ZA200609228B - Methods of using and compositions comprising PDE4 modulators for the treatment and management of pulmonary hypertension - Google Patents

Methods of using and compositions comprising PDE4 modulators for the treatment and management of pulmonary hypertension Download PDF

Info

Publication number: ZA200609228B
Authority: ZA; South Africa
Prior art keywords: carbon atoms; pulmonary hypertension; alkyl; pde4 modulator; solvate
Prior art date: 2004-04-23

Application number

ZA200609228A

Other languages

English (en)

Inventor

Jerome B Zeldis

Original Assignee

Celgene Corp

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.)

2004-04-23

Filing date

2005-04-21

Publication date

2008-05-28

2005-04-21 Application filed by Celgene Corp filed Critical Celgene Corp

2008-05-28 Publication of ZA200609228B publication Critical patent/ZA200609228B/en

Links

208000002815 pulmonary hypertension Diseases 0.000 title claims description 97
101100296720 Dictyostelium discoideum Pde4 gene Proteins 0.000 title claims description 75
101100082610 Plasmodium falciparum (isolate 3D7) PDEdelta gene Proteins 0.000 title claims description 75
238000000034 method Methods 0.000 title claims description 29
238000011282 treatment Methods 0.000 title claims description 9
239000000203 mixture Substances 0.000 title description 3
125000004432 carbon atom Chemical group C* 0.000 claims description 182
-1 carbethoxy, carbomethoxy, carbopropoxy, acetyl Chemical group 0.000 claims description 150
125000000217 alkyl group Chemical group 0.000 claims description 115
125000003545 alkoxy group Chemical group 0.000 claims description 61
125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims description 56
125000004093 cyano group Chemical group *C#N 0.000 claims description 52
125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 51
125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 51
239000001257 hydrogen Substances 0.000 claims description 45
229910052739 hydrogen Inorganic materials 0.000 claims description 45
125000001424 substituent group Chemical group 0.000 claims description 43
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 42
150000003839 salts Chemical class 0.000 claims description 37
239000012453 solvate Substances 0.000 claims description 36
239000013543 active substance Substances 0.000 claims description 26
206010064911 Pulmonary arterial hypertension Diseases 0.000 claims description 23
208000004248 Familial Primary Pulmonary Hypertension Diseases 0.000 claims description 22
150000002431 hydrogen Chemical class 0.000 claims description 22
125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 21
201000008312 primary pulmonary hypertension Diseases 0.000 claims description 21
239000003814 drug Substances 0.000 claims description 20
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 16
BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims description 14
125000003282 alkyl amino group Chemical group 0.000 claims description 13
238000002054 transplantation Methods 0.000 claims description 13
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LMHIPJMTZHDKEW-XQYLJSSYSA-M Epoprostenol sodium Chemical compound [Na+].O1\C(=C/CCCC([O-])=O)C[C@@H]2[C@@H](/C=C/[C@@H](O)CCCCC)[C@H](O)C[C@@H]21 LMHIPJMTZHDKEW-XQYLJSSYSA-M 0.000 claims description 9
GJPICJJJRGTNOD-UHFFFAOYSA-N bosentan Chemical compound COC1=CC=CC=C1OC(C(=NC(=N1)C=2N=CC=CN=2)OCCO)=C1NS(=O)(=O)C1=CC=C(C(C)(C)C)C=C1 GJPICJJJRGTNOD-UHFFFAOYSA-N 0.000 claims description 9
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KZJWDPNRJALLNS-VJSFXXLFSA-N sitosterol 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)CC[C@@H](CC)C(C)C)[C@@]1(C)CC2 KZJWDPNRJALLNS-VJSFXXLFSA-N 0.000 claims description 6
IMOZEMNVLZVGJZ-UHFFFAOYSA-N n-[2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-1,3-dioxoisoindol-4-yl]acetamide Chemical compound C1=C(OC)C(OCC)=CC(C(CS(C)(=O)=O)N2C(C3=C(NC(C)=O)C=CC=C3C2=O)=O)=C1 IMOZEMNVLZVGJZ-UHFFFAOYSA-N 0.000 claims description 5
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210000002345 respiratory system Anatomy 0.000 description 1
230000000284 resting effect Effects 0.000 description 1
230000037390 scarring Effects 0.000 description 1
125000002072 seryl group Chemical group 0.000 description 1
229940126586 small molecule drug Drugs 0.000 description 1
150000003384 small molecules Chemical class 0.000 description 1
210000002460 smooth muscle Anatomy 0.000 description 1
230000037439 somatic mutation Effects 0.000 description 1
238000011301 standard therapy Methods 0.000 description 1
PJANXHGTPQOBST-UHFFFAOYSA-N stilbene Chemical group C=1C=CC=CC=1C=CC1=CC=CC=C1 PJANXHGTPQOBST-UHFFFAOYSA-N 0.000 description 1
150000003440 styrenes Chemical class 0.000 description 1
239000000126 substance Substances 0.000 description 1
KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical class O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 description 1
229940124530 sulfonamide Drugs 0.000 description 1
150000003456 sulfonamides Chemical class 0.000 description 1
230000004083 survival effect Effects 0.000 description 1
230000002459 sustained effect Effects 0.000 description 1
206010042772 syncope Diseases 0.000 description 1
208000011580 syndromic disease Diseases 0.000 description 1
230000009885 systemic effect Effects 0.000 description 1
YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
125000001544 thienyl group Chemical group 0.000 description 1
125000001239 threonyl group Chemical group 0.000 description 1
125000002233 tyrosyl group Chemical group 0.000 description 1
125000002114 valyl group Chemical group 0.000 description 1
210000005166 vasculature Anatomy 0.000 description 1
229940094720 viagra Drugs 0.000 description 1
230000009385 viral infection Effects 0.000 description 1

Classifications

- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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
- A61K31/366—Lactones having six-membered rings, e.g. delta-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
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
- 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
- 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
- A61K31/4035—Isoindoles, e.g. phthalimide
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives

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

ZA200609228A 2004-04-23 2005-04-21 Methods of using and compositions comprising PDE4 modulators for the treatment and management of pulmonary hypertension ZA200609228B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US56517404P	2004-04-23	2004-04-23

Publications (1)

Publication Number	Publication Date
ZA200609228B true ZA200609228B (en)	2008-05-28

Family

ID=35196722

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
ZA200609228A ZA200609228B (en)	2004-04-23	2005-04-21	Methods of using and compositions comprising PDE4 modulators for the treatment and management of pulmonary hypertension

Country Status (12)

Country	Link
US (1)	US20050239867A1 (zh)
EP (1)	EP1755589A4 (zh)
JP (1)	JP2007533760A (zh)
KR (1)	KR20070007945A (zh)
CN (1)	CN1972684A (zh)
AU (1)	AU2005234783A1 (zh)
BR (1)	BRPI0510166A (zh)
CA (1)	CA2563377A1 (zh)
IL (1)	IL178788A0 (zh)
MX (1)	MXPA06012279A (zh)
WO (1)	WO2005102317A1 (zh)
ZA (1)	ZA200609228B (zh)

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2005
- 2005-04-21 ZA ZA200609228A patent/ZA200609228B/en unknown
- 2005-04-21 EP EP05749368A patent/EP1755589A4/en not_active Withdrawn
- 2005-04-21 US US11/111,187 patent/US20050239867A1/en not_active Abandoned
- 2005-04-21 CN CNA2005800211887A patent/CN1972684A/zh active Pending
- 2005-04-21 JP JP2007509624A patent/JP2007533760A/ja not_active Abandoned
- 2005-04-21 WO PCT/US2005/013597 patent/WO2005102317A1/en active Application Filing
- 2005-04-21 CA CA002563377A patent/CA2563377A1/en not_active Abandoned
- 2005-04-21 AU AU2005234783A patent/AU2005234783A1/en not_active Abandoned
- 2005-04-21 BR BRPI0510166-2A patent/BRPI0510166A/pt not_active IP Right Cessation
- 2005-04-21 MX MXPA06012279A patent/MXPA06012279A/es not_active Application Discontinuation
- 2005-04-21 KR KR1020067024520A patent/KR20070007945A/ko not_active Application Discontinuation
2006
- 2006-10-22 IL IL178788A patent/IL178788A0/en unknown

Also Published As

Publication number	Publication date
US20050239867A1 (en)	2005-10-27
CN1972684A (zh)	2007-05-30
AU2005234783A1 (en)	2005-11-03
KR20070007945A (ko)	2007-01-16
CA2563377A1 (en)	2005-11-03
BRPI0510166A (pt)	2007-10-02
MXPA06012279A (es)	2007-01-31
EP1755589A4 (en)	2007-11-07
EP1755589A1 (en)	2007-02-28
WO2005102317A1 (en)	2005-11-03
IL178788A0 (en)	2007-05-15
JP2007533760A (ja)	2007-11-22

Publication	Publication Date	Title
ZA200609228B (en)	2008-05-28	Methods of using and compositions comprising PDE4 modulators for the treatment and management of pulmonary hypertension
CA2641952C (en)	2011-02-01	Treatment of early stage idiopathic pulmonary fibrosis
US20050239842A1 (en)	2005-10-27	Methods of using and compositions comprising immunomodulatory compounds for the treatment and management of pulmonary hypertension
KR20070092276A (ko)	2007-09-12	Ｐｄｅ４ 조절인자를 포함하는 조성물 및 이의 기도염의치료 또는 예방을 위한 용도
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JP2007533759A (ja)	2007-11-22	肺高血圧症の治療及び管理のためのサリドマイドを含む組成物及びその使用方法
JPS6197228A (ja)	1986-05-15	ジヒドロピリジン類とａｃｅ阻害剤との配合物
WO2015175956A1 (en)	2015-11-19	Compositions and methods for the treatment of atherosclerotic cardiovascular diseases with pde4 modulators
EP1811992A2 (en)	2007-08-01	Methods and compositions using pde4 modulators for treatment and management of central nervous system injury
AU2003229724B2 (en)	2009-07-02	Novel use of guanylate cyclase activators for the treatment of respiratory insufficiency
BRPI0612582A2 (pt)	2010-11-23	combinação de compostos orgánicos
US20090131443A1 (en)	2009-05-21	Method for prevention and/or treatment of rheumatoid arthritis