US 2006/0135613 A1Published application

Carboxamides derivatives

AssigneeBayer HealthCare LLC

InventorsMakoto Shimazaki, Osamu Sakurai, Kanako Hirai, Klaus Urbahns, Noriyuki Yamamoto, Satoru Yoshikawa, Masaomi Umeda, Masaomi Tajimi

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Abstract

The present invention relates to carboxamides which are useful as an active ingredient of pharmaceutical preparations. The carboxamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the diseases are alleviated by treatment with an IP receptor antagonist.

Claims17

Dependent claims

A carboxamide derivative of the formula (I), its tautomeric or stereoisomeric form, or a salt thereof:

wherein
m and n independently represent an integer from 0 to 2;
—X— represents —CH2—CH2—, —CH═CH—, or —C≡C—;
R1 represents —OR11, —SR11, —SOR11, —SO2R11, —NR12R13, or —CHR14R15,
wherein
R11 represents (C2-6)alkenyl optionally substituted by aryl or heteroaryl, (C2-6)alkynyl optionally substituted by aryl or heteroaryl, or (C1-6) alkyl optionally substituted by aryl or heteroaryl;
R12 and R13 independently represent hydrogen, (C2-6)alkenyl optionally substituted by aryl or heteroaryl, (C2-6)alkynyl optionally substituted by aryl or heteroaryl, or (C1-6) alkyl optionally substituted by aryl or heteroaryl,
or
R12 and R13 together with the nitrogen atom to which they are attached, form a 5-7 membered saturated hetero ring optionally interrupted by O or NH;
R14 and R15 independently represent hydrogen, (C2-6)alkenyl optionally substituted by aryl or heteroaryl, (C2-6)alkynyl optionally substituted by aryl or heteroaryl, (C1-6) alkyl optionally substituted by aryl or heteroaryl, or (C1-6) alkoxy optionally substituted by aryl or heteroaryl,
or
R14 and R15 together with the CH to which they are attached, form a (C3-8)cycloalkyl optionally interrupted by NH, or O, or a phenyl optionally substituted by hydroxy, halogen or (C1-6) alkyl;
and
R2 represents hydrogen, cyano, (C1-6) alkoxy, (C2-6)alkenyl, (C2-6)alynyl, (C3-7)cycloalkyl, or (C1-6) alkyl optionally substituted by amino, (C1-6)alkylamino, or phenyl.

11 more elements

A carboxamide derivative of the formula (I′), its tautomeric or stereoisomeric form, or a salt thereof:

wherein
—X— represents —CH2—CH2—, —CH═CH—, or —C≡C—;
R1 represents —OR11, —SR11, —SOR11, —SO2R11, —NR12R13, or —CHR14R15,
wherein
R11 represents (C2-6)alkenyl optionally substituted by aryl or heteroaryl, (C2-6)alkynyl optionally substituted by aryl or heteroaryl, or (C1-6) alkyl optionally substituted by aryl or heteroaryl;
R12 and R13 independently represent hydrogen, (C2-6)alkenyl optionally substituted by aryl or heteroaryl, (C2-6)alkynyl optionally substituted by aryl or heteroaryl, or (C1-6) alkyl optionally substituted by aryl or heteroaryl,
or
R12 and R13 together with the nitrogen atom to which they are attached, form a 5-7 membered saturated hetero ring optionally interrupted by O or NH;
R14 and R15 independently represent hydrogen, (C2-6)alkenyl optionally substituted by aryl or heteroaryl, (C2-6)alkynyl optionally substituted by aryl or heteroaryl, (C1-6) alkyl optionally substituted by aryl or heteroaryl, or (C1-6) alkoxy optionally substituted by aryl or heteroaryl,
or
R14 and R15 together with the CH to which they are attached, form a (C3-8)cycloalklyl optionally interrupted by NH, or O, or a phenyl optionally substituted by hydroxy, halogen or (C1-6) alkyl;
and
R2 represents hydrogen, cyano, (C1-6) alkoxy, (C2-6)alkenyl, (C2-6)alkynyl, (C3-7)cycloalkyl, or (C1-6) alkyl optionally substituted by amino, (C1-6)alkylamino, or phenyl.

10 more elements

Dependencies are inferred from the claim text.

Facts

Application: 10/517,646Filed 12 Jun 2003
Priority: GB 0213598.613 Jun 2002
Published: 22 Jun 2006
Term ends: Not estimatedThe source records don’t support an estimate.

Classification14 codes

C07C 235/34
The carbon skeleton containing six-membered aromatic rings: having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to…
A61P 1/02
Drugs for disorders of the alimentary tract or the digestive system: stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
A61P 7/04
Drugs for disorders of the blood or the extracellular fluid: antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
A61P 9/00
Drugs for disorders of the cardiovascular system