New di:peptide neurokinin antagonists - useful in treating respiratory disorders, inflammatory eye and skin disorders, polyarthritis, osteoarthritis and pain
Dipeptide derivs. of formula R1-C(O)-A1-A2-N(R2)(R3) (I) and their salts are new. R1 = vinyl; Ar1; Het1; Ar1-alkyl; Het1-alkyl; Ar1-vinyl; Het1-vinyl; Ar1-oxyalkyl; Ar1-alkoxy; di(Ar1-alkyl)-aminoalkyl or Ar1-alkylaminoalkyl; R2, R3 = alkyl; Ar2-alkyl; Het2; or OH; or NR2R3 forms a gp. of formula (a...
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| creator | JUNG, BIRGIT., 6530 BINGEN, DE BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE ESSER, FRANZ. DR., 6507 INGELHEIM, DE DOLLINGER, HORST. DR., 6507 INGELHEIM, DE |
| description | Dipeptide derivs. of formula R1-C(O)-A1-A2-N(R2)(R3) (I) and their salts are new. R1 = vinyl; Ar1; Het1; Ar1-alkyl; Het1-alkyl; Ar1-vinyl; Het1-vinyl; Ar1-oxyalkyl; Ar1-alkoxy; di(Ar1-alkyl)-aminoalkyl or Ar1-alkylaminoalkyl; R2, R3 = alkyl; Ar2-alkyl; Het2; or OH; or NR2R3 forms a gp. of formula (a) or (b): m, n = 0-3 (but m + n = 2-5); s = 2 or 3; X = -(CH2)0-2-Ar2; -CH(Ar2)2; cyclopentyl; -(CH2)0-2-cyclohexyl; pyridyl; N-methyl-N-phenylamino-carbonylmethyl; etc.; A1 = Ala, Val, Leu, Ile, Ser, Thr, alloThr, Cys, Met, Phe, Trp (opt. N-protected by CHO), Tyr, Pro, APro, Azt, Tpr, Pro(NH2), pGlu, Aib, 2,3-diaminopropionic acid, 2,4-diaminobutyric acid, Glu, Asp, Gln, Asn, Lys, Arg, His, Orn, hydroxypiperidinecarboxylic acid, Pro(SH), Tpr(O or O2) or Met(O or O2) in the D- or L-configuration or as a geometric isomer and OH and NH2 gps. are opt. protected; A2 = (i) a lipophilic amino acid contg. an Ar3, heteroaryl, cyclopentyl, cyclohexyl or mono- or di-(1-3C alkyl)amino gp. sepd. from the amino acid backbone by a 1-8 membered chain of the formula -(CHR4)1-8-, -(CHR4)0-p-G1(CHR4)0-q- or -(CHR4)1-p-G2(CHR4)0-q-; G1 = -COO- or CONR4-; G2 = -O-; -S-; -NR4-COO-; -NR4-CO-; -NR4-CO-NR4-; or -O-CO-NR4-; R4 = alkyl; Ar1; or Ar1-alkyl; p, q = 1-6; provided that the chain is not -CH2- when R2 and R3 = alkyl or Ar2-alkyl and when NR2R3 = gp. (a); or (ii) Leu; Ile; Nle; Val; Met; or e.g. a gp. of formula (i)-(iii): x, y = 1 or 2; Ar1 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl or CN; or naphthyl; Ar2 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, alkylthio, OH, NO2 or CN or on adjacent C by -O-(CH2)1 or 2-O-; or naphthyl; Ar3 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, CN or 1-pyrrolidinyl; or naphthyl; Het1 = indolyl opt. 1-substd. by alkyl or benzyl; pyridyl; pyrrolyl; imidazolyl; or thienyl; Het2 = indolyl; pyridyl; pyrrolyl; imidazolyl; or thienyl. USE - Cpds. (I) are inhibitors of neurokinin (tachykinin), esp. substance P. They are useful in treating respiratory disorders (e.g. asthma, bronchitis, rhinitis and cough), inflammatory eye disorders (e.g. conjunctivitis), inflammatory skin disorders (e.g. dermatitis and urticaria), polyarthritis, osteoarthritis and pain. Dosage is 1-55 mg for patient weighing 67 kg. |
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| fullrecord | <record><control><sourceid>epo_EVB</sourceid><recordid>TN_cdi_epo_espacenet_DE4243496A1</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>DE4243496A1</sourcerecordid><originalsourceid>FETCH-epo_espacenet_DE4243496A13</originalsourceid><addsrcrecordid>eNqNjbEKwlAMRbs4iPoP-QA7aIugm2jFycm9BJvWYPveI0mRfoz_6kNFHJ3CvZx7Mk4eJ7pDxZtAwbgicNSLv7FjB-gMG-9YTSGFXqnuW4i9CaGxa0BIAwualyEq1EtFovOI1C123bungaKoAo3OXyj4dkCxq7BxjF6N_De_FgHZTZNRja3S7HMnCRyK8-6YUvBl_I4XcmTlvsiXeZavV9tF9gfyBDXeVPQ</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>patent</recordtype></control><display><type>patent</type><title>New di:peptide neurokinin antagonists - useful in treating respiratory disorders, inflammatory eye and skin disorders, polyarthritis, osteoarthritis and pain</title><source>esp@cenet</source><creator>JUNG, BIRGIT., 6530 BINGEN, DE ; BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE ; SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE ; ESSER, FRANZ. DR., 6507 INGELHEIM, DE ; DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</creator><creatorcontrib>JUNG, BIRGIT., 6530 BINGEN, DE ; BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE ; SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE ; ESSER, FRANZ. DR., 6507 INGELHEIM, DE ; DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</creatorcontrib><description>Dipeptide derivs. of formula R1-C(O)-A1-A2-N(R2)(R3) (I) and their salts are new. R1 = vinyl; Ar1; Het1; Ar1-alkyl; Het1-alkyl; Ar1-vinyl; Het1-vinyl; Ar1-oxyalkyl; Ar1-alkoxy; di(Ar1-alkyl)-aminoalkyl or Ar1-alkylaminoalkyl; R2, R3 = alkyl; Ar2-alkyl; Het2; or OH; or NR2R3 forms a gp. of formula (a) or (b): m, n = 0-3 (but m + n = 2-5); s = 2 or 3; X = -(CH2)0-2-Ar2; -CH(Ar2)2; cyclopentyl; -(CH2)0-2-cyclohexyl; pyridyl; N-methyl-N-phenylamino-carbonylmethyl; etc.; A1 = Ala, Val, Leu, Ile, Ser, Thr, alloThr, Cys, Met, Phe, Trp (opt. N-protected by CHO), Tyr, Pro, APro, Azt, Tpr, Pro(NH2), pGlu, Aib, 2,3-diaminopropionic acid, 2,4-diaminobutyric acid, Glu, Asp, Gln, Asn, Lys, Arg, His, Orn, hydroxypiperidinecarboxylic acid, Pro(SH), Tpr(O or O2) or Met(O or O2) in the D- or L-configuration or as a geometric isomer and OH and NH2 gps. are opt. protected; A2 = (i) a lipophilic amino acid contg. an Ar3, heteroaryl, cyclopentyl, cyclohexyl or mono- or di-(1-3C alkyl)amino gp. sepd. from the amino acid backbone by a 1-8 membered chain of the formula -(CHR4)1-8-, -(CHR4)0-p-G1(CHR4)0-q- or -(CHR4)1-p-G2(CHR4)0-q-; G1 = -COO- or CONR4-; G2 = -O-; -S-; -NR4-COO-; -NR4-CO-; -NR4-CO-NR4-; or -O-CO-NR4-; R4 = alkyl; Ar1; or Ar1-alkyl; p, q = 1-6; provided that the chain is not -CH2- when R2 and R3 = alkyl or Ar2-alkyl and when NR2R3 = gp. (a); or (ii) Leu; Ile; Nle; Val; Met; or e.g. a gp. of formula (i)-(iii): x, y = 1 or 2; Ar1 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl or CN; or naphthyl; Ar2 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, alkylthio, OH, NO2 or CN or on adjacent C by -O-(CH2)1 or 2-O-; or naphthyl; Ar3 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, CN or 1-pyrrolidinyl; or naphthyl; Het1 = indolyl opt. 1-substd. by alkyl or benzyl; pyridyl; pyrrolyl; imidazolyl; or thienyl; Het2 = indolyl; pyridyl; pyrrolyl; imidazolyl; or thienyl. USE - Cpds. (I) are inhibitors of neurokinin (tachykinin), esp. substance P. They are useful in treating respiratory disorders (e.g. asthma, bronchitis, rhinitis and cough), inflammatory eye disorders (e.g. conjunctivitis), inflammatory skin disorders (e.g. dermatitis and urticaria), polyarthritis, osteoarthritis and pain. Dosage is 1-55 mg for patient weighing 67 kg.</description><edition>5</edition><language>eng ; ger</language><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS ; CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PEPTIDES ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><creationdate>1994</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19940310&DB=EPODOC&CC=DE&NR=4243496A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,780,885,25563,76418</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&date=19940310&DB=EPODOC&CC=DE&NR=4243496A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>JUNG, BIRGIT., 6530 BINGEN, DE</creatorcontrib><creatorcontrib>BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE</creatorcontrib><creatorcontrib>SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE</creatorcontrib><creatorcontrib>ESSER, FRANZ. DR., 6507 INGELHEIM, DE</creatorcontrib><creatorcontrib>DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</creatorcontrib><title>New di:peptide neurokinin antagonists - useful in treating respiratory disorders, inflammatory eye and skin disorders, polyarthritis, osteoarthritis and pain</title><description>Dipeptide derivs. of formula R1-C(O)-A1-A2-N(R2)(R3) (I) and their salts are new. R1 = vinyl; Ar1; Het1; Ar1-alkyl; Het1-alkyl; Ar1-vinyl; Het1-vinyl; Ar1-oxyalkyl; Ar1-alkoxy; di(Ar1-alkyl)-aminoalkyl or Ar1-alkylaminoalkyl; R2, R3 = alkyl; Ar2-alkyl; Het2; or OH; or NR2R3 forms a gp. of formula (a) or (b): m, n = 0-3 (but m + n = 2-5); s = 2 or 3; X = -(CH2)0-2-Ar2; -CH(Ar2)2; cyclopentyl; -(CH2)0-2-cyclohexyl; pyridyl; N-methyl-N-phenylamino-carbonylmethyl; etc.; A1 = Ala, Val, Leu, Ile, Ser, Thr, alloThr, Cys, Met, Phe, Trp (opt. N-protected by CHO), Tyr, Pro, APro, Azt, Tpr, Pro(NH2), pGlu, Aib, 2,3-diaminopropionic acid, 2,4-diaminobutyric acid, Glu, Asp, Gln, Asn, Lys, Arg, His, Orn, hydroxypiperidinecarboxylic acid, Pro(SH), Tpr(O or O2) or Met(O or O2) in the D- or L-configuration or as a geometric isomer and OH and NH2 gps. are opt. protected; A2 = (i) a lipophilic amino acid contg. an Ar3, heteroaryl, cyclopentyl, cyclohexyl or mono- or di-(1-3C alkyl)amino gp. sepd. from the amino acid backbone by a 1-8 membered chain of the formula -(CHR4)1-8-, -(CHR4)0-p-G1(CHR4)0-q- or -(CHR4)1-p-G2(CHR4)0-q-; G1 = -COO- or CONR4-; G2 = -O-; -S-; -NR4-COO-; -NR4-CO-; -NR4-CO-NR4-; or -O-CO-NR4-; R4 = alkyl; Ar1; or Ar1-alkyl; p, q = 1-6; provided that the chain is not -CH2- when R2 and R3 = alkyl or Ar2-alkyl and when NR2R3 = gp. (a); or (ii) Leu; Ile; Nle; Val; Met; or e.g. a gp. of formula (i)-(iii): x, y = 1 or 2; Ar1 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl or CN; or naphthyl; Ar2 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, alkylthio, OH, NO2 or CN or on adjacent C by -O-(CH2)1 or 2-O-; or naphthyl; Ar3 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, CN or 1-pyrrolidinyl; or naphthyl; Het1 = indolyl opt. 1-substd. by alkyl or benzyl; pyridyl; pyrrolyl; imidazolyl; or thienyl; Het2 = indolyl; pyridyl; pyrrolyl; imidazolyl; or thienyl. USE - Cpds. (I) are inhibitors of neurokinin (tachykinin), esp. substance P. They are useful in treating respiratory disorders (e.g. asthma, bronchitis, rhinitis and cough), inflammatory eye disorders (e.g. conjunctivitis), inflammatory skin disorders (e.g. dermatitis and urticaria), polyarthritis, osteoarthritis and pain. Dosage is 1-55 mg for patient weighing 67 kg.</description><subject>ACYCLIC OR CARBOCYCLIC COMPOUNDS</subject><subject>CHEMISTRY</subject><subject>HETEROCYCLIC COMPOUNDS</subject><subject>HUMAN NECESSITIES</subject><subject>HYGIENE</subject><subject>MEDICAL OR VETERINARY SCIENCE</subject><subject>METALLURGY</subject><subject>ORGANIC CHEMISTRY</subject><subject>PEPTIDES</subject><subject>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</subject><fulltext>true</fulltext><rsrctype>patent</rsrctype><creationdate>1994</creationdate><recordtype>patent</recordtype><sourceid>EVB</sourceid><recordid>eNqNjbEKwlAMRbs4iPoP-QA7aIugm2jFycm9BJvWYPveI0mRfoz_6kNFHJ3CvZx7Mk4eJ7pDxZtAwbgicNSLv7FjB-gMG-9YTSGFXqnuW4i9CaGxa0BIAwualyEq1EtFovOI1C123bungaKoAo3OXyj4dkCxq7BxjF6N_De_FgHZTZNRja3S7HMnCRyK8-6YUvBl_I4XcmTlvsiXeZavV9tF9gfyBDXeVPQ</recordid><startdate>19940310</startdate><enddate>19940310</enddate><creator>JUNG, BIRGIT., 6530 BINGEN, DE</creator><creator>BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE</creator><creator>SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE</creator><creator>ESSER, FRANZ. DR., 6507 INGELHEIM, DE</creator><creator>DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</creator><scope>EVB</scope></search><sort><creationdate>19940310</creationdate><title>New di:peptide neurokinin antagonists - useful in treating respiratory disorders, inflammatory eye and skin disorders, polyarthritis, osteoarthritis and pain</title><author>JUNG, BIRGIT., 6530 BINGEN, DE ; BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE ; SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE ; ESSER, FRANZ. DR., 6507 INGELHEIM, DE ; DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-epo_espacenet_DE4243496A13</frbrgroupid><rsrctype>patents</rsrctype><prefilter>patents</prefilter><language>eng ; ger</language><creationdate>1994</creationdate><topic>ACYCLIC OR CARBOCYCLIC COMPOUNDS</topic><topic>CHEMISTRY</topic><topic>HETEROCYCLIC COMPOUNDS</topic><topic>HUMAN NECESSITIES</topic><topic>HYGIENE</topic><topic>MEDICAL OR VETERINARY SCIENCE</topic><topic>METALLURGY</topic><topic>ORGANIC CHEMISTRY</topic><topic>PEPTIDES</topic><topic>PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES</topic><toplevel>online_resources</toplevel><creatorcontrib>JUNG, BIRGIT., 6530 BINGEN, DE</creatorcontrib><creatorcontrib>BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE</creatorcontrib><creatorcontrib>SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE</creatorcontrib><creatorcontrib>ESSER, FRANZ. DR., 6507 INGELHEIM, DE</creatorcontrib><creatorcontrib>DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</creatorcontrib><collection>esp@cenet</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>JUNG, BIRGIT., 6530 BINGEN, DE</au><au>BUERGER, ERICH-BIOL. DR., 6530 BINGEN, DE</au><au>SCHNORRENBERG, GERD. DR., 6535 GAU-ALGESHEIM, DE</au><au>ESSER, FRANZ. DR., 6507 INGELHEIM, DE</au><au>DOLLINGER, HORST. DR., 6507 INGELHEIM, DE</au><format>patent</format><genre>patent</genre><ristype>GEN</ristype><title>New di:peptide neurokinin antagonists - useful in treating respiratory disorders, inflammatory eye and skin disorders, polyarthritis, osteoarthritis and pain</title><date>1994-03-10</date><risdate>1994</risdate><abstract>Dipeptide derivs. of formula R1-C(O)-A1-A2-N(R2)(R3) (I) and their salts are new. R1 = vinyl; Ar1; Het1; Ar1-alkyl; Het1-alkyl; Ar1-vinyl; Het1-vinyl; Ar1-oxyalkyl; Ar1-alkoxy; di(Ar1-alkyl)-aminoalkyl or Ar1-alkylaminoalkyl; R2, R3 = alkyl; Ar2-alkyl; Het2; or OH; or NR2R3 forms a gp. of formula (a) or (b): m, n = 0-3 (but m + n = 2-5); s = 2 or 3; X = -(CH2)0-2-Ar2; -CH(Ar2)2; cyclopentyl; -(CH2)0-2-cyclohexyl; pyridyl; N-methyl-N-phenylamino-carbonylmethyl; etc.; A1 = Ala, Val, Leu, Ile, Ser, Thr, alloThr, Cys, Met, Phe, Trp (opt. N-protected by CHO), Tyr, Pro, APro, Azt, Tpr, Pro(NH2), pGlu, Aib, 2,3-diaminopropionic acid, 2,4-diaminobutyric acid, Glu, Asp, Gln, Asn, Lys, Arg, His, Orn, hydroxypiperidinecarboxylic acid, Pro(SH), Tpr(O or O2) or Met(O or O2) in the D- or L-configuration or as a geometric isomer and OH and NH2 gps. are opt. protected; A2 = (i) a lipophilic amino acid contg. an Ar3, heteroaryl, cyclopentyl, cyclohexyl or mono- or di-(1-3C alkyl)amino gp. sepd. from the amino acid backbone by a 1-8 membered chain of the formula -(CHR4)1-8-, -(CHR4)0-p-G1(CHR4)0-q- or -(CHR4)1-p-G2(CHR4)0-q-; G1 = -COO- or CONR4-; G2 = -O-; -S-; -NR4-COO-; -NR4-CO-; -NR4-CO-NR4-; or -O-CO-NR4-; R4 = alkyl; Ar1; or Ar1-alkyl; p, q = 1-6; provided that the chain is not -CH2- when R2 and R3 = alkyl or Ar2-alkyl and when NR2R3 = gp. (a); or (ii) Leu; Ile; Nle; Val; Met; or e.g. a gp. of formula (i)-(iii): x, y = 1 or 2; Ar1 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl or CN; or naphthyl; Ar2 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, alkylthio, OH, NO2 or CN or on adjacent C by -O-(CH2)1 or 2-O-; or naphthyl; Ar3 = phenyl opt. mono-, di- or tri-substd. by halo, trihalomethyl, alkoxy, alkyl, CN or 1-pyrrolidinyl; or naphthyl; Het1 = indolyl opt. 1-substd. by alkyl or benzyl; pyridyl; pyrrolyl; imidazolyl; or thienyl; Het2 = indolyl; pyridyl; pyrrolyl; imidazolyl; or thienyl. USE - Cpds. (I) are inhibitors of neurokinin (tachykinin), esp. substance P. They are useful in treating respiratory disorders (e.g. asthma, bronchitis, rhinitis and cough), inflammatory eye disorders (e.g. conjunctivitis), inflammatory skin disorders (e.g. dermatitis and urticaria), polyarthritis, osteoarthritis and pain. Dosage is 1-55 mg for patient weighing 67 kg.</abstract><edition>5</edition><oa>free_for_read</oa></addata></record> |
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| subjects | ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES |
| title | New di:peptide neurokinin antagonists - useful in treating respiratory disorders, inflammatory eye and skin disorders, polyarthritis, osteoarthritis and pain |
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