KHK 7580 structure cracked

KHK 7580 .....example no 3.001  R¹-X- group\
 
HCl salt
MS · APCI: 361 [M+H] +

in EP1757582
4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1- yl)phenylacetic acid
4-​[(3S)​-​3-​[[(1R)​-​1-​(1-​naphthalenyl)​ethyl]​amino]​-​1-​pyrrolidinyl]​-Benzeneacetic acid,
cas will be updated
BASE ....870964-67-3
DI HCL SALT .......870856-31-8
MF C₂₄ H₂₆ N₂ O₂ BASE
MW 374.48 BASE
KHK-7580
KHK-7580; MT-4580
Mitsubishi Tanabe Pharma Corp... innovator
Kyowa Hakko Kirin Co Ltd.. licencee
4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid,
useful as calcium-sensitive receptor (CaSR) agonists for treating hyperparathyroidism.  a CaSR agonist, being developed by Kyowa Hakko Kirin, under license from Mitsubishi Tanabe, for treating secondary hyperparathyroidism (phase 2 clinical, as of March 2015).
WILL BE UPDATED
WO2005115975,/EP1757582
http://www.google.co.in/patents/EP1757582A1?cl=en
Example no 3.001  R¹-X- group
HCl salt
MS · APCI: 361 [M+H] +




WO 2015034031A1
http://worldwide.espacenet.com/publicationDetails/biblio?DB=worldwide.espacenet.com&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20150312&CC=WO&NR=2015034031A1&KC=A1
Mitsubishi Tanabe Pharma Corporation

The present invention provides a novel crystal form of an arylalkylamine
compound. Specifically, a novel crystal form of
4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1- yl)phenylacetic acid has
excellent stability, and is therefore useful as an active ingredient for
a medicine. The present invention also provides an industrially
advantageous method for producing an arylalkylamine compound.

WO 2015034031A1
http://worldwide.espacenet.com/publicationDetails/biblio?DB=worldwide.espacenet.com&II=0&ND=3&adjacent=true&locale=en_EP&FT=D&date=20150312&CC=WO&NR=2015034031A1&KC=A1
Mitsubishi Tanabe Pharma Corporation
The present invention provides a novel crystal form of an arylalkylamine compound. Specifically, a novel crystal form of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1- yl)phenylacetic acid has excellent stability, and is therefore useful as an active ingredient for a medicine. The present invention also provides an industrially advantageous method for producing an arylalkylamine compound.

see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
see all at   http://drugpatentsint.blogspot.in/2015/03/wo-2015034031.html
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 http://www.kyowa-kirin.com/research_and_development/pipeline/

KHK7580 -Secondary Hyperparathyroidism

JP

Company	Mitsubishi Tanabe Pharma Corp.
Description	Calcium receptor agonist
Molecular Target
Mechanism of Action	Calcium-sensing receptor (CaSR) agonist
Therapeutic Modality	Small molecule

Latest Stage of Development	Phase II
Standard Indication	Thyroid disease
Indication Details	Treat hyperparathyroidism in patients receiving hemodialysis; Treat secondary hyperparathyroidism (SHPT)
Regulatory Designation
Partner	Kyowa Hakko Kirin Co. Ltd.

August 29, 2014

Kyowa Hakko Kirin Announces Commencement of Phase 2b Clinical Study of KHK7580 in Patients with Secondary Hyperparathyroidism in Japan

Tokyo, Japan, August 29, 2014 --- Kyowa Hakko Kirin Co., Ltd. (Tokyo: 4151, President and CEO: Nobuo Hanai, "Kyowa Hakko Kirin") today announced the initiation of a phase 2b clinical study evaluating KHK7580 for secondary hyperparathyroidism patients receiving hemodialysis in Japan.
This randomized, placebo-controlled, double-blind, parallel-group, multi-center study is designed to evaluate efficacy and safety in cohorts comprising KHK7580, its placebo and cinacalcet and initial dose of KHK7580 for secondary hyperparathyroidism patients receiving hemodialysis.
KHK7580 is a small molecular compound produced by Mitsubishi Tanabe Pharma Corporation (President & Representative Director, CEO: Masayuki Mitsuka, "Mitsubishi Tanabe Pharma"). Kyowa Hakko Kirin signed a license agreement of KHK7580 with Mitsubishi Tanabe Pharma for the rights to cooperative research, develop, market and manufacture the product in Japan and some part of Asia on March 2008.
The Kyowa Hakko Kirin Group is contributing to the health and prosperity of the world's people by pursuing advances in life sciences and technology and creating new value.
Outline of this study

ClinicalTrials.gov Identifier	NCT02216656
Target Population	Secondary hyperparathyroidism patients receiving hemodialysis
Trial Design	Randomized, placebo-controlled, double-blind (included open arm of cinacalcet), parallel-group, multi-center study
Administration Group	KHK7580, Placebo, cinacalcet
Target Number of Subjects	150
Primary Objective	Efficacy
Trial Location	Japan
Trial Duration	Jul. 2014 to Jun. 2015

Contact:

Kyowa Hakko Kirin
Media Contact:
+81-3-3282-1903
or
Investors:
+81-3-3282-0009

Update on march 2016

New comment waiting approval on New Drug Approvals

M.F. Balandrin commented on KHK 7580 structure cracked KHK 7580 .....example 3.008 2HCl MS · APCI: 375[M + H]+ in … The calcimimetic agent, KHK-7580, currently entering Phase III clinical trials, has now been given the INN (WHO) generic name, evocalcet. Its chemical structure has also now been published and it is, in fact, correct as proposed by Dr. Crasto (Well Done!!): http://www.drugspider.com/drug/evocalcet https://tripod.nih.gov/ginas/app/substance/f580b9fd http://www.medkoo.com/products/6729 (Etymologically, in classical Latin, "evolutio" refers to "the unrolling of a scroll" and "evocare" refers to a "call out"...).

http://www.medkoo.com/products/6729

Name: Evocalcet
CAS#: 870964-67-3
Chemical Formula: C24H26N2O2
Exact Mass: 374.19943
Evocalcet is a calcium-sensing receptor agonist. The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion. The calcium-sensing receptor controls calcium homeostasis by regulating the release of parathyroid hormone (PTH). CaSR is expressed in all of the organs of the digestive system. CaSR plays a key role in gastrointestinal physiological function and in the occurrence of digestive disease. High dietary Ca2+ may stimulate CaSR activation and could both inhibit tumor development and increase the chemotherapeutic sensitivity of cancer cells in colon cancer tissues. (Last update: 12/15/2015).
Synonym: MT-4580; MT 4580; MT4580; KHK-7580; KHK7580; KHK 7580; Evocalcet
IUPAC/Chemical Name: 2-(4-((S)-3-(((R)-1-(naphthalen-1-yl)ethyl)amino)pyrrolidin-1-yl)phenyl)acetic acid

2
https://tripod.nih.gov/ginas/app/substance/f580b9fd

http://www.drugspider.com/drug/evocalcet

INN name	Evocalcet
Lab Code(s)	MT-4580 KHK-7580
Chemical name	{4-[(3S)-3-{[(1R)-1-(Naphthalen-1-yl)ethyl]amino}pyrrolidin-1-yl]phenyl}acetic acid
Chemical structure
Molecular formula	C24H26N2O2
SMILES	O=C(O)CC1=CC=C(N2C[C@@H](N[C@@H](C3=C4C=CC=CC4=CC=C3)C)CC2)C=C1
CAS registry number	870964-67-3
Orphan Drug Status	No
On Fast track	No
New Molecular Entity	Yes
Originator	Mitsubishi Tanabe Pharma Corporation
Developer(s)	Kyowa Hakko Kirin
Class	Antithyroids
Mechanism of action	Calcium-sensing receptor agonists
WHO ATC code(s)	H05 (Calcium Homeostasis)
EPhMRA code(s)	H3 (Thyroid Therapy)
Clinical trial(s)	Conditions Interventions Phases Recruitment Sponsor/Collaborators Conditions Interventions Phases Recruitment Sponsor/Collaborators Secondary Hyperparathyroidism Drug: KHK7580 Phase 3 Recruiting Kyowa Hakko Kirin Company, Limited Secondary Hyperparathyroidism Drug: KHK7580 Phase 3 Recruiting Kyowa Hakko Kirin Company, Limited Secondary Hyperparathyroidism Drug: KHK7580|Drug: KRN1493 Phase 2|Phase 3 Recruiting Kyowa Hakko Kirin Company, Limited Secondary Hyperparathyroidism Drug: Placebo|Drug: KHK7580 low dose|Drug: KHK7580 middle dose|Drug: KHK7580 high dose|Drug: KRN1493 Phase 2 Completed Kyowa Hakko Kirin Company, Limited Hyperparathyroidism Drug: KHK7580 Phase 1|Phase 2 Completed Kyowa Hakko Kirin Company, Limited Secondary Hyperparathyroidism Drug: KHK7580 Phase 1 Completed Kyowa Hakko Kirin Company, Limited
Updated on	11 Oct 2015

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SMILES Code: O=C(O)CC1=CC=C(N2C[C@@H](N[C@@H](C3=C4C=CC=CC4=CC=C3)C)CC2)C=C1