZOOGRGPOEVQQDX-UUOKFMHZSA-N 3',5'-cyclic GMP Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=C(NC2=O)N)=C2N=C1 ZOOGRGPOEVQQDX-UUOKFMHZSA-N 0.000 description 3
102000004190 Enzymes Human genes 0.000 description 3
108090000790 Enzymes Proteins 0.000 description 3
102000004861 Phosphoric Diester Hydrolases Human genes 0.000 description 3
108090001050 Phosphoric Diester Hydrolases Proteins 0.000 description 3
235000021152 breakfast Nutrition 0.000 description 3
ZOOGRGPOEVQQDX-UHFFFAOYSA-N cyclic GMP Natural products O1C2COP(O)(=O)OC2C(O)C1N1C=NC2=C1NC(N)=NC2=O ZOOGRGPOEVQQDX-UHFFFAOYSA-N 0.000 description 3
208000002173 dizziness Diseases 0.000 description 3
201000006549 dyspepsia Diseases 0.000 description 3
235000013601 eggs Nutrition 0.000 description 3
235000012054 meals Nutrition 0.000 description 3
239000007935 oral tablet Substances 0.000 description 3
229940096978 oral tablet Drugs 0.000 description 3
239000000047 product Substances 0.000 description 3
239000000725 suspension Substances 0.000 description 3
230000009885 systemic effect Effects 0.000 description 3
229960000278 theophylline Drugs 0.000 description 3
208000004998 Abdominal Pain Diseases 0.000 description 2
206010019233 Headaches Diseases 0.000 description 2
206010061218 Inflammation Diseases 0.000 description 2
208000005314 Multi-Infarct Dementia Diseases 0.000 description 2
244000061456 Solanum tuberosum Species 0.000 description 2
235000002595 Solanum tuberosum Nutrition 0.000 description 2
201000004810 Vascular dementia Diseases 0.000 description 2
239000002253 acid Substances 0.000 description 2
238000007792 addition Methods 0.000 description 2
OIRDTQYFTABQOQ-KQYNXXCUSA-N adenosine Chemical compound C1=NC=2C(N)=NC=NC=2N1[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O OIRDTQYFTABQOQ-KQYNXXCUSA-N 0.000 description 2
210000005091 airway smooth muscle Anatomy 0.000 description 2
235000015241 bacon Nutrition 0.000 description 2
235000014121 butter Nutrition 0.000 description 2
FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 2
210000004027 cell Anatomy 0.000 description 2
210000003169 central nervous system Anatomy 0.000 description 2
239000011248 coating agent Substances 0.000 description 2
238000000576 coating method Methods 0.000 description 2
239000000599 controlled substance Substances 0.000 description 2
239000006071 cream Substances 0.000 description 2
235000019700 dicalcium phosphate Nutrition 0.000 description 2
229940095079 dicalcium phosphate anhydrous Drugs 0.000 description 2
KYFWUBJMTHVBIF-QFIPXVFZSA-N dsstox_cid_27248 Chemical compound N([C@@H]1N=C(C=2C=3N(C1=O)CCC=3C=C(C=2)C)C=1C=CC=CC=1)C(=O)C1=CC=NC=C1 KYFWUBJMTHVBIF-QFIPXVFZSA-N 0.000 description 2
239000012467 final product Substances 0.000 description 2
235000013305 food Nutrition 0.000 description 2
231100000869 headache Toxicity 0.000 description 2
208000024798 heartburn Diseases 0.000 description 2
210000002865 immune cell Anatomy 0.000 description 2
238000000338 in vitro Methods 0.000 description 2
210000004969 inflammatory cell Anatomy 0.000 description 2
230000004054 inflammatory process Effects 0.000 description 2
230000005764 inhibitory process Effects 0.000 description 2
239000000463 material Substances 0.000 description 2
239000011159 matrix material Substances 0.000 description 2
230000007246 mechanism Effects 0.000 description 2
238000002156 mixing Methods 0.000 description 2
239000002674 ointment Substances 0.000 description 2
235000012015 potatoes Nutrition 0.000 description 2
208000024981 pyrosis Diseases 0.000 description 2
150000003839 salts Chemical class 0.000 description 2
230000002459 sustained effect Effects 0.000 description 2
231100001274 therapeutic index Toxicity 0.000 description 2
238000004448 titration Methods 0.000 description 2
FTNJQNQLEGKTGD-UHFFFAOYSA-N 1,3-benzodioxole Chemical compound C1=CC=C2OCOC2=C1 FTNJQNQLEGKTGD-UHFFFAOYSA-N 0.000 description 1
HJPRDDKCXVCFOH-UHFFFAOYSA-N 1,3-dibutyl-7-(2-oxopropyl)purine-2,6-dione Chemical compound O=C1N(CCCC)C(=O)N(CCCC)C2=C1N(CC(C)=O)C=N2 HJPRDDKCXVCFOH-UHFFFAOYSA-N 0.000 description 1
SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
MSYGAHOHLUJIKV-UHFFFAOYSA-N 3,5-dimethyl-1-(3-nitrophenyl)-1h-pyrazole-4-carboxylic acid ethyl ester Chemical compound CC1=C(C(=O)OCC)C(C)=NN1C1=CC=CC([N+]([O-])=O)=C1 MSYGAHOHLUJIKV-UHFFFAOYSA-N 0.000 description 1
MRHCSNNEUHXNIC-UHFFFAOYSA-N 9-benzylpurin-6-amine Chemical compound C1=NC=2C(N)=NC=NC=2N1CC1=CC=CC=C1 MRHCSNNEUHXNIC-UHFFFAOYSA-N 0.000 description 1
208000008035 Back Pain Diseases 0.000 description 1
239000002126 C01EB10 - Adenosine Substances 0.000 description 1
101100296719 Caenorhabditis elegans pde-4 gene Proteins 0.000 description 1
206010008531 Chills Diseases 0.000 description 1
241001023573 Geothlypis philadelphia Species 0.000 description 1
208000022559 Inflammatory bowel disease Diseases 0.000 description 1
GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
229920000168 Microcrystalline cellulose Polymers 0.000 description 1
208000011623 Obstructive Lung disease Diseases 0.000 description 1
229910019142 PO4 Inorganic materials 0.000 description 1
229940099471 Phosphodiesterase inhibitor Drugs 0.000 description 1
244000269722 Thea sinensis Species 0.000 description 1
108060008682 Tumor Necrosis Factor Proteins 0.000 description 1
102000011017 Type 4 Cyclic Nucleotide Phosphodiesterases Human genes 0.000 description 1
108010037584 Type 4 Cyclic Nucleotide Phosphodiesterases Proteins 0.000 description 1
150000001253 acrylic acids Chemical class 0.000 description 1
230000009471 action Effects 0.000 description 1
229960005305 adenosine Drugs 0.000 description 1
-1 allyl ethers Chemical class 0.000 description 1
229940086737 allyl sucrose Drugs 0.000 description 1
238000004458 analytical method Methods 0.000 description 1
229940069428 antacid Drugs 0.000 description 1
239000003159 antacid agent Substances 0.000 description 1
230000001430 anti-depressive effect Effects 0.000 description 1
230000003110 anti-inflammatory effect Effects 0.000 description 1
239000000935 antidepressant agent Substances 0.000 description 1
229940005513 antidepressants Drugs 0.000 description 1
230000004888 barrier function Effects 0.000 description 1
230000008901 benefit Effects 0.000 description 1
239000011230 binding agent Substances 0.000 description 1
239000008280 blood Substances 0.000 description 1
210000004369 blood Anatomy 0.000 description 1
230000007883 bronchodilation Effects 0.000 description 1
229940124630 bronchodilator Drugs 0.000 description 1
239000000168 bronchodilator agent Substances 0.000 description 1
239000011575 calcium Substances 0.000 description 1
229940082484 carbomer-934 Drugs 0.000 description 1
125000002843 carboxylic acid group Chemical group 0.000 description 1
229940096529 carboxypolymethylene Drugs 0.000 description 1
235000013351 cheese Nutrition 0.000 description 1
238000006243 chemical reaction Methods 0.000 description 1
230000007278 cognition impairment Effects 0.000 description 1
208000010877 cognitive disease Diseases 0.000 description 1
238000007906 compression Methods 0.000 description 1
230000006835 compression Effects 0.000 description 1
239000008358 core component Substances 0.000 description 1
238000004132 cross linking Methods 0.000 description 1
230000009260 cross reactivity Effects 0.000 description 1
125000004122 cyclic group Chemical group 0.000 description 1
229950004687 denbufylline Drugs 0.000 description 1
230000001419 dependent effect Effects 0.000 description 1
239000007933 dermal patch Substances 0.000 description 1
238000009826 distribution Methods 0.000 description 1
238000012377 drug delivery Methods 0.000 description 1
235000013399 edible fruits Nutrition 0.000 description 1
235000019197 fats Nutrition 0.000 description 1
230000009246 food effect Effects 0.000 description 1
230000002496 gastric effect Effects 0.000 description 1
229920006158 high molecular weight polymer Polymers 0.000 description 1
239000012728 immediate-release (IR) tablet Substances 0.000 description 1
238000001802 infusion Methods 0.000 description 1
239000007924 injection Substances 0.000 description 1
238000002347 injection Methods 0.000 description 1
230000003834 intracellular effect Effects 0.000 description 1
239000007927 intramuscular injection Substances 0.000 description 1
238000010255 intramuscular injection Methods 0.000 description 1
239000007928 intraperitoneal injection Substances 0.000 description 1
239000003456 ion exchange resin Substances 0.000 description 1
229920003303 ion-exchange polymer Polymers 0.000 description 1
239000008101 lactose Substances 0.000 description 1
230000000670 limiting effect Effects 0.000 description 1
239000007788 liquid Substances 0.000 description 1
229940016286 microcrystalline cellulose Drugs 0.000 description 1
235000019813 microcrystalline cellulose Nutrition 0.000 description 1
239000008108 microcrystalline cellulose Substances 0.000 description 1
235000013336 milk Nutrition 0.000 description 1
239000008267 milk Substances 0.000 description 1
210000004080 milk Anatomy 0.000 description 1
239000012740 non-selective inhibitor Substances 0.000 description 1
230000003204 osmotic effect Effects 0.000 description 1
WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 1
NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
239000010452 phosphate Substances 0.000 description 1
229920000642 polymer Polymers 0.000 description 1
239000002243 precursor Substances 0.000 description 1
230000002035 prolonged effect Effects 0.000 description 1
108090000623 proteins and genes Proteins 0.000 description 1
230000000506 psychotropic effect Effects 0.000 description 1
206010039073 rheumatoid arthritis Diseases 0.000 description 1
HJORMJIFDVBMOB-UHFFFAOYSA-N rolipram Chemical compound COC1=CC=C(C2CC(=O)NC2)C=C1OC1CCCC1 HJORMJIFDVBMOB-UHFFFAOYSA-N 0.000 description 1
229950005741 rolipram Drugs 0.000 description 1
230000009291 secondary effect Effects 0.000 description 1
230000000391 smoking effect Effects 0.000 description 1
239000000126 substance Substances 0.000 description 1
239000000829 suppository Substances 0.000 description 1
238000004885 tandem mass spectrometry Methods 0.000 description 1
238000002560 therapeutic procedure Methods 0.000 description 1
230000000699 topical effect Effects 0.000 description 1
102000003390 tumor necrosis factor Human genes 0.000 description 1
230000003442 weekly effect Effects 0.000 description 1

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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/192—Carboxylic acids, e.g. valproic acid having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
- 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
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- 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
- A61K31/74—Synthetic polymeric materials
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/2027—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
- 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
- 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]
- 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

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Public Health (AREA)
Medicinal Chemistry (AREA)
General Health & Medical Sciences (AREA)
Animal Behavior & Ethology (AREA)
Pharmacology & Pharmacy (AREA)
Epidemiology (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Engineering & Computer Science (AREA)
Bioinformatics & Cheminformatics (AREA)
Pulmonology (AREA)
Inorganic Chemistry (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Psychiatry (AREA)
Hospice & Palliative Care (AREA)
Rheumatology (AREA)
Pain & Pain Management (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Medicinal Preparation (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Enzymes And Modification Thereof (AREA)

OA1200200126A 1999-10-29 2000-10-26 Method for administering a phosphodiesterase 4 inhibitor. OA12078A (en)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date
US16247799P	1999-10-29	1999-10-29
US16264199P	1999-11-01	1999-11-01
US17981700P	2000-02-02	2000-02-02

Publications (1)

Publication Number	Publication Date
OA12078A true OA12078A (en)	2003-05-28

Family

ID=27388757

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
OA1200200126A OA12078A (en)	1999-10-29	2000-10-26	Method for administering a phosphodiesterase 4 inhibitor.

Country Status (29)

Country	Link
US (1)	US20030212112A1 (fr)
EP (1)	EP1225884A4 (fr)
JP (1)	JP2003513038A (fr)
KR (1)	KR20020050249A (fr)
CN (1)	CN1387433A (fr)
AP (1)	AP2002002446A0 (fr)
AR (1)	AR026254A1 (fr)
AU (1)	AU772909B2 (fr)
BG (1)	BG106623A (fr)
BR (1)	BR0015039A (fr)
CA (1)	CA2389293A1 (fr)
CO (1)	CO5271676A1 (fr)
CZ (1)	CZ20021443A3 (fr)
DZ (1)	DZ3249A1 (fr)
EA (1)	EA200200502A1 (fr)
HK (1)	HK1049105A1 (fr)
HU (1)	HUP0203682A3 (fr)
IL (1)	IL148813A0 (fr)
MA (1)	MA25562A1 (fr)
MX (1)	MXPA02004220A (fr)
NO (1)	NO20021937L (fr)
NZ (1)	NZ518002A (fr)
OA (1)	OA12078A (fr)
PE (1)	PE20011004A1 (fr)
PL (1)	PL355262A1 (fr)
SK (1)	SK7292002A3 (fr)
TR (1)	TR200201150T2 (fr)
UY (1)	UY26422A1 (fr)
WO (1)	WO2001032165A1 (fr)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
AR029984A1 (es) *	2000-07-27	2003-07-23	Smithkline Beecham Corp	Metodo para reducir las exacerbaciones asociadas copd ambito
DE10207160A1 (de) *	2002-02-20	2003-12-18	Altana Pharma Ag	Darreichungsform enthaltend PDE 4-Hemmer als Wirkstoff
MY140561A (en)	2002-02-20	2009-12-31	Nycomed Gmbh	Dosage form containing pde 4 inhibitor as active ingredient
US20060084684A1 (en) *	2002-05-28	2006-04-20	Altana Pharma Ag	Topically applicable pharmaceutical preparation
US6822114B1 (en)	2002-10-08	2004-11-23	Albemarle Corporation	Process for production of fluoroalkoxy-substituted benzamides and their intermediates
SI1606261T1 (sl)	2003-03-10	2010-03-31	Nycomed Gmbh	Novi postopek za pripravo roflumilasta
EP1634606A1 (fr) *	2003-03-31	2006-03-15	Kyowa Hakko Kogyo Co., Ltd.	Medicament administre par voie orale
US20050026883A1 (en) *	2003-07-31	2005-02-03	Robinson Cynthia B.	Combination of dehydroepiandrosterone or dehydroepiandrosterone-sulfate with a PDE-4 inhibitor for treatment of asthma or chronic obstructive pulmonary disease
US8663694B2 (en)	2005-03-16	2014-03-04	Takeda Gmbh	Taste masked dosage form containing roflumilast
EP2506711B1 (fr) *	2009-12-03	2019-04-03	OPKO Health, Inc.	Formulations de disaccharides hypersulfatés
BR112014015923B1 (pt) *	2011-12-27	2022-02-01	Amgen (Europe) GmbH	Comprimidos revestidos de (+)-2-[1-(3-etoxi-4-metoxi-fenil)-2-metano-sulfoniletil]-4 - acetilaminoisoindolina-1,3-diona
CN103536582A (zh) *	2013-10-12	2014-01-29	云南龙海天然植物药业有限公司	罗氟司特干粉吸入剂
WO2019147824A1 (fr)	2018-01-26	2019-08-01	Progenity, Inc.	Traitement d'une maladie du tractus gastro-intestinal avec un inhibiteur de pde4
CN116726361A (zh)	2018-11-19	2023-09-12	比奥拉治疗股份有限公司	用生物治疗剂治疗疾病的方法和装置
WO2021119482A1 (fr)	2019-12-13	2021-06-17	Progenity, Inc.	Dispositif ingérable pour administrer un agent thérapeutique dans le tractus gastro-intestinal

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4684516A (en) *	1983-08-01	1987-08-04	Alra Laboratories, Inc.	Sustained release tablets and method of making same
AR028986A1 (es) *	1999-02-23	2003-06-04	Smithkline Beecham Corp	USO DE UN INHIBIDOR DE PDE4 EN LA FABRICACIoN DE UNA PREPARACIoN DE LIBERACIoN CONTROLADA; FORMULACION DE LIBERACION CONTROLADA PARA EL TRATAMIENTO DE COPD, UN PROCEDIMIENTO PARA SU PREPARACIoN Y COMPOSICIoN FARMACÉUTICA
AR035987A1 (es) *	1999-03-01	2004-08-04	Smithkline Beecham Corp	Uso de un compuesto inhibidor de la pde 4 para la manufactura de un medicamento y el medicamento para tratar asma inducida por ejercicio

2000
- 2000-10-26 SK SK729-2002A patent/SK7292002A3/sk unknown
- 2000-10-26 DZ DZ003249A patent/DZ3249A1/fr active
- 2000-10-26 HU HU0203682A patent/HUP0203682A3/hu unknown
- 2000-10-26 AU AU13445/01A patent/AU772909B2/en not_active Ceased
- 2000-10-26 MX MXPA02004220A patent/MXPA02004220A/es unknown
- 2000-10-26 KR KR1020027005448A patent/KR20020050249A/ko not_active Withdrawn
- 2000-10-26 EA EA200200502A patent/EA200200502A1/ru unknown
- 2000-10-26 AP APAP/P/2002/002446A patent/AP2002002446A0/en unknown
- 2000-10-26 CZ CZ20021443A patent/CZ20021443A3/cs unknown
- 2000-10-26 CA CA002389293A patent/CA2389293A1/fr not_active Abandoned
- 2000-10-26 JP JP2001534370A patent/JP2003513038A/ja not_active Withdrawn
- 2000-10-26 WO PCT/US2000/029453 patent/WO2001032165A1/fr not_active Ceased
- 2000-10-26 CO CO00081570A patent/CO5271676A1/es not_active Application Discontinuation
- 2000-10-26 TR TR2002/01150T patent/TR200201150T2/xx unknown
- 2000-10-26 HK HK02109231.8A patent/HK1049105A1/zh unknown
- 2000-10-26 NZ NZ518002A patent/NZ518002A/en unknown
- 2000-10-26 BR BR0015039-8A patent/BR0015039A/pt not_active IP Right Cessation
- 2000-10-26 IL IL14881300A patent/IL148813A0/xx unknown
- 2000-10-26 OA OA1200200126A patent/OA12078A/en unknown
- 2000-10-26 CN CN00815150A patent/CN1387433A/zh active Pending
- 2000-10-26 PL PL00355262A patent/PL355262A1/xx unknown
- 2000-10-26 EP EP00975385A patent/EP1225884A4/fr not_active Withdrawn
- 2000-10-26 AR ARP000105644A patent/AR026254A1/es not_active Application Discontinuation
- 2000-10-27 PE PE2000001157A patent/PE20011004A1/es not_active Application Discontinuation
- 2000-10-30 UY UY26422A patent/UY26422A1/es not_active Application Discontinuation
2002
- 2002-04-17 BG BG106623A patent/BG106623A/bg unknown
- 2002-04-24 NO NO20021937A patent/NO20021937L/no not_active Application Discontinuation
- 2002-04-26 MA MA26618A patent/MA25562A1/fr unknown
2003
- 2003-05-02 US US10/429,666 patent/US20030212112A1/en not_active Abandoned

Also Published As

Publication number	Publication date
WO2001032165A1 (fr)	2001-05-10
BG106623A (bg)	2003-02-28
PL355262A1 (en)	2004-04-05
AR026254A1 (es)	2003-02-05
MA25562A1 (fr)	2002-10-01
SK7292002A3 (en)	2002-12-03
PE20011004A1 (es)	2001-09-28
EP1225884A1 (fr)	2002-07-31
TR200201150T2 (tr)	2002-09-23
BR0015039A (pt)	2002-06-25
NO20021937D0 (no)	2002-04-24
JP2003513038A (ja)	2003-04-08
KR20020050249A (ko)	2002-06-26
HUP0203682A2 (hu)	2003-04-28
NO20021937L (no)	2002-05-30
IL148813A0 (en)	2002-09-12
HK1049105A1 (zh)	2003-05-02
EA200200502A1 (ru)	2002-10-31
AP2002002446A0 (en)	2002-03-31
AU1344501A (en)	2001-05-14
HUP0203682A3 (en)	2003-10-28
DZ3249A1 (fr)	2001-05-10
MXPA02004220A (es)	2002-10-17
CN1387433A (zh)	2002-12-25
CA2389293A1 (fr)	2001-05-10
CZ20021443A3 (cs)	2003-01-15
NZ518002A (en)	2004-01-30
AU772909B2 (en)	2004-05-13
US20030212112A1 (en)	2003-11-13
CO5271676A1 (es)	2003-04-30
EP1225884A4 (fr)	2005-06-15
UY26422A1 (es)	2001-07-31

Publication	Publication Date	Title
OA12078A (en)	2003-05-28	Method for administering a phosphodiesterase 4 inhibitor.
US6511985B1 (en)	2003-01-28	Combination of cerivastatin and fibrates
JP6174666B2 (ja)	2017-08-02	ナルトレキソンの徐放型配合物
TWI224013B (en)	2004-11-21	Controlled release formulation for treating COPD
US20040005995A1 (en)	2004-01-08	Method for reducing exacerbations associated with copd
AU2001279023B2 (en)	2005-11-10	Method for reducing exacerbations associated with COPD
JPH0141608B2 (fr)	1989-09-06
AU2001279023A1 (en)	2002-05-09	Method for reducing exacerbations associated with COPD
Bays	2004	Extended-release niacin/lovastatin: the first combination product for dyslipidemia
Kelly et al.	1989	Pharmacokinetic properties and clinical efficacy of once-daily sustained-release naproxen
ZA200203349B (en)	2003-04-29	Method for administering a phosphodiesterase 4 inhibitor.
JP2016514125A (ja)	2016-05-19	バルサルタン及びロスバスタチンカルシウムを含む複合製剤及びその製造方法
Awni et al.	1995	The influence of multiple oral doses of zileuton on the steady-state pharmacokinetics of sulfasalazine and its metabolites, sulfapyridine and N-acetylsulfapyridine
WO2020053218A1 (fr)	2020-03-19	Traitement du psoriasis
WO2020053219A1 (fr)	2020-03-19	Traitement du psoriasis
AU2004201503A1 (en)	2004-05-06	Controlled Release Formulation for Treating COPD
MXPA06014463A (es)	2008-11-26	Composicion farmaceutica que contiene una combinacion de antiespasmodico y analgesico y su uso.